Carvedilol

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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[[Script error: No such module "String".]]
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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.).[1], 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,[2] 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,[3] which also lowers blood pressure.

Relative to other beta blockers, carvedilol has minimal inverse agonist activity.[4] 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.[5]

A case report of a patient with panic disorder associated sleep disturbances and nightmares with the improper usage of carvedilol.[6]

Enantiomers

Carvedilol has enantiomers with distinct pharmacodynamics.[7]

The term "racemic carvedilol" is sometimes used to explicitly denote that both enantiomers are applied.[8]

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.[9] 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.[10]

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

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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


Sympatholytic (and closely related) antihypertensives (C02)
Sympatholytics
(antagonize α-adrenergic
vasoconstriction)
Central
Adrenergic release inhibitors
Peripheral
Indirect
Direct
Non-selective α blocker
Other antagonists
dual (Bosentan) • selective (Ambrisentan, Sitaxentan)
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ru:Карведилол
  1. ↑ Press Release, FDA Approves First Generic Versions of Coreg, U.S. Food and Drug Administration, Sep. 5, 2007
  2. ↑ Stafylas PC, Sarafidis PA (2008). "Carvedilol in hypertension treatment". Vasc Health Risk Manag. 4 (1): 23–30. doi:10.2147/vhrm.2008.04.01.23. PMC 2464772 Freely accessible. PMID 18629377. 
  3. ↑ Othman AA, Tenero DM, Boyle DA, Eddington ND, Fossler MJ (2007). "Population pharmacokinetics of S(-)-carvedilol in healthy volunteers after administration of the immediate-release (IR) and the new controlled-release (CR) dosage forms of the racemate". AAPS J. 9 (2): E208–18. doi:10.1208/aapsj0902023. PMC 2751410 Freely accessible. PMID 17614362. 
  4. ↑ 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
  5. ↑ Carvedilol Official FDA information, side effects and uses. Drugs.com, October 11, 2009.
  6. ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
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  10. ↑ http://www.fda.gov/cder/drug/shortages/Coreg_Pharmacist_Letter_27Apr06.pdf PDF at FDA.govdead link
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