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20-September-2008 09:55:49 - Phentolamine Phentolamine Systematic IUPAC name 3-4,5-dihydro-1H-imidazol-2-ylmethyl- 4-methylphenyl-aminophenol Identifiers CAS number 50-60-2 ATC code C04AB01 G04BE05 PubChem 5775 DrugBank APRD00615 Chemical data Formula C17H19N3O Mol. mass 281.352 g/mol Pharmacokinetic data Bioavailability ? Metabolism Hepatic Half life 19 minutes Excretion ? Therapeutic considerations Pregnancy cat. C U.S. Legal status Routes Usually IV or IM Phentolamine Regitine is a reversible1 nonselective alpha-adrenergic antagonist. 2 Mechanism Its primary action is vasodilation due to α1 blockade.3 It also can lead to reflex tachycardia because of hypotension and α2 inhibition, which increases sympathetic tone.4 Uses The primary application for phentolamine is for the control of hypertensive emergencies, most notably due to phaeochromocytoma pheochromocytoma.5 It also has usefulness in the treatment of cocaine induced hypertension, where one would generally avoid beta blockers and where calcium channel blockers are not effective.67 In this context it is probably most safely given by infusion since bolus doses have a propensity towards causing precipitous falls in blood pressure. When given by injection it causes blood vessels to expand, thereby increasing blood flow. When injected into the penis intracavernosal, it increases blood flow to the penis, which results in an erection.8 It may be stored in crash carts to counteract severe peripheral vasoconstriction secondary to extravasation of peripherally placed vasopressor infusions, typically of norepinephrine. Epinephrine infusions are less vasoconstrictive than norepinephrine as they primarily stimulate beta receptor more than alpha receptors, but the effect remains dose dependent. Phentolamine also has diagnostic and therapeutic roles in complex regional pain syndrome reflex sympathetic dystrophy.9 References ^ Jewell, John R.; Longworth, David L.; Stoller, James K.; Casey, David 2003. The Cleveland Clinic internal medicine case reviews. Hagerstown, MD: Lippincott Williams Wilkins, 32. ISBN 0-7817-4266-8. ^ MeSH Phentolamine ^ Brock G. Oral phentolamine Vasomax. Drugs Today Barcelona. 2000 Feb-Mar;362-3:121-4. ^ Shen, Howard 2008. Illustrated Pharmacology Memory Cards: PharMnemonics. Minireview, 14. ISBN 1-59541-101-1. ^ Tuncel M, Ram VC. Hypertensive emergencies. Etiology and management. American Journal of Cardiovascular Drugs. 2003;31:21-31. ^ Hollander JE, Henry TD. Evaluation and management of the patient who has cocaine-associated chest pain. Cardiology Clinics. 2006 Feb;241:103-14. ^ Chan GM, Sharma R, Price D, Hoffman RS, Nelson LS. Phentolamine Therapy for Cocaine-Association Acute Coronary Syndrome CAACS. Journal of Medical Toxicology. 2006 Sep;23:108-11. ^ Bella AJ, Brock GB. Intracavernous pharmacotherapy for erectile dysfunction. Endocrine. 2004 Mar-Apr;232-3:149-55. ^ Rowbotham MC. Pharmacologic management of complex regional pain syndrome. Clinical Journal of Pain. 2006 Jun;225:425-9. 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 Peripheral vasodilators C04 Imidazoline derivatives Phentolamine - Tolazoline Niacin and derivatives Niacin Purine derivatives Pentoxifylline Ergot alkaloids Ergoloid- Nicergoline Other peripheral vasodilators Phenoxybenzamine - Vincamine - Naftidrofuryl v d e Urologicals G04 Acidifiers Ammonium chloride, Calcium chloride Urinary antispasmodics primarily antimuscarinics Darifenacin, Emepronium, Fesoterodine, Flavoxate, Imidafenacin, Meladrazine, Oxybutynin, Propiverine, Solifenacin, Terodiline, Tolterodine, Trospium For erectile dysfunction Prostaglandins E Alprostadil PDE5 inhibitors Avanafil - Sildenafil - Tadalafil - Udenafil - Vardenafil Alpha blockers Moxisylyte - Phentolamine - Yohimbine Others Apomorphine - Papaverine Other urologicals Acetohydroxamic acid, Collagen, Dimethyl sulfoxide, Magnesium hydroxide, Pentosan polysulfate, Phenazopyridine, Phenyl salicylate, Succinimide For BPH 5α-reductase inhibitors Dutasteride, Finasteride Alpha blockers α1 Alfuzosin, Doxazosin, Silodosin, Tamsulosin, Terazosin Herbals Pygeum africanum, Serenoa repens v d e Adrenergic antagonists α α1 selective Doxazosin · Prazosin · Alfuzosin · Terazosin · Indoramin · Urapidil · Trimazosin · Moxisylyte · 1A Tamsulosin, Silodosin α2 selective Atipamezole · Efaroxan · Idazoxan · Yohimbine · Benzylpiperazine · Rauwolscine · Mirtazapine Non-selective α reversible Phentolamine · irreversible Phenoxybenzamine β β1 selective cardioselective Atenolol · Acebutolol · Celiprolol · Betaxolol · Bisoprolol · Esmolol · Metoprolol · Nebivolol β2 selective Butaxamine · ICI 118551 β3 selective SR 59230A Non-selective β Alprenolol · Amosulalol · Metipranolol · Nadolol · Oxprenolol · Penbutolol · Pindolol · Propranolol · Tertatolol · Timolol · Tilisolol · Sotalol Mixed α1/β Carvedilol · Labetalol · Arotinolol Retrieved from http://en..org/wiki/Phentolamine Categories: Antihypertensive agents | Vasodilators | Imidazolines | Alpha blockers 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 Español This page was last modified on 10 August 2008, at 02:47
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