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Pharmacology: Pharmacodynamics and Pharmacokinetics: Peak plasma concentrations of Piperacillin and Tazobactam are attained immediately after completion of an intravenous infusion of Piperacillin/Tazobactam.
Steady state plasma concentrations were not different from those attained after the first dose when 2.25 g or 4.5 g doses of Piperacillin/Tazobactam were administered via 30 minute infusions every 6 hours.
Piperacillin is metabolized to a minor microbiologically active desethyl metabolite. Tazobactam is metabolized 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 drug 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 drug 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.
Piperacillin and Tazobactam are widely distributed into tissues and body fluids including intestinal mucosa, gallbladder, lungs, female reproductive tissues (uterus, ovary, and fallopian tube), interstitial fluid, and bile.
