Drug intelligence / Profile preview

carvedilol

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

Overview

Carvedilol is a non-selective beta-adrenergic antagonist (beta-blocker) with additional alpha-1 adrenergic blocking activity. It is used to treat mild to severe chronic heart failure, hypertension (high blood pressure), and left ventricular dysfunction following myocardial infarction in clinically stable patients. Carvedilol works by blocking beta-1 receptors in the heart and alpha-1 receptors in blood vessels, leading to decreased heart rate and relaxation of blood vessels, which improves cardiac output and lowers blood pressure. The drug is a racemic mixture; the S(-) enantiomer blocks both beta and alpha-1 adrenoceptors while the R(+) enantiomer blocks only alpha-1 adrenoceptors[4][7]. Carvedilol was first approved by the FDA on September 14, 1995[4].

Brand names
CoregCoreg CR
Other names
carvedilol CRcarvedilol phosphate extended-releasecarvedilol extended-release capsules
02

Targets

ADRB1 (β1)ADRB2 (β2)ADRA1A (α1A)

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