Summary
1.) Circulatory effects of standard commercial and two slow-release preparations of oxprenolol, each containing 80 mg were compared with placebo in a double-blind randomized cross-over study in six normal subjects. 2.) After both slow-release preparations, the concentration of oxprenolol in blood was significantly less at one hour but significantly greater at 4, 8 and 12 hours than after the standard preparation. Variability of blood oxprenolol concentration between individuals was similar after all three formulations. 3.) Blood oxprenolol concentration was linearly related to the suppression of isoprenaline tachycardia and logarithmically related to the reduction in maximum exercise heart rate. 4.) The reduced maximum, but more sustained, blood oxprenolol concentration after the slow release preparations had no significant effect on the reduction of exercise tachycardia at one hour but significantly extended the duration of its activity compared with the commercial preparation. 5.) These results indicate that the pharmacological activity of beta-adrenoceptor antagonists with a relatively short duration of action may be usefully extended by slow-release formulation.
Similar content being viewed by others
References
Davidson, C., Singleton, W., Thadani, U., Taylor, S.H.: Comparison of antihypertensive activity of beta-adrenoceptor antagonists. In: Hypertension — its nature and treatment. (eds. D.M. Burley, G.F.B. Birdwood, J.H. Fryer and S.H. Taylor) Horsham, England: Ciba Publications 1975
Dollery, C.T., Paterson, J.W., Conolly, M.E.: Clinical pharmacology of beta-receptor blocking drugs. Clin. Pharmacol. Ther.10, 765–799 (1969)
Coltart, D.J., Shand, D.G.: Plasma propranolol levels in the quantitative assessment of beta-adrenergic blockade in man. Brit. med. J.3, 731–734 (1970)
Jack, D.B., Riess, W.: Determination of low levels of oxprenolol in blood or plasma by gas-liquid chromatography. J. Chromatography88, 173–176 (1974)
Robinson, B.F.: The mode of action of beta-antagonists in angina pectoris. Postgrad. med. J. Suppl.47, 41–43 (1971)
Robinson, S., Pearcy, M., Brineckman, F.R., Nicholas, J.H., Miller, D.I.: Effects of atropine on heart rate and oxygen uptake in working man. J. appl. Physiol.5, 508–512 (1953)
Sharma, B., Meeran, M.K., Galvin, M.C., Tulpule, A.T., Whitaker, W., Taylor, S.H.: Comparison of adrenergic beta-blocking drugs in angina pectoris. Brit. med. J.1970 III, 152–155
Taggart, P., Carruthers, M.: Suppression by oxprenolol of adrenergic response to stress. Lancet1972 II, 256–258
Taylor, S.H.: Mechanism of action of adrenergic beta-receptor antagonists in angina pectoris (eds. D.M. Burley, J.H. Fryer, R.K. Rondel, S.H. Taylor) Horsham, England: Ciba Publications 1973
Taylor, S.H.: The circulation in hypertension. In: Hypertension — its nature and treatment (eds. D.M. Burley, G.F.B. Birdwood, J.H. Fryer, S.H. Taylor) Horsham, England: Ciba Publications 1975
Taylor, S.H., Meeran, M.K.: Different effects of adrenergic beta-receptor blockade on the heart rate response to mental stress, catecholamines and exercise. Brit. med. J.1973aIV, 257–259
Taylor, S.H., Meeran, M.K.: Cardiovascular response to some environmental stresses and their modification by oxprenolol. In: New perspectives in beta-blockade (eds. D.M. Burley, J.H. Fryer, R.K. Rondel, S.H. Taylor) Horsham, England: Ciba Publications 1973b
Taylor, S.H., Pearson, M.C., Myint, S.: Circulatory and metabolic effects of cigarette smoking and their attenuation by tobacco substitute or beta-adrenoceptor bockade. Quart. J. Med.43, 617 (1974)
Thadani, U., Sharma, B., Meeran, M.K., Majid, P.A., Whitaker, W., Taylor, S.H.: Comparison of adrenergic beta-receptor antagonists in angina pectoris. Brit. med. J.1973 I, 138–142
Thadani, U., Davidson, C., Singleton, W., Taylor, S.H.: Comparative activity of beta-adrenoceptor antagonists in man. Brit. J. clin. Pharmacol. In press 1976
Author information
Authors and Affiliations
Rights and permissions
About this article
Cite this article
Davidson, C., Thadani, U., Taylor, S.H. et al. Pharmacological studies with slow-release formulations of oxprenolol in man. Eur J Clin Pharmacol 10, 189–195 (1976). https://doi.org/10.1007/BF00558328
Received:
Revised:
Accepted:
Issue Date:
DOI: https://doi.org/10.1007/BF00558328