Evaluation of the beta-adrenoceptor blocking activity of the Class Ic antiarrhythmic drug diprafenone in man.

Abstract:

:The beta-adrenoceptor blocking activity of the new Class Ic-antiarrhythmic drug diprafenone has been determined in man in comparison with that of propranolol, using the standardized isoproterenol test. Following placebo, the dose of isoproterenol which increased the heart rate by 25 beats.min-1 (CD25) was 0.84 (0.1-2.72) micrograms (median and range). Two hours following single oral doses of 200 mg diprafenone (3.61 micrograms; 1.53-44.15) or 40 mg propranolol (16.06 micrograms; 9.15-27.04) significantly higher CD25-values were found. The affinity constants for the beta-adrenergic receptors calculated on the basis of free drug in the plasma were similar for propranolol and diprafenone (2.79 vs. 2.60 nM-1, respectively). Thus, diprafenone showed a definite degree of beta-blocking activity in a clinically relevant range of plasma concentrations.

journal_name

Eur J Clin Pharmacol

authors

Wagner F,Jähnchen E,Trenk D

doi

10.1007/BF00637739

subject

Has Abstract

pub_date

1989-01-01 00:00:00

pages

579-82

issue

6

eissn

0031-6970

issn

1432-1041

journal_volume

36

pub_type

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