Grapefruit juice has been shown to reduce levels of fexofenadine, and increase levels of quinidine. It is unclear whether this applies to intestinal P-gp, for which digoxin is not considered to be a sensitive probe. Two small clinical studies in healthy adults using digoxin as a probe substrate show that grapefruit juice does not inhibit P-gp in the kidneys. While most in vitro research shows that grapefruit products inhibit P-gp, research in humans is less clear. Theoretically, it might inhibit intestinal P-gp, but evidence is conflicting. Grapefruit juice does not seem to affect renal P-glycoprotein (P-gp). Application of cryopreserved human intestinal mucosa and cryopreserved human enterocytes in the evaluation of herb-drug interactions: evaluation of CYP3A inhibitory potential of grapefruit juice and commercial f Loretz C, Ho MD, Alam N, Mitchell W, Li AP.Is the clinical relevance of drug-food and drug-herb interactions limited to grapefruit juice and Saint-John's Wort? Pharmacol Res. Mouly S, Lloret-Linares C, Sellire PO, Sene D, Bergmann JF.Predicting clinical relevance of grapefruit-drug interactions: a complicated process. Comparison of inhibitory duration of grapefruit juice on organic anion-transporting polypeptide and cytochrome P450 3A4. Tanaka S, Uchida S, Miyakawa S, Inui N, Takeuchi K, Watanabe H, Namiki N.Pharmacokinetic and pharmacodynamic interaction between grapefruit juice and halofantrine. Charbit, B., Becquemont, L., Lepere, B., Peytavin, G., and Funck-Brentano, C.The effects of grapefruit juice on the pharmacokinetics of erythromycin. Effects of grapefruit juice and smoking on verapamil concentrations in steady state. Fuhr U, Muller-Peltzer H, Kern R, et al.Effects of grapefruit juice on the pharmacokinetics of sildenafil.
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