Abstract
Bisoprolol is a new beta-adrenoceptor antagonist which has shown beta-adrenoceptor selectivity in studies in isolated tissues. Bronchial and cardiac beta-adrenoceptor blockade were assessed in eight normal subjects before and after oral ingestion of placebo, bisoprolol 20 and 40 mg, metoprolol 200 mg and propranolol 80 mg in random order. Bronchial beta-adrenoceptor blockade was assessed as the displacement of the bronchodilator dose-response curve to inhaled isoprenaline after each beta-adrenoceptor blocking drug compared to placebo and expressed as the dose ratio. Bronchodilatation was measured as change in specific airway conductance (sGaw) in the body plethysmograph. Cardiac beta-adrenoceptor blockade was assessed as the percentage reduction in exercise heart rate during the fifth minute of exercise at 70% of the subject's maximum work rate. Bisoprolol 20 and 40 mg caused a 24 and 25% reduction in exercise heart rate respectively, compared to 26% with metoprolol 200 mg and 20% with propranolol 80 mg. The dose ratios for the airway dose-response curves for the four beta-adrenoceptor blocking drugs were 1.04 and 3.4 for bisoprolol 20 and 40 mg, 1.4 for metoprolol 200 mg and 30 for propranolol 80 mg. Both doses of bisoprolol produced considerably less bronchial beta-adrenoceptor blockade than propranolol 80 mg despite causing a greater reduction in exercise heart rate. Bisoprolol 20 mg caused a similar amount of bronchial beta-adrenoceptor blockade and a similar reduction in exercise heart rate as metoprolol 200 mg, confirming that it is cardio-selective in man.
Full text
PDF
Selected References
These references are in PubMed. This may not be the complete list of references from this article.
- Gribbin H. R., Baldwin C. J., Tattersfield A. E. Quantitative assessment of bronchial beta-adrenoceptor blockade in man. Br J Clin Pharmacol. 1979 Jun;7(6):551–556. doi: 10.1111/j.1365-2125.1979.tb04641.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Gribbin H. R., Mackay A. D., Baldwin C. J., Tattersfield A. E. Bronchial and cardiac beta-adrenoceptor blockade--a comparison of atenolol, acebutolol and labetalol. Br J Clin Pharmacol. 1981 Jul;12(1):61–65. doi: 10.1111/j.1365-2125.1981.tb01855.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Harron D. W., Balnave K., Kinney C. D., Wilson R., Russell C. J., Shanks R. G. Effects on exercise tachycardia during forty-eight hours of a series of doses of atenolol, sotalol, and metoprolol. Clin Pharmacol Ther. 1981 Mar;29(3):295–302. doi: 10.1038/clpt.1981.39. [DOI] [PubMed] [Google Scholar]
- Kermode J. C., Edmonds C. J. Pathways of transepithelial potassium movement in the epithelium of distal colon in man. Clin Sci (Lond) 1980 Jul;59(1):29–39. doi: 10.1042/cs0590029. [DOI] [PubMed] [Google Scholar]
- Mackay A. D., Gribbin H. R., Baldwin C. J., Tattersfield A. E. Assessment of bronchial beta blockade after oral bevantolol. Clin Pharmacol Ther. 1981 Jan;29(1):1–6. doi: 10.1038/clpt.1981.1. [DOI] [PubMed] [Google Scholar]
- Manalan A. S., Besch H. R., Jr, Watanabe A. M. Characterization of [3H](+/-)carazolol binding to beta-adrenergic receptors. Application to study of beta-adrenergic receptor subtypes in canine ventricular myocardium and lung. Circ Res. 1981 Aug;49(2):326–336. doi: 10.1161/01.res.49.2.326. [DOI] [PubMed] [Google Scholar]
- Oh V. M., Kaye C. M., Warrington S. J., Taylor E. A., Wadsworth J. Studies of cardioselectivity and partial agonist activity in beta-adrenoceptor blockade comparing effects on heart rate and peak expiratory flow rate during exercise. Br J Clin Pharmacol. 1978 Feb;5(2):107–120. doi: 10.1111/j.1365-2125.1978.tb01609.x. [DOI] [PMC free article] [PubMed] [Google Scholar]