Phentolamine

Phentolamine

Clinical data
Pregnancy category	C (U.S.)
Routes of administration	Usually IV or IM
ATC code	C04AB01 (WHO) G04BE05 (WHO)
Pharmacokinetic data
Metabolism	Hepatic
Elimination half-life	19 minutes
Identifiers
IUPAC name 3-[4,5-dihydro-1H-imidazol-2-ylmethyl- (4-methylphenyl)-amino]phenol
CAS Number	50-60-2
PubChem CID	5775
DrugBank	APRD00615
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}
Chemical and physical data
Formula	C17H19N3O
Molar mass	281.352 g/mol

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Overview

Phentolamine (Regitine) is a reversible nonselective alpha-adrenergic antagonist. Its primary action is vasodilation. The primary application for phentolamine is for the control of hypertensive emergencies, most notably due to phaeochromocytoma (pheochromocytoma). It also has usefulness in the treatment of cocaine induced hypertension, where one would generally avoid beta blockers and where calcium channel blockers are not effective. In this context it is probably most safely given by infusion since bolus doses have a propensity towards causing precipitous falls in blood pressure.

When given by injection it causes blood vessels to expand, 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 beta receptor more than alpha receptors, but the effect remains dose dependent.

Phentolamine also has diagnostic and therapeutic roles in complex regional pain syndrome (reflex sympathetic dystrophy).

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