Effect of omeprazole on the pharmacokinetics of itraconazole

Eur J Clin Pharmacol. 1998 Apr;54(2):159-61. doi: 10.1007/s002280050438.

Abstract

Objective: To investigate the effect of omeprazole on the pharmacokinetics of itraconazole.

Methods: Eleven healthy volunteers received a single dose of oral itraconazole (200 mg) on days 1 and 15 and oral omeprazole (40 mg) once daily from day 2 to day 15. Itraconazole pharmacokinetics were studied on days 1 and 15.

Results: Concentrations of itraconazole were higher when it was taken alone than when it was taken with omeprazole. With concomitant omeprazole treatment, the mean AUC0-24 and Cmax of itraconazole were significantly reduced by 64% and 66%, respectively.

Conclusion: Omeprazole affects itraconazole kinetics, leading to a reduction in bioavailability and Cmax. These two drugs should not be used together.

Publication types

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

MeSH terms

  • Adult
  • Anti-Ulcer Agents / pharmacology*
  • Antifungal Agents / blood
  • Antifungal Agents / pharmacokinetics*
  • Biological Availability
  • Drug Interactions
  • Female
  • Humans
  • Itraconazole / blood
  • Itraconazole / pharmacokinetics*
  • Male
  • Omeprazole / pharmacology*
  • Reference Values

Substances

  • Anti-Ulcer Agents
  • Antifungal Agents
  • Itraconazole
  • Omeprazole