- 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).
Reference: FDA Prescribing Information
Quick GuideLower Your Cholesterol, Save Your Heart
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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Lipitor (atorvastatin) is a drug in the statin drug classed prescribed to patients to lower blood cholesterol, LDL, and triglycerides, elevate HDL cholesterol, to prevent angina, stroke, heart attack, congestive heart failure, revascularization procedures in heart disease, and prevent heart attacks, and strokes in patients with type 2 diabetes. Side effects of Lipitor include:
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Drug interactions, dosing, and pregnancy and breastfeeding safety should be reviewed prior to taking any medication.
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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.
ezetimibeEzetimibe (Zetia) is a medication prescribed alone or in combination with statins to improve levels of total cholesterol. Side effects, drug interactions, warnings and precautions, and pregnancy information should be reviewed prior to taking any medication.
fluvastatinFluvastatin (Lescol, Lescol XL) is a drug belonging to the drug class "statins." Fluvastatin is prescribed for reducing total blood cholesterol, LDL cholesterol, triglycerides, and increasing HDL cholesterol levels in conjunction with a healthy diet. Fluvastatin is also prescribed to reduce the risks of coronary revascularization procedures and slows the progression of coronary heart disease. Side effects, drug interactions, and patient safety information should be reviewed prior to taking this medication.
Heart AttackHeart attack happens when a blood clot completely obstructs a coronary artery supplying blood to the heart muscle. A heart attack can cause chest pain, heart failure, and electrical instability of the heart.
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Heart disease and heart attacks can be prevented by leading a healthy lifestyle with diet, exercise, and stress management. Symptoms of heart attack in men and women include chest discomfort and pain in the shoulder, neck, jaw, stomach, or back. Women experience the same symptoms as men; however, they also may experience:
- Extreme fatigue
- Pain in the upper abdomen
Leading a healthy lifestyle with a heart healthy low-fat diet, and exercise can help prevent heart disease and heart attack.
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
lovastatinLovastatin (Mevacor, Altoprev) is in the drug class of statins. Lovastatin (Mevacor, Altoprev) is prescribed for reducing total cholesterol and triglycerides in patients with elevated cholesterol levels. Side effects, drug interactions, and pregnancy safety should be reviewed prior to taking this medication.
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Peripheral vascular disease (PVD) refers to diseases of the blood vessels (arteries and veins) located outside the heart and brain. While there are many causes of peripheral vascular disease, doctors commonly use the term peripheral vascular disease to refer to peripheral artery disease (peripheral arterial disease, PAD), a condition that develops when the arteries that supply blood to the internal organs, arms, and legs become completely or partially blocked as a result of atherosclerosis. Peripheral artery disease symptoms include:
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pravastatinPravastatin (Pravachol, Pravigard PAC [discontinued]) is a drug that belongs to the drug class of statins and is prescribed for the treating individuals at risk of the consequences of arteriosclerotic vascular disease, strokes, transient ischemic attacks (TIAs or mini-strokes), and heart attacks. Side effects, dosing, drug interactions, and warnings and precautions should be reviewed prior to taking any medication.
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simvastatinZocor (simvastatin) belongs to the drug class of statins and is prescribed for lowering cholesterol and triglyceride levels. Side effects, drug interactions, warnings and precautions, and patient safety information should be reviewed prior to taking any medication.
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