Source: Health Products Regulatory Authority (ZA) Revision Year: 2024 Publisher: Aurogen South Africa (Pty) Ltd, Woodhill Office Park, Building 1, 53 Phillip Engelbrecht Avenue, Meyersdal, Ext. 12, 1448, Johannesburg, South Africa
A 20.1.1 Broad and medium spectrum antibiotics
Piperacillin is a broad spectrum, semi-synthetic penicillin. It is active against many Gram-positive and Gram-negative aerobic and anaerobic bacteria, and exerts bactericidal activity by inhibition of both septum and cell wall synthesis. Tazobactam, a triazolylmethyl penicillanic acid sulfone, is an inhibitor of many β-lactamases, including the plasmid and chromosomally mediated enzymes. The antibiotic spectrum of piperacillin is enhanced and extended by the presence of tazobactam in the piperacillin/tazobactam formulation.
A wide range of gram-positive and gram-negative organisms are susceptible to RAZOBIN.
The following are resistant:
Peak plasma concentrations of piperacillin and tazobactam are attained immediately after completion of an intravenous infusion of RAZOBIN.
Piperacillin is metabolised to a minor microbiologically active desethyl metabolite. Tazobactam is metabolised to a single metabolite that lacks pharmacological and antibacterial activities.
Both piperacillin and tazobactam are eliminated via the kidney by glomerular filtration and tubular secretion. Piperacillin is excreted rapidly as unchanged substance, with 68% of the administered dose excreted in the urine. Tazobactam and its metabolite are eliminated primarily by renal excretion with 80% of the administered dose excreted as unchanged substance and the remainder as the single metabolite. Piperacillin, tazobactam and desethyl piperacillin are also secreted into the bile.
Both piperacillin and tazobactam are approximately 30% bound to plasma proteins. The protein binding of either piperacillin or tazobactam is unaffected by the presence of the other compound. Protein binding of the tazobactam metabolite is negligible.
Piperacillin and tazobactam are widely distributed into tissues and body fluids including intestinal mucosa, gallbladder, lung, female reproductive tissues (uterus, ovary, and fallopian tube), interstitial fluid, and bile. Mean tissue concentrations are generally 50% to 100% of those in plasma. Distribution of piperacillin and tazobactam into cerebrospinal fluid is low in subjects with non-inflamed meninges.
After the administration of single doses of piperacillin/tazobactam to subjects with renal impairment, the half-life of piperacillin and of tazobactam increases with decreasing creatinine clearance. The increase in half-life in two-fold and four-fold for piperacillin and tazobactam, respectively at creatinine clearance below 20mL/min compared to patients with normal renal function. Dosage adjustments for piperacillin and tazobactam are recommended in patients where creatinine clearance is below 40 mL/min receiving the usual recommended daily dose piperacillin and tazobactam (See "DOSAGE AND DIRECTIONS FOR USE").
The half-life of piperacillin and of tazobactam increases by approximately 25% and 18%, respectively, in patients with hepatic cirrhosis compared to healthy patients.
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