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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. mass 406.474
Pharmacokinetic data
Bioavailability 25–35%
Protein binding 98%
Metabolism hepatic (CYP2D6, CYP2C9)
Half life 7–10 hours
Excretion renal 16%, faecal 60%
Therapeutic considerations
Pregnancy cat.

C(AU) C(US)

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), and (as of September 5, 2007 in the U.S.) as a generic drug.[1]

Additional recommended knowledge

Contents

Pharmacology

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 (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. 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.

Clinical use

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 changes in documentation procedures at a plant. This was lifted in April 27 2006 in a Dear Pharmacist letter. [1]

References

  1. ^ Press Release, FDA Approves First Generic Versions of Coreg, U.S. Food and Drug Administration, Sep. 5, 2007

General 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]
 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Carvedilol". A list of authors is available in Wikipedia.
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