Comparison of the serum and intracellular pharmacokinetics of azithromycin in healthy and diabetic volunteers

Pharmacotherapy. 2000 Jun;20(6):657-61. doi: 10.1592/phco.20.7.657.35176.

Abstract

Study objective: To compare serum and intracellular pharmacokinetics of azithromycin in healthy volunteers and patients with diabetes.

Design: Open-label, parallel study.

Setting: Clinical research center.

Subjects: Twelve patients with diabetes and 12 healthy volunteers.

Interventions: Subjects were given a single 500-mg dose of azithromycin followed by 250 mg/day for 2 days. Blood samples were obtained just before and after the third dose for up to 24 hours for serum and 168 hours for intracellular measurement of azithromycin.

Measurements and main results: Pharmacokinetic parameters were calculated by noncompartmental methods and compared with a t test. The groups did not differ in maximum concentration, time to maximum concentration, or area under the concentration-time curve in serum or polymorphonuclear cells (PMNs). Differences in the PMN:serum ratio were observed at the 24-hour time point (healthy 1209 +/- 432, diabetic 859 +/- 286, p=0.051).

Conclusion: In general, the pharmacokinetics of azithromycin are comparable in diabetics and healthy volunteers. Accumulation of drug in macrophages was slightly lower in patients.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Adult
  • Anti-Bacterial Agents / pharmacokinetics*
  • Azithromycin / pharmacokinetics*
  • Diabetes Mellitus / metabolism*
  • Female
  • Humans
  • Male
  • Neutrophils / metabolism*

Substances

  • Anti-Bacterial Agents
  • Azithromycin