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
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Randomized Controlled Trial
MeSH terms
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Adult
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Anticholesteremic Agents / pharmacokinetics*
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Area Under Curve
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Atorvastatin
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Beverages*
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Citrus paradisi / metabolism*
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Cross-Over Studies
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Cytochrome P-450 CYP3A
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Cytochrome P-450 Enzyme System / metabolism
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Enzyme Inhibitors / pharmacokinetics*
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Food-Drug Interactions / physiology
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Heptanoic Acids / pharmacokinetics*
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Humans
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Male
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Pyrroles / pharmacokinetics*
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Quinolines / pharmacokinetics*
Substances
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Anticholesteremic Agents
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Enzyme Inhibitors
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Heptanoic Acids
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Pyrroles
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Quinolines
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Cytochrome P-450 Enzyme System
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Atorvastatin
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CYP3A protein, human
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Cytochrome P-450 CYP3A
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CYP3A4 protein, human
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pitavastatin