Article: Carvedilol

Carvedilol
Systematic (IUPAC) name
1-(9H-carbazol-4-yloxy)- 3-[2-(2-methoxyphenoxy)ethylamino]propan-2-ol
Identifiers
CAS number	72956-09-3
ATC code	C07AG02
PubChem	2585
DrugBank	APRD00091
Chemical data
Formula	C24H26N2O4
Mol. weight	406.474
Pharmacokinetic data
Bioavailability	25–35%
Metabolism	hepatic (CYP2D6, CYP2C9)
Half life	6–10 hours
Excretion	renal 16%, faecal 60%
Therapeutic considerations
Pregnancy cat.	C(AU)
Legal status	S4(AU)
Routes	oral

Carvedilol is a non-selective beta 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) and Eucardic (Roche).

Pharmacology

In addition to blocking both β₁- and β₂-adrenergic receptors, carvedilol also displays α₁-adrenergic antagonism as well, which confers the added benefit of reducing blood pressure through vasodilation.

Relative to other beta blockers, carvedilol has minimal inverse agonist activity (Vanderhoff et al., 1998). 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.

Clinical use

Main article: Beta blocker

Carvedilol 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 (Packer et al., 2002).

U.S. supply issues

On January 10, 2006 carvedilol supply became limited in the United States, due to manufacturing issues, with an unknown date for re-establishment of normal supply.