Carvedilol

Carvedilol

File:Carvedilol.svg
File:Carvedilol-I-3D-balls.png
Systematic (IUPAC) name
(±)-[3-(9H-carbazol-4-yloxy)-2-hydroxypropyl][2-(2-methoxyphenoxy)ethyl]amine
Clinical data
Pregnancy category	C
Routes of administration	Oral
Legal status
Legal status	℞ (Prescription only)
Pharmacokinetic data
Bioavailability	25–35%
Protein binding	98%
Metabolism	Liver (CYP2D6, CYP2C9)
Biological half-life	7–10 hours
Excretion	Urine (16%), Feces (60%)
Identifiers
CAS Number	72956-09-3
ATC code	C07AG02 (WHO)
PubChem	CID 2585
IUPHAR/BPS	551
DrugBank	APRD00091
ChemSpider	2487
Chemical data
Formula	C24H26N2O4
Molar mass	406.474[[]]
(verify)

Carvedilol 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).

Pharmacology

Carvedilol is both a beta blocker (β₁, β₂) and alpha blocker (α₁):

• 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 effects

The most common side effects include dizziness, fatigue, hypotension, diarrhea, asthenia, bradycardia, and weight gain.

A case report of a patient with panic disorder associated sleep disturbances and nightmares with the improper usage of carvedilol.

Enantiomers

Carvedilol has enantiomers with distinct pharmacodynamics.

The term "racemic carvedilol" is sometimes used to explicitly denote that both enantiomers are applied.

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. Carvedilol (Coreg) is available at the following doses 3.125 mg (smallest), followed by 6.25 mg, 12.5 mg, and 25 mg white tablets.

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.

Approval of controlled-release formulation

On October 20, 2006, the FDA approved a controlled release formulation of carvedilol; it is marketed as Coreg CR.

References

11. Subhashis Chakraborty , Dali Shukla, Brahmeshwar Mishra & Sanjay Singh.Clinical updates on carvedilol: a first choice beta-blocker in the treatment of cardiovascular diseases. Expert Opin Drug Metab Toxicol. 2010 Feb;6(2):237-50. DOI 10.1517/17425250903540220, PMID: 20073998

External links

• Coreg CR official website
• Physicians Desk Reference Info on Carvedilol
• Info on carvedilol through rxlist.com

de:Carvedilol ru:Карведилол