Ezetimibe is used together with lifestyle changes diet, weight-loss, exercise to reduce the amount of cholesterol a fat-like substance and other fatty substances in the blood. Ezetimibe is in a class of medications called cholesterol-lowering medications. It works by preventing the absorption of cholesterol in the intestine.
Buildup of cholesterol and fats along the walls of the blood vessels a process known as atherosclerosis decreases blood flow, which decreases the oxygen supply to the heart, brain, and other parts of the body. Lowering blood levels of cholesterol and fats may help reduce this buildup and may decrease your chances of developing heart conditions such as angina chest pain , strokes, and heart attacks. Results of a clinical study that compared people who took ezetimibe and simvastatin with people who took simvastatin alone found that although the group of people taking ezetimibe and simvastatin had lower amounts of cholesterol in the blood, there was no difference between the two groups in the amount of cholesterol and fat buildup on the insides of the blood vessels in the neck.
It is not currently understood why the additional lowering of cholesterol levels in the blood did not lead to a greater decrease in cholesterol and fat buildup along the walls of the blood vessels in people taking ezetimibe and simvastatin. Further studies are underway to compare treatment with ezetimibe and simvastatin to treatment with simvastatin alone to see if there is a difference in the risk of developing heart disease.
Talk to your doctor if you have questions about the risks and benefits of treating increased amounts of cholesterol in your blood with ezetimibe and other medications. In addition to taking a cholesterol-lowering medication, making certain changes in your daily habits can also lower your blood cholesterol levels. Ezetimibe comes as a tablet to take by mouth.
It is usually taken once a day with or without food. To help you remember to take ezetimibe, take it around the same time every day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand.
Take ezetimibe exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor. There is a total of 5 error s on this form, details are below. Please enter your name Please enter your email Your email is invalid. Please check and try again Please enter recipient's email Recipient's email is invalid. Please check and try again Agree to Terms required. Thank you for sharing our content.
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Because it is known that the risk of myopathy during treatment with HMG-CoA reductase inhibitors is increased with concurrent administration of fenofibrates, VYTORIN should be administered with caution when used concomitantly with a fenofibrate [see Warnings and Precautions 5. Fenofibrates may increase cholesterol excretion into the bile, leading to cholelithiasis. If cholelithiasis is suspected in a patient receiving VYTORIN and a fenofibrate, gallbladder studies are indicated and alternative lipid-lowering therapy should be considered [see the product labeling for fenofibrate and fenofibric acid].
In such patients, prothrombin time should be determined before starting VYTORIN and frequently enough during early therapy to ensure that no significant alteration of prothrombin time occurs. Once a stable prothrombin time has been documented, prothrombin times can be monitored at the intervals usually recommended for patients on coumarin anticoagulants. Simvastatin therapy has not been associated with bleeding or with changes in prothrombin time in patients not taking anticoagulants.
Concomitant administration of ezetimibe 10 mg once daily had no significant effect on bioavailability of warfarin and prothrombin time in a study of twelve healthy adult males. There have been postmarketing reports of increased INR in patients who had ezetimibe added to warfarin.
Most of these patients were also on other medications. Cases of myopathy, including rhabdomyolysis, have been reported with simvastatin coadministered with colchicine, and caution should be exercised when prescribing VYTORIN with colchicine. Both VYTORIN and daptomycin can cause myopathy and rhabdomyolysis when given alone and the risk of myopathy and rhabdomyolysis may be increased by coadministration. Lipid-lowering drugs offer no benefit during pregnancy, because cholesterol and cholesterol derivatives are needed for normal fetal development.
Atherosclerosis is a chronic process, and discontinuation of lipid-lowering drugs during pregnancy should have little impact on long-term outcomes of primary hypercholesterolemia therapy. There are no adequate and well-controlled studies of VYTORIN use during pregnancy; however, there are rare reports of congenital anomalies in infants exposed to statins in utero. Animal reproduction studies of simvastatin in rats and rabbits showed no evidence of teratogenicity.
Serum cholesterol and triglycerides increase during normal pregnancy, and cholesterol or cholesterol derivatives are essential for fetal development. Because statins, such as simvastatin, decrease cholesterol synthesis and possibly the synthesis of other biologically active substances derived from cholesterol, VYTORIN may cause fetal harm when administered to a pregnant woman.
If VYTORIN is used during pregnancy or if the patient becomes pregnant while taking this drug, the patient should be apprised of the potential hazard to the fetus. Ezetimibe crossed the placenta when pregnant rats and rabbits were given multiple oral doses.
Multiple-dose studies of ezetimibe coadministered with statins in rats and rabbits during organogenesis result in higher ezetimibe and statin exposures. Reproductive findings occur at lower doses in coadministration therapy compared to monotherapy. However, in studies with another structurally-related statin, skeletal malformations were observed in rats and mice.
There are rare reports of congenital anomalies following intrauterine exposure to statins. The number of cases is adequate only to exclude a 3- to 4-fold increase in congenital anomalies over the background incidence.
It is not known whether simvastatin is excreted in human milk. Because a small amount of another drug in this class is excreted in human milk and because of the potential for serious adverse reactions in nursing infants, women taking simvastatin should not nurse their infants. A decision should be made whether to discontinue nursing or discontinue drug, taking into account the importance of the drug to the mother [see Contraindications 4 ].
In rat studies, exposure to ezetimibe in nursing pups was up to half of that observed in maternal plasma. It is not known whether ezetimibe or simvastatin are excreted into human breast milk. Because a small amount of another drug in the same class as simvastatin is excreted in human milk and because of the potential for serious adverse reactions in nursing infants, women who are nursing should not take VYTORIN [see Contraindications 4 ].
In a multicenter, double-blind, controlled study followed by an open-label phase, boys and postmenarchal girls, 10 to 17 years of age mean age The patients received coadministered ezetimibe and simvastatin 10 mg, 20 mg, or 40 mg or simvastatin monotherapy 10 mg, 20 mg, or 40 mg for 6 weeks, coadministered ezetimibe and 40 mg simvastatin or 40 mg simvastatin monotherapy for the next 27 weeks, and open-label coadministered ezetimibe and simvastatin 10 mg, 20 mg, or 40 mg for 20 weeks thereafter.
The results of the study at Week 6 are summarized in Table 3. Results at Week 33 were consistent with those at Week 6. In this limited controlled study, there was no significant effect on growth or sexual maturation in the adolescent boys or girls, or on menstrual cycle length in girls. No overall differences in safety or effectiveness were observed between these subjects and younger subjects, and other reported clinical experience has not identified differences in responses between the elderly and younger patients but greater sensitivity of some older individuals cannot be ruled out.
In the SHARP trial of patients with moderate to severe renal impairment non-dialysis patients with median serum creatinine 2. VYTORIN is contraindicated in patients with active liver disease or unexplained persistent elevations in hepatic transaminases. Chinese patients may be at higher risk for myopathy, monitor patients appropriately. In the event of an overdose, symptomatic and supportive measures should be employed. A few cases of overdosage have been reported; most have not been associated with adverse experiences.
Reported adverse experiences have not been serious. No specific diagnostic signs were observed in rodents. At these doses the only signs seen in dogs were emesis and mucoid stools. A few cases of overdosage with simvastatin have been reported; the maximum dose taken was 3. All patients recovered without sequelae.
The chemical name of ezetimibe is 1- 4-fluorophenyl -3 R -[3- 4-fluorophenyl -3 S -hydroxypropyl]-4 S - 4-hydroxyphenyl azetidinone. Ezetimibe is a white, crystalline powder that is freely to very soluble in ethanol, methanol, and acetone and practically insoluble in water. Its structural formula is:. The empirical formula of simvastatin is C 25 H 38 O 5 and its molecular weight is Simvastatin is a white to off-white, nonhygroscopic, crystalline powder that is practically insoluble in water and freely soluble in chloroform, methanol and ethanol.
Plasma cholesterol is derived from intestinal absorption and endogenous synthesis. Ezetimibe reduces blood cholesterol by inhibiting the absorption of cholesterol by the small intestine.
The molecular target of ezetimibe has been shown to be the sterol transporter, Niemann-Pick C1-Like 1 NPC1L1 , which is involved in the intestinal uptake of cholesterol and phytosterols. Ezetimibe had no clinically meaningful effect on the plasma concentrations of the fat-soluble vitamins A, D, and E and did not impair adrenocortical steroid hormone production.
Ezetimibe localizes at the brush border of the small intestine and inhibits the absorption of cholesterol, leading to a decrease in the delivery of intestinal cholesterol to the liver. This causes a reduction of hepatic cholesterol stores and an increase in clearance of cholesterol from the blood; this distinct mechanism is complementary to that of statins [see Clinical Studies 14 ].
Simvastatin is a specific inhibitor of 3-hydroxymethylglutaryl-coenzyme A HMG-CoA reductase, the enzyme that catalyzes the conversion of HMG-CoA to mevalonate, an early and rate limiting step in the biosynthetic pathway for cholesterol. In addition, decreased levels of HDL-C are associated with the development of atherosclerosis. Epidemiologic studies have established that cardiovascular morbidity and mortality vary directly with the level of total-C and LDL-C and inversely with the level of HDL-C.
The independent effect of raising HDL-C or lowering TG on the risk of coronary and cardiovascular morbidity and mortality has not been determined. After oral administration, ezetimibe is absorbed and extensively conjugated to a pharmacologically active phenolic glucuronide ezetimibe-glucuronide. Effect of Food on Oral Absorption.
Concomitant food administration high-fat or non-fat meals had no effect on the extent of absorption of ezetimibe when administered as mg tablets. Relative to the fasting state, the plasma profiles of both active and total inhibitors of HMG-CoA reductase were not affected when simvastatin was administered immediately before an American Heart Association recommended low-fat meal.
When radiolabeled simvastatin was administered to rats, simvastatin-derived radioactivity crossed the blood-brain barrier. Ezetimibe is primarily metabolized in the small intestine and liver via glucuronide conjugation with subsequent biliary and renal excretion.
Minimal oxidative metabolism has been observed in all species evaluated. In humans, ezetimibe is rapidly metabolized to ezetimibe-glucuronide. Both ezetimibe and ezetimibe-glucuronide are eliminated from plasma with a half-life of approximately 22 hours for both ezetimibe and ezetimibe-glucuronide. Plasma concentration-time profiles exhibit multiple peaks, suggesting enterohepatic recycling.
After 48 hours, there were no detectable levels of radioactivity in the plasma. Other clinical studies have compared Vytorin with different statin drugs. A statin is a type of cholesterol-lowering drug. Simvastatin, one of the active drugs in Vytorin, is a statin. In a 6-week study, Vytorin was compared with a statin drug called rosuvastatin Crestor.
These results varied depending on the dosage of Vytorin or rosuvastatin that people took. Studies have also compared Vytorin with a different statin drug, called atorvastatin Lipitor. HoFH is a rare genetic condition.
With HoFH, you inherit abnormal genes from both of your parents. Having HoFH increases your risk for heart attack and stroke. Vytorin is typically an add-on therapy for HoFH. This is a procedure in which your blood is passed through a machine that filters out LDL cholesterol. In this study, people had been taking 40 mg of simvastatin. Simvastatin is one of the active drugs in Vytorin. One group of people switched to a higher simvastatin dose, of 80 mg. Vytorin is FDA-approved for use in children ages 10 years and older.
Vytorin is approved to treat certain forms of high cholesterol. If you have a very high cholesterol level, your doctor might have you take Vytorin with certain other cholesterol-lowering drugs. The other treatments your doctor recommends for you may depend on your risk for heart attack and stroke , and what form of high cholesterol you have. Other types of cholesterol-lowering drugs that your doctor may prescribe for you to take with Vytorin include:.
Bile acid sequestrant drugs work by removing bile acids from the body. This causes your body to make more bile acids by breaking down cholesterol, which lowers your cholesterol levels. Vytorin can cause mild or serious side effects. The following lists contain some of the key side effects that may occur while taking Vytorin.
For more information about the possible side effects of Vytorin, talk with your doctor or pharmacist. They can give you tips on how to deal with any side effects that may be bothersome. Most of these side effects may go away within a few days or a couple of weeks. Call your doctor right away if you have serious side effects. Vytorin is approved for use in children ages 10 years and older. Side effects of Vytorin in children ages 10 years and older are similar to those seen in adults, as described above and below.
You may wonder how often certain side effects occur with Vytorin. Below are details about certain side effects this drug may cause. As with most drugs, some people can have an allergic reaction after taking Vytorin.
However, allergic reactions have been reported since the drug was released onto the market. A more severe allergic reaction is rare but possible. Symptoms of a severe allergic reaction can include:. Call your doctor right away if you have an allergic reaction to Vytorin, as the reaction could become severe. Some people may have muscle pain while taking Vytorin.
In some clinical studies , people took either Vytorin or a placebo for approximately 7 months. In these studies, muscle pain occurred in:. Muscle pain and muscle weakness can be a symptom of myopathy muscle damage. Myopathy is a known side effect of all statin drugs, including simvastatin one of the active drugs in Vytorin. Your risk for muscle pain or myopathy while taking Vytorin is highest during your first year of taking the drug.
But after the first year, your risk for these side effects gets lower as you continue taking the drug. For example, in a long-term clinical study , myopathy occurred in:. And some groups of people have a higher risk for muscle damage while taking Vytorin. Note: Muscle pain and weakness may also be signs of a serious side effect of Vytorin called immune-mediated necrotizing myopathy.
This is an overactive immune system response that causes muscle cell death. Immune-mediated necrotizing myopathy is a rare side effect of statin drugs, including simvastatin one of the active drugs in Vytorin. Call your doctor right away if you have any unusual muscle pain, tenderness, or weakness while taking Vytorin.
Muscle problems with other symptoms, such as fever, can sometimes be a sign of a more serious side effect called rhabdomyolysis. If you have muscle problems while taking Vytorin, your doctor may recommend a creatinine phosphokinase CPK blood test. CPK is an enzyme a type of protein that helps with muscle function. Having high levels of CPK can be a sign of muscle damage. If you have high CPK or other symptoms of muscle damage, your doctor will usually recommend that you stop taking Vytorin.
Muscle pain and weakness usually gets better after you stop taking Vytorin. But tell your doctor if you continue to have these symptoms after you stop taking Vytorin.
Having increased liver enzymes is a possible side effect of Vytorin. And this can be a sign of liver damage. Liver enzymes are proteins that help your liver function. Vytorin can sometimes cause liver damage. And if cells in your liver are damaged, liver enzymes can leak into your bloodstream.
This shows up as increased liver enzymes in blood tests called liver function tests. In clinical studies , increased liver enzymes occurred in 1. In a long-term clinical study , increased liver enzymes occurred in:. As you continue to take Vytorin, your liver enzymes tend to return to normal levels.
However, sometimes increased liver enzymes can be a sign of more serious damage to your liver. Before you start taking Vytorin, your doctor will order liver function tests to check your liver enzyme levels. You may also have liver function tests during your Vytorin treatment. Call your doctor right away if you have any symptoms of liver damage while taking Vytorin.
These symptoms may include:. If you have any of these symptoms, your doctor will order liver function tests to check your liver enzymes. If the tests show a problem with your liver, your doctor will usually recommend that you stop taking Vytorin. Some people may have alopecia hair loss or thinning while taking Vytorin. Alopecia has also been reported in people taking simvastatin and ezetimibe since these drugs were released. Simvastatin and ezetimibe are the active drugs in Vytorin.
Memory loss may occur while taking Vytorin. But simvastatin , one of the active drugs in Vytorin, is a statin. And problems with memory have been reported as a side effect of simvastatin as well as other statin drugs. In some cases, memory problems have developed within a few days after starting a statin drug. In other cases, memory problems have developed after people have been taking a statin drug for years.
Most memory problems get better within a few weeks after stopping statin treatment. If you have memory problems while taking Vytorin, talk with your doctor.
They may recommend switching to a different treatment. Some people may have depression while taking Vytorin. Depression has also been reported in people taking simvastatin and ezetimibe since these drugs were released.
And if you have symptoms of depression while taking Vytorin, tell your doctor right away. Typically, your doctor will start you on a low dosage. Your doctor will ultimately prescribe the smallest dosage that provides the desired effect. The following information describes dosages that are commonly used or recommended.
However, be sure to take the dosage your doctor prescribes for you. Your doctor will determine the best dosage to fit your needs. The active drugs in Vytorin are ezetimibe and simvastatin. Vytorin is approved to treat certain types of high cholesterol when used with a low-cholesterol diet.
Vytorin is approved to treat high cholesterol caused by homozygous familial hypercholesterolemia HoFH.
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