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News About Eplerenone

20-September-2008 09:55:48 - Eplerenone Eplerenone Systematic IUPAC name pregn-4-ene-7,21-dicarboxylic acid, 9,11-epoxy-17-hydroxy-3-oxo, γ-lactone, methyl ester 7α, 11α, 17α Identifiers CAS number 107724-20-9 ATC code C03DA04 PubChem 5282131 DrugBank APRD00707 Chemical data Formula C24H30O6 Mol. mass 414.49 Pharmacokinetic data Bioavailability 69% Metabolism hepatic CYP3A4 Half life 3-5 hours Excretion 67% renal 32% biliary Therapeutic considerations Pregnancy cat. B3 Aust Legal status Schedule 4 Aust, Rx only US Routes oral Eplerenone INN pronounced /ɛpˈlɛrənoʊn/ is an aldosterone antagonist used as an adjunct in the management of chronic heart failure. It is similar to spironolactone, though it may be more specific for the mineralocorticoid receptor and is specifically marketed for reducing cardiovascular risk in patients following myocardial infarction. It is marketed by Pfizer under the trade name Inspra. Contents 1 Clinical use 1.1 Indications 1.2 Contraindications 1.3 Adverse effects 1.4 Drug interactions 2 General considerations 3 See also 4 References Clinical use Indications Eplerenone is specifically indicated for the reduction of risk of cardiovascular death in patients with heart failure and left ventricular dysfunction within 3-14 days of an acute myocardial infarction, in combination with standard therapies and as treatment against hypertension. Contraindications Eplerenone is contraindicated in patients with hyperkalaemia, severe renal impairment creatinine Cl less than 30 ml/min, or severe hepatic impairment Child-Pugh C. The manufacturer of eplerenone also contraindicates relative C.I. concomitant treatment with ketoconazole, itraconazole or other potassium-sparing diuretics though the manufacturer still considers taking these drugs to be absolute C.I. Potential benefits should be weighted against possible risks. Adverse effects Common adverse drug reactions ADRs associated with the use of eplerenone include: hyperkalaemia, hypotension, dizziness, altered renal function, and increased creatinine concentration.1 Drug interactions Eplerenone is primarily metabolised by the cytochrome P450 enzyme CYP3A4. Thus the potential exists for adverse drug interactions with other drugs that induce or inhibit CYP3A4. Specifically, the concomitant use of the CYP3A4 potent inhibitors ketoconazole and itraconazole is contraindicated. Other CYP3A4 inhibitors including erythromycin, saquinavir, and verapamil should be used with caution. Other drugs that increase potassium concentrations may increase the risk of hyperkalaemia associated with eplerenone therapy, including salt substitutes,2 potassium supplements and other potassium-sparing diuretics. General considerations Due to the high risk of elevated potassium levels in individuals taking eplerenone, The United States FDA suggests routine checks on the individual's potassium level to screen for hyperkalemia. See also Spironolactone Aldosterone antagonist Canrenone References ^ Rossi S, or. Australian Medicines Handbook 2006. Adelaide: Australian Medicines Handbook; 2006 ^ LoSalt Advisory Statement PDF v d e Antihypertensives C02 and diuretics C03 Sympatholytic agents Centrally acting/antiadrenergics α2 agonist Clonidine, Guanfacine, Methyldopa imidazoline receptor agonist Moxonidine, Rilmenidine adrenergic uptake inhibitor Rescinnamine, Reserpine Ganglion-blocking/nicotinic antagonist Mecamylamine, Trimethaphan Peripherally acting/antiadrenergics α1 blockers: Prazosin Indoramin Trimazosin Doxazosin Urapidil Guanidine derivatives: Betanidine Guanethidine Guanoxan Debrisoquine Guanoclor Guanazodine Guanoxabenz Vasodilators Diazoxide hydrazinophthalazine Hydralazine, Dihydralazine, Endralazine, Cadralazine Minoxidil Nitroprusside Phentolamine Other antihypertensives serotonin antagonist Ketanserin endothelin receptor antagonist Bosentan, Ambrisentan, Sitaxsentan MAOI Pargyline THI Metirosine Diuretics Low ceiling Thiazides at DCT Bendroflumethiazide Hydroflumethiazide Hydrochlorothiazide Chlorothiazide Polythiazide Trichlormethiazide Cyclopenthiazide Methyclothiazide Cyclothiazide Mebutizide Sulfonamides Quinethazone Clopamide Chlortalidone Mefruside Clofenamide Metolazone Meticrane Xipamide Indapamide Clorexolone Fenquizone Other Mersalyl Theobromine Cicletanine osmotic Mannitol, Urea carbonic anhydrase inhibitor at PT Acetazolamide High ceiling Loop diuretic at AL Bumetanide, Furosemide, Torasemide, Ethacrynic acid Potassium-sparing at CD ESC blockers Amiloride, Triamterene aldosterone antagonists Spironolactone, Eplerenone, Potassium canrenoate, Canrenone Retrieved from http://en..org/wiki/Eplerenone Categories: Aldosterone antagonists 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 Deutsch Español 日本語 This page was last modified on 31 May 2008, at 18:34

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