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HOME >> API >> API List1 >> Carvedilol >> Drug Description

DRUG DESCRIPTION
Carvedilol CAS No [72956-09-3]

Carvedilol is used for treating high blood pressure and congestive heart failure. It is related to labetalol (Normodyne, Trandate). Carvedilol blocks receptors of the adrenergic nervous system, the system of nerves in which epinephrine (adrenalin) is active. Nerves from the adrenergic system enter the heart and release an adrenergic chemical (norepinephrine) that attaches to receptors on the heart's muscle and stimulates the muscle to beat more rapidly and forcefully. By blocking the receptors, carvedilol reduces the heart's rate and force of contraction and thereby reduces the work of the heart. Carvedilol also blocks adrenergic receptors on arteries and causes the arteries to relax and the blood pressure to fall. The drop in blood pressure further reduces the work of the heart since it is easier to pump blood against a lower pressure

Carvedilol is a beta blocker and an alpha blocker:Norepinephrine stimulates the nerves that control the muscles of the heart by binding to the β1- and β2-adrenergic receptors. Carvedilol blocks the binding to those receptorswhich both slows the heart rhythm and reduces the force of the heart's pumping. This lowers blood pressure and reduces heart failure.Norepinephrine also binds to the α1-adrenergic receptors on blood vessels, causing them to constrict and raise blood pressure. Carvedilol blocks this binding to the α1-adrenergic receptors toowhich also lowers blood pressure.Relative to other beta blockers, carvedilol has minimal inverse agonist activityThis suggests that carvedilol has a reduced negative chronotropic and inotropic effect compared to other beta blockers, which may decrease its potential to worsen symptoms of heart failure. However, to date this theoretical benefit has not been established in clinical trials, and the current version of the ACC/AHA guidelines on congestive heart failure management does not give preference to carvedilol over other beta-blockers

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