ezetimibe, Zetia

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GENERIC NAME: ezetimibe

BRAND NAME: Zetia

DRUG CLASS AND MECHANISM: Ezetimibe is an oral 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 alone or in combination with statins to improve levels of total cholesterol, low-density lipoprotein cholesterol, non-HDL 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 before or 4 hours after administration of these drugs. Cyclosporine (Gengraf, Neoral) increases the levels of ezetimibe while ezetimibe increases levels of cyclosporine. Combining both drugs may increase side effects of either drug.

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

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

SIDE EFFECTS: The most common side effects of ezetimibe are diarrhea, abdominal pain, back pain, joint pain, muscle aches, and sinusitis. 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: 3/22/2012




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