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
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 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?
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.
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.
(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
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.
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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
Because of the risk of adverse effects to the
developing infant, Vytorin should not be administered to
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