- What is ezetimibe and simvastatin, and how does it work (mechanism of action)?
- What brand names are available for ezetimibe and simvastatin?
- Is ezetimibe and simvastatin available as a generic drug?
- Do I need a prescription for ezetimibe and simvastatin?
- What are the side effects of ezetimibe and simvastatin?
- What is the dosage for ezetimibe and simvastatin?
- Which drugs or supplements interact with ezetimibe and simvastatin?
- Is ezetimibe and simvastatin safe to take if I'm pregnant or breastfeeding?
- What else should I know about ezetimibe and simvastatin?
What is ezetimibe and simvastatin, and how does it work (mechanism of action)?
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.
What are the side effects of ezetimibe and simvastatin?
The most common side effects of Vytorin are:
Hypersensitivity reactions also have been reported. The most serious potential side effects are liver damage and muscle inflammation or breakdown. The simvastatin component of Vytorin is a statin. Therefore it shares side effects, such as liver and muscle damage associated with statins. Serious liver damage caused by statins is rare. More often, statins cause abnormalities of liver tests, and, therefore, periodic measurement of liver tests in the blood is recommended for all statins. Abnormal tests usually return to normal even if a statin is continued, but if the abnormal test value is greater than three times the upper limit of normal, the statin usually is stopped. Liver tests should be measured before Vytorin is started and periodically thereafter or if there is a medical concern about liver damage.
Inflammation of the muscles caused by statins can lead to a serious breakdown of muscle cells called rhabdomyolysis. Rhabdomyolysis causes the release of muscle protein (myoglobin) into the blood. Myoglobin can cause kidney failure and even death. When used alone, statins cause rhabdomyolysis in less than one percent of patients. To prevent the development of rhabdomyolysis, patients taking Vytorin should contact their health care professional immediately if they develop unexplained muscle pain, weakness, or muscle tenderness.
Statins have been associated with increases in HbA1c and fasting serum glucose levels that are seen in diabetes. There are also post-marketing reports of memory loss, forgetfulness, amnesia, confusion, and memory impairment. Symptoms may start 1 day to years after starting treatment and resolve within a median of 3 weeks after stopping the statin.
Quick GuideLower Your Cholesterol, Save Your Heart
What is the dosage for ezetimibe and simvastatin?
The recommended dose range of Vytorin is 10/10 mg to 10/40 mg, and it is administered once daily in the evening with or without food. Therapy usually is initiated with 10/10 or 10/20 mg daily, but individuals who need more than a 55% reduction in LDL cholesterol can be started on 10/40 mg daily.
Vytorin 10/80 mg is restricted to patients who have been taking Vytorin 10/80 mg chronically (for example, for 12 months or more) without evidence of muscle toxicity because the 10/80 mg dose is associated with increased risk of muscle toxicity, including rhabdomyolysis. Patients who are currently tolerating the 10/80-mg dose of Vytorin and who need an interacting drug that should not be taken with high doses of simvastatin should be switched to an alternative statin or statin-based regimen with less potential for the drug-drug interaction. Patients new to treatment with Vytorin who require more than the 10/40 mg dose should be switched to alternative agents.
Which drugs or supplements interact with ezetimibe and simvastatin?
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), boceprevir (Victrelis), telaprevir (incivek), voriconazole (Vfend), posaconazole (Noxafil), 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 and should be avoided.
Amiodarone (Cordarone), verapamil (Calan Verelan, Isoptin), diltiazem, amlodipine (Norvasc), danazol (Danocrine), ranolazine (Ranexa) 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, amlodipine, or ranolazine should not exceed 10/20 mg, and those taking verapamil or diltiazem should not exceed 10/10 mg of of Vytorin daily.
Patients taking gemfibrozil or danazol should not take 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, and, therefore, Vytorin should be administer two hours before or at least four hours after cholestyramine is administered.
Chinese patients taking more than 1 gram of niacin daily in combination with simvastatin, 40 mg, have an increased risk of muscle-related side effects. Therefore, these patients should not receive Vytorin 10/80 mg combined with niacin doses greater than 1 gram daily. Other doses of Vytorin should be administered cautiously when combined with niacin, 1 gram daily.
Is ezetimibe and simvastatin safe to take if I'm pregnant or breastfeeding?
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.
Because of the risk of adverse effects to the developing infant, Vytorin should not be administered to nursing mothers.
What else should I know about ezetimibe and simvastatin?
What preparations of ezetimibe and simvastatin are available?
Tablets of 10/10, 10/20, 10/40, and 10/80 mg (ezetimibe/simvastatin)
How should I keep ezetimibe and simvastatin stored?
Vytorin should be stored at room temperature, 20 C - 25 C (68 F - 77 F).
Vytorin 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.
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