Trade Names:Vytorin 10/10- Tablets ezetimibe 10 mg/simvastatin 10 mg
Trade Names:Vytorin 10/20- Tablets ezetimibe 10 mg/simvastatin 20 mg
Trade Names:Vytorin 10/40- Tablets ezetimibe 10 mg/simvastatin 40 mg
Trade Names:Vytorin 10/80- Tablets ezetimibe 10 mg/simvastatin 80 mg
Inhibits absorption of cholesterol by the small intestine.Simvastatin
Inhibits the conversion of HMG-CoA to mevalonate, an early step in the biosynthetic pathway for cholesterol.
Adjunctive treatment to diet for reduction of elevated total-cholesterol, LDL cholesterol, triglycerides, non-HDL cholesterol, and apolipoprotein B (Apo B), and to increase HDL cholesterol in patients with primary hypercholesterolemia or mixed hyperlipidemia; as an adjunct to other lipid-lowering treatment for the reduction of total cholesterol and LDL cholesterol in patients with homozygous familial hypercholesterolemia.
Active liver disease or unexplained persistent elevations in serum transaminases; pregnancy and lactation; hypersensitivity to any component of the product.
PO Dosage range is 10/10 mg through 10/80 mg daily in the evening. Start with 10/20 mg daily. Lipid levels may be analyzed after 2 or more wk and dosage adjusted. For patients requiring a large reduction in LDL cholesterol (more than 55%), therapy may be started at 10/40 mg daily.Homozygous Familial HypercholesterolemiaAdults
PO 10/40 mg daily or 10/80 mg daily in the evening. Use as an adjunct to other lipid lowering treatments.
Administer without regard to meals. Administer with food if GI upset occurs.
Store tablets at controlled room temperature (68° to 77°F).
Risk of myopathy/rhabdomyolysis may be increased. Dose of ezetimibe/simvastatin should not exceed 10/20 mg daily.Antacids
Aluminum and magnesium antacids decreased C max of ezetimibe by 30%.Bile acid sequestrant (eg, cholestyramine)
Ezetimibe concentrations may be reduced, decreasing the therapeutic effect. Give at least 2 h before or 4 h after the bile acid sequestrant.Carbamazepine, rifampin
Simvastatin concentrations may be reduced, decreasing the efficacy.Cyclosporine, danazol
Exposure to ezetimibe may be increased, especially in patients with severe renal function impairment. Dose of ezetimibe/simvastatin should not exceed 10/10 mg daily.Digoxin
Digoxin plasma concentrations may be slightly elevated.Fibrates (eg, fenofibrate, gemfibrozil)
Ezetimibe and simvastatin concentrations may be increased. Avoid coadministration.Niacin
Risk of myopathy may be increased, especially with doses of niacin 1 g/day or more.Potent inhibitors of CYP3A4 (eg, clarithromycin, cyclosporine, delaviridine, diltiazem, efavirenz, erythromycin, HIV protease inhibitors, itraconazole, ketoconazole, nefazodone, telithromycin, large quantities of grapefruit juice [more than 1 quart daily])
May reduce the elimination of simvastatin, increasing the risk of myopathy. Avoid coadministration.Propranolol
Simvastatin peak plasma concentrations may be reduced.St. John's wort
Coadministration may result in decreased simvastatin levels.Warfarin
The anticoagulant effect, as measured by the INR, may be modestly potentiated.
None well documented.
The incidences stated for the following adverse reactions were reported with Vytorin (ezetimibe/simvastatin) administration. Adverse reactions occurring with administration of either ezetimibe or simvastatin can be found in their respective monographs.
Cholelithiasis, cholecystitis, elevated CPK, elevated liver transaminases, (postmarketing).
Hypersensitivity reactions, including anaphylaxis, angioedema, rash, and urticaria (postmarketing).
Myalgia (4%); pain in extremity (2%); arthralgia (postmarketing).
Upper respiratory tract infection (4%).
Influenza (3%); myopathy, nausea, pancreatitis, rhabdomyolysis, thrombocytopenia (postmarketing).
Ensure that lipid levels are measured before therapy is started, at least 2 wk after starting ezetimibe/simvastatin therapy or changing the dose, and then periodically thereafter. Monitor LFTs before the initiation of treatment and thereafter when clinically indicated.
Category X .
Safety and efficacy not established.
Use with caution in patients with severe renal function impairment.
Use is not recommended in patients with moderate or severe hepatic function impairment.
Ensure that serum transaminases are determined before starting therapy and periodically thereafter as clinically indicated. For patients being titrated to 10/80 mg dose, ensure that transaminases are determined before titration, 3 mo after titration to 10/80 mg dose, and periodically thereafter (eg, every 6 mo) for first yr of treatment. If elevated serum transaminase levels develop during treatment, repeat levels more frequently. If transaminase levels rise to 3 times upper limit of normal or greater and persist, be prepared to discontinue therapy.
Use with caution in patients who consume substantial quantities of alcohol or who have history of liver disease. Marked, persistent increases in serum transaminases can occur.
Simvastatin administration has been associated with dose-related myopathy/rhabdomyolysis. Discontinue therapy immediately if myopathy occurs or is suspected.
Rule out or treat secondary causes of hyperlipidemia before starting treatment.
Rhabdomyolysis with renal function impairment secondary to myoglobinuria has occurred with statin administration. Consider myopathy in any patient with diffuse myalgias, muscle tenderness or weakness, or marked CPK elevation.
Limited data are available. Supportive treatment is recommended.
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