Drug intelligence / Profile preview

carvedilol controlled release + lisinopril

Development stage
Phase 3
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

Carvedilol controlled release (CR) plus lisinopril is a fixed-dose combination therapy used primarily for the management of hypertension and heart failure. Carvedilol is a non-selective beta-adrenergic antagonist with additional alpha-1 adrenergic blocking activity, leading to decreased heart rate, reduced myocardial contractility, and vasodilation. Lisinopril is an angiotensin-converting enzyme inhibitor (ACEI) that prevents the conversion of angiotensin I to angiotensin II, resulting in vasodilation and reduced aldosterone-mediated volume expansion. The combination targets multiple pathways involved in blood pressure regulation and cardiac remodeling. Clinical studies have shown that this combination can improve endothelial function and reduce oxidative stress in patients with hypertension or heart failure[1][2]. Both drugs are well-established therapies individually; their combined use aims to achieve better blood pressure control and cardiovascular protection than monotherapy.

Brand names
Coreg CR + ZestrilCoreg CR + Prinivil
Other names
carvedilol CR + lisinoprilextended-release carvedilol + lisinopril
02

Targets

HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))ACE (Angiotensin Converting Enzyme)DRD2 (Dopamine D2 Receptor)ADRA1A (α1A)ADRB1 (β1)ADRB2 (β2)

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