Effects of grapefruit juice on the pharmacokinetics of pitavastatin and atorvastatin.
OBJECTIVE
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.
Ando
Hitoshi
H
Division of Clinical Pharmacology, Department of Pharmacology, Jichi Medical School, Tochigi 329-0498, Japan.
Tsuruoka
Shuichi
S
Yanagihara
Hayato
H
Sugimoto
Koh-ichi
K
Miyata
Masaaki
M
Yamazoe
Yasushi
Y
Takamura
Toshinari
T
Kaneko
Shuichi
S
Fujimura
Akio
A
D000328:Adult; D000924:Anticholesteremic Agents / Q000493:pharmacokinetics*; D019540:Area Under Curve; D000069059:Atorvastatin; D001628:Beverages; D032083:Citrus paradisi / Q000378:metabolism*; D018592:Cross-Over Studies; D051544:Cytochrome P-450 CYP3A; D003577:Cytochrome P-450 Enzyme System / Q000378:metabolism; D004791:Enzyme Inhibitors / Q000493:pharmacokinetics*; D018565:Food-Drug Interactions / Q000502:physiology; D006538:Heptanoic Acids / Q000493:pharmacokinetics*; D006801:Humans; D008297:Male; D011758:Pyrroles / Q000493:pharmacokinetics*; D011804:Quinolines / Q000493:pharmacokinetics*
D000924:Anticholesteremic Agents; D004791:Enzyme Inhibitors; D006538:Heptanoic Acids; D011758:Pyrroles; D011804:Quinolines; D003577:Cytochrome P-450 Enzyme System; D000069059:Atorvastatin; C104464:CYP3A protein, human; D051544:Cytochrome P-450 CYP3A; C510163:CYP3A4 protein, human; C108475:pitavastatin