Drug intelligence / Profile preview

labetalol

Development stage
Approved
Lead developer
GSK
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Labetalol is a non-selective beta-adrenergic receptor antagonist (beta blocker) with additional selective alpha-1 adrenergic receptor blocking activity. It is used primarily to treat hypertension (high blood pressure), including hypertensive emergencies and high blood pressure in pregnancy. Labetalol works by relaxing blood vessels and slowing the heart rate, which improves blood flow and decreases blood pressure. Its mechanism of action involves competitive antagonism at both beta-1, beta-2, and alpha-1 adrenergic receptors, leading to decreased peripheral vascular resistance without significant alteration of heart rate or cardiac output. Labetalol is available as oral tablets or intravenous injection[1][2][5][6][7].

Brand names
TrandateNormodyne
Other names
IbidomideAH-5158 hydrochlorideAH5158 hydrochlorideAH 5158 hydrochloride
02

Targets

ADRA1A (α1A)ADRB2 (β2)ADRB1 (β1)

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