China Greatvista Chemicals

Carvedilol

Carvedilol is in a class of drugs called beta-blockers. Beta-blockers affect the heart and circulatory system (arteries and veins). Carvedilol is a nonselective -adrenergic blocking agent with 1-blocking activity. Carvedilol is a potent antihypertenisve agent, and this action has been demonstrated in animals and in the clinical set. The reduction of the blood pressure is a consequence o a fall of the peripheral resistance produced by its alpha -blocking effect. It has the advantage that is not associated with an increase of the heart rate as observed with other vasodilators.

Carvedilol does not interfere with the autoregulation mechanisms of the kidney, including glomerular filtration and the excretion of sodium. By virtue of its ability to block beta-adrenoreceptors, carvedilol inhibits the renin-angiotensin system, blocking the production of angiotensin II. Additionally, through its ability of blocking beta1, beta2, and alfa1 adrenoreceptors, carvedilol inhibits the sympathetic nervous system. It also suppresses the synthesis of endothelin in patients with CHF, a mechanism yet not fully understood. The capacity of carvedilol for blocking alpha and beta receptors explains its benefit in preventing ventricular remodeling.

Carvedilol is a nonselective beta-adrenergic blocking agent with alpha 1 blocking activity. It is indicated for the treatment of mild to moderate (NYHA class II or III) heart failure of ischemic or cardiomyopathic origin. It is prescribed in conjunction with digitalis, diuretics, and ace inhibitors to reduce the progression of disease as evidenced by cardiovascular death and cardiovascular hospitalization. It is also used to reduce the need to adjust other heart failure medications. Carvedilol is also indicated for the management of essential hypertension. It can be used alone or in combination with other antihypertensive agents, especially thiazide type diuretics.

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.

Action/Kinetics: Has both alpha- and beta-adrenergic blocking activity. Decreases cardiac output, reduces exercise- or isoproterenol-induced tachycardia, reduces reflex orthostatic hypotension, causes vasodilation, and reduces peripheral vascular resistance. Significant beta-blocking activity occurs within 60 min while alpha-blocking action is observed within 30 min. BP is lowered more in the standing than in the supine position. Significantly lowers plasma renin activity when given for at least 4 weeks. Rapidly absorbed after PO administration, but there is a significant first-pass effect. Terminal t1/2: 7-10 hr. Food delays the rate of absorption. Over 98% is bound to plasma protein. Plasma levels average 50% higher in geriatric compared with younger clients. Extensively metabolized in the liver, with metabolites excreted primarily via the bile into the feces.

CAS No.: 72956-09-3
Molecular formula: C24H26N2O4
Molecular weight: 406.480