Pharmacokinetics of cefotaxime in normal human volunteers

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Abstract
The pharmacokinetic parameters of cefotaxime after either intramuscular (Lm.) or intravenous (i.v.) administration were determined in several studies involving about 200 healthy volunteers. In single-dose studies, the pharmacokinetics of cefotaxime appeared to be linear and dose-independent for doses up to 2 g. The mean peak concentration in serum after i.m. injection of 1 g of cefotaxime was ≃22 μg/ml at 0.5 h, whereas the level at 6 h was ≃1.5 μg. After i.v. bolus injection of 1 g of cefotaxime, the mean peak level was ≃105 μg, with an apparent volume of distribution of ≃25 1. After i.v. infusion serum levels ranged from ≃15 μg to ≃40μg, depending on the duration of infusion. Cefotaxime is rapidly eliminated: serum half-life ranged from 0.92 to 1.35 h after 1 g i.m. injection, and from 0.84 to 1.25 h after i.v. injection (terminal phase), the majority of the dose being excreted unchanged in the urine (≃51% within 8 h). Protein binding of cefotaxime ranged from 35 to 45 %. Thus the pharmacokinetic profile of cefotaxime was similar to that reported for cefoxitin, cefamandole and cefuroxime. Co-administration of lignocaine had no significant effect on the absorption and elimination kinetics of cefotaxime while probenecid increased and sustained plasma levels, acting primarily by inhibition of renal tubular secretion. In multiple-dose studies, cefotaxime was administered i.m. and i.v. at different doses, dosing intervals and for periods of 6 to 14 days. There was no evidence that the administration of cefotaxime up to 1 g 6-hourly for 14 days caused any significant accumulation in healthy volunteers.

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