Abstract
The beta-adrenoceptor blocking effects of orally administered atenolol on tachycardia induced by intravenous isoprenaline or by exercise have been studied in normal volunteers, and compared with the effects of similar doses of propranolol. The blood levels of atenolol at various times after oral administration were determined by g.l.c. and correlated with the degree of inhibition of tachycardia. Atenolol was shown to be a beta-adrenoceptor blocker in man, as in animals, in that it antagonized the chronotropic effects of isoprenaline and of exercise. The inhibitory effect of atenolol on exercise-induced tachycardia was evident at a concentration in blood of 0.2 mug/ml and virtually complete at 0.5 mug/ml. Higher concentrations than this did not produce significantly greater blockade. The effects of atenolol on exercise-induced tachycardia were similar to those of propranolol but it was less effective in blocking the rise in heart rate and fall in diastolic blood-pressure induced by intravenous infusion of isoprenaline. This separation of effects is considered characteristic of drugs causing preferential blockade of cardiac beta-adrenoreceptors. The half-life of atenolol in blood was calculated to ablut 9 hours.
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Selected References
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- Barrett A. M., Carter J., Fitzgerald J. D., Hull R., Le Count D. A new type of cardioselective adrenoceptive blocking drug. Br J Pharmacol. 1973 Jun;48(2):340P–340P. [PMC free article] [PubMed] [Google Scholar]
- Hainsworth R., Karim F., Stoker J. B. Blockade of peripheral vascular responses to isoprenaline by three beta-adrenoceptor antagonists in the anaesthetized dog. Br J Pharmacol. 1974 Jun;51(2):161–168. doi: 10.1111/j.1476-5381.1974.tb09643.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Harry J. D., Knapp M. F., Linden R. J. The action of ICI-66082 on the heart. Br J Pharmacol. 1973 Jun;48(2):340P–341P. [PMC free article] [PubMed] [Google Scholar]
- Harry J. D., Knapp M. F., Linden R. J. The actions of a new beta-adrenoceptor blocking drug, ICI 66082, on the rabbit papillary muscle and on the dog heart. Br J Pharmacol. 1974 Jun;51(2):169–177. doi: 10.1111/j.1476-5381.1974.tb09644.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Scales B., Copsey P. B. The gas chromatographic determination of atenolol in biological samples. J Pharm Pharmacol. 1975 Jun;27(6):430–433. doi: 10.1111/j.2042-7158.1975.tb09473.x. [DOI] [PubMed] [Google Scholar]