Pharmacokinetics of cefotaxime in healthy volunteers and patients

Diagn Microbiol Infect Dis. 1995 May-Jun;22(1-2):49-55. doi: 10.1016/0732-8893(95)00072-i.

Abstract

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.

MeSH terms

  • Cefotaxime / analogs & derivatives*
  • Cefotaxime / metabolism
  • Cefotaxime / pharmacokinetics*
  • Cefotaxime / therapeutic use
  • Cephalosporins / metabolism
  • Cephalosporins / pharmacokinetics*
  • Cephalosporins / therapeutic use
  • Clinical Trials as Topic
  • Dose-Response Relationship, Drug
  • Gram-Negative Bacterial Infections / drug therapy*
  • Gram-Negative Bacterial Infections / metabolism
  • Humans
  • Microbial Sensitivity Tests
  • Reference Values

Substances

  • Cephalosporins
  • desacetylcefotaxime
  • Cefotaxime