Carvedilol detailed information

Carvedilol detailed information
Clinical data
Pregnancy; category	AU: C ; US: C (Risk not ruled out) ; ;
Routes of; administration	oral
ATC code	C07AG02 (WHO) ;
Legal status
Legal status	AU: S4 (Prescription only) ;
Pharmacokinetic data
Bioavailability	25–35%
Protein binding	98%
Metabolism	hepatic (CYP2D6, CYP2C9)
Elimination half-life	7–10 hours
Excretion	renal 16%, faecal 60%
Identifiers
	IUPAC name 1-(9H-carbazol-4-yloxy)-; 3-[2-(2-methoxyphenoxy)ethylamino]propan-2-ol;
CAS Number	72956-09-3;
PubChem CID	2585;
DrugBank	APRD00091;
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value).
Chemical and physical data
Formula	C24H26N2O4
Molar mass	406.474
3D model (JSmol)	Interactive image;
	SMILES COc1ccccc1OCCNCC(O)COc1cccc2[nH]c3ccccc3c12;

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Overview

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]

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. [3]

References

↑ 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

External links

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de:Carvedilol hr:Karvedilol

Template:WikiDoc Sources

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

[1]

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