Effects of grapefruit juice on the pharmacokinetics of pitavastatin and atorvastatin

Br J Clin Pharmacol. 2005 Nov;60(5):494-7. doi: 10.1111/j.1365-2125.2005.02462.x.

Abstract

Aims: To compare the effects of grapefruit juice (GFJ) on the pharmacokinetics of pitavastatin and atorvastatin.

Methods: In a randomized, four-phase crossover study, eight healthy subjects consumed either GFJ or water t.i.d. for 4 days in each trial. On each final day, a single dose of 4 mg pitavastatin or 20 mg atorvastatin was administered.

Results: GFJ increased the mean AUC(0-24) of atorvastatin acid by 83% (95% CI 23-144%) and that of pitavastatin acid by 13% (-3 to 29%).

Conclusions: Pitavastatin, unlike atorvastatin, appears to be scarcely affected by the CYP3A4-mediated metabolism.

Publication types

  • Randomized Controlled Trial

MeSH terms

  • Adult
  • Anticholesteremic Agents / pharmacokinetics*
  • Area Under Curve
  • Atorvastatin
  • Beverages*
  • Citrus paradisi / metabolism*
  • Cross-Over Studies
  • Cytochrome P-450 CYP3A
  • Cytochrome P-450 Enzyme System / metabolism
  • Enzyme Inhibitors / pharmacokinetics*
  • Food-Drug Interactions / physiology
  • Heptanoic Acids / pharmacokinetics*
  • Humans
  • Male
  • Pyrroles / pharmacokinetics*
  • Quinolines / pharmacokinetics*

Substances

  • Anticholesteremic Agents
  • Enzyme Inhibitors
  • Heptanoic Acids
  • Pyrroles
  • Quinolines
  • Cytochrome P-450 Enzyme System
  • Atorvastatin
  • CYP3A protein, human
  • Cytochrome P-450 CYP3A
  • CYP3A4 protein, human
  • pitavastatin