Carvedilol

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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. mass	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	Prescription Only (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).

1 Pharmacology
2 Clinical use
- 2.1 U.S. supply issues
3 References
4 External links

[edit] Pharmacology

In addition to blocking both β₁- and β₂-adrenergic receptors, carvedilol also displays α₁-adrenergic antagonism, 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.

[edit] 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).

[edit] U.S. supply issues

On 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. [1]

[edit] References

Packer M, Fowler MB, Roecker EB, et al. 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;106(17):2194-9. PMID 12390947

Packer M, Coats AJ, Fowler MB, et al. Effect of carvedilol on survival in severe chronic heart failure. N Engl J Med. 2001 May 31;344(22):1651-8. PMID 11386263. Carvedilol improves survival in severe heart failure, as well as in mild-to-moderate heart failure.

Vanderhoff BT, Ruppel HM, Amsterdam PB. Carvedilol: The new role of beta blockers in congestive heart failure. Am Fam Physician 1998;58(7):1627-34. PMID 9824960

[edit] External links

v • d • e Beta blockers (C07)
Non-selective β antagonists (C07AA)	Metipranolol, Nadolol, Oxprenolol, Penbutolol, Pindolol, Propranolol, Timolol, Sotalol
β₁ antagonists (cardioselective) (C07AB)	Atenolol, Acebutolol, Betaxolol, Bisoprolol, Esmolol, Metoprolol, Nebivolol
Mixed α₁/β antagonists (C07AG)	Carvedilol, Labetalol