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QuickView for Carvedilol (compound)


PubChem
Name: carvedilol
PubChem Compound ID: 185394
Molecular formula: C24H26N2O4
Molecular weight: 406.474 g/mol
Synonyms:
95093-99-5
DrugBank
Identification
Name: carvedilol
Name (isomeric): DB01136
Drug Type: small molecule
Synonyms:
Carvedilolum [Latin]
Brand: Coreg CR, Coreg
Category: Vasodilator Agents, Adrenergic Agents, Adrenergic beta-Antagonists, Adrenergic alpha-Antagonists, Antihypertensive Agents
CAS number: 72956-09-3
Pharmacology
Indication: For the treatment of mild or moderate (NYHA class II or III) heart failure of ischemic or cardiomyopathic origin.
Pharmacology:
Carvedilol is a nonselective beta-adrenergic blocking agent with alpha1-blocking activity and is indicated for the treatment of hypertension and mild or moderate (NYHA class II or III) heart failure of ischemic or cardiomyopathic origin. Carvedilol is a racemic mixture in which nonselective b-adrenoreceptor blocking activity is present in the S(-) ...
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Mechanism of Action:
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 ...
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Absorption: Carvedilol is rapidly and extensively absorbed following oral administration, with an absolute bioavailability of approximately 25% to 35% due to a significant degree of first-pass metabolism.
Protein binding: 98%
Biotransformation: Hepatic. Carvedilol is metabolized primarily by aromatic ring oxidation and glucuronidation. The oxidative metabolites are further metabolized by conjugation via glucuronidation and sulfation. Demethylation and hydroxylation at the phenol ring produce three active metabolites with b-receptor blocking activity. The 4'-hydroxyphenyl metabolite is approximately 13 times more potent than carvedilol for b-blockade.
Route of elimination: 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.
Half Life: 7-10 hours
Clearance: 500-700 mL/min
Toxicity: Not expected to be toxic following ingestion.
Affected organisms: Humans and other mammals
Interactions
Food interaction:
Take with food, food slows the absorption rate and reduces the incidence of adverse effects (extent of absorption is not affected).
Drug interaction:
IbuprofenRisk of inhibition of renal prostaglandins
GlisoxepideThe beta-blocker, carvedilol, may decrease symptoms of hypoglycemia.
ProcaterolAntagonism
CitalopramThe SSRI, citalopram, may increase the bradycardic effect of the beta-blocker, carvedilol.
SalmeterolAntagonism
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