Drug intelligence / Profile preview

glyceryl trinitrate + phentolamine

Development stage
Preclinical
Modality
Small Molecules
Administration
Intracavernosal, Intravenous, Topical, Rectal
01

Overview

This is a combination of two vasodilator drugs, glyceryl trinitrate (also known as nitroglycerin) and phentolamine. Glyceryl trinitrate is an organic nitrate that acts primarily as a nitric oxide donor, leading to the activation of guanylate cyclase in vascular smooth muscle and resulting in vasodilation. It is widely used for the treatment and prevention of angina pectoris, heart failure, hypertension, and anal fissures[4][9][10]. Phentolamine is a reversible nonselective alpha-adrenergic antagonist that blocks both alpha-1 and alpha-2 adrenergic receptors. This blockade leads to vasodilation by relaxing vascular smooth muscle; it also increases blood flow when injected locally (e.g., intracavernosal injection for erectile dysfunction)[6][7][8]. The combination may be considered for synergistic or additive vasodilatory effects—for example, in settings where rapid reduction of vascular tone or increased local blood flow is desired (such as certain cases of erectile dysfunction or management of hypertensive emergencies)[3][1]. Both agents act via different but complementary mechanisms to reduce peripheral resistance and increase tissue perfusion.

Other names
nitroglycerin + phentolamineGTN + phentolamine
02

Targets

ADRA1A (α1A)ADRA2A (α2A)sGC (Soluble Guanylyl Cyclase)

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