Carvedilol, sold under the brand nameCoreg among others, is abeta blockermedication, that may be prescribed for the treatment ofhigh blood pressure (hypertension) and chronicheart failure with reduced ejection fraction (also known as HFrEF or systolic heart failure).[1][2] Beta-blockers as a collective medication class are not recommended as routine first-line treatment of high blood pressure for all patients, due to evidence demonstrating less effective cardiovascular protection and a less favourable safety profile when compared to other classes of blood pressure-lowering medications.[1][3][4]
Carvedilol was patented in 1978 and approved for medical use in the United States in 1995.[5][8] Carvedilol is a therapeutic alternative on theWorld Health Organization's List of Essential Medicines.[9] It is available as ageneric medication.[5] In 2023, it was the 35th most commonly prescribed medication in the United States, with more than 16million prescriptions.[10][11]
Carvedilol is indicated in the management ofcongestive heart failure (CHF), commonly as an adjunct to angiotensin-converting-enzyme inhibitor (ACE inhibitors) anddiuretics. It has been clinically shown to reduce mortality and hospitalizations in people with CHF.[12] The mechanism of carvedilol in heart failure is due to its inhibition of receptors in the adrenergic nervous system, which releasesnoradrenaline to the body, including the heart.[13] Noradrenaline is a hormone that causes the heart to beat faster and work harder.[13] Blocking its binding to adrenergic receptors in the heart causes vasodilation, decreases heart rate and blood pressure, and improves myocardial contractility,[14] which ultimately decreases the heart's workload.[13]
Carvedilol reduces the risk of death, hospitalisations, and recurring heart attacks in patients with moderate to severe heart failure (with an ejection fraction <40%) following a heart attack[15][16][17] Carvedilol has also been proven to reduce death and hospitalization in patients with severe heart failure.[18]
Carvedilol is not considered a first-line treatment for hypertension; however, research has demonstrated that it exhibits an antihypertensive effect when compared to a placebo or other antihypertensive medications.[19][20]
Carvedilol has shown efficacy in preventing bleeding from oesophageal varices in patients with mild to moderate cirrhosis and may have benefit in avoiding successive bleeds.[21][22]
Carvedilol is used in the treatment of acute cardiovasculartoxicity (e.g.overdose) withsympathomimetics, for instance caused byamphetamine,methamphetamine,cocaine, orephedrine.[23][24] It has also specifically been found to block the sympathomimetic effects ofMDMA.[25][23][26] Dual α1 and beta blockers like carvedilol andlabetalol may be more favorable for such purposes due to the possibility of "unopposed α-stimulation" with selective beta blockers.[23]
Carvedilol is not recommended for people with uncontrolled bronchospastic disease (e.g. current asthma symptoms) as it can block receptors that assist in opening the airways.[27]
The meanelimination half-life of carvedilol following oral administration ranges from 7 to 10hours. The pharmaceutical product is a mix of twoenantiomorphs,R(+)-carvedilol andS(–)-carvedilol, with differing metabolic properties. R(+)-Carvedilol undergoes preferential selection for metabolism, which results in a fractional half-life of about 5 to 9 hours, compared with 7 to 11 hours for the S(-)-carvedilol fraction.[27]
Carvedilol is a highlylipophiliccompound with an experimentallog P of 3.8 to 4.19 and a predicted log P of 3.05 to 4.2.[43][44][45][46][47] It showed the third highest predicted lipophilicity of 30clinically relevant beta blockers, with the second and third most lipophilic beta blockers predicted to bebopindolol andpenbutolol, respectively.[48]
^abMancia G, Kreutz R, Brunström M, Burnier M, Grassi G, Januszewicz A, et al. (December 2023). "2023 ESH Guidelines for the management of arterial hypertension The Task Force for the management of arterial hypertension of the European Society of Hypertension: Endorsed by the International Society of Hypertension (ISH) and the European Renal Association (ERA)".Journal of Hypertension.41 (12):1874–2071.doi:10.1097/HJH.0000000000003480.hdl:11379/603005.PMID37345492.
^McDonagh TA, Metra M, Adamo M, Gardner RS, Baumbach A, Böhm M, et al. (September 2021). "2021 ESC Guidelines for the diagnosis and treatment of acute and chronic heart failure".European Heart Journal.42 (36):3599–3726.doi:10.1093/eurheartj/ehab368.PMID34447992.
^Bangalore S, Parkar S, Grossman E, Messerli FH (October 2007). "A meta-analysis of 94,492 patients with hypertension treated with beta blockers to determine the risk of new-onset diabetes mellitus".The American Journal of Cardiology.100 (8):1254–1262.doi:10.1016/j.amjcard.2007.05.057.PMID17920367.
^World Health Organization (2025).The selection and use of essential medicines, 2025: WHO Model List of Essential Medicines, 24th list. Geneva: World Health Organization.hdl:10665/382243.
^Kubon C, Mistry NB, Grundvold I, Halvorsen S, Kjeldsen SE, Westheim AS (April 2011). "The role of beta-blockers in the treatment of chronic heart failure".Trends in Pharmacological Sciences.32 (4):206–212.doi:10.1016/j.tips.2011.01.006.PMID21376403.
^Dargie HJ (May 2001). "Effect of carvedilol on outcome after myocardial infarction in patients with left-ventricular dysfunction: the CAPRICORN randomised trial".Lancet.357 (9266):1385–1390.doi:10.1016/s0140-6736(00)04560-8.PMID11356434.S2CID1840228.
^Huang BT, Huang FY, Zuo ZL, Liao YB, Heng Y, Wang PJ, et al. (June 2015). "Meta-Analysis of Relation Between Oral β-Blocker Therapy and Outcomes in Patients With Acute Myocardial Infarction Who Underwent Percutaneous Coronary Intervention".The American Journal of Cardiology.115 (11):1529–1538.doi:10.1016/j.amjcard.2015.02.057.PMID25862157.
^Packer M, Fowler MB, Roecker EB, Coats AJ, Katus HA, Krum H, et al. (October 2002). "Effect of carvedilol on the morbidity of patients with severe chronic heart failure: results of the carvedilol prospective randomized cumulative survival (COPERNICUS) study".Circulation.106 (17):2194–9.doi:10.1161/01.cir.0000035653.72855.bf.PMID12390947.
^Weber MA, Sica DA, Tarka EA, Iyengar M, Fleck R, Bakris GL (October 2006). "Controlled-release carvedilol in the treatment of essential hypertension".The American Journal of Cardiology.98 (7A):32L –38L.doi:10.1016/j.amjcard.2006.07.017.PMID17023230.
^Saul SM, Duprez DA, Zhong W, Grandits GA, Cohn JN (June 2013). "Effect of carvedilol, lisinopril and their combination on vascular and cardiac health in patients with borderline blood pressure: the DETECT Study".Journal of Human Hypertension.27 (6):362–367.doi:10.1038/jhh.2012.54.PMID23190794.
^abcRichards JR, Albertson TE, Derlet RW, Lange RA, Olson KR, Horowitz BZ (May 2015). "Treatment of toxicity from amphetamines, related derivatives, and analogues: a systematic clinical review".Drug Alcohol Depend.150:1–13.doi:10.1016/j.drugalcdep.2015.01.040.PMID25724076.
^Richards JR, Hollander JE, Ramoska EA, Fareed FN, Sand IC, Izquierdo Gómez MM, et al. (May 2017). "β-Blockers, Cocaine, and the Unopposed α-Stimulation Phenomenon".J Cardiovasc Pharmacol Ther.22 (3):239–249.doi:10.1177/1074248416681644.PMID28399647.
^Fonseca DA, Ribeiro DM, Tapadas M, Cotrim MD (July 2021). "Ecstasy (3,4-methylenedioxymethamphetamine): Cardiovascular effects and mechanisms".Eur J Pharmacol.903 174156.doi:10.1016/j.ejphar.2021.174156.PMID33971177.
^Kotlyar E, Keogh AM, Macdonald PS, Arnold RH, McCaffrey DJ, Glanville AR (December 2002). "Tolerability of carvedilol in patients with heart failure and concomitant chronic obstructive pulmonary disease or asthma".The Journal of Heart and Lung Transplantation.21 (12):1290–5.doi:10.1016/s1053-2498(02)00459-x.PMID12490274.
^Lo GH, Chen WC, Wang HM, Yu HC (November 2012). "Randomized, controlled trial of carvedilol versus nadolol plus isosorbide mononitrate for the prevention of variceal rebleeding".Journal of Gastroenterology and Hepatology.27 (11):1681–7.doi:10.1111/j.1440-1746.2012.07244.x.PMID22849337.S2CID23494154.
^abKoshman SL, Paterson I (15 March 2023)."Heart Failure".Canadian Pharmacists Association (CPS). Retrieved29 April 2024.
^Xu XL, Zang WJ, Lu J, Kang XQ, Li M, Yu XJ (December 2006). "Effects of carvedilol on M2 receptors and cholinesterase-positive nerves in adriamycin-induced rat failing heart".Autonomic Neuroscience.130 (1–2):6–16.doi:10.1016/j.autneu.2006.04.005.PMID16798104.S2CID22480332.
^Ruffolo RR, Gellai M, Hieble JP, Willette RN, Nichols AJ (1990). "The pharmacology of carvedilol".European Journal of Clinical Pharmacology.38 (Suppl 2):S82 –S88.doi:10.1007/BF01409471.PMID1974511.S2CID2901620.
^Mannhold R (February 2005). "The impact of lipophilicity in drug research: a case report on beta-blockers".Mini Rev Med Chem.5 (2):197–205.doi:10.2174/1389557053402701.PMID15720289.
Chakraborty S, Shukla D, Mishra B, Singh S (February 2010). "Clinical updates on carvedilol: a first choice beta-blocker in the treatment of cardiovascular diseases".Expert Opinion on Drug Metabolism & Toxicology.6 (2):237–50.doi:10.1517/17425250903540220.PMID20073998.S2CID25670550.
