Carvedilol is a vasodilating beta-blocker useful in the treatment of hypertension and
angina pectoris. In addition to lowering blood pressure, carvedilol decreases total
vascular resistance without the reflex tachycardia usually occurring with vasodilators.
It is reported to be well tolerated with renal sparing effects.
화학적 성질
Colourless Crystalline Solid
용도
Carvedilol is a nonselective β-adrenergic blocker with α1-blocking activity. Carvedilol is an antihypertensive used in the treatment of congestive heart failure.
정의
ChEBI: A member of the class of carbazoles that is an adrenergic antagonist with non-selective beta- and alpha-1 receptor blocking properties which helps in the management of congestive heart failure.
일반 설명
Carvedilol (Coreg) is a β-blocker that hasa unique pharmacological profile. Like labetalol, it is aβ-blocker that possesses α1-blocking activity. Only the(S) enantiomer possesses the β-blocking activity, althoughboth enantiomers are blockers of the α1-receptor. Overall,its β-blocking activity is 10- to 100-fold of its α-blocking activity.
생물학적 활성
Potent β -adrenoceptor and α 1 -adrenoceptor antagonist (K i values are 0.81, 0.96 and 2.2 nM for β 1 -, β 2 - and α 1 -adrenoceptors respectively) that displays antihypertensive and peripheral vasodilatory activity. Blocks cardiac inward-rectifier K + (K IR ) channels, voltage-dependent Ca 2+ channels and exhibits antioxidant properties at higher concentrations.
Clinical Use
Carvedilol is also unique in that it possesses antioxidantactivity and an antiproliferative effect on vascular smoothmuscle cells. It thus has a neuroprotective effect and the abilityto provide major cardiovascular organ protection. It isused in treating hypertension and congestive heart failure.
