rifampin has been researched along with benidipine* in 1 studies
1 trial(s) available for rifampin and benidipine
Article | Year |
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Effect of rifampin on enantioselective disposition and anti-hypertensive effect of benidipine.
In vitro study showed that benidipine is exclusively metabolized by cytochrome P450 (CYP) 3A. This study evaluated the effect of rifampin on the enantioselective disposition and anti-hypertensive effect of benidipine.. Benidipine (8 mg) was administered to healthy subjects with or without repeated rifampin dosing, in a crossover design. Plasma concentrations of (S)-(S)-(+)-α and (R)-(R)-(-)-α isomers of benidipine and blood pressure were measured for up to 24 h after dosing. In addition, CYP3A metabolic capacity was evaluated in each subject using oral clearance of midazolam.. The exposure of (S)-(S)-(+)-α-benidipine was greater than that of (R)-(R)-(-)-α-benidipine by approximately three-fold following single dose of benidipine. Repeated doses of rifampin significantly decreased the exposure of both isomers. Geometric mean ratios (GMRs) (95% CI) of C. After single administration of racemic benidipine, enantioselective disposition of (S)-(S)-(+)-α- and (R)-(R)-(-)-α-benidipine was observed. Treatments with rifampin significantly decreased the exposure of both isomers but appeared to marginally affect its blood pressure-lowering effect in healthy subjects. Impact of coadministration of rifampin on the treatment effects of benidipine should be assessed in hypertensive patients. Topics: Adult; Antihypertensive Agents; Area Under Curve; Biological Availability; Cross-Over Studies; Cytochrome P-450 CYP3A; Dihydropyridines; Dose-Response Relationship, Drug; Drug Interactions; Healthy Volunteers; Humans; Hypertension; Male; Rifampin; Stereoisomerism; Young Adult | 2019 |