Premium
Effects of Ezetimibe on Cyclosporine Pharmacokinetics in Healthy Subjects
Author(s) -
Bergman Arthur J.,
Burke Joanne,
Larson Patrick,
JohnsonLevonas Amy O.,
Reyderman Larisa,
Statkevich Paul,
Kosoglou Teddy,
Greenberg Howard E.,
Kraft Walter K.,
Frick Glenn,
Murphy Gail,
Gottesdiener Keith,
Paolini John F.
Publication year - 2006
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1177/0091270005284851
Subject(s) - pharmacokinetics , crossover study , ezetimibe , medicine , dosing , washout , pharmacology , confidence interval , geometric mean , gastroenterology , cholesterol , pathology , alternative medicine , placebo , statistics , mathematics
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 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 (∼1.3 hours) was similar with and without EZE ( P >.200). Mean CyA exposure slightly increased (∼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.