Seville orange juice-felodipine interaction: Comparison with dilute grapefruit juice and involvement of furocoumarins

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Seville 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...

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A 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...

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6',7'-Dihydroxybergamottin in grapefruit juice and Seville orange juice: effects on cyclosporine disposition, enterocyte CYP3A4, and P-glycoprotein.

BACKGROUND 6',7'-Dihydroxybergamottin is a furanocoumarin that inhibits CYP3A4 and is found in grapefruit juice and Seville orange juice. Grapefruit juice increases the oral bioavailability of many CYP3A4 substrates, including cyclosporine (INN, ciclosporin), but intestinal P-glycoprotein may be a more important determinant of cyclosporine availability. OBJECTIVES To evaluate the contribution...

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Interaction between Grapefruit Juice and Drugs*

There is a possibility that even a glass of grapefruit juice (GFJ) taken several hours before oral medication may enhance the bioavailability of many drugs, exaggerate the drug action, and increase the toxic effect by exaggerating the potency of the drug. This can be explained by inhibition of CYP3A4 in the small intestine by GFJ, thus suppressing drug metabolism. This interaction with GFJ is l...

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Bergamottin 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...

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ژورنال

عنوان ژورنال: Clinical Pharmacology & Therapeutics

سال: 2001

ISSN: 0009-9236

DOI: 10.1067/mcp.2001.113185