13.03.4 Ezetimibe

Ezetimibe inhibits the transporter for cholesterol absorption from the gastrointestinal tract, and this reduces cholesterol absorption.  This leads to decreased levels of plasma LDL cholesterol, but has little effect on HDL cholesterol and triglycerides.  Ezetimibe is active after oral administration.  It undergoes extensive enterohepatic recycling.  Ezetimibe can be used alone in subjects with high LDL cholesterol levels, but the statins are usually preferred for monotherapy.  A few people cannot tolerate statins, as it can cause myopathy (muscle weakness), and then ezetimibe is used as an alternative to statins to lower LDL cholesterol.  More commonly, ezetimibe is used in combination with simvastatin, when the simvastatin alone fails to lower LDL cholesterol sufficiently.  Ezetimibe and simvastatin have different mechanisms of action, and this allows them to have an additive effect when combined to lower LDL cholesterol.