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14-September-2008 10:43:22 - Ezetimibe Ezetimibe Systematic IUPAC name 3R,4S-1-4-fluorophenyl- 3-3S-3-4-fluorophenyl-3-hydroxypropyl-4- 4-hydroxyphenyl-2-azetidinone Identifiers CAS number 163222-33-1 ATC code C10AX09 PubChem 150311 DrugBank APRD00619 Chemical data Formula C24H21F2NO3 Mol. mass 409.4 g.mol-1 SMILES eMolecules PubChem Pharmacokinetic data Bioavailability 35-65% Protein binding 90% Metabolism Intestinal wall, hepatic Half life 19-30 hours Excretion Renal 11%, faecal 78% Therapeutic considerations Pregnancy cat. C Au, C U.S. Legal status S4 Au, POM UK, ℞-only U.S. Routes Oral Ezetimibe pronounced /ɛˈzɛtəmɪb/ is an anti-hyperlipidemic medication which is used to lower cholesterol levels. It acts by decreasing cholesterol absorption in the intestine. It may be used alone when other cholesterol-lowering medications are not tolerated, or together with statins e.g. ezetimibe/simvastatin, marketed as Vytorin and Inegy when cholesterol levels are unable to be controlled on statins alone. It is marketed by Schering-Plough and Merck under the trade names Ezetrol, Zetia and Ezemibe. Ezetimibe was originally discovered by a team of four Schering-Plough research chemists: Drs. Stuart B. Rosenblum, Duane A. Burnett, John W. Clader and Brian A. McKittrick. Contents 1 Pharmacology 2 Clinical use 2.1 Indications 2.2 Adverse effects 2.3 Dosage forms 3 Clinical trial controversy 4 References 5 See also 6 External links Pharmacology Ezetimibe localises at the brush border of the small intestine, where it inhibits the absorption of cholesterol from the diet. Specifically, it appears to bind to a critical mediator of cholesterol absorption, the Niemann-Pick C1-Like 1 NPC1L1 protein on the gastrointestinal tract epithelial cells1 as well as in hepatocytes2. In addition to this direct effect, decreased cholesterol absorption leads to an increase in LDL-cholesterol uptake into cells, thus decreasing levels in the blood plasma. Clinical use Indications Ezetimibe is indicated as an adjunct to dietary measures in the management of: Hypercholesterolaemia Homozygous sitosterolemia phytosterolemia3 On 9 June 2006, U.S. regulators approved the use of ezetimibe in combination with fenofibrate to treat mixed hyperlipidaemia. Adverse effects Common adverse drug reactions ≥1% of patients associated with ezetimibe therapy include: headache and/or diarrhea. Infrequent adverse effects 0.1-1% of patients include: myalgia and/or raised liver function test ALT/AST results. Rarely 0.1% of patients, hypersensitivity reactions rash, angioedema or myopathy may occur.3 Zetia Logo Zetia Logo Dosage forms Ezetimibe is available as 10 mg tablets in most markets. A combination preparation ezetimibe/simvastatin, which combines ezetimibe with a statin, is also available. Clinical trial controversy On January 14, 2008, it was reported in the New York Times that a clinical trial ENHANCE trial of Zetia that was designed to show that the drug could reduce the growth of fatty plaques in arteries instead resulted in growth of plaques. However, the growth noted was less than it would have been had the patients been on placebo alone. Merck and Schering-Plough completed the clinical trial in April 2006 and had initially planned to release the findings no later than March 2007. The companies missed several self-imposed deadlines, and in December 2007, finally agreed to publish the results soon after the delays were publicized in news reports.4 It should be recognized that the ENHANCE trial was not a clinical-outcome trial, but merely an imaging study. Formally, the American College of Cardiology ACC maintains that Zetia may be a reasonable option for patients who cannot tolerate a statin or cannot be controlled on a high dose statin. 5 Results from the trial have provoked three large clinical-outcome trials. The results from these trials will be presented in the next three to four years. However, a March 30th, 2008 meeting of the ACC resulted in negative press for drugs like Zetia as Yale University Cardiologist Harlan Krumholz and concurring colleagues called into question the efficacy of such drugs. 6 Krumholz' statements maintained that such pharmaceuticals should not be the first or even second option for prescribing doctors. Definitive conclusions of the efficacy and safety of Zetia can be made such a time when the results of more substantial and comprehensive trials are released, such as the upcoming IMPROVE-IT Trial which has an enrollment of 18000 patients and will report results in 2012. Results of the Simvastatin and Ezetimibe in Aortic Stenosis SEAS trial ClinicalTrials.gov number, NCT00092677 ClinicalTrials.gov showed a potential increase in cancer in association with the use of these drugs together. www.nejm.org September 2, 2008 10.1056/NEJMe0807200. The actual significance has yet to be determined. References ^ Garcia-Calvo M, Lisnock J, Bull HG, Hawes BE, Burnett DA, Braun MP, et al. The target of ezetimibe is Niemann-Pick C1-Like 1 NPC1L1. Proc Natl Acad Sci U S A 2005;10223:8132-7. PMID 15928087 ^ Temel, Ryan E., Tang, Weiqing, Ma, Yinyan, Rudel, Lawrence L., Willingham, Mark C., Ioannou, Yiannis A., Davies, Joanna P., Nilsson, Lisa-Mari, Yu, Liqing. Hepatic Niemann-Pick C1-like 1 regulates biliary cholesterol concentration and is a target of ezetimibe J. Clin. Invest. 2007 0: JCI30060 ^ a b Rossi S, or. Australian Medicines Handbook 2006. Adelaide: Australian Medicines Handbook; 2006. ISBN 0-9757919-2-3 ^ Berenson, A 2008-01-14. Drug Has No Benefit in Trial, Makers Say, NY Times. Retrieved on 2008-01-14. ^ ACC Statement on ENHANCE Trial, ACC 2008-01-15. Retrieved on 2008-02-04. ^ Carey, J 2008-03-31. A Weak Prognosis for Vytorin and Zetia, Business Week. Retrieved on 2008-04-01. See also Ezetimibe/simvastatin Statin External links Zetia U.S. Prescribing Information v d e Merck Co., Inc. Corporate Directors: Richard Clark · Johnnetta Cole · William Harrison · William Kelley · Rochelle Lazarus · Thomas Shenk · Anne Tatlock · Samuel Thier · Wendell Weeks · Peter Wendell Products: Alendronate · Aprepitant · Ertapenem · Ezetimibe · Ezetimibe/simvastatin · Finasteride · Fosaprepitant · Indinavir · Losartan · Lovastatin · Montelukast · Raltegravir · Rizatriptan · Rofecoxib · Simvastatin · Sitagliptin · Vorinostat Publications: The Merck Index · The Merck Manual Annual Revenue: $22.9 billion USD ▲2% FY 2004 · Employees: 63,000 · Stock Symbol: NYSE: MRK · Website: www.merck.com v d e Lipid modifying agents C10 Statins HMG-CoA reductase Atorvastatin Cerivastatin‡ Fluvastatin Lovastatin Mevastatin Pitavastatin Pravastatin Rosuvastatin Simvastatin Fibrates PPAR Clofibrate‡ Bezafibrate Aluminium clofibrate Gemfibrozil Fenofibrate Simfibrate Ronifibrate Ciprofibrate Etofibrate Clofibride Clinofibrate Bile acid sequestrants Colestyramine Colestipol Colestilan Colextran Colesevelam Niacin and derivatives Niceritrol Niacin Nicofuranose Aluminium nicotinate Nicotinyl alcohol Acipimox CETP inhibitors Anacetrapib† Torcetrapib§ Combinations Niacin/lovastatin Niacin/simvastatin Ezetimibe/simvastatin Other Dextrothyroxine Probucol Tiadenol Benfluorex Meglutol Omega-3-triglycerides Magnesium pyridoxal 5-phosphate glutamate Policosanol Ezetimibe Lapaquistat§ †Undergoing clinical trials. ‡Withdrawn from market. §Development terminated. Retrieved from http://en..org/wiki/Ezetimibe Categories: Hypolipidemic agents | Lactams | Merck | Schering-Plough Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page Languages Italiano Polski Português This page was last modified on 13 September 2008, at 22:46
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