Ezetimibe is a drug that is used for the treatment of elevated levels of 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. Ezetimibe was approved by the FDA in October, 2002.
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 is estimated that 60% of the 13 million patients who are already taking drugs (primarily statins) for elevated levels of cholesterol continue to have levels of LDL cholesterol (“”bad”” cholesterol) that are higher than recommended levels. These patients may need to take an additional drug to bring levels of cholesterol down to recommended levels. Ezetimibe can be used together with the statins such as lovastatin (Mevacor), atorvastatin (Lipitor), simvastatin (Zocor), pravastatin (Pravachol), or rosuvastatin (Crestor) to further lower the levels of cholesterol.
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. Cyclosporin 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 the potential but 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 the potential and unknown 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. Rarely, hypersensitivity reactions, including angioedema (swelling of the skin and underlying tissues of the head and neck that can be life-threatening) and skin rash. Pancreatitis and nausea may occur. Muscle damage (myopathy or rhabdomyolysis) and hepatitis have rarely been associated with the use of ezetimibe.