About: Carvedilol     Goto   Sponge   Distinct   Permalink

An Entity of Type : http://linked.opendata.cz/ontology/drugbank/Drug, within Data Space : linked.opendata.cz associated with source document(s)

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http://linked.open...gbank/description
  • Carvedilol is a non-selective beta blocker indicated in the treatment of mild to moderate congestive heart failure (CHF). It blocks beta-1 and beta-2 adrenergic receptors as well as the alpha-1 adrenergic receptors. (en)
http://linked.open...y/drugbank/dosage
http://linked.open...generalReferences
  • # Packer M, Fowler MB, Roecker EB, Coats AJ, Katus HA, Krum H, Mohacsi P, Rouleau JL, Tendera M, Staiger C, Holcslaw TL, Amann-Zalan I, DeMets DL: Effect of carvedilol on the morbidity of patients with severe chronic heart failure: results of the carvedilol prospective randomized cumulative survival (COPERNICUS) study. Circulation. 2002 Oct 22;106(17):2194-9. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/12390947 # Packer M, Coats AJ, Fowler MB, Katus HA, Krum H, Mohacsi P, Rouleau JL, Tendera M, Castaigne A, Roecker EB, Schultz MK, DeMets DL: Effect of carvedilol on survival in severe chronic heart failure. N Engl J Med. 2001 May 31;344(22):1651-8. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/11386263 # Vanderhoff BT, Ruppel HM, Amsterdam PB: Carvedilol: the new role of beta blockers in congestive heart failure. Am Fam Physician. 1998 Nov 1;58(7):1627-34, 1641-2. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/9824960 (en)
http://linked.open...gy/drugbank/group
  • approved (en)
  • investigational (en)
http://linked.open...drugbank/halfLife
  • 7-10 hours (en)
http://linked.open...ugbank/indication
  • For the treatment of mild or moderate (NYHA class II or III) heart failure of ischemic or cardiomyopathic origin. (en)
sameAs
Title
  • Carvedilol (en)
adms:identifier
http://linked.open...mechanismOfAction
  • Carvedilol is a racemic mixture in which nonselective beta-adrenoreceptor blocking activity is present in the S(-) enantiomer and alpha-adrenergic blocking activity is present in both R(+) and S(-) enantiomers at equal potency. Carvedilol's beta-adrenergic receptor blocking ability decreases the heart rate, myocardial contractility, and myocardial oxygen demand. Carvedilol also decreases systemic vascular resistance via its alpha adrenergic receptor blocking properties. Carvedilol and its metabolite BM-910228 (a less potent beta blocker, but more potent antioxidant) have been shown to restore the inotropic responsiveness to Ca<sup>2+</sup> in OH<sup>-</sup> free radical-treated myocardium. Carvedilol and its metabolites also prevent OH<sup>-</sup> radical-induced decrease in sarcoplasmic reticulum Ca<sup>2+</sup>-ATPase activity. Therefore, carvedilol and its metabolites may be beneficial in chronic heart failure by preventing free radical damage. (en)
http://linked.open...drugbank/packager
http://linked.open...y/drugbank/patent
http://linked.open...outeOfElimination
  • Carvedilol is extensively metabolized. Less than 2% of the dose was excreted unchanged in the urine. Carvedilol is metabolized primarily by aromatic ring oxidation and glucuronidation. The oxidative metabolites are further metabolized by conjugation via glucuronidation and sulfation. The metabolites of carvedilol are excreted primarily via the bile into the feces. (en)
http://linked.open.../drugbank/synonym
  • Carvedilol (en)
  • Carvedilolum (en)
  • SKF 105517 (en)
  • (+-)-1-(Carbazol-4-yloxy)-3-((2-(O-methoxyphenoxy)ethyl)amino)-2-propanol (en)
http://linked.open...drugbank/toxicity
  • Not expected to be toxic following ingestion. (en)
http://linked.open...umeOfDistribution
  • * 115 L (en)
http://linked.open.../drug/hasAHFSCode
http://linked.open...k/foodInteraction
  • Take with food, food slows the absorption rate and reduces the incidence of adverse effects (extent of absorption is not affected). (en)
http://linked.open...nk/proteinBinding
  • 98% (en)
http://linked.open...ynthesisReference
  • Ilan Kor, "Crystalline solids of carvedilol and processes for their preparation." U.S. Patent US20030166702, issued September 04, 2003. (en)
http://linked.open...y/mesh/hasConcept
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