NCIt definition : The hydrochloride form of labetalol, a third generation selective alpha-1-adrenergic
antagonist and non-selective beta-adrenergic antagonist with vasodilatory and antihypertensive
properties. Labetalol competitively binds to alpha-1-adrenergic receptors in vascular
smooth muscle, thereby inhibiting the adrenergic stimulation of endothelial cell function
and vasoconstriction in peripheral blood vessels. This agent also binds to beta-receptors
in the bronchial and vascular smooth muscle, resulting in a decrease in adrenergic
stimulation. The result is a decrease in resting and exercise heart rates, cardiac
output, and in both systolic and diastolic blood pressure, thereby resulting in vasodilation,
and negative chronotropic and inotropic cardiac effects.;