Effects of ezetimibe on cyclosporine pharmacokinetics in healthy subjects.

This single-center, open-label, 2-period crossover study investigated the effects of multiple-dose ezetimibe (EZE) on a single dose of cyclosporine(CyA). Healthy subjects received 2 treatments in random order with a 14-day washout: (1) CyA 100 mg alone and (2) EZE 20 mg for 7 days with CyA 100 mg coadministered on day 7; EZE 20 mg alone was adiministered on day 8. AUC(0-last) and C-max geometric mean ratios(90% confidence interval) for ([CyA +EZE]/CyA alone) were 1.15 (1,07, 1.25) and 1.10 (0.97, 1.26), respectively. T-max (similar to 1.3 hours) was similar with and without EZE (P > .200). Mean CyA exposure slightly increased (similar to 15%) with multiple-dose EZE 20 mg; however, this value was contained within (0.80, 1.25). The implications for chronic EZE dosing within the usual clinical paradigm of chronic CyA dosing have not been established; caution is recommended when Using these agents concomitantly. CyA concentrations should be monitored in patients receiving EZE and GyA.