Interactions between zetia(ezetimibe) and Neoral (cycloSPORINE)
cycloSPORINE and ezetimibe (Moderate Drug-Drug)
MONITOR: Coadministration with cyclosporine may significantly increase the plasma concentrations of ezetimibe. The mechanism of interaction is unknown. In a study of eight post-renal transplant patients with mildly impaired or normal renal function (CrCl greater than 50 mL/min), concomitant administration of cyclosporine (75 to 150 mg twice daily) increased the mean peak plasma concentration (Cmax) and area under the concentration-time curve (AUC) of total ezetimibe 3.9-fold and 3.3-fold, respectively, compared to a historical healthy control population. In another study, a renal transplant patient with severe renal dysfunction who was receiving multiple medications, including cyclosporine, demonstrated a 12-fold greater exposure to total ezetimibe compared to healthy subjects.
MANAGEMENT: Caution is advised if ezetimibe is prescribed to patients receiving cyclosporine due to the potential for increased exposure to ezetimibe. This exposure may be greater in patients with severe renal impairment.