Pharmacokinetics of cefotaxime in healthy volunteers and patients.

Cefotaxime is a third-generation cephalosporin that has maintained good susceptibility pattern despite its extensive use. It is available for intravenous and intramuscular administration. Its pharmacokinetic property includes a small volume of distribution with low protein binding. Cefotaxime's half-life is approximately 1.1 h, and it is primarily eliminated by the kidney. It has an active metabolite desacetyl-cefotaxime that displays pharmacokinetic properties similar to cefotaxime. Desacetyl-cefotaxime has a half-life of 1.5 h and also is eliminated by the kidneys by both glomerular filtration and active secretion. The half-life of cefotaxime and its metabolite is altered in patients with severe renal dysfunction requiring dosage adjustment. Despite its relatively short half-life, cefotaxime may be dosed every 12 h based on its pharmacokinetic and pharmacodynamic properties.