Drug intelligence / Profile preview

Tolazoline

Development stage
Discontinued
Modality
Small Molecules
Administration
Intravenous, Intra-arterial, Intramuscular, Subcutaneous
01

Overview

Tolazoline is a non-selective competitive alpha-adrenergic receptor antagonist and vasodilator primarily used to treat spasms of peripheral blood vessels and persistent pulmonary hypertension of the newborn. It acts by directly relaxing vascular smooth muscle, leading to decreased total peripheral resistance and increased cardiac output. Tolazoline exhibits moderate alpha-adrenergic blocking activity (antagonist at both alpha-1 and alpha-2 adrenergic receptors) as well as histamine agonist activity at H1 and H2 receptors. Its therapeutic effects are mediated through both direct action on blood vessels and indirect effects via release of endogenous histamine. In veterinary medicine, it is commonly used to reverse xylazine-induced sedation[1][2][3][4][5][6].

Brand names
PriscolineTolazine
Other names
Tolazoline hydrochlorideTolazoline HCl
02

Targets

ADRA2A (α2A)HRH2 (Histamine H2 Receptor)ADRA1A (α1A)HRH1 (Histamine H1 Receptor)

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