Coreg
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Coreg
CarvedilolSystematic (IUPAC) nameamineIdentifiersCAS number72956-09-3ATC codeC07AG02PubChem2585DrugBankAPRD00091ChemSpider2487Chemical dataFormulaC24H26N2O4 Mol. mass406.474SMILESeMolecules & PubChemPharmacokinetic dataBioavailability25–35%Protein binding98%Metabolismhepatic (CYP2D6, CYP2C9)Half life7–10 hoursExcretionrenal 16%, faecal 60%Therapeutic considerationsPregnancy cat.C(AU) C(US)Legal statusPrescription Only (S4)(AU) POM(UK) ℞-only(US)RoutesoralCarvedilol is a non-selective beta blocker/alpha-1 blocker indicated in the treatment of mild to moderate congestive heart failure (CHF). It is marketed under various trade names including Coreg (GSK), Dilatrend (Roche), Eucardic (Roche), and Carloc (Cipla) as a generic drug (as of September 5, 2007 in the U.S.)., and as a controlled-release formulation, marketed in the US as Coreg CR (GSK).// PharmacologyCarvedilol is a beta blocker and an alpha blocker:Norepinephrine stimulates the nerves that control the muscles of the heart by binding to the β1- and β2-adrenergic receptors. Carvedilol blocks the binding to those receptors, which both slows the heart rhythm and reduces the force of the heart's pumping. This lowers blood pressure and reduces heart failure.Norepinephrine also binds to the α1-adrenergic receptors on blood vessels, causing them to constrict and raise blood pressure. Carvedilol blocks this binding to the α1-adrenergic receptors too, which also lowers blood pressure.Relative to other beta blockers, carvedilol has minimal inverse agonist activity. This suggests that carvedilol has a reduced negative chronotropic and inotropic effect compared to other beta blockers, which may decrease its potential to worsen symptoms of heart failure. However, to date this theoretical benefit has not been established in clinical trials, and the current version of the ACC/AHA guidelines on congestive heart failure management does not give preference to carvedilol over other beta-blockers. Side effectsSide effects of carvedilol may be dose related and can include, sleep disturbance, nightmares and anxiety and panic attacks. EnantiomersCarvedilol has enantiomers with distinct pharmacodynamics.The term "racemic carvedilol" is sometimes used to explicitly denote that both enantiomers are applied. Clinical useCarvedilol is indicated in the management of congestive heart failure (CHF), as an adjunct to conventional treatments (ACE inhibitors and diuretics). The use of carvedilol has been shown to provide additional morbidity and mortality benefits in CHF. Carvedilol (Coreg) is available at the following doses 6.25mg (smallest), followed by 12.5mg, and 25mg white tablets. U.S. supply issuesOn January 10, 2006 carvedilol supply became limited in the United States, due to changes in documentation procedures at a plant. This was lifted in April 27, 2006 in a Dear Pharmacist letter. Approval of controlled-release formulationOn October 20, 2006, the FDA approved a controlled release formulation of carvedilol, to be marketed as Coreg CR.
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