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Effects of grapefruit juice on the pharmacokinetics of pitavastatin and atorvastatin
Author(s) -
Ando Hitoshi,
Tsuruoka Shuichi,
Yanagihara Hayato,
Sugimoto Kohichi,
Miyata Masaaki,
Yamazoe Yasushi,
Takamura Toshinari,
Kaneko Shuichi,
Fujimura Akio
Publication year - 2005
Publication title -
british journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.216
H-Index - 146
eISSN - 1365-2125
pISSN - 0306-5251
DOI - 10.1111/j.1365-2125.2005.02462.x
Subject(s) - pitavastatin , atorvastatin , grapefruit juice , crossover study , pharmacology , pharmacokinetics , citrus paradisi , cyp3a4 , chemistry , bioavailability , medicine , metabolism , biochemistry , cytochrome p450 , biology , alternative medicine , pathology , rutaceae , horticulture , placebo
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.