Effects of ezetimibe on cyclosporine pharmacokinetics in healthy subjects.
Publication/Presentation Date
3-1-2006
Abstract
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 administered on day 8. AUC(0-last) and Cmax 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. Tmax (approximately 1.3 hours) was similar with and without EZE (P >.200). Mean CyA exposure slightly increased (approximately 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 CyA.
Volume
46
Issue
3
First Page
321
Last Page
327
ISSN
0091-2700
Published In/Presented At
Bergman, A. J., Burke, J., Larson, P., Johnson-Levonas, A. O., Reyderman, L., Statkevich, P., Kosoglou, T., Greenberg, H. E., Kraft, W. K., Frick, G., Murphy, G., Gottesdiener, K., & Paolini, J. F. (2006). Effects of ezetimibe on cyclosporine pharmacokinetics in healthy subjects. Journal of clinical pharmacology, 46(3), 321–327. https://doi.org/10.1177/0091270005284851
Disciplines
Business Administration, Management, and Operations | Health and Medical Administration | Management Sciences and Quantitative Methods
PubMedID
16490808
Department(s)
Administration and Leadership
Document Type
Article