1.beta blocker that can reduce the progression of heart failure in individuals whose disease is not advanced
beta-adrenergic blocker, beta adrenergic blocking agent, beta-adrenergic blocking agent, beta adrenergic receptor blocking agent, beta-adrenergic receptor blocking agent, beta blocker, beta-blocker, beta blocking agent, beta-blocking agent, beta-receptor blocking agent[Hyper.]
|Systematic (IUPAC) name|
|Legal status||℞ Prescription only|
|Metabolism||Liver (CYP2D6, CYP2C9)|
|Excretion||Urine (16%), Feces (60%)|
| (what is this?)
Carvedilol is a nonselective beta blocker/alpha-1 blocker indicated in the treatment of mild to severe congestive heart failure (CHF). It is marketed under various trade names including Carvil (Zydus Cadila), Coreg (GSK), Dilatrend (Roche), Coronis (Bilim), 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). Carvedilol was discovered by Robert R. Ruffolo, Jr. It has had a significant role in the treatment of congestive heart failure.
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.
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 severe CHF. Carvedilol (Carvil) is available at the following doses 3.125 mg (smallest), followed by 6.25 mg,12.5 mg, and 25 mg white tablets.
On January 10, 2006 carvedilol supply became limited in the United States, due to changes in documentation procedures at a plant. This was lifted on April 27, 2006 in a Dear Pharmacist letter.
On October 20, 2006, the FDA approved a controlled release formulation of carvedilol; it is marketed as Coreg CR.
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
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