Amsul

Ampicillin sodium, sulbactam sodium.

Each 750 mg vial contains: Ampicillin Sodium 500 mg, Sulbactam Sodium 250 mg.
Each 1.5 g vial contains: Ampicillin Sodium 1000 mg, Sulbactam Sodium 500 mg.
Ampicillin Sodium is a white to off-white, crystalline powder, hygroscopic and has a molecular weight of 371.39.

Pharmacology: Pharmacokinetics: Peak plasma concentrations of ampicillin after a 500-mg intramuscular dose given as the sodium salt occur within about 1 hour and are reported to range from 7 to 14 micrograms/mL. Ampicillin is widely distributed and therapeutic concentrations can be achieved in ascitic, pleural, and joint fluids. It crosses the placenta and small amounts are distributed into breast milk. There is little diffusion into the CSF except when the meninges are inflamed. About 20% is bound to plasma proteins and the plasma half-life is about 1 to 1.5 hours, but this may be increased in neonates, the elderly, and patients with renal impairment; in severe renal impairment half-lives of 7 to 20 hours have been reported. Ampicillin is metabolised to some extent to penicilloic acid which is excreted in the urine. Renal clearance of ampicillin occurs partly by glomerular filtration and partly by tubular secretion; it is reduced by probenecid. About 20 to 40% of an oral dose may be excreted unchanged in the urine in 6 hours; urinary concentrations have ranged from 0.25 to 1 mg/mL after a dose of 500 mg. After parenteral use about 60 to 80% is excreted in the urine within 6 hours. Ampicillin is removed by haemodialysis. High concentrations are reached in bile; it undergoes enterohepatic recycling and some is excreted in the faeces.
Sulbactam is poorly absorbed from the gastrointestinal tract and is given by injection as a sodium salt. It has pharmacokinetic characteristics in humans similar to those of ampicillin and amoxicillin. Its half life in humans is approximately 1 hour. In a two compartment pharmacokinetic model, the apparent volume of distribution for the central compartment is approximately 12 liters, and half of the dose is found in the central compartment in the post distributive phase. After a 30 minutes infusion of 500 mg of Sulbactam, a peak serum concentration of approximately 20 μg/mL was obtained; 1,000 mg produced a peak of 43 μg/mL. The half-life for elimination was about 1 hour. Approximately 75% of a parenteral dose is excreted unchanged in urine.

Ampicillin + Sulbactam is indicated for infections where beta-lactamase production is suspected. Typical indications are upper and lower respiratory tract infections including sinusitis, otitis media and epiglottitis; bacterial pneumonia; urinary tract infections and pyelonephritis; intra-abdominal infections including peritonitis, cholecystitis, endometritis and pelvic cellulitis; bacterial septicemia; skin; soft tissue, bone and joint infections and gonococcal infections.
It may also be administered pre-operatively to reduce the incidence of post-operative wound infections in patients undergoing abdominal or pelvic surgery, in which peritoneal contamination may be present. In termination of pregnancy or caesarian section, Ampicillin + Sulbactam may be used as prophylaxis to reduce postoperative sepsis.

1.5 to 12 g/day in divided doses.
Mild infections: 1.5 g to 3 g.
Moderate infections: up to 6 g.
Severe infections: up to 12 g.
Neonate: 150 mg/kg/day.
Or as prescribed by the Physician.

The use of this combination is contraindicated in individuals with a history of an allergic reaction to any of the penicillins.

Serious and occasionally fatal hypersensitivity (anaphylactic) reactions have been reported in patients on penicillin therapy.
These reactions are more to occur in individuals with a history of penicillin hypersensitivity who have experienced severe reactions when treated with cephalosporins.
Before therapy with penicillin, careful inquiry should be made concerning previous hypersensitivity reactions to penicillins, cephalosporins and other allergens. If allergic reactions occur, the drug should be discontinued and the appropriate therapy instituted.
Serious anaphylactic reactions required immediate emergency treatment with adrenaline. Oxygen, intravenous steroids and airway management, including intubations should be administered as indicated.

As with any antibiotic preparation, constant observation for signs of overgrowth of non-susceptible organisms, including fungi, is essential. Should super infection occur, the drug should be discontinued and/or appropriate therapy instituted. As with any potent systemic agent, it is advisable to check periodically for organ system dysfunction during extended therapy; this includes renal, hepatic, and hematopoietic systems. This is particularly important in neonates, especially when premature and other infants.

Animal re-production studies have revealed no evidence of impaired fertility to harm to the fetus due to Sulbactam and Ampicillin. However, safety for use in pregnancy and lactation has not been established.

As with other parenteral antibiotics, the principal side effects observed is injection site pain, especially associated with the intramuscularly route of administration. A small number of patients may develop phlebitis after intravenous administration.
Gastro-intestinal: the most common are nausea, vomiting and diarrhea.
Skin/skin structure: the most common are rash, itching and other skin reactions.
Hematopoietic and Lymphatic System: anemia, thrombocytopenia, eosinophilia and leukopenia have been reported during therapy with sulbactam Ampicillin/Sulbactam sodium. These reactions are reversible on discontinuation of therapy and believed to be sensitivity reactions.
Hepatic: transient elevations of alanine and aspartic transaminases have been observed.
It is expected that the adverse reaction associated with the use of ampicillin will be occasionally observed.

Directions for Reconstitution: Solution is prepared immediately before use by addition of 10 mL water for injection. Prepared solution must be used immediately. Discard remaining solution after use.
Incompatibility: Do not use as an additive with any other drug. Do not mix in any solutions other than those specifically recommended. Some drugs may be administered through the Y-tubing in small amounts.

Store at temperatures not exceeding 30°C. Protect from moisture.

Penicillins

J01CR01 - ampicillin and beta-lactamase inhibitor ; Belongs to the class of penicillin combinations, including beta-lactamase inhibitors. Used in the systemic treatment of infections.

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