Feronia HP
1.0 Generic Name
Ferrous ascorbate, Folic Acid, Methylcobalamin and Zinc sulphate
2.0 Qualitative and Quantitative Composition
Each Film-coated tablet contains:
Ferrous ascorbate equivalent to Elemental iron 100mg
Folic Acid IP 1.5mg
Methylcobalamin IP 1.5 mg
Zinc sulphate monohydrate eq. 22.5 mg
to Elemental Zinc
Excipients q.s.
Colour: Red Oxide of Iron and Titanium Dioxide IP
3.0 Dosage Form and Strength
Film coated tablet
Ferrous Ascorbate 100 mg, Folic Acid 1.5 mg, Methylcobalamin 1.5 mg, Zinc Sulphate 22.5mg
4.0 Clinical particulars
4.1 Therapeutic indications
For the treatment of iron deficiency anemia.
4.2 Posology and method of administration
Adults
One tablet should be taken once daily by mouth.
Pediatric Population
There is no relevant use of Feronia HP Tablets in the pediatric population.
4.3 Contraindications
- Hypersensitivity to the active substances or any of the excipients.
- Paroxysmal nocturnal hemoglobinuria, hemosiderosis, haemochromatosis, active peptic ulcer, repeated blood transfusion, regional enteritis and ulcerative colitis.
- Feronia HP Tablets must not be used in the treatment of anemias other than those due to iron deficiency.
- Copper deficiency: Zinc may inhibit the absorption of Copper
4.4 Special warnings and precautions for use
CAUTION: Tablets are hygroscopic in nature. Exposure to humid conditions may soften the tablets affecting their appearance and shape. Cutting of strip should be avoided while dispensing/usage.
The label will state “Important warning: Contains Iron. Keep out of reach and sight of children, as overdose may be fatal”.
This will appear on the front of the pack within a rectangle in which there is no other information.
Some post-gastrectomy patients show poor absorption of iron. Care is needed when treating iron deficiency anemia in patients with treated or controlled peptic ulceration. Caution should be exercised when administering folic acid to patients who may have folate dependent tumors.
Since anemia due to combined iron and vitamin B12 or folate deficiencies may be microcytic in type, patients with microcytic anemia resistant to therapy with iron alone should be screened for vitamin B12 or folate deficiency.
Accumulation of zinc may occur in cases of renal failure.
Pregnancy
Safety is not established in pregnant women; therefore Feronia HP is not recommended in pregnancy.
Lactation
Safety is not established in lactating women; therefore Feronia HP is not recommended during lactation.
Pediatric population
Feronia HP Tablets should be kept out of the reach of children.
4.5 Interaction with other medicinal products and other forms of interaction
- Iron reduces the absorption of penicillamine. Iron compounds impair the bioavailability of fluoroquinolones, levodopa, carbidopa, thyroxine and bisphosphonates.
- Absorption of both iron and antibiotic may be reduced if Feronia HP is given with tetracycline.
- Concurrent administration of antacids may reduce absorption of iron. Co- trimoxazole, chloramphenicol, sulphasalazine, aminopterin, methotrexate, pyrimethamine or sulphonamides may interfere with folate metabolism. Serum levels of anticonvulsant drugs may be reduced by administration of folate.
- Oral chloramphenicol delays plasma iron clearance, incorporation of iron into red blood cells and interferes with erythropoiesis.
- Some inhibition of iron absorption may occur if it is taken with cholestyramine, trientine, tea, eggs or milk.
- Administration of oral iron may increase blood pressure in patients receiving methyldopa.
- Coffee may be a factor in reducing iron bioavailability. Neomycin may alter the absorption of iron.
- The absorption of zinc may be reduced by calcium supplements, tetracyclines and phosphorus-containing compounds, agents which increase gastric pH, such as H2 blockers, may decrease zinc absorption while zinc may reduce the absorption of penicillamine, tetracyclines, fluoroquinolones.
Food
Studies of the co-administration of zinc with food performed in healthy volunteers showed that the absorption of zinc was significantly delayed by many foods (including bread, hard boiled eggs, coffee and milk). Substances in food, especially phytates and fibres, bind zinc and prevent it from entering the intestinal cells. However, protein appears to interfere the least.
4.6 Fertility, pregnancy and lactation
Pregnancy
Safety is not established in pregnant women; therefore Feronia HP is not recommended in pregnancy. Breast-feeding Safety is not established in lactating women; therefore Feronia HP is not recommended during lactation. Fertility No fertility data is available.
4.7 Effects on ability to drive and use machines
Feronia HP Tablets has no influence on the ability to drive and use machines.
4.8 Undesirable effects
Very rare (<1/10,000)
Very rare (<1/10,000):
Rarely allergic reactions may occur.
Not known (cannot be estimated from the available data)
Not known: Gastrointestinal disorders Gastro-intestinal discomfort, anorexia, nausea, vomiting, constipation, diarrhea.
Not known: Renal and urinary disorders Darkening of the stools may occur. Blood amylase, lipase and alkaline phosphatase increased
Reporting of suspected adverse reactions
Reporting suspected adverse reactions after authorization of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via email to:medico@zuventus.com
Website: http://www.zuventus.co.in/safety.aspx
4.9 Overdose
Symptoms
Symptoms and signs of abdominal pain, vomiting and diarrhea appear within 60 minutes. Cardiovascular collapse with coma may follow. Some improvement may occur after this phase which, in some patients, is followed by recovery. In others, after about 16 hours, deterioration may occur involving diffuse vascular congestion, pulmonary edema, convulsions, anuria, hypothermia, severe shock, metabolic acidosis, coagulation abnormalities and hypoglycemia.
Management
Vomiting should be induced immediately, followed as soon as possible by parenteral injection of desferrioxamine mesylate, and then gastric lavage. In the meantime, it is helpful to give milk and/or 5% sodium bicarbonate solution by mouth.
Dissolve 2g desferrioxamine mesylate in 2 to 3ml of water for injections and give intramuscularly. A solution of 5g desferrioxamine in 50 to 100ml of fluid may be left in the stomach. If desferrioxamine is not available, leave 300ml of 1 % to 5 % sodium bicarbonate in the stomach. Fluid replacement is essential.
Recovery may be complicated by long-term sequelae such as hepatic necrosis, pyloric stenosis or acute toxic encephalitis which may lead to CNS damage.
Treatment of overdose should be with gastric lavage or induced emesis as quickly as possible to remove unabsorbed zinc. Heavy metal chelation therapy should be considered if plasma zinc levels are markedly elevated (> 10 mg/l).
Pediatric population
Acute overdose of oral iron requires emergency treatment. In young children 200-250mg/kg Ferrous Ascorbate is considered to be extremely dangerous.
5.0 Pharmacological properties
5.1 Mechanism of Action/ Pharmacodynamic properties
Iron absorption occurs predominantly in the duodenum and upper jejunum. Iron is oxidized to the Fe3+ state no matter its original form when taken in orally. Gastric acidity as well as solubilizing agents such as ascorbate prevent precipitation of the normally insoluble Fe3+. Intestinal mucosal cells in the duodenum and upper jejunum absorb the iron. The iron is coupled to transferrin (Tf) in the circulation which delivers it to the cells of the body. A feedback mechanism exists that enhances iron absorption in people who are iron deficient. In contrast, people with iron overload dampen iron absorption. A number of dietary factors influence iron absorption. Ascorbate increase iron uptake in part by acting as weak chelators to help to solubilize the metal in the duodenum. Iron is readily transferred from these compounds into the mucosal lining cells.
Zinc supplementation improves immunity.
Zinc deficiency also has direct effects on the gastrointestinal tract such as impaired intestinal brush border, increased secretion in response to bacterial enterotoxins and perturbations in intestinal permeability. Zinc supplementation improves the transport of water and electrolytes across the intestinal mucosa in experimental zinc deficiency.
Zinc plays a fundamental role in cellular metabolism and is postulated to modulate host resistance to various infections.
5.2 Pharmacokinetic properties
Absorption
Iron is absorbed chiefly in the duodenum and jejunum. Folic Acid is absorbed mainly from the proximal part of the small intestine.
Distribution
The amounts of Folic Acid absorbed from normal diets are rapidly distributed in body tissues.
Biotransformation
Absorption being aided by the acid secretion of the stomach and being more readily affected when the iron is in the ferrous state.
Folic acid rapidly appears in the blood, where it is extensively bound to plasma proteins.
When larger amounts are absorbed, a high proportion is metabolized in the liver to other active forms of folate and a proportion is stored as reduced and methylated folate.
Elimination
Larger amounts of folate are rapidly excreted in the urine and about 4 to 5 micrograms is excreted in the urine daily.
Zinc is absorbed in the small intestine and its absorption kinetics suggest a tendency to saturation at increasing doses. Fractional zinc absorption is negatively correlated with zinc intake. It ranges from 30 to 60% with usual dietary intake (7-15 mg/d) and decreases to 7% with pharmacological doses of 100 mg/d.
In the blood, about 80% of absorbed zinc is distributed to erythrocytes, with most of the remainder being bound to albumin and other plasma proteins. The liver is the main storage for zinc and hepatic zinc levels are increased during maintenance therapy with zinc. The plasma elimination half-life of zinc in healthy subjects is around 1 hour after a dose of 45 mg. The elimination of zinc results primarily from fecal excretion with relatively little from urine and sweat. The fecal excretion is in the greatest part due to the passage of unabsorbed zinc but it is also due to endogenous intestinal secretion.
6.0. Description
This Product (tablet) contains: Ferrous Ascorbate, Folic Acid, Methylcobalamin and Zinc sulphate as active ingredients, for the treatment of iron deficiency anemia.
Ferrous Ascorbate is an iron supplement used to treat or prevent low blood levels of iron (such as those caused by anemia or during pregnancy). Ascorbic acid (vitamin C) improves the absorption of iron from the stomach.
Molecular Formula- C12H14FeO12 Molecular Weight: 406.08g/mol

Folic acid is used to treat anemia caused by folate deficiency. Folic acid is also used as a supplement by women during pregnancy to reduce the risk of neural tube defects (NTDs) in the baby.
Molecular Formula-C19H19N7O6
Molecular Weight- 441.4 g/mol

Zinc is an essential trace element for humans, animals, plants and for microorganisms and is necessary for prenatal and postnatal development. Zinc is also an essential nutrient element for coral growth as it is an important cofactor for many enzymes.

Molecular Formula-ZnSO4
Molecular Weight- 179.47 g/mol
Methylcobalamin a form of vitamin B12.
Methylcobalamin is equivalent physiologically to vitamin B12, and can be used to prevent or treat pathology arising from a lack of vitamin B12 intake. Methylcobalamin is also used in the treatment of peripheral neuropathy, diabetic neuropathy, and as a preliminary treatment for amyotrophic lateral sclerosis.

Molecular formula: C63H91CoN13O14P
Molecular weight: 1344.405 g·mol−1
8.0 Pharmaceutical particulars
8.1 Incompatibilities
Not applicable.
8.2 Shelf-life
Refer on pack.
8.3 Packaging information
3 blister strips of 10 tablets each
8.4 Storage and handing instructions
Store at a temperature not exceeding 25°C. Protect from light.
Keep out of reach of children.
9.0 Patient Counselling Information
Patient Counselling Information
- WARNING: Accidental overdose of iron-containing products is a leading cause of fatal poisoning in children under 6. Keep this product out of reach of children. In case of accidental overdose, call a doctor immediately.
- Feronia HP Tablet is given to fulfil your nutritional requirement and to prevent any related diseases.
- Avoid taking antacids 2 hours before or after taking Feronia HP Tablet as they may make it harder for your body to absorb the medicine.
- Let your doctor know if you are taking any other medications like antihypertensive, antibiotics, or medicines for heart disease or bone disorders.
12.0 Date of revision
Sept 2024
Read this entire leaflet carefully before you start taking this medicine because it contains important information for you
- Keep this leaflet. You may need to read it again.
- If you have any further questions, ask your doctor or pharmacist.
- This medicine has been prescribed for you only. Do not pass it on to others. It may harm them, even if their signs of illness are the same as yours.
- If you get any side effects, talk to your doctor or pharmacist. This includes any possible side effects not listed in this leaflet.
1. What Feronia HP Tablets is and what it is used for?
Feronia HP film-coated Tablets (referred to as Feronia HP in this leaflet) contains Ferrous Ascorbate 100 mg, Folic Acid 1.5 mg, Methylcobalamin 1.5 mg, Zinc Sulphate 22.5mg. These work together in the medicine.
Feronia HP belongs to a group of medicines called haematinics and vitamin, mineral supplement.
Feronia HP works as a supplement. It provides the body with more iron and folic acid. These are important substances that your body needs to form red blood cells. If you do not have the right amount of these substances, it is possible that you may develop anemia.
Feronia HP is used to prevent and treat low levels of iron and folic acid in the blood (such as those caused by anemia or during pregnancy). Ascorbic acid (vitamin C) improves the absorption of iron from the stomach. Zinc supplementation improves immunity. Methylcobalamin is a form of Vitamin B12, important for the brain and nerves and for the production of red blood cells.
2. What you need to know before you take Feronia HP Tablets?
Do not take Feronia HP:
- if you are allergic to Ferrous Ascorbate and Folic Acid or any of the other ingredients of this medicine
- if you are breast-feeding or trying to become pregnant
- if you suffer from a blood disorder
- if you have had or are having repeated blood transfusions
- if you have a stomach ulcer or other digestive conditions such as regional enteritis or ulcerative colitis
- if you are suffering from anemia that is not due to a lack of iron
If any of the above applies to you, talk to your doctor or pharmacist.
Warnings and precautions
Talk to your doctor before taking Feronia HP
- if you have been or you are being treated for a stomach ulcer
- if you have had or you have a folate dependent tumour
- if you have had all or part of your stomach removed
Feronia HP contains iron. Keep out of reach and sight of children, as overdose may be fatal.
Children
There is no relevant use of Feronia HP in children.
Other medicines and Feronia HP
Tell your doctor if you are taking any other medicines.
- Antibiotics e.g. fluoroquinolones, cotrimoxazole, chloramphenicol, sulphonamides, tetracyclines, neomycin (used for infections)
- Anticonvulsant medicines (used for epilepsy)
- Antacids
- Penicillamine (used for rheumatoid arthritis)
- Sulfasalazine (used for rheumatoid arthritis and bowel disease, e.g. Crohn’s disease)
- Cholestyramine (used for reducing blood cholesterol or control diarrhea)
- Levodopa or Carbidopa (used for Parkinson’s disease)
- Thyroxine (used for thyroid disease)
- Bisphosphonates (used for bone disease)
- Aminopterin and Methotrexate (used for certain cancers)
- Pyrimethamine (used for malaria)
- Trientine (used for Wilson’s disease)
- Methyldopa (used for high blood pressure)
- Any other medicine, including medicines obtained without a prescription
Feronia HP with food and drink
If you drink tea, coffee or milk or eat eggs at the same time as taking Feronia HP, your body may absorb less of the iron and zinc supplement, which may reduce the effect of this medicine.
Pregnancy and breast-feeding
If you are pregnant or think you may be pregnant, ask your doctor for advice before taking this medicine.
Driving and using machines.
There are no known effects on driving or using machines.
3. How to take Feronia HP Tablets?
Always take Feronia HP Tablets exactly as your doctor has told you. You should check with your doctor or pharmacist if you are not sure.
The recommended dose for adults
- The usual dose is one tablet each day to be taken by mouth.
Method of administration: For oral administration only.
Swallow the tablet whole with a glass of water.
4. Possible side effects
Like all medicines, this medicine can cause side effects, although not everybody gets them.
Seek immediate medical help if you have an allergic reaction.
This includes any of the following symptoms:
- Difficulties in breathing
- Swelling of your eyelids, face or lips
- Rash or itching
Not known: frequency cannot be estimated from the available data
- Upset stomach
- Anorexia (e.g. loss of appetite)
- Sickness
- Constipation
- Diarrhea
- Darkening of stools
Reporting of side effects: If you experience any side effects, talk to your doctor or pharmacist. This includes any possible side effects not listed in this leaflet.You can also report side effects directly: Website: www.zuventus.com in and click the tab “Safety Reporting” located on the top end of the home page.
Website link: https://www.zuventus.co.in/drug-safety-reporting
5. How should I store Feronia HP Tablets?
- Keep this medicine out of the sight and reach of children. An overdose can be fatal.
- Do not use this medicine after the expiry date which is stated on the carton and blister after EXP. The expiry date refers to the last day of that month.
- Store below 25°C. Keep the blister in the outer carton in order to protect from light.
- Do not throw away any medicines via wastewater or household waste.
- Ask your pharmacist how to throw away medicines you no longer use. These measures will help protect the environment.
6. Contents of the pack and other information
- Ferrous Ascorbate 100 mg
- Folic Acid 1.5 mg
- Methylcobalamin 1.5 mg
- Zinc Sulphate 22.5mg
Pack size:
3 blister strips of 10 tablets each
Manufacturer:
Emcure Pharmaceuticals Ltd.
Lane no.3, phase II, SIDCO,
Bari-Brahamana, Jammu- 181133,
India
For More Information About This Product
Feronia D3 Tablets
1.0 Generic Name
Ferrous Ascorbate, Folic Acid, Cyanocobalamin, Pyridoxine Hydrochloride & Cholecalciferol Tablets
2.0 Qualitative and Quantitative Composition
Each film coated tablet contains:
Ferrous Ascorbate IP
equivalent to Elemental Iron 100 mg
Folic Acid IP 1.5 mg
Cyanocobalamin IP 7.5 mcg
(Vitamin B12)
Pyridoxine Hydrochloride IP 1.5 mg
(Vitamin B6)
Cholecalciferol IP 1000 IU (Vitamin D3) (As stabilized form) Excipients q.s. Colours: Lake of Sunset Yellow,
Lake of Erythrosine & Titanium Dioxide IP
3.0 Dosage Form and Strength
Film coated tablet
Ferrous ascorbate (100mg), Folic Acid (1.5mg), Cyanocobalamin (7.5 mcg), Pyridoxine Hydrochloride (1.5 mg), Cholecalciferol IP (1000 IU)
4.0 Clinical particulars
4.1 Therapeutic indications
Treatment and prevention of anemia with multivitamin deficiency
4.2 Posology and method of administration
Adults
One tablet to be taken daily orally
Pediatric Population
There is no relevant use of Feronia-D3 Tablets in the pediatric population.
4.3 Contraindications
- Hypersensitivity to the active substances or any of the excipients.
- Paroxysmal nocturnal hemoglobinuria, hemosiderosis, haemochromatosis, active peptic ulcer, repeated blood transfusion, regional enteritis and ulcerative colitis.
- Hypercalcaemia and/or hypercalciuria
- Nephrolithiasis (Renal calculi)
- Hypervitaminosis
- Severe renal impairment
4.4 Special warnings and precautions for use
- CAUTION: Tablets are hygroscopic in nature. Exposure to humid conditions may soften the tablets affecting their appearance and shape. Cutting of strip to be avoided while dispensing /usage.
- Important warning: Contains Iron. Keep out of reach and sight of children, as overdose may be fatal.
- Some post-gastrectomy patients show poor absorption of iron. Care is needed when treating iron deficiency anemia in patients with treated or controlled peptic ulceration. Caution should be exercised when administering folic acid to patients who may have folate dependent tumors.
- Since anemia due to combined iron and vitamin B12 or folate deficiencies may be microcytic in type, patients with microcytic anemia resistant to therapy with iron alone should be screened for vitamin B12 or folate deficiency.
- Cholecalciferol should be used with caution in patients with impairment of renal function and the effect on calcium and phosphate levels should be monitored. The risk of soft tissue calcification should be taken into account. In patients with severe renal insufficiency, vitamin D in the form of Cholecalciferol is not metabolised normally and other forms of vitamin D should be used. Cholecalciferol should not be taken by patients with a tendency to form calcium-containing renal calculi.
- Caution is required in patients receiving treatment for cardiovascular disease
Pediatric population
Feronia D3 Tablets should be kept out of the reach of children.
4.5 Interaction with other medicinal products and other forms of interaction
- Iron reduces the absorption of penicillamine. Iron compounds impair the bioavailability of fluoroquinolones, levodopa, carbidopa, thyroxine and bisphosphonates.
- Absorption of both iron and antibiotic may be reduced if Feronia D3 is given with tetracycline.
- Absorption of both iron and zinc are reduced if taken concomitantly. Concurrent administration of antacids may reduce absorption of iron. Co- trimoxazole, chloramphenicol, sulphasalazine, aminopterin, methotrexate, pyrimethamine or sulphonamides may interfere with folate metabolism. Serum levels of anticonvulsant drugs may be reduced by administration of folate.
- Oral chloramphenicol delays plasma iron clearance, incorporation of iron into red blood cells and interferes with erythropoiesis.
- Patients treated with cardiac glycosides may be susceptible to high calcium levels and should have ECG parameters and calcium levels monitored. It is recommended to reduce the dose or interrupt treatment if the calcium content in the urine exceeds 7.5 mmol/24 hours (300 mg/24 hours).
- Simultaneous administration of benzothiadiazine derivatives (thiazide diuretics) increases the risk of hypercalcaemia because they decrease the calcium excretion in the urine. The calcium levels in plasma and urine should therefore be monitored for patients undergoing long-term treatment.
- If Cholecalciferol is combined with metabolites or analogues of vitamin D careful monitoring of serum calcium levels is recommended.
- Some inhibition of iron absorption may occur if it is taken with cholestyramine, trientine, tea, eggs or milk.
- Administration of oral iron may increase blood pressure in patients receiving methyldopa.
- Coffee may be a factor in reducing iron bioavailability. Neomycin may alter the absorption of iron.
- Anti-convulsants e.g. phenytoin, phenobarbital, primidone may diminish the effect of Cholecalciferol due to hepatic enzyme induction.
- Rifampicin may reduce the effectiveness of Cholecalciferol due to hepatic enzyme induction.
- Isoniazid may reduce the effectiveness of Colecalciferol due to inhibition of the metabolic activation of Colecalciferol.
- Drugs leading to fat malabsorption, e.g. orlistat, liquid paraffin, cholestyramine, may impair the absorption of Cholecalciferol.
- The cytotoxic agent actinomycin and imidazole antifungal agents interfere with vitamin D activity.
- Concomitant use of glucocorticoids can decrease the effect of vitamin D.
4.6 Fertility, pregnancy and lactation
Pregnancy
The use of Feronia D3 Tablets may be considered during pregnancy, if necessary.
The development of anemia despite prophylaxis with Feronia D3 Tablets calls for investigation. During pregnancy women should follow the advice of their medical practitioner as their requirements may vary depending on the severity of their disease and their response to treatment.
Breast-feeding
It is unknown whether Ferrous Ascorbate and Folic Acid / metabolites are excreted in human milk.
A risk to the newborns/infants cannot be excluded.
Cholecalciferol and its metabolites are excreted in breast milk. Overdose in infants induced by nursing mothers has not been observed. However, when prescribing additional vitamin D to a breast-fed child the practitioner should consider the dose of any additional vitamin D given to the mother.
Fertility
No fertility data is available.
4.7 Effects on ability to drive and use machines
Feronia D3 Tablets has no influence on the ability to drive and use machines. Cholecalciferol has no known side effects that are likely to affect the ability to drive and use or operate machines.
4.8 Undesirable effects
Very rare (<1/10,000)
Very rare (<1/10,000): Rarely allergic reactions may occur. Not known (cannot be estimated from the available data) Not known: Gastrointestinal disorders Gastro-intestinal discomfort, anorexia, nausea, vomiting, constipation, diarrhea. Not known: Renal and urinary disorders Darkening of the stools may occur. Rarely Hypercalcemia, Hypercalciuria
Reporting of suspected adverse reactions
Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via email to:medico@zuventus.com
Website: Website: https://www.zuventus.com/drug-safety-reporting
By reporting side effects, you can help provide more information on the safety of this medicine.
4.9 Overdose
Symptoms
Symptoms and signs of abdominal pain, vomiting and diarrhea appear within 60 minutes. Cardiovascular collapse with coma may follow. Some improvement may occur after this phase which, in some patients, is followed by recovery. In others, after about 16 hours, deterioration may occur involving diffuse vascular congestion, pulmonary edema, convulsions, anuria, hypothermia, severe shock, metabolic acidosis, coagulation abnormalities and hypoglycemia.
Acute or chronic overdose of Cholecalciferol can cause hypercalcaemia, an increase in the serum and urinary concentrations of calcium. The symptoms of hypercalcaemia are not very specific and consist of nausea, vomiting, diarrhoea often in the early stages and later constipation, anorexia, fatigue, headache, muscle and joint pain, muscle weakness, polydipsia, polyuria formation of renal calculi, nephrocalcinosis, kidney failure, calcification of soft tissues, changes in ECG measurements, arrhythmias and pancreatitis. In rare and isolated cases there are reports that hypercalcaemia is fatal.
Management
Vomiting should be induced immediately, followed as soon as possible by parenteral injection of desferrioxamine mesylate, and then gastric lavage. In the meantime, it is helpful to give milk and/or 5% sodium bicarbonate solution by mouth.
Dissolve 2g desferrioxamine mesylate in 2 to 3ml of water for injections and give intramuscularly. A solution of 5g desferrioxamine in 50 to 100ml of fluid may be left in the stomach. If desferrioxamine is not available, leave 300ml of 1 % to 5 % sodium bicarbonate in the stomach. Fluid replacement is essential.
Recovery may be complicated by long-term sequelae such as hepatic necrosis, pyloric stenosis or acute toxic encephalitis which may lead to CNS damage.
A normalisation of hypercalcaemia due to vitamin D intoxication lasts several weeks. The recommendation for the treatment of hypercalcaemia is the avoidance of any further administration of vitamin D, including supplements, dietary intakes and the avoidance of sunlight. A low calcium or calcium-free diet can also be considered.
Rehydration and the treatment with diuretics e.g. furosemide to ensure adequate diuresis should be considered. Additional treatment with calcitonin or corticosteroids can also be considered.
Phosphate infusions should not be administered to lower hypercalcaemia of hypervitaminosis D because of the dangers of metastatic calcification.
Pediatric population
Acute overdose of oral iron requires emergency treatment. In young children 200-250mg/kg Ferrous Ascorbate is considered to be extremely dangerous.
5.0 Pharmacological properties
5.1 Mechanism of Action/ Pharmacodynamic properties
Iron absorption occurs predominantly in the duodenum and upper jejunum. Iron is oxidized to the Fe3+ state no matter its original form when taken in orally. Gastric acidity as well as solubilizing agents such as ascorbate prevent precipitation of the normally insoluble Fe3+. Intestinal mucosal cells in the duodenum and upper jejunum absorb the iron. The iron is coupled to transferrin (Tf) in the circulation which delivers it to the cells of the body. A feedback mechanism exists that enhances iron absorption in people who are iron deficient. In contrast, people with iron overload dampen iron absorption. A number of dietary factors influence iron absorption. Ascorbate increase iron uptake in part by acting as weak chelators to help to solubilize the metal in the duodenum. Iron is readily transferred from these compounds into the mucosal lining cells.
Cholecalciferol is produced within the skin under the influence of UV radiation including sunlight. In its biologically active form, Cholecalciferol stimulates intestinal calcium absorption, incorporation of calcium into the osteoid, and release of calcium from bone tissue. In the small intestine it promotes rapid and delayed calcium uptake. The passive and active transport of phosphate is also stimulated. In the kidney, it inhibits the excretion of calcium and phosphate by promoting tubular resorption. The production of parathyroid hormone (PTH) in the parathyroids is inhibited directly by the biologically active form of Cholecalciferol. PTH secretion is inhibited additionally by the increased calcium uptake in the small intestine under the influence of biologically active Cholecalciferol.
Elimination: Cholecalciferol and other forms of vitamin D are excreted in feces and urine.
- Iron participates in the second activation step of vitamin D, necessary to make this hormone functional.
- This conversion is done by a renal 25-hydroxyvitamin D 1α-hydroxylase (1α-OHase) enzyme which comprises a CYP-450, a ferredoxin, and a ferredoxin reductase.
- Therefore, less available iron could compromise production of the active form of vitamin D.
5.2 Pharmacokinetic properties
Folic Acid is absorbed mainly from the proximal part of the small intestine.
Distribution
The amounts of Folic Acid absorbed from normal diets are rapidly distributed in body tissues.
Biotransformation
Absorption being aided by the acid secretion of the stomach and being more readily affected when the iron is in the ferrous state.
Folic acid rapidly appears in the blood, where it is extensively bound to plasma proteins.
When larger amounts are absorbed, a high proportion is metabolized in the liver to other active forms of folate and a proportion is stored as reduced and methylated folate.
Elimination
Larger amounts of folate are rapidly excreted in the urine and about 4 to 5 micrograms is excreted in the urine daily.
The pharmacokinetics of Cholecalciferol have been widely studied and are well-known. Cholecalciferol from nutritional sources is almost completely absorbed from within the gastro-intestinal tract in the presence of dietary lipids and bile acids. Cholecalciferol is stored in fat cells and its biological half-life is approximately 50 days.
Cholecalciferol is metabolised by microsomal hydroxylase to form 25-hydroxycolecalciferol (25(OH)D3, calcidiol), the primary storage form of vitamin D3. 25(OH)D3 undergoes a secondary hydroxylation within the kidney to form the predominant active metabolite 1,25-hydroxycolecalciferol (1,25(OH)2D3, calcitriol). The metabolites circulate in the blood bound to a specific α -globin.
After a single oral dose of Cholecalciferol, the maximum serum concentrations of the primary storage form are reached after approximately 7 days. 25(OH)D3 is then slowly eliminated with an apparent half-life in serum of about 50 days. Cholecalciferol and its metabolites are excreted mainly in the bile and feces.
After high doses of Cholecalciferol, serum concentrations of 25(OH)D3 may be increased for months. Overdose-induced hypercalcemia may persist for weeks
6.0 Description
This Product (tablet) contains: Ferrous Ascorbate, Folic Acid Cyanocobalamin, Pyridoxine and Cholecalciferol as active ingredients, for the treatment and prevention of Anemia with multivitamin deficiency.
Ferrous Ascorbate is an iron supplement used to treat or prevent low blood levels of iron (such as those caused by anemia or during pregnancy). Ascorbic acid (vitamin C) improves the absorption of iron from the stomach.

Vitamin D promotes calcium absorption in the gut and maintains adequate serum calcium and phosphate concentrations to enable normal bone mineralization and to prevent hypocalcemic tetany.

Folic acid is used to treat anemia caused by folate deficiency. Folic acid is also used as a supplement by women during pregnancy to reduce the risk of neural tube defects (NTDs) in the baby.
Molecular Formula-C19H19N7O6
Molecular Weight- 441.4 g/mol

8.0 Pharmaceutical particulars
8.1 Incompatibilities
Not applicable.
8.2 Shelf-life
Refer on pack.
8.3 Packaging information
3 Blister strips of 10 tablets each
8.4 Storage and handing instructions
Store in a cool & dry place. Protect from moisture. Protect from light. Keep out of reach of children.
9.0 Patient Counselling Information
- WARNING: Accidental overdose of iron-containing products is a leading cause of fatal poisoning in children under 6. Keep this product out of reach of children. In case of accidental overdose, call a doctor immediately.
- Feronia -D3 Tablet is given to fulfill your nutritional requirement and to prevent any related diseases.
- Avoid taking antacids 2 hours before or after taking Feronia-D3 Tablet as they may make it harder for your body to absorb the medicine.
- Let your doctor know if you are taking any other medications like antihypertensive, antibiotics, or medicines for heart disease or bone disorders.
12.0 Date of revision
25th Sept 2024
Read this entire leaflet carefully before you start taking this medicine because it contains important information for you
- Keep this leaflet. You may need to read it again.
- If you have any further questions, ask your doctor or pharmacist.
- This medicine has been prescribed for you only. Do not pass it on to others. It may harm them, even if their signs of illness are the same as yours.
- If you get any side effects, talk to your doctor or pharmacist. This includes any possible side effects not listed in this leaflet.
1. What Feronia D3 Tablets is and what it is used for?
Feronia D3 film-coated Tablets (referred to as Feronia D3 in this leaflet) contains active substances Ferrous Ascorbate 100mg (an iron supplement) and Folic Acid 1.5mg, Cyanocobalamin (Vitamin B12) IP-7.5 mcg, Pyridoxine Hydrochloride (Vitamin B6) IP-1.5 mg, Cholecalciferol (Vitamin D3) IP-1000 IU. These work together in the medicine.
Feronia D3 belongs to a group of medicines called haematinics and multivitamins supplement.
Feronia D3 works as a supplement. It provides the body with more iron and folic acid, vitamin D3, B12, B6. These are important substances that your body needs to form red blood cells, bone mineralisation. If you do not have the right amount of these substances, it is possible that you may develop anemia, osteoporosis.
Feronia D3 is used to prevent and treat low levels of iron and folic acid, vitamin D, B12, B6 in the blood (such as those caused by anemia or during pregnancy). Ascorbic acid (vitamin C) improves the absorption of iron from the stomach.
2. What you need to know before you take Feronia D3 Tablets?
Do not take Feronia D3:
- if you are allergic to any of the other ingredients of this medicine
- if you are breast-feeding or trying to become pregnant
- if you have been told you suffer from Vitamin B12 deficiency
- if you suffer from a blood disorder
- if you have had or are having repeated blood transfusions
- if you have a stomach ulcer or other digestive conditions such as regional enteritis or ulcerative
colitis
- if you are suffering from anemia that is not due to a lack of iron
- If any of the above applies to you, talk to your doctor or pharmacist.
Warnings and precautions
Talk to your doctor before taking Feronia D3
- if you have been or you are being treated for a stomach ulcer
- if you have had or you have a folate dependent tumour
- if you have had all or part of your stomach removed
Feronia D3 contains iron. Keep out of reach and sight of children, as overdose may be fatal.
Children
There is no relevant use of Feronia D3 in children.
Other medicines and Feronia D3
Tell your doctor if you are taking any other medicines.
- Antibiotics e.g. fluoroquinolones, cotrimoxazole, chloramphenicol, sulphonamides, tetracyclines, neomycin (used for infections)
- Anticonvulsant medicines (used for epilepsy)
- Antacids
- Penicillamine (used for rheumatoid arthritis)
- Sulfasalazine (used for rheumatoid arthritis and bowel disease, e.g. Crohn’s disease)
- Cholestyramine (used for reducing blood cholesterol or control diarrhea)
- Levodopa or Carbidopa (used for Parkinson’s disease)
- Thyroxine (used for thyroid disease)
- Bisphosphonates (used for bone disease)
- Aminopterin and Methotrexate (used for certain cancers)
- Pyrimethamine (used for malaria)
- Trientine (used for Wilson’s disease)
- Methyldopa (used for high blood pressure)
- Zinc
- Any other medicine, including medicines obtained without a prescription
Feronia D3 with food and drink
If you drink tea, coffee or milk or eat eggs at the same time as taking Feronia D3 your body may absorb less of the iron supplement, which may reduce the effect of this medicine.
Pregnancy and breast-feeding
If you are pregnant or think you may be pregnant, ask your doctor for advice before taking this medicine.
Driving and using machines.
There are no known effects on driving or using machines.
3. How to take Feronia D3 Tablets?
Always take Feronia D3 Tablets exactly as your doctor has told you. You should check with your doctor or pharmacist if you are not sure.
The recommended dose for adults
- The usual dose is one tablet each day to be taken by mouth.
Method of administration: For oral administration only.
Swallow the tablet whole with a glass of water.
4. Possible side effects
Like all medicines, this medicine can cause side effects, although not everybody gets them.
Seek immediate medical help if you have an allergic reaction.
This includes any of the following symptoms:
- Difficulties in breathing
- Swelling of your eyelids, face or lips
- Rash or itching Not known: frequency cannot be estimated from the available data
- Upset stomach
- Anorexia (e.g. loss of appetite)
- Sickness
- Constipation
- Diarrhea
- Darkening of stools
Reporting of side effects: If you experience any side effects, talk to your doctor or pharmacist. This includes any possible side effects not listed in this leaflet.You can also report side effects directly: Website: www.zuventus.com in and click the tab “Safety Reporting” located on the top end of the home page.
Website link: https://www.zuventus.com/drug-safety-reporting
By reporting side effects, you can help provide more information on the safety of this product.
5. How should I store Feronia D3 Tablets?
- Keep this medicine out of the sight and reach of children. An overdose can be fatal.
- Do not use this medicine after the expiry date which is stated on the carton and blister after EXP. The expiry date refers to the last day of that month.
- Store below 25°C. Keep the blister in the outer carton in order to protect from light.
- Do not throw away any medicines via wastewater or household waste.
- Ask your pharmacist how to throw away medicines you no longer use. These measures will help protect the environment.
6. Contents of the pack and other information
- The active substances are Ferrous Ascorbate, Folic Acid, Cyanocobalamin, Pyridoxine and Cholecalciferol
- Each tablet contains Ferrous Ascorbate 100mg, Folic Acid 1.5mg, Cyanocobalamin IP-7.5 mcg, Pyridoxine Hydrochloride IP-1.5 mg, Cholecalciferol IP-1000 IU Pack size: 3 Blister strips of 10 tablets each
For More Information About This Product
Efnocar 40 Tablet
1.0 Generic Name
Efonidipine Hydrochloride Ethanolate Tablets 10 mg / 20 mg / 40 mg
2.0 Qualitative and quantitative composition
EFNOCAR-10
Each film coated tablet contains:
Efonidipine Hydrochloride Ethanolate 10 mg
Excipients q.s.
Colour: Titanium Dioxide IP
EFNOCAR-20
Each film coated tablet contains:
Efonidipine Hydrochloride Ethanolate 20 mg
Excipients q.s.
Colour: Titanium Dioxide IP
EFNOCAR-40
Each film coated tablet contains:
Efonidipine Hydrochloride Ethanolate 40 mg
Excipients q.s.
Colour: Titanium Dioxide IP
3.0 Dosage form and strength
Film coated tablet
10/ 20/40 mg
4.0 Clinical particulars
4.1 Therapeutic Indication
Efonidipine is indicated for the management of
- Essential hypertension and renal parenchymal hypertension
- Angina
4.2 Posology and method of administration
Adults
- Essential hypertension and renal parenchymal hypertension: 20-40 mg orally once daily. A dose of up to 80 mg/day has been reported to be safe and effective in clinical trials.
- Angina: 40 mg/day.
Elderly
Efonidipine should be started with a low dose (20mg/day) and the patient's condition should be monitored. The dose should be halved in case the patient is intolerant to the higher dose.
In Children
Efonidipine is not recommended in infants and children as safety is not established in this group of patients.
4.3 Contraindications
- In patients with known hypersensitivity to Efonidipine or any other component of the formulation
- In pregnant women
4.4 Special warnings and precautions for use
- Should be administered with caution in patients with hepatic impairment.
- Should be administered with caution in patients with low BP and/or sinus node dysfunction.
- The drug should be withdrawn gradually to prevent rebound hypertension or worsening of angina.
- Administration of the drug may cause hypotension. Under such circumstances appropriate measures should be taken to either reduce the dose or withdraw the drug.
- Should not be taken with grapefruit juice as there may be excessive lowering of blood pressure.
- Dizziness may occur while taking antihypertensive agents. Hence, working on aerial platform, working with dangerous machinery and/or driving should be avoided.
- To be sold by retail on the prescription of Cardiologist / Nephrologist / Endocrinologist and Specialist in General / Internal medicine / Critical Care medicine only.
4.5 Drugs interactions
Concomitant administration of other antihypertensive agent/s may enhance the antihypertensive effect of efonidipine.
- Administration of calcium channel blockers (CCBs) with Cimetidine may cause elevated levels of CCBs.
- Increased levels of CCBs observed when taken concomitantly with grapefruit juice which may result in excessive lowering of blood pressure.
- Efonidipine when taken along with Tacrolimus may cause increased blood levels of Tacrolimus.
4.6 Use in special populations
Pregnancy
Efonidipine should not be administered in pregnant women.
Nursing Mothers
Efonidipine should not be administered in lactating women.
4.7 Effects on ability to drive and use machines
If patients taking Efonidipine suffer from dizziness, headache, fatigue or nausea the ability to react may be impaired. Caution is recommended especially at the start of treatment.
4.8 Undesirable effects
The common side effects are hot flushes, palpitations, facial flushing and headache. In addition, elevation in serum total cholesterol, ALT (SGPT), AST (SGOT) and BUN may occur.
Tabulated list of adverse reactions


Reporting of suspected adverse reactions
Reporting of suspected adverse reactions
Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via email to:medico@zuventus.com
Website: https://www.zuventus.com/drug-safety-reporting
4.9 Overdose
In humans, experience with intentional overdose is limited. The stomach should be emptied by aspiration and gastric lavage if the patient reports immediately or up to two hours after overdosage.
Clinically significant hypotension due to Efonidipine overdosage calls for active cardiovascular support including frequent monitoring of cardiac and respiratory function, elevation of extremities, and attention to circulating fluid volume and urine output. A vasoconstrictor may be helpful in restoring vascular tone and blood pressure, provided that there is no contraindication to its use. Intravenous calcium gluconate may be beneficial in reversing the effects of calcium channel blockade.
5.0 Pharmacological properties
5.1 Mechanism of Action
Efonidipine, a new generation dihydropyridine (DHP) calcium channel blocker, inhibits both L-type and T-type calcium channels.
5.2 Pharmacodynamic properties
- Efonidipine exhibits antihypertensive effect through vasodilatation by blocking L-type and T-type calcium channels.
- Efonidipine has a negative chronotropic effect. Working on sino atrial node cells by inhibiting T-type calcium channel activation, Efonidipine prolongs the late phase-4 depolarization of the sino atrial node action potential and suppresses an elevated HR. The negative chronotropic effect of Efonidipine decreases heart rate, myocardial oxygen demand and increases coronary blood flow.
- Efonidipine increases coronary blood flow by blocking L & T-type calcium channels and attenuates myocardial ischaemia.
- By reducing synthesis and secretion of aldosterone, Efonidipine prevents hypertrophy and remodeling of cardiac myocytes.
- Efonidipine increases glomerular filtration rate without increasing intra-glomerular pressure and filtration fraction. This prevents hypertension induced renal damage.
- Efonidipine prevents Rho-kinase and NF-kB induced renal parenchymal fibrosis and provides long term renal protection.
- Efonidipine suppresses renin secretion from the Juxta Glomerular apparatus in the kidneys. •Efonidipine enhances sodium excretion from the kidneys by suppressing aldosterone synthesis and secretion from the adrenal glands. Aldosterone induced renal parenchymal fibrosis is suppressed by Efonidipine. •Efonidipine prevents NF-kB induced hypertrophy and inflammation in the renal vasculature and protects the kidneys.
- Efonidipine protects against endothelial dysfunction due to its anti-oxidant activity and by restoring nitric oxide bioavailability.
- Efonidipine has anti-atherogenic activity and protects the blood vessels from atherosclerosis.
- Efonidipine lowers blood pressure in cerebral resistance vessels and prevents hypertension induced brain damage.
5.3 Pharmacokinetic properties
Absorption
Peak plasma concentration is achieved in about 1.5 to 3.67 hours after administration. The bioavailability of Efonidipine is ~25% and half-life is approximately 4 hours.
Efonidipine 40mg when administered to healthy volunteers under fasting conditions shows the following pharmacokinetic profile:

The dissociation constant of Efonidipine from dihydropyridine receptors is very low (0.0042/min/nM), signifying very slow dissociation from the receptors. This explains the long duration of action of Efonidipine.
Metabolism
Efonidipine is primarily metabolized in the liver. The important metabolites are N-dephenylated Efonidipine (DPH), deaminated Efonidipine (AL) and N-debenzylated Efonidipine (DBZ). DBZ and DPH exhibit activity as calcium antagonists. The vasodilating properties of DBZ and DPH were about two-thirds and one-third respectively than that of the parent compound. Results suggest that the majority of the pharmacological effect after oral dosing of Efonidipine hydrochloride in man is due to unchanged compound and its metabolites make a small contribution to the pharmacological effect.
Elimination
Biliary route is the main pathway of excretion. No significant amount of unchanged drug is excreted in urine. In the urine collected for 24 h after an oral dosing, 1.1% of the dose was excreted as deaminated Efonidipine, and 0.5% as a pyridine analogue of deaminated Efonidipine.
6.0 Nonclinical properties
6.1 Animal Toxicology or Pharmacology
The acute toxicology of efonidipine was studied in male and female mice, rats, and dogs following oral or intravenous administration. The intravenous LD, values in male mice and rats were 77 and 51 mg/kg, respectively. The oral LD, values for efonidipine in mice, rats, and dogs were higher than 1,500 mag. The signs of toxicity observed in mice and rats were depression of spontaneous movement, hypothermia, sedation, piloerection, lying, gasping, and clonic convulsion. The dogs developed mild diarrhea, soft stools, or a temporary decrease in food consumption.
A 13-week oral subacute toxicity study of efonidipine was performed in male or female rats and dogs. Increases in water consumption and urine volume were observed in male and female rats receiving efonidipine at 300 mg/kg/day. Urinalysis revealed a high concentration of Na+ and C1- in the rats receiving 100 or 300 mg/kg/day. Organ weight measurement revealed an increase in liver and heart weight in male animals receiving 10 mg/kg/day or more and in female animals receiving 30 mg/kg/day or more.
Thus, in this study, the noneffective dose level was 3 mg/kg/day in rats. The effects observed at 300 or 100 mg/kg/day in groups of male or female dogs included reversible hyperemia of the sclera. Pathological examination revealed a dose-induced increase in the absolute and relative heart weight in female dogs treated with the drug at 100 mg/kg/day or more. Thus, the maximum noneffective dose of efonidipine in dogs of either sex was estimated to be around 30 mg/kg/day.
An oral chronic toxicity study of efonidipine was carried out in rats and dogs. Efonidipine was administered to rats at a daily dose of 1.5, 7, or 30 mg/kg for one year.
Organ weight measurement revealed an increase or a tendency of increase in heart weight in male or female rats receiving 30 mg/kg/day. A decreased thyroid weight in the males and an elevated liver weight in the females were found in the 30 mg/kg/day group.
Therefore, the noneffective estimated oral dose of efonidipine in rats was 7 mg/kg/day. Efonidipine in a gelatin capsule containing 2.0, 6.5, or 20 mg/kg/day was administered to dogs once daily for one year. The estimated effective dose was ca 20 mg/kg/day and the noneffective dose was ca 6.5 mg/kg/day
7.0 Description
Efonidipine is a novel dihydropyridine calcium channel blocker having anti-hypertensive and anti-anginal properties.
Chemical name: (±) -2 - [benzyl (phenyl) amino] ethyl 1, 4-dihydro-2 ,6-dimethyl- 5-(5,5-dimethyl-2-oxo-1 ,3,2-dioxaphosphorinan-2-yl) -4 - (3-nitrophenyl) -3-pyridinecarboxylate hydrochloride ethanol.
Molecular formula: C34H38 N3O7P • HCl •C2H6O
Molecular mass: 714.18 g/mol

8.0 Pharmaceutical particulars
8.1 Incompatibilities
Not applicable.
8.2 Shelf-life
Refer on pack
8.3 Packaging information
10 Blister strips of 10 tablets each
8.4 Storage and handing instructions
- Store below 25°C. Protected from light & moisture.
- Keep out of reach of children.
9.0 Patient Counselling Information
Efnocar is a type of medicine known as a calcium channel blocker (CCB). It is used to treat high blood pressure (hypertension) and a type of chest pain called angina. It can be used by itself or with other medicines to treat these conditions. Do not use Efnocar if you are allergic to efonidipine (the active ingredient in Efnocar), or to the inactive ingredients.
Tell your doctor about any prescription and non-prescription medicines you are taking, including natural or herbal remedies. Tell your doctor if you:
- ever had heart disease
- ever had liver problems
- are pregnant, or plan to become pregnant.
- are breast-feeding. Do not breast-feed while taking Efnocar.
You can stop breast-feeding or take a different medicine.
It may be easier to take your dose if you do it at the same time every day, such as with breakfast or dinner, or at bedtime.
While you are taking Efnocar do not stop taking your other prescription medicines, including any other blood pressure medicines, without talking to your doctor.
12.0 Date of revision
09/10/2024
About Leaflet
The name of your medicine is EFNOCAR 10 mg / 20 mg / 40 mg Tablets. We refer to them as EFNOCAR Tablets or EFNOCAR throughout this leaflet
Read all of this leaflet carefully before you start taking this medicine because it contains important information for you.
Keep this leaflet. You may need to read it again.
If you have any more questions, please ask your doctor or your pharmacist.
This medicine has been prescribed for you personally and you should not pass it on to anyone else. It may harm them, even if their symptoms are the same as yours.
If any of the side effects get serious, or if you notice any side effects that are not listed in the leaflet, please tell your doctor or pharmacist.
In this leaflet:
1. What EFNOCAR Tablets are and what they are used for
2. What you need to know before you take EFNOCAR Tablets
3. How to take EFNOCAR Tablets
4. Possible side effects
5. How to store EFNOCAR Tablets
6. Contents of the pack and other information
1. What Efnocar Tablets Are and What They Are Used for
EFNOCAR Tablets contain the active substance efonidipine which belongs to a group of medicines called calcium antagonists.
EFNOCAR Tablets may be used to treat:
- High blood pressure (hypertension)
- hypertension caused by kidney disease
- A certain type of chest pain called angina
In patients with high blood pressure, these medicines work by relaxing blood vessels, so that blood passes through them more easily. In patients with angina, EFNOCAR works by improving blood supply to the heart muscle which then receives more oxygen and as a result chest pain is prevented. EFNOCAR Tablets do not immediately relieve chest pain caused by angina.
2. What You Need to Know Before You Take Efnocar Tablets
Do not take EFNOCAR Tablets if you:
- Have ever had an allergic reaction to efonidipine or any of the ingredients in the tablet. An allergic reaction may include a rash, itching, difficulty breathing or swelling of the face, lips, throat or tongue;
- If you are pregnant
Take special care with EFNOCAR Tablets
You should inform you doctor if you have or have had any of the following conditions:
Liver disease;
Recent heart attack;
Heart failure;
Severe increase in blood pressure (Hypertensive crisis).
Use in children and adolescents
EFNOCAR is not recommended in infants and children as safety is not established in this group of patients.
For more information, talk to your doctor.
Taking other medicines and EFNOCAR
Please tell your doctor or pharmacist if you are taking or have recently taken other medicines, including medicines obtained without a prescription.
EFNOCAR may affect or be affected by other medicines, such as:
- Other antihypertensive agent/s (BP lowering drugs)
- Cimetidine (stomach acid reducer)
- Tacrolimus (a drug to suppress immunity)
EFNOCAR may lower your blood pressure even more if you are already taking other medicines to treat your high blood pressure.
If you see another doctor or go into hospital for any reason, tell them that you are taking EFNOCAR Tablets.
Taking EFNOCAR Tablets with food and drink
You should not drink grapefruit juice or eat grapefruit while taking this medicine. Grapefruit and grapefruit juice can lead to an increase in the blood levels of efonidipine, which can cause an unpredictable increase in its blood pressure lowering effect.
Pregnancy
The safety of efonidipine in human pregnancy has not been established. Efonidipine should not be administered in pregnant women.
Breast-feeding
It is not known whether efonidipine is passed into breast milk. Efonidipine should not be administered in breast-feeding women.
Ask your doctor or pharmacist for advice before taking any medicine.
Driving and using machines
Dizziness may occur while taking antihypertensive agents. Hence, working on aerial platform, working with dangerous machinery and/or driving should be avoided.
3. How to Take Efnocar Tablets
Swallow these tablets with a glass of water at the same time each day. You can take the tablets after meals.
Follow your doctor’s instructions. Check the pharmacy label to see how many tablets to take and how often to take them. If you are still not sure, ask your pharmacist or doctor. The usual doses are described below.
Adults
Essential hypertension and renal parenchymal hypertension: 20-40 mg orally once daily. A dose of up to 80 mg/day has been reported to be safe and effective in clinical trials.
Angina: 40 mg/day.
Children
EFNOCAR is not recommended in infants and children as safety is not established in this group of patients.
Elderly
EFNOCAR should be started with a low dose (20mg/day). Your doctor will closely monitor your response to any decrease in the dose.
Patients with liver disease
Your doctor may give you a different dose to normal.
If you take more EFNOCAR Tablets than you should
If you (or someone else) swallow a lot of tablets all together, or if you think a child has swallowed any of the tablets, contact your nearest hospital casualty department or your doctor immediately. Take your medication and the packaging with you to the doctor or casualty department. If you have taken an overdose, you may you may appear flushed (your skin will look red), or you may feel dizzy or faint. If blood pressure drop is severe enough shock can occur.
If you forget to take EFNOCAR Tablets
If you forget to take a tablet, take one as soon as you remember, unless it is nearly time to take the next one. Never take two doses together. Take the remaining doses at the correct time.
If you stop taking EFNOCAR Tablets
Take this medicine for as long as your doctor tells you to, as you may become unwell if you stop.
4. Possible Side Effects
Like all medicines, this medicine can cause side effects, although not everybody gets them. The common side effects are hot flushes, palpitations, facial flushing and headache. In addition, elevation in serum total cholesterol, ALT (SGPT), AST (SGOT) and BUN may occur. Other known side effects are as follows. Tell your doctor if you notice or are worried by any of the side effects listed.
Frequency 0.1 to < 5%
Increased AST (SGOT), ALT (SGPT), LDH, Alkaline Phosphatase
BUN rise, serum creatinine rise, proteinuria
Decreased hemoglobin, decreased hematocrit, decreased red blood cells
Rash, itching
Palpitations, chest pain, decreased blood pressure
Flushing of the face
Headache, sluggishness and light-headedness
Nausea, stomach discomfort, abdominal pain
Malaise, serum total cholesterol rise, CK (CPK) increased, uric acid increased, hypokalemia
Frequency Less than 0.1%
- Increase in bilirubin
- Eosinophilia, leukopenia, thrombocytopenia
- Bradycardia, tachycardia, atrial fibrillation, premature ventricular contraction
- Hot flushes, sweating
- Drowsiness, numbness, and tinnitus
- Vomiting, constipation
- Frequent urination, edema, increased triglycerides
Frequency unknown
- Sick sinus syndrome, atrioventricular junctional rhythm, atrioventricular block, shock
- Diarrhea, Gingival hyperplasia
Tell your doctor or pharmacist if you notice any other effects not listed.
Reporting of side effects
If you get any side effects, talk to your doctor, pharmacist or nurse. This includes any possible side effects not listed in this leaflet. You can also report side effects directly: Website: www.zuventus.co.in and click the tab “Safety Reporting” located on the top right end of the home page.
By reporting side effects, you can help provide more information on the safety of this medicine.
You can also report the side effect with the help of your treating physician.
5. How to Store Efnocar Tablets
Do not use the tablets after the end of the expiry month (use-by date) shown on the product packaging.
Store below 25°C. Protected from light & moisture.
Keep This Medicine Out of the Sight and Reach of Children
Medicines should not be disposed of via wastewater or household waste. Ask your pharmacist how to dispose of medicines no longer required. These measures will help to protect the environment.
6. Contents of the Pack and Other Information
What EFNOCAR Tablets contain
- The active substance is Efonidipine Hydrochloride Ethanolate.
Each tablet contains 10 mg / 20 mg / 40 mg of Efonidipine.
- Other ingredients: Excipients q.s.
Marketing authorisation holder:
Zuventus Healthcare Ltd.
A Joint venture of Emcure, India
Manufacturer responsible for batch release:
Zuventus Healthcare Ltd.
A Joint venture of Emcure,
Kamerey Bhasmay, Elaka Pakyong,
Rangpo, East-Sikkim 737 132.
For More Information About This Product
Efnocar 20 Tablet
1.0 Generic Name
Efonidipine Hydrochloride Ethanolate Tablets 10 mg / 20 mg / 40 mg
2.0 Qualitative and quantitative composition
EFNOCAR-10
Each film coated tablet contains:
Efonidipine Hydrochloride Ethanolate 10 mg
Excipients q.s.
Colour: Titanium Dioxide IP
EFNOCAR-20
Each film coated tablet contains:
Efonidipine Hydrochloride Ethanolate 20 mg
Excipients q.s.
Colour: Titanium Dioxide IP
EFNOCAR-40
Each film coated tablet contains:
Efonidipine Hydrochloride Ethanolate 40 mg
Excipients q.s.
Colour: Titanium Dioxide IP
3.0 Dosage form and strength
Film coated tablet
10/ 20/40 mg
4.0 Clinical particulars
4.1 Therapeutic Indication
Efonidipine is indicated for the management of
- Essential hypertension and renal parenchymal hypertension
- Angina
4.2 Posology and method of administration
Adults
- Essential hypertension and renal parenchymal hypertension: 20-40 mg orally once daily. A dose of up to 80 mg/day has been reported to be safe and effective in clinical trials.
- Angina: 40 mg/day.
Elderly
Efonidipine should be started with a low dose (20mg/day) and the patient's condition should be monitored. The dose should be halved in case the patient is intolerant to the higher dose.
In Children
Efonidipine is not recommended in infants and children as safety is not established in this group of patients.
4.3 Contraindications
- In patients with known hypersensitivity to Efonidipine or any other component of the formulation
- In pregnant women
4.4 Special warnings and precautions for use
- Should be administered with caution in patients with hepatic impairment.
- Should be administered with caution in patients with low BP and/or sinus node dysfunction.
- The drug should be withdrawn gradually to prevent rebound hypertension or worsening of angina.
- Administration of the drug may cause hypotension. Under such circumstances appropriate measures should be taken to either reduce the dose or withdraw the drug.
- Should not be taken with grapefruit juice as there may be excessive lowering of blood pressure.
- Dizziness may occur while taking antihypertensive agents. Hence, working on aerial platform, working with dangerous machinery and/or driving should be avoided.
- To be sold by retail on the prescription of Cardiologist / Nephrologist / Endocrinologist and Specialist in General / Internal medicine / Critical Care medicine only.
4.5 Drugs interactions
Concomitant administration of other antihypertensive agent/s may enhance the antihypertensive effect of efonidipine.
- Administration of calcium channel blockers (CCBs) with Cimetidine may cause elevated levels of CCBs.
- Increased levels of CCBs observed when taken concomitantly with grapefruit juice which may result in excessive lowering of blood pressure.
- Efonidipine when taken along with Tacrolimus may cause increased blood levels of Tacrolimus.
4.6 Use in special populations
Pregnancy
Efonidipine should not be administered in pregnant women.
Nursing Mothers
Efonidipine should not be administered in lactating women.
4.7 Effects on ability to drive and use machines
If patients taking Efonidipine suffer from dizziness, headache, fatigue or nausea the ability to react may be impaired. Caution is recommended especially at the start of treatment.
4.8 Undesirable effects
The common side effects are hot flushes, palpitations, facial flushing and headache. In addition, elevation in serum total cholesterol, ALT (SGPT), AST (SGOT) and BUN may occur.
Tabulated list of adverse reactions


Reporting of suspected adverse reactions
Reporting of suspected adverse reactions
Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via email to:medico@zuventus.com
Website: https://www.zuventus.com/drug-safety-reporting
4.9 Overdose
In humans, experience with intentional overdose is limited. The stomach should be emptied by aspiration and gastric lavage if the patient reports immediately or up to two hours after overdosage.
Clinically significant hypotension due to Efonidipine overdosage calls for active cardiovascular support including frequent monitoring of cardiac and respiratory function, elevation of extremities, and attention to circulating fluid volume and urine output. A vasoconstrictor may be helpful in restoring vascular tone and blood pressure, provided that there is no contraindication to its use. Intravenous calcium gluconate may be beneficial in reversing the effects of calcium channel blockade.
5.0 Pharmacological properties
5.1 Mechanism of Action
Efonidipine, a new generation dihydropyridine (DHP) calcium channel blocker, inhibits both L-type and T-type calcium channels.
5.2 Pharmacodynamic properties
- Efonidipine exhibits antihypertensive effect through vasodilatation by blocking L-type and T-type calcium channels.
- Efonidipine has a negative chronotropic effect. Working on sino atrial node cells by inhibiting T-type calcium channel activation, Efonidipine prolongs the late phase-4 depolarization of the sino atrial node action potential and suppresses an elevated HR. The negative chronotropic effect of Efonidipine decreases heart rate, myocardial oxygen demand and increases coronary blood flow.
- Efonidipine increases coronary blood flow by blocking L & T-type calcium channels and attenuates myocardial ischaemia.
- By reducing synthesis and secretion of aldosterone, Efonidipine prevents hypertrophy and remodeling of cardiac myocytes.
- Efonidipine increases glomerular filtration rate without increasing intra-glomerular pressure and filtration fraction. This prevents hypertension induced renal damage.
- Efonidipine prevents Rho-kinase and NF-kB induced renal parenchymal fibrosis and provides long term renal protection.
- Efonidipine suppresses renin secretion from the Juxta Glomerular apparatus in the kidneys. •Efonidipine enhances sodium excretion from the kidneys by suppressing aldosterone synthesis and secretion from the adrenal glands. Aldosterone induced renal parenchymal fibrosis is suppressed by Efonidipine. •Efonidipine prevents NF-kB induced hypertrophy and inflammation in the renal vasculature and protects the kidneys.
- Efonidipine protects against endothelial dysfunction due to its anti-oxidant activity and by restoring nitric oxide bioavailability.
- Efonidipine has anti-atherogenic activity and protects the blood vessels from atherosclerosis.
- Efonidipine lowers blood pressure in cerebral resistance vessels and prevents hypertension induced brain damage.
5.3 Pharmacokinetic properties
Absorption
Peak plasma concentration is achieved in about 1.5 to 3.67 hours after administration. The bioavailability of Efonidipine is ~25% and half-life is approximately 4 hours.
Efonidipine 40mg when administered to healthy volunteers under fasting conditions shows the following pharmacokinetic profile:

The dissociation constant of Efonidipine from dihydropyridine receptors is very low (0.0042/min/nM), signifying very slow dissociation from the receptors. This explains the long duration of action of Efonidipine.
Metabolism
Efonidipine is primarily metabolized in the liver. The important metabolites are N-dephenylated Efonidipine (DPH), deaminated Efonidipine (AL) and N-debenzylated Efonidipine (DBZ). DBZ and DPH exhibit activity as calcium antagonists. The vasodilating properties of DBZ and DPH were about two-thirds and one-third respectively than that of the parent compound. Results suggest that the majority of the pharmacological effect after oral dosing of Efonidipine hydrochloride in man is due to unchanged compound and its metabolites make a small contribution to the pharmacological effect.
Elimination
Biliary route is the main pathway of excretion. No significant amount of unchanged drug is excreted in urine. In the urine collected for 24 h after an oral dosing, 1.1% of the dose was excreted as deaminated Efonidipine, and 0.5% as a pyridine analogue of deaminated Efonidipine.
6.0 Nonclinical properties
6.1 Animal Toxicology or Pharmacology
The acute toxicology of efonidipine was studied in male and female mice, rats, and dogs following oral or intravenous administration. The intravenous LD, values in male mice and rats were 77 and 51 mg/kg, respectively. The oral LD, values for efonidipine in mice, rats, and dogs were higher than 1,500 mag. The signs of toxicity observed in mice and rats were depression of spontaneous movement, hypothermia, sedation, piloerection, lying, gasping, and clonic convulsion. The dogs developed mild diarrhea, soft stools, or a temporary decrease in food consumption.
A 13-week oral subacute toxicity study of efonidipine was performed in male or female rats and dogs. Increases in water consumption and urine volume were observed in male and female rats receiving efonidipine at 300 mg/kg/day. Urinalysis revealed a high concentration of Na+ and C1- in the rats receiving 100 or 300 mg/kg/day. Organ weight measurement revealed an increase in liver and heart weight in male animals receiving 10 mg/kg/day or more and in female animals receiving 30 mg/kg/day or more.
Thus, in this study, the noneffective dose level was 3 mg/kg/day in rats. The effects observed at 300 or 100 mg/kg/day in groups of male or female dogs included reversible hyperemia of the sclera. Pathological examination revealed a dose-induced increase in the absolute and relative heart weight in female dogs treated with the drug at 100 mg/kg/day or more. Thus, the maximum noneffective dose of efonidipine in dogs of either sex was estimated to be around 30 mg/kg/day.
An oral chronic toxicity study of efonidipine was carried out in rats and dogs. Efonidipine was administered to rats at a daily dose of 1.5, 7, or 30 mg/kg for one year.
Organ weight measurement revealed an increase or a tendency of increase in heart weight in male or female rats receiving 30 mg/kg/day. A decreased thyroid weight in the males and an elevated liver weight in the females were found in the 30 mg/kg/day group.
Therefore, the noneffective estimated oral dose of efonidipine in rats was 7 mg/kg/day. Efonidipine in a gelatin capsule containing 2.0, 6.5, or 20 mg/kg/day was administered to dogs once daily for one year. The estimated effective dose was ca 20 mg/kg/day and the noneffective dose was ca 6.5 mg/kg/day
7.0 Description
Efonidipine is a novel dihydropyridine calcium channel blocker having anti-hypertensive and anti-anginal properties.
Chemical name: (±) -2 - [benzyl (phenyl) amino] ethyl 1, 4-dihydro-2 ,6-dimethyl- 5-(5,5-dimethyl-2-oxo-1 ,3,2-dioxaphosphorinan-2-yl) -4 - (3-nitrophenyl) -3-pyridinecarboxylate hydrochloride ethanol.
Molecular formula: C34H38 N3O7P • HCl •C2H6O
Molecular mass: 714.18 g/mol

8.0 Pharmaceutical particulars
8.1 Incompatibilities
Not applicable.
8.2 Shelf-life
Refer on pack
8.3 Packaging information
10 Blister strips of 10 tablets each
8.4 Storage and handing instructions
- Store below 25°C. Protected from light & moisture.
- Keep out of reach of children.
9.0 Patient Counselling Information
Efnocar is a type of medicine known as a calcium channel blocker (CCB). It is used to treat high blood pressure (hypertension) and a type of chest pain called angina. It can be used by itself or with other medicines to treat these conditions. Do not use Efnocar if you are allergic to efonidipine (the active ingredient in Efnocar), or to the inactive ingredients.
Tell your doctor about any prescription and non-prescription medicines you are taking, including natural or herbal remedies. Tell your doctor if you:
- ever had heart disease
- ever had liver problems
- are pregnant, or plan to become pregnant.
- are breast-feeding. Do not breast-feed while taking Efnocar.
You can stop breast-feeding or take a different medicine.
It may be easier to take your dose if you do it at the same time every day, such as with breakfast or dinner, or at bedtime.
While you are taking Efnocar do not stop taking your other prescription medicines, including any other blood pressure medicines, without talking to your doctor.
12.0 Date of revision
09/10/2024
About Leaflet
The name of your medicine is EFNOCAR 10 mg / 20 mg / 40 mg Tablets. We refer to them as EFNOCAR Tablets or EFNOCAR throughout this leaflet
Read all of this leaflet carefully before you start taking this medicine because it contains important information for you.
Keep this leaflet. You may need to read it again.
If you have any more questions, please ask your doctor or your pharmacist.
This medicine has been prescribed for you personally and you should not pass it on to anyone else. It may harm them, even if their symptoms are the same as yours.
If any of the side effects get serious, or if you notice any side effects that are not listed in the leaflet, please tell your doctor or pharmacist.
In this leaflet:
1. What EFNOCAR Tablets are and what they are used for
2. What you need to know before you take EFNOCAR Tablets
3. How to take EFNOCAR Tablets
4. Possible side effects
5. How to store EFNOCAR Tablets
6. Contents of the pack and other information
1. What Efnocar Tablets Are and What They Are Used for
EFNOCAR Tablets contain the active substance efonidipine which belongs to a group of medicines called calcium antagonists.
EFNOCAR Tablets may be used to treat:
- High blood pressure (hypertension)
- hypertension caused by kidney disease
- A certain type of chest pain called angina
In patients with high blood pressure, these medicines work by relaxing blood vessels, so that blood passes through them more easily. In patients with angina, EFNOCAR works by improving blood supply to the heart muscle which then receives more oxygen and as a result chest pain is prevented. EFNOCAR Tablets do not immediately relieve chest pain caused by angina.
2. What You Need to Know Before You Take Efnocar Tablets
Do not take EFNOCAR Tablets if you:
- Have ever had an allergic reaction to efonidipine or any of the ingredients in the tablet. An allergic reaction may include a rash, itching, difficulty breathing or swelling of the face, lips, throat or tongue;
- If you are pregnant
Take special care with EFNOCAR Tablets
You should inform you doctor if you have or have had any of the following conditions:
Liver disease;
Recent heart attack;
Heart failure;
Severe increase in blood pressure (Hypertensive crisis).
Use in children and adolescents
EFNOCAR is not recommended in infants and children as safety is not established in this group of patients.
For more information, talk to your doctor.
Taking other medicines and EFNOCAR
Please tell your doctor or pharmacist if you are taking or have recently taken other medicines, including medicines obtained without a prescription.
EFNOCAR may affect or be affected by other medicines, such as:
- Other antihypertensive agent/s (BP lowering drugs)
- Cimetidine (stomach acid reducer)
- Tacrolimus (a drug to suppress immunity)
EFNOCAR may lower your blood pressure even more if you are already taking other medicines to treat your high blood pressure.
If you see another doctor or go into hospital for any reason, tell them that you are taking EFNOCAR Tablets.
Taking EFNOCAR Tablets with food and drink
You should not drink grapefruit juice or eat grapefruit while taking this medicine. Grapefruit and grapefruit juice can lead to an increase in the blood levels of efonidipine, which can cause an unpredictable increase in its blood pressure lowering effect.
Pregnancy
The safety of efonidipine in human pregnancy has not been established. Efonidipine should not be administered in pregnant women.
Breast-feeding
It is not known whether efonidipine is passed into breast milk. Efonidipine should not be administered in breast-feeding women.
Ask your doctor or pharmacist for advice before taking any medicine.
Driving and using machines
Dizziness may occur while taking antihypertensive agents. Hence, working on aerial platform, working with dangerous machinery and/or driving should be avoided.
3. How to Take Efnocar Tablets
Swallow these tablets with a glass of water at the same time each day. You can take the tablets after meals.
Follow your doctor’s instructions. Check the pharmacy label to see how many tablets to take and how often to take them. If you are still not sure, ask your pharmacist or doctor. The usual doses are described below.
Adults
Essential hypertension and renal parenchymal hypertension: 20-40 mg orally once daily. A dose of up to 80 mg/day has been reported to be safe and effective in clinical trials.
Angina: 40 mg/day.
Children
EFNOCAR is not recommended in infants and children as safety is not established in this group of patients.
Elderly
EFNOCAR should be started with a low dose (20mg/day). Your doctor will closely monitor your response to any decrease in the dose.
Patients with liver disease
Your doctor may give you a different dose to normal.
If you take more EFNOCAR Tablets than you should
If you (or someone else) swallow a lot of tablets all together, or if you think a child has swallowed any of the tablets, contact your nearest hospital casualty department or your doctor immediately. Take your medication and the packaging with you to the doctor or casualty department. If you have taken an overdose, you may you may appear flushed (your skin will look red), or you may feel dizzy or faint. If blood pressure drop is severe enough shock can occur.
If you forget to take EFNOCAR Tablets
If you forget to take a tablet, take one as soon as you remember, unless it is nearly time to take the next one. Never take two doses together. Take the remaining doses at the correct time.
If you stop taking EFNOCAR Tablets
Take this medicine for as long as your doctor tells you to, as you may become unwell if you stop.
4. Possible Side Effects
Like all medicines, this medicine can cause side effects, although not everybody gets them. The common side effects are hot flushes, palpitations, facial flushing and headache. In addition, elevation in serum total cholesterol, ALT (SGPT), AST (SGOT) and BUN may occur. Other known side effects are as follows. Tell your doctor if you notice or are worried by any of the side effects listed.
Frequency 0.1 to < 5%
Increased AST (SGOT), ALT (SGPT), LDH, Alkaline Phosphatase
BUN rise, serum creatinine rise, proteinuria
Decreased hemoglobin, decreased hematocrit, decreased red blood cells
Rash, itching
Palpitations, chest pain, decreased blood pressure
Flushing of the face
Headache, sluggishness and light-headedness
Nausea, stomach discomfort, abdominal pain
Malaise, serum total cholesterol rise, CK (CPK) increased, uric acid increased, hypokalemia
Frequency Less than 0.1%
- Increase in bilirubin
- Eosinophilia, leukopenia, thrombocytopenia
- Bradycardia, tachycardia, atrial fibrillation, premature ventricular contraction
- Hot flushes, sweating
- Drowsiness, numbness, and tinnitus
- Vomiting, constipation
- Frequent urination, edema, increased triglycerides
Frequency unknown
- Sick sinus syndrome, atrioventricular junctional rhythm, atrioventricular block, shock
- Diarrhea, Gingival hyperplasia
Tell your doctor or pharmacist if you notice any other effects not listed.
Reporting of side effects
If you get any side effects, talk to your doctor, pharmacist or nurse. This includes any possible side effects not listed in this leaflet. You can also report side effects directly: Website: www.zuventus.co.in and click the tab “Safety Reporting” located on the top right end of the home page.
By reporting side effects, you can help provide more information on the safety of this medicine.
You can also report the side effect with the help of your treating physician.
5. How to Store Efnocar Tablets
Do not use the tablets after the end of the expiry month (use-by date) shown on the product packaging.
Store below 25°C. Protected from light & moisture.
Keep This Medicine Out of the Sight and Reach of Children
Medicines should not be disposed of via wastewater or household waste. Ask your pharmacist how to dispose of medicines no longer required. These measures will help to protect the environment.
6. Contents of the Pack and Other Information
What EFNOCAR Tablets contain
- The active substance is Efonidipine Hydrochloride Ethanolate.
Each tablet contains 10 mg / 20 mg / 40 mg of Efonidipine.
- Other ingredients: Excipients q.s.
Marketing authorisation holder:
Zuventus Healthcare Ltd.
A Joint venture of Emcure, India
Manufacturer responsible for batch release:
Zuventus Healthcare Ltd.
A Joint venture of Emcure,
Kamerey Bhasmay, Elaka Pakyong,
Rangpo, East-Sikkim 737 132.
For More Information About This Product
Boroflex Capsule
1.0 Generic name
Calcium Fructoborate Capsules
2.0 Qualitative and quantitative composition
Each serving per capsule contains:
Calcium Fructoborate equivalent to elemental Boron 6 mg
Ingredients:
Calcium Fructoborate, Bulking Agent [INS 460 (i)], Anticaking Agent [INS 553 (iii)], Antisticking Agent [INS 470 (i)], Ingredient of capsule shell [INS 464], Synthetic food colour [INS 102] & [INS 171]
Nutritional Information

* % RDA calculated as per ICMR Guidelines, 2020 for sedentary work men.
** % RDA values calculated as per FSSAI Labeling and Display Regulation 2020 for average adult.
# % RDA not established.
3.0 Dosage form and strength
Capsule
6 mg (elemental Boron)
BoroflexTM is a Natural-identical form Calcium Fructoborate
100% Vegan and non-genetically modified (Non-GMO)
4.0 Clinical particulars
4.1 Therapeutic indication
Helps for bone and joint health.
4.2 Posology and method of administration
NUTRACEUTICAL
Target Consumer Group: Adults
Recommended usage: One capsule twice a day
Not to exceed the recommended daily dose.
Capsule should be swallowed whole & not to be opened, chewed or crushed.
4.3 Contraindications
Don't take this preparation if you are allergic to it or any ingredients contained in this preparation.
4.4 Special warnings and precautions for use
- It is Nutraceutical and Not for Medicinal Use.
- Allergen Information: Allergen free.
- This product is not intended to diagnose, treat, cure or prevent any disease.
- This product is not to be used as a substitute for a varied diet.
4.5 Drugs interactions
Boron is not known to have any clinically relevant interactions with medications.
- Fructoborates have positive synergic interactions with calcium, magnesium, zinc, iron, and copper.
- The amount of fructoborate should be increased when the amount of iodine, fluoride, and silicon from the body increases as well.
- Antagonism: Fructoborates are antagonized by silicon as orthosilicic acid, by iodine, and by fluoride.
4.6 Use in special populations
Pregnant / lactating women, children & people with medical conditions should consult a Healthcare Professional before use.
4.7 Effects on ability to drive and use machines
No effect anticipated. There isn’t specific research directly linking boron supplementation to driving performance.
4.8 Undesirable effects
Generally recognized as safe (GRAS certified) by United States Food and Drug Administration (FDA). Generally well-tolerated; possible mild side effects include gastrointestinal discomfort, headaches, or skin reactions.
Reporting of suspected adverse reactions
Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via email to:medico@zuventus.com
Website: https://www.zuventus.com/drug-safety-reporting
By reporting side effects, you can help provide more information on the safety of this medicine.
5.0 Pharmacological properties
5.1 Pharmacodynamic properties
Boron is a trace element found in various foods and available as a dietary supplement. It plays essential roles in the metabolism of plants, animals, and humans, and recent research suggests it may have been significant for the evolution of life on Earth. The World Health Organization recognizes boron as "probably essential" for humans. In food and beverages, boron appears as inorganic borates or as mono- or di-sugar-borate esters, such as calcium fructoborate.
Calcium fructoborate (CaFB) is a plant-based boron compound that enters cells via sugar transporters (GLUTs), facilitating the absorption of fructoboric acid. It acts as a catalyst for CO2 hydration, enhancing buffering capacity at physiological pH. CaFB modulates various cell signaling pathways, influencing inflammatory mediators and transcription factors, and exhibits antioxidant properties by reducing reactive oxygen species (ROS). Compared to traditional boric acid, CaFB has more complex mechanisms of action, including the formation of sugar borate esters (SBEs) that interact with key amino acids. SBEs are considered conditionally essential nutrients, potentially influencing metabolic processes and disorders like arthritis and diabetes. Additionally, CaFB demonstrates anti-inflammatory effects by regulating cytokine production and lowering inflammatory markers. Importantly, it exists as a non-toxic boron reservoir, allowing safe biological activity inside and outside cells. Overall, CaFB's diverse mechanisms distinguish it from conventional boron compounds.
5.2 Boron and Bone Health
Clinical studies suggest that boron may help reduce osteoarthritis symptoms by inhibiting inflammation. It plays a crucial role in bone growth and formation, potentially influencing osteoblast and osteoclast activity, serum steroid hormone levels, and calcium metabolism. Boron deficiency has been linked to abnormal limb development, delayed growth plate maturation, and decreased bone strength. Supplementation has shown to improve bone strength measures in animal studies.
Boron and Calcium Metabolism: Research indicates that boron deprivation leads to increased urinary excretion of calcium and magnesium and decreased levels of key hormones in postmenopausal women. Boron may positively influence calcium and vitamin D metabolism, reducing the risk of osteoporosis. A study found that 6 mg of boron supplementation per day for 60 days raised serum vitamin D levels by about 20% in vitamin D-deficient subjects. Additionally, a trial with female athletes and sedentary women showed that 3 mg/day of boron for 10 months reduced serum phosphorus and increased magnesium levels, potentially enhancing bone mineral density.
Boron and Arthritis: Lower boron intake has been associated with higher rates of arthritis. Studies have shown a negative correlation between soil boron levels and arthritis incidence. In areas with daily boron intakes of 1.0 mg or less, arthritis rates range from 20% to 70%, while in areas with 3–10 mg intake, rates drop to 0%–10%. A double-blind study indicated that 6 mg/day of boron significantly improved joint conditions and reduced pain in osteoarthritis patients after 8 weeks of supplementation compared to a placebo.
Stimulates Osteogenesis: Promotes osteoblast differentiation and reduces superoxide formation. Boosts testosterone, increases muscle mass, improves calcium absorption, and maintains bone density. Enhances the bioavailability of sex hormones and Vitamin D. Anti-oxidant Action: Acts as an anti-inflammatory by inhibiting oxidative bursts and improving free radical scavenging. Inhibits collagenase enzymes, protecting skin, joints, and bones.
Safety and Efficacy: Improves osteoarthritis symptoms and reduces inflammatory markers. Reduces knee discomfort and improves joint flexibility. Improves inflammatory and cardiovascular biomarkers. It reduces the use of painkillers.
Overall, boron appears to play a beneficial role in bone health, calcium metabolism, and potentially in reducing arthritis symptoms.
5.3 Pharmacokinetic properties
Absorption
Boroflex is water soluble and highly bioavailable. Most ingested boron is hydrolyzed to boric acid within the gastrointestinal tract. Fructoborates are absorbed in the small intestine. The body absorbs about 85%–90% of ingested boron.
Our bodies have no capability to synthesize them from fructose and boric acid. Studies have shown that Calcium Fructoborate (CaFB) absorbed from the gastrointestinal tract to the bloodstream in an intact form and time-dependent manner. Study results show that CaFB can be detected intact in blood following oral administration. Thus, it has been confirmed that CaFB could:
(a) have a distinct purpose and bioactivity of its own or
(b) serve as a controlled-release supply of Boron that does not convert back to Boric acid in tissues and blood
Some studies have identified three types of B-containing molecules of CaFB in aqueous solutions (the speciation of fructoborates is highlighted in Fig. 2): Free Boric Acid (5%), Diester (85%) and Monoester complex (10 %).

Figure: FBE speciation in the human metabolism
Subsequently, Fructoborate species may possess a biological role such as functioning as a coenzyme or cofactor (Fig.).

Metabolism of Fructoborates in enzymatic system
The biological and clinical benefits observed thus far for CaFB suggest that B-containing sugars are indeed unique and extraordinary participants in the realm of B-containing molecules. Studies have shown that CaFB is a good adjuvant in the treatment of osteoporosis, possibly the best in dietetic prevention of osteoporosis based on the large study group.
Storage
Fructoborates have been found in mice bone, heart, brain, liver, and muscle.
Excretion
In animal metabolism (mice), fructoborates are metabolized initially in fructoboric acid and then in boric acid and excreted mainly through urine.
6.0 Nonclinical properties
6.1 Animal Toxicology or Pharmacology
Not available
7.0 Description
Calcium fructoborate is a natural identical product with molecular composition Ca[(C6H10O6)2B]2°4H2O, identical with the calcium fructoborate molecule found in nature.
Sugar–borates (SBs) are mono- or di-sugar–borate esters (SBEs) comprised of one or two monosaccharide molecules linked to a boron (B) atom.
Using liquid- and solid-state 11B and 13C nuclear magnetic resonance (NMR) spectroscopy, the fructoborate anion structure was defined (figure-1).

Fructoborate anion structure
Three basic types of boron-containing molecules are found in aqueous solutions of Boroflex: free boric acid, the diester complex, and the monoester complex. The relative molar concentrations of these 3 types of boron-containing molecules were found to be approx. 5%, 85%, and 10 %, respectively.
8.0 Pharmaceutical properties
8.1 Incompatibilities
None
8.2 Shelf-life
Refer on pack.
8.3 Packaging information
1 Blister strip of 10 capsules
1 x 10 N Capsules
8.4 Storage and handing instructions
Store below 30°C. Protect from light & moisture.
Keep out of reach of children
9.0 Patient counselling information
- Pregnant or nursing mothers, children, and people with medical conditions must consult a physician before taking this supplement
- Generally well-tolerated; possible mild side effects include gastrointestinal discomfort, headaches, or skin reactions.
- Long-term high doses may lead to toxicity, so adherence to recommended doses is crucial.
- Inform your healthcare provider about any medications or supplements you are currently taking, as CaFB may interact with certain drugs, especially those affecting bone health or hormone levels.
- Regular follow-up appointments with your healthcare provider are recommended to assess your response to the supplement and make necessary adjustments.
- Keep track of any changes in your symptoms, especially concerning bone and joint health.
12.0 Date of revision of the text
27th September 2024
About leaflet
Read all of this leaflet carefully before you start taking this medicine because it contains important information for you.
- Keep this leaflet. You may need to read it again.
- If you have any further questions, ask your doctor or pharmacist.
- This medicine has been prescribed for you only. Do not pass it on to others. It may harm them, even if their signs of illness are the same as yours.
- If you get any side effects, talk to your doctor or pharmacist. This includes any possible side effects not listed in this leaflet. See section 4.
What is in this leaflet:
- What Boroflex is and what it is used for
- What you need to know before you take Boroflex
- How to take Boroflex
- Possible side effects
- How to store Boroflex
- Contents of the pack and other information
1. What Boroflex is and what it is used for
Boroflex contains Calcium Fructoborate, a natural-identical form of boron. Boron is a trace mineral important for bone health due to several key benefits:
1. Enhances Calcium Absorption: It aids in the effective absorption of calcium, vital for strong bones.
2. Supports Vitamin D Function: Boron prolongs the activity of vitamin D, essential for calcium absorption.
3. Regulates Hormones: It influences the metabolism of steroid hormones like estrogen and testosterone, crucial for bone density.
4. Prevents Bone Diseases: By optimizing calcium and magnesium use, boron helps prevent osteoporosis and arthritis.
Boroflex™ capsules are used as a dietary supplement to support bone and joint health.
2. What you need to know before you take Boroflex
Do not take Boroflex:
- If you are allergic to Calcium Fructoborate or any of the other ingredients of this medicine (listed in section 6).
Warnings and precautions:
- This product is a nutraceutical and not for medicinal use.
- Consult your healthcare provider before use if you are pregnant, breastfeeding, have any medical conditions, or are taking any other medications.
Other medicines and Boroflex:
- Boron is not known to have any clinically relevant interactions with medications. However, it has positive synergic interactions with calcium, magnesium, zinc, iron, and copper.
Use in special populations
Pregnant / lactating women, children & people with medical conditions should consult a Healthcare Professional before use.
Effects on ability to drive and use machines
No effect anticipated. There isn’t specific research directly linking boron supplementation to driving performance.
3. How to take Boroflex
Dosage:
- The recommended dose is one capsule twice a day. Do not exceed the recommended daily dose.
Method of administration:
- Swallow the capsule whole with water. Do not open, chew, or crush the capsule.
4. Possible side effects
Boroflex is generally well-tolerated. However, some people may experience mild side effects such as:
- Gastrointestinal discomfort
- Headaches
- Skin reactions
If you experience any side effects, talk to your doctor or pharmacist. Reporting of side effects: If you experience any side effects, talk to your doctor or pharmacist. This includes any possible side effects not listed in this leaflet.You can also report side effects directly: Website: www.zuventus.com in and click the tab “Safety Reporting” located on the top end of the home page.
Website link: https://www.zuventus.com/drug-safety-reporting
By reporting side effects, you can help provide more information on the safety of this product.
5. How to store Boroflex
- Store below 30°C. Protect from light and moisture.
- Keep out of the reach of children.
6. Contents of the pack and other information
What Boroflex contains:
- The active substance is Calcium Fructoborate equivalent to elemental Boron 6 mg.
- Other ingredients include bulking agents, anticaking agents, antisticking agents, and synthetic food colors.
For More Information About This Product
Cortimax 12 mg Tablets
1.0 Generic name
Deflazacort Tablets 6 mg/12mg/24 mg/30 mg
2.0 Qualitative and quantitative composition
Each uncoated tablet contains
Deflazacort 6 mg/12 mg/24 mg/30 mg.
Excipients q.s.
3.0 Dosage form and strength
Tablets for oral administration.
6 mg/12 mg/24 mg/30 mg
4.0 Clinical particulars
4.1. Therapeutic indication
For asthma, rheumatoid arthritis when glucocorticosteriod therapy is warranted.
4.2.Posology and method of administration
Deflazacort is a glucocorticoid derived from prednisolone and 6mg of deflazacort has approximately the same anti-inflammatory potency as 5mg prednisolone or prednisone. Doses vary widely in different diseases and different patients. In more serious and lifethreatening conditions, high doses of deflazacort may need to be given. When deflazacort is used long term in relatively benign chronic diseases, the maintenance dose should be kept as low as possible. Dosage may need to be increased during periods of stress or in exacerbation of illness. The dosage should be individually titrated according to diagnosis, severity of disease and patient response and tolerance. The lowest dose that will produce an acceptable response should be used.
Adults
For acute disorders, up to 120 mg/day deflazacort may need to be given initially. Maintenance doses in most conditions are within the range 3-18 mg/day. The following regimens are for guidance only
Rheumatoid arthritis: The maintenance dose is usually within the range 3 - 18 mg/day. The smallest effective dose should be used and increased if necessary.
Bronchial asthma: In the treatment of an acute attack, high doses of 48-72 mg/day may be needed depending on severity and gradually reduced once the attack has been controlled. For maintenance in chronic asthma, doses should be titrated to the lowest dose that controls symptoms.
Other conditions: The dose of deflazacort depends on clinical need titrated to the lowest effective dose for maintenance. Starting doses may be estimated on the basis of ratio of 5mg prednisone or prednisolone to 6mg deflazacort.
Hepatic Impairment
In patients with hepatic impairment, blood levels of deflazacort may be increased. Therefore, the dose of deflazacort should be carefully monitored and adjusted to the minimum effective dose.
Renal Impairment
In renally impaired patients, no special precautions other than those usually adopted in patients receiving glucocorticoid therapy are necessary.
Elderly
In elderly patients, no special precautions other than those usually adopted in patients receiving glucocorticoid therapy are necessary. The common adverse effects of systemic corticosteroids may be associated with more serious consequences in old age.
Paediatric Population
There has been limited exposure of children to deflazacort in clinical trials. In children, the indications for glucocorticoids are the same as for adults, but it is important that the lowest effective dosage is used. Alternate day administration may be appropriate.
Doses of deflazacort usually lie in the range 0.25 - 1.5 mg/kg/day. The following ranges provide general guidance:
Juvenile chronic arthritis: The usual maintenance dose is between 0.25 - 1.0 mg/kg/day
Nephrotic syndrome: Initial dose of usually 1.5 mg/kg/day followed by down titration according to clinical need.
Bronchial asthma: On the basis of the potency ratio, the initial dose should be between 0.25 - 1.0 mg/kg deflazacort on alternate days.
Deflazacort withdrawal
In patients who have received more than physiological doses of systemic corticosteroids (approximately 9mg per day or equivalent) for greater than 3 weeks, 3 withdrawal should not be abrupt. How dose reduction should be carried out depends largely on whether the disease is likely to relapse as the dose of systemic corticosteroids is reduced. Clinical assessment of disease activity may be needed during withdrawal. If the disease is unlikely to relapse on withdrawal of systemic corticosteroids but there is uncertainty about HPA suppression, the dose of systemic corticosteroids may be reduced rapidly to physiological doses. Once a daily dose equivalent to 9mg deflazacort is reached, dose reduction should be slower to allow the HPA-axis to recover. Abrupt withdrawal of systemic corticosteroid treatment, which has continued up to 3 weeks is appropriate if it is considered that the disease is unlikely to relapse. Abrupt withdrawal of doses up to 48 mg daily of deflazacort, or equivalent for 3 weeks is unlikely to lead to clinically relevant HPA-axis suppression, in the majority of patients. In the following patient groups, gradual withdrawal of systemic corticosteroid therapy should be considered even after courses lasting 3 weeks or less:
- Patients who have had repeated courses of systemic corticosteroids, particularly if taken for greater than 3 weeks.
- When a short course has been prescribed within one year of cessation of long-term therapy (months or years).
- Patients who may have reasons for adrenocortical insufficiency other than exogenous corticosteroid therapy.
- Patients receiving doses of systemic corticosteroid greater than 48 mg daily of deflazacort (or equivalent),
- Patients repeatedly taking doses in the evening
4.3.Contraindications
Systemic infection unless specific anti-infective therapy is employed. Hypersensitivity to the active substance, deflazacort or any of the excipients. Patients receiving live virus immunisation.
4.4.Special warnings and precautions for use
Patients with rare hereditary problems of galactose intolerance, the Lapp lactose deficiency or glucose-galactose malabsorption should not take this medicine. Undesirable effects may be minimised by using the lowest effective dose for the minimum period, and by administering the daily requirement as a single morning dose or whenever possible as a single morning dose on alternate days. Frequent patient review is required to appropriately titrate the dose against disease activity.
Adrenal suppression
Adrenal cortical atrophy develops during prolonged therapy and may persist for years after stopping treatment. Withdrawal of corticosteroids after prolonged therapy must therefore always be gradual to avoid acute adrenal insufficiency which could be fatal, being tapered off over weeks or months according to the dose and duration of treatment. During prolonged therapy, any intercurrent illness, trauma or surgical procedure will require a temporary increase in dosage; if corticosteroids have been stopped following prolonged therapy, they may need to be temporarily re-introduced. Patients should carry 'Steroid treatment' cards which give clear guidance on the precautions to be taken to minimise risk and which provide details of prescriber, drug, dosage and the duration of treatment.
Anti-inflammatory/immunosuppressive effects and infection
Suppression of the inflammatory response and immune function increases the susceptibility to infections and their severity. The clinical presentation may often be atypical and serious infections such as septicaemia and tuberculosis may be masked and may reach an advanced stage before being recognised. Chickenpox is of particular concern since this normally minor illness may be fatal in immunosuppressed patients. Patients (or parents of children) without a definite history of chicken pox should be advised to avoid close personal contact with chickenpox or herpes zoster and, if exposed, they should seek urgent medical attention. Passive immunisation with varicella zoster immunoglobulin (VZIG) is needed by exposed non-immune patients who are receiving systemic corticosteroids or who have used them within the previous 3 months; this should be given within 10 days of exposure to chickenpox. If a diagnosis of chickenpox is confirmed, the illness warrants specialist care and urgent treatment. Corticosteroids should not be stopped and the dose may need to be increased. Patients should be advised to take particular care to avoid exposure to measles and to seek immediate medical advice if exposure occurs. Prophylaxis with intramuscular normal immunoglobulin may be needed. Live vaccines should not be given to individuals with impaired responsiveness. The antibody response to other vaccines may be diminished.
Visual disturbance
Visual disturbance may be reported with systemic and topical corticosteroid use. If a patient presents with symptoms such as blurred vision or other visual disturbances, the patient should be considered for referral to an ophthalmologist for evaluation of possible causes which may include cataract, glaucoma or rare diseases such as central serous chorioretinopathy (CSCR) which have been reported after use of systemic and topical corticosteroids. Prolonged use of glucocorticoids may produce posterior subcapsular cataracts, glaucoma with possible damage to the optic nerves and may enhance the establishment of secondary ocular infections due to fungi or viruses. Use in active tuberculosis should be restricted to those cases of fulminating and disseminated tuberculosis in which deflazacort is used for management with appropriate antituberculosis regimen. If glucocorticoids are indicated in patients with latent tuberculosis or tuberculin reactivity, close observation is necessary as reactivation of the disease may occur. During prolonged glucocorticoid therapy, these patients should receive chemoprophylaxis. Tendonitis and tendon rupture are known class effect of glucocorticoids. The risk of such reactions may be increased by co-administration of quinolones. Pheochromocytoma crisis, which can be fatal, has been reported after administration of systemic corticosteroids. Corticosteroids should only be administered to patients with suspected or identified pheochromocytoma after an appropriate risk/benefit evaluation.
Special precautions
The following clinical conditions require special caution and frequent patient monitoring is necessary: -
- Cardiac disease or congestive heart failure (except in the presence of active rheumatic carditis), hypertension, thromboembolic disorders. Glucocorticoids can cause salt and water retention and increased excretion of potassium. Dietary salt restriction and potassium supplementation may be necessary.
- Gastritis or oesophagitis, diverticulitis, ulcerative colitis if there is probability of impending perforation, abscess or pyogenic infections, fresh intestinal anastomosis, active or latent peptic ulcer.
- Diabetes mellitus or a family history, osteoporosis, myasthenia gravis, renal insufficiency.
- Emotional instability or psychotic tendency, epilepsy.
- Previous corticosteroid-induced myopathy.
- Liver failure.
- Hypothyroidism and cirrhosis, which may increase glucocorticoid effect.
- Ocular herpes simplex because of possible corneal perforation.
Patients and/or carers should be warned that potentially severe psychiatric adverse reactions may occur with systemic steroids. Symptoms typically emerge within a few days or weeks of starting the treatment. Risks may be higher with high doses/systemic exposure, although dose levels do not allow prediction of the onset, type, severity or duration of reactions. Most reactions recover after either dose reduction or withdrawal, although specific treatment may be necessary. Patients/carers should be encouraged to seek medical advice if worrying psychological symptoms develop, especially if depressed mood or suicidal ideation is suspected. Patients/carers should also be alert to possible psychiatric disturbances that may occur either during or immediately after dose tapering/withdrawal of systemic steroids, although such reactions have been reported infrequently.
Particular care is required when considering the use of systemic corticosteroids in patients with existing or previous history of severe affective disorders in themselves or in their first degree relatives. These would include depressive or manic-depressive illness and previous steroid psychosis. Glucocorticoids are known to cause irregular menstruation and leukocytosis, care should be taken with deflazacort.
Paediatric population
Corticosteroids cause dose-related growth retardation in infancy, childhood and adolescence which may be irreversible. Hypertrophic cardiomyopathy has been reported after systemic administration of glucocorticosteroids in preterm infants. In infants receiving administration of systemic glucocorticosteroids, echocardiograms should be performed to monitor myocardial structure and function.
Use in Elderly
The common adverse effects of systemic corticosteroids may be associated with more serious consequences in old age, especially osteoporosis, hypertension, hypokalaemia, diabetes, susceptibility to infection and thinning of the skin. Close clinical supervision is required to avoid life-threatening reactions. Since complications of glucocorticoid therapy are dependent on dose and duration of therapy, the lowest possible dose must be given and a risk/benefit decision must be made as to whether intermittent therapy should be used.
4.5.Interaction with other medicinal products and other forms of interaction
- The same precautions should be exercised as for other glucocorticoids. Deflazacort is metabolised in the liver. It is recommended to increase the maintenance dose of deflazacort if drugs which are liver enzyme inducers are co-administered, e.g. rifampicin, rifabutin, carbamazepine, phenobarbitone, phenytoin, primidone and aminoglutethimide. For drugs which inhibit liver enzymes, e.g. ketoconazole it may be possible to reduce the maintenance dose of deflazacort.
- In patients taking estrogens, corticosteroid requirements may be reduced.
- The desired effects of hypoglycaemic agents (including insulin), anti-hypertensives and diuretics are antagonised by corticosteroids and the hypokalaemic effects of acetazolamide, loop diuretics, thiazide diuretics, beta 2-agonists, xanthines and carbenoxolone are enhanced.
- The efficacy of coumarin anticoagulants may be enhanced by concurrent corticosteroid therapy and close monitoring of the INR or prothrombin time is required to avoid spontaneous bleeding.
- In patients treated with systemic corticosteroids, use of non-depolarising muscle relaxants can result in prolonged relaxation and acute myopathy. Risk factors for this include prolonged and high dose corticosteroid treatment, and prolonged duration of muscle paralysis. This interaction is more likely following prolonged ventilation (such as in the ITU setting).
- The renal clearance of salicylates is increased by corticosteroids and steroid withdrawal may result in salicylate intoxication.
- As glucocorticoids can suppress the normal responses of the body to attack by micro-organisms, it is important to ensure that any anti-infective therapy is effective and it is recommended to monitor patients closely. Concurrent use of glucocorticoids and oral contraceptives should be closely monitored as plasma levels of glucocorticoids may be increased. This effect may be due to a change in metabolism or binding to serum proteins. Antacids may reduce bioavailability; leave at least 2 hours between administration of deflazacort and antacids. 8
- Co-treatment with CYP3A inhibitors, including cobicistat-containing products, is expected to increase the risk of systemic side-effects. The combination should be avoided unless the benefit outweighs the increased risk of systemic corticosteroid side-effects, in which case patients should be monitored for systemic corticosteroid side-effects.
4.6.Fertility, pregnancy and lactation
Pregnancy
The ability of corticosteroids to cross the placenta varies between individual drugs, however, deflazacort does cross the placenta. Administration of corticosteroids to pregnant animals can cause abnormalities of foetal development including cleft palate, intra-uterine growth retardation and effects on brain growth and development. There is no evidence that corticosteroids result in an increased incidence of congenital abnormalities, such as cleft palate/lip in man. However, when administered for prolonged periods or repeatedly during pregnancy, corticosteroids may increase the risk of intra-uterine growth retardation. Hypoadrenalism may, in theory, occur in the neonate following prenatal exposure to corticosteroids but usually resolves spontaneously following birth and is rarely clinically important. As with all drugs, corticosteroids should only be prescribed when the benefits to the mother and child outweigh the risks. When corticosteroids are essential however, patients with normal pregnancies may be treated as though they were in the non-gravid state.
Breast-feeding
Corticosteroids are excreted in breast milk, although no data are available for deflazacort. Doses of up to 50 mg daily of deflazacort are unlikely to cause systemic effects in the infant. Infants of mothers taking higher doses than this may have a degree of adrenal suppression but the benefits of breast feeding are likely to outweigh any theoretical risk.
Fertility
No data is available on Deflazacort and its effects on fertility.
4.7.Effects on ability to drive and use machines
The effect of corticosteroids on the ability to drive or use machinery has not been systematically evaluated. Vertigo is a possible undesirable effect after treatment with deflazacort. If affected, patients should not drive or operate machinery.
4.8.Undesirable effects
The incidence of predictable undesirable effects, including hypothalamic-pituitaryadrenal suppression correlates with the relative potency of the drug, dosage; timing of administration and the duration of treatment. The following CIOMS frequency rating is used: Very common (≥1/10); common (≥1/100 to <1/10); uncommon (≥1/1000 to <1/100); rare (≥1/10000 to <1/1000); very rare (<1/10000), not known (cannot be estimated from the available data).
Endocrine disorders
Uncommon: Suppression of the hypothalamic-pituitary-adrenal axis, amenorrhoea, Cushingoid facies. Not known: Growth suppression in infancy, childhood and adolescence.
Metabolism and nutrition disorders
Common: Weight gain. Uncommon: impaired carbohydrate tolerance with increased requirement for antidiabetic therapy, sodium and water retention with hypertension, potassium loss and hypokalaemic alkalosis when co-administered with beta 2-agonist and xanthines. Not known: Negative protein and calcium balance, increased appetite.
Infections and Infestations
Uncommon: Increased susceptibility and severity of infections with suppression of clinical symptoms and signs, opportunistic infections, recurrence of dormant tuberculosis. Not known: candidiasis.
Musculoskeletal and connective tissue disorders
Uncommon: Osteoporosis, vertebral and long bone fractures. Rare: Muscle wasting. Not known: avascular osteonecrosis, tendonitis and tendon rupture when coadministered with quinolones, myopathy (acute myopathy may be precipitated by nondepolarising muscle relaxants, negative nitrogen balance.
Reproductive system and breast disorders
Not known: Menstrual irregularity.
Cardiac disorders
Not known: Heart failure, hypertrophic cardiomyopathy in preterm infants.
Nervous system disorders
Uncommon: Headache, vertigo.
Not known: restlessness, Increased intra-cranial pressure with papilloedema in children (pseudotumour cerebri), usually after treatment withdrawal, aggravation of epilepsy.
Psychiatric disorders
A wide range of psychiatric reactions including affective disorders such as: Uncommon: depressed and labile mood. Not known: irritable, euphoric, suicidal thoughts. Psychotic reactions including: Not known: mania, delusions, hallucinations, aggravation of schizophrenia Other reactions including: Uncommon: behavioural disturbances. Not known: anxiety, sleep disturbances, and cognitive dysfunction including confusion and amnesia have been reported. Reactions are common and may occur in both adults and children. In adults, the frequency of severe reactions has been estimated to be 5-6%. Psychological effects have been reported on withdrawal of corticosteroids; the frequency is unknown.
Eye disorders
Not known: Vision blurred, increased intra-ocular pressure, glaucoma, papilloedema, posterior subcapsular cataracts especially in children, chorioretinopathy, corneal or scleral thinning, exacerbation of ophthalmic viral or fungal diseases.
Gastrointestinal disorders
Uncommon: Dyspepsia, peptic ulceration, haemorrhage, nausea. Not known: perforation of peptic ulcer, acute pancreatitis (especially in children), candidiasis.
Skin and subcutaneous tissue disorders
Uncommon: hirsutism, striae, acne.
Rare: bruising.
Not known: Skin atrophy, telangiectasia.
General disorders and administration site conditions
Uncommon: Oedema.
Not known: impaired healing.
Immune system disorders
Uncommon: Hypersensitivity including anaphylaxis has been reported.
Blood and lymphatic system disorders
Not known: Leukocytosis.
Vascular disorders
Not known: Thromboembolism in particular in patients with underlying conditions associated with increased thrombotic tendency, rare incidence of benign intracranial hypertension.
Withdrawal symptoms and signs
Not known: Too rapid a reduction of corticosteroid dosage following prolonged treatment can lead to acute adrenal insufficiency, hypotension and death. A 'withdrawal syndrome' may also occur including fever, myalgia, arthralgia, rhinitis, conjunctivitis, painful itchy skin nodules and loss of weight. This may occur in patients even without evidence of adrenal insufficiency.
Class effect
Pheochromocytoma crisis has been reported with other systemic corticosteroids and is a known class effect.
Reporting of suspected adverse reactions
Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via email to: medico@zuventus.com By reporting side effects, you can help provide more information on the safety of this medicine.
4.9. Overdose
It is unlikely that treatment is needed in cases of acute overdosage. The LD50 for the oral dose is greater than 4000 mg/kg in laboratory animals.
5.0 Pharmacological properties
5.1 Pharmacodynamic properties
Pharmacotherapeutic group: corticosteroids for systemic use; Glucocorticoids. ATC code: H02AB13. Deflazacort is a glucocorticoid. Its anti-inflammatory and immunosuppressive effects are used in treating a variety of diseases and are comparable to other antiinflammatory steroids. Clinical studies have indicated that the average potency ratio of deflazacort to prednisolone is 0.69-0.89.
5.2 Pharmacokinetic properties
Absorption: Orally administered deflazacort appears to be well absorbed.
Distribution: The active metabolite D 21-OH achieves peak plasma concentrations in 1.5 to 2 hours. It is 40% protein-bound and has no affinity for corticosteroid-binding-globulin (transcortin).
Biotransformation: Orally administered deflazacort is immediately converted by plasma esterases to the pharmacologically active metabolite (D 21-OH). Metabolism of D 21-OH is extensive. The metabolite of D 21-OH is deflazacort 6- beta-OH.
Elimination: Its elimination plasma half-life is 1.1 to 1.9 hours. Elimination takes place primarily through the kidneys; 70% of the administered dose is excreted in the urine. The remaining 30% is eliminated in the faeces. Metabolism of D 21-OH is extensive; only 18% of urinary excretion represents D 21-OH. The metabolite of D 21-OH, deflazacort 6-beta-OH, represents one third of the urinary elimination.
6.0 Nonclinical properties
Safety studies have been carried out in the rat, dog, mouse and monkey. The findings are consistent with other glucocorticoids at comparable doses. Teratogenic effects demonstrated in rodents and rabbits are typical of those caused by other glucocorticoids. Deflazacort was not found to be carcinogenic in the mouse, but studies in the rat produced carcinogenic findings consistent with the findings with other glucocorticoids.
7.0 Description
Deflazacort, is an oxaline derivative of Prednisolone.

Figure: Structure of Deflazacort
IUPAC Name: (11β,16β)-21-(acetyloxy)-11-hydroxy-2'-methyl-5'H-pregna-1,4- dieno[17,16-d]oxazole-3,20-dione Molecular Formula: C25H31NO6 Molecular Weight: 441.5 g/mol
8.0 Pharmaceutical particulars
1. Incompatibilities Not applicable.
2. Shelf-life
3. Packaging information
4. Storage and handing instructions
- Keep out of reach of children. Keep out of the sight and reach of children. Store in a dry place at a temperature not exceeding 25°C.
9.0 Patient Counselling Information
A patient information leaflet is available for this product.
Administration
Warn patients and/or caregivers to not stop taking Cortimax abruptly or without first checking with their healthcare providers as there may be a need for gradual dose reduction to decrease the risk of adrenal insufficiency.
Cortimax may be taken with or without food. Do not take Cortimax with grapefruit juice.
Tablets
Cortimax Tablets may be taken whole or crushed and taken immediately after mixing with applesauce.
Increased Risk of Infection
Tell patients and/or caregivers to inform their healthcare provider if the patient has had recent or ongoing infections or if they have recently received a vaccine. Medical advice should be sought immediately if the patient develops fever or other signs of infection. Patients and/or caregivers should be made aware that some infections can potentially be severe and fatal. Warn patients who are on corticosteroids to avoid exposure to chickenpox or measles and to alert their healthcare provider immediately if they are exposed.
Alterations in Cardiovascular/Renal Function
Inform patients and/or caregivers that Cortimax can cause an increase in blood pressure and water retention. If this occurs, dietary salt restriction and potassium supplementation may be needed.
Behavioral and Mood Disturbances
Advise patients and/or caregivers about the potential for severe behavioral and mood changes with Cortimax and encourage them to seek medical attention if psychiatric symptoms develop.
Decreases in Bone Mineral Density
Advise patients and/or caregivers about the risk of osteoporosis with prolonged use of Cortimax, which can predispose the patient to vertebral and long bone fractures.
Ophthalmic Effects
Inform patients and/or caregivers that Cortimax may cause cataracts or glaucoma and advise monitoring if corticosteroid therapy is continued for more than 6 weeks.
Vaccination
Advise patients and/or caregivers to bring immunizations up-to-date according to immunization guidelines prior to starting therapy with Cortimax. Live-attenuated or live vaccines should be administered at least 4 to 6 weeks prior to starting Cortimax. Inform patients and/or caregivers that they may receive concurrent vaccinations with use of Cortimax, except for live-attenuated or live vaccines.
Serious Skin Rashes
Instruct patients and/or caregivers to seek medical attention at the first sign of a rash.
Drug Interactions
Certain medications can cause an interaction with Cortimax. Advise patients and/or caregivers to inform their healthcare provider of all the medicines the patient is taking, including over-the-counter medicines (such as insulin, aspirin or other NSAIDS), dietary supplements, and herbal products. Inform patients and/or caregivers that alternate therapy, dosage adjustment, and/or special test(s) may be needed during the treatment.
About leaflet
Important things you need to know about Cortimax
Cortimax is a steroid medicine. This can be prescribed for many different
conditions, including serious illnesses.
You need to take it regularly to get the maximum benefit.
Do not stop taking this medicine without talking to your doctor - you may need to lower the dose gradually.
Cortimax can cause side effects in some people (read section 4 for more information). These include problems such as mood changes (feeling depressed, or ‘high’), or stomach problems, which can happen straight away. If you feel unwell in any way, keep taking your tablets, but see your doctor straight away.
Some side effects only happen after weeks or months. These include weakness of arms and legs, or developing a rounder face (read section 4 for more information).
If you take it for more than 3 weeks, you will be given a blue ‘steroid card’:
always keep it with you and show it to any doctor or nurse treating you.
Keep away from people who have chickenpox, measles or shingles, if you have never had them. They could affect you severely. If you do come into contact with chickenpox or shingles, see your doctor straight away.
Now read the rest of this leaflet. It includes other important information on the safe and effective use of this medicine that might be especially important for you.
Read all of this leaflet carefully before you start taking this medicine
- Keep this leaflet. You may need to read it again.
- If you have any further questions, please ask your doctor or pharmacist.
- This medicine has been prescribed for you. Do not give it to others. It may harm them, even if their symptoms are the same as yours.
- If any of the side effects gets serious, or if you notice any side effects not listed in this leaflet, please tell your doctor or pharmacist.
- Your doctor may have given you this medicine before from another company. It may have looked slightly different. However, either brand will have the same effect.
In this leaflet:
- What Cortimax is and what it is used for
- Before you take Cortimax
- How to take Cortimax
- Possible side effects
- How to store Cortimax
- Further information
1. What Cortimax is and what it is used for
The name of your medicine is Cortimax 6mg/12mg/24mg/30mg Tablets (called Cortimax throughout this leaflet). Cortimax is a steroid medicine. Their full name is glucocorticoids.
How Cortimax works
- These corticosteroids occur naturally in the body, and help to maintain health and wellbeing.
- Boosting your body with extra corticosteroid (such as Cortimax) is an effective way to treat various illnesses involving inflammation in the body.
- Cortimax works by reducing this inflammation, which could otherwise go on making your condition worse.
- Cortimax also works by stopping reactions known as autoimmune reactions. These reactions happen when your body’s immune system attacks the body itself and causes damage.
- You must take this medicine regularly to get maximum benefit from it.
Cortimax can be used to:
- Treat inflammation including asthma, arthritis and allergies.
- Treat problems with your skin, kidney, heart, digestive system, eyes or blood.
- Suppress the immune system in transplant operations.
2. Before you take Cortimax
Do not take this medicine and tell your doctor if:
- You are allergic (hypersensitive) to deflazacort or any of the other ingredients in these tablets (see Section 6: Further information). Signs of an allergic reaction include: a rash, swallowing or breathing problems, swelling of your lips, face, throat or tongue.
- You have an infection that affects your whole body (systemic infection), which is not already being treated.
- You are having or have recently had any vaccinations with live viruses (see “vaccinations” below).
Do not take this medicine if any of the above apply to you. If you are not sure, talk to your doctor or pharmacist before taking Cortimax.
Take special care and check with your doctor before you take Cortimax if:
- You have ever had severe depression or manic-depression (bipolar disorder). This includes having had depression before while taking steroid medicines like Cortimax.
- Any of your close family has had these illnesses.
- You have or ever had mental problems such as depression or psychoses. If any of the above applies to you, talk to a doctor before taking Cortimax.
Mental problems while taking Cortimax
Mental health problems can happen while taking steroids like Cortimax (see also section 4 Possible Side Effects).
- These illnesses can be serious.
- Usually they start within a few days or weeks of starting the medicine.
- They are more likely to happen at high doses.
- Most of these problems go away if the dose is lowered or the medicine is stopped. However, if problems do happen, they might need treatment.
Talk to a doctor if you (or someone taking this medicine), show any signs of mental problems. This is particularly important if you are depressed, or might be thinking about suicide. In a few cases, mental problems have happened when doses are being lowered or stopped
Check with your doctor before taking this medicine if:
- You have epilepsy (fits).
- You or anyone in your family has diabetes.
- You have high blood pressure.
- You have kidney, liver or heart problems.
- You have brittle or weak bones called osteoporosis.
- You have an eye disease that causes detachment of your retina and bulging eyes.
- You or anyone in your family has an eye problem called glaucoma.
- You have an underactive thyroid gland.
- You have problems with your digestive system, including your food pipe (oesophagitis), gut (ulcerative colitis, diverticulitis) or stomach (peptic ulcer).
- You have ever had a bad reaction such as muscle weakness to any steroid.
- You have or ever had an infection caused by a virus or fungus. This includes infections such as athlete’s foot, thrush and cold sores (that may also affect the eye).
- You have or ever had ‘tuberculosis’ (TB).
- You have any problems with your blood vessels such as a blood clot.
- You have a pheochromocytoma (a tumour of adrenal gland tissue. The adrenal glands are located above the kidneys.).
Cortimax may cause inflammation of tendons and easy tearing especially when given together with antibiotics such as ciprofloxacin.
Irregular periods in women and blood problems such as leukocytosis (increase in white blood cells count) may also occur.
If any of the above apply to you, your doctor may want to see you more often during your treatment. Contact your doctor if you experience blurred vision or other visual disturbances.
Taking other medicines
Please tell your doctor or pharmacist if you are taking or have recently taken any other medicines. This includes medicines you obtain without a prescription, including herbal medicines. This is because Cortimax and other medicines can affect the way some other medicines work.
Some medicines may increase the effects of Cortimax and your doctor may wish to monitor you carefully if you are taking these medicines (including some medicines for HIV: ritonavir, cobicistat). In particular, check with your doctor if you are taking any of the following medicines. Your doctor may want to change the dose of Cortimax, or the other medicine.
- Painkillers such as aspirin.
- Aminoglutethimide - used for some types of cancer.
- Ketoconazole - used to treat infections
- Water tablets (diuretics) such as spironolactone, triamterene or amiloride.
- Medicines for thinning your blood (such as warfarin).
- Medicines for diabetes.
- Medicines for epilepsy such as phenobarbitone, primidone, phenytoin, carbamazepine, acetazolamide.
- Medicines which contain oestrogens including oral contraceptives.
- Medicines for tuberculosis (TB) such as rifampicin or rifabutin.
- Medicines for high blood pressure.
- Medicines for indigestion and heartburn (antacids). If you are taking an antacid leave at least 2 hours between taking it and Cortimax.
- Medicines for asthma such as salbutamol and theophylline.
Vaccinations
If you have just had any injections or vaccinations, tell your doctor before you take Cortimax. If you are going to have any injections or vaccinations, tell your doctor or nurse you are taking Cortimax. This includes those needed for a foreign holiday. Some vaccines should not be given to patients taking Cortimax. This is because Cortimax can affect the way some vaccines work.
Operations
If you are going to have an operation, tell your doctor or nurse you are taking Cortimax. Muscle relaxants are sometimes used during an operation or in intensive care unit. Cortimax and muscle relaxants can affect one another.
Pregnancy and breast-feeding
Talk to your doctor before taking Cortimax if:
- You are pregnant, plan to get pregnant, or think you may be pregnant.
- You are breast-feeding, or planning to breast-feed.
Driving and using machines
These tablets may make you feel dizzy, feel like everything around you is spinning, or feel disorientated (vertigo). If this happens, do not drive or use any tools or machines. Cortimax and infections Taking Cortimax can mean that you get infections more easily than usual, and these infections can be more serious.
Chickenpox, measles or shingles
If you get chickenpox, measles or shingles while taking Cortimax, you can become seriously ill.
- Keep away from people who have chickenpox, measles or shingles, if you have never had them. They could affect you severely. If you do come into contact with chickenpox, measles or shingles, see your doctor straight away. Your doctor may want to give you a vaccination to help you from getting these infections.
- If you do catch Chickenpox, measles or shingles, tell your doctor straight away. Your doctor will advise you on how to take Cortimax. You may be told to increase the number of tablets that you use.
3. How to take Cortimax
Always take Cortimax exactly as your doctor has told you. The dose will depend on the illness being treated and any other medicines you are taking. You should check with your doctor or pharmacist if you are not sure.
Taking this medicine
- Take this medicine by mouth.
- Swallow your tablets whole with a glass of water.
- It is important to take your medicine at the right times.
Adults
- The usual dose for most conditions, including rheumatoid arthritis is half to three tablets each day.
- The dose for severe asthma may be up to 8 or 12 tablets each day. This dose may be gradually reduced once the asthma attack has been controlled.
- For some problems up to 20 tablets may be needed each day for several days.
- Children
- Cortimax may be given every day or every other day.
- The doctor will work out the dose based on your child’s age and weight.
- Your child will be given the lowest possible dose.
- The usual dose for chronic arthritis is between 0.25 mg and 1 mg of the medicine for each kg of your child’s bodyweight, each day. The usual dose for kidney problems (nephrotic syndrome) is 1.5 mg of the medicine for each kg of your child’s bodyweight, each day. Depending on how well the medicine works for your child, this dose may then be slowly lowered.
- The usual dose for asthma is between 0.25 mg and 1 mg of the medicine for each kg of your child’s bodyweight, every other day.
- In infants, an echocardiogram (ultrasound) should be performed by the doctor to monitor the structure and function of the muscular tissue of the heart.
Elderly
Your doctor may need to check you more carefully for side effects.
If you take more Cortimax than you should
Tell your doctor or go to the nearest hospital casualty department straight away. Remember to take with you any tablets that are left and the pack. This is so the doctor knows what you have taken.
If you forget to take Cortimax
If you forget to take a dose take it as soon as you remember, unless it is time for your next dose. Do not take a double dose to make up for a forgotten dose.
Stopping treatment
- You need to take Cortimax regularly to get the maximum benefit.
- Do not stop taking this medicine without talking to your doctor – you may need to lower the dose gradually.
- Stopping the treatment suddenly can sometimes cause problems such as a high temperature, a runny nose, sore, red, sticky eyes, aching muscles and joints, itchy skin and weight loss. Also, sickness (vomiting), headaches and drowsiness – this is more likely to happen in children.
You may also notice the following symptoms if you stop treatment with Cortimax.
If this happens, tell a doctor straight away as these could be signs of a serious illness:
- Sudden, severe pain in the back, stomach and legs.
- Being sick (vomiting) and diarrhoea.
- Feeling faint or dizzy, this could be a sign of low blood pressure.
4. Possible side effects
Like all medicines, Cortimax can cause side effects, although not everybody gets them.
Stop taking your medicine and see a doctor or go to a hospital straight away if:
Uncommon (affects 1 to 10 users in 1,000)
- You get swelling of the hands, feet, ankles, face, lips or throat which may cause difficulty in swallowing or breathing. You could also notice an itchy, lumpy rash (hives) or nettle rash (urticaria). This may mean you are having an allergic reaction to Cortimax.
- You pass black tarry stools or notice fresh or clotted blood in your stools (faeces). You may also notice dark bits that look like coffee grounds in your vomit. These could be signs of a stomach ulcer. Not known (frequency cannot be estimated from the available data)
- You get severe stomach pain which may reach through to your back. This could be a sign of pancreatitis. Serious effects: Tell a doctor straight away if you notice any of the following side effects: Steroids including Cortimax can cause serious mental health problems. These are common in both adults and children. They can affect about 5 in every 100 people taking medicines like Cortimax.
Serious effects: Tell a doctor straight away if you notice any of the following side effects.
Uncommon (affects 1 to 10 users in 1,000)
- Feeling depressed, including thinking about suicide.
Not known (frequency cannot be estimated from the available data)
- Feeling high (mania) or moods that go up and down.
- Feeling anxious, having problems sleeping, difficulty in thinking or being confused and losing your memory.
- Feeling, seeing or hearing things which do not exist. Having strange and frightening thoughts, changing how you act or having feelings of being alone.
- Pheochromocytoma crisis (symptoms can include an awareness of your heart beat, increase in heart rate (palpitations), excessive sweating, high blood pressure, severe headaches or have a tremor (feeling shaky)). Other serious side effects include: Not known (frequency cannot be estimated from the available data)
- A very sore throat. You may also have difficulty in swallowing and the inside of your mouth may have white areas on the surface.
- Headache, which is usually worse in the morning, on coughing or straining, and feeling sick (nausea). Also, fits, fainting, eyesight problems, painful eyes or confusion can occur.
- In infants with a low birth weight a heart muscle disease (hypertrophic cardiomyopathy) may occur. If you notice any of these problems talk to a doctor straight away. Other side effects: Please tell your doctor or pharmacist if any of the following side effects gets serious or lasts longer than a few days.
Uncommon (affects 1 to 10 users in 1,000)
- Stomach or bowel problems such as feeling full or bloated, indigestion, heartburn or stomach pain.
- Increase in appetite and weight gain including around your face. Or, you may lose weight or feel weak.
- Hair, including body or facial hair, grows more than normal.
- Increased thirst and needing to pass water more often than usual. These could be signs of diabetes. If you are already diabetic, your doctor may prescribe more of your diabetes medicine to balance the effects of deflazacort. You should discuss this with your doctor.
- Raised blood pressure and increased water retention.
- Tiredness, confusion, muscle weakness or muscle cramps. This may be due to low levels of potassium in your body.
- Mood changes, difficulty in sleeping.
- If you have had tuberculosis (TB) in the past it may return.
- Skin problems such as acne, appearance of stretch marks.
- You may get infections more easily than usual. Rare (affects 1 to 10 users in 10,000)
- Bleeding under the skin, redness.
- General muscle weakness or tiredness. Not known (frequency cannot be estimated from the available data)
- Bones and tendons may break or tear more easily than usual. Also tendons may get inflamed and become painful.
- Irregular periods in women or they may stop altogether.
- Becoming dependent on deflazacort (also called psychological dependence).
- If you have schizophrenia your symptoms may get worse.
- Fungal infection such as thrush.
- Eye disease that causes detachment of the retina and bulging eyes.
- Eye problems such as glaucoma and cataracts can happen if you take this medicine for a long time.
- Eye infections (viral) may spread or return if you have had them in the past.
- Blurred vision.
- Increase in the risk of clots forming in your blood.
- Blood problems such as leukocytosis.
- Wounds and cuts do not heal as quickly as usual.
- Noticeable blood vessels, thinning of the skin.
- Sudden or severe muscle weakness or tiredness following an operation.
Some of the side effects are more likely to happen if you are elderly. Children and teenagers taking this medicine may grow less than normal. (Not known: frequency cannot be estimated from the available data). If you think this is happening to a child, tell your doctor.
Reporting of side effects
If you get any side effects, talk to your doctor, pharmacist or nurse. This includes any possible side effects not listed in this leaflet. You can also report side effects directly: Website: www.zuventus.com and click the tab “Safety Reporting” located on the top of the home page.
By reporting side effects, you can help provide more information on the safety of this medicine.
You can also report the side effect with the help of your treating physician.
5. How to store Cortimax
Keep out of the sight and reach of children. Store in a dry place at a temperature
not exceeding 25°C.
Do not take this medicine after the expiry date, which is stated on the carton after “EXP”. The expiry date refers to the last day of that month.
Keep it in the pack in which it was given to you. Do not transfer your medicine to another container.
Do not dispose of medicines by flushing down a toilet or a sink or by throwing out with your normal household rubbish. This will help to protect the environment.
6. Further information
What Cortimax contains
10 Strips of 6 tablets in each strips
- Each tablet contains Cortimax 6mg/12mg/24mg/30mg of the active substance, Deflazacort.
For More Information About This Product
Cortimax XL Suspension
1.0 Generic name
Deflazacort Suspension 6 mg/ 5 ml
2.0 Qualitative and quantitative composition
Each 5 ml of suspension contains:
Deflazacort 6 mg
Excipients q.s.
Colour: quinolone yellow
3.0 Dosage form and strength
Oral Suspension, 6 mg/ 5 ml
Cortimax Suspension: a bottle of 30 ml
Cortimax-XL Suspension: a bottle of 60 ml
4.0 Clinical particulars
4.1. Therapeutic indication
For asthma, rheumatoid arthritis when glucocorticosteriod therapy is warranted.
4.2.Posology and method of administration
Deflazacort is a glucocorticoid derived from prednisolone and 6mg of deflazacort has approximately the same anti-inflammatory potency as 5mg prednisolone or prednisone.
Doses vary widely in different diseases and different patients. In more serious and life-threatening conditions, high doses of deflazacort may need to be given. When deflazacort is used long term in relatively benign chronic diseases, the maintenance dose should be kept as low as possible. Dosage may need to be increased during periods of stress or in exacerbation of illness.
The dosage should be individually titrated according to diagnosis, severity of disease and patient response and tolerance. The lowest dose that will produce an acceptable response should be used.
There has been limited exposure of children to deflazacort in clinical trials.
In children, the indications for glucocorticoids are the same as for adults, but it is important that the lowest effective dosage is used. Alternate day administration may be appropriate.
Doses of deflazacort usually lie in the range 0.25 - 1.5 mg/kg/day.
The following ranges provide general guidance:
Juvenile chronic arthritis: usual maintenance dose is between 0.25 - 1.0 mg/kg/day.
Nephrotic syndrome: Initial dose of usually 1.5 mg/kg/day followed by down titration according to clinical need.
Bronchial asthma: On the basis of the potency ratio, the initial dose should be between 0.25 - 1.0 mg/kg deflazacort on alternate days.
Hepatic Impairment
In patients with hepatic impairment, blood levels of deflazacort may be increased. Therefore, the dose of deflazacort should be carefully monitored and adjusted to the minimum effective dose.
Renal Impairment
In renally impaired patients, no special precautions other than those usually adopted in patients receiving glucocorticoid therapy are necessary.
Deflazacort withdrawal
In patients who have received more than physiological doses of systemic corticosteroids (approximately 9 mg/day or equivalent) for > 3 weeks, withdrawal should not be abrupt. How dose reduction should be carried out depends largely on whether the disease is likely to relapse as the dose of systemic corticosteroids is reduced. Clinical assessment of disease activity may be needed during withdrawal. If the disease is unlikely to relapse on withdrawal of systemic corticosteroids but there is uncertainty about HPA suppression, the dose of systemic corticosteroids may be reduced rapidly to physiological doses. Once a daily dose equivalent to 9 mg deflazacort is reached, dose reduction should be slower to allow the HPA-axis to recover.
Abrupt withdrawal of systemic corticosteroid treatment, which has continued up to 3 weeks is appropriate if it is considered that the disease is unlikely to relapse. Abrupt withdrawal of doses up to 48 mg daily of deflazacort, or equivalent for 3 weeks is unlikely to lead to clinically relevant HPA-axis suppression, in the majority of patients. In the following patient groups, gradual withdrawal of systemic corticosteroid therapy should be considered even after courses lasting 3 weeks or less:
- Patients who have had repeated courses of systemic corticosteroids, particularly if taken for greater than 3 weeks.
- When a short course has been prescribed within one year of cessation of long-term therapy (months or years).
- Patients who may have reasons for adrenocortical insufficiency other than exogenous corticosteroid therapy.
- Patients receiving doses of systemic corticosteroid > 48 mg daily of deflazacort (or equivalent),
- Patients repeatedly taking doses in the evening.
4.3. Contraindications
Systemic infection unless specific anti-infective therapy is employed. Hypersensitivity to the active substance, deflazacort or any of the excipients. Patients receiving live virus immunisation.
4.4. Special warnings and precautions for use
Patients with rare hereditary problems of galactose intolerance, the Lapp lactose deficiency or glucose-galactose malabsorption should not take this medicine. Undesirable effects may be minimised by using the lowest effective dose for the minimum period, and by administering the daily requirement as a single morning dose or whenever possible as a single morning dose on alternate days. Frequent patient review is required to appropriately titrate the dose against disease activity.
Adrenal suppression
Adrenal cortical atrophy develops during prolonged therapy and may persist for years after stopping treatment. Withdrawal of corticosteroids after prolonged therapy must therefore always be gradual to avoid acute adrenal insufficiency which could be fatal, being tapered off over weeks or months according to the dose and duration of treatment. During prolonged therapy, any intercurrent illness, trauma or surgical procedure will require a temporary increase in dosage; if corticosteroids have been stopped following prolonged therapy, they may need to be temporarily re-introduced.
Patients should carry 'Steroid treatment' cards which give clear guidance on the precautions to be taken to minimise risk and which provide details of prescriber, drug, dosage and the duration of treatment.
Anti-inflammatory/immunosuppressive effects and infection
Suppression of the inflammatory response and immune function increases the susceptibility to infections and their severity. The clinical presentation may often be atypical and serious infections such as septicaemia and tuberculosis may be masked and may reach an advanced stage before being recognised.
Chickenpox is of particular concern since this normally minor illness may be fatal in immunosuppressed patients. Patients (or parents of children) without a definite history of chicken pox should be advised to avoid close personal contact with chickenpox or herpes zoster and, if exposed, they should seek urgent medical attention. Passive immunisation with varicella zoster immunoglobulin (VZIG) is needed by exposed non-immune patients who are receiving systemic corticosteroids or who have used them within the previous 3 months; this should be given within 10 days of exposure to chickenpox. If a diagnosis of chickenpox is confirmed, the illness warrants specialist care and urgent treatment. Corticosteroids should not be stopped and the dose may need to be increased. Patients should be advised to take particular care to avoid exposure to measles and to seek immediate medical advice if exposure occurs. Prophylaxis with intramuscular normal immunoglobulin may be needed.
Live vaccines should not be given to individuals with impaired responsiveness. The antibody response to other vaccines may be diminished.
Visual disturbance
Visual disturbance may be reported with systemic and topical corticosteroid use. If a patient presents with symptoms such as blurred vision or other visual disturbances, the patient should be considered for referral to an ophthalmologist for evaluation of possible causes which may include cataract, glaucoma or rare diseases such as central serous chorioretinopathy (CSCR) which have been reported after use of systemic and topical corticosteroids.
Prolonged use of glucocorticoids may produce posterior subcapsular cataracts, glaucoma with possible damage to the optic nerves and may enhance the establishment of secondary ocular infections due to fungi or viruses. Use in active tuberculosis should be restricted to those cases of fulminating and disseminated tuberculosis in which deflazacort is used for management with appropriate antituberculosis regimen. If glucocorticoids are indicated in patients with latent tuberculosis or tuberculin reactivity, close observation is necessary as reactivation of the disease may occur. During prolonged glucocorticoid therapy, these patients should receive chemoprophylaxis.
Tendonitis and tendon rupture are known class effect of glucocorticoids. The risk of such reactions may be increased by co-administration of quinolones. Pheochromocytoma crisis, which can be fatal, has been reported after administration of systemic corticosteroids. Corticosteroids should only be administered to patients with suspected or identified pheochromocytoma after an appropriate risk/benefit evaluation.
Special precautions
The following clinical conditions require special caution and frequent patient monitoring is necessary: -
- Cardiac disease or congestive heart failure (except in the presence of active rheumatic carditis), hypertension, thromboembolic disorders. Glucocorticoids can cause salt and water retention and increased excretion of potassium. Dietary salt restriction and potassium supplementation may be necessary.
- Gastritis or oesophagitis, diverticulitis, ulcerative colitis if there is probability of impending perforation, abscess or pyogenic infections, fresh intestinal anastomosis, active or latent peptic ulcer.
- Diabetes mellitus or a family history, osteoporosis, myasthenia gravis, renal insufficiency. • Emotional instability or psychotic tendency, epilepsy.
- Previous corticosteroid-induced myopathy.
- Liver failure.
- Hypothyroidism and cirrhosis, which may increase glucocorticoid effect.
- Ocular herpes simplex because of possible corneal perforation. Patients and/or carers should be warned that potentially severe psychiatric adverse reactions may occur with systemic steroids. Symptoms typically emerge within a few days or weeks of starting the treatment. Risks may be higher with high doses/systemic exposure, although dose levels do not allow prediction of the onset, type, severity or duration of reactions. Most reactions recover after either dose reduction or withdrawal, although specific treatment may be necessary. Patients/carers should be encouraged to seek medical advice if worrying psychological symptoms develop, especially if depressed mood or suicidal ideation is suspected. Patients/carers should also be alert to possible psychiatric disturbances that may occur either during or immediately after dose tapering/withdrawal of systemic steroids, although such reactions have been reported infrequently. Particular care is required when considering the use of systemic corticosteroids in patients with existing or previous history of severe affective disorders in themselves or in their first degree relatives. These would include depressive or manic-depressive illness and previous steroid psychosis. Glucocorticoids are known to cause irregular menstruation and leukocytosis, care should be taken with deflazacort. Paediatric population Corticosteroids cause dose-related growth retardation in infancy, childhood and adolescence which may be irreversible. Hypertrophic cardiomyopathy has been reported after systemic administration of glucocorticosteroids in preterm infants. In infants receiving administration of systemic glucocorticosteroids, echocardiograms should be performed to monitor myocardial structure and function.
4.5.Interaction with other medicinal products and other forms of interaction
- The same precautions should be exercised as for other glucocorticoids. Deflazacort is metabolised in the liver. It is recommended to increase the maintenance dose of deflazacort if drugs which are liver enzyme inducers are co-administered, e.g. rifampicin, rifabutin, carbamazepine, phenobarbitone, phenytoin, primidone and aminoglutethimide. For drugs which inhibit liver enzymes, e.g. ketoconazole it may be possible to reduce the maintenance dose of deflazacort.
- In patients taking estrogens, corticosteroid requirements may be reduced.
- The desired effects of hypoglycaemic agents (including insulin), anti-hypertensives and diuretics are antagonised by corticosteroids and the hypokalaemic effects of acetazolamide, loop diuretics, thiazide diuretics, beta 2-agonists, xanthines and carbenoxolone are enhanced.
- The efficacy of coumarin anticoagulants may be enhanced by concurrent corticosteroid therapy and close monitoring of the INR or prothrombin time is required to avoid spontaneous bleeding.
- In patients treated with systemic corticosteroids, use of non-depolarising muscle relaxants can result in prolonged relaxation and acute myopathy. Risk factors for this include prolonged and high dose corticosteroid treatment, and prolonged duration of muscle paralysis. This interaction is more likely following prolonged ventilation (such as in the ITU setting).
- The renal clearance of salicylates is increased by corticosteroids and steroid withdrawal may result in salicylate intoxication.
- As glucocorticoids can suppress the normal responses of the body to attack by micro-organisms, it is important to ensure that any anti-infective therapy is effective and it is recommended to monitor patients closely. Concurrent use of glucocorticoids and oral contraceptives should be closely monitored as plasma levels of glucocorticoids may be increased. This effect may be due to a change in metabolism or binding to serum proteins. Antacids may reduce bioavailability; leave at least 2 hours between administration of deflazacort and antacids.
- Co-treatment with CYP3A inhibitors, including cobicistat-containing products, is expected to increase the risk of systemic side-effects. The combination should be avoided unless the benefit outweighs the increased risk of systemic corticosteroid side-effects, in which case patients should be monitored for systemic corticosteroid side-effects.
4.6.Fertility, pregnancy and lactation
Pregnancy
The ability of corticosteroids to cross the placenta varies between individual drugs, however, deflazacort does cross the placenta. Administration of corticosteroids to pregnant animals can cause abnormalities of foetal development including cleft palate, intra-uterine growth retardation and effects on brain growth and development. There is no evidence that corticosteroids result in an increased incidence of congenital abnormalities, such as cleft palate/lip in man. However, when administered for prolonged periods or repeatedly during pregnancy, corticosteroids may increase the risk of intra-uterine growth retardation. Hypoadrenalism may, in theory, occur in the neonate following prenatal exposure to corticosteroids but usually resolves spontaneously following birth and is rarely clinically important. As with all drugs, corticosteroids should only be prescribed when the benefits to the mother and child outweigh the risks. When corticosteroids are essential however, patients with normal pregnancies may be treated as though they were in the non-gravid state.
Breast-feeding
Corticosteroids are excreted in breast milk, although no data are available for deflazacort. Doses of up to 50 mg daily of deflazacort are unlikely to cause systemic effects in the infant. Infants of mothers taking higher doses than this may have a degree of adrenal suppression but the benefits of breast feeding are likely to outweigh any theoretical risk.
Fertility
No data is available on Deflazacort and its effects on fertility.
4.7.Effects on ability to drive and use machines
The effect of corticosteroids on the ability to drive or use machinery has not been systematically evaluated. Vertigo is a possible undesirable effect after treatment with deflazacort. If affected, patients should not drive or operate machinery.
4.8.Undesirable effects
The incidence of predictable undesirable effects, including hypothalamic-pituitary-adrenal suppression correlates with the relative potency of the drug, dosage; timing of administration and the duration of treatment.
The following CIOMS frequency rating is used: Very common (≥1/10); common (≥1/100 to <1/10); uncommon (≥1/1000 to <1/100); rare (≥1/10 000 to <1/1000); very rare (<1/10 000), not known (cannot be estimated from the available data).
Endocrine disorders
Uncommon: Suppression of the hypothalamic-pituitary-adrenal axis, amenorrhoea, Cushingoid facies.
Not known: Growth suppression in infancy, childhood and adolescence.
Metabolism and nutrition disorders
Common: Weight gain.
Uncommon: impaired carbohydrate tolerance with increased requirement for anti-diabetic therapy, sodium and water retention with hypertension, potassium loss and hypokalaemic alkalosis when co-administered with beta 2-agonist and xanthines.
Not known: Negative protein and calcium balance, increased appetite.
Infections and Infestations
Uncommon: Increased susceptibility and severity of infections with suppression of clinical symptoms and signs, opportunistic infections, recurrence of dormant tuberculosis.
Not known: candidiasis.
Musculoskeletal and connective tissue disorders
Uncommon: Osteoporosis, vertebral and long bone fractures.
Rare: Muscle wasting.
Not known: avascular osteonecrosis, tendonitis and tendon rupture when co-administered with quinolones, myopathy (acute myopathy may be precipitated by non-depolarising muscle relaxants, negative nitrogen balance.
Reproductive system and breast disorders
Not known: Menstrual irregularity.
Cardiac disorders
Not known: Heart failure, hypertrophic cardiomyopathy in preterm infants.
Nervous system disorders
Uncommon: Headache, vertigo.
Not known: restlessness, Increased intra-cranial pressure with papilloedema in children (pseudotumour cerebri), usually after treatment withdrawal, aggravation of epilepsy.
Psychiatric disorders
A wide range of psychiatric reactions including affective disorders such as:
Uncommon: depressed and labile mood.
Not known: irritable, euphoric, suicidal thoughts.
Psychotic reactions including:
Not known: mania, delusions, hallucinations, aggravation of schizophrenia
Other reactions including:
Uncommon: behavioural disturbances.
Not known: anxiety, sleep disturbances, and cognitive dysfunction including confusion and amnesia have been reported.
Reactions are common and may occur in both adults and children. In adults, the frequency of severe reactions has been estimated to be 5-6%. Psychological effects have been reported on withdrawal of corticosteroids; the frequency is unknown.
Eye disorders
Not known: Vision blurred, increased intra-ocular pressure, glaucoma, papilloedema, posterior subcapsular cataracts especially in children, chorioretinopathy, corneal or scleral thinning, exacerbation of ophthalmic viral or fungal diseases.
Gastrointestinal disorders
Uncommon: Dyspepsia, peptic ulceration, haemorrhage, nausea.
Not known: perforation of peptic ulcer, acute pancreatitis (especially in children), candidiasis.
Skin and subcutaneous tissue disorders
Uncommon: hirsutism, striae, acne.
Rare: bruising.
Not known: Skin atrophy, telangiectasia.
General disorders and administration site conditions
Uncommon: Oedema.
Not known: impaired healing.
Immune system disorders
Uncommon: Hypersensitivity including anaphylaxis has been reported.
Blood and lymphatic system disorders
Not known: Leukocytosis.
Vascular disorders
Not known: Thromboembolism in particular in patients with underlying conditions associated with increased thrombotic tendency, rare incidence of benign intracranial hypertension.
Withdrawal symptoms and signs
Not known: Too rapid a reduction of corticosteroid dosage following prolonged treatment can lead to acute adrenal insufficiency, hypotension and death.
A 'withdrawal syndrome' may also occur including fever, myalgia, arthralgia, rhinitis, conjunctivitis, painful itchy skin nodules and loss of weight. This may occur in patients even without evidence of adrenal insufficiency.
Class effect
Pheochromocytoma crisis has been reported with other systemic corticosteroids and is a known class effect.
Reporting of suspected adverse reactions
Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via email to: medico@zuventus.com
Website: https://www.zuventus.com/drug-safety-reporting
By reporting side effects, you can help provide more information on the safety of this medicine.
4.9. Overdose
It is unlikely that treatment is needed in cases of acute overdosage. The LD50 for the oral dose is greater than 4000 mg/kg in laboratory animals.
5.0 Pharmacological properties
5.1 Pharmacodynamic properties
Pharmacotherapeutic group: corticosteroids for systemic use; Glucocorticoids.
ATC code: H02AB13.
Deflazacort is a glucocorticoid. Its anti-inflammatory and immunosuppressive effects are used in treating a variety of diseases and are comparable to other anti-inflammatory steroids. Clinical studies have indicated that the average potency ratio of deflazacort to prednisolone is 0.69-0.89.
5.2 Pharmacokinetic properties
Absorption: Orally administered deflazacort appears to be well absorbed.
Distribution: The active metabolite D 21-OH achieves peak plasma concentrations in 1.5 to 2 hours. It is 40% protein-bound and has no affinity for corticosteroid-binding-globulin (transcortin).
Biotransformation: Orally administered deflazacort is immediately converted by plasma esterases to the pharmacologically active metabolite (D 21-OH). Metabolism of D 21-OH is extensive. The metabolite of D 21-OH is deflazacort 6-beta-OH.
Elimination: Its elimination plasma half-life is 1.1 to 1.9 hours. Elimination takes place primarily through the kidneys; 70% of the administered dose is excreted in the urine. The remaining 30% is eliminated in the faeces. Metabolism of D 21-OH is extensive; only 18% of urinary excretion represents D 21-OH. The metabolite of D 21-OH, deflazacort 6-beta-OH, represents one third of the urinary elimination.
6.0 Nonclinical properties
Safety studies have been carried out in the rat, dog, mouse and monkey. The findings are consistent with other glucocorticoids at comparable doses. Teratogenic effects demonstrated in rodents and rabbits are typical of those caused by other glucocorticoids. Deflazacort was not found to be carcinogenic in the mouse, but studies in the rat produced carcinogenic findings consistent with the findings with other glucocorticoids.
7.0 Description
Deflazacort, is an oxaline derivative of Prednisolone.
Figure: Structure of Deflazacort
IUPAC Name: (11β,16β)-21-(acetyloxy)-11-hydroxy-2'-methyl-5'H-pregna-1,4-dieno[17,16-d]oxazole-3,20-dione Molecular Formula: C25H31NO6
Molecular Weight: 441.5 g/mol
8.0 Pharmaceutical Particulars
1.Incompatibilities
Not applicable.
2.Shelf-life
Refer on pack
3.Packaging information
Cortimax Suspension: a bottle of 30 ml
Cortimax-XL Suspension: a bottle of 60 ml
4. Storage and handing instructions
- Keep out of reach of children. Keep out of the sight and reach of children.
- Store in a dry place at a temperature not exceeding 25°C.
9.0 Patient counselling information
A patient information leaflet is available for this product.
Administration
- Warn patients and/or caregivers to not stop taking Cortimax abruptly or without first checking with their healthcare providers as there may be a need for gradual dose reduction to decrease the risk of adrenal insufficiency.
- Cortimax may be taken with or without food. Do not take Cortimax with grapefruit juice.
Increased Risk of Infection
Tell patients and/or caregivers to inform their healthcare provider if the patient has had recent or ongoing infections or if they have recently received a vaccine. Medical advice should be sought immediately if the patient develops fever or other signs of infection. Patients and/or caregivers should be made aware that some infections can potentially be severe and fatal. Warn patients who are on corticosteroids to avoid exposure to chickenpox or measles and to alert their healthcare provider immediately if they are exposed.
Alterations in Cardiovascular/Renal Function
Inform patients and/or caregivers that Cortimax can cause an increase in blood pressure and water retention. If this occurs, dietary salt restriction and potassium supplementation may be needed.
Behavioural and Mood Disturbances
Advise patients and/or caregivers about the potential for severe behavioral and mood changes with Cortimax and encourage them to seek medical attention if psychiatric symptoms develop.
Decreases in Bone Mineral Density
Advise patients and/or caregivers about the risk of osteoporosis with prolonged use of Cortimax, which can predispose the patient to vertebral and long bone fractures.
Ophthalmic Effects
Inform patients and/or caregivers that Cortimax may cause cataracts or glaucoma and advise monitoring if corticosteroid therapy is continued for more than 6 weeks.
Vaccination
Advise patients and/or caregivers to bring immunizations up-to-date according to immunization guidelines prior to starting therapy with Cortimax. Live-attenuated or live vaccines should be administered at least 4 to 6 weeks prior to starting Cortimax. Inform patients and/or caregivers that they may receive concurrent vaccinations with use of Cortimax, except for live-attenuated or live vaccines.
Serious Skin Rashes
Instruct patients and/or caregivers to seek medical attention at the first sign of a rash.
Drug Interactions
Certain medications can cause an interaction with Cortimax. Advise patients and/or caregivers to inform their healthcare provider of all the medicines the patient is taking, including over-the-counter medicines (such as insulin, aspirin or other NSAIDS), dietary supplements, and herbal products. Inform patients and/or caregivers that alternate therapy, dosage adjustment, and/or special test(s) may be needed during the treatment.
About Leaflet
Important things you need to know about Cortimax
- Cortimax is a steroid medicine. This can be prescribed for many different conditions, including serious illnesses.
- You need to take it regularly to get the maximum benefit.
- Do not stop taking this medicine without talking to your doctor - you may need to lower the dose gradually.
- Cortimax can cause side effects in some people (read section 4 for more information). These include problems such as mood changes (feeling depressed, or ‘high’), or stomach problems, which can happen straight away. If you feel unwell in any way, keep taking your Cortimax Suspension, but see your doctor straight away.
- Some side effects only happen after weeks or months. These include weakness of arms and legs, or developing a rounder face (read section 4 for more information).
- If you take it for more than 3 weeks, you will be given a blue ‘steroid card’: always keep it with you and show it to any doctor or nurse treating you.
- Keep away from people who have chickenpox, measles or shingles, if you have never had them. They could affect you severely. If you do come into contact with chickenpox or shingles, see your doctor straight away. Now read the rest of this leaflet. It includes other important information on the safe and effective use of this medicine that might be especially important for you.
Read all of this leaflet carefully before you start taking this medicine
- Keep this leaflet. You may need to read it again.
- If you have any further questions, please ask your doctor or pharmacist.
- This medicine has been prescribed for you. Do not give it to others. It may harm them, even if their symptoms are the same as yours.
- If any of the side effects gets serious, or if you notice any side effects not listed in this leaflet, please tell your doctor or pharmacist.
- Your doctor may have given you this medicine before from another company. It may have looked slightly different. However, either brand will have the same effect.
In this leaflet:
- What Cortimax is and what it is used for
- Before you take Cortimax
- How to take Cortimax
- Possible side effects
- How to store Cortimax
- Further information
1. What Cortimax is and what it is used for
The name of your medicine is Cortimax Suspension/Cortimax-XL Suspension (called Cortimax throughout this leaflet). Cortimax is a steroid medicine. Their full name is glucocorticoids.
How Cortimax works
- These corticosteroids occur naturally in the body, and help to maintain health and wellbeing.
- Boosting your body with extra corticosteroid (such as Cortimax) is an effective way to treat various illnesses involving inflammation in the body.
- Cortimax works by reducing this inflammation, which could otherwise go on making your condition worse.
- Cortimax also works by stopping reactions known as autoimmune reactions. These reactions happen when your body’s immune system attacks the body itself and causes damage.
- You must take this medicine regularly to get maximum benefit from it.
Cortimax can be used to:
- Treat inflammation including asthma, arthritis and allergies.
- Treat problems with your skin, kidney, heart, digestive system, eyes or blood.
- Suppress the immune system in transplant operations.
2. Before you take Cortimax
Do not take this medicine and tell your doctor if:
- You are allergic (hypersensitive) to deflazacort or any of the other ingredients in these Suspension (see Section 6: Further information). Signs of an allergic reaction include: a rash, swallowing or breathing problems, swelling of your lips, face, throat or tongue.
- You have an infection that affects your whole body (systemic infection), which is not already being treated.
- You are having or have recently had any vaccinations with live viruses (see “vaccinations” below).
Do not take this medicine if any of the above apply to you. If you are not sure, talk to your doctor or pharmacist before taking Cortimax.
Take special care and check with your doctor before you take Cortimax if:
- You have ever had severe depression or manic-depression (bipolar disorder). This includes having had depression before while taking steroid medicines like Cortimax.
- Any of your close family has had these illnesses.
- You have or ever had mental problems such as depression or psychoses. If any of the above applies to you, talk to a doctor before taking Cortimax.
Mental problems while taking Cortimax
Mental health problems can happen while taking steroids like Cortimax (see also section 4
Possible Side Effects).
- These illnesses can be serious.
- Usually they start within a few days or weeks of starting the medicine.
- They are more likely to happen at high doses.
- Most of these problems go away if the dose is lowered or the medicine is stopped. However, if problems do happen, they might need treatment. Talk to a doctor if you (or someone taking this medicine), show any signs of mental problems. This is particularly important if you are depressed, or might be thinking about suicide. In a few cases, mental problems have happened when doses are being lowered or stopped
Check with your doctor before taking this medicine if:
- You have epilepsy (fits).
- You or anyone in your family has diabetes.
- You have high blood pressure.
- You have kidney, liver or heart problems.
- You have brittle or weak bones called osteoporosis.
- You have an eye disease that causes detachment of your retina and bulging eyes.
- You or anyone in your family has an eye problem called glaucoma.
- You have an underactive thyroid gland.
- You have problems with your digestive system, including your food pipe (oesophagitis), gut (ulcerative colitis, diverticulitis) or stomach (peptic ulcer).
- You have ever had a bad reaction such as muscle weakness to any steroid.
- You have or ever had an infection caused by a virus or fungus. This includes infections such as athlete’s foot, thrush and cold sores (that may also affect the eye).
- You have or ever had ‘tuberculosis’ (TB).
- You have any problems with your blood vessels such as a blood clot.
- You have a pheochromocytoma (a tumour of adrenal gland tissue. The adrenal glands are located above the kidneys.).
Cortimax may cause inflammation of tendons and easy tearing especially when given together with antibiotics such as ciprofloxacin.
Irregular periods in women and blood problems such as leukocytosis (increase in white blood cells count) may also occur.
If any of the above apply to you, your doctor may want to see you more often during your treatment. Contact your doctor if you experience blurred vision or other visual disturbances.
Taking other medicines
Please tell your doctor or pharmacist if you are taking or have recently taken any other medicines. This includes medicines you obtain without a prescription, including herbal medicines. This is because Cortimax and other medicines can affect the way some other medicines work.
Some medicines may increase the effects of Cortimax and your doctor may wish to monitor you carefully if you are taking these medicines (including some medicines for HIV: ritonavir, cobicistat). In particular, check with your doctor if you are taking any of the following medicines. Your doctor may want to change the dose of Cortimax, or the other medicine.
- Painkillers such as aspirin.
- Aminoglutethimide - used for some types of cancer.
- Ketoconazole - used to treat infections
- Water tablets (diuretics) such as spironolactone, triamterene or amiloride.
- Medicines for thinning your blood (such as warfarin).
- Medicines for diabetes.
- Medicines for epilepsy such as phenobarbitone, primidone, phenytoin, carbamazepine, acetazolamide.
- Medicines which contain oestrogens including oral contraceptives.
- Medicines for tuberculosis (TB) such as rifampicin or rifabutin.
- Medicines for high blood pressure.
- Medicines for indigestion and heartburn (antacids). If you are taking an antacid leave at least 2 hours between taking it and Cortimax.
- Medicines for asthma such as salbutamol and theophylline.
Vaccinations
If you have just had any injections or vaccinations, tell your doctor before you take Cortimax. If you are going to have any injections or vaccinations, tell your doctor or nurse you are taking Cortimax. This includes those needed for a foreign holiday. Some vaccines should not be given to patients taking Cortimax. This is because Cortimax can affect the way some vaccines work.
Operations
If you are going to have an operation, tell your doctor or nurse you are taking Cortimax. Muscle relaxants are sometimes used during an operation or in intensive care unit. Cortimax and muscle relaxants can affect one another.
Pregnancy and breast-feeding
Not applicable.
Driving and using machines
Not applicable.
Chickenpox, measles or shingles
If you get chickenpox, measles or shingles while taking Cortimax, you can become seriously ill.
- Keep away from people who have chickenpox, measles or shingles, if you have never had them. They could affect you severely. If you do come into contact with chickenpox, measles or shingles, see your doctor straight away. Your doctor may want to give you a vaccination to help you from getting these infections.
- If you do catch Chickenpox, measles or shingles, tell your doctor straight away. Your doctor will advise you on how to take Cortimax.
3. How to take Cortimax
Always take Cortimax exactly as your doctor has told you. The dose will depend on the illness being treated and any other medicines you are taking. You should check with your doctor or pharmacist if you are not sure.
Taking this medicine
- Take this medicine by mouth. It is important to take your medicine at the right times.
Children
- Cortimax may be given every day or every other day.
- The doctor will work out the dose based on your child’s age and weight.
- Your child will be given the lowest possible dose.
- The usual dose for chronic arthritis is between 0.25 mg and 1 mg of the medicine for each kg of your child’s bodyweight, each day. The usual dose for kidney problems (nephrotic syndrome) is 1.5 mg of the medicine for each kg of your child’s bodyweight, each day. Depending on how well the medicine works for your child, this dose may then be slowly lowered.
- The usual dose for asthma is between 0.25 mg and 1 mg of the medicine for each kg of your child’s bodyweight, every other day.
- In infants, an echocardiogram (ultrasound) should be performed by the doctor to monitor the structure and function of the muscular tissue of the heart.
If you take more Cortimax than you should
Tell your doctor or go to the nearest hospital casualty department straight away. Remember to take with you bottle that are left and the pack. This is so the doctor knows what you have taken.
If you forget to take Cortimax
If you forget to take a dose take it as soon as you remember, unless it is time for your next dose. Do not take a double dose to make up for a forgotten dose.
Stopping treatment
- You need to take Cortimax regularly to get the maximum benefit.
- Do not stop taking this medicine without talking to your doctor – you may need to lower the dose gradually.
- Stopping the treatment suddenly can sometimes cause problems such as a high temperature, a runny nose, sore, red, sticky eyes, aching muscles and joints, itchy skin and weight loss. Also, sickness (vomiting), headaches and drowsiness – this is more likely to happen in children.
You may also notice the following symptoms if you stop treatment with Cortimax.
If this happens, tell a doctor straight away as these could be signs of a serious illness:
- Sudden, severe pain in the back, stomach and legs.
- Being sick (vomiting) and diarrhoea.
- Feeling faint or dizzy, this could be a sign of low blood pressure.
4. Possible side effects
Like all medicines, Cortimax can cause side effects, although not everybody gets them.
Stop taking your medicine and see a doctor or go to a hospital straight away if:
Uncommon (affects 1 to 10 users in 1,000)
- You get swelling of the hands, feet, ankles, face, lips or throat which may cause difficulty in swallowing or breathing. You could also notice an itchy, lumpy rash (hives) or nettle rash (urticaria). This may mean you are having an allergic reaction to Cortimax.
- You pass black tarry stools or notice fresh or clotted blood in your stools (faeces). You may also notice dark bits that look like coffee grounds in your vomit. These could be signs of a stomach ulcer. Not known (frequency cannot be estimated from the available data)
- You get severe stomach pain which may reach through to your back. This could be a sign of pancreatitis. Serious effects: Tell a doctor straight away if you notice any of the following side effects:
Steroids including Cortimax can cause serious mental health problems. These are common in both adults and children. They can affect about 5 in every 100 people taking medicines like Cortimax.
Serious effects: Tell a doctor straight away if you notice any of the following side effects.
Uncommon (affects 1 to 10 users in 1,000)
- You get swelling of the hands, feet, ankles, face, lips or throat which may cause difficulty in swallowing or breathing. You could also notice an itchy, lumpy rash (hives) or nettle rash (urticaria). This may mean you are having an allergic reaction to Cortimax.
- You pass black tarry stools or notice fresh or clotted blood in your stools (faeces). You may also notice dark bits that look like coffee grounds in your vomit. These could be signs of a stomach ulcer.
Not known (frequency cannot be estimated from the available data)
- You get severe stomach pain which may reach through to your back. This could be a sign of pancreatitis.
Serious effects: Tell a doctor straight away if you notice any of the following side effects:
Steroids including Cortimax can cause serious mental health problems. These are common in both adults and children. They can affect about 5 in every 100 people taking medicines like Cortimax.
Serious effects: Tell a doctor straight away if you notice any of the following side effects.
Uncommon (affects 1 to 10 users in 1,000)
- Feeling depressed, including thinking about suicide.
Not known (frequency cannot be estimated from the available data)
- Feeling high (mania) or moods that go up and down.
- Feeling anxious, having problems sleeping, difficulty in thinking or being confused and losing your memory.
- Feeling, seeing or hearing things which do not exist. Having strange and frightening thoughts, changing how you act or having feelings of being alone.
- Pheochromocytoma crisis (symptoms can include an awareness of your heart beat, increase in heart rate (palpitations), excessive sweating, high blood pressure, severe headaches or have a tremor (feeling shaky)). Other serious side effects include: Not known (frequency cannot be estimated from the available data)
- A very sore throat. You may also have difficulty in swallowing and the inside of your mouth may have white areas on the surface.
- Headache, which is usually worse in the morning, on coughing or straining, and feeling sick (nausea). Also, fits, fainting, eyesight problems, painful eyes or confusion can occur.
- In infants with a low birth weight a heart muscle disease (hypertrophic cardiomyopathy) may occur. If you notice any of these problems talk to a doctor straight away.
- Other side effects: Please tell your doctor or pharmacist if any of the following side effects gets serious or lasts longer than a few days. Uncommon (affects 1 to 10 users in 1,000)
- Stomach or bowel problems such as feeling full or bloated, indigestion, heartburn or stomach pain.
- Increase in appetite and weight gain including around your face. Or, you may lose weight or feel weak.
- Hair, including body or facial hair, grows more than normal.
- Increased thirst and needing to pass water more often than usual. These could be signs of diabetes. If you are already diabetic, your doctor may prescribe more of your diabetes medicine to balance the effects of deflazacort. You should discuss this with your doctor.
- Raised blood pressure and increased water retention.
- Tiredness, confusion, muscle weakness or muscle cramps. This may be due to low levels of potassium in your body.
- Mood changes, difficulty in sleeping.
- If you have had tuberculosis (TB) in the past it may return.
- Skin problems such as acne, appearance of stretch marks.
- You may get infections more easily than usual. Rare (affects 1 to 10 users in 10,000)
- Bleeding under the skin, redness.
- General muscle weakness or tiredness. Not known (frequency cannot be estimated from the available data)
- Bones and tendons may break or tear more easily than usual. Also tendons may get inflamed and become painful.
- Irregular periods in women or they may stop altogether.
- Becoming dependent on deflazacort (also called psychological dependence).
- If you have schizophrenia your symptoms may get worse.
- Fungal infection such as thrush.
- Eye disease that causes detachment of the retina and bulging eyes.
- Eye problems such as glaucoma and cataracts can happen if you take this medicine for a long time.
- Eye infections (viral) may spread or return if you have had them in the past.
- Blurred vision.
- Increase in the risk of clots forming in your blood.
- Blood problems such as leukocytosis.
- Wounds and cuts do not heal as quickly as usual.
- Noticeable blood vessels, thinning of the skin.
- Sudden or severe muscle weakness or tiredness following an operation.
Some of the side effects are more likely to happen if you are elderly.
Children and teenagers taking this medicine may grow less than normal.
(Not known: frequency cannot be estimated from the available data). If you think this is happening to a child, tell your doctor.
Reporting of side effects
If you get any side effects, talk to your doctor, pharmacist or nurse. This includes any possible side effects not listed in this leaflet. You can also report side effects directly: Website: www.zuventus.com and click the tab “Drug Safety Reporting” located on the top of the home page.
By reporting side effects, you can help provide more information on the safety of this medicine.
You can also report the side effect with the help of your treating physician.
5. How to store Cortimax
- Keep out of the sight and reach of children. Store in a dry place at a temperature
- not exceeding 25°C.
- Do not take this medicine after the expiry date, which is stated on the carton after “EXP”. The expiry date refers to the last day of that month.
- Keep it in the pack in which it was given to you. Do not transfer your medicine to another container.
- Do not dispose of medicines by flushing down a toilet or a sink or by throwing out with your normal household rubbish. This will help to protect the environment.
6. Further information
What Cortimax contains
Cortimax Suspension or Cortimax-XL suspension contains 6 mg of the active substance, Deflazacort.
Cortimax Suspension: a bottle of 30 ml
Cortimax-XL Suspension: a bottle of 60 ml
For More Information About This Product
Soventus DC Syrup
1.0 Generic Name
Levocloperastine Fendizoate Oral Suspension
2.0 Qualitative and quantitative composition
Each 5 ml oral suspension contains:
Levocloperastine Fendizoate 35.4 mg (equivalent to 20 mg of Levocloperastine Hydrochloride)
Excipients q.s.
In a flavoured syrup base
Colour: Sunset Yellow FCF
Flavour: Mango
3.0 Dosage form and strength
Oral suspension
20mg of Levocloperastine per 5ml
4.0 Clinical particulars
4.1 Therapeutic Indication
For the treatment of non-productive cough in adult patients
4.2 Posology and method of administration
Dose for Adults: 5 ml (20mg) three times daily.
4.3 Contraindications
- Known hypersensitivity to cloperastine or to any of the excipients.
- It should not be used in children under 2 years of age.
- Pregnant or breast-feeding women.
- Known hypersensitivity to antihistaminic agents.
- Patients receiving concomitant treatment with MAO inhibitors.
- Patients with hereditary fructose intolerance, glucose or galactose malabsorption, or sucrose isomaltase deficiency.
- Consumption of Alcohol is strictly contraindicated with Levocloperastine suspension.
4.4 Special warnings and precautions for use
Caution should be observed while prescribing Levocloperastine Fendizoate suspension to adults and children with hypertension, cardiovascular disease, uncontrolled diabetes mellitus, hyperthyroidism, seizures or in patients who are unusually hypersensitive to sympathomimetic amines.
Due to its mild anticholinergic activity, cloperastine should be administered with caution in patients with intraocular hypertension, narrow-angle glaucoma, prostatic hypertrophy, urine retention, hypertension, cardiac arrhythmia, myasthenia gravis, stenosing peptic ulcer or bowel obstruction affecting the oesophagus, intestine or bladder.
Persistent cough.
Caution is recommended in patients with chronic cough such as smoker's cough, pulmonary emphysema or asthma, as it inhibits the cough reflex and could therefore alter expectoration and increase airway resistance.
4.5 Drugs interactions
Levocloperastine Fendizoate suspension should not be concomitantly prescribed with sedatives or tranquilizers. Similarly, other antihistamine drugs should not be prescribed concomitantly.
As it has some antihistaminic activity, cloperastine can enhance the sedative effect of CNS
depressors such as anxiolytics, antipsychotic drugs, barbiturates, hypnotics, narcotics, sedatives, tranquilizers, some analgesics and alcohol.
Also due to this activity, cloperastine, antihistaminic agents and anticholinergic drugs (anti-parkinson's drugs, tricyclic antidepressants, MAO inhibitors, neuroleptic agents) can reciprocally increase their effects.
Expectorants and mucolytic drugs: Inhibition of the cough reflex could give rise to pulmonary obstruction in case of elevated volume or fluidity of bronchial secretions.
4.6 Use in special populations
Animal studies have not shown any evidence of damage to the foetus. In humans, its safety for use in pregnancy and lactation has not been established. Cloperastine should therefore not be used during pregnancy unless a doctor believes that the treatment's potential benefit for the mother exceeds all risks for the developing foetus or infant. As it is unknown whether the drug is excreted in human milk, its use during lactation is not recommended.
4.7 Effects on ability to drive and use machines
Levocloperastine can cause drowsiness, so caution is recommended when driving or using dangerous machinery. If drowsiness is noted at normal doses of cloperastine, do not drive or handle dangerous machinery.
4.8 Undesirable effects
Levocloperastine can produce minor and transient adverse reactions such as Dry mouth, GI effects, exhaustion, fainting, somnolence, sedation, clouding of consciousness, numbness, dizziness, headache, palpitations and allergic reaction.

Reporting of suspected adverse reactions
Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via email to:medico@zuventus.com
Website: https://www.zuventus.co.in/drug-safety-reporting
By reporting side effects, you can help provide more information on the safety of this medicine.
4.9 Overdose
No cases of overdose have been reported.
Intoxication can occur after ingesting quantities that are much higher than the therapeutic doses.
Overdose could cause symptoms such as drowsiness, anticholinergic symptoms, hallucinations, excitation, ataxia, lack of motor coordination and convulsions. In case of overdose, symptomatic and maintenance treatment is recommended. Vomiting should be induced or stomach lavage should be performed with saline serum.
5.0 Pharmacological properties
5.1 Mechanism of action
Levocloperastine is a cough suppressant. Levocloperastine is a novel antitussive agent having dual mechanism of action, it acts on both the central bulbar cough centre and on peripheral receptors in the tracheobronchial tree.
As demonstrated in a number of animal models, Levocloperastine acts at the CNS level by inhibiting the bulbar cough centre. In addition to this primary mechanism of action, peripheral effects related to its antihistamine, anti-serotonergic and smooth muscle-relaxant properties also contribute to the overall efficacy of Levocloperastine in the treatment of cough, bronchospasm and related symptoms.
5.2 Pharmacodynamic properties
The therapeutic efficacy of DL-cloperastine in reducing the intensity and frequency of cough is well established, with efficacy similar to that of codeine and superior to that of dextromethorphan.
In clinical trials, levocloperastine had a faster onset of action and produced greater reductions in the intensity and frequency of cough compared with DL-cloperastine, codeine and levodropropizine.
The antitussive effects (reduction in intensity and frequency of cough) of levocloperastine were observed after the first day of treatment in patients of all ages. In children, levocloperastine reduced night-time awakenings and irritability; in adults, it was also effective in treating ACE inhibitor cough.
Levocloperastine was generally well tolerated. There was no evidence of clinically significant central adverse events, whereas drowsiness, dry mouth and nausea were reported with comparator agents (levodropropizine, codeine, DL-cloperastine).
Levocloperastine represents an effective alternative to currently used antitussive agents with the added advantage of faster onset of action and improved tolerability in all patient groups.
5.3 Pharmacokinetic properties
The product is absorbed from the gastrointestinal tract and mostly excreted in urine.
After administration of 10ml of oral suspension containing levocloperastine fendizoate, peak plasma concentrations of 10 μg/L were reached 2 to 4 hours after administration, with a lag-time of approximately 45 minutes before detection of the drug in the bloodstream, suggesting a gradual and protracted absorption from the intestine.
Oral bioavailability was >40% based on the ratio of area under the plasma concentrationtime curve (AUC) of unmodified drug calculated after oral and intravenous administration, while substantially higher values were obtained in excretion studies conducted with radiolabelling techniques (14C).
The half-life of levocloperastine is 0.80 hours (distribution half-life), 1.68 hours (elimination half-life), and 6.58 hours (terminal elimination half-life). The volumes of distribution (Vd) were found to be 80 ml/kg (terminal) and 57 ml/kg (at steady state), and the protein-bound fraction was high. Total body clearance was 7.5 L/hour.
6.0 Nonclinical properties
In preclinical studies, levocloperastine demonstrated antitussive effects similar to those observed with codeine. In acute and repeated-dose toxicity studies, levocloperastine was well tolerated in rodents and dogs, with no clinically significant cardiovascular or gastrointestinal adverse events. The pharmacokinetic behaviour of levocloperastine, best described by a two-compartmental model with absorption phase, is similar to that of the racemic compound DL-cloperastine.
Administration of levocloperastine 1 to 9 mg/kg to guinea pigs dose-dependently inhibited cough induced by citric acid or ammonia vapour, showing an antitussive effect similar to that of codeine. The 50% effective dose (ED50) values for levocloperastine vs codeine were, respectively, 2.6 vs 3.6 mg/kg in the citric acid test, and 2.9 vs 3.1 mg/kg in the ammonia test. Activities of levocloperastine, DL-cloperastine and dextrocloperastine were similar in the citric acid-induced cough model, suggesting that the antitussive efficacy of cloperastine compounds is independent of their enantiomeric structure.
Levocloperastine (as well as dextrocloperastine and DL-cloperastine) exhibited spasmolytic activity in guinea-pigs via its antihistamine properties in vitro (inhibition of histamine-induced contraction in isolated tracheal rings) and in vivo (dose-dependent inhibition of bronchospasm induced by histamine aerosol). Similarly, serotonin-antagonist activity was demonstrated in vitro.
Unlike opioid antitussives, such as codeine, the CNS activity of levocloperastine is highly selective for the cough centre, thus avoiding central adverse effects such as sedation. This attenuation of CNS adverse effects is a differential feature of levocloperastine and is related to its specific stereoisomeric properties, since dextrocloperastine and DL-cloperastine, administered orally or intraperitoneally, induced sedative and stimulant effects of much greater magnitude (by approximately 50%) in tests of CNS function in rodents.
Both acute and repeated-dose toxicity studies found levocloperastine to be well tolerated in rodents and dogs. The 50% lethal dose (LD50) value of levocloperastine could not be calculated because the oral/intraperitoneal doses tested (up to 2000 mg/kg) did not cause death in any of the experimental animals. By comparison, the enantiomer dextrocloperastine was more toxic, with LD50 values of 466 mg/kg in the mouse and 1226 mg/kg in the rat after oral administration, and 155 and 177 mg/kg, respectively, after intraperitoneal administration.
In chronic toxicity studies, levocloperastine at dosages up to 75 mg/kg/day (corresponding to 45 times the therapeutic daily dosage in humans) for 6 months was considered 'safe' in rats and dogs. Mild adverse events (including vomiting, anorexia and transient biochemical/ histological signs of liver and kidney dysfunction) were observed only with dosages of 250 mg/kg/day following 6 months' treatment. Levocloperastine did not show mutagenic or carcinogenic effects in specific in vitro and in vivo studies.
7.0 Description
Levocloperastine, the levorotatory isomer of DLcloperastine, is a centrally active, non-opioid antitussive agent with a chemical structure and pharmacological profile distinct from that of the racemate. It is devoid of central antinociceptive activities, does not cause addiction or dependence phenomena, and does not interfere with cardiovascular or gastrointestinal functions.
Cloperastine fendizoate is a N-oxyethylpiperidine. It is functionally related to a benzoate.

Structure of Cloperastine fendizoate
Molecular Formula: C40H38ClNO5
Molecular Weight: 648.2 g/mol
8.0 Pharmaceutical particulars
8.1 Incompatibilities
None known.
8.2 Shelf-life
Refer on the pack.
8.3 Packaging information
A bottle of 100 ml.
8.4 Storage and handing instructions
Store in a cool place. Protect from light. Keep out of reach of children. Shake well before each use.
9.0 Patient Counselling Information
- You have been prescribed Soventus-DC Oral Suspension for the symptomatic relief of dry cough.
- It is usually taken for a short time, until the symptoms clear up.
- Measure the syrup with a special dose-measuring spoon or cup, not a regular table spoon.
- Drink extra fluids to help loosen the congestion and lubricate your throat while you are taking this medication.
- It should not be administered to patients with chronic cough or where cough is accompanied by excessive secretions.
- Inform your doctor if your cough lasts more than 7 days, comes back, or occurs with fever, rash or headache. These could be signs of a serious condition.
12.0 Date of revision of text
19-09-2024
Read all of this leaflet carefully before you start taking this medicine because it contains important information for you.
- Keep this leaflet. You may need to read it again.
- If you have any further questions, ask your doctor or pharmacist.
- This medicine has been prescribed for you only. Do not pass it on to others. It may harm them, even if their signs of illness are the same as yours.
- If you get any side effects, talk to your doctor or pharmacist. This includes any possible side effects not listed in this leaflet.
What is in this leaflet:
1. What Soventus®-DC Oral Suspension is and what it is used for
2. What you need to know before you take Soventus®-DC Oral Suspension
3. How to take Soventus®-DC Oral Suspension
4. Possible side effects
5. How to store Soventus®-DC Oral Suspension
6. Contents of the pack and other Information
1. What is Soventus®-DC Oral Suspension and what it is used for
Soventus®-DC Oral Suspension contains Levocloperastine as an active ingredient. Levocloperastine is an antitussive (cough suppressant) used primarily for the treatment of dry cough. It works by blocking receptors in the brain, reduces the activity of the cough center in the brain that trigger the cough reflex. It helps to alleviate coughing.
Soventus®-DC Oral Suspension is commonly used for the treatment of non-productive cough in adult patients. Non-productive coughs, which do not bring up mucus, can be particularly bothersome and may arise from various conditions, such as allergies or respiratory irritations.
2. What you need to know before you take Soventus®-DC Oral Suspension
Do not take Soventus®-DC Oral Suspension if:
- Known hypersensitivity to cloperastine or to any of the excipients.
- Children under 2 years of age.
- Pregnant or breast-feeding women.
- Known hypersensitivity to antihistaminic agents.
- Patients receiving concomitant treatment with MAO inhibitors.
- Patients with hereditary fructose intolerance, glucose or galactose malabsorption, or sucrose isomaltase deficiency.
- Consumption of Alcohol.
Warnings and precautions
Caution should be observed while prescribing Soventus®-DC Oral Suspension to adults and children with hypertension, cardiovascular disease, uncontrolled diabetes mellitus, hyperthyroidism, seizures or in patients who are unusually hypersensitive to sympathomimetic amines.
Due to its mild anticholinergic activity, cloperastine should be administered with caution in patients with intraocular hypertension, narrow-angle glaucoma, prostatic hypertrophy, urine retention, hypertension, cardiac arrhythmia, myasthenia gravis, stenosing peptic ulcer or bowel obstruction affecting the oesophagus, intestine or bladder.
Persistent cough.
Caution is recommended in patients with chronic cough such as smoker's cough, pulmonary emphysema or asthma, as it inhibits the cough reflex and could therefore alter expectoration and increase airway resistance.
Other medicines and Soventus®-DC Oral Suspension
Soventus®-DC Oral Suspension should not be concomitantly prescribed with sedatives or tranquilizers. Similarly, other antihistamine drugs should not be prescribed concomitantly. As it has some antihistaminic activity, cloperastine can enhance the sedative effect of CNS depressors such as anxiolytics, antipsychotic drugs, barbiturates, hypnotics, narcotics, sedatives, tranquilizers, some analgesics and alcohol.
Also due to this activity, cloperastine, antihistaminic agents and anticholinergic drugs (anti-parkinson's drugs, tricyclic antidepressants, neuroleptic agents) can reciprocally increase their effects.
Expectorants and mucolytic drugs: Inhibition of the cough reflex could give rise to pulmonary obstruction in case of elevated volume or fluidity of bronchial secretions.
Use in Special Population:
Pregnancy and Lactation
In humans, its safety for use in pregnancy and lactation has not been established.
Therefore, Soventus®-DC Oral Suspension should not be used during pregnancy and lactation unless a doctor believes that the treatment's potential benefit for the mother exceeds all risks for the developing foetus or infant. As it is unknown whether the drug is excreted in human milk, its use during lactation is not recommended.
Pediatric population
Not recommended for children below 2 years of age.
Hepatic & Renal Insufficiency
Caution should be exercised in patients with severe renal impairment and liver disease.
Effects on ability to drive and use machine
Levocloperastine can cause drowsiness, so caution is recommended when driving or using dangerous machinery. If drowsiness is noted at normal doses of cloperastine, do not drive or handle dangerous machinery.
3. How to take Soventus®-DC Oral Suspension
Always take Soventus®-DC Oral Suspension exactly as your doctor has told you. You should check with your doctor or pharmacist if you are not sure.
Taking this medicine
- Take this medicine by mouth.
- If you feel that this medicine is too weak or too strong, do not change the dose yourself, but ask your doctor.
How much to take
Dose for Adults: 5 ml (20mg) three times daily.
If you take more Soventus®-DC Oral Suspension than you should
If you take more Soventus®-DC Oral Suspension than you should, tell a doctor or go to a hospital casualty department straight away. Take the medicine pack with you. This is so the doctor knows what you have taken.
If you forget to take Soventus®-DC Oral Suspension
If you forget a dose, do not worry. Just wait until the next dose is due. Do not take a double dose to make up for a forgotten dose.
4. Possible Side Effects
Levocloperastine can produce minor and transient adverse reactions such as dry mouth, gastrointestinal (GI) side effects include: nausea, vomiting, constipation etc. Other adverse effects are like exhaustion, fainting, somnolence, sedation, clouding of consciousness, numbness, dizziness, headache, palpitations and allergic reaction.
Reporting of side effects
If you get any side effects, talk to your doctor. This includes any possible side effects not listed in this leaflet. You can also report side effects directly: Website: www.zuventus.co.in and click the tab “Safety Reporting” located on the top of the home page.
By reporting side effects, you can help provide more information on the safety of this medicine.
5. How to store Soventus®-DC Oral Suspension
Store in a cool place. Protect from light.
Keep out of reach of children.
Shake well before each use.
6. Contents of the pack and other information
What Soventus®-DC Oral Suspension contains
Each 5 ml oral suspension contains:
Levocloperastine Fendizoate 35.4 mg
(equivalent to 20 mg of Levocloperastine Hydrochloride)
Excipients q.s.
In a flavoured syrup base
Colour: Sunset Yellow FCF
Flavour: Mango
1x100ml, PET Bottle
For More Information About This Product
Monobact Kid Injection
1.0 Generic name
Ceftriaxone & Sulbactam for Injection IP
2.0 Qualitative and quantitative composition
Monobact Kid
Each vial contains :
Ceftriaxone Sodium IP equivalent to Ceftriaxone 125 mg
Sulbactam Sodium IP equivalent to Sulbactam 62.5 mg
This pack contains Sterile Water for Injections IP 5 ml.
Monobact 375 mg
Each vial contains :
Ceftriaxone Sodium IP equivalent to Ceftriaxone 250 mg
Sulbactam Sodium IP equivalent to Sulbactam 125 mg
This pack contains Sterile Water for Injections IP 5 ml.
Monobact 750 mg
Each vial contains :
Ceftriaxone Sodium IP equivalent to Ceftriaxone 500 mg
Sulbactam Sodium IP equivalent to Sulbactam 250 mg
This pack contains Sterile Water for Injections IP 5 ml.
Monobact 1.5 gm
Each vial contains :
Ceftriaxone Sodium IP equivalent to Ceftriaxone 1000 mg
Sulbactam Sodium IP equivalent to Sulbactam 500 mg
This pack contains Sterile Water for Injections IP 10 ml.
3.0 Dosage form and strength
Powder for solution for injection.
187.5 mg / 375 mg / 750 mg / 1.5 gm
4.0 Clinical particulars
4.1 Therapeutic indication
- Bacterial meningitis
- Infections of bones and joints
- Community acquired pneumonia
- Complicated skin and soft tissue infections
- Hospital acquired pneumonia
- Gonorrhoea
- Acute otitis media
- Syphilis
- Intra-abdominal infections
- Bacterial endocarditis
- Complicated urinary tract infections
- Surgical prophylaxis
4.2 Posology and method of administration
To be administered by deep intramuscular (I.M.) injection, slow intravenous (I.V.) injection, or as a slow I.V. infusion, after reconstitution with sterile water for injection (SWFI).
Dosage recommendations in adults
Usual Recommended Dose : 1.5 g to 3 g of Monobact Injection (1 g / 2 g ceftriaxone + 0.5 g / 1 g sulbactam) per day given once a day or in two equally divided doses every 12 hours. The total daily dose of ceftriaxone should not exceed 4 grams. Also, the total dose of sulbactam should not exceed 4 grams per day
For Uncomplicated Gonococcal Infections : A single dose of 750 mg of Monobact Injection (500 mg ceftriaxone + 250 mg sulbactam) to be administered by I.M. route. For Preoperative Use (Surgical Prophylaxis): A single dose of 1.5 g of Monobact Injection (1g ceftriaxone + 0.5 g sulbactam) to be administered intravenously 30 minutes to 2 hours before surgery
The usual duration of therapy is 4 to 14 days. In complicated infections, longer therapy may be required. Or, as prescribed by the physician.
Dosage in adult patients with renal impairment and hepatic dysfunction
In patients with both hepatic dysfunction and significant renal disease, caution should be exercised and the ceftriaxone dosage should not exceed 2 grams daily. Dose of sulbactam should be adjusted in patients with marked decrease in renal function (creatinine clearance of < 30 ml/min) and to compensate for reduced clearance less than 15ml/min, maximum dose of sulbactam should not exceed 1 gram per day.
Dosage recommendations in pediatric patients
For children with bodyweight above 50 kg or age over 12 years, the usual adult dosage should be administered. Although, ceftriaxone can be administered in neonates and infants, the safety and efficacy of this combination product (ceftriaxone + sulbactam injection) has not been established in children below 1 year of age. Thus, Monobact Injection is recommended only in pediatric patients 1 year of age or older.
Following doses in children are expressed in terms of ceftriaxone content of the formulation. Usual Recommended Dosage : 50 to 75 mg/kg/day, given in divided doses every 12 hours. The total daily dose of ceftriaxone should not exceed 2 grams. Sulbactam dose in children should not exceed 100 mg/kg/day.
Treatment of Meningitis : The initial therapeutic dose should be 100 mg/kg body weight. Thereafter, daily dose of 100 mg/kg may be administered once a day or in equally divided doses every 12 hours. The total daily dose of ceftriaxone should not exceed 4 grams. The usual duration of therapy is 7 to 14 days depending on the type and severity of infection. Or, as prescribed by the physician
Geriatric patients
Dosage adjustments are not necessary for geriatric patients with ceftriaxone dosages up to 2 grams per day provided there is no severe renal and hepatic impairment.
Pharmaceutical precautions
Ceftriaxone-containing injection should not be mixed with other drugs in infusion bottle since compatibility has not been established. Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit.
Directions for reconstitution and dilution for use
Monobact comes in a composite pack containing one vial of dry powder and Sterile Water for Injections IP in ampoule. Each Monobact 1.5 gm pack contains 1 ampoule of 10 ml Sterile Water for Injections IP [SWFI]. Monobact 750 mg contains 1 ampoule of 5 ml Sterile Water for Injections IP, Monobact 375 mg and Monobact Kid packs contain 1 ampoule of 5 ml Sterile Water for Injections IP per pack. SWFI IP from the ampoule should be used to dissolve the dry powder present in the vial, just prior to the use. After adding the SWFI IP into the vial, agitate the vial gently until the powder dissolves completely into the solution.
Though, stability studies have shown that the solution is stable for 24 hrs at 25°C and up to days under 2°C to 8°C. It is advisable to use the solution immediately after reconstitution. Following are the recommendation for diluting the solution

4.3 Contraindications
- In patients with known hypersensitivity to ceftriaxone, cephalosporin class of antibiotics, or to tazobactam or to any component of the formulation.
- In hyperbilirubinemic neonates/preterm newborns : Ceftriaxone can displace bilirubin from its binding to serum albumin, leading to a risk of bilirubin encephalopathy in these patients.
- Premature neonates : Ceftriaxone is contraindicated in premature neonates up to a postmenstrual age of 41 weeks (gestational age + chronological age).
- In neonates (≤ 28 days) if they require (or are expected to require) treatment with calcium-containing I.V. solutions, including continuous calcium-containing infusions such as parenteral nutrition because of the risk of precipitation of ceftriaxone-calcium.
- Intravenous administration of ceftriaxone solutions containing lidocaine is contraindicated.
4.4 Special warnings and precautions
Test dose
Hypersensitivity
Before initiation of therapy, careful inquiry should be made to determine whether the patient has had previous hypersensitivity reactions to cephalosporins, penicillins and other beta-lactam agents or other drugs. As with all beta-lactam antibacterial agents, serious and occasionally fatal hypersensitivity reactions (i.e., anaphylaxis) have been reported. In case of severe hypersensitivity reactions, treatment with ceftriaxone must be discontinued immediately and adequate emergency measures must be initiated.
Clostridium difficile-associated diarrhea (CDAD)
CDAD has been reported with use of nearly all antibacterial agents, including ceftriaxone, and may range in severity from mild diarrhea to fatal colitis. Treatment with antibacterial agents alters the normal flora of the colon leading to overgrowth of C. difficile. If CDAD is suspected or confirmed, ongoing antibiotic use not directed against C. difficile may need to be discontinued. Appropriate fluid and electrolyte management, protein supplementation, antibiotic treatment of C. difficile, and surgical evaluation should be instituted as clinically indicated.
Hemolytic anemia
An immune mediated hemolytic anemia has been observed in patients receiving cephalosporin class of antibacterial drugs including ceftriaxone. Severe cases of hemolytic anemia, including fatalities, have been reported during treatment in both adults and children. If a patient develops anemia while on ceftriaxone, the diagnosis of a cephalosporin associated anemia should be considered and ceftriaxone stopped until the etiology is determined.
Development of drug-resistant bacteria
Prescribing ceftriaxone in the absence of a proven or strongly suspected bacterial infection or a prophylactic indication is unlikely to provide benefit to the patient and increases the risk of the development of drug-resistant bacteria. Prolonged use of ceftriaxone may result in overgrowth of nonsusceptible organisms. Careful observation of the patient is essential. If superinfection occurs during therapy, appropriate measures should be taken.
Pancreatitis
Cases of pancreatitis, possibly secondary to biliary obstruction, have been reported in patients treated with ceftriaxone. Most patients presented with risk factors for biliary stasis and biliary sludge (preceding major therapy, severe illness, and total parenteral nutrition). A cofactor role of ceftriaxone-related biliary precipitation cannot be ruled out.
Urolithiasis and post-renal acute renal failure
Ceftriaxone-calcium precipitates in the urinary tract have been observed in patients receiving ceftriaxone. The probability of such precipitates appears to be greatest in pediatric patients. Patients may be asymptomatic or may develop symptoms of urolithiasis, and ureteral obstruction and post-renal acute renal failure. The condition appears to be reversible upon discontinuation of ceftriaxone and institution of appropriate management. Ensure adequate hydration in patients receiving ceftriaxone. Discontinue ceftriaxone in patients who develop signs and symptoms suggestive of urolithiasis, oliguria or renal failure and/or the sonographic findings.
Gallbladder pseudolithiasis
Ceftriaxone-calcium precipitates in the gallbladder have been observed in patients receiving ceftriaxone. The probability of such precipitates appears to be greatest in pediatric patients. Patients may be asymptomatic or may develop symptoms of gallbladder disease. The condition appears to be reversible upon discontinuation of ceftriaxone and institution of conservative management. Discontinue ceftriaxone sodium in patients who develop signs and symptoms suggestive of gallbladder disease and/or the sonographic findings.
Effect on prothrombin time
Alterations in prothrombin times have occurred in patients treated with ceftriaxone. Monitor prothrombin time during ceftriaxone treatment in patients with impaired vitamin K synthesis or low vitamin K stores (e.g., chronic hepatic disease and malnutrition). Vitamin K administration (10 mg weekly) may be necessary if the prothrombin time is prolonged before or during therapy.
Altered laboratory tests
Positive direct Coombs' test and galactosemia test, false-positive test for urinary glucose and elevated lactate dehydrogenase (LDH).
4.5 Drug interactions
Ceftriaxone
Amsacrine, Vancomycin, Fluconazole, and Aminoglycosides : Ceftriaxone is incompatible with these drugs.
Oral Contraceptives : Ceftriaxone may adversely affect the efficacy of oral hormonal contraceptives. Consequently, it is advisable to use supplementary (non-hormonal) contraceptive measures during treatment and in the month following treatment. Chloramphenicol : Caution is advised if concurrent administration of ceftriaxone with chloramphenicol is proposed.
Vitamin K Antagonist : Concomitant use of ceftriaxone with vitamin K antagonists may increase the risk of bleeding. Coagulation parameters should be monitored frequently, and the dose of the anticoagulant adjusted accordingly, both during and after treatment with ceftriaxone.
Sulbactam
Probenecid : Probenecid decreases the renal tubular secretion of sulbactam. Concurrent use of probenecid with sulbactam may result in increased and prolonged blood levels of sulbactam.
4.6 Use in special populations
Pregnancy
Animal studies have revealed no evidence of impaired fertility or harm to the fetus. There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, Monobact Injection should be used during pregnancy only if clearly needed.
Lactation
Although sulbactam is distributed into breast milk in small amounts, no adverse effects have been seen in breast-fed infants and it is usually compatible with breast feeding. Low concentration of ceftriaxone is excreted in human milk. Therefore, caution should be exercised when Monobact Injection is administered to a nursing woman.
Pediatric patients
Safety and effectiveness of ceftriaxone has been established in pediatric patients. In vitro studies have shown that ceftriaxone, like some other cephalosporins, can displace bilirubin from serum albumin. Thus, ceftriaxone-containing preparations should not be administered to hyperbilirubinemic children. Safety and efficacy of Monobact Injection has not been established in children below 1 year of age.
4.7 Effects on the ability to drive and use machines
During treatment undesirable effects such as dizziness, headache, and convulsions may occur, which may influence the ability to drive and use machines. If affected by such events, patients should not drive or operate machinery.
4.8 Undesirable effects
Ceftriaxone-containing preparations are generally well tolerated. In clinical trials, the following adverse reactions were observed (related to ceftriaxone therapy or of uncertain etiology). Local Reactions : Injection site pain, induration, tenderness, phlebitis, warmth, tightness. Hypersensitivity : Rash, pruritus, fever or chills.
Infections and Infestations : Genital fungal infection. Hematologic : Eosinophilia, thrombocytosis, leukopenia. Less frequently reported were anemia, hemolytic anemia, neutropenia, lymphopenia, thrombocytopenia and prolongation of the prothrombin time.
Blood and Lymphatic Disorders : Granulocytopenia, coagulopathy. Gastrointestinal : Diarrhea/loose stools, nausea, vomiting, dysgeusia, pseudomembranous colitis.
Hepatic : Elevations of aspartate aminotransferase (AST), alanine aminotransferase (ALT), alkaline phosphatase, and bilirubin.
Renal : Elevations of the blood urea nitrogen (BUN), creatinine and the presence of casts in the urine.
Central Nervous System : Headache, dizziness.
Dermatologic : Exanthema, allergic dermatitis, urticaria, edema; acute generalized exanthematous pustulosis (AGEP) and isolated cases of severe cutaneous adverse reactions (erythema multiforme, Stevens-Johnson syndrome or Lyell's syndrome / toxic epidermal necrolysis) have been reported.
Miscellaneous : Diaphoresis, flushing, increased blood creatinine.
Other rarely observed adverse reactions (< 0.1%) include abdominal pain, agranulocytosis, allergic pneumonitis, anaphylaxis, basophilia, biliary lithiasis, bronchospasm, colitis, dyspepsia, epistaxis, flatulence, gallbladder sludge, glycosuria, hematuria, jaundice, leukocytosis, lymphocytosis, monocytosis, nephrolithiasis, palpitations, decrease in the prothrombin time, renal precipitations, seizures, and serum sickness.
Reporting of side effects
Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via
email to : medico@zuventus.com
Website : https://www.zuventus.co.in/drug-safety-reporting
By reporting side effects, you can help provide more information on the safety of this medicine.
4.9 Overdose
In the case of overdose nausea, vomiting, and diarrhea can occur. There is no specific antidote. Treatment should be supportive and symptomatic according the patient's clinical presentation.
5.0 Pharmacological properties
5.1 Mechanism of action
Ceftriaxone
Ceftriaxone is a third generation cephalosporin class of beta-lactam antibiotic. Ceftriaxone inhibits bacterial cell wall synthesis and produces bactericidal effect. Ceftriaxone has activity in the presence of some beta-lactamases, both penicillinases and cephalosporinases, of Gramnegative and Gram-positive bacteria.
Sulbactam
Beta-lactamases are the enzymes produced by certain bacteria to develop resistant to penicillin and cephalosporin class of beta-lactam antibiotics. Sulbactam inhibits action of these enzymes irreversibly. In particular, sulbactam has good inhibitory activity against the clinically important plasmid mediated beta-lactamases most frequently responsible for transferred drug resistance. The addition of sulbactam effectively extends the antibacterial spectrum of concurrently administered beta-lactam antibiotic (e.g., ceftriaxone) to include many bacteria normally resistant to it.
5.2 Pharmacodynamic properties
The combination of ceftriaxone and sulbactam is active against wide variety of beta-lactamase producing gram-positive and gram-negative bacteria. In addition, it demonstrates synergistic activity (reduction in MICs of combination therapy versus ceftriaxone alone) in a variety of organisms which are sensitive to ceftriaxone.
Monobact Injection has been shown to be active against most isolates of the following bacteria, both in vitro and in clinical infections :
Gram-negative Bacteria
Acinetobacter calcoaceticus Moraxella catarrhalis
Enterobacter aerogenes Morganella morganii
Enterobacter cloacae Neisseria gonorrhoeae
Escherichia coli Neisseria meningitidis
Haemophilus influenzae Proteus mirabilis
Haemophilus parainfluenzae Proteus vulgaris
Klebsiella oxytoca Pseudomonas aeruginosa
Klebsiella pneumoniae Serratia marcescens
Gram-positive Bacteria
Staphylococcus aureus Streptococcus pyogenes
Staphylococcus epidermidis Viridans group streptococci
Streptococcus pneumoniae
Anaerobic Bacteria
Bacteroides fragilis Peptostreptococcus species
Clostridium species
The following in vitro data are available, but their clinical significance is unknown. At least 90% of the following microorganisms exhibit an in vitro minimum inhibitory concentration (MIC) less than or equal to the susceptible breakpoint for ceftriaxone. However, the efficacy of ceftriaxone in treating clinical infections due to these microorganisms has not been established in adequate and well-controlled clinical trials.
Gram-negative Bacteria
Citrobacter diversus Salmonella species (including Citrobacter freundii Salmonella typhi)
Providencia species (including Providencia rettgeri) Shigella species
Gram-positive Bacteria
Streptococcus agalactiae
Anaerobic Bacteria
Porphyromonas (Bacteroides) melaninogenicus Prevotella (Bacteroides) bivius
5.3 Pharmacokinetic properties
Ceftriaxone
Absorption : Following intramuscular injection, mean peak plasma ceftriaxone levels are approximately half those observed after intravenous administration of an equivalent dose. The maximum plasma concentration after a single intramuscular dose of 1 gram is about 81 mg/l and is reached in 2 to 3 hours after administration. The area under the plasma concentrationtime curve after intramuscular administration is equivalent to that after intravenous administration of an equivalent dose.
After intravenous bolus administration of ceftriaxone 500 mg and 1 g, mean peak plasma ceftriaxone (Cmax) levels are approximately 120 and 200 mg/l respectively. After intravenous infusion of ceftriaxone 500 mg, 1 g and 2 g, the plasma ceftriaxone levels are approximately 80, 150 and 250 mg/l respectively. An 8 to 15 % increase in Cmax is seen on repeated administration; steady state is reached in most cases within 48 to 72 hours depending on the route of administration.
Distribution : The volume of distribution of ceftriaxone is 7 to 12 litre. Ceftriaxone is reversibly bound to albumin. Plasma protein binding is about 95 % at plasma concentrations below 100 mg/l.
Binding is saturable and the bound portion decreases with rising concentration (up to 85 % at a plasma concentration of 300 mg/l).
Metabolism : Ceftriaxone is not metabolized systemically; but is converted to inactive metabolites by the gut flora. Elimination : Plasma clearance of total ceftriaxone (bound and unbound) is 10 to 22 ml/min. Renal clearance is 5 to 12 ml/min. 50 to 60 % of ceftriaxone is excreted unchanged in the urine, primarily by glomerular filtration, while 40 to 50 % is excreted unchanged in the bile. The elimination half-life of total ceftriaxone in adults is about 8 hours.
Sulbactam
After a 30-minute infusion of 1g of sulbactam, a peak concentration of approximately 43 mcg/ml is obtained. Plasma protein binding is approximately 38%. The mean serum half-life of sulbactam is approximately 1 hour in healthy volunteers. Approximately 75 to 85% of sulbactam is excreted unchanged in the urine during the first 8 hours after administration to individuals with normal renal function.
6.0 Nonclinical properties
6.1 Animal toxicology or pharmacology
Ceftriaxone
LD50 values after administration of ceftriaxone by intravenous route were in mice 1840 mg/kg, in rat 2240 mg/kg, and in rabbit 240 mg/kg. LD50 value reported after administration of ceftriaxone by oral route in mice and rats was >10,000 mg/kg. In a 2-week intravenous administration study, groups of eight male Füllinsdorf rats were administered 0, 25 or 60 mg/kg/day of ceftriaxone. Body weight gain was slightly depressed by 9.2 and 20.1% in the 25 and 60 mg/kg/day groups respectively. The average weight of the thyroid glands was increased in the treated groups by 11 to 14% in comparison to the control animals. A 50% reduction in plasma bilirubin in the treated rats was reported along with a decrease in the number of leucocytes. 11 Genetic toxicology tests included the Ames test, a micronucleus test and a test for chromosomal aberrations in human lymphocytes cultured in vitro with ceftriaxone. Ceftriaxone showed no potential for mutagenic activity in these studies. Carcinogenicity studies on ceftriaxone were not conducted. Reproductive studies have been performed in mice and rats at doses up to 20 times the usual human dose and have no evidence of embryotoxicity, fetotoxicity or teratogenicity. In primates, no embryotoxicity or teratogenicity was demonstrated at a dose approximately 3 times the human dose. Ceftriaxone produced no impairment of fertility when given intravenously to rats at daily doses up to 586 mg/kg/day, approximately 20 times the recommended clinical dose of 2 g/day.
Sulbactam
Relevant data is not available.
7.0 Description
Monobact is a combination of Ceftriaxone Sodium and Sulbactam Sodium available as dry powder for reconstitution.
Ceftriaxone
Ceftriaxone is a beta-lactam, third-generation cephalosporin antibiotic with bactericidal activity. Molecular Weight : 554.6g/mol.
Molecular Formula : C18H18N8O7S3.
Chemical Name : (6R,7R)-7-[[(2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-methoxyiminoacetyl] amino]- 3-[(2-methyl-5,6-dioxo-1H-1,2,4-triazin-3-yl)sulfanylmethyl]-8-oxo-5-thia-1- azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid.
Sulbactam sodium
Sulbactam is a β-lactamase inhibitor given in combination with β-lactam antibiotics to inhibit β- lactamase, an enzyme produced by bacteria that destroys antibiotic activity. Sulbactam sodium is a derivative of the basic penicillin nucleus. Molecular Weight : 255.22 g/mol.
Molecular Formula : C8H10NNaO5S.
Chemical Name : Sodium (2S, 5R)-3,3-dimethyl-7-oxo-4-thia- 1-azabicyclo [3.2.0] heptane- 2- carboxylate 4,4- dioxide.
8.0 Pharmaceutical particulars
8.1 Incompatibilities
Do not use diluents containing calcium, such as Ringer's solution or Hartmann's solution, to reconstitute or to further dilute a reconstituted vial for I.V. administration because a precipitate can form. Precipitation of ceftriaxone-calcium can also occur when ceftriaxone is mixed with calcium-containing solutions in the same I.V. administration line. Ceftriaxone with sulbactam must not be administered simultaneously with calcium-containing I.V. solutions, including continuous calcium-containing infusions such as parenteral nutrition.
8.2 Shelf-life
Refer on the pack.
8.3 Packaging information
Monobact Kid : A vial of 187.5 mg with SWFI IP 5 ml.
Monobact 375 mg : A vial of 375 mg with SWFI IP 5 ml.
Monobact 750 mg : A vial of 750 mg with SWFI IP 5 ml.
Monobact 1.5 gm : A vial of 1.5 gm with SWFI IP 10 ml.
8.4 Storage and handling instructions
Store below 25°C. Protect from light. Do not freeze.
Keep out of reach of children. After reconstitution, do not use in case any foreign particulate matter is observed inside the vial.
9.0 Patient counselling information
- Instruct patient to store medication as advised and not to expose the vial to moisture or direct light.
- When ceftriaxone with sulbactam is prescribed to treat a bacterial infection, patients should be told that although it is common to feel better early in the course of therapy, the medication should be taken exactly as directed. Skipping doses or not completing the full course of therapy may decrease the effectiveness of therapy and increase the likelihood that bacteria will develop antimicrobial resistance.
- Diarrhea is a common problem caused by antibiotics which usually ends when the antibiotic is discontinued. Sometimes after starting treatment with antibiotics, patients can develop watery and bloody stools even as late as two months after the last dose of the antibiotic. If this occurs, instruct patients to contact their physician immediately.
- Instruct patient not to freeze the reconstituted solution and use it immediately after the preparation. Unused portion of solution, if any, should be discarded.
12.0 Date of revision
16 August 2024
About leaflet
The name of your medicine is Monobact injection. We refer to them as Monobact injection or Monobact throughout this leaflet.
Read all of this leaflet carefully before you are given this medicine because it contains important information for you.
- Keep this leaflet. You may need to read it again.
- If you have any further questions, ask your doctor, pharmacist or nurse.
- This medicine has been prescribed for you only. Do not pass it on to others. It may harm them, even if their signs of illness are the same as yours.
- If you get any side effects, talk to your doctor, pharmacist or nurse. This includes any possible side effects not listed in this leaflet. See section 4.
What is in this leaflet
1. What MONOBACT injection is and what it is used for
2. What you need to know before you are given MONOBACT injection
3. How MONOBACT injection is given
4. Possible side effects
5. How to store MONOBACT injection
6. Contents of the pack and other information
1. What MONOBACT injection is and what it is used for
MONOBACT injection is an antibiotic given to adults and children including new-born babies. It contains a combination of antibiotics such as Sulbactam & Ceftriaxone. Sulbactam is a β-lactamase inhibitor whereas Ceftriaxone is a third-generation semi-synthetic cephalosporin. It works by killing bacteria that cause infections. It belongs to a group of medicines called cephalosporins. MONOBACT injection is used for the treatment of:
- Lower Respiratory Tract infections like pneumonia, bronchitis etc.
- Skin and Skin Structure Infections
- Pelvic Inflammatory Disease
- Bone and Joint Infections
- Infection coverings of brain (meningitis)
- Use before surgery to prevent infection
- Internal Ear infection
- Urinary Tract Infections
- Bacterial Sepsis (severe infection)
- Intra-Abdominal Infections
- Uncomplicated gonorrhoea, Syphilis (sexually transmitted infection)
2. What you need to know before you are given MONOBACT injection
You must not be given MONOBACT injection if you have:
- Hypersensitivity to the active substance, to any other cephalosporin or to any of the excipients listed in the formulation.
- History of severe hypersensitivity (e.g. anaphylactic reaction) to any other type of beta-lactam antibacterial agent (penicillins, monobactams and carbapenems).
- Premature neonates up to a postmenstrual age of 41 weeks (gestational age + chronological age)
- Full-term neonates (up to 28 days of age):
with hyper-bilirubinaemia, jaundice, or who are hypo-albuminaemic or acidotic because these are conditions in which bilirubin binding is likely to be impaired.
if they require (or are expected to require) intravenous calcium treatment, or calcium-containing infusions due to the risk of precipitation of a ceftriaxone-calcium salt
Warnings and precautions
Talk to your doctor or pharmacist or nurse before you are given MONOBACT injection if:
- You experience serious and occasionally fatal hypersensitivity (anaphylactic) reactions. These reactions are more apt to occur in individual with history of hypersensitivity reactions to multiple allergens.
- You have biliary obstruction, liver or kidney problems.
- You have other illnesses, such as vitamin K deficiency
If you need a blood or urine test
Ceftriaxone can affect the results of urine tests for sugar and a give false positive results. If you are having tests:
- Tell the person taking the sample that you have been given MONOBACT injection.
MONOBACT in babies:
- MONOBACT injection has been effectively used in infants
- It has not been extensively studied in premature infants or neonates. Thus, your doctor will decide if MONOBACT can be given in such babies, on the basis of potential benefits and possible risks involved before instituting therapy.
Other medicines and MONOBACT
Tell your doctor or pharmacist if you are taking, have recently taken or might take any other medicines.
In particular, tell your doctor or pharmacist if you are taking:
- Alcohol
Pregnancy and breast-feeding and fertility
If you are pregnant or breast-feeding, think you may be pregnant or are planning to have a baby, ask your doctor for advice before taking this medicine. The doctor will consider the benefit of treating you with MONOBACT against the risk to your baby.
Driving and using machines
Clinical experience with MONOBACT indicates that it is unlikely to impair a patient's ability to drive or use machinery.
3. How MONOBACT injection is given
MONOBACT injection is usually given by a doctor or nurse. It can be given as a drip (intravenous infusion) or as an injection directly into a vein or into a muscle.
The usual dose
Your doctor will decide the correct dose of MONOBACT for you. The dose will depend on the severity and type of infection; whether you are on any other antibiotics; your weight and age; how well your kidneys and liver are working. The number of days or weeks that you are given MONOBACT depends on what sort of infection you have.
Adults
2 to 4 gram is given in equally divided doses twice a day depending on the severity and type of infection.
If you have a severe infection, your doctor will give you a higher dose (up to 8 grams in equally divided doses twice a day). The recommended maximum daily dosage of Sulbactam is 4 grams (8 gram of Ceftriaxone-Sulbactam).
Children aged > 7 days
The usual dosage of MONOBACT in children is 40 to 80 mg/kg/day (i.e. 20 to 40 mg/kg/day of Ceftriaxone activity) in 2 to 4 equally divided doses, depending on the severity and type of infection. If you have a severe infection, your doctor will give you a higher dose up to 160 mg/kg/day of MONOBACT in 2 to 4 equally divided doses.
Newborn babies (0-7 days)
For neonates in the first week of life, MONOBACT will be given every 12 hours. The maximum daily dosage of Sulbactam in these patients should not exceed 80 mg/kg/day (160 mg/kg/day MONOBACT). In cases where dose above 80 mg/kg/day of Ceftriaxone are necessary, additional Ceftriaxone will be administered separately.
People with liver and kidney problems
You may be given a different dose to the usual dose. Your doctor will decide how much MONOBACT you will need and will check you closely depending on the severity of the liver and kidney disease.
If you are given more MONOBACT than you should
If you accidentally receive more than your prescribed dose, contact your doctor or nearest hospital straight away.
If you forget to use MONOBACT injection
If you miss an injection, you should have it as soon as possible. However, if it is almost time for your next injection, skip the missed injection. Do not take a double dose (two injections at the same time) to make up for a missed dose.
If you stop using MONOBACT injection
Do not stop taking MONOBACT injection unless your doctor tells you to. If you have any further questions on the use of this medicine, ask your doctor or nurse.
4. Possible side effects
Like all medicines, this medicine can cause side effects, although not everybody gets them.
The following side effects may happen with this medicine:
Local Reactions: pain, induration and tenderness and phlebitis. The incidence of warmth, tightness or induration after Intra Muscular injection.
Hypersensitivity: rash, less frequently reported were pruritus, fever or chills.
Hematologic: eosinophilia, thrombocytosis and leukopenia. Less frequently reported were anemia, haemolytic anemia, neutropenia, lymphopenia, thrombocytopenia and prolongation of the prothrombin time.
Gastrointestinal: diarrhea. Less frequently reported were nausea or vomiting, and loss of taste. The onset of pseudomembranous colitis symptoms may occur during or after antibacterial treatment
Hepatic: elevations of liver enzymes. Less frequently reported were elevations of alkaline phosphatase and bilirubin.
Renal: elevations of the blood urea. Less frequently reported were elevations of creatinine and the presence of casts in the urine.
Central Nervous System: headache or dizziness were reported occasionally.
Genitourinary: Fungal infections were reported occasionally.
Skin and subcutaneous tissue disorders: Fixed Drug Eruption.
Miscellaneous: diaphoresis and flushing were reported occasionally.
Other rarely observed adverse reactions include abdominal pain, agranulocytosis, allergic pneumonitis, anaphylaxis, basophilia, biliary lithiasis, bronchospasm, colitis, dyspepsia, epistaxis, flatulence, gallbladder sludge, glycosuria, hematuria, jaundice, leucocytosis, lymphocytosis, monocytosis, nephrolithiasis, palpitations, a decrease in the prothrombin time, renal precipitations, seizures, and serum sickness.
Reporting of side effects
If you get any side effects, talk to your doctor, pharmacist or nurse. This includes any possible side effects not listed in this leaflet.
You can also report side effects directly: Website: www.zuventus.com and click the tab “Safety Reporting” located on the top of the home page.
By reporting side effects, you can help provide more information on the safety of this medicine. You can also report the side effect with the help of your treating physician.
You can also report the side effect with the help of your treating physician.
5. How to store MONOBACT injection
Keep out of the sight and reach of children. Protect from light. After reconstitution, do not use it in case any foreign particulate matter is observed inside the vial.
Do not use MONOBACT injection after the expiry date which is printed on the label and carton.
Do not store above 25°C. Your doctor, pharmacist or nurse will know how to store MONOBACT Injection properly.
6. Contents of the pack and other information
What MONOBACT injection contains
The active substance in MONOBACT injection is Ceftriaxone and Sulbactam.
MONOBACT Kid
Each vial contains:
Ceftriaxone Sodium IP equivalent to Ceftriaxone 125 mg
Sulbactam Sodium IP equivalent to Sulbactam 62.5 mg
This pack contains Sterile Water for Injections IP 5 ml.
MONOBACT 375 mg
Each vial contains:
Ceftriaxone Sodium IP equivalent to Ceftriaxone 250 mg
Sulbactam Sodium IP equivalent to Sulbactam 125 mg
This pack contains Sterile Water for Injections IP 5 ml.
MONOBACT 750 mg
Each vial contains:
Ceftriaxone Sodium IP equivalent to Ceftriaxone 500 mg
Sulbactam Sodium IP equivalent to Sulbactam 250 mg
This pack contains Sterile Water for Injections IP 5 ml.
MONOBACT 1.5 gm
Each vial contains: Ceftriaxone Sodium IP equivalent to Ceftriaxone 1000 mg
Sulbactam Sodium IP equivalent to Sulbactam 500 mg
This pack contains Sterile Water for Injections IP 10 ml.
Pack size/presentation
MONOBACT Kid: A vial of 187.5 mg with sterile water for injection IP 5 ml.
MONOBACT 375 mg: A vial of 375 mg with sterile water for injection IP 5 ml.
MONOBACT 750 mg: A vial of 750 mg with sterile water for injection IP 5 ml.
MONOBACT 1.5 gm: A vial of 1.5 gm with sterile water for injection IP 10 ml.