Pharmacokinetic analysis of felodipine-grapefruit juice interaction based on an irreversible enzyme inhibition model
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منابع مشابه
Pharmacokinetic analysis of felodipine-grapefruit juice interaction based on an irreversible enzyme inhibition model.
UNLABELLED Aims Ingestion of grapefruit juice (GFJ) alters the pharmacokinetics of various orally administered drugs. Quantitative evaluation of this GFJ-drug interaction is required for the proper clinical management of patients. Methods Using felodipine as a model drug, we constructed a pharmacokinetic model based on irreversible inhibition of intestinal cytochrome P450 3A4 (CYP3A4) by GFJ. W...
متن کاملA furanocoumarin-free grapefruit juice establishes furanocoumarins as the mediators of the grapefruit juice-felodipine interaction.
BACKGROUND Grapefruit juice (GFJ) enhances the systemic exposure of numerous CYP3A4 drug substrates, including felodipine, by inhibiting intestinal (but not hepatic) first-pass metabolism. Furanocoumarins have been identified as major CYP3A4 inhibitors contained in the juice, but their contribution to the GFJ effect in vivo remains unclear. OBJECTIVE To ascertain whether furanocoumarins media...
متن کاملSeville orange juice-felodipine interaction: comparison with dilute grapefruit juice and involvement of furocoumarins.
OBJECTIVE Our objective was to determine whether Seville orange juice produces a grapefruit juice-like interaction with felodipine and whether bergamottin, 6',7'-dihydroxybergamottin, or other furocoumarins are involved. METHODS In a randomized three-way crossover design, 10 volunteers received a felodipine 10-mg extended-release tablet with 240 mL of Seville orange juice, dilute grapefruit j...
متن کاملBergamottin contribution to the grapefruit juice-felodipine interaction and disposition in humans.
OBJECTIVES Our objectives were to evaluate the contribution of bergamottin to the grapefruit juice-felodipine interaction and to characterize bergamottin disposition. METHODS In this study 250 mL grapefruit juice; 2-, 6-, or 12-mg capsules of bergamottin plus water; or water was administered with 5 mg extended-release felodipine to 11 volunteers in a partially randomized, 5-way crossover stud...
متن کاملRelationship between lipophilicities of 1,4-dihydropyridine derivatives and pharmacokinetic interaction strengths with grapefruit juice.
It is well known fact that the strengths of drug interactions with grapefruit juice (GFJ) differ greatly depending on the 1,4-dihydropyridine calcium channel antagonist (DHP) used. However, there are no available data on the relationship between interactions with GFJ and its physicochemical attributes. Therefore we endeavored to study the correlation between calculated logP values, indicating l...
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ژورنال
عنوان ژورنال: British Journal of Clinical Pharmacology
سال: 2000
ISSN: 0306-5251
DOI: 10.1046/j.1365-2125.2000.00140.x