Beta-blocking effect and serum levels of alprenolol in man after administration of ordinary and sustained release tablets
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The effect of alprenolol administered as ordinary and as sustained release tablets was compared by studies on the inhibition of the haemodynamic response to physical work. Serum levels of alprenolol were also determined. Two types of double-blind cross-over studies were performed in healthy volunteers. In one the effects of ordinary tablets, sustained release tablets and a placebo were followed for 12 h. In two other studies each preparation was given for five days. The sustained release tablets were given b.i.d., and were compared with ordinary tablets administered q.i.d., or with a placebo. A dose of 200 mg alprenolol in sustained release tablets had almost the same initial peak effect as 100 mg in ordinary tablets. The duration of the effect was longer after the sustained release tablets, and 200 mg b.i.d. gave approximately the same degree of beta-blockade during the day as 100 mg in ordinary tablets given q.i.d. The results indicated that both dosage regimens had an effect for 24 h, and that more constantive effect levels were obtained by the use of sustained release tablets. No accumulation was found in the five day study, neither in terms of the pharmacological effects nor of serum levels of alprenolol. The concentration of alprenolol in serum rarely exceeded 10 ng per ml, and approximately the same steady state level was obtained after sustained release tablets as after ordinary tablets.
Key-wordsSerum levels β-blockade alprenolol sustained release tablets and man
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- 1.Åblad, B., Johnsson, G., Norrby, A., Sölvell, L.: Potency and time-effect relationship in man of propranolol and H 56/28 — comparative studies after oral administration. Acta Pharmacol. et Toxicol.25, Suppl. 2, 85–94 (1967).Google Scholar
- 2.-- Ervik, M., Hallgren, J., Johnsson, G., Sölvell, L.: Pharmacological effects and plasma levels of orally administered alprenolol in man. To be published 1971.Google Scholar
- 3.Björntorp, P.: Treatment of angina pectoris with beta-receptor blocking agents. Effects of long-term treatment and treatment with sustained release tablets. Acta Med. In press.Google Scholar
- 4.Dollery, C.T., Paterson, J.Kl., Conelly, M.E.: Clinical pharmacology of beta-receptor blocking drugs. Clin. pharmacol. Ther.10, 765–769 (1969).Google Scholar
- 5.Ervik, M.: Gas chromatographic determination of the secondary amine alprenolol, as its trifluoroacetyl derivative, at nanogram levels in biological fluids. Acta Pharm. Suecica6, 393–400 (1969).Google Scholar
- 6.Johansson, R., Regårdh, C., Sjögren, J.: Absorption of alprenolol in man from tablets with different rate of release. Acta Pharm. Suecica. In press.Google Scholar
- 7.Johnsson, G., Norrby, A., Sölvell, L.: Potency and time-effect relationship in man of propranolol and H 56/28. Acta Pharmacol. et Toxicol.25, Suppl. 2, 95–105 (1967).Google Scholar
- 8.Robinson, B. F., Epstein, S. E., Beisa, G. D., Braunwald, E.: Control of heart rate by the autonomic nervous system. Circulation Res.19, 410–411 (1966).Google Scholar