Ezetimib

Ezetimib, also known as ezetimibe, is a lipid-lowering medication that inhibits the intestinal absorption of cholesterol by blocking the Niemann-Pick C1-like 1 (NPC1L1) transporter in the brush border of the small intestine. This reduces dietary and biliary cholesterol entering the circulation and lowers hepatic cholesterol stores, promoting clearance of LDL cholesterol from the blood.

Indications include monotherapy or combination therapy with a statin to reduce LDL-C and total cholesterol in adults with primary hyperlipidemia or mixed dyslipidemia. It is also used for familial hypercholesterolemia and, when added to statin therapy, has been shown to reduce cardiovascular events in high-risk patients (notably in the IMPROVE-IT trial after acute coronary syndrome).

Typical dosing is 10 mg once daily, with or without food. No routine adjustment is required for mild hepatic impairment, but use with caution in significant liver disease. It is not recommended for use in children under 10.

Common adverse effects include diarrhea, abdominal pain, upper respiratory tract infection, arthralgia, and back pain. Serious but rare risks include hepatotoxicity and myopathy, especially with concomitant statin therapy; hypersensitivity reactions may occur.

Drug interactions include reduced ezetimibe absorption when given with bile acid sequestrants (separate dosing by at least 2 hours before or 4 hours after). Cyclosporine can increase ezetimibe exposure; combining ezetimibe with statins may increase the risk of myopathy or rhabdomyolysis.

Pharmacokinetics: Ezetimib is rapidly absorbed and metabolized to an active glucuronide; excreted mainly in the feces with a relatively long elimination half-life.

Regulatory status: Ezetimib was approved in 2002 in the United States and is available as a generic medication; brand names include Zetia.