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{{Ezetimibe/Simvastatin}} | |||
{{CMG}}; {{AE}} {{SS}} | |||
'''''For patient information about Ezetimibe/Simvastatin, click [[Ezetimibe/Simvastatin (patient information)|here]].''''' | |||
[[ | |||
{{SB}} VYTORIN<sup>®</sup> | |||
==Overview== | |||
'''Ezetimibe/simvastatin''' {{IPAc-en|ɛ|ˈ|z|ɛ|t|ɨ|m|ɪ|b|_|ˌ|s|ɪ|m|v|ə|ˈ|s|t|æ|t|ɨ|n}} is a drug combination used for the treatment of [[dyslipidemia]]. It is a combination of [[ezetimibe]] (known as Zetia in the [[United States]] and Ezetrol elsewhere) and the [[statin]] drug [[simvastatin]] (known as Zocor in the U.S.). The combination preparation is marketed by [[Merck & Co.]] under the trade names '''Vytorin''' and '''Inegy'''. | |||
[ | |||
[[Ezetimibe]] reduces blood cholesterol by acting at the [[brush border]] of the small intestine and inhibiting the absorption of cholesterol, leading to a decrease in the delivery of intestinal cholesterol to the liver. | |||
[ | |||
[ | |||
[[Simvastatin]] is an [[HMG-CoA reductase]] inhibitor or [[statin]]. It works by blocking an [[enzyme]] that is necessary for the body to make cholesterol. | |||
[[ | |||
Even though ezetimibe decreases cholesterol levels, as of 2009 it has not been found to lead to improvement in real world outcomes.<ref>{{cite web |url=http://content.nejm.org/cgi/content/full/NEJMoa0907569 |title=NEJM -- Extended-Release Niacin or Ezetimibe and Carotid Intima-Media Thickness |format= |work= |accessdate=}}</ref> The combination of simvastatin and ezetimibe has not been found to be any better than simvastatin alone. A panel of experts thus concluded in 2008 that it should "only be used as a last resort".<ref>{{cite journal |author=Mitka M |title=Cholesterol drug controversy continues |journal=JAMA |volume=299 |issue=19 |pages=2266 |date=May 2008 |pmid=18492963 |doi=10.1001/jama.299.19.2266 |url=}}</ref> | |||
< | ==Category== | ||
< | Category:Schering-Plough;Merck;Hypolipidemic agents;Cardiovascular Drugs | ||
==FDA Package Insert== | |||
[ | |||
''' [[Ezetimibe/Simvastatin indications and usage|Indications and Usage]]''' | |||
'''| [[Ezetimibe/Simvastatin dosage and administration|Dosage and Administration]]''' | |||
[ | '''| [[Ezetimibe/Simvastatin dosage forms and strengths|Dosage Forms and Strengths]]''' | ||
'''| [[Ezetimibe/Simvastatin contraindications|Contraindications]]''' | |||
'''| [[Ezetimibe/Simvastatin warnings and precautions|Warnings and Precautions]]''' | |||
[ | '''| [[Ezetimibe/Simvastatin adverse reactions|Adverse Reactions]]''' | ||
'''| [[Ezetimibe/Simvastatin drug interactions|Drug Interactions]]''' | |||
'''| [[Ezetimibe/Simvastatin use in specific populations|Use in Specific Populations]]''' | |||
[ | '''| [[Ezetimibe/Simvastatin overdosage|Overdosage]]''' | ||
'''| [[Ezetimibe/Simvastatin description|Description]]''' | |||
'''| [[Ezetimibe/Simvastatin clinical pharmacology|Clinical Pharmacology]]''' | |||
[ | '''| [[Ezetimibe/Simvastatin nonclinical toxicology|Nonclinical Toxicology]]''' | ||
'''| [[Ezetimibe/Simvastatin clinical studies|Clinical Studies]]''' | |||
'''| [[Ezetimibe/Simvastatin how supplied storage and handling|How Supplied/Storage and Handling]]''' | |||
'''| [[Ezetimibe/Simvastatin patient counseling information|Patient Counseling Information]]''' | |||
'''| [[Ezetimibe/Simvastatin labels and packages|Labels and Packages]]''' | |||
== | ==Mechanism of Action== | ||
===VYTORIN=== | |||
Plasma [[cholesterol]] is derived from intestinal absorption and endogenous synthesis. VYTORIN contains ezetimibe and simvastatin, two lipid-lowering compounds with complementary mechanisms of action. VYTORIN reduces elevated total-C, LDL-C, Apo B, TG, and non-HDL-C, and increases HDL-C through dual inhibition of [[cholesterol]] absorption and synthesis. | |||
===Ezetimibe=== | |||
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. In a 2-week clinical study in 18 hypercholesterolemic patients, ezetimibe inhibited intestinal [[cholesterol]] absorption by 54%, compared with placebo. 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=== | |||
Simvastatin is a prodrug and is hydrolyzed to its active β-hydroxyacid form, simvastatin acid, after administration. Simvastatin is a specific inhibitor of 3-hydroxy-3-methylglutaryl-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, simvastatin reduces very-low-density lipoproteins (VLDL) and TG and increases HDL-C. | |||
==Interaction with Alcohol== | |||
VYTORIN should be used with caution in patients who consume substantial quantities of alcohol and/or have a past history of liver disease. | |||
==References== | |||
{{Reflist|2}} | |||
{{Statins}} | |||
[[Category:Schering-Plough]] | |||
[[Category:Merck]] | |||
[[Category:Hypolipidemic agents]] | |||
[[Category:Cardiovascular Drugs]] | |||
[[Category:Drugs]] | [[Category:Drugs]] | ||
Latest revision as of 16:20, 19 February 2014
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Sheng Shi, M.D. [2]
For patient information about Ezetimibe/Simvastatin, click here.
Synonyms / Brand Names: VYTORIN®
Overview
Ezetimibe/simvastatin /ɛˈzɛt[invalid input: 'ɨ']mɪb
Ezetimibe reduces blood cholesterol by acting at the brush border of the small intestine and inhibiting the absorption of cholesterol, leading to a decrease in the delivery of intestinal cholesterol to the liver.
Simvastatin is an HMG-CoA reductase inhibitor or statin. It works by blocking an enzyme that is necessary for the body to make cholesterol.
Even though ezetimibe decreases cholesterol levels, as of 2009 it has not been found to lead to improvement in real world outcomes.[1] The combination of simvastatin and ezetimibe has not been found to be any better than simvastatin alone. A panel of experts thus concluded in 2008 that it should "only be used as a last resort".[2]
Category
Category:Schering-Plough;Merck;Hypolipidemic agents;Cardiovascular Drugs
FDA Package Insert
Indications and Usage | Dosage and Administration | Dosage Forms and Strengths | Contraindications | Warnings and Precautions | Adverse Reactions | Drug Interactions | Use in Specific Populations | Overdosage | Description | Clinical Pharmacology | Nonclinical Toxicology | Clinical Studies | How Supplied/Storage and Handling | Patient Counseling Information | Labels and Packages
Mechanism of Action
VYTORIN
Plasma cholesterol is derived from intestinal absorption and endogenous synthesis. VYTORIN contains ezetimibe and simvastatin, two lipid-lowering compounds with complementary mechanisms of action. VYTORIN reduces elevated total-C, LDL-C, Apo B, TG, and non-HDL-C, and increases HDL-C through dual inhibition of cholesterol absorption and synthesis.
Ezetimibe
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. In a 2-week clinical study in 18 hypercholesterolemic patients, ezetimibe inhibited intestinal cholesterol absorption by 54%, compared with placebo. 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
Simvastatin is a prodrug and is hydrolyzed to its active β-hydroxyacid form, simvastatin acid, after administration. Simvastatin is a specific inhibitor of 3-hydroxy-3-methylglutaryl-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, simvastatin reduces very-low-density lipoproteins (VLDL) and TG and increases HDL-C.
Interaction with Alcohol
VYTORIN should be used with caution in patients who consume substantial quantities of alcohol and/or have a past history of liver disease.
References
- ↑ "NEJM -- Extended-Release Niacin or Ezetimibe and Carotid Intima-Media Thickness".
- ↑ Mitka M (May 2008). "Cholesterol drug controversy continues". JAMA. 299 (19): 2266. doi:10.1001/jama.299.19.2266. PMID 18492963.