![]() The mean AUC(0-24) of diazepam was increased 3.2-fold (P < 0.001) and Cmax was increased 1.5-fold (P < 0.05) by the grapefruit juice. Blood samples were collected for a 24 h period, and whole blood concentrations of diazepam were measured enzyme immunoassay. Oral (5 mg) diazepam was administered with either 250 ml water and grapefruit juice. Eight healthy male and female subjects participated in this study. In this study, our aim was to investigate the effects of grapefruit juice on plasma concentrations of diazepam. Because these drugs are metabolized by the hepatic cytochrome P450 isozyme (CYP) 3A4, the inhibitory effect of grapefruit juice is thought to results from inhibition of CYP3A4. Grapefruit juice has been reported to markedly improve the bioavailability of triazolam, midazolam, terfenadine, cyclosporine and several dihydropyridine calcium channel blockers including felodipine, nifedipine, nitrendipine and nisoldipine. Ozdemir M, Aktan Y, Boydag BS, Cingi MI, Musmul A.ĭepartment of Pharmacology, Medical Faculty, University of Osmangazi, Eskisehir, Turkey. Interaction between grapefruit juice and diazepam in humans. ![]() The present study shows that grapefruit juice is unlikely to affect pharmacokinetics or pharmacodynamics of alprazolam due to its high bioavailability.Įur J Drug Metab Pharmacokinet. Grapefruit juice altered neither the steady-state plasma concentration of alprazolam nor the clinical status in patients. Blood samples were collected before and during grapefruit juice ingestion and 1 week after its discontinuation together with an assessment of clinical status. In study 2, 11 patients with anxiety disorders receiving alprazolam (0.8-2.4 mg/day) ingested grapefruit juice (600 ml/day) for 7 days. Grapefruit juice altered neither the plasma concentrations of alprazolam at any time points, any pharmacokinetic parameters, nor the majority of psychomotor function parameters in subjects. Plasma drug concentrations were monitored up to 48 h after alprazolam dosing together with evaluation of psychomotor function. In study 1, eight healthy volunteers ingesting 600 ml/day water or grapefruit juice for 10 days took a single oral 0.8-mg dose of alprazolam on the eighth day. The effects of repeated ingestion of grapefruit juice, an inhibitor of cytochrome P450 3A4 (CYP3A4), on the pharmacokinetics and pharmacodynamics of both single and multiple oral doses of alprazolam, a substrate of CYP3A4, were examined. ![]() Yasui N, Kondo T, Furukori H, Kaneko S, Ohkubo T, Uno T, Osanai T, Sugawara K, Otani K.ĭepartment of Neuropsychiatry, Hirosaki University School of Medicine, Japan. Related Articles,LinksĮffects of repeated ingestion of grapefruit juice on the single and multiple oral-dose pharmacokinetics and pharmacodynamics of alprazolam. Grapefruit + Valium (diazepam) = potentiation Grapefruit + Xanax (alprazolam) = no difference
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