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Interactions Between Grapefruit Juice and Cardiovascular Drugs

Interactions Between Grapefruit Juice and Cardiovascular Drugs Grapefruit juice can alter oral drug pharmacokinetics by different mechanisms. Irreversible inactivation of intestinal cytochrome P450 (CYP) 3A4 is produced by commercial grapefruit juice given as a single normal amount (e. g. 200–300mL) or by whole fresh fruit segments. As a result, presystemic metabolism is reduced and oral drug bioavailability increased. Enhanced oral drug bioavailability can occur 24 hours after juice consumption. Inhibition of P-glycoprotein (P-gp) is a possible mechanism that increases oral drug bioavailability by reducing intestinal and/or hepatic efflux transport. Recently, inhibition of organic anion transporting polypeptides by grapefruit juice was observed in vitro; intestinal uptake transport appeared decreased as oral drug bioavailability was reduced. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png American Journal of Cardiovascular Drugs Springer Journals

Interactions Between Grapefruit Juice and Cardiovascular Drugs

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References (114)

Publisher
Springer Journals
Copyright
Copyright © 2004 by Adis Data Information BV
Subject
Pharmacy; Pharmacy
ISSN
1175-3277
eISSN
1179-187X
DOI
10.2165/00129784-200404050-00002
pmid
15449971
Publisher site
See Article on Publisher Site

Abstract

Grapefruit juice can alter oral drug pharmacokinetics by different mechanisms. Irreversible inactivation of intestinal cytochrome P450 (CYP) 3A4 is produced by commercial grapefruit juice given as a single normal amount (e. g. 200–300mL) or by whole fresh fruit segments. As a result, presystemic metabolism is reduced and oral drug bioavailability increased. Enhanced oral drug bioavailability can occur 24 hours after juice consumption. Inhibition of P-glycoprotein (P-gp) is a possible mechanism that increases oral drug bioavailability by reducing intestinal and/or hepatic efflux transport. Recently, inhibition of organic anion transporting polypeptides by grapefruit juice was observed in vitro; intestinal uptake transport appeared decreased as oral drug bioavailability was reduced.

Journal

American Journal of Cardiovascular DrugsSpringer Journals

Published: Aug 17, 2012

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