Summary
Epanolol is a beta-adrenoceptor antagonist with partial agonist activity, a property which could be useful in reducing the fatigue associated with beta blockers. In a double-blind, randomized, crossover study we have investigated the effects of metoprolol 100 mg b.d., epanolol 100 mg b.d., and epanolol 200 mg b.d. on blood pressure, heart rate, and exercise-induced fatigue in 10 hypertensive men.
Fatigue was measured subjectively by the Borg rating scale and objectively by blood lactate concentrations.
Resting and exercise heart rates were lower with metoprolol than with either dose of epanolol. Preexercise standing diastolic blood pressure was lowered by metoprolol, but there were no other treatment effects on blood pressure. Exercise-induced fatigue was not altered by any treatment, whether measured subjectively or objectively.
These results do not support the hypothesis that partial agonist activity improves exercise tolerance in hypertensive patients treated with beta-adrenoceptor antagonists.
References
Norris SC, Harry JD, Young J, Sharman P (1984) Demonstrating the cardioselectivity of the beta adrenoceptor blocking agent ICI 141,292 in man. Br J Clin Pharmacol 18: 271P-272P
Pringle TH, O'Connor PG, McNeill AJ, Finch MB, Riddell JG, Shanks RG (1986) Effects of ICI 141, 292 on exercise tachycardia and isoprenaline-induced beta-adrenoceptor responses in man. Br J Clin Pharmacol 21: 249–258
Reid W, Ewing DJ, Harry JD, Smith HJ, Neilson JMM, Clarke BF (1986) Heart rate and physiological tremor after beta adrenoceptor blockade in diabetics with autonomic neuropathy. Br J Clin Pharmacol 21: 281p
Borg GAV (1982) Psychophysical bases of perceived exertion. Med Sci Sports Exerc 14 No. 5: 377–381
Norris SC, Harry JD, Smith HJ, Morton P Cook SK (1985) Does ISA alter subjective awareness of beta adrenoceptor blockade? Br J Clin Pharmacol 20: 242
Noll F (1974) L-(+)-Lactate. Determination with LDH, GPT and NAD. In: Bergmeyer HU (ed) Methods of enzymatic analysis, 2nd edk (Transl from 3rd German edn) Verlag Chemie, Weinheim Academic Press, New York London, p 1475
Dorow P (1982) Effects of beta-adrenoceptor blockade on carbohydrate metabolism during exercise-comparison of pindolol and metoprolol. Br J Clin Pharmacol 13: 429–430
Laustiola K, Uusitalo A, Koivula T, Sovijarvi A, Seppala E, Nikkari T, Vapaatalo H (1983) Divergent effects of atenolol, practolol and propranolol on the peripheral metabolic changes induced by dynamic exercise in men. Eur J Clin Pharmacol 25: 293–297
Author information
Authors and Affiliations
Rights and permissions
About this article
Cite this article
Lees, K.R., Curzio, J., Farish, E. et al. The influence of beta-adrenoceptor antagonists with and without partial agonist activity on exercise tolerance and muscle lactate production. Eur J Clin Pharmacol 33, 415–417 (1987). https://doi.org/10.1007/BF00637640
Received:
Accepted:
Issue Date:
DOI: https://doi.org/10.1007/BF00637640