Phentolamine Mesylate 5 mg/mL Suppliers & Bulk Manufacturers

Available Forms: Injection

Available Strengths: 5 mg/mL

Reference Brands: Regitine (USA)

Category: Heart Disorder

Phentolamine Mesylate is a Heart Disorder product available as Injection in strengths 5 mg/mL. It corresponds to the reference brand Regitine (USA). Verified GMP manufacturers and suppliers on PharmaTradz offer it in bulk for import worldwide, with regulatory documentation and dossier support available on request.

Product Description:

Phentolamine mesylate is the mesylate salt of a synthetic imidazoline compound with potent alpha-adrenergic antagonist activity. It acts as a competitive, non-selective blocker of both alpha-1 and alpha-2 adrenergic receptors, leading to peripheral vasodilatation and a reduction in peripheral vascular resistance. Through this mechanism, phentolamine produces a rapid decrease in blood pressure. In addition to its alpha-adrenergic effects, phentolamine may also block 5-hydroxytryptamine (5-HT) receptors and stimulate the release of histamine from mast cells, contributing further to its vasodilatory action.

The primary clinical application of phentolamine is in the management of hypertensive emergencies, particularly those associated with pheochromocytoma, where excessive catecholamine release causes severe and potentially life-threatening hypertension. Its rapid onset of action makes it especially useful in acute care and hospital settings.

Phentolamine also has a role in the management of cocaine-induced cardiovascular complications. In such cases, beta-blockers are generally avoided due to the risk of unopposed alpha-adrenergic stimulation, which can worsen coronary vasoconstriction, myocardial ischemia, and hypertension. Phentolamine is not considered a first-line treatment for this indication and is reserved for patients who do not adequately respond to standard therapies such as benzodiazepines, nitroglycerin, and calcium channel blockers.