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RX BIN: 015558RX PCN: HTGroup ID: DDN6600Card Holder ID: DDN6600
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Phentolamine volume of distribution

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What is Phentolamine

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.

Phentolamine 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 alpha adrenergic receptors is relatively transient and the blocking effect is incomplete. The drug is more effective in antagonizing responses to circulating epinephrine and/or norepinephrine than in antagonizing responses to mediator released at the adrenergic nerve ending. Phentolamine also stimulates -adrenergic receptors and produces a positive inotropic and chronotropic effect on the heart and increases cardiac output.

Dosage forms of Phentolamine

Injection, solutionsubmucosal.235 mg/mL
Solutionsubmucosal0.4 mg
Injection, powder, for solutionintramuscular; intravenous5 mg/mL

Prescription Generics


International Brands



2-(N-(m-Hydroxyphenyl)-P-toluidinomethyl)imidazoline Fentolamina



CAS number






Affected organisms

Humans and other mammals

Indication of Phentolamine

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.

Toxicity of Phentolamine

RX24 Drugs Disclaimer: before buying a Phentolamine on prescription, consult your healthcare provider. Content on this page is provided for informational purposes only. Any use of this information is at your own risk.

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