Document Detail

Carvedilol, a novel multiple action antihypertensive agent with antioxidant activity and the potential for myocardial and vascular protection.
MedLine Citation:
PMID:  8521883     Owner:  NLM     Status:  MEDLINE    
Carvedilol is a vasodilating, beta-adrenoceptor antagonist currently marketed for the treatment of mild to moderate hypertension. Carvedilol acts to reduce total peripheral resistance by blocking peripheral vascular alpha 1-adrenoceptors, thereby producing systemic arterial vasodilation, while at the same time inhibiting reflex tachycardia through the blockade of myocardial beta-adrenoceptors. In addition to its established efficacy and safety as an antihypertensive agent, carvedilol has been shown to produce significant cardioprotection in experimental animal models of acute myocardial infarction, with the most dramatic effect being observed in the pig model of myocardial ischaemia and reperfusion, where the reduction in infarct size reached 91%. Recent pharmacological studies have revealed additional novel properties of carvedilol which may account for the marked protection produced by the drug in the ischaemic myocardium and which may also result in protection against other chronic pathological processes, such as atherosclerosis and acute vascular injuries. The latter arise from surgical procedures, such as percutaneous transluminal coronary angioplasty and coronary artery bypass grafting. Specifically, carvedilol, as well as some of its hydroxylated metabolites, are potent antioxidants. In physicochemical, biochemical and cellular assays, carvedilol and several of its metabolites prevent lipid peroxidation and the depletion of endogenous antioxidants, such as vitamin E and glutathione. Moreover, carvedilol and its metabolites prevent the oxidation of LDL to oxidized LDL, the latter being directly cytotoxic and known to activate monocytes/macrophages and to stimulate foam cell formation. In addition, carvedilol was found to inhibit both rat and human vascular smooth muscle cell proliferation and migration.(ABSTRACT TRUNCATED AT 250 WORDS)
G Z Feuerstein; R R Ruffolo
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Publication Detail:
Type:  Journal Article; Review    
Journal Detail:
Title:  European heart journal     Volume:  16 Suppl F     ISSN:  0195-668X     ISO Abbreviation:  Eur. Heart J.     Publication Date:  1995 Jul 
Date Detail:
Created Date:  1996-01-24     Completed Date:  1996-01-24     Revised Date:  2013-05-28    
Medline Journal Info:
Nlm Unique ID:  8006263     Medline TA:  Eur Heart J     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  38-42     Citation Subset:  IM    
Division of Pharmacological Sciences, SmithKline Beecham Pharmaceuticals, King of Prussia, PA 19406, USA.
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MeSH Terms
Adrenergic alpha-Antagonists / adverse effects,  therapeutic use
Antihypertensive Agents / adverse effects,  therapeutic use*
Antioxidants / adverse effects,  therapeutic use*
Arteriosclerosis / drug therapy*,  physiopathology
Carbazoles / adverse effects,  therapeutic use*
Cell Division / drug effects,  physiology
Hemodynamics / drug effects,  physiology
Hypertension / drug therapy*,  physiopathology
Hypertrophy, Left Ventricular / drug therapy,  physiopathology
Lipid Peroxidation / drug effects*,  physiology
Muscle, Smooth, Vascular / drug effects,  physiology
Myocardial Infarction / drug therapy,  physiopathology
Propanolamines / adverse effects,  therapeutic use*
Reg. No./Substance:
0/Adrenergic alpha-Antagonists; 0/Antihypertensive Agents; 0/Antioxidants; 0/Carbazoles; 0/Propanolamines; 0K47UL67F2/carvedilol

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