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Profile Profile Uses and Administration Adverse Effects And Etacrynic Acid/Ezetimibe 1379 unchanged and partly in the form of metabolites. It is Efortil; Etilefril; Chile: Elfortilt; Fin.: Elfortil; Fr.: Effortil; Ger.: over 10 years, may be given ezetimibe for the same indica­ extensively bound to plasma proteins. Bioflutin; Effortil; Etil; Pholdyston; Thomasin; Gr.: Effortil; tions and at the same doses as in adults (see above). ' Efortil; Ita/. : Elfortil; Jpn: Effortil; Mex.: Effortil; Quimtatil; Pol.: Effortil; Port.: Effortil; S.Afr.: Effortilt; Spain: Efortil; Swed.: Hyperlipidaemias. Ezetimibe inhibits the absorption of �:.�!?.�.��.!��-��--·········································································· Effortil; Switz. : Effortil; Thai.: Buracard; Circula; Circuman; dietary cholesterol' and, although there is a compensatory Proprietary Preparations (details are given in Volume B) Venez. : Elfortilt; Effrine; Efxine; Hyposia; Hyprosiat; Effontil. increase in cholesterol synthesis in the liver.' overall Single-ingredient Preparations. Austral.: Edecrin; Canad.: Multi-ingredient Preparations. Austria: Agilan; Amphodynt; plasma LDL-cholesterol concentrations are reduced.2 Ezeti­ Edecrin; Hung.: Uregyt; Ita!. : Reomax; Rus.: Uregyt (Ypei"HT); Effortil camp; Hypodynt; Influbenet; Ger.: Dibydergot plus; mibe may be used alone' in the management of hyperlipi­ Ukr.: Uregyt (YperHT); USA: Edecrin. Effortil plust; Switz.: Dibydergot plust; Elfortil plust. daentias (p. 1248.1) but use with lipid regulating drugs Phannacopoeial Preparations that act by reducing cholesterol synthesis may produce BP 2014: Sodium Etacrynate Injection; additive effects. In patients already taking statins, addition USP 36: Ethacrynate Sodium for Injection; Ethacrynic Add Etofibrate(riNNJ of ezetintibe results in a further reduction in LDL-choles­ terol, 4 which may increase the number of patients achiev­ ing lipid targets, or allow lower doses of statins to be used. However, the clinical relevance of this is unclear; a study' in patients with familial hypercholesterolaemia found no difference in the progression of carotid atherosclerosis (measured by intima-media thickness) in those given eze­ tintibe with simvastatin compared with those given simva­ statin alone, despite a larger reduction in LDL-cholesterol. Sintilar effects on LDL-cholesterol have been reported6 for ezetimibe with fibrates. As well as inhibiting cholesterol absorption, ezetintibe also blocks the absorption of plant sterols such as Etofibrate, a derivative of clofibrate (p. 1338.3) and carnpesterol and sitosterol, and may be effective in patients Profile nicotinic add (p. 2083.1), is a lipid regulating drug used in with sitosterolaentia,7 an inherited disorder in which the treatment of hyperlipidaentias (p. 1248,1). The usual increased absorption of plant sterols leads to premature Ethadzine, an analogue of moracizine (p. 1441.2), is oral dose is SOOmg daily. atherosclerosis. reported to be a class Ic antiarrhythntic. It is used in the 1, Sudhop T, et al. Inhibition of intestinal cholesterol absorption by treatment of ventricular and supraventricular arrhythntias ezetimibe in humans. Circulation 2002; 106: 1943-8. and has been given orally in doses starting at SO mg three �-��-��!����---········································································· 2. Knopp RH, et al. Effects of ezetimibe, a new cholesterol absorption times daily, increased if necessary to a maximum of 100mg Proprietary Preparations (details are given io Volume E) inhibitor. on plasma lipids in patients with primary hypercholester­ olemia. Bur Heart J 2003; 24: 729-41. three times daily. It has also been given intravenously. Single-ingredient Preparations. Braz. : Tricero� Ger.: Lipo-Merzt; 3. Pandor A, etal. Ezetimibe monotherapy for cholesterol lowering in 2, 722 Hong Kong: Lipo-Merz; Port,: Lipo-Merz. people: systematic review and meta-analysis of randomized controlled trials. J Intern Med 2009; 265: 568-80. 4. Pearson TA, et al. A community-basecl randomized trial of ezetimibe added to statin therapy to attain NCEP ATP m goals for LDL cholesterol in hypercholesterolemic patients: the ezetimibe add-on to statin for .effectiveness (EASE) trial. Mayo Clin Proc 2005; 80: 587-95. 5. Kastelein JJP, et al. The ENHANCE Investigators. Simvastatin with or without ezetimibe in familial hypercholesterolemia. N Eng! J Med 2008; 358: 1431-43. 6. McKenney JM, et al. Safety and efficacy of long-term co-administration of fenofibrate and ezetimibe in patients with mixed hyperlipidemia. J Am Col/ Cardiol 2006; 47: 1584-7. 7. Salen G, et al. Ezetimibe effectively reduces plasma plant sterols in patients with sitosterolemia. Circulation 2004; 109: 966--71. Adverse Effects and Precautions Ezethnibe is generally well tolerated. The most common adverse effects include headache, abdominal pain, and Etofylline clofibrate, a fibric add derivative (see Bezafibrate, diarrhoea; other gastrointestinal disorders, hypersensitivity Pharmacopoeias. In Eur. (see p. vii) and Jpn. p. 1323.2), is a lipid regulating drug that has been used in reactions including rash and angioedema, fatigue, chest Ph. Bur. 8: (Etilefrine Hydrochloride). A white or almost the treatment of hyperlipidaentias (p. 1248. 1). An oral dose pain, and arthralgia have also been reported. Rare adverse white, crystalline powder or colourless crystals. Freely of 250 mg two or three thnes daily has been given. effects include raised liver enzymes or hepatitis, pancreat­ soluble in water; soluble in alcohol; practically insoluble in itis, thrombocytopenia, cholelithiasis, and cholecystitis. dichloromethane. Store in airtight containers. Protect from �:.��-��t����············································································ Myalgia has occurred in patients taking ezetimibe either light. alone or when added to a statin (see Effects on Skeletal Proprietary Preparations (details are given in Volume B) Muscle, p. 1380.1). Ezetimibe should be stopped if Profile Single-ingredient Preparations. Cz. : Duolipt; Ger.: Duolipt; myopathy is suspected or creatine phosphokinase increases Hong Kong: Duolipt. significantly. Etilefrine is a direct-acting sympathontimetic (p. 1507.3) Ezetimibe should be avoided in patients with moderate with beta -agonist properties, and some alpha- and betar 1 or severe hepatic impairment. agonist actions. It is used for the treatment of hypotensive (BAN, USAN, r/NN) states (p. 1277.2). It is given orally as the hydrochloride in E:zetimibe Reviews. usual doses of 5 or 10 mg three times daily; modified-release l. Jacobson TA, et al. Safety considerations with gastrointestinally active lipid-lowering drugs: Am J Cardiol 2007; 99 (Issue 6 suppl l): 47C-55C. dosage forms may be given in doses of 2 5 mg once or twice 2. Kashani A, et al. Review of side-effect profile of combination ezetimibe daily. Etilefrine hydrochloride can also be given parent­ and statin therapy in randomized clinical trials. Am J Cardio/ 2008; 101: erally. 1606-13. Etilefrine polistirex has been used in the management of rhinitis. Carcinogenicity. Statins are not thought to cause cancer (for a discussion, see Malignant Neoplasms under Uses Parphyria. The Drug Database for Acute Porphyria, com­ and Adntinistration of Simvastatin, p. 1491.3). However, piled by the Norwegian Porphyria Centre (NAPOS) and an excess of incident cancer and fatal cancer was seen 1 in the Porphyria Centre Sweden, classifies etilefrine as prob­ patients given combination therapy with simvastatin and ably not porphyrinogenic; it may be used as a drug of first Uses and Administration ezetintibe when compared with placebo. To better exam­ choice and no precautions are needed.1 ine the association, the data were pooled with those of 1. The Drug Database for Acute Porphyria. Available at: http:/lwww. Ezetimibe is an inhibitor of intestinal sterol absorption and two large, uncompleted studies;2 the authors concluded drugs-porphyria.org (accessed 18110/11) inhibits the absorption of cholesterol and plant sterols. It is that there was no evidence that the combination caused used to reduce total cholesterol, low-density lipoprotein cancer, a conclusion that has been criticised.'·' Neither the Priapism. Priapism is a common complication of sickle-cell (LDL)-cholesterol, and apolipoprotein Bin the management FDA6 nor MHRA7 considered that a conclusion could be disease (p. 1123.2) and is often treated with intracavemo­ of hyperlipidaentias (below), and to reduce sitosterol and drawn as to the effect of ezetimibe on cancer. carnpesterol in patients with homozygous fantilial sitoster­ sal alpha agonists (see under Uses of Metarantinol, 1. Rosseb0 AB, et a!. SEAS Investigators. Intensive lipid lowering with p. 1430.2). There have also been reports of the successful olaemia. It is given orally in a usual dose of 10 mg once simvastatin and ezetimibe in aortic stenosis. N Engl J Med 2008; 359: use of etilefrine, both by intracavemosal injection for daily. 1343-56. acute treatment, 1•2 and orally for prophylaxis 1·3 For use in children, see below. 2. Peto R, etal. Analyses of cancer data from three ezetimibe trials. N Eng! J Med 2008; 359: 1357-66. 1. Virag R, et al. Preventive treatment of priapism in sickle cell disease with Reviews. 3. Drazen JM, et al. Ezetimibe and cancer-an uncertain association. N Eng! oral and self-administered intracavemous injection of etilefrine. Urology 1. Sudhop T, von Bergmann K. Cholesterol absorption inhibitors for the J Med 2008; 359: 1398-9. 1996; 47: 777-81. treatment of hypercholesterolaemia. Drugs 2002; 62: 2333-47. 4. Nissen
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