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Phentalamine

Phentalamine - General Information

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. [PubChem]

 

Pharmacology of Phentalamine

Phentalamine 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. Phentalamine is a long-acting, adrenergic, alpha-receptor blocking agent which can produce and maintain "chemical sympathectomy" by oral administration. It increases blood flow to the skin, mucosa and abdominal viscera, and lowers both supine and erect blood pressures. It has no effect on the parasympathetic system. Phentalamine works by blocking alpha receptors in certain parts of the body. Alpha receptors are present in the muscle that lines the walls of blood vessels. When the receptors are blocked by Phentalamine, the muscle relaxes and the blood vessels widen. This widening of the blood vessels results in a lowering of blood pressure.

 

Phentalamine for patients

 

Phentalamine Interactions

Diagnosis of pheochromocytoma - phentolamine blocking test.

The test is most reliable in detecting pheochromocytoma in patients with sustained hypertension and least reliable in those with paroxysmal hypertension. False-positive tests may occur in patients with hypertension without pheochromocytoma.

 

Phentalamine Contraindications

Myocardial infarction, history of myocardial infarction, coronary insufficiency, angina, or other evidence suggestive of coronary artery disease; hypersensitivity to phentolamine or related compounds.

 

Additional information about Phentalamine

Phentalamine Indication: For the prevention or treatment of dermal necrosis and sloughing following intravenous administration or extravasation of norepinephrine. Also for the prevention or control of hypertensive episodes that may occur in a patient with pheochromocytoma as a result of stress or manipulation during preoperative preparation and surgical excision.
Mechanism Of Action: Phentalamine produces its therapeutic actions by blocking alpha receptors, 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.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Phentolamine
Synonyms: Not Available
Drug Category: Antihypertensive Agents; Sympatholytics
Drug Type: Small Molecule; Approved

Other Brand Names containing Phentolamine: Phenotolamine; Phentalamine; Phentolamine Mesilate; Phentolamine Mesylate; Phentolamine Mesylate [USAN]; Phentolamine Methanesulfonate; Phentolamine Methanesulphonate; Phentolamine, Methyl Sulfonate; Regitin; Regitin Methanesulphonate; Regitine; Regitine Mesylate; Regitine Methanesulfonate; Regitipe; Rogitine;
Absorption: Not Available
Toxicity (Overdose): Not Available
Protein Binding: Not Available
Biotransformation: Not Available
Half Life: 19 minutes
Dosage Forms of Phentalamine: Solution Intravenous
Tablet, extended release Oral
Chemical IUPAC Name: 3-[4,5-dihydro-1H-imidazol-2-ylmethyl-(4-methylphenyl)amino]phenol
Chemical Formula: C17H19N3O
Phentolamine on Wikipedia: https://en.wikipedia.org/wiki/Phentolamine
Organisms Affected: Humans and other mammals