Bactomin Tablet
Therapy Area
Anti Infective
Composition
Bactomin 375
Each film coated tablet contains :
Sultamicillin Tosilate Dihydrate BP
equivalent to Sultamicillin 375 mg
Excipients q.s.
Colour : Titanium Dioxide IP
Bactomin 750
Each film coated tablet contains :
Sultamicillin Tosilate Dihydrate BP
equivalent to Sultamicillin 750 mg
Excipients q.s.
Colour : Titanium Dioxide IP
Description
Sultamicillin is a double ester in which Ampicillin and the beta-lactamase inhibitor sulbactam are linked via a methylene group
Chemical name : Oxymethylpenicillinate Sulphone ester of Ampicillin
Molecular weight : 594.7
Clinical Pharmacology
Pharmacodynamics
Biochemical studies with cell-free bacterial systems have shown sulbactam to be an irreversible inhibitor of most important beta-lactamases that occur in penicillin-resistant organisms. While antibacterial activity of sulbactam is mainly limited to Neisseriaceae, the potential of sulbactam sodium in preventing the destruction of penicillins and cephalosporins by resistant organisms was confirmed in whole organism studies using resistant strains, in which sulbactam sodium exhibited marked synergistic effects with penicillins and cephalosporins. Since sulbactam also binds to some penicillin-binding proteins, some sensitive strains are rendered more susceptible to the combination than to the beta-lactam antibiotic alone. The bactericidal component of this product is Ampicillin which, like Benzyl penicillin, acts against sensitive organisms during the stage of active multiplication by the inhibition of biosynthesis of cell wall mucopeptide.
Pharmacokinetics
Following oral administration in humans, Sultamicillin is hydrolysed during absorption to provide Sulbactam and Ampicillin in a 1:1 molar ratio in the systemic circulation. The bioavailability of an oral dose is 80% of an equal intravenous dose of Sulbactam and Ampicillin. Administration following food does not affect the systemic bioavailability of Sultamicillin. Peak serum levels of Ampicillin following administration of Sultamicillin are approximately twice those of an equal dose of oral Ampicillin. Elimination half-lives are approximately 0.75 and 1 hour for Sulbactam and Ampicillin respectively in healthy volunteers, with 50-75% of each agent being excreted in the urine unchanged. Elimination half-lives are increased in the elderly and in patients with renal dysfunction. Probenecid decreases the renal tubular secretion of both Ampicillin and Sulbactam. Concurrent use of probenecid with Sultamicillin results in increased and prolonged blood levels of Ampicillin and Sulbactam.
Microbiology
Sultamicillin is effective against a wide range of gram-positive and gram-negative bacteria including : Staphylococcus aureus and S. epidermidis (including penicillin-resistant and some methicillin resistant strains); Streptococcus pneumoniae, Streptococcus faecalis and other Streptococcus species; Haemophilus influenzae and H. parainfluenzae (both beta-lactamase positive and negative strains); Moraxella catarrhalis; anaerobes including Bacteroides fragilis and related species; Escherichia coli; Klebsiella species; Proteus species (both indole-positive and indole-negative); Enterobacter species; Morganella morganii; Citrobacter species; Neisseria meningitidis and Neisseria gonorrhoeae.
Indications
Sultamicillin is indicated for infections caused by susceptible micro-organisms. Typical indications are :
Upper respiratory tract infections including sinusitis, otitis media and tonsillitis
Lower respiratory tract infections including bacterial pneumonias and bronchitis
Urinary tract infections and pyelonephritis
Skin and soft tissue infections
Intra-abdominal infections
Gonococcal infections
Sultamicillin may also be indicated in patients requiring oral Sulbactam/Ampicillin therapy following initial treatment with Sulbactam /Ampicillin IM/IV
Dosage and Administration
The recommended dose of Sultamicillin in adults (including elderly patients) is 375-750 mg orally twice daily. In both adults and children treatment is usually continued until 48 hours after pyrexia and other abnormal signs have resolved. Treatment is normally given for 5-14 days but the treatment period may be extended if necessary. In the treatment of uncomplicated gonorrhea, Sultamicillin can be given as a single oral dose of 2.25 grams (six 375 mg tablets). Concomitant probenecid 1.0 gram should be administered in order to prolong plasma concentrations of Sulbactam and Ampicillin. Cases of gonorrhea with a suspected lesion of syphilis should have dark field examinations before receiving Sultamicillin and monthly serological tests for a minimum of four months. It is recommended that there be at least 10 days treatment for any infection caused by hemolytic streptococci to prevent the occurrence of acute rheumatic fever or glomerulonephritis.
Use in Children and Infants
For children weighing less than 30 kg the dosage of Sultamicillin for most infections is 25-50 mg/kg/day orally in 2 divided doses depending on the severity of the infection and the physician's judgment. For children weighing 30 kg or more the usual adult dose should be given.
Use in Patients with Renal Impairment
In patients with severe impairment of renal function (creatinine clearance < 30 ml/min), the elimination kinetics of Sulbactam and Ampicillin are similarly affected and hence the plasma ratio of one to the other will remain constant. The dose of Sultamicillin in such patients should be administered less frequently in accordance with usual practice for Ampicillin.
Contraindications
BACTOMIN is contraindicated in patients with known hypersensitivity to any of its ingredients or with a history of an allergic reaction to any of the penicillins.
Use in Special Populations
Pregnancy
Animal reproduction studies have revealed no evidence of impaired fertility or harm to the fetus due to Sultamicillin. Sulbactam crosses the placental barrier. However, safety for use in human pregnancy has not been established. Therefore, Sultamicillin should be used during pregnancy only if the potential benefits outweigh the potential risk.
Lactation
Low concentrations of Ampicillin and Sulbactam are excreted in the milk. This should be considered as the neonate may be exposed, particularly since renal function is not fully developed in neonates.
Warning and Precautions
Serious and occasionally fatal hypersensitivity (anaphylactic) reactions have been reported in patients on penicillin therapy including Sultamicillin. These reactions are more apt to occur in individuals with a history of penicillin hypersensitivity and/or hypersensitivity reactions to multiple allergens. Before therapy with a penicillin, careful inquiry should be made concerning previous hypersensitivity reactions to penicillins, cephalosporins, and other allergens. If an allergic reaction occurs, the drug should be discontinued and appropriate therapy be instituted.
Serious anaphylactic reactions require immediate treatment with adrenaline. oxygen, intravenous steroids, and airway management, including intubation as indicated.
As with any antibiotic preparation, constant observation for signs of overgrowth of nonsusceptible organisms, including fungi, is essential. If superinfection occurs, the drug should be discontinued and/or appropriate therapy be instituted.
Clostridium difficile associated diarrhea (CDAD) has been reported with use of nearly all antibacterial agents, including Sultamicillin, and may range in severity from mild diarrhea to fatal colitis. Careful medical history is necessary since CDAD has been reported to occur over two months after the administration of antibacterial agents.
Since infectious mononucleosis is viral in origin, Ampicillin should not be used in the treatment. A high percentage of patients with mononucleosis who receive Ampicillin develop a skin rash.
It is advisable to check periodically for organ system dysfunction during prolonged therapy; this includes renal, hepatic and hematopoietic systems
Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.
Drug Interactions
1. Allopurinol : The concurrent administration of Allopurinol and Ampicillin increases substantially the incidence of rashes in patients receiving both drugs as compared to patients receiving Ampicillin alone.
2. Anticoagulants : Penicillins can produce alterations in platelet aggregation and coagulation tests. These effects may be additive with anticoagulants.
3. Bacteriostatic drugs (Chloramphenicol, Erythromycin, Sulfonamides and Tetracyclines) : Bacteriostatic drugs may interfere with the bactericidal effect of penicillins; it is best to avoid concurrent therapy
4. Estrogen-containing oral contraceptives : There have been case reports of reduced oral contraceptive effectiveness in women taking Ampicillin, resulting in unplanned pregnancy. Although the association is weak, patients should be given the option to use an alternate or additional method of contraception while taking Ampicillin
5. Methotrexate : Concurrent use with penicillins has resulted in decreased clearance of Methotrexate and a corresponding increase in methotrexate toxicity. Patients should be closely monitored. Leucovorin dosages may need to be increased and administered for longer periods of time.
6. Probenecid : Probenecid decreases renal tubular secretion of Ampicillin and Sulbactam when used concurrently; this effect results in increased and prolonged serum concentrations, prolonged elimination half-life, and increased risk of toxicity
7. Laboratory Test Interactions : False positive glycosuria may be observed in urinalysis using Benedict reagent, Fehling reagent, and Clinitest. Following administration of Ampicillin to pregnant women, a transient decrease in plasma concentration of total conjugated estriol, estriol-glucuronide, conjugated estrone and estradiol has been noted.
Adverse Effects
Sultamicillin is generally well tolerated. The majority of the side effects observed were of mild or moderate severity and were normally tolerated with continued treatment
Infections & Infestations : pseudomembranous colitis
Immune System Disorders : anaphylactic shock, anaphylactic reaction, hypersensitivity
Nervous System Disorders : dizziness, somnolence, sedation, headache.
Respiratory, Thoracic & Mediastinal Disorders : dyspnoea
Gastrointestinal Disorders : enterocolitis, melaena, diarrhoea, vomiting, abdominal pain, dyspepsia, nausea.
Skin & Subcutaneous Tissue Disorders : angioedema, urticaria, dermatitis, rash, pruritus.
General Disorders & Administration Site Conditions : fatigue, malaise
Adverse reactions associated with use of Ampicillin alone may be observed with Sultamicillin.
Overdosage
Limited information is available on the acute toxicity of Ampicillin Sodium and Sulbactam sodium in humans. Overdosage of the dr ug would be expected to produce manifestations that are principally extensions of the adverse reactions reported with the drug. The fact that high CSF concentrations of β-lactam antibiotics may cause neurologic effects, including seizures, should be considered. Because Ampicillin and Sulbactam are both removed from the circulation by hemodialysis, these procedures may enhance elimination of the drug from the body if overdosage occurs in patients with impaired renal function.
Storage
Store below 30°C. Protect from light.
Keep out of reach of children.
Presentation:
Bactomin 375 : A blister strip of 10 tablets
Bactomin 750 : A blister strip of 6 tablets.