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20-September-2008 09:55:46 - Amiloride Amiloride Systematic IUPAC name 3,5-diamino-6-chloro-N-diaminomethylenepyrazine-2-carboxamide Identifiers CAS number 2016-88-8 ATC code C03DB01 PubChem 16231 DrugBank APRD00790 Chemical data Formula C6H8ClN7O Mol. mass 229.627 g/mol Pharmacokinetic data Bioavailability Readily absorbed Metabolism none Half life 6 to 9 hours Excretion unchanged in urine Therapeutic considerations Pregnancy cat. ? Legal status Routes oral Amiloride is a potassium-sparing diuretic, first approved for use in 1967 then known as MK 870, used in the management of hypertension and congestive heart failure. Contents 1 Structure 2 Mode of action 3 See also 4 References Structure Amiloride is a guanidinium group containing pyrazine derivative. Mode of action Amiloride works by directly blocking the epithelial sodium channel ENaC thereby inhibiting sodium reabsorption in the distal convoluted tubules and collecting ducts in the kidneys this mechanism is the same for triamterene. This promotes the loss of sodium and water from the body, but without depleting potassium. The drug is often used in conjunction with thiazide e.g. co-amilozide or loop diuretics e.g. co-amilofruse. Due to its potassium-sparing capacities, hyperkalemia high blood potassium levels are occasionally observed in patients taking amiloride. The risk is high in concurrent use of ACE inhibitors or spironolactone. Patients are also advised not to use potassium-containing salt replacements.1 Amiloride also carries the risk of developing an acidosis. A fraction of the effects of amiloride is inhibition of cyclic GMP-gated cation channels in the inner medullary collecting duct.2 See also Benzamil References ^ LoSalt Advisory Statement PDF ^ Walter F., PhD. Boron. Medical Physiology: A Cellular And Molecular Approaoch. Elsevier/Saunders. ISBN 1-4160-2328-3. page 875 v d e Membrane transport modulators Calcium channel blockers Amlodipine Amrinone Anandamide Anipamil Azimilide Bencyclane Benidipine Bepridil Berbamine Bevantolol Canadine Carboxyamido-Triazole Cilnidipine Cinnarizine Clentiazem Conotoxins Darodipine Dauricine Devapamil Diltiazem Dimiapramine Dotarizine Efonidipine Emopamil Enpiperate Eperisone Falipamil Fantofarone Fasudil Felodipine Fenamic acid Fendiline Flunarizine Fosfedil Gabapentin Gallopamil Isradipine Lacidipine Lamotrigine Lercanidipine Lidoflazine Magnesium sulfate Manidipine Manoalide Mepirodipine Mibefradil Monatepil Naftopidil Nicardipine Nifedipine Niguldipine Niludipin Nilvadipine Nimodipine Nisoldipine Nitrendipine Norverapamil Ochratoxin A Octylonium Osthol Oxodipine Perhexiline Pinaverium Piperidine Pranidipine Prenylamine Risedronic acid Ryodipine Sesamodil Stepholidine Terodiline Tetrahydropalmatine Tetrandrine Tolfenamic acid Tranilast Verapamil Potassium channel blockers 3,4-Diaminopyridine 4-Aminopyridine Dofetilide Linopirdine Paxilline Tetraethylammonium Sodium channel blockers Amiloride Encainide Pilsicainide Tetrodotoxin Tocainide Sodium chloride symporter inhibitors Bendroflumethiazide Chlorothiazide Chlorthalidone Cyclopenthiazide Hydrochlorothiazide Hydroflumethiazide Methyclothiazide Polythiazide Trichlormethiazide Sodium potassium chloride symporter inhibitors Bumetanide Furosemide 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 Tablets This pharmacology-related article is a stub. Retrieved from http://en..org/wiki/Amiloride Categories: Pharmacology stubs | Potassium-sparing diuretics | Pyrazines | Guanidines 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 Français Hrvatski Magyar 日本語 Português ไทย This page was last modified on 1 August 2008, at 02:37
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