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Drugs
Erschienen in: Drugs 18/2010

01.12.2010 | Review Article

Grapefruit-Drug Interactions

verfasst von: Miss Kay Seden, Laura Dickinson, Saye Khoo, David Back

Erschienen in: Drugs | Ausgabe 18/2010

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Abstract

Grapefruit juice and grapefruit product consumption have potential health benefits; however, their intake is also associated with interactions with certain drugs, including calcium channel blockers, immunosuppressants and antihistamines. The primary mechanism through which interactions are mediated is mechanism-based intestinal cytochrome P450 3A4 inhibition by furanocoumarins resulting in increased bioavailability of administered medications that are substrates. Grapefruit products have also been associated with interactions with P-glycoprotein (P-gp) and uptake transporters (e.g. organic anion-transporting polypeptides [OATPs]). Polyphenolic compounds such as flavonoids have been proposed as the causative agents of the P-gp and OATP interactions. The mechanisms and magnitudes of the interactions can be influenced by the concentrations of furanocoumarins and flavonoids in the grapefruit product, the volume of juice consumed, and the inherent variability of specific enzymes and transporter components in humans. It is therefore challenging to predict the extent of grapefruit product-drug interactions and to compare available in vitro and in vivo data. The clinical significance of such interactions also depends on the disposition and toxicity profile of the drug being administered. The aim of this review is to outline the mechanisms of grapefruit-drug interactions and present a comprehensive summary of those agents affected and whether they are likely to be of clinical relevance.
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Metadaten
Titel
Grapefruit-Drug Interactions
verfasst von
Miss Kay Seden
Laura Dickinson
Saye Khoo
David Back
Publikationsdatum
01.12.2010
Verlag
Springer International Publishing
Erschienen in
Drugs / Ausgabe 18/2010
Print ISSN: 0012-6667
Elektronische ISSN: 1179-1950
DOI
https://doi.org/10.2165/11585250-000000000-00000

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