Effect of grapefruit juice on clarithromycin pharmacokinetics

Antimicrob Agents Chemother. 1998 Apr;42(4):927-9. doi: 10.1128/AAC.42.4.927.

Abstract

To investigate whether grapefruit juice inhibits the metabolism of clarithromycin, 12 healthy subjects were given water or grapefruit juice before and after a clarithromycin dose of 500 mg in a randomized crossover study. Administration of grapefruit juice increased the time to peak concentration of both clarithromycin (82 +/- 35 versus 148 +/- 83 min; P = 0.02) and 14-hydroxyclarithromycin (84 +/- 38 min versus 173 +/- 85; P = 0.01) but did not affect other pharmacokinetic parameters.

Publication types

  • Clinical Trial
  • Randomized Controlled Trial

MeSH terms

  • Adult
  • Anti-Bacterial Agents / pharmacokinetics*
  • Area Under Curve
  • Beverages*
  • Citrus / chemistry*
  • Clarithromycin / pharmacokinetics*
  • Cross-Over Studies
  • Cytochrome P-450 CYP3A
  • Cytochrome P-450 Enzyme System / metabolism
  • Female
  • Food-Drug Interactions
  • Humans
  • Male
  • Mixed Function Oxygenases / metabolism

Substances

  • Anti-Bacterial Agents
  • Cytochrome P-450 Enzyme System
  • Mixed Function Oxygenases
  • CYP3A protein, human
  • Cytochrome P-450 CYP3A
  • Clarithromycin