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Drug treatments: Cholesterol absorption inhibitors

Your gastrointestinal (GI) tract normally absorbs cholesterol, which comes from food in your diet and from bile made by your liver. Drugs in this category block the absorption of cholesterol in your GI tract.

Cholesterol absorption inhibitors can be used alone or in combination with statins. Ezetimibe (Zetia) is a cholesterol absorption inhibitor currently on the market in the U.S. Like all cholesterol medications, it must be used in addition to, not instead of, dietary changes. Ezetimibe reduces total and LDL cholesterol levels by as much as 10 - 20%. When used in combination with statins, a greater percentage of people are able to lower their cholesterol and reach their treatment goals than when statins are used alone.

Ezetimibe should be used only after all other cholesterol-lowering drugs have failed.

Ezetimibe cannot be used if you have liver disease, or if you are pregnant or nursing.

Side Effects

Potential side effects include joint and back pain, abdominal pain, diarrhea, fatigue, and cough.

Drug Interactions

Ezetimibe should not be taken with fibrates (another class of cholesterol lowering medication). If you are also taking bile acid sequestrants to lower your cholesterol, you should take that drug either 2 hours before or 4 hours after ezetimibe.


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Review Date: 12/31/2012
Reviewed By: Glenn Gandelman, MD, MPH, FACC Assistant Clinical Professor of Medicine at New York Medical College; Private Practice specializing in Cardiovascular Disease in Greenwich, CT. Review provided by VeriMed Healthcare Network.
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