Pharmacy Author: Emmanuel Saltiel, Pharm.D.
Medical Editor: Jay Marks, M.D.

GENERIC NAME: Ezetimibe

BRAND NAME: Zetia

DRUG CLASS AND MECHANISM: Ezetimibe is a drug that is used for the treatment of elevated blood cholesterol levels. It is estimated that sixty percent of the 13 million patients who are already taking drugs for elevated cholesterol levels continue to have LDL cholesterol ("bad" cholesterol) higher than recommended levels. Ezetimibe lowers blood cholesterol by blocking the absorption of cholesterol, including dietary cholesterol, from the intestines. It does not affect, however, the absorption of triglycerides or fat-soluble vitamins. Ezetimibe was approved by the FDA in October, 2002

PRESCRIPTION: Yes

GENERIC AVAILABLE: No

PREPARATIONS: Tablets: 10 mg.

STORAGE: Ezetimibe tablets should be stored at room temperature, 59-86°F (15-30°C).

PRESCRIBED FOR: Ezetimibe is used to reduce LDL cholesterol ("bad" cholesterol) concentrations in the blood. It can be used alone or together with statin drugs such as lovastatin (Mevacor), atorvastatin (Lipitor), simvastatin (Zocor), or pravastatin (Pravachol).

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

DRUG INTERACTIONS: Cholestyramine (Questran), a drug that can be used for reducing cholesterol levels, binds to ezetimibe and reduces its absorption from the intestine by about 50%. Therefore, ezetimibe should be taken at least two hours after or one hour before cholestyramine. It is assumed that colestipol (Colestid) and colesevelam (WelChol), two drugs that have actions similar to cholestyramine, also will bind and prevent the absorption 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 the potential 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 the potential risks.

SIDE EFFECTS: Ezetimibe is well-tolerated. The overall rate of side effects with ezetimibe in clinical studies was 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 1 in every 25 to 30 patients.

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