The steady-state disposition of indinavir is not altered by the concomitant administration of clarithromycin

Clin Pharmacol Ther. 2000 Apr;67(4):351-9. doi: 10.1067/mcp.2000.105151.

Abstract

Study objectives: To evaluate the safety and potential pharmacokinetic interaction between indinavir and clarithromycin.

Study methods: In a randomized, three-period, crossover fashion, 12 healthy adults received the following for 1 week: 800 mg oral indinavir sulfate every 8 hours with placebo, 500 mg oral clarithromycin every 12 hours with placebo, and indinavir sulfate with clarithromycin. Plasma indinavir, clarithromycin, and 14-hydroxyclarithromycin concentrations were determined after the last dose in each treatment period.

Results: Administration of indinavir sulfate with clarithromycin caused a statistically significant increase in four pharmacokinetic parameters: a 58% increase in plasma indinavir concentrations at 8 hours (P = .029), a 47% increase in values for clarithromycin area under the plasma concentration versus time curve from time zero to the last measured concentration [AUC(0-12h); P = .0002], and 49% and 48% decreases in 14-hydroxyclarithromycin AUC(0-12h) and maximum plasma concentration (Cmax) values, respectively (P = .0001 and P = .0001). These effects are not considered to be clinically significant in view of the insignificant effects on the values for indinavir area under the plasma concentration versus time curve from time zero to the last measured concentration [AUC(0-8h)] and Cmax, as well as the safety profile of clarithromycin.

Conclusions: The combination of indinavir sulfate and clarithromycin is generally well tolerated and can be coadministered without dose adjustment.

Publication types

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

MeSH terms

  • Administration, Oral
  • Adult
  • Anti-Bacterial Agents / blood
  • Anti-Bacterial Agents / pharmacokinetics*
  • Area Under Curve
  • Calcium / urine
  • Chromatography, High Pressure Liquid
  • Clarithromycin / analogs & derivatives
  • Clarithromycin / blood
  • Clarithromycin / pharmacokinetics*
  • Cross-Over Studies
  • Drug Interactions
  • HIV Protease Inhibitors / blood
  • HIV Protease Inhibitors / pharmacokinetics*
  • Humans
  • Indinavir / blood
  • Indinavir / pharmacokinetics*
  • Male
  • Uric Acid / urine

Substances

  • Anti-Bacterial Agents
  • HIV Protease Inhibitors
  • 14-hydroxyclarithromycin
  • Uric Acid
  • Indinavir
  • Clarithromycin
  • Calcium