Skip to main content
PMC home page
British Journal of Clinical Pharmacology logoLink to British Journal of Clinical Pharmacology
. 1986 Sep;22(3):293–300. doi: 10.1111/j.1365-2125.1986.tb02890.x

Pharmacodynamic profile of bisoprolol, a new beta 1-selective adrenoceptor antagonist.

G Leopold, W Ungethüm, J Pabst, Z Simane, K U Bühring, H Wiemann
PMCID: PMC1401121  PMID: 2876722

Abstract

The pharmacodynamic profile of bisoprolol, a new beta 1-selective adrenoceptor antagonist, was investigated in four independent studies including 36 healthy male volunteers. Using the model of exercise-induced tachycardia (ET) the beta-adrenoceptor blocking properties of bisoprolol (2.5-40 mg) were examined in comparison to metoprolol (50 and 100 mg), propranolol (40 and 80 mg) and atenolol (50 and 100 mg). The maximal reduction of ET was achieved between 1 and 4 h following single oral administration. The dose-response relationship using individual maximal reduction of ET showed, on a molar basis, that bisoprolol is about 5, 7 and 10 times more effective than propranolol, atenolol and metoprolol, respectively. In the model of insulin-induced hypoglycaemia bisoprolol behaved as a beta 1-selective adrenoceptor antagonist. There was a good correlation (r = 0.94) between the log bisoprolol concentration and the reduction in exercise-induced tachycardia. Bisoprolol is a potent new cardioselective beta-adrenoceptor antagonist with a competitive action at beta 1-adrenoceptors.

Full text

PDF
293

Selected References

These references are in PubMed. This may not be the complete list of references from this article.

  1. Armitstead J. G., Lightman S. L., Brown M. J., Causon R. C., Vaughan N. J. The effect of selective and non-selective beta-adrenoceptor blockade, and of naloxone infusion, on the hormonal mechanisms of recovery from insulin-induced hypoglycaemia in man. Br J Clin Pharmacol. 1983 Dec;16(6):718–721. doi: 10.1111/j.1365-2125.1983.tb02248.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  2. Brown J. E., McLeod A. A., Shand D. G. Evidence for cardiac beta 2-adrenoceptors in man. Clin Pharmacol Ther. 1983 Apr;33(4):424–428. doi: 10.1038/clpt.1983.57. [DOI] [PubMed] [Google Scholar]
  3. Brown M. J., Brown D. C., Murphy M. B. Hypokalemia from beta2-receptor stimulation by circulating epinephrine. N Engl J Med. 1983 Dec 8;309(23):1414–1419. doi: 10.1056/NEJM198312083092303. [DOI] [PubMed] [Google Scholar]
  4. Davidson N. M., Corrall R. J., Shaw T. R., French E. B. Observations in man of hypoglycaemia during selective and non-selective beta-blockade. Scott Med J. 1977 Jan;22(1):69–72. doi: 10.1177/003693307702200117. [DOI] [PubMed] [Google Scholar]
  5. Deacon S. P., Barnett D. Comparison of atenolol and propranolol during insulin-induced hypoglycaemia. Br Med J. 1976 Jul 31;2(6030):272–273. doi: 10.1136/bmj.2.6030.272. [DOI] [PMC free article] [PubMed] [Google Scholar]
  6. Dorow P., Tönnesmann U. Dose-response relationship of the beta-adrenoceptor antagonist bisoprolol in patients with coronary heart disease and chronic obstructive bronchitis. Eur J Clin Pharmacol. 1984;27(2):135–139. doi: 10.1007/BF00544035. [DOI] [PubMed] [Google Scholar]
  7. Harry J. D. The demonstration of atenolol as a beta-adrenoceptor blocking drug in man. Postgrad Med J. 1977;53 (Suppl 3):65–69. [PubMed] [Google Scholar]
  8. Johnsson G., Nyberg G., Sölvell L. Influence of metoprolol and propranolol on hemodynamic effects induced by physical work and isoprenaline. Acta Pharmacol Toxicol (Copenh) 1975;36(Suppl 5):69–75. doi: 10.1111/j.1600-0773.1975.tb03323.x. [DOI] [PubMed] [Google Scholar]
  9. Johnsson G., Regårdh C. G., Sölvell L. Combined pharmacokinetic and pharmacodynammc studies in man of the adrenergic beta1-receptor antagonist metoprolol. Acta Pharmacol Toxicol (Copenh) 1975;36(Suppl 5):31–44. doi: 10.1111/j.1600-0773.1975.tb03320.x. [DOI] [PubMed] [Google Scholar]
  10. Kohli R. S., Khurmi N. S., Kardash M. M., Hughes L. O., Lahiri A., Raftery E. B. Efficacy of once daily bisoprolol in stable angina pectoris: an objective comparison with atenolol and long term follow-up. Eur Heart J. 1985 Oct;6(10):845–850. doi: 10.1093/oxfordjournals.eurheartj.a061771. [DOI] [PubMed] [Google Scholar]
  11. Lager I. Adrenergic blockade and hypoglycaemia. Acta Med Scand Suppl. 1983;672:63–67. doi: 10.1111/j.0954-6820.1983.tb01615.x. [DOI] [PubMed] [Google Scholar]
  12. Lammers J. W., Folgering H. T., van Herwaarden C. L. Ventilatory effects of beta 1-receptor-selective blockade with bisoprolol and metoprolol in asthmatic patients. Eur J Clin Pharmacol. 1984;27(2):141–145. doi: 10.1007/BF00544036. [DOI] [PubMed] [Google Scholar]
  13. Manalan A. S., Besch H. R., Jr, Watanabe A. M. Characterization of [3H](+/-)carazolol binding to beta-adrenergic receptors. Application to study of beta-adrenergic receptor subtypes in canine ventricular myocardium and lung. Circ Res. 1981 Aug;49(2):326–336. doi: 10.1161/01.res.49.2.326. [DOI] [PubMed] [Google Scholar]
  14. McDevitt D. G. The assessment of beta-adrenoceptor blocking drugs in man. Br J Clin Pharmacol. 1977 Aug;4(4):413–425. doi: 10.1111/j.1365-2125.1977.tb00756.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  15. Newman R. J. Comparison of propranolol, metoprolol, and acebutolol on insulin-induced hypoglycaemia. Br Med J. 1976 Aug 21;2(6033):447–449. doi: 10.1136/bmj.2.6033.447. [DOI] [PMC free article] [PubMed] [Google Scholar]
  16. Newman R. J. Comparison of the antilipolytic effect of metoprolol, acebutolol, and propranolol in man. Br Med J. 1977 Sep 3;2(6087):601–603. doi: 10.1136/bmj.2.6087.601. [DOI] [PMC free article] [PubMed] [Google Scholar]
  17. Ostman J. beta-adrenergic blockade and diabetes mellitus. A review. Acta Med Scand Suppl. 1983;672:69–77. [PubMed] [Google Scholar]
  18. Prager G., Wagner G. Wirkung von Bisoprolol bei koronarer Herzkrankheit. Einfluss auf Herz-Kreislauf-Parameter und ischämische ST-Streckensenkung: Untersuchungen zur Wirkungsdauer. Dtsch Med Wochenschr. 1984 Dec 14;109(50):1914–1917. doi: 10.1055/s-2008-1069478. [DOI] [PubMed] [Google Scholar]
  19. Robinson B. F. Relation of heart rate and systolic blood pressure to the onset of pain in angina pectoris. Circulation. 1967 Jun;35(6):1073–1083. doi: 10.1161/01.cir.35.6.1073. [DOI] [PubMed] [Google Scholar]
  20. Schliep H. J., Harting J. Beta 1-selectivity of bisoprolol, a new beta-adrenoceptor antagonist, in anesthetized dogs and guinea pigs. J Cardiovasc Pharmacol. 1984 Nov-Dec;6(6):1156–1160. [PubMed] [Google Scholar]
  21. Tattersfield A. E., Cragg D. J., Bacon R. J. Assessment of beta-adrenoceptor selectivity of a new beta-adrenoceptor antagonist, bisoprolol, in man. Br J Clin Pharmacol. 1984 Sep;18(3):343–347. doi: 10.1111/j.1365-2125.1984.tb02474.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  22. Weiner L., Frithz G. Antihypertensive effects of bisoprolol during once daily administration in patients with essential hypertension. A dose-ranging study with parallel groups. Eur J Clin Pharmacol. 1986;29(5):517–521. doi: 10.1007/BF00635886. [DOI] [PubMed] [Google Scholar]

Articles from British Journal of Clinical Pharmacology are provided here courtesy of British Pharmacological Society

RESOURCES