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News About Bosentan

20-September-2008 09:55:47 - Bosentan Bosentan Systematic IUPAC name N-6-2-hydroxyethoxy-5- 2-methoxyphenoxy -2-pyrimidin-2-yl-pyrimidin-4-yl -4-tert- butyl-benzenesulfonamide Identifiers CAS number 147536-97-8 ATC code C02KX01 PubChem 104865 DrugBank APRD00829 Chemical data Formula C27H29N5O6S Mol. mass 551.615 g/mol SMILES eMolecules PubChem Pharmacokinetic data Bioavailability 50% Protein binding 98% Metabolism Hepatic Half life 5 hours Excretion ? Therapeutic considerations Pregnancy cat. X Legal status ℞ Prescription only Routes Oral Bosentan BOZENTAN is a dual endothelin receptor antagonist important in the treatment of pulmonary artery hypertension PAH. It is licensed in the United States, the European Union and other countries by Actelion Pharmaceuticals for the management of PAH under the trade name Tracleer. Contents 1 Mechanism of Action 2 Clinical uses 3 External links 4 See also Mechanism of Action Bosentan is a competitive antagonist of endothelin-1 at the endothelin-A ET-A and endothelin-B ET-B receptors. When endothelin-1 binds to these receptors, pulmonary artery pressure is elevated. By blocking this interaction, bosentan is able to lower pulmonary artery pressure. Bosentan has a slightly higher affinity for ET-A than ET-B. Clinical uses Bosentan is indicated mainly for the treatment of pulmonary hypertension. In 2007, Tracleer® bosentan was approved in the European Union also for reducing the number of new digital ulcers in patients with systemic sclerosis and ongoing digital ulcer disease. External links Tracleer official website Tracleer prescribing information See also Sitaxsentan Ambrisentan v d e Medications used in the management of pulmonary arterial hypertension B01, C02 Prostacyclin analogues Beraprost, Epoprostenol, Iloprost, Treprostinil Endothelin receptor antagonists Ambrisentan, Bosentan, Sitaxsentan PDE5 inhibitors Sildenafil, Tadalafil Adjunctive therapy Calcium channel blockers, Diuretics, Digoxin, Oxygen therapy, Warfarin 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/Bosentan Categories: Endothelin receptor antagonists | Orphan drugs 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 Italiano This page was last modified on 11 August 2008, at 09:38

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