EZETIMIBE/SIMVASTATIN contains two cholesterol-lowering medications, ezetimibe and simvastatin, available as a tablet
in four strengths:
- EZETIMIBE/SIMVASTATIN 10/10 (ezetimibe 10 mg/simvastatin 10 mg)
- EZETIMIBE/SIMVASTATIN 10/20 (ezetimibe 10 mg/simvastatin 20 mg)
- EZETIMIBE/SIMVASTATIN 10/40 (ezetimibe 10 mg/simvastatin 40 mg)
- EZETIMIBE/SIMVASTATIN 10/80 (ezetimibe 10 mg/simvastatin 80 mg)
EZETIMIBE/SIMVASTATIN is a medicine used to lower levels of total cholesterol, LDL (bad) cholesterol, and fatty
substances called triglycerides in the blood. In addition, EZETIMIBE/SIMVASTATIN raises levels of HDL (good) cholesterol.
It is used for patients who cannot control their cholesterol levels by diet alone. You should stay on a
cholesterol-lowering diet while taking this medicine.
EZETIMIBE/SIMVASTATIN works to reduce your cholesterol in two ways. It reduces the cholesterol absorbed in your
digestive tract.
Merck/Schering-Plough Pharmaceuticals announced the regulatory approval of Ezetimibe/Simvastatin (Ezetimibe & Simvastatin) on April 2nd 2004 in Germany and on July 26, 2004 in the United States for the treatment of elevated cholesterol (hypercholesterolemia).
Take EZETIMIBE/SIMVASTATIN once a day, in the evening, with or without food.
Cholesterol is a type of fat found in your blood. Cholesterol comes from two sources. It is produced by
your body and it comes from the food you eat. Your total cholesterol is made up of both LDL and HDL
cholesterol.
LDL cholesterol is called "bad" cholesterol because it can build up in the wall of your arteries and form
plaque. Over time, plaque build-up can cause a narrowing of the arteries. This narrowing can slow or
block blood flow to your heart, brain, and other organs. High LDL cholesterol is a major cause of heart
disease and stroke.
HDL cholesterol is called "good" cholesterol because it keeps the bad cholesterol from building up in the
arteries.
Triglycerides also are fats found in your body.
Primary Hypercholesterolemia: EZETIMIBE/SIMVASTATIN is indicated as adjunctive therapy to diet for the reduction of elevated total-C, LDL-C, Apo B, TG, and non-HDL-C, and to increase HDL-C in patients with primary (heterozygous familial and nonfamilial)hypercholesterolemia or mixed hyperlipidemia.
Homozygous Familial Hypercholesterolemia (HoFH): EZETIMIBE/SIMVASTATIN is indicated for the reduction of elevated total-C and LDL-C in patients with homozygous
familial hypercholesterolemia, as an adjunct to other lipid-lowering treatments (e.g., LDL apheresis) or if
such treatments are unavailable.
Therapy with lipid-altering agents should be a component of multiple risk-factor intervention in
individuals at increased risk for atherosclerotic vascular disease due to hypercholesterolemia. Lipidaltering
agents should be used in addition to an appropriate diet (including restriction of saturated fat and
cholesterol) and when the response to diet and other non-pharmacological measures has been
inadequate.
Important information about Ezetimibe/Simvastatin side effects .<br>
In clinical trials of ezetimibe co-administered with simvastatin, there was no increased incidence of Ezetimibe/Simvastatin side effects like myopathy or rhabdomyolysis associated with ezetimibe/simvastatin. However, myopathy and rhabdomyolysis are known Ezetimibe/Simvastatin side effects to statins and other lipid-lowering drugs. All patients starting therapy with ezetimibe/simvastatin or whose dose of ezetimibe/simvastatin is being increased should be advised of the risk of Ezetimibe/Simvastatin side effects like myopathy and told to report promptly any unexplained muscle pain, tenderness or weakness because they could be signs of serious side effects. It is recommended that liver function tests be performed before treatment with ezetimibe/simvastatin begins and thereafter as clinically indicated. Patients titrated to the 10/80 mg dose should receive an additional liver function test prior to titration, three months after titration to the 10/80 mg dose, and periodically thereafter (e.g. semiannually) for the first year of treatment. Due to the unknown Ezetimibe/Simvastatin side effects of the increased exposure to ezetimibe/simvastatin in patients with moderate or severe hepatic insufficiency, ezetimibe/simvastatin is not recommended in these patients. The safety and effectiveness of ezetimibe/simvastatin with fibrates have not been established; therefore, co-administration with fibrates is not recommended.
Ezetimibe/simvastatin should not be used in pregnant or nursing women. In clinical trials, ezetimibe/simvastatin was generally well tolerated. The most common Ezetimibe/Simvastatin side effects included headache, dizziness, arthralgia, myalgia and asthenia.
Important information about ezetimibe
When ezetimibe is used with a statin, liver function tests should be performed at the start of therapy and after that in accordance with the label for that statin. Due to the unknown effects of the increased exposure to ezetimibe in patients with moderate or severe hepatic insufficiency, ezetimibe is not recommended in these patients. In clinical trials, there was no increased incidence of myopathy or rhabdomyolysis associated with ezetimibe. However, myopathy and rhabdomyolysis are known adverse reactions to statins and other lipid-lowering drugs. There are no adequate and well-controlled studies of ezetimibe in pregnant women. Ezetimibe should not be used in pregnant or nursing women unless the benefit outweighs the potential risks. The safety and effectiveness of ezetimibe with fibrates have not been established; therefore, co-administration with fibrates is not recommended.
Important information about simvastatin
Simvastatin should not be used by anyone allergic to any of its components, with liver disease, or by women who are pregnant, breast-feeding or likely to become pregnant.Ezetimibe/Simvastatin side effects like muscle pain or weakness in people taking simvastatin should be reported to a doctor because these could be signs of a serious side effect. Doctors may perform blood tests before and periodically during treatment with simvastatin to check for liver problems. People taking 80 mg of simvastatin should receive an additional liver function test at three months. To help avoid serious Ezetimibe/Simvastatin side effects, discuss with your doctor medicine or food you should avoid while taking simvastatin. In clinical trials, Ezetimibe/Simvastatin side effects usually have been mild and transient. Most common Ezetimibe/Simvastatin side effects included headache (3.5 percent), abdominal pain (3.2 percent) and constipation (2.3 percent).
Ezetimibe/Simvastatin is the first product to reduce low-density lipoprotein cholesterol (LDL-C or 'bad' cholesterol) through Dual Inhibition of both cholesterol production in the liver and absorption in the intestine. Germany is the first European country to give regulatory approval for INEGY. The approval in Germany represents the first step in seeking marketing approval throughout the European Union (EU) under the EU's mutual recognition procedure. Ezetimibe/simvastatin has also been approved in Mexico.
"INEGY is an important treatment that offers more LDL-C-lowering compared to statins alone, and will, therefore, allow significantly more patients in Europe to reach their LDL-C targets," said Professor Heiner Greten, Universitatskrankenhaus, Eppendorf, Medizinische Klinik, Hamburg, Germany.
To provide physicians with choices for dosing based on patients' needs, INEGY, which contains both ezetimibe and simvastatin, will be available in several tablet strengths - ezetimibe 10 mg with simvastatin 10, 20, 40 or 80 mg.
Ezetimibe with simvastatin more efficacious than atorvastatin as demonstrated in studies presented at ACC The regulatory approval of INEGY is based on extensive clinical data that has shown INEGY provides greater LDL-C-reduction than statin alone.
Ezetimibe with simvastatin, the active ingredients in INEGY, have been shown to be significantly more effective at reducing LDL-C than atorvastatin (LIPITOR®) across all dosages. New data released this month at the American College of Cardiology from a 24-week study of ezetimibe 10 mg taken with simvastatin (doses ranging from 10 mg to 80 mg) compared to atorvastatin alone (does ranging from 10 mg to 80 mg) showed greater LDL-C reductions in patients taking ezetimibe/simvastatin compared to patients taking atorvastatin across the dosing ranges.
After six weeks of therapy, patients taking ezetimibe 10 mg with simvastatin 10 mg and patients taking ezetimibe 10 mg with simvastatin 20 mg experienced greater LDL-C reductions (46 percent and 50 percent, respectively) compared to atorvastatin 10 mg, which produced a 37 percent reduction. In addition, as each treatment group was titrated through the dosing ranges, ezetimibe with simvastatin provided greater LDL-C reductions than atorvastatin at all points in the treatment period.1
What is Dual Inhibition?
Cholesterol in the body originates from two main sources: production by hepatic and extra hepatic tissues and absorption in the intestine. Cholesterol-lowering agents (statins) reduce cholesterol levels by single inhibition, that is, by inhibiting the synthesis (production) of cholesterol in the liver. Ezetimibe, the first cholesterol absorption inhibitor, works by inhibiting intestinal absorption of cholesterol, both dietary and the cholesterol which is a component of bile. INEGY provides Dual Inhibition by targeting both of the main sources of cholesterol in the body, production and absorption, providing significantly more effective reduction of LDL-C plasma levels.
About INEGY / EZETIMIBE/SIMVASTATIN
INEGY will be marketed by a partnership between Merck & Co., Inc. and Schering-Plough Corporation. Ezetimibe/Simvastatin is also currently under review by the Food and Drug Administration for marketing approval under the brand name Ezetimibe/Simvastatin in the United States.