Carvedilol: molecular and cellular basis for its multifaceted therapeutic potential.
Carvedilol is a unique cardiovascular drug of multifaceted therapeutic potential. Its major molecular targets recognized to date are membrane adrenoceptors (beta 1, beta 2, and alpha 1), reactive oxygen species, and ion channels (K+ and Ca2+). Carvedilol provides prominent hemodynamic benefits mainly through a balanced adrenoceptor blockade, which causes a reduction in cardiac work in association with peripheral vasodilation. This drug assures remarkable cardiovascular protection through its antiproliferative/atherogenic, antiischemic, antihypertrophic, and antiarrhythmic actions. These actions are a consequence of its potent antioxidant effects, amelioration of glucose/lipid metabolism, modulation of neurohumoral factors, and modulation of cardiac electrophysiologic properties. The usefulness of carvedilol in the treatment of hypertension, ischemic heart disease, and congestive heart failure is based on a combination of hemodynamic benefits and cardiovascular protection.
Cheng
J
J
Department of Circulation, Research Institute of Environmental Medicine, Nagoya University, Furo-cho, Chikusa-ku, Nagoya 464-8601, Japan.
Kamiya
K
K
Kodama
I
I
D000317:Adrenergic alpha-Antagonists / Q000494:pharmacology / Q000627:therapeutic use; D000319:Adrenergic beta-Antagonists / Q000494:pharmacology / Q000627:therapeutic use; D000818:Animals; D000959:Antihypertensive Agents / Q000494:pharmacology / Q000627:therapeutic use; D000975:Antioxidants / Q000494:pharmacology / Q000627:therapeutic use; D001786:Blood Glucose / Q000378:metabolism; D002227:Carbazoles / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use*; D002317:Cardiovascular Agents / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use*; D002319:Cardiovascular System / Q000187:drug effects / Q000503:physiopathology; D000077261:Carvedilol; D006329:Heart Conduction System / Q000187:drug effects; D006333:Heart Failure / Q000188:drug therapy; D006801:Humans; D006973:Hypertension / Q000188:drug therapy; D008055:Lipids / Q000097:blood; D017202:Myocardial Ischemia / Q000188:drug therapy; D018377:Neurotransmitter Agents / Q000502:physiology; D011412:Propanolamines / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use*
D000317:Adrenergic alpha-Antagonists; D000319:Adrenergic beta-Antagonists; D000959:Antihypertensive Agents; D000975:Antioxidants; D001786:Blood Glucose; D002227:Carbazoles; D002317:Cardiovascular Agents; D008055:Lipids; D018377:Neurotransmitter Agents; D011412:Propanolamines; D000077261:Carvedilol