PMID: 7981009Aug 1, 1994Paper

The effects of lower than conventional doses of oral nadolol on relative beta 1/beta 2-adrenoceptor blockade

British Journal of Clinical Pharmacology
N M WheeldonB J Lipworth

Abstract

1. The aim of the present study was to evaluate the relative beta 1/beta 2 antagonist selectivity of the beta-adrenoceptor blocker nadolol, in lower than conventional clinical doses. 2. Eight normal volunteers received single oral doses of either placebo (PL), nadolol 5 mg (N5), 20 mg (N20) or 80 mg (N80) in a single-blind, randomised crossover design. beta 1-adrenoceptor antagonism was assessed by attenuation of exercise tachycardia, and beta 2-adrenoceptor blockade by effects on salbutamol-induced chronotropic, hypokalaemic and finger tremor responses. The relative percentage attenuation of beta 2 and beta 1-mediated responses was calculated and expressed as beta 2:beta 1 selectivity ratios. 3. Nadolol produced dose-related reductions in exercise tachycardia in keeping with increasing beta 1-adrenoceptor blockade; mean % reduction (95% CI) compared with placebo: N5 10.7 (6.6 to 14.8), N20 21.4 (17.3 to 25.4), N80 38.9 (34.8 to 42.9). However, even the lowest dose of nadolol (5 mg) produced almost complete blunting of beta 2-mediated effects and significantly increase exercise hyperkalaemia; peak exercise hyperkalaemia (mmol l-1) (means and 95% CI): PL 4.88 (4.68 to 5.07), N5 5.36 (5.17 to 5.55), N20 5.48 (5.28 to 5.67), N80 5...Continue Reading

References

May 1, 1977·Clinical Pharmacology and Therapeutics·D G McDevittR G Shanks
Oct 1, 1992·British Journal of Clinical Pharmacology·N M WheeldonB J Lipworth
Apr 1, 1992·British Journal of Clinical Pharmacology·N M WheeldonB J Lipworth
Jul 1, 1990·British Journal of Clinical Pharmacology·N A IrvineD G McDevitt
Jan 1, 1989·European Journal of Clinical Pharmacology·B J Lipworth, D G McDevitt
Jan 1, 1989·European Journal of Clinical Pharmacology·B J LipworthD G McDevitt
Mar 28, 1985·The New England Journal of Medicine·M E WilliamsF H Epstein
May 1, 1983·Journal of Cardiovascular Pharmacology·A J BilskiJ L Wale
Dec 1, 1976·British Journal of Clinical Pharmacology·S G CarruthersD G McDevitt

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Citations

Nov 15, 2011·British Journal of Clinical Pharmacology·Philip M ShortBrian J Lipworth
Oct 8, 2009·Clinical Science·Brian J Lipworth, Peter A Williamson
Nov 1, 1995·Thorax·R E Jonkers, R P Koopmans
Mar 28, 1998·British Journal of Clinical Pharmacology·A H AbdelmawlaC M Bradshaw

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