Name: | Phentolamine |
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PubChem Compound ID: | 5775 |
Description: | A nonselective alpha-adrenergic antagonist. It is used in the treatment of hypertension and hypertensive emergencies, pheochromocytoma, vasospasm of RAYNAUD DISEASE and frostbite, clonidine withdrawal syndrome, impotence, and peripheral vascular disease. |
Molecular formula: | C17H19N3O |
Molecular weight: | 281.352 g/mol |
Synonyms: |
Phentolaminum [INN-Latin]; C 7337; BRN 0272944; 2-((N-(m-Hydroxyphenyl)-p-toluidino)methyl)-2-imidazoline; 2-(N'-p-Tolyl-N'-m-hydroxyphenylaminomethyl)-2-imidazoline; Phenol, 3-[[(4,5-dihydro-1H-imidazol-2-yl)methyl](4-methylphenyl)amino]-; Dibasin; KBio2_003045; Spectrum4_000899; KBio2_000477.
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Name: | Phentolamine |
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Name (isomeric): | DB00692 |
Drug Type: | small molecule |
Description: | A nonselective alpha-adrenergic antagonist. It is used in the treatment of hypertension and hypertensive emergencies, pheochromocytoma, vasospasm of RAYNAUD DISEASE and frostbite, clonidine withdrawal syndrome, impotence, and peripheral vascular disease. |
Brand: | Regitin Methanesulphonate, Phentolamine Mesylate [USAN], Phentolamine Methanesulphonate, Phenotolamine, Regitine Mesylate, Phentolamine Mesilate, Regitine Methanesulfonate, Phentalamine, Regitin, Regitine, Phentolamine Mesylate, Regitipe, Phentolamine Methanesulfonate, Phentolamine, Methyl Sulfonate, Rogitine |
Category: | Sympatholytics, Adrenergic alpha-Antagonists, Antihypertensive Agents |
CAS number: | 50-60-2 |
Indication: | Used as an aid for the diagnosis of pheochromocytoma, and may be administered immediately prior to or during pheochromocytomectomy to prevent or control paroxysmal hypertension resulting from anesthesia, stress, or operative manipulation of the tumor. Phentolamine has also been used to treat hypertensive crisis caused by sympathomimetic amines or catecholamine excess by certain foods or drugs in patients taking MAO inhibitors, or by clonidine withdrawal syndrome. Other indications include the prevention of dermal necrosis and sloughing following IV administration or extravasation of norepinephrine, decrease in impedance to left ventricular ejection and the infarct size in patients with MI associated with left ventricular failure, treatment of erectile dysfunction through self-injection of small doses combined with papaverine hydrochloride into the corpus cavernosum, and as an adjunct to the management of cocaine overdose to reverse coronary vasoconstriction following use of oxygen, benzodiazepines,and nitroglycerin. |
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Pharmacology: |
Phentolamine is indicated for the control of episodes of hypertension and sweating that occur with a disease called pheochromocytoma. If tachycardia is excessive, it may be necessary to use a beta-blocking agent concomitantly. Phentolamine is a long-acting, adrenergic, alpha-receptor blocking agent which can produce and maintain "chemical sympathec...
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Mechanism of Action: |
Phentolamine produces its therapeutic actions by competitively blocking alpha-adrenergic receptors (primarily excitatory responses of smooth muscle and exocrine glands), leading to a muscle relaxation and a widening of the blood vessels. This widening of the blood vessels results in a lowering of blood pressure. The action of phentolamine on the al...
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Route of elimination: | 10-13% of the drug is excreted unchanged in urine, and the fate of the remainder of the drug is unknown. |
Half Life: | 19 minutes |
Affected organisms: | Humans and other mammals |
Drug interaction: |
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