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Penbutolol and propranolol: a comparison of their effects on antipyrine clearance in man.
Author(s) -
Bax ND,
Jones RW,
Lennard MS,
Tucker GT,
Woods HF
Publication year - 1985
Publication title -
british journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.216
H-Index - 146
eISSN - 1365-2125
pISSN - 0306-5251
DOI - 10.1111/j.1365-2125.1985.tb02685.x
Subject(s) - propranolol , chemistry , pharmacology , potency , distribution (mathematics) , antagonist , endocrinology , beta (programming language) , medicine , volume of distribution , metabolism , pharmacokinetics , in vitro , receptor , biochemistry , mathematical analysis , mathematics , computer science , programming language
The effects of two beta‐adrenoceptor antagonists, penbutolol (administered on separate occasions as (+/‐)‐ and (‐)‐forms) and propranolol, on the kinetics of antipyrine were studied in eight normal subjects. At the same degree of beta‐adrenoceptor blockade, as assessed by the lowering of exercise tachycardia, propranolol decreased antipyrine clearance by 31 +/‐ 11 s.d.% (P less than 0.001) whereas neither of the two penbutolol formulations had a significant effect. The volume of distribution of antipyrine was unchanged following any of the beta‐adrenoceptor antagonist treatments. The lack of effect of penbutolol on oxidative drug metabolism is not consistent with in vitro data suggesting a relationship between the lipid solubility of beta‐ adrenoceptor antagonists and inhibition of metabolism.