There’s only one cholesterol absorption inhibitor. Called ezetimibe (Zetia), it works by blocking the absorption of cholesterol from the small intestine, including cholesterol from food and cholesterol that enters the intestine in bile. Zetia is typically prescribed to people who experience intolerable side effects with a statin or cannot reach their lipid goals with a statin alone.

Benefits of Cholesterol Absorption Inhibitors

Zetia lowers LDL cholesterol levels by about 15 to 25 percent and triglyceride levels by 8 percent. When added to a statin, Zetia lowers LDL cholesterol levels more than doubling the statin dose does. Specifically, Zetia in combination with a statin reduces LDL cholesterol levels by as much as 60 percent and triglycerides by 14 percent. Unfortunately, a recent study found that Zetia doesn’t appear to slow atherosclerosis when used in combination with a statin.

Side effects of Cholesterol Absorption Inhibitors

These are infrequent and include dizziness, headache, diarrhea, and back pain. A recent study suggested that Zetia may increase the risk of cancer, but a broader analysis revealed that the concern is unfounded.

Publication Review By: Roger S. Blumenthal, M.D. and Simeon Margolis, M.D., Ph.D.

Published: 08 Jul 2011

Last Modified: 15 Jan 2015