Grapefruit juice increases felodipine oral availability in humans by decreasing intestinal CYP3A protein expression.
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چکیده
منابع مشابه
Grapefruit juice increases felodipine oral availability in humans by decreasing intestinal CYP3A protein expression.
The increase in oral availability of felodipine and other commonly used medications when taken with grapefruit juice has been assumed to be due to inhibition of CYP3A4, a cytochrome P450 that is present in liver and intestine. To evaluate the effect of repeated grapefruit juice ingestion on CYP3A4 expression, 10 healthy men were given 8 oz of grapefruit juice three times a day for 6 d. Before a...
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 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 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 کاملGrapefruit juice-drug interactions.
The novel finding that grapefruit juice can markedly augment oral drug bioavailability was based on an unexpected observation from an interaction study between the dihydropyridine calcium channel antagonist, felodipine, and ethanol in which grapefruit juice was used to mask the taste of the ethanol. Subsequent investigations showed that grapefruit juice acted by reducing presystemic felodipine ...
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ژورنال
عنوان ژورنال: Journal of Clinical Investigation
سال: 1997
ISSN: 0021-9738
DOI: 10.1172/jci119439