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EzetimibeThis page contains recent news articles, when available, and an overview of Ezetimibe but does not offer medical advice. You should contact your physician with regard to any health issues or concerns.Overview: Ezetimibe (when available) Ezetimibe is in a class of lipid-lowering compounds that selectively inhibits the intestinal absorption of cholesterol and related phytosterols. Ezetimibe, administered alone is indicated as adjunctive therapy to diet for the reduction of elevated total-C, LDL-C, and Apo B in patients with primary (heterozygous familial and non-familial) hypercholesterolemia. It is also used in combination therapy with HMG-CoA reductase inhibitors. Ezetimibe has a mechanism of action that differs from those of other classes of cholesterol-reducing compounds (HMG-CoA reductase inhibitors, bile acid sequestrants, fibric acid derivatives, and plant stanols). Ezetimibe does not inhibit cholesterol synthesis in the liver, or increase bile acid excretion but instead localizes and appears to act 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 HMG-CoA reductase inhibitors. For use as adjunctive therapy to diet for the reduction of elevated total-C, LDL-C, and Apo B in patients with primary (heterozygous familial and non-familial) hypercholesterolemia. Mechanism Of Action: Ezetimibe localizes and appears to act 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. News Articles on Ezetimibe Zetia and Vytorin Side Effects Not Linked to Cancer According to Study - Mar 30, 2009 Zetia (ezetimibe) is a prescription drug which decreases cholesterol delivery to the liver by inhibiting its intestinal absorption. Vytorin is a combination AboutLawsuits.com 2-in-1: Merck and Schering-Plough - Apr 8, 2009 Zetia (ezetimibe) was launched in 2003, and is the first in a new class of cholesterol lowering drugs which works by blocking the body's absorption of Pharmafocus Evaluating and Understanding Articles About Treatment - Apr 15, 2009 Cholesterol lowering and ezetimibe. N Engl J Med. 2008; 358(14):1507-1508. 4. Nissen SE, Wolski K. Effect of rosiglitazone on the risk of myocardial AAFP News Now Sunset for Statins after AURORA? - Mar 30, 2009 Since SHARP is evaluating the effect of combined simvastatin–ezetimibe therapy, it is concerned with an overlapping but different research question. New England Journal of Medicine (subscription) A cuidarse ese colesterol - Apr 19, 2009 Debido a todos esos factores, tenemos otra herramienta: Ezetimibe. Con esa droga, que tiene un mecanismo de acción diferente, se evita que el colesterol que Correo del Caroní 위기 'MSD ë°”ì?´í† 린' 기사회ìƒ? 길 ë³´ì?´ë‚˜ - Apr 13, 2009 ...ì?´ëŠ” 지난해 9ì›” 발표ë?œ SEAS(Simvastatin and Ezetimibe in Aortic Stenosis) 연구ì—?서 ë°”ì?´í† 린ì?´ 위약 대비 발암 위험성ì?´ ì¦?가했다는 ë³´ê³ ì™€ëŠ” ìƒ?ë°˜ë?œ 결과다. 데일리메디 ë°”ì?´í† 린, ì•” ë°˜ì?‘ 1백만건 당 1.3회 불과 - Apr 8, 2009 ...ì?´ ê°™ì?€ 결과는 2008ì›” 9ì›” SEAS(Simvastatin and Ezetimibe in Aortic Stenosis) ìž„ìƒ? ê²°ê³¼ 발표 ì?´í›„ ì œê¸°ë?œ ì—?ì œí‹°ë¯¸ë¸Œì™€ ì—?ì œí‹°ë¯¸ë¸Œ/심바스타틴 ë³µí•©ì œ(ë°”ì?´í† 린) 메디팜뉴스 Rosuvastatina nei pazienti in emodialisi - Apr 9, 2009 ...che ha arruolato circa 9000 pazienti con insufficienza renale cronica (in dialisi e non) e che sta testando l'associazione simvastatina/ezetimibe. Pillole.org 全世界引用率最高的医å¦è®ºæ–‡ - Apr 2, 2009 77 JJP Kastelein, et al., "Simvastatin with or without ezetimibe in familial hypercholesterolemia," New Engl. J. Med., 358(14): 1431-3, 3 April 2008. 科讯网 More Evidence That ACAT Is the Wrong Target for Lipid Lowering - 18 Mar 2009 The findings take on significance beyond the academic when examined in context with trial results on another drug -- the widely used ezetimibe, MedPage Today Lowering Cholesterol May Decrease Prostate Cancer Risk - 18 Mar 2009 They found that high cholesterol promoted tumor growth while the cholesterol-lowering drug ezetimibe (Zetia), which blocks the absorption of cholesterol NewsMax.com BREAKING NEWS: Merck & Co to buy Schering-Plough - Mar 9, 2009 Merck and SP, which already sell the cholesterol-lowering drugs Vytorin (ezetimibe plus simvastatin) and Zetia (ezetimibe) through a joint venture, Motley Fool Amid Lingering Questions, FDA Reprieves LDL Cholesterol–Lowering ... - Feb 24, 2009 After a months-long investigation, the US Food and Drug Administration (FDA) reiterated on January 8 that ezetimibe/simvastatin is an acceptable medication Journal of American Medical Association (subscription) Transparent Zebrafish A Must-see Model For Atherosclerosis - Mar 5, 2009 To explore the potential of zebrafish for atherosclerosis-related drug screening, the researchers administered the drug ezetimibe by adding it to the fish Science Daily (press release) Cholesterol may affect prostrate cancer risk - Feb 24, 2009 They found that high cholesterol levels promoted tumour growth and that Ezetimibe (Zetia), which blocks the absorption of cholesterol from the intestine, Times of India Cholesterol-lowering drugs may delay growth of prostate tumors - Feb 23, 2009 When mice with human prostate tumors were fed a no-cholesterol diet in combination with the cholesterol-lowering drug ezetimibe (Zetia, Schering-Plough), Insciences Organisation Safety Review on Cholesterol-Lowering Drugs Updated - Mar 6, 2009 ...of data from the ENHANCE clinical trial that compared Zocor (simvastatin) and Vytorin, a combination drug consisting of Zocor and Zetia (ezetimibe). Renal and Urology News Medicine 101: Advertising vs. reality - Mar 17, 2009 Another example, ezetimibe, a drug used to lower bad cholesterol (LDL). Combined in a single pill with simvastatin, a statin drug also used to lower bad Examiner.com What Are the Indications for Combination Therapy With Statins Plus ... - Feb 23, 2009 Triple drug therapy with a statin, one of the intestinally active agents (resin, plant sterols, or ezetimibe), and niacin may be required in individuals Medscape A Big Pharma Merger Made in Hell - Mar 13, 2009 ...drug that combined Merck's statin drug Zocor (simvastatin) with Schering-Plough's anti-hyperlipidemic drug Zetia (ezetimibe) -- was marketed in 2004. AlterNet NICE diabetes targets 'too tough' - Mar 13, 2009 ...city hospital in Birmingham, concluded: ‘Recent NICE guidelines suggest using 80 mg of simvastatin or adding ezetimibe in patients not meeting targets; Pulse Waxman and Stupak Request Further Information on Vytorin Studies - Feb 19, 2009 Back on September 5, 2008, counsel for the companies provided a briefing to Committee staff on a clinical trial called the Simvastatin and Ezetimibe in RTT News Ezetimibe: riduce mortalità e morbidità cardiovascolari? - Feb 20, 2009 Alcuni effetti fisiopatologici di ezetimibe potrebbero spiegare, forse, i risultati non brillanti ottenuti finora negli studi clinici. Pillole.org Quando l'unione fa la forza - Mar 8, 2009 Entrambi gli studi sono stati condotti con un’associazione di farmaci (simvastatina- ezetimibe), che rappresenta una marcia in più rispetto al trattamento La Stampa Resultados positivos para su tratamiento - Feb 22, 2009 Un análisis del estudio de un grupo de pacientes con diabetes tipo 2 demostró que un tratamiento con estatinas solas o con estatinas más ezetimibe, El Dia.com.do 美 심바스타틴, ë¦¬í”¼í† ì²˜ë°© ì œì³? - Mar 5, 2009 ...다ì?Œìœ¼ë¡œ ‘바ì?´í† 린’(Vytorin, ezetimibe/simvastatin)ì?´ ìž„ìƒ?(ENHANCE)ê²°ê³¼ 죽ìƒ?ë?™ë§¥ê²½í™”ì¦?ì—? 별 효과가 없는 것으로 드러난 타격ì—? 26% 하ë?½í•œ 1650만건 처방ì—? ê·¸ì³? 디지틀보사 머í?¬, ì‰?ë§?푸ë?¼ìš° 411ì–µ 달러ì—? ì?¸ìˆ˜ - Mar 9, 2009 ...머í?¬ì™€ ì‰?ë§?푸ë?¼ìš°ëŠ” 합작으로 ì?´ë¯¸ í• ì½œë ˆìŠ¤í…Œë¡¤ 약 ë°”ì?´í† 린(Vytorin: ezetimibe+ simvastatin)ê³¼ ì œí‹°ì•„(ezetimibe)를 íŒ?매하여 기존 ì œí’ˆì?˜ 새로운 ë³µí•©ì œë¡œ ì œí’ˆ 메디포뉴스 默克公å?¸å°‡èˆ‡å…ˆé?ˆè‘†é›…å…¬å?¸å?ˆä½µ - Mar 11, 2009 ...把心血管藥å“?ZETIA(ezetimibe))和VYTORIN2(ezetimibe/simvastatin)èž?入默克的心血管產å“?組å?ˆï¼Œå°‡ç°¡åŒ–æ–°å…¬å?¸çš„心血管藥å“?å¸‚å ´è¡ŒéŠ·ç–略,é€?é?Žæ–°çš„è—¥å“?組å?ˆä½¿å…¬å?¸çš„心 Business Wire (press release) Merck und Schering-Plough schließen sich zusammen - Mar 11, 2009 Die Konsolidierung der Cholesterinmedikamente ZETIA (Ezetimibe) und VYTORIN 2 (Ezetimibe/Simvastatin) zum kardiovaskulären Portfolio von Merck wird die Business Wire (press release) Cholestagel werkzaam bij Familiaire Hypercholesterolemie - Mar 2, 2009 De resultaten onderstrepen het mogelijke voordeel dat het toevoegen van colesevelam aan een therapie van statine en ezetimibe heeft, om LDL-C waarden bij FH Nieuwsbank (persbericht) (abonnement) Понижение уровнÑ? холеÑ?терина Ñ?нижает риÑ?к рака - Feb 25, 2009 Они обнаружили, что выÑ?окие уровни холеÑ?терина подталкивают опухоли к роÑ?ту, а препарат Ezetimibe (Zetia â„¢), блокирующий поглощение холеÑ?терина в кишечнике, МЕДСТРИМ.РУ - консультации врачей, новости медицины Merck en Schering-Plough fuseren - Mar 11, 2009 De toevoeging van de cholesterolgeneesmiddelen ZETIA (ezetimibe) en VYTORIN 2 (ezetimibe/simvastatin) aan Merck's aanbod aan cardiovasculair geneesmiddelen Business Wire (press release) Fusione tra Merck e Schering-Plough - Mar 11, 2009 La consolidazione dei farmaci anticolesterolo ZETIA (ezetimibe) e VYTORIN 2 (ezetimibe/simvastatina) nel portafoglio cardiovascolare di Merck semplificherà Business Wire (press release) Fuzja Merck i Schering-Plough - Mar 11, 2009 Włączenie leków regulujÄ…cych poziom cholesterolu ZETIA (ezetimibe) oraz VYTORIN (2) (ezetimibe/simvastatin) w ofertÄ™ leków Merck w zakresie chorób Business Wire (press release) Inegy: l'FDA ha aperto un’inchiesta sul possibile rischio di ... - Feb 24, 2009 Negli Stati Uniti la combinazione di Simvastatina ed Ezetimibe è venduta con il nome commerciale di Vytorin. L’FDA, l’Agenzia statunitense per il controllo XagenaSalute Merck et Schering-Plough fusionnent - Mar 11, 2009 Le regroupement des médicaments pour le traitement du cholestérol, ZETIA (ezetimibe) et VYTORIN 2 (ezetimibe/simvastatin), au sein du portefeuille Business Wire (press release) Desarrollo aterosclerosis - Mar 9, 2009 Además, pudieron comprobar cómo la sustancia ezetimibe, utilizada también en los humanos, redujo el ensanchamiento de las paredes. De acuerdo con el equipo, Cadena de Noticias Colesterolo e diabete, accoppiata pericolosa - Feb 25, 2009 ...le caratteristiche della nostra popolazione, abbiamo dimostrato che aggiungere una sostanza chiamata ezetimibe ad una statina (simvastatina) consente di Il Secolo XIX 2008年最çƒé—¨è®ºæ–‡æŽ’å??出炉 - Mar 4, 2009 71 14 JJP Kastelein, et al., "Simvastatin with or without ezetimibe in familial hypercholesterolemia," New Engl. J. Med., 358(14): 1431-3, 3 April 2008. 生物通 Zebrafish offer glimpse of heart disease - Mar 6, 2009 SAN DIEGO, Mar 7, 2009 (UPI via COMTEX) -- Researchers in California are using young zebrafish to study the effects of excess cholesterol on arteries. MarketWatch (press release) What’s good for the heart is good for the prostate - Feb 26, 2009 By Solmaz Barazesh At left is a cross section of a prostate tumor from a mouse fed a no cholesterol diet with Zetia. At right is a cross section of a Science News Brand Names/Synonyms: Ezetimibe is also known by the following brand names and/or synonymsEzedoc; Ezetimibe; Ezetimibe [Usan:Inn]; Ezetimibe [Usan]; Vytorin; Zetia Drug Category: Ezetimibe is categorized under the following by the FDA: Anticholesteremic Agents; Cholesterol Absorption Inhibitors; ATC:C10AX09 Dosage Forms: TABLET Absorption: Not Available Interactions: -->Interactions for Ezetimibe: Cholestyramine: Concomitant cholestyramine administration decreased the mean AUC of total ezetimibe approximately 55%. The incremental LDL-C reduction due to adding ezetimibe to cholestyramine may be reduced by this interaction. Fibrates: The safety and effectiveness of ezetimibe administered with fibrates have not been established. Fibrates may increase cholesterol excretion into the bile, leading to cholelithiasis. In a preclinical study in dogs, ezetimibe increased cholesterol in the gallbladder bile. Co-administration of ZETIA with fibrates is not recommended until use in patients is studied. Fenofibrate: In a pharmacokinetic study, concomitant fenofibrate administration increased total ezetimibe concentrations approximately 1.5-fold. Gemfibrozil: In a pharmacokinetic study, concomitant gemfibrozil administration increased total ezetimibe concentrations approximately 1.7-fold. HMG-CoA reductase inhibitors: No clinically significant pharmacokinetic interactions were seen when ezetimibe was co-administered with atorvastatin, simvastatin, pravastatin, lovastatin, or fluvastatin. Cyclosporine: The total ezetimibe level increased 12-fold in one renal transplant patient receiving multiple medications, including cyclosporine. Patients who take both ezetimibe and cyclosporine should be carefully monitored. Carcinogenesis, Mutagenesis, Impairment of Fertility A 104-week dietary carcinogenicity study with ezetimibe was conducted in rats at doses up to 1500 mg/kg/day (males) and 500 mg/kg/day (females) (~20 times the human exposure at 10 mg daily based on AUC0-24hr for total ezetimibe). A 104-week dietary carcinogenicity study with ezetimibe was also conducted in mice at doses up to 500 mg/kg/day (>150 times the human exposure at 10 mg daily based on AUC0-24hr for total ezetimibe). There were no statistically significant increases in tumor incidences in drug-treated rats or mice. No evidence of mutagenicity was observed in vitro in a microbial mutagenicity (Ames) test with Salmonella typhimurium and Escherichia coli with or without metabolic activation. No evidence of clastogenicity was observed in vitro in a chromosomal aberration assay in human peripheral blood lymphocytes with or without metabolic activation. In addition, there was no evidence of genotoxicity in the in vivo mouse micronucleus test. In oral (gavage) fertility studies of ezetimibe conducted in rats, there was no evidence of reproductive toxicity at doses up to 1000 mg/kg/day in male or female rats (~7 times the human exposure at 10 mg daily based on AUC0-24hr for total ezetimibe). Pregnancy Pregnancy Category: C There are no adequate and well-controlled studies of ezetimibe in pregnant women. Ezetimibe should be used during pregnancy only if the potential benefit justifies the risk to the fetus. In oral (gavage) embryo-fetal development studies of ezetimibe conducted in rats and rabbits during organogenesis, there was no evidence of embryolethal effects at the doses tested (250, 500, 1000 mg/kg/day). In rats, increased incidences of common fetal skeletal findings (extra pair of thoracic ribs, unossified cervical vertebral centra, shortened ribs) were observed at 1000 mg/kg/day (~10 times the human exposure at 10 mg daily based on AUC0-24hr for total ezetimibe). In rabbits treated with ezetimibe, an increased incidence of extra thoracic ribs was observed at 1000 mg/kg/day (150 times the human exposure at 10 mg daily based on AUC0-24hr for total ezetimibe). Ezetimibe crossed the placenta when pregnant rats and rabbits were given multiple oral doses. Multiple dose studies of ezetimibe given in combination with HMG-CoA reductase inhibitors (statins) in rats and rabbits during organogenesis result in higher ezetimibe and statin exposures. Reproductive findings occur at lower doses in combination therapy compared to monotherapy. All HMG-CoA reductase inhibitors are contraindicated in pregnant and nursing women. When ZETIA is administered with an HMG-CoA reductase inhibitor in a woman of childbearing potential, refer to the pregnancy category and package labeling for the HMG-CoA reductase inhibitor. Labor and Delivery The effects of ZETIA on labor and delivery in pregnant women are unknown. Nursing Mothers In rat studies, exposure to total ezetimibe in nursing pups was up to half of that observed in maternal plasma. It is not known whether ezetimibe is excreted into human breast milk; therefore, ZETIA should not be used in nursing mothers unless the potential benefit justifies the potential risk to the infant. Pediatric Use The pharmacokinetics of ZETIA in adolescents (10 to 18 years) have been shown to be similar to that in adults. Treatment experience with ZETIA in the pediatric population is limited to 4 patients (9 to 17 years) in the sitosterolemia study and 5 patients (11 to 17 years) in the HoFH study. Treatment with ZETIA in children (<10 years) is not recommended. Geriatric Use Of the patients who received ZETIA in clinical studies, 948 were 65 and older (this included 206 who were 75 and older). The effectiveness and safety of ZETIA were similar between these patients and younger subjects. Greater sensitivity of some older individuals cannot be ruled out. Chemical IUPAC Name: 1-(4-fluorophenyl)-3-[3-(4-fluorophenyl)-3-hydroxy-propyl]-4-(4-hydroxyphenyl)-azetidin-2-one : |
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