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20-September-2008 09:55:48 - Guanethidine Guanethidine Systematic IUPAC name 2-2-azocan-1-ylethylguanidine Identifiers CAS number 645-43-2 ATC code C02CC02 S01EX01 PubChem 3518 DrugBank APRD01007 Chemical data Formula C10H22N4 Mol. mass 198.309 g/mol Pharmacokinetic data Bioavailability ? Metabolism ? Half life 1.5 days Excretion ? Therapeutic considerations Pregnancy cat. ? Legal status Routes ? Guanethidine is an antihypertensive drug that reduces the release of catecholamines, such as noradrenaline. Its mechanism is inhibition of the Mg++ATPase dependent pump. Side effects include orthostatic and exercise hypotension, sexual dysfunction, and diarrhea. It is no longer available in the US due to side effects and because substantially better drugs are available. It is still licensed in some countries, e.g. UK, for the rapid control of blood pressure in a hypertensive emergency. Guanethidine is transported by uptake 1 into the presynaptic terminal. In this it competes with noradrenaline so can potentiate exogenously applied noradrenaline. Once inside the terminal it blocks the release of noradrenaline in response to arrival of an action potential. Spontaneous release is not affected. Intravenous nerve block Bier block using guanethidine can be used to treat chronic pain caused by complex regional pain syndrome. v d e Adrenergic agonists models/most important in CAPS α α1 METHOXAMINE - Methylnorepinephrine - Oxymetazoline - PHENYLEPHRINE - Metaraminol α2 4-NEMD - CLONIDINE - Guanfacine - Guanabenz - Guanoxabenz - Guanethidine - Xylazine - METHYLDOPA - Apraclonidine - Brimonidine - Detomidine - Dexmedetomidine - Lofexidine - Romifidine - Tizanidine - Xylometazoline Undetermined/ unsorted Amidephrine - Amitraz - Anisodamine - Ergotamine - Indanidine - Medetomidine - Mephentermine - Midodrine - Mivazerol - Naphazoline - Norfenefrine - Octopamine - Phenylpropanolamine - Rilmenidine - Synephrine - Talipexole - Tetrahydrozoline - Xylometazoline β β1 DOBUTAMINE - Dopamine - Denopamine - Xamoterol β2 Short acting β2-agonists: SALBUTAMOL/Levosalbutamol - Fenoterol - TERBUTALINE - Pirbuterol - Procaterol - Bitolterol - Rimiterol - Carbuterol - Tulobuterol - Reproterol - Dopexamine Long acting β2-agonists LABA: Arformoterol - Bambuterol - Clenbuterol - Formoterol - Salmeterol Orciprenaline/metaproterenol - Ritodrine - Hexoprenaline - Indacaterol β3 Amibegron - Solabegron Undetermined/ unsorted Arbutamine - Befunolol - Isoxsuprine - Nylidrin - Oxyfedrine - Prenalterol - Ractopamine - Bromoacetylalprenololmenthane - Broxaterol - Cimaterol - Higenamine - Mabuterol - Methoxyphenamine - Tretoquinol - Zinterol Nonselective β ISOPRENALINE/ISOPROTERENOL α and β Epinephrine α1+2, β1+2 - Norepinephrine α1+2, β1 - Cirazoline - Etilefrine Indirect/ mixed Indirect presynaptic norepinephrine release: Amphetamine - Tyramine Mixed: Ephedrine - Pseudoephedrine Cocaine see also monoamine oxidase inhibitor 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 v d e Ophthalmologicals: antiglaucoma preparations and miotics S01E Sympathomimetics Apraclonidine Brimonidine Clonidine Dipivefrine Epinephrine Parasympathomimetics M: Aceclidine Pilocarpine M/N: Acetylcholine Carbachol AI: Demecarium Echothiophate Stigmine Fluostigmine, Neostigmine, Physostigmine Paraoxon Carbonic anhydrase inhibitors Acetazolamide Brinzolamide Diclofenamide Dorzolamide Methazolamide Beta blocking agents Befunolol Betaxolol Carteolol Levobunolol Metipranolol Timolol Prostaglandin analogues Bimatoprost Latanoprost Travoprost Unoprostone Other agents Dapiprazole Guanethidine Structure of captopril, the first clinically successful ACE inhibitor This antihypertensive-related article is a stub. Retrieved from http://en..org/wiki/Guanethidine Categories: Antihypertensive agent stubs 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 Magyar Polski РуÑ?Ñ?кий This page was last modified on 10 August 2008, at 13:5
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