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Effects of grapefruit juice on the pharmacokinetics of pitavastatin and atorvastatin
Hitoshi Ando1, Shuichi Tsuruoka, Hayato Yanagihara
1Division of Clinical Pharmacology, Department of Pharmacology, Jichi Medical School, Tochigi 329-0498, Japan.
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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