ezetimibe + cyclosporine

**Ezetimibe + cyclosporine** is a combination of two pharmaceutical agents that are sometimes co-administered in clinical practice but is not a fixed-dose combination product. Ezetimibe is an intestinal cholesterol absorption inhibitor that acts at the brush border of the small intestine, reducing the absorption of cholesterol, leading to decreased plasma cholesterol levels. Cyclosporine is an immunosuppressant that primarily inhibits calcineurin, thereby suppressing T-cell activation and cytokine production. The co-administration of ezetimibe and cyclosporine is clinically significant due to a documented pharmacokinetic interaction: cyclosporine can dramatically increase plasma concentrations of ezetimibe (by 2.3–12 fold), raising the risk of ezetimibe toxicity. Ezetimibe can also modestly increase cyclosporine concentrations. This combination may be encountered in transplant patients with hyperlipidemia, but requires careful monitoring and dose adjustment due to these interactions[1][2][3][4][5][6].

Brand names

ZetiaNeoralSandimmuneGengraf

Other names

ezetimibecyclosporinecyclosporin A