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European Journal of Clinical Pharmacology

, Volume 15, Issue 4, pp 229–233 | Cite as

Exercise responses of healthy subjects in the evaluation of cardioselectivity ofβ-blockers

  • K. L. Woods
  • S. P. Linton
  • M. J. Kendall
  • E. B. Faragher
  • R. J. Grieve
Originals

Summary

The effects of intravenous propranolol, metoprolol, acebutolol and placebo on exercise-induced changes in heart rate and peak flow rate (PFR) have been studied in a group of healthy subjects. The three β-blockers produced significant and comparable reductions in exercise-induced tachycardia and the magnitude of the reduction was related to the log plasma concentration of each drug. Significant cardiac β-blockade was detectable for three hours after giving propranolol and for four hours after metoprolol and acebutolol. The exercise-induced changes in PFR were small and variable and were not significantly affected by any of the drugs. We conclude that, contrary to published reports, exercise-induced changes in heart rate and PFR in healthy subjects do not provide a satisfactory test system for assessing the selectivity of β-blockers.

Key words

propranolol metoprolol acebutolol exercise testing healthy subjects 

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References

  1. Basil, B., Jordan, R., Loveless, A. H., Maxwell, D. R.: β-Adrenoceptor blocking properties and cardioselectivity of M & B 17803A. Br. J. Pharmacol.48, 198–211 (1973)Google Scholar
  2. Benson, M. K., Berrill, W. T., Cruickshank, J. M., Sterling, G. S.: A comparison of four β-adrenoceptor antagonists in patients with asthma. Br. J. clin. Pharmacol.5, 415–419 (1978)Google Scholar
  3. Briant, R. H., Dollery, C. T., Fenyvesi, T., George, C. F.: Assessment of selective β-adrenoceptor blockade in man. Br. J. Pharmacol.49, 106–114 (1973)Google Scholar
  4. Cuthbert, M. F., Collins, R. F.: Plasma levels and β-adrenoceptor blockade with acebutolol, practolol and propranolol in man. Br. J. clin. Pharmacol.2, 49–55 (1975)Google Scholar
  5. Daly, M. J., Flook, J. J., Levy, G. P.: The selectivity of β-adrenoceptor antagonists on cardiovascular and bronchodilator response to isoprenaline in the anaesthetized dog. Br. J. Pharmacol.53, 173–181 (1975)Google Scholar
  6. Decalmer, P. B. S., Chatterjee, S. S., Cruickshank, J. M., Benson, M. K., Sterling, G. M.: Beta-blockers and asthma. Br. Heart J.40, 184–189 (1978)Google Scholar
  7. Harms, H. H., Spoelstra, A. J. G.: Cardiac and bronchial β-adrenoceptor antagonistic potencies of atenolol, metoprolol, acebutolol, practolol, propranolol and pindolol in the anaesthetized dog. Clin. exp. Pharmacol. Physiol.5, 53–59 (1978)Google Scholar
  8. Jack, D. B., Riess, W.: Determination of low levels of oxprenolol in blood or plasma by gas-liquid chromatography. J. Chromatogr.88, 173–176 (1974)Google Scholar
  9. 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. Europ. J. clin. Pharmacol.8, 175–180 (1975)Google Scholar
  10. 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/IV, 444–447Google Scholar
  11. Kumana, C. R., Kaye, C. M., Leighton, M., Turner, P., Hamer, J.: Cardiac and pulmonary effects of acebutolol. Lancet1975/II, 89–93Google Scholar
  12. McDevitt, D. G.: β-Adrenoceptor antagonists and respiratory function. Br. J. clin. Pharmacol.5, 97–99 (1978)Google Scholar
  13. Oh, V. M. S., Kaye, C. M., Warrington, S. J., Taylor, E. A., Wadsworth, J.: Studies of cardioselectivity and partial agonist activity in β-adrenoceptor blockade comparing effects on heart rate and peak expiratory flow rate during exercise. Br. J. clin. Pharmacol.5, 107–120 (1978)Google Scholar
  14. Paterson, J. W., Conolly, M. E., Dollery, C. T., Hayes, A., Cooper, R. G.: The pharmacodynamics and metabolism of propranolol in man. Pharmacol. Clin.2, 127–133 (1970)Google Scholar
  15. Shand, D. G., Nuckolls, E. M., Oates, J. A.: Plasma propranolol levels in adults. Clin. Pharmacol. Ther.11, 112–120 (1970)Google Scholar
  16. Tivenius, L.: Effects of multiple doses of metoprolol and propranolol on ventilatory function in patients with chronic obstructive lung disease. Scand. J. Respir. Dis.57, 190–196 (1976)Google Scholar
  17. West, M. J., Kendall, M. J., Mitchard, M., Faragher, E. B.: A comparison of slow release with conventional oxprenolol: plasma concentrations and clinical effects. Br. J. clin. Pharmacol.3, 439–443 (1976)Google Scholar

Copyright information

© Springer-Verlag 1979

Authors and Affiliations

  • K. L. Woods
    • 1
  • S. P. Linton
    • 2
  • M. J. Kendall
    • 1
  • E. B. Faragher
    • 3
  • R. J. Grieve
    • 4
  1. 1.Department of Therapeutics and Clinical PharmacologyUniversity of BirminghamUnited Kingdom
  2. 2.Selly Oak HospitalBirminghamUnited Kingdom
  3. 3.Mathematical Analysis SectionGeigy PharmaceuticalsMacclesfieldUnited Kingdom
  4. 4.Department of MedicineUniversity of BirminghamUnited Kingdom

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