Pharmacokinetics and tissue tolerance of azithromycin after intramuscular administration to rabbits

Res Vet Sci. 2006 Dec;81(3):366-72. doi: 10.1016/j.rvsc.2006.01.006. Epub 2006 Mar 10.

Abstract

The pharmacokinetics of azithromycin after intravenous and intramuscular injection at a single dose rate of 10mg/kg bodyweight were investigated in rabbits by using a modified agar diffusion bioassay for determining plasma concentrations. The plasma creatine kinase activity was determined after i.m. administration for the evaluation of the tissue tolerance. The elimination half-lives of azithromycin after intravenous and intramuscular administration were 24.1 and 25.1h, respectively. After intramuscular administration mean peak plasma concentration was 0.26+/-0.01 mg/L and bioavailability was 97.7%. Plasma CK activity rose sharply within 8h after i.m. injection of azithromycin; activity returned to pre-treatment level by 48-72 h post-treatment. The transient rise in serum CK activity indicates some degree of muscle tissue damage at the injection site.

Publication types

  • Clinical Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Bacterial Agents / administration & dosage*
  • Anti-Bacterial Agents / adverse effects
  • Anti-Bacterial Agents / blood
  • Anti-Bacterial Agents / pharmacokinetics*
  • Azithromycin / administration & dosage*
  • Azithromycin / adverse effects
  • Azithromycin / blood
  • Azithromycin / pharmacokinetics*
  • Cross-Over Studies
  • Dose-Response Relationship, Drug
  • Female
  • Injections, Intramuscular
  • Injections, Intravenous
  • Male
  • Rabbits / metabolism*
  • Random Allocation

Substances

  • Anti-Bacterial Agents
  • Azithromycin