DILEVALOL

Description

Dilevalol is a "dual-mechanism" antihypertensive reportedly suitable for a wide range of patients. Its partial beta2-agonist action is expected to induce vasodilation, whereas its beta1-antagonist component may protect against stress-induced hemodynamic charges without altering the cardiac output. Dilevalol is the R,R-isomer of labetalol.

Originator

Schering Plough (USA)

Uses

Specific competitive antagonist at both α-and β-adrenergic receptor sites. Antihypertensive.

Uses

(R,R)-Labetalol is a specific competitive antagonist at both α-and β-adrenergic receptor sites. (R,R)-Labetalol is used as an antihypertensive.

Definition

ChEBI: (R,R)-labetalol is a 2-hydroxy-5-{1-hydroxy-2-[(4-phenylbutan-2-yl)amino]ethyl}benzamide that has 1R,2R-configuration. It is a conjugate base of a dilevalol(1+).

brand name

Levadil; Dilevalon

World Health Organization (WHO)

Dilevalol, a beta-adrenoreceptor antagonist, was introduced into medicine in 1989 for the treatment of hypertension. Shortly afterwards, its use became associated with isolated cases of hepatic toxicity. Although few cases were reported, the manufacturer discontinued sales in Japan and Portugal, the only countries where the drug was marketed, and withdrew applications for registration elsewhere.