Full Prescribing Info
Contents
Sultamicillin: Sulbactam & ampicillin.
Description
Each tablet contains the tosylate salt equivalent to sultamicillin 375 mg which is a mutual prodrug of sulbactam and ampicillin yielding the equivalent of sulbactam 147 mg and ampicillin 220 mg.
Each 750- and 1500-mg vial contains sulbactam sodium/ampicillin as a dry powder for reconstitution of 250 mg/500 mg and 500 mg/1000 mg, respectively.
Action
Pharmacology: The bactericidal component of Bactesyn is ampicillin which, like benzylpenicillin, acts against sensitive organisms during the stage of active multiplication by the inhibition of biosynthesis of cell wall mucopeptide.
The potential for 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 β-lactam antibiotic alone.
Biochemical studies with cell-free bacterial systems have shown sulbactam to be an irreversible inhibitor of several important β-lactamases that occur in penicillin-resistant organisms. It does not possess any useful antibacterial activity, except against Neisseriaceae.
Microbiology: Bactesyn is effective against a wide range of gram-positive and gram-negative bacteria including Staphylococcus aureus and epidermidis (including penicillin-resistant and some methicillin-resistant strains); Streptococcus pneumoniae, Streptococcus faecalis and other Streptococcus sp; Haemophilus influenzae and parainfluenzae (both β-lactamase-positive and -negative strains); Branhamella catarrhalis, anaerobes including Bacteroides fragilis and related species; Escherichia coli, Klebsiella, Proteus (both indole-positive and indole-negative) and Enterobacter spp; Morganella morganii; Citrobacter sp; Neisseria meningitidis and Neisseria gonorrhoeae.
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 IV dose of sulbactam and ampicillin. Administration following food does not affect the systemic bioavailability of sultamicillin. Peak serum levels of ampicillin following sultamicillin are approximately twice those of an equal dose of oral ampicillin. Elimination half-lives are approximately 0.75 and 1 hr 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.
Sulbactam/ampicillin diffuses readily into most body tissues and fluids in the human. Penetration into brain and spinal fluid is low except when meninges are inflamed. High concentrations of sulbactam and ampicillin are achieved in the blood following IV or IM administration and both components have a half-life of approximately 1 hr. Most of the sulbactam/ampicillin is excreted unchanged in the urine.
Indications/Uses
For infections caused by susceptible microorganisms. Typical indications are upper respiratory tract infections including sinusitis, otitis media, epiglotitis and tonsillitis; lower respiratory tract infections including bacterial pneumonias and bronchitis; urinary tract infections and pyelonephritis; intra-abdominal infections including peritonitis, cholecystitis, endometritis and pelvic cellulitis; skin and soft tissue infections and gonococcal infections; bacterial septicaemia; bone and joint infections.
For patients requiring sulbactam-ampicillin therapy following initial treatment with Bactesyn IM/IV.
Bactesyn IM/IV may also be administered preoperatively to reduce the incidence of postoperative wound infections in patients undergoing abdominal or pelvic surgery, in which peritoneal contamination may be present. In termination of pregnancy or caesarean section, Bactesyn IM/IV may be used prophylactically to reduce postoperative sepsis.
Dosage/Direction for Use
Tablet: Adults (including the elderly): Recommended Dose: 1-2 tabs (375-750 mg) twice daily. The dosage for most infections in children weighing <30 kg is 25-50 mg/kg/day in 2 divided doses depending on the severity of the infection and the physician's judgment. For children weighing >30 kg, the usual adult dose should be given.
In both adults and children, treatment is usually continued until 48 hrs 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 gonorrhoea, sultamicillin can be given as a single oral dose of 2.25 g (six 375-mg tabs). Concomitant probenecid 1 g should be administered in order to prolong plasma concentrations of sulbactam and ampicillin.
Cases of gonorrhoea with a suspected lesion of syphilis should have darkfield examinations before receiving sultamicillin and monthly serological tests for a minimum of 4 months.
It is recommended that there be at least a 10-day treatment for any infection caused by haemolytic streptococci to prevent the occurrence of acute rheumatic fever or glomerulonephritis.
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.
Vial: Bactesyn IM/IV can be administered by either IV or IM routes. The following dilutions may be used: See Table 1.


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For IV administration, Bactesyn IM/IV should be reconstituted with sterile water for injection or any compatible solution and allowed to stand to allow any formation to dissipate to permit visual inspection for complete dissolution. The dosage can be given by bolus injection over a minimum of 3 min or can be used in greater dilutions either as a bolus or as an IV infusion over 15-30 min. Bactesyn IM/IV may also be administered by deep IM injection; if pain is experienced, 0.5% sterile solution for injection of anhydrous lignocaine HCl may be used for reconstitution of the powder.
The usual dosage range of Bactesyn IM/IV in adults is 1.5-12 g/day in divided doses every 6-8 hrs up to a maximum daily dosage of sulbactam of 4 g. Less severe infections may be treated on 12-hourly schedule.
Daily Dose of Bactesyn IM/IV: Mild infection: 1.5-3 (0.5 + 1 to 1 + 2) g; moderate infection: Up to 6 (2 + 4) g; severe infection: Up to 12 (4 + 8) g.
The dosage of Bactesyn IM/IV for most infections in children, infants and neonates is 150 mg/kg/day (corresponding to sulbactam 50 mg/kg/day and ampicillin 100 mg/kg/day). In children, infants and neonates, dosing is usually every 6 or 8 hrs in accordance with the usual practice for ampicillin. In neonates during the 1st week of life (especially pre-terms), dosing is usually every 12 hrs. More or less frequent dosing may be indicated depending on the severity of the illness and the renal function of the patient. Treatment is usually continued until 48 hrs after pyrexia and other abnormal signs have resolved. Treatment is normally given for 5-14 days, but the treatment period may be extended or additional ampicillin may be administered in severely ill cases.
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 Bactesyn IM/IV in such patients should be administered less frequently in accordance with the usual practice for ampicillin. In treating patients on restricted sodium intake, it should be noted that Bactesyn 1500 mg IM/IV contains sodium approximately 115 mg (5 mmol).
For the prophylaxis of surgical infections, Bactesyn 1.5-3 g IM/IV should be given at induction of anaesthesia which allows sufficient time to achieve serum and tissue concentrations during the procedure. The dose may be repeated 6-8 hourly; administration is usually stopped 24 hrs after the majority of surgical procedures, unless a therapeutic course on Bactesyn IM/IV is indicated.
Bactesyn may be taken with or without food.
Contraindications
Individuals with a history of allergic reaction to any of the penicillins.
Warnings
Serious and occasionally fatal hypersensitivity (anaphylactic) reactions have been reported by patients on penicillin therapy. These reactions are more apt to occur in individuals with a history of penicillin hypersensitivity and/or hypersensitivity reactions to multiple allergens.
There have been reports of individuals with a history of penicillin hypersensitivity who have experienced severe reactions when treated with cephalosporins. 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, Bactesyn should be discontinued and the appropriate therapy instituted.
Serious anaphylactic reactions require immediate emergency treatment with adrenaline. Oxygen, IV steroids and airway management, including intubation, should be administered as indicated.
Special Precautions
As with any antibiotic preparations, constant observation for signs of overgrowth of nonsusceptible organisms, including fungi, is essential. Should superinfection occur, Bactesyn should be discontinued and/or appropriate therapy instituted.
It is advisable to check periodically for organ system dysfunction during therapy; this includes renal, hepatic and haematopoietic systems.
Use in pregnancy & lactation: Animal reproduction studies have revealed no evidence of impaired fertility or harm to the foetus due to sultamicillin. However, safety for use in human pregnancy and lactation has not been established.
Use in children: The principal route of excretion of sulbactam and ampicillin following oral administration of sultamicillin is via the urine. Because renal function is not fully developed in neonates, this should be considered when using sultamicillin in neonates.
Adverse Reactions
Sultamicillin is generally well tolerated. The majority of adverse effects observed were of mild or moderate severity and were normally tolerated with continued treatment.
Gastrointestinal: As with other ampicillin class antibiotics, the most frequent adverse effect observed was diarrhoea and/or loose stools. Enterocolitis and pseudomembranous colitis may rarely occur. Nausea and abdominal pain and/or cramps have been infrequently observed; epigastric distress and vomiting were rare.
Skin and/or Skin Structures: Rash and itching were infrequently observed.
Miscellaneous: Drowsiness and/or sedation, fatigue, malaise and headache have been rarely observed.
Since infectious mononucleosis is viral in origin, ampicillin should not be used in the treatment. A high percentage of patients with mononucleosis who received ampicillin developed a skin rash.
It is expected that the adverse reactions associated with use of ampicillin will occasionally be observed.
IM/IV: As with other parenteral antibiotics, the principal adverse effect observed is pain at the injection site, especially with the IM route of administration. A small number of patients may develop phlebitis after IV administration.
Caution For Usage
Stability and Compatibility: Sulbactam sodium is compatible with most IV solutions but ampicillin sodium and hence Bactesyn IM/IV is less stable in solutions containing dextrose or other carbohydrates and should not be mixed with blood products or protein hydrolysates. Ampicillin and hence Bactesyn IM/IV are incompatible with aminoglycosides and should not be physically mixed in the same container. The concentrated solution for IM administration should be used within 1 hr of reconstitution. Time periods for use in different diluents for IV infusion are as follows: See Table 2.


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Storage
Store below 30°C in a dry place.
MIMS Class
ATC Classification
J01CR04 - sultamicillin ; Belongs to the class of penicillin combinations, including beta-lactamase inhibitors. Used in the systemic treatment of infections.
J01CR01 - ampicillin and beta-lactamase inhibitor ; Belongs to the class of penicillin combinations, including beta-lactamase inhibitors. Used in the systemic treatment of infections.
Presentation/Packing
Tab 375 mg x 30's. Vial (IM/IV) 0.75 g x 1's. 1.5 g x 1's.
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