ezetimibe and simvastatin (Vytorin) - medication uses, drug interactions, and side effects.

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Medications and Drugs

Pharmacy Author: Omudhome Ogbru, PharmD
Medical and Pharmacy Editor: Jay W. Marks, MD

GENERIC NAME: ezetimibe/simvastatin

BRAND NAME: Vytorin

DRUG CLASS AND MECHANISM: Vytorin is a combination of ezetimibe (Zetia) and simvastatin (Zocor) that is used for treating high levels of cholesterol in the blood. Vytorin reduces total cholesterol and low density lipoprotein (LDL or "bad") cholesterol while it increases high density lipoprotein (HDL or "good") cholesterol. The ezetimibe component of Vytorin lowers blood cholesterol by blocking the absorption of cholesterol, including dietary cholesterol, from the intestine. It does not affect the absorption of triglycerides. The simvastatin component of Vytorin belongs to a class of drugs called HMG-CoA reductase inhibitors, commonly called "statins." Statins reduce cholesterol by blocking an enzyme in the liver (HMG-CoA reductase) that produces cholesterol. Statins lower total and LDL cholesterol in the blood as well as triglycerides. They also increase HDL cholesterol.

LDL cholesterol is believed to be an important cause of coronary artery disease. Lowering LDL cholesterol levels slows and may even reverse coronary artery disease. Raising HDL cholesterol levels also may slow coronary artery disease. The FDA approved Vytorin in July 2004.

PRESCRIPTION: Yes

GENERIC AVAILABLE: No

PREPARATIONS: Tablets of 10/10, 10/20, 10/40, and 10/80 mg (ezetimibe/simvastatin)

STORAGE: Vytorin should be stored at room temperature, 20°-25°C (68°-77°F).

PRESCRIBED FOR: Vytorin is used for reducing total cholesterol, LDL cholesterol and triglycerides, and increasing HDL cholesterol.

DOSING: The recommended dose range of Vytorin is 10/10 mg to 10/80 mg, and it is administered once daily in the evening with or with out food. Therapy is usually initiated with 10/20 mg daily, but individuals who need more than a 55% reduction in LDL cholesterol can be started on 10/40 mg daily.

DRUG INTERACTIONS: Vytorin contains simvastatin (Zocor), and numerous drugs block the elimination of simvastatin by the liver. Decreased elimination of simvastatin could increase the levels of simvastatin in the body and increase the risk of muscle toxicity from simvastatin. Vytorin should not be combined with drugs that decrease its elimination. Examples of these drugs include erythromycin (E-Mycin), ketoconazole (Nizoral), itraconazole (Sporanox), clarithromycin (Biaxin), telithromycin (Ketek), cyclosporine (Sandimmune), nefazodone (Serzone), and HIV protease inhibitors such as indinavir (Crixivan) and ritonavir (Norvir). Large quantities of grape fruit juice (>1 quart daily) also will increase blood levels of simvastatin.

Amiodarone (Cordarone), verapamil (Calan Verelan, Isoptin), danazol (Danocrine), cyclosporine (Gengraf, Neoral), niacin (Niacor, Niaspan, Slo-Niacin), gemfibrozil (Lopid) and fenofibrate (Tricor) also may increase the risk of muscle toxicity when combined with simvastatin. Patients taking amiodarone or verapamil should not exceed 10/20 mg of Vytorin. Patients taking danazol or cyclosporine should not exceed 10/10 mg of Vytorin.

Simvastatin increases the effect of warfarin (Coumadin) and the blood concentration of digoxin (Lanoxin). Patients taking simvastatin and warfarin or digoxin should be monitored carefully.

Cholestyramine (Questran) decreases the absorption of ezetimibe (Zetia). Administer Vytorin 2 hours before or at least 4 hours after cholestyramine administration.

PREGNANCY: Vytorin should not be taken during pregnancy because the developing fetus requires cholesterol for development and Vytorin, due to the simvastatin component, reduces the production of cholesterol. Vytorin should only be administered to women of child bearing age if they are not likely to become pregnant.