Phentolamine mesilate is alpha receptor blockers, and indirect excited by blocking alpha receptors beta receptors, rapidly expand blood vessels around, can significantly reduce the peripheral vascular resistance, increase peripheral blood volume, improve microcirculation. This product has an exciting effect on the heart, making the myocardial contractile force increase, heart rate accelerate, cardiac output increase.
The primary application for phentolamine is for the control of hypertensive emergencies, most notably due to pheochromocytoma.It also has usefulness in the treatment of cocaine-induced cardiovascular complications, where one would generally avoid β-blockers (z.B. metoprolol), as they can cause unopposed α-adrenergic mediated coronary vasoconstriction, worsening myocardial ischemia and hypertension.It is important to note that phentolamine is not a first-line agent for this indication. Phentolamine should only be given to patients who do not fully respond to benzodiazepines, nitroglycerin, and calcium channel blockers.
When given by injection it causes blood vessels to dilate, thereby increasing blood flow. When injected into the penis (intracavernosal), it increases blood flow to the penis, which results in an erection.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 β receptor more than α receptors, but the effect remains dose-dependent.
Phentolamine also has diagnostic and therapeutic roles in complex regional pain syndrome (reflex sympathetic dystrophy).Phentolamine is marketed in the dental field as a local anesthetic reversal agent. Branded as OraVerse, it is a phentolamine mesylate injection designed to reverse the local vasoconstrictor properties used in many local anesthetics to prolong anesthesia.
