The manufacturer’s package insert warns about concomitant use of ezetimibe with the following drugs1:
- Cyclosporin: concomitant use results in excess exposure to both drugs, particularly in patients with renal disease
- Fibrates: concomitant use may increase the risk of cholelithiasis
- Cholestyramine: concomitant use decreased area under the curve of ezetimibe by 55%
- Warfarin: concomitant use may affect the anticoagulation effect of warfarin; regular monitoring of the International Normalized Ratio is indicated
The safety of the use of ezetimibe in combination with statin medications, including rosuvastatin and simvastatin, has also been demonstrated.2–4 These studies summarized the evidence of drug interactions of each drug and further examined the effects of statin/ezetimibe co-administration. Toth et al. reported that fibrates increased the bioavailability of ezetimibe by 50% or more, and cholestyramine reduced the area under the curve of ezetimibe by up to 80%.2 These authors also reported no significant effect of ezetimibe on the bioavailability of digoxin, warfarin, statins, ethinyl or glipizide. Kei et al reported that cyclosporin increased the bioavailability of ezetimibe by a factor of four.4
- Ezetimibe [package insert]. Whitehouse Station , NJ: Merck & Co, Inc; 2007.
- Toth PP, Davidson MH. Simvastatin plus ezetimibe: combination therapy for the management of dyslipidaemia. Expert Opin Pharmacother 2005; 6 (1): 131-139.
- Kim CH, An H, Kim SH, Shin D. Pharmacokinetic and pharmacodynamic interaction between ezetimibe and rosuvastatin in healthy male subjects. Drug Des Devel Ther 2017; 11 : 3461-3469.
- Kei AA, Filippatos TD, Elisaf MS. The safety of ezetimibe and simvastatin combination for the treatment of hypercholesterolemia. Expert Opin Drug Saf 2016; 15 (4): 559-569.