Cardio-Selective Beta-Blocker: Pharmacological Evidence and Their Influence on Exercise Capacity

Cardiovascular Therapeutics

Volumn 31, Issue 2, 2013, Pages 76-83

  Ladage, Dennis ^a,c   Schwinger, Robert H G ^b   Brixius, Klara ^a  

^a GERMAN SPORT UNIVERSITY COLOGNE   (Germany)

^b Clinic II of Internal Medicine and Cardiology   (Germany)

^c UNIVERSITY OF COLOGNE   (Germany)

Author keywords

Beta blocker; Cardiovascular disease; Hypertension

Indexed keywords

ATENOLOL; BETA ADRENERGIC RECEPTOR BLOCKING AGENT; BISOPROLOL; CARVEDILOL; METOPROLOL; NEBIVOLOL;

AEROBIC EXERCISE; COMPETITIVE INHIBITION; DRUG HALF LIFE; DRUG MECHANISM; EXERCISE; EXERCISE TEST; HEART FAILURE; HUMAN; MEMBRANE TRANSPORT; NONHUMAN; PRIORITY JOURNAL; REVIEW;

ADRENERGIC BETA-ANTAGONISTS; ANIMALS; CARDIOVASCULAR AGENTS; CARDIOVASCULAR DISEASES; COMORBIDITY; EXERCISE TOLERANCE; HUMANS; MUSCLE, SKELETAL; RECOVERY OF FUNCTION; RISK ASSESSMENT; TREATMENT OUTCOME;

EID: 84875806102     PISSN: 17555914     EISSN: 17555922     Source Type: Journal    
DOI: 10.1111/j.1755-5922.2011.00306.x     Document Type: Review

References (86)

1. Black JW, Stephenson JS. Pharmacology of a new adrenergic beta-receptor-blocking compound (Nethalide]. Lancet 1962;2:311-314.
2. Mukherjee D, Fang J, Chetcuti S, Moscucci M, Kline-Rogers E, Eagle KA. Impact of combination evidence-based medical therapy on mortality in patients with acute coronary syndromes. Circulation 2004;109:745-749.
3. Benovic JL, Bouvier M, Caron MG, Lefkowitz RJ. Regulation of adenylyl cyclase-coupled beta-adrenergic receptors. Annu Rev Cell Biol 1988;4:405-428.
4. Bylund DB, Eikenberg DC, Hieble JP, et al. International Union of Pharmacology nomenclature of adrenoceptors. Pharmacol Rev 1994;46:121-136.
5. Lopez-Sendon J, Swedberg K, McMurray J, et al. Expert consensus document on beta-adrenergic receptor blockers. Eur Heart J 2004;25:1341-1362.
6. Pott C, Brixius K, Bundkirchen A, et al. The preferential beta3-adrenoceptor agonist BRL 37344 increases force via beta1-/beta2-adrenoceptors and induces endothelial nitric oxide synthase via beta3-adrenoceptors in human atrial myocardium. Br J Pharmacol 2003;138:521-529.
7. Pott C, Steinritz D, Napp A, Bloch W, Schwinger RH, Brixius K. On the function of beta3-adrenoceptors in the human heart: Signal transduction, inotropic effect and therapeutic prospects. Wien Med Wochenschr 2006;156:451-458.
8. Moniotte S, Kobzik L, Feron O, Trochu JN, Gauthier C, Balligand JL. Upregulation of beta(3)-adrenoceptors and altered contractile response to inotropic amines in human failing myocardium. Circulation 2001;103:1649-1655.
9. Berlan M, Galitzky J, Bousquet-Melou A, Lafontan M, Montastruc JL. Beta-3 adrenoceptor-mediated increase in cutaneous blood flow in the dog. J Pharmacol Exp Ther 1994;268:1444-1451.
10. Kaumann AJ, Molenaar P. Modulation of human cardiac function through 4 beta-adrenoceptor populations. Naunyn Schmiedebergs Arch Pharmacol 1997;355:667-681.
11. Michel MC, Harding SE, Bond RA. Are there functional beta-adrenoceptors in the human heart?Br J Pharmacol 2011;162:817-822.
12. Daaka Y, Luttrell LM, Ahn S, Della Rocca GJ, Ferguson SS, Caron MG, Lefkowitz RJ. Essential role for G protein-coupled receptor endocytosis in the activation of mitogen-activated protein kinase. J Biol Chem 1998;273:685-688.
13. Baker JG, Hall IP, Hill SJ. Agonist and inverse agonist actions of beta-blockers at the human beta 2-adrenoceptor provide evidence for agonist-directed signaling. Mol Pharmacol 2003;64:1357-1369.
14. Lemoine H, Schonell H, Kaumann AJ. Contribution of beta 1- and beta 2-adrenoceptors of human atrium and ventricle to the effects of noradrenaline and adrenaline as assessed with (-)-atenolol. Br J Pharmacol 1988;95:55-66.
15. Gaemperli O, Liga R, Spyrou N, et al. Myocardial beta-adrenoceptor down-regulation early after infarction is associated with long-term incidence of congestive heart failure. Eur Heart J 2010;31:1722-1729.
16. Bristow MR, Ginsburg R, Umans V, et al. Beta 1- and beta 2-adrenergic-receptor subpopulations in nonfailing and failing human ventricular myocardium: Coupling of both receptor subtypes to muscle contraction and selective beta 1-receptor down-regulation in heart failure. Circ Res 1986;59:297-309.
17. Schafers M, Dutka D, Rhodes CG, Lammertsma AA, Hermansen F, Schober O, Camici PG. Myocardial presynaptic and postsynaptic autonomic dysfunction in hypertrophic cardiomyopathy. Circ Res 1998;82:57-62.
18. Ungerer M, Bohm M, Elce JS, Erdmann E, Lohse MJ. Altered expression of beta-adrenergic receptor kinase and beta 1-adrenergic receptors in the failing human heart. Circulation 1993;87:454-463.
19. Varghese P, Harrison RW, Lofthouse RA, Georgakopoulos D, Berkowitz DE, Hare JM. beta(3)-adrenoceptor deficiency blocks nitric oxide-dependent inhibition of myocardial contractility. J Clin Invest 2000;106:697-703.
20. Wood AJ. Pharmacologic differences between beta blockers. Am Heart J 1984;108:1070-1077.
21. Covinsky JO. Esmolol: A novel cardioselective, titratable, intravenous beta-blocker with ultrashort half-life. Drug Intell Clin Pharm 1987;21:316-321.
22. Kirch W, Gorg KG. Clinical pharmacokinetics of atenolol-a review. Eur J Drug Metab Pharmacokinet 1982;7:81-91.
23. McDevitt DG. Comparison of pharmacokinetic properties of beta-adrenoceptor blocking drugs. Eur Heart J 1987;8 Suppl M:9-14.
24. Kalinowski L, Dobrucki LW, Szczepanska-Konkel M, Jankowski M, Martyniec L, Angielski S, Malinski T. Third-generation beta-blockers stimulate nitric oxide release from endothelial cells through ATP efflux: A novel mechanism for antihypertensive action. Circulation 2003;107:2747-2752.
25. Yue TL, Wang X, Gu JL, Ruffolo RR, Jr., Feuerstein GZ. Carvedilol, a new vasodilating beta-adrenoceptor blocker, inhibits oxidation of low-density lipoproteins by vascular smooth muscle cells and prevents leukocyte adhesion to smooth muscle cells. J Pharmacol Exp Ther 1995;273:1442-1449.
26. Wolf SC, Sauter G, Jobst J, Kempf VA, Risler T, Brehm BR. Major differences in gene expression in human coronary smooth muscle cells after nebivolol or metoprolol treatment. Int J Cardiol 2008;125:4-10.
27. Beutler B, Cerami A. The biology of cachectin/TNF-a primary mediator of the host response. Annu Rev Immunol 1989;7:625-655.
28. Hernandez-Presa MA, Martin-Ventura JL, Ortego M, et al. Atorvastatin reduces the expression of cyclooxygenase-2 in a rabbit model of atherosclerosis and in cultured vascular smooth muscle cells. Atherosclerosis 2002;160:49-58.
29. Prichard BN. Pharmacologic aspects of intrinsic sympathomimetic activity in beta-blocking drugs. Am J Cardiol 1987;59:13F-17F.
30. McDevitt DG. Pharmacologic aspects of cardioselectivity in a beta-blocking drug. Am J Cardiol 1987;59:10F-12F.
31. Bristow MR. beta-adrenergic receptor blockade in chronic heart failure. Circulation 2000;101:558-569.
32. Weber MA. The role of the new beta-blockers in treating cardiovascular disease. Am J Hypertens 2005;18:169S-176S.
33. Van de Water A, Janssens W, Van Neuten J, et al. Pharmacological and hemodynamic profile of nebivolol, a chemically novel, potent, and selective beta 1-adrenergic antagonist. J Cardiovasc Pharmacol 1988;11:552-563.
34. Baker JG. The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors. Br J Pharmacol 2005;144:317-322.
35. Psaty BM, Smith NL, Siscovick DS, et al. Health outcomes associated with antihypertensive therapies used as first-line agents. A systematic review and meta-analysis. JAMA 1997;277:739-745.
36. Freemantle N, Cleland J, Young P, Mason J, Harrison J. Beta blockade after myocardial infarction: Systematic review and meta regression analysis. BMJ 1999;318:1730-1737.
37. Hunt SA, Baker DW, Chin MH, et al. ACC/AHA Guidelines for the Evaluation and Management of Chronic Heart Failure in the Adult: Executive Summary A Report of the American College of Cardiology/American Heart Association Task Force on Practice Guidelines (Committee to Revise the 1995 Guidelines for the Evaluation and Management of Heart Failure): Developed in Collaboration With the International Society for Heart and Lung Transplantation; Endorsed by the Heart Failure Society of America. Circulation 2001;104:2996-3007.
38. Willenheimer R, van Veldhuisen DJ, Silke B, et al. Effect on survival and hospitalization of initiating treatment for chronic heart failure with bisoprolol followed by enalapril, as compared with the opposite sequence: Results of the randomized Cardiac Insufficiency Bisoprolol Study (CIBIS) III. Circulation 2005;112:2426-2435.
39. Effect of metoprolol CR/XL in chronic heart failure: Metoprolol CR/XL Randomised Intervention Trial in Congestive Heart Failure (MERIT-HF). Lancet 1999;353:2001-2007.
40. Packer M, Bristow MR, Cohn JN, Colucci WS, Fowler MB, Gilbert EM, Shusterman NH. The effect of carvedilol on morbidity and mortality in patients with chronic heart failure. U.S. Carvedilol Heart Failure Study Group. N Engl J Med 1996;334:1349-1355.
41. Robb OJ, Webster J, Petrie JC, Harry JD, Young J. Effects of the beta 2-adrenoceptor antagonist ICI 118, 551 on blood pressure in hypertensive patients known to respond to beta 1-adrenoceptor antagonists. Br J Clin Pharmacol 1988;25:433-438.
42. Prichard BN, Ross EJ. Use of propranolol in conjunction with alpha receptor blocking drugs in pheochromocytoma. Am J Cardiol 1966;18:394-398.
43. Cruickshank JM. Beta-blockers continue to surprise us. Eur Heart J 2000;21:354-364.
44. Beta-Blocker Evaluation of Survival Trial Investigators. A trial of the beta-blocker bucindolol in patients with advanced chronic heart failure. N Engl J Med 2001;344:1659-1667.
45. Kaye DM, Lefkovits J, Jennings GL, Bergin P, Broughton A, Esler MD. Adverse consequences of high sympathetic nervous activity in the failing human heart. J Am Coll Cardiol 1995;26:1257-1263.
46. Winniford MD, Fulton KL, Hillis LD. Long-term therapy of paroxysmal supraventricular tachycardia: A randomized, double-blind comparison of digoxin, propranolol and verapamil. Am J Cardiol 1984;54:1138-1139.
47. Geffner DL, Hershman JM. Beta-adrenergic blockade for the treatment of hyperthyroidism. Am J Med 1992;93:61-68.
48. Plouin PF, Gimenez-Roqueplo AP. Pheochromocytomas and secreting paragangliomas. Orphanet J Rare Dis 2006;1:49.
49. Ziegelstein RC. Acute emotional stress and cardiac arrhythmias. JAMA 2007;298:324-329.
50. Tacoy G, Balcioglu AS, Arslan U, Durakoglugil E, Erdem G, Ozdemir M, Cengel A. Effect of metoprolol on heart rate variability in symptomatic patients with mitral valve prolapse. Am J Cardiol 2007;99:1568-1570.
51. Schwartz PJ, La Rovere MT, Vanoli E. Autonomic nervous system and sudden cardiac death. Experimental basis and clinical observations for post-myocardial infarction risk stratification. Circulation 1992;85:I77-191.
52. Jacob S, Rett K, Henriksen EJ. Antihypertensive therapy and insulin sensitivity: Do we have to redefine the role of beta-blocking agents?Am J Hypertens 1998;11:1258-1265.
53. Cruickshank JM. Are we misunderstanding beta-blockers. Int J Cardiol 2007;120:10-27.
54. Steinberg HO, Baron AD. Vascular function, insulin resistance and fatty acids. Diabetologia. 2002;45:623-634.
55. Lithell H, Pollare T, Berne C, Saltin B. The metabolic and circulatory response to beta-blockade in hypertensive men is correlated to muscle capillary density. Blood Pressure 1992;1:20-26.
56. Myers MG, Hope-Gill HF. Effect of d- and dl-propranolol on glucose-stimulated insulin release. Clin Pharmacol Ther 1979;25:303-308.
57. Efficacy of atenolol and captopril in reducing risk of macrovascular and microvascular complications in type 2 diabetes: UKPDS 39. UK Prospective Diabetes Study Group. BMJ 1998;317:713-720.
58. Caro JF. Clinical review 26: Insulin resistance in obese and nonobese man. J Clin Endocrinol Metab 1991;73:691-695.
59. Ladage D, Reidenbach C, Rieckeheer E, Graf C, Schwinger RH, Brixius K. Nebivolol lowers blood pressure and increases weight loss in patients with hypertension and diabetes in regard to age. J Cardiovasc Pharmacol 2010;56:275-281.
60. Nuttall SL, Routledge HC, Kendall MJ. A comparison of the beta1-selectivity of three beta1-selective beta-blockers. J Clin Pharm Ther 2003;28:179-186.
61. Dominguez LJ, Barbagallo M, Jacober SJ, Jacobs DB, Sowers JR. Bisoprolol and captopril effects on insulin receptor tyrosine kinase activity in essential hypertension. Am J Hypertens 1997;10:1349-1355.
62. Seguchi H, Nakamura H, Aosaki N, Homma Y, Mikami Y, Takahashi S. Effects of carvedilol on serum lipids in hypertensive and normotensive subjects. Eur J Clin Pharmacol 1990;38 Suppl 2: S139-S142.
63. Poirier L, Cleroux J, Nadeau A, Lacourciere Y. Effects of nebivolol and atenolol on insulin sensitivity and haemodynamics in hypertensive patients. J Hypertens 2001;19:1429-1435.
64. Chobanian AV, Bakris GL, Black HR, et al. Seventh report of the Joint National Committee on Prevention, Detection, Evaluation, and Treatment of High Blood Pressure. Hypertension 2003;42:1206-1252.
65. Arch JR. beta(3)-Adrenoceptor agonists: Potential, pitfalls and progress. Eur J Pharmacol 2002;440:99-107.
66. Brixius K, Bloch W, Pott C, et al. Mechanisms of beta 3-adrenoceptor-induced eNOS activation in right atrial and left ventricular human myocardium. Br J Pharmacol 2004;143:1014-1022.
67. Westhoff TH, Franke N, Schmidt S, Vallbracht-Israng K, Zidek W, Dimeo F, van der Giet M. Beta-blockers do not impair the cardiovascular benefits of endurance training in hypertensives. J Hum Hypertens 2007;21:486-493.
68. Gullestad L, Hallen J, Medbo JI, Gronnerod O, Holme I, Sejersted OM. The effect of acute vs chronic treatment with beta-adrenoceptor blockade on exercise performance, haemodynamic and metabolic parameters in healthy men and women. Br J Clin Pharmacol 1996;41:57-67.
69. Van Baak MA. Beta-adrenoceptor blockade and exercise. An update. Sports Med 1988;5:209-225.
70. Ades PA, Gunther PG, Meyer WL, Gibson TC, Maddalena J, Orfeo T. Cardiac and skeletal muscle adaptations to training in systemic hypertension and effect of beta blockade (metoprolol or propranolol). Am J Cardiol 1990;66:591-596.
71. Van Bortel LM, van Baak MA. Exercise tolerance with nebivolol and atenolol. Cardiovasc Drugs Ther 1992;6:239-247.
72. Beloka S, Gujic M, Deboeck G, et al. Beta-adrenergic blockade and metabo-chemoreflex contributions to exercise capacity. Med Sci Sports Exerc 2008;40:1932-1938.
73. Houssiere A, Najem B, Ciarka A, Velez-Roa S, Naeije R, van de Borne P. Chemoreflex and metaboreflex control during static hypoxic exercise. Am J Physiol Heart Circ Physiol 2005;288:H1724-H1729.
74. Cogliati C, Colombo S, Ruscone TG, et al. Acute beta-blockade increases muscle sympathetic activity and modifies its frequency distribution. Circulation 2004;110:2786-2791.
75. Ji LL, Lennon DL, Kochan RG, Nagle FJ, Lardy HA. Enzymatic adaptation to physical training under beta-blockade in the rat. Evidence of a beta 2-adrenergic mechanism in skeletal muscle. J Clin Invest 1986;78:771-778.
76. Miura S, Kai Y, Kamei Y, Ezaki O. Isoform-specific increases in murine skeletal muscle peroxisome proliferator-activated receptor-gamma coactivator-1alpha (PGC-1alpha) mRNA in response to beta2-adrenergic receptor activation and exercise. Endocrinology 2008;149:4527-4533.
77. Miura S, Kawanaka K, Kai Y, Tamura M, Goto M, Shiuchi T, Minokoshi Y, Ezaki O. An increase in murine skeletal muscle peroxisome proliferator-activated receptor-gamma coactivator-1alpha (PGC-1alpha) mRNA in response to exercise is mediated by beta-adrenergic receptor activation. Endocrinology 2007;148:3441-3448.
78. Chua TP, Clark AL, Amadi AA, Coats AJ. Relation between chemosensitivity and the ventilatory response to exercise in chronic heart failure. J Am Coll Cardiol 1996;27:650-657.
79. Schneider DA, McEniery MT, Solomon C, Jurimae J, Wehr MS. Ventilatory and hyperkalemic responses to incremental exercise after propranolol treatment. J Appl Physiol 1994;77:1907-1912.
80. Conway MA, Petersen ES. Effects of beta-adrenergic blockade on the ventilatory responses to hypoxic and hyperoxic exercise in man. J Physiol 1987;393:43-55.
81. Jilka SM, Joyner MJ, Nittolo JM, Kalis JK, Taylor JA, Lohman TG, Wilmore JH. Maximal exercise responses to acute and chronic beta-adrenergic blockade in healthy male subjects. Med Sci Sports Exerc 1988;20:570-573.
82. Mutlu GM, Koch WJ, Factor P. Alveolar epithelial beta 2-adrenergic receptors: Their role in regulation of alveolar active sodium transport. Am J Respir Crit Care Med 2004;170:1270-1275.
83. Piepoli MF, Guazzi M, Boriani G, et al. Exercise intolerance in chronic heart failure: mechanisms and therapies. Part I. Eur J Cardiovasc Prev Rehabil 2010;17:637-642.
84. Agostoni P, Contini M, Magini A, et al. Carvedilol reduces exercise-induced hyperventilation: A benefit in normoxia and a problem with hypoxia. Eur J Heart Fail 2006;8:729-735.
85. Baker JG. The selectivity of beta-adrenoceptor agonists at human beta1-, beta2- and beta3-adrenoceptors. Br J Pharmacol 2010;160:1048-1061.
86. Bond RA, Spina D, Parra S, Page CP. Getting to the heart of asthma: Can "beta blockers" be useful to treat asthma?Pharmacol Ther 2007;115:360-374.