Intrapulmonary steady-state concentrations of clarithromycin and azithromycin in healthy adult volunteers

Antimicrob Agents Chemother. 1997 Jun;41(6):1399-402. doi: 10.1128/AAC.41.6.1399.

Abstract

The steady-state concentrations of clarithromycin and azithromycin in plasma were compared with concomitant concentrations in epithelial lining fluid (ELF) and alveolar macrophages (AM) obtained in intrapulmonary samples during bronchoscopy and bronchoalveolar lavage from 40 healthy, nonsmoking adult volunteers. Mean plasma clarithromycin, 14-(R)-hydroxyclarithromycin, and azithromycin concentrations were similar to those previously reported. Clarithromycin was extensively concentrated in ELF (range of mean +/- standard deviation concentrations, 34.4 +/- 29.3 microg/ml at 4 h to 4.6 +/- 3.7 microg/ml at 24 h) and AM (480 +/- 533 microg/ml at 4 h to 99 +/- 50 microg/ml at 24 h). The concentrations of azithromycin in ELF were 1.01 +/- 0.45 microg/ml at 4 h to 1.22 +/- 0.59 microg/ml at 24 h, and those in AM were 42.7 +/- 28.7 microg/ml at 4 h to 41.7 +/- 12.1 microg/ml at 24 h. The concentrations of 14-(R)-hydroxyclarithromycin in the AM ranged from 89.3 +/- 52.8 microg/ml at 4 h to 31.3 +/- 17.7 microg/ml at 24 h. During the period of 24 h after drug administration, azithromycin and clarithromycin achieved mean concentrations in ELF and AM higher than the concomitant concentrations in plasma.

Publication types

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

MeSH terms

  • Administration, Oral
  • Adolescent
  • Adult
  • Anti-Bacterial Agents / blood
  • Anti-Bacterial Agents / metabolism
  • Anti-Bacterial Agents / pharmacokinetics*
  • Azithromycin / blood
  • Azithromycin / metabolism
  • Azithromycin / pharmacokinetics*
  • Bronchoalveolar Lavage Fluid / chemistry
  • Clarithromycin / analogs & derivatives
  • Clarithromycin / blood
  • Clarithromycin / metabolism
  • Clarithromycin / pharmacokinetics*
  • Drug Administration Schedule
  • Epithelium / metabolism
  • Female
  • Humans
  • Lung / metabolism*
  • Macrophages, Alveolar / metabolism*
  • Male
  • Middle Aged

Substances

  • Anti-Bacterial Agents
  • 14-hydroxyclarithromycin
  • Azithromycin
  • Clarithromycin