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Phentolamine
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Systematic (IUPAC) name
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3-[4,5-dihydro-1H-imidazol-2-ylmethyl- (4-methylphenyl)-amino]phenol
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Identifiers
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CAS number
| 50-60-2
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ATC code
| C04AB01 G04BE05
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PubChem
| 5775
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DrugBank
| APRD00615
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Chemical data
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Formula | C17H19N3O
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Mol. mass | 281.352 g/mol
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Pharmacokinetic data
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Bioavailability | ?
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Metabolism | Hepatic
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Half life | 19 minutes
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Excretion | ?
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Therapeutic considerations
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Pregnancy cat.
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C (U.S.)
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Legal status
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Routes
| Usually IV or IM
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Phentolamine (Regitine) is a reversible nonselective alpha-adrenergic antagonist. Its primary action is vasodilation.[1] The primary application for phentolamine is for the control of hypertensive emergencies, most notably due to phaeochromocytoma (pheochromocytoma).[2] 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.[3][4] In this context it is probably most safely given by infusion since bolus doses have a propensity towards causing precipitous falls in blood pressure.
Additional recommended knowledge
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.[5]
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).[6]
References
- ^ Brock G. Oral phentolamine (Vasomax). Drugs Today (Barcelona). 2000 Feb-Mar;36(2-3):121-4.
- ^ Tuncel M, Ram VC. Hypertensive emergencies. Etiology and management. American Journal of Cardiovascular Drugs. 2003;3(1):21-31.
- ^ Hollander JE, Henry TD. Evaluation and management of the patient who has cocaine-associated chest pain.
Cardiology Clinics. 2006 Feb;24(1):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;2(3):108-11.
- ^ Bella AJ, Brock GB. Intracavernous pharmacotherapy for erectile dysfunction. Endocrine. 2004 Mar-Apr;23(2-3):149-55.
- ^ Rowbotham MC. Pharmacologic management of complex regional pain syndrome. Clinical Journal of Pain. 2006 Jun;22(5):425-9.
Antihypertensives (C02) and diuretics (C03) |
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Sympatholytic agents (including alpha) | centrally acting/antiadrenergics (Clonidine, Guanfacine, Methyldopa, Moxonidine, Rescinnamine, Reserpine, Rilmenidine) • ganglion-blocking/nicotinic antagonist (Mecamylamine, Trimethaphan) • peripherally acting/antiadrenergics (Prazosin, Guanethidine, Indoramin, Doxazosin) |
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Vasodilators | Diazoxide • Hydralazine • Minoxidil • Nitroprusside • Phentolamine |
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Other antihypertensives | serotonin antagonist (Ketanserin) • endothelin receptor antagonist (Bosentan, Ambrisentan, Sitaxsentan) |
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Low ceiling diuretics | Thiazide (Bendroflumethiazide, Chlorothiazide, Hydrochlorothiazide) • Chlortalidone • Indapamide • Quinethazone • Mersalyl • Metolazone • Theobromine • Cicletanine |
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High ceiling diuretics | Loop diuretic (Bumetanide, Furosemide, Torasemide) |
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Potassium-sparing diuretics | ESC blockers (Amiloride, Triamterene) • aldosterone antagonists (Spironolactone, Eplerenone, Potassium canrenoate, Canrenone) |
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Peripheral vasodilators (C04) |
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Imidazoline derivatives | Phentolamine - Tolazoline |
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Niacin and derivatives | Niacin |
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Purine derivatives | Pentoxifylline |
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Ergot alkaloids | Ergoloid- Nicergoline |
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Other peripheral vasodilators | Phenoxybenzamine - Vincamine - Naftidrofuryl |
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Urologicals (G04) |
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Acidifiers | Ammonium chloride, Calcium chloride |
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Urinary antispasmodics (primarily antimuscarinics) | Darifenacin, Emepronium, Flavoxate, Meladrazine, Oxybutynin, Propiverine, Solifenacin, Terodiline, Tolterodine, Trospium |
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For erectile dysfunction | Alprostadil, Apomorphine, Moxisylyte, Papaverine, Phentolamine, Yohimbine, PDE5 inhibitors (Avanafil, Sildenafil, Tadalafil, Udenafil, Vardenafil) |
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Other urologicals | Acetohydroxamic acid, Collagen, Dimethyl sulfoxide, Magnesium hydroxide, Pentosan polysulfate, Phenazopyridine, Phenyl salicylate, Succinimide |
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For benign prostatic hypertrophy | 5α-reductase inhibitors: Dutasteride, Finasteride
Alpha blockers: Alfuzosin, Doxazosin, Tamsulosin, Terazosin
Herbals: Pygeum africanum, Serenoa repens |
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