Skip to main content
British Journal of Clinical Pharmacology logoLink to British Journal of Clinical Pharmacology
. 1978 Feb;5(2):107–120. doi: 10.1111/j.1365-2125.1978.tb01609.x

Studies of cardioselectivity and partial agonist activity in beta-adrenoceptor blockade comparing effects on heart rate and peak expiratory flow rate during exercise.

V M Oh, C M Kaye, S J Warrington, E A Taylor, J Wadsworth
PMCID: PMC1429244  PMID: 23136

Abstract

1 The effects of beta-adrenoceptor antagonists given in single doses by oral or intravenous routes were examined in two double-blind controlled studies performed in healthy volunteers. Heart rate and peak expiratory flow rate (PEFR) were measured at rest and during standardized exercise. 2 Propranolol 80 mg and metoprolol 100 mg orally tended to reduce, and propranolol and metoprolol 0.2 mg/kg intravenously did reduce the physiological increase in PEFR during exercise; oxprenolol 80 mg orally and 0.2 mg/kg intravenously did not. Practolol 200 mg orally reduced this increase, but practolol 1 mg/kg intravenously did not. 3 In a third study of similar design, pindolol 0.05 mg/kg intravenously did not affect exercise-induced increase in PEFR. 4 Heart rate during exercise was reduced to a comparable extent at different times by all the active treatments. 5 Oxprenolol and pindolol share with practolol the property of partial agonist activity, which might contribute to their apparent lack of effect on airways resistance. A further possibility is that alpha-adrenoceptor blockade helps to maintain exercise-induced increase in PEFR.

Full text

PDF
107

Selected References

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

  1. Bianco S., Griffin J. P., Kamburoff P. L., Prime F. J. Prevention of exercise-induced asthma by indoramin. Br Med J. 1974 Oct 5;4(5935):18–20. doi: 10.1136/bmj.4.5935.18. [DOI] [PMC free article] [PubMed] [Google Scholar]
  2. Degen P. H., Riess W. Simplified method for the determination of oxprenolol and other beta-receptor-blocking agents in biological fluids by gas-liquid chromatography. J Chromatogr. 1976 Jun 9;121(1):72–75. doi: 10.1016/s0021-9673(00)82299-2. [DOI] [PubMed] [Google Scholar]
  3. Harms H. H. Isoproterenol antagonism of cardioselective beta adrenergic receptor blocking agents: a comparative study of human and guinea-pig cardiac and bronchial beta adrenergic receptors. J Pharmacol Exp Ther. 1976 Nov;199(2):329–335. [PubMed] [Google Scholar]
  4. 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]
  5. Johnsson G., Svedmyr N., Thiringer G. Effects of intravenous propranolol and metoprolol and their interaction with isoprenaline on pulmonary function, heart rate and blood pressure in asthmatics. Eur J Clin Pharmacol. 1975 Apr 4;8(3-4):175–180. doi: 10.1007/BF00567111. [DOI] [PubMed] [Google Scholar]
  6. Kamburoff P. L. Bronchomotor tone and its modification by certain drugs. Postgrad Med J. 1976 Apr;52(606):190–196. doi: 10.1136/pgmj.52.606.190. [DOI] [PMC free article] [PubMed] [Google Scholar]
  7. Kumana C. R., Marlin G. E., Kaye C. M., Smith D. M. New approach to assessment of cardioselectivity of beta-blocking drugs. Br Med J. 1974 Nov 23;4(5942):444–447. doi: 10.1136/bmj.4.5942.444. [DOI] [PMC free article] [PubMed] [Google Scholar]
  8. Lertora J. J., Mark A. L., Johannsen J., Wilson W. R., Abboud F. M. Selective beta-1 receptor blockade with oral practolol in man. A dose-related phenomenon. J Clin Invest. 1975 Sep;56(3):719–724. doi: 10.1172/JCI108143. [DOI] [PMC free article] [PubMed] [Google Scholar]
  9. Maconochie J. G., Woodings E. P., Richards D. A. Effects of labetalol and propranolol on histamine-induced bronchoconstriction in normal subjects. Br J Clin Pharmacol. 1977 Apr;4(2):157–162. doi: 10.1111/j.1365-2125.1977.tb00688.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  10. 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]
  11. 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]
  12. Pacha W. L. A method for the fluorimetric determination of 4-(2-hydroxy-3-isopropylaminopropoxy)-indole (LB46), a beta-blocking agent, in plasma and urine. Experientia. 1969 Aug 15;25(8):802–803. doi: 10.1007/BF01897885. [DOI] [PubMed] [Google Scholar]
  13. Paterson J. W. Beta-adrenergic blocking drugs. Br Med J. 1971 Jun 12;2(5762):652–652. doi: 10.1136/bmj.2.5762.652-b. [DOI] [PMC free article] [PubMed] [Google Scholar]
  14. Richards D. A., Woodings E. P., Maconochie J. G. Comparison of the effects of labetalol and propranolol in healthy men at rest and during exercise. Br J Clin Pharmacol. 1977 Feb;4(1):15–21. doi: 10.1111/j.1365-2125.1977.tb00660.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  15. Scales B., Cosgrove M. B. The metabolism and distribution of the selective adrenergic beta blocking agent, practolol. J Pharmacol Exp Ther. 1970 Nov;175(2):338–347. [PubMed] [Google Scholar]
  16. Shand D. G., Nuckolls E. M., Oates J. A. Plasma propranolol levels in adults with observations in four children. Clin Pharmacol Ther. 1970 Jan-Feb;11(1):112–120. doi: 10.1002/cpt1970111112. [DOI] [PubMed] [Google Scholar]
  17. Singh B. N., Whitlock R. M., Comber R. H., Williams F. H., Harris E. A. Effects of cardioselective beta adrenoceptor blockade on specific airways resistance in normal subjects and in patients with bronchial asthma. Clin Pharmacol Ther. 1976 May;19(5 Pt 1):493–501. doi: 10.1002/cpt1976195part1493. [DOI] [PubMed] [Google Scholar]
  18. Turner P., Burman J., Hicks D. C., Cherrington N. K., MacKinnon J., Wallet T., Woolnough M. A comparison of the effects of propranolol and practolol on forced expiratory volume and resting heart rate in normal subjects. Arch Int Pharmacodyn Ther. 1971 May;191(1):104–110. [PubMed] [Google Scholar]
  19. Waal-Manning H. J., Simpson F. O. Practolol treatment in asthmatics. Lancet. 1971 Dec 4;2(7736):1264–1265. doi: 10.1016/s0140-6736(71)90585-x. [DOI] [PubMed] [Google Scholar]

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

RESOURCES