Specificity of Chemical Constituents in Grapefruit Juice Which Are Known to Inhibit CYP3A4 Activity.
نویسندگان
چکیده
منابع مشابه
Two major grapefruit juice components differ in time to onset of intestinal CYP3A4 inhibition.
Grapefruit juice elevates blood levels of some drugs taken orally, primarily by inhibiting intestinal CYP3A4-mediated first-pass metabolism. Two prominent furanocoumarins in the juice, 6',7'-dihydroxybergamottin (DHB) and bergamottin (BG), have been demonstrated as important contributors to grapefruit juice-drug interactions. Using CYP3A4-expressing Caco-2 cells and representative probes from d...
متن کاملTwo major grapefruit juice components differ in intestinal CYP3A4 inhibition kinetic and binding properties.
Bergamottin (BG) and 6',7'-dihydroxybergamottin (DHB) are the most abundant furanocoumarins present in grapefruit juice and have been proposed as major intestinal CYP3A4 inhibitors contributing to grapefruit juice-drug interactions. The relative contribution of BG versus DHB to the interaction potential is unclear, in part due to inconsistencies in the literature regarding inhibitory potency. T...
متن کامل6',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...
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 ...
متن کاملMechanism-based inhibition of recombinant human cytochrome P450 3A4 by tomato juice extract.
This study investigates whether tomato juice can inhibit cytochrome P450 (CYP) 3A4-mediated drug metabolism. Three commercially available, additive-free tomato juices, along with homogenized fresh tomato, were analyzed for their ability to inhibit testosterone 6β-hydroxylation activity using human recombinant CYP3A4. Results were compared to that of grapefruit juice. Ethyl acetate extracts of t...
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ژورنال
عنوان ژورنال: Rinsho yakuri/Japanese Journal of Clinical Pharmacology and Therapeutics
سال: 1999
ISSN: 1882-8272,0388-1601
DOI: 10.3999/jscpt.30.113