Exercise increases plasma concentrations of (R)- and (S)-propranolol.

Abstract:

OBJECTIVE:We recently reported a highly stereoselective increase in plasma concentrations of (S)-atenolol during exercise which is most likely due to a release of the drug from adrenergic cells. The objective of the present study was to investigate the influence of physical exercise on plasma concentrations of the (R)- and (S)-enantiomers of propranolol. METHODS:Blood samples were taken immediately before and at the end of exercise in 12 patients receiving chronic treatment with racemic (R, S)-propranolol. Plasma concentrations of (R)- and (S)-propranolol were determined by HPLC. RESULTS:In contrast to atenolol, mean plasma concentrations of (S)-propranolol were significantly higher (+20%) than those of (R)-propranolol at rest. During exercise there was an increase in plasma concentrations of both (R)-propranolol (+129%) and (S)-propranolol (+109%). CONCLUSION:Based on information from in vitro studies we conclude that the increase in plasma concentrations of (S)-propranolol during exercise is caused by a release of the drug from adrenergic nerves, whereas the reason for the increase in (R)-propranolol remains to be determined. This release of the beta-adrenoceptor blocking (S)-enantiomer directly at the synaptic gaps might be one reason for the poor correlation between plasma concentration and effect of beta-adrenoceptor antagonists repeatedly described in the literature.

journal_name

Eur J Clin Pharmacol

authors

Stoschitzky K,Schumacher M,Stark G,Dimai HP,Stauber R,Stoschitzky P,Krejs GJ,Klein W,Lindner W

doi

10.1007/s002280050119

subject

Has Abstract

pub_date

1996-01-01 00:00:00

pages

339-42

issue

4

eissn

0031-6970

issn

1432-1041

journal_volume

50

pub_type

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