- What is ezetimibe, and how does it work (mechanism of action)?
- What brand names are available for ezetimibe?
- Is ezetimibe available as a generic drug?
- Do I need a prescription for ezetimibe?
- What are the side effects of ezetimibe?
- What is the dosage for ezetimibe?
- Which drugs or supplements interact with ezetimibe?
- Is ezetimibe safe to take if I'm pregnant or breastfeeding?
- What else should I know about ezetimibe?
What is ezetimibe, and how does it work (mechanism of action)?
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.
What are the side effects of ezetimibe?
The most common side effects of ezetimibe are:
Other important side effects include:
Quick GuideLower Your Cholesterol, Save Your Heart
What is the dosage for ezetimibe?
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.
Which drugs or supplements interact with ezetimibe?
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.
Is ezetimibe safe to take if I'm pregnant or breastfeeding?
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.
What else should I know about ezetimibe?
What preparations of ezetimibe are available?
Tablets, 10 mg
How should I keep ezetimibe stored?
Ezetimibe tablets should be stored between 15-30 C (59-86 F).
Reference: FDA Prescribing Information
Quick GuideLower Your Cholesterol, Save Your Heart
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Treatment & Diagnosis
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Cholesterol Drugs SlidesWhen diet and exercise aren't enough, should you turn to drugs? Learn cholesterol basics, drug classes, and available drugs along with their benefits and side effects.
Cholesterol ManagementHigh cholesterol and triglyceride levels increase the risk of cardiovascular disease. Getting your cholesterol and triglyceride levels in an optimal range will help protect your heart and blood vessels. Cholesterol management may include lifestyle interventions (diet and exercise) as well as medications to get your total cholesterol, LDL, HDL, and triglycerides in an optimal range.
Cholesterol PictureCholesterol carried in particles of low density (LDL cholesterol) is referred to as the "bad" cholesterol because elevated levels of LDL cholesterol are associated with an increased risk of coronary heart disease. See a picture of Cholesterol and learn more about the health topic.
ezetimibe and simvastatinVytorin is a cholesterol lowering drug. Vytorin is a combination of ezetimibe (Zetia) and simvastatin (Zocor). The simvastatin component of Vytorin is in a drug class called statins. Vytorin drug interactions include erythromycin, (E-Mycin), ketoconazole (Nizoral), itraconazole (Sporanox), clarithromycin (Biaxin), telithromycin (Ketek), cyclosporine (Sandimmune), nefazodone (Serzone), protease inhibitors such as indinavir (Crixivan) and ritonavir (Norvir) for HIV. Amiodarone (Cordarone), verapamil (Calan Verelan, Isoptin), danazol, niacin (Niacor, Niaspan, Slo-Niacin), gemfibrozil (Lopid) and fenofibrate (Tricor) warfarin (Coumadin), and digoxin (Lanoxin). Blood levels of simvastatin will increase when mixed with large quantities of grapefruit juice. This list is not all inclusive. Side effects include muscle pain, abnormal liver tests, headache, nausea, vomiting, diarrhea, and muscle pain.
Fatty LiverNonalcoholic fatty liver disease occurs due to the accumulation of abnormal amounts of fat within the liver. Fatty liver most likely caused by obesity and diabetes. Symptoms of fatty liver disease are primarily the complications of cirrhosis of the liver; and may include:
- mental changes,
- liver cancer,
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- gastrointestinal bleeding.
- weight loss, and
- bariatric surgery.
High Cholesterol: Frequently Asked QuestionsCholesterol occurs naturally in the body. High blood cholesterol levels increase a person's risk of developing heart disease, heart attacks, strokes, TIAs, and more. In addition to medication (fibrates, statins, bile acid sequestrants, and niacin), lifestyle changes can be made to lower blood cholesterol levels
Statins is a class of drugs prescribed to lower blood cholesterol. Statins also are prescribed for preventing and treating atherosclerosis. Common side effects of statins are
- constipation, and
Serious side effects can occur.
Examples of statins available in the US are
- atorvastatin (Lipitor),
- fluvastatin (Lescol, Lescol XL),
- lovastatin (Mevacor, Altoprev),
- pravastatin (Pravachol),
- rosuvastatin (Crestor),
- simvastatin (Zocor), and
- pitavastatin (Livalo).
Drug interactions, dosing, storage, and pregnancy safety should be reviewed prior to taking this medication.