![]() Drug Metab Dispos 1997 Nov 25(11): 1228–33įukuda K, Ohta T, Oshima Y, et al. Mechanisms of enhanced oral availability of CYP3A4 substrates by grapefruit constituents: decreased enterocyte CYP3A4 concentration and mechanism-based inactivation by furanocoumarins. Schmiedlin-Ren P, Edwards DJ, Fitzsimmons ME, et al. Identification of 60,70-dihydroxybergamottin, a cytochrome P450 inhibitor, in grapefruit juice. Chem Res Toxicol 1998 Apr 11(4): 252–9Įdwards DJ, Bellevue 3rd FH, Woster PM. Inactivation of cytochrome P450 3A4 by bergamottin, a component of grapefruit juice. Bergamottin contribution to the grapefruit juice-felodipine interaction and disposition in humans. Effect of grapefruit juice on blood cyclosporin concentration. Effect of grapefruit juice on cyclosporine pharmacokinetics in renal transplant patients. The effect of grapefruit juice on cyclosporine and prednisone metabolism in transplant patients. Hollander AA, van Rooij J, Lentjes GW, et al. Disposition of intravenous and oral cyclosporine after administration with grapefruit juice. Clin Pharmacol Ther 1997 Apr 61(4): 401–9ĭucharme MP, Warbasse LH, Edwards DJ. Grapefruit juiceterfenadine single-dose interaction: magnitude, mechanism, and relevance. Grapefruit juice alters the systemic bioavailability and cardiac repolarization of terfenadine in poor metabolizers of terfenadine. The cardiac effects of terfenadine after inhibition of its metabolism by grapefruit juice. Clin Pharmacol Ther 1996 Apr 59(4): 383–8Ĭlifford CP, Adams DA, Murray S, et al. Grapefruit juice alters terfenadine pharmacokinetics, resulting in prolongation of repolarization on the electrocardiogram. Eur J Drug Metab Pharmacokinet 1998 Jan-Mar 23(1): 55–9īenton RE, Honig PK, Zamani K, et al. Interaction between grapefruit juice and diazepam in humans. Interaction between grapefruit juice and midazolam in humans. Kupferschmidt HH, Ha HR, Ziegler WH, et al. Plasma concentrations of triazolam are increased by concomitant ingestion of grapefruit juice. Interaction of grapefruit juice and calcium channel blockers. Pharmacokinetic comparison of the potential over-the-counter statins simvastatin, lovastatin, fluvastatin and pravastatin. Interactions between grapefruit juice and cardiovascular drugs. Clin Invest Med 1989 Dec 12(6): 357–62īailey DG, Dresser GK. Ethanol enhances the hemodynamic effects of felodipine. Trends Genet 2001 Sep 17(9): 536–40īailey DG, Spence JD, Edgar B, et al. Oranges and lemons: clues to the taxonomy of Citrus from molecular markers. Citrus phylogeny and genetic origin of important species as investigated by molecular markers. Origin, evolution and breeding of the grapefruit. Grapefruit-drug interactions: can interactions with drugs be avoided? J Clin Pharmacol 2006 Dec 46(12): 1390–416 ![]() Mertens-Talcott SU, Zadezensky I, De Castro WV, et al. 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. ![]() The clinical significance of such interactions also depends on the disposition and toxicity profile of the drug being administered. It is therefore challenging to predict the extent of grapefruit product-drug interactions and to compare available in vitro and in vivo data. 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. Polyphenolic compounds such as flavonoids have been proposed as the causative agents of the P-gp and OATP interactions. organic anion-transporting polypeptides ). ![]() Grapefruit products have also been associated with interactions with P-glycoprotein (P-gp) and uptake transporters (e.g. 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 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. ![]()
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