Drug intelligence / Profile preview

phentolamine

Development stage
Approved
Lead developer
Novartis
Modality
Small Molecules
Administration
Intravenous, Intramuscular, Subcutaneous, Submucosal Injection, Intracavernosal Injection, Ophthalmic
01

Overview

Phentolamine is a reversible, non-selective alpha-adrenergic antagonist (alpha blocker) that induces vasodilation by competitively blocking both alpha-1 and alpha-2 adrenergic receptors. It is primarily used for the prevention or control of hypertensive episodes in patients with pheochromocytoma, for the diagnosis of pheochromocytoma via the phentolamine blocking test, and to prevent or treat dermal necrosis following norepinephrine extravasation. Phentolamine can also be used to reverse soft tissue anesthesia and pharmacologically induced mydriasis. Additionally, it has been used as an intracavernosal injection to induce erections by increasing penile blood flow through smooth muscle relaxation. Its mechanism involves direct antagonism at alpha-1 and alpha-2 adrenergic receptors on vascular smooth muscle as well as indirect endothelium-mediated mechanisms involving nitric oxide synthase activation[1][3][6][8].

Brand names
RegitineOraVerseRyzumvi
Other names
phentolamine mesylate
02

Targets

ADRA1A (α1A)ADRA2A (α2A)

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