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Randomized Controlled Trial
. 2005 Nov;60(5):494-7.
doi: 10.1111/j.1365-2125.2005.02462.x.

Effects of grapefruit juice on the pharmacokinetics of pitavastatin and atorvastatin

Hitoshi Ando  1 , Shuichi Tsuruoka, Hayato Yanagihara, Koh-ichi Sugimoto, Masaaki Miyata, Yasushi Yamazoe, Toshinari Takamura, Shuichi Kaneko, Akio Fujimura
Affiliations
Randomized Controlled Trial

Effects of grapefruit juice on the pharmacokinetics of pitavastatin and atorvastatin

Hitoshi Ando et al. Br J Clin Pharmacol. 2005 Nov.

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.

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