Ezetimibe/simvastatin is a combination of drugs used for the treatment of dyslipidemia. It is a combination of ezetimibe (known as Zetia in the United States and Ezetrol elsewhere) and simvastatin statin drug (known as Zocor in the US).
Ezetimibe reduces blood cholesterol by acting on the border of the small intestine brush and inhibits cholesterol absorption, leading to a decrease in intestinal cholesterol delivery to the liver.
Simvastatin is a HMG-CoA reductase inhibitor or statin. It works by blocking the enzymes that the body needs to make cholesterol. The generic version is approved in 2017. The combination preparation is marketed by Merck & amp; Co. with the trade names Vytorin in the US and Inegy in Europe.
Video Ezetimibe/simvastatin
Contraindications
- Acute liver disease
- Pregnancy and breastfeeding
Maps Ezetimibe/simvastatin
Side effects
- Miopathy
- Rhabdomyolysis
- Mentalgia
- Pain in the extremities, abdomen
- Angioedema
- Hepatitis
- Eczema
- Fatigue
- Headaches
- Influenza, pharyngitis, sinusitis, and upper respiratory tract infection
Interactions
- Cyclosporine
- Danazol
- Protease inhibitor
- Verapamil
- Amiodarone
- A large amount of niacin (nicotinic acid), grapefruit juice
- Erythromycin, telithromycin, clarithromycin
- Nefazodone
Pharmacology
The combination of ezetimibe and simvastatin is currently the only product to treat both sources of cholesterol; absorption in the intestines of both biliary and dietary cholesterol, and production in the liver and peripheral tissues. It is estimated that high cholesterol treatment from both sources tends to produce lower cholesterol levels, especially LDL cholesterol. In a clinical study, it showed that the combination of ezetimibe and simvastatin was superior to atorvastatin in lowering LDL cholesterol.
Clinical test
UPGRADE-IT experiment
Published in 2015, IMProved Reduction of Outcomes: Vytorin Efficacy International Trial (IMPROVE-IT) randomized 18,144 patients with ACS to simvastatin 40 mg/d plus ezetimibe 10 mg/day or simvastatin alone. With a median follow-up of 6 years, simvastatin ezetimibe was found to reduce primary CV mortality outcomes, major CV events, or nonfatal stroke (34.7% vs 32.7%; P = 0.016; NNT 50 per 7 years or NNT 350 per 1 year). There was no decrease in all causes or deaths of CV with simvastatin ezetimibe, although there was a decrease in MI and stroke.
ENHANCE experimental data
The two-year ENHANCE study failed to provide evidence that ezetimibe/simvastatin was better than simvastatin (generic drugs) in terms of achieving a lower change of baseline in carotid intima-media thickness despite lower LDL levels in patients with heterozygous hypercholesterolaemic families (a form high cholesterol that affects less than 1% of patients). Clinical events such as heart attack and stroke are not measured as primary or secondary endpoints of the study making it impossible to determine the effect of Vytorin on these events.
Debates and subsequent queries
The American College of Cardiology released a statement showing that "major clinical decisions are not made on the basis of ENHANCE studies alone", given the small and unique patient population, 720 patients in Amsterdam hospital with heterozygous familial hypercholesterolemia.
Merck and Schering Plow have reported that they have three ongoing trials to focus on results, measuring the effects of drugs on heart attacks and strokes on patients.
These results were presented in full at the American College of Cardiology meeting on March 30, 2008, two years after the last patient completed the study. The House Committee on Energy and Trade conducted an investigation into the disclosure of pending research data.
Ad campaigns
In the United States, Vytorin displays a television advertising campaign featuring a series of separate screen images of a person and a food item to make the point that cholesterol comes from two sources and can be absorbed from food or produced by the body, and that offspring play a role in the latter. This point is a departure from the commonly held belief that high cholesterol only comes from the food you eat. In each ad, the person's features or clothing and layered food to emphasize the resemblance between people and food. For example, in a single ad, a woman wore a yellow shirt and pin juxtaposed with a similarly colored cake.
References
External links
- Vytorin's official website
- Vytorin Information Sheet
- US. National Medical Library: Drug Information Portal - Ezetimibe/simvastatin
Source of the article : Wikipedia
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