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February 9, 2012

ezetimibe, Zetia

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GENERIC NAME: ezetimibe

BRAND NAME: Zetia

DRUG CLASS AND MECHANISM: Ezetimibe is a drug that is used for the treatment of elevated blood cholesterol. The most commonly used class of drugs for lowering cholesterol levels, the statins, act by preventing the production of cholesterol by the liver. Ezetimibe has a different mechanism of action and lowers blood cholesterol by reducing the absorption of cholesterol from the intestine. It does not affect the absorption of triglycerides or fat-soluble vitamins. The FDA approved ezetimibe in October 2002.

PRESCRIPTION: Yes

GENERIC AVAILABLE: No

PREPARATIONS: Tablets, 10 mg

STORAGE: Ezetimibe tablets should be stored between 15°-30°C (59°-86°F).

PRESCRIBED FOR: Ezetimibe is used in combination with statins to improve levels of total cholesterol, low-density lipoprotein cholesterol, triglycerides, high-density lipoprotein cholesterol, and apolipoprotein B. Combining ezetimibe with a statin is more effective than either drug alone. Ezetimibe may be used alone or in combination with fibrates [for example, fenofibrate (Tricor)] to improve levels of cholesterol, low-density lipoprotein cholesterol, and apolipoprotein B.

DOSING: The recommended dose of ezetimibe is 10 mg daily. Ezetimibe can be taken with or without food and at the same time as statin drugs.

DRUG INTERACTIONS: Cholestyramine (Questran), colestipol (Colestid) and colesevelam (WelChol), bile acid-binding drugs that may be used to treat elevated levels of cholesterol, bind to ezetimibe and reduce its absorption from the intestine by about 50%. Therefore, ezetimibe should be taken at least two hours after or one hour before these drugs. Cyclosporine (Gengraf, Neoral) increases the levels of ezetimibe and could lead to greater side effects of ezetimibe.

PREGNANCY: There are no adequate studies of ezetimibe in pregnant women. Therefore, physicians must weight the benefit of prescribing ezetimibe during pregnancy against potential unknown risks.

NURSING MOTHERS: There are no adequate studies of ezetimibe in nursing women. Therefore, physicians must weight the benefit of prescribing ezetimibe to nursing women against potential unknown risks.

SIDE EFFECTS: Ezetimibe is well-tolerated. The overall rate of side effects with ezetimibe in clinical studies were similar to that reported with placebo (an inactive sugar pill). Diarrhea, abdominal pain, back pain, joint pain, and sinusitis were the most commonly reported side effects, occurring in one in every 25 to 30 patients. Hypersensitivity reactions, including angioedema (swelling of the skin and underlying tissues of the head and neck that can be life-threatening) and skin rash rarely occur. Nausea, pancreatitis, muscle damage (myopathy or rhabdomyolysis) and hepatitis have been reported in post-marketing studies.

Reference: FDA Prescribing Information


Last Editorial Review: 4/16/2008




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ezetimibe, Zetia

1) What Is Cholesterol?

Cholesterol is a waxy, fat-like substance that occurs naturally in all parts of the body and is made by the liver. Cholesterol also is present in foods we eat. People need cholesterol for the body to function normally. Cholesterol is present in the cell walls or membranes everywhere in the body, including the brain, nerves, muscles, skin, liver, intestines, and heart.

2) Why Should I Be Concerned About Cholesterol?

Too much cholesterol in your body means that you have an increased risk of getting cardiovascular diseases such as heart disease. If you have too much cholesterol in your body, the cholesterol can build up on the walls of the arteries that carry blood to your heart. This buildup, which occurs over time, causes less blood and oxygen to get to your heart. This can cause chest pain and heart attacks.

3) What's the Difference between "Good" and "Bad" Cholesterol?

...

Read the High Cholesterol: Frequently Asked Questions article »







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