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Chemical Compound Review

AC1O535C     1-(9H-carbazol-3-yloxy)-3-[2- (2...

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Disease relevance of carvedilol


Psychiatry related information on carvedilol


High impact information on carvedilol

  • METHODS: In the U.S. Carvedilol Heart Failure Trials Program, 217 black and 877 nonblack patients (in New York Heart Association class II, III, or IV and with a left ventricular ejection fraction of no more than 0.35) were randomly assigned to receive placebo or carvedilol (at doses of 6.25 to 50 mg twice daily) for up to 15 months [10].
  • In addition, as compared with placebo, carvedilol therapy was accompanied by a 27 percent reduction in the risk of hospitalization for cardiovascular causes (19.6 percent vs. 14.1 percent, P = 0.036), as well as a 38 percent reduction in the combined risk of hospitalization or death (24.6 percent vs, 15.8 percent, P < 0.001) [11].
  • In addition, hemodynamic responses to beta-receptor blockade were greater in Arg389 mice, and homozygosity for Arg389 was associated with improvement in ventricular function during carvedilol treatment in heart failure patients [12].
  • DATA SYNTHESIS: Of the 4 beta-blockers tested in large randomized controlled clinical trials of patients with heart failure, 3 are available in the United States, bisoprolol, carvedilol, and metoprolol; 2 of these, carvedilol and metoprolol, have Food and Drug Administration indications for the treatment of heart failure [13].
  • These specific effects of carvedilol on the Arg389 variant of the beta(1)-AR were also seen for control of beating frequency in rat cardiac myocytes expressing the 2 receptor variants [14].

Chemical compound and disease context of carvedilol


Biological context of carvedilol


Anatomical context of carvedilol


Associations of carvedilol with other chemical compounds

  • Compared with metoprolol, carvedilol was associated with greater improvement in New York Heart Association functional class [23].
  • The peak oxygen consumption of trained patients treated with either carvedilol or propranolol increased from 12.9 +/- 1.4 to 16.0 +/- 1.6 (P < .001) and 12.4 +/- 1.0 to 15.7 +/- 0.9 (P < .001), respectively, whereas it did not change in the sedentary patients [24].
  • METHODS: Plasma N-BNP and adrenomedullin were measured in 297 patients with chronic ischemic (LV) dysfunction before randomization to carvedilol or placebo, added to established treatment with a converting enzyme inhibitor and loop diuretic (with or without digoxin) [25].
  • CONCLUSIONS: Carvedilol added to angiotensin-converting enzyme inhibition reduces hospitalization risk as well as severity of illness and resource utilization during admission in patients with chronic heart failure [26].
  • Plethysmography and blood sampling were obtained serially at baseline (day 0), 3 days after carvedilol, arotinolol or placebo administration (day 3) and 3 days after application of a 20 mg/24 h NTG tape concomitantly with carvedilol, arotinolol or placebo (day 6) [27].

Gene context of carvedilol

  • The AUC and fecal excretion of intravenous carvedilol were correlated with the intestinal expression of MDR1 messenger ribonucleic acid (mRNA) (r = -0.67, P =.001; r = 0.83, P =.002) and MRP2 mRNA (r = -0.74, P <.001; r = 0.70, P =.025) [28].
  • Rifampin decreased the AUC of carvedilol to an extent independent of the CYP2D6 genotype (poor metabolizers, 341 +/- 147 ng. h/mL versus 126 +/- 41.7 ng. h/mL; extensive metabolizers, 173 +/- 102 ng. h/mL versus 74 +/- 41.4 ng. h/mL; both P <.05) [28].
  • The enzyme kinetics for carvedilol glucuronidation by UGT1A1, UGT2B4, and UGT2B7 in addition to human liver microsomes were examined by Lineweaver-Burk analysis [29].
  • Involvement of human hepatic UGT1A1, UGT2B4, and UGT2B7 in the glucuronidation of carvedilol [29].
  • A combination of multivariate correlation analysis, the use of selective inhibitors of P450, and microsomes from human lymphoblastoid cells expressing various human P450s enabled phenotyping of the enzymes involved in the oxidative metabolism of carvedilol [30].

Analytical, diagnostic and therapeutic context of carvedilol

  • RESULTS: As compared with placebo, carvedilol lowered the risk of death from any cause or hospitalization for any reason by 48 percent in black patients and by 30 percent in nonblack patients [10].
  • BACKGROUND: Carvedilol has improved the symptomatic status of patients with moderate to severe heart failure in single-center studies, but its clinical effects have not been evaluated in large, multicenter trials [31].
  • Quantitative image analysis demonstrated that carvedilol reduced the neointimal growth following angioplasty by 84% without altering either medial or adventitial cross-sectional areas [21].
  • In clinical trials, the third-generation, nonselective beta-blocker carvedilol was the first among several beta-blockers to reduce mortality in heart failure [32].
  • We conclude that carvedilol is a useful adjunctive therapy for patients with NYHA class IV heart failure; however, they require close observation during initiation and titration of the drug [33].


  1. Effect of carvedilol on outcome after myocardial infarction in patients with left-ventricular dysfunction: the CAPRICORN randomised trial. Dargie, H.J. Lancet (2001) [Pubmed]
  2. Metabolic and cardiovascular effects of carvedilol and atenolol in non-insulin-dependent diabetes mellitus and hypertension. A randomized, controlled trial. Giugliano, D., Acampora, R., Marfella, R., De Rosa, N., Ziccardi, P., Ragone, R., De Angelis, L., D'Onofrio, F. Ann. Intern. Med. (1997) [Pubmed]
  3. Double-blind, placebo-controlled study of the long-term efficacy of carvedilol in patients with severe chronic heart failure. Krum, H., Sackner-Bernstein, J.D., Goldsmith, R.L., Kukin, M.L., Schwartz, B., Penn, J., Medina, N., Yushak, M., Horn, E., Katz, S.D. Circulation (1995) [Pubmed]
  4. Possible involvement of stress-activated protein kinase signaling pathway and Fas receptor expression in prevention of ischemia/reperfusion-induced cardiomyocyte apoptosis by carvedilol. Yue, T.L., Ma, X.L., Wang, X., Romanic, A.M., Liu, G.L., Louden, C., Gu, J.L., Kumar, S., Poste, G., Ruffolo, R.R., Feuerstein, G.Z. Circ. Res. (1998) [Pubmed]
  5. Influence of pretreatment systolic blood pressure on the effect of carvedilol in patients with severe chronic heart failure: the Carvedilol Prospective Randomized Cumulative Survival (COPERNICUS) study. Rouleau, J.L., Roecker, E.B., Tendera, M., Mohacsi, P., Krum, H., Katus, H.A., Fowler, M.B., Coats, A.J., Castaigne, A., Scherhag, A., Holcslaw, T.L., Packer, M. J. Am. Coll. Cardiol. (2004) [Pubmed]
  6. Nightmares and panic disorder associated with carvedilol overdose. Maebara, C., Ohtani, H., Sugahara, H., Mine, K., Kubo, C., Sawada, Y. The Annals of pharmacotherapy. (2002) [Pubmed]
  7. Adrenergic blocker carvedilol attenuates the cardiovascular and aversive effects of nicotine in abstinent smokers. Sofuoglu, M., Mouratidis, M., Yoo, S., Kosten, T. Behavioural pharmacology (2006) [Pubmed]
  8. General pharmacological profiles of the new beta-adrenoceptor antagonist carvedilol. Hirohashi, M., Takasuna, K., Tamura, K., Yamaguchi, K., Maekawa, K., Yamada, S., Iwasaki, S., Yoshida, M., Nomura, M., Taguchi, K. Arzneimittel-Forschung. (1990) [Pubmed]
  9. Pre-discharge initiation of beta-blocker therapy in elderly patients hospitalized for acute decompensation of chronic heart failure: an effective strategy for the implementation of beta-blockade in heart failure. Tarantini, L., Cioffi, G., Opasich, C., Di Lenarda, A., Pulignano, G., Del Sindaco, D., De Feo, S., Stefenelli, C., Russo, P., Catania, G. Italian heart journal : official journal of the Italian Federation of Cardiology. (2004) [Pubmed]
  10. Race and the response to adrenergic blockade with carvedilol in patients with chronic heart failure. Yancy, C.W., Fowler, M.B., Colucci, W.S., Gilbert, E.M., Bristow, M.R., Cohn, J.N., Lukas, M.A., Young, S.T., Packer, M. N. Engl. J. Med. (2001) [Pubmed]
  11. The effect of carvedilol on morbidity and mortality in patients with chronic heart failure. U.S. Carvedilol Heart Failure Study Group. Packer, M., Bristow, M.R., Cohn, J.N., Colucci, W.S., Fowler, M.B., Gilbert, E.M., Shusterman, N.H. N. Engl. J. Med. (1996) [Pubmed]
  12. Beta 1-adrenergic receptor polymorphisms confer differential function and predisposition to heart failure. Mialet Perez, J., Rathz, D.A., Petrashevskaya, N.N., Hahn, H.S., Wagoner, L.E., Schwartz, A., Dorn, G.W., Liggett, S.B. Nat. Med. (2003) [Pubmed]
  13. beta-Blocker therapy in heart failure: scientific review. Foody, J.M., Farrell, M.H., Krumholz, H.M. JAMA (2002) [Pubmed]
  14. Real-time optical recording of beta(1)-adrenergic receptor activation reveals supersensitivity of the Arg389 variant to carvedilol. Rochais, F., Vilardaga, J.P., Nikolaev, V.O., B??nemann, M., Lohse, M.J., Engelhardt, S. J. Clin. Invest. (2007) [Pubmed]
  15. Randomized comparison of long-term carvedilol and propranolol administration in the treatment of portal hypertension in cirrhosis. Bañares, R., Moitinho, E., Matilla, A., García-Pagán, J.C., Lampreave, J.L., Piera, C., Abraldes, J.G., De Diego, A., Albillos, A., Bosch, J. Hepatology (2002) [Pubmed]
  16. Long-term effects of carvedilol in idiopathic dilated cardiomyopathy with persistent left ventricular dysfunction despite chronic metoprolol. The Heart-Muscle Disease Study Group. Di Lenarda, A., Sabbadini, G., Salvatore, L., Sinagra, G., Mestroni, L., Pinamonti, B., Gregori, D., Ciani, F., Muzzi, A., Klugmann, S., Camerini, F. J. Am. Coll. Cardiol. (1999) [Pubmed]
  17. Carvedilol alone or in combination with digoxin for the management of atrial fibrillation in patients with heart failure? Khand, A.U., Rankin, A.C., Martin, W., Taylor, J., Gemmell, I., Cleland, J.G. J. Am. Coll. Cardiol. (2003) [Pubmed]
  18. Effect of carvedilol in comparison with metoprolol on myocardial collagen postinfarction. Wei, S., Chow, L.T., Sanderson, J.E. J. Am. Coll. Cardiol. (2000) [Pubmed]
  19. Antiarrhythmic effect of carvedilol after acute myocardial infarction: results of the Carvedilol Post-Infarct Survival Control in Left Ventricular Dysfunction (CAPRICORN) trial. McMurray, J., Køber, L., Robertson, M., Dargie, H., Colucci, W., Lopez-Sendon, J., Remme, W., Sharpe, D.N., Ford, I. J. Am. Coll. Cardiol. (2005) [Pubmed]
  20. Beneficial effects of intravenous and oral carvedilol treatment in acute myocardial infarction. A placebo-controlled, randomized trial. Basu, S., Senior, R., Raval, U., van der Does, R., Bruckner, T., Lahiri, A. Circulation (1997) [Pubmed]
  21. Carvedilol, a cardiovascular drug, prevents vascular smooth muscle cell proliferation, migration, and neointimal formation following vascular injury. Ohlstein, E.H., Douglas, S.A., Sung, C.P., Yue, T.L., Louden, C., Arleth, A., Poste, G., Ruffolo, R.R., Feuerstein, G.Z. Proc. Natl. Acad. Sci. U.S.A. (1993) [Pubmed]
  22. Congestive heart failure induces endothelial cell apoptosis: protective role of carvedilol. Rössig, L., Haendeler, J., Mallat, Z., Hugel, B., Freyssinet, J.M., Tedgui, A., Dimmeler, S., Zeiher, A.M. J. Am. Coll. Cardiol. (2000) [Pubmed]
  23. Comparative hemodynamic, left ventricular functional, and antiadrenergic effects of chronic treatment with metoprolol versus carvedilol in the failing heart. Gilbert, E.M., Abraham, W.T., Olsen, S., Hattler, B., White, M., Mealy, P., Larrabee, P., Bristow, M.R. Circulation (1996) [Pubmed]
  24. Nonselective beta-adrenergic blockade with carvedilol does not hinder the benefits of exercise training in patients with congestive heart failure. Demopoulos, L., Yeh, M., Gentilucci, M., Testa, M., Bijou, R., Katz, S.D., Mancini, D., Jones, M., LeJemtel, T.H. Circulation (1997) [Pubmed]
  25. Plasma N-terminal pro-brain natriuretic peptide and adrenomedullin: prognostic utility and prediction of benefit from carvedilol in chronic ischemic left ventricular dysfunction. Australia-New Zealand Heart Failure Group. Richards, A.M., Doughty, R., Nicholls, M.G., MacMahon, S., Sharpe, N., Murphy, J., Espiner, E.A., Frampton, C., Yandle, T.G. J. Am. Coll. Cardiol. (2001) [Pubmed]
  26. Influence of carvedilol on hospitalizations in heart failure: incidence, resource utilization and costs. U.S. Carvedilol Heart Failure Study Group. Fowler, M.B., Vera-Llonch, M., Oster, G., Bristow, M.R., Cohn, J.N., Colucci, W.S., Gilbert, E.M., Lukas, M.A., Lacey, M.J., Richner, R., Young, S.T., Packer, M. J. Am. Coll. Cardiol. (2001) [Pubmed]
  27. Preventive effects of carvedilol on nitrate tolerance--a randomized, double-blind, placebo-controlled comparative study between carvedilol and arotinolol. Watanabe, H., Kakihana, M., Ohtsuka, S., Sugishita, Y. J. Am. Coll. Cardiol. (1998) [Pubmed]
  28. CYP2D6 genotype and induction of intestinal drug transporters by rifampin predict presystemic clearance of carvedilol in healthy subjects. Giessmann, T., Modess, C., Hecker, U., Zschiesche, M., Dazert, P., Kunert-Keil, C., Warzok, R., Engel, G., Weitschies, W., Cascorbi, I., Kroemer, H.K., Siegmund, W. Clin. Pharmacol. Ther. (2004) [Pubmed]
  29. Involvement of human hepatic UGT1A1, UGT2B4, and UGT2B7 in the glucuronidation of carvedilol. Ohno, A., Saito, Y., Hanioka, N., Jinno, H., Saeki, M., Ando, M., Ozawa, S., Sawada, J. Drug Metab. Dispos. (2004) [Pubmed]
  30. In vitro identification of the human cytochrome P450 enzymes involved in the metabolism of R(+)- and S(-)-carvedilol. Oldham, H.G., Clarke, S.E. Drug Metab. Dispos. (1997) [Pubmed]
  31. Double-blind, placebo-controlled study of the effects of carvedilol in patients with moderate to severe heart failure. The PRECISE Trial. Prospective Randomized Evaluation of Carvedilol on Symptoms and Exercise. Packer, M., Colucci, W.S., Sackner-Bernstein, J.D., Liang, C.S., Goldscher, D.A., Freeman, I., Kukin, M.L., Kinhal, V., Udelson, J.E., Klapholz, M., Gottlieb, S.S., Pearle, D., Cody, R.J., Gregory, J.J., Kantrowitz, N.E., LeJemtel, T.H., Young, S.T., Lukas, M.A., Shusterman, N.H. Circulation (1996) [Pubmed]
  32. Carvedilol increases the production of interleukin-12 and interferon-gamma and improves the survival of mice infected with the encephalomyocarditis virus. Nishio, R., Shioi, T., Sasayama, S., Matsumori, A. J. Am. Coll. Cardiol. (2003) [Pubmed]
  33. Tolerability and efficacy of carvedilol in patients with New York Heart Association class IV heart failure. Macdonald, P.S., Keogh, A.M., Aboyoun, C.L., Lund, M., Amor, R., McCaffrey, D.J. J. Am. Coll. Cardiol. (1999) [Pubmed]
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