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European Journal of Clinical Pharmacology

, Volume 50, Issue 4, pp 339–342 | Cite as

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

  • K. Stoschitzky
  • M. Schumacher
  • G. Stark
  • H.-P. Dimai
  • R. Stauber
  • P. Stoschitzky
  • G. J. Krejs
  • W. Klein
  • W. Lindner
PHARMACOKINETICS AND DISPOSITION

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 β-adrenoceptor blocking (S)-enantiomer directly at the synaptic gaps might be one reason for the poor correlation between plasma concentration and effect of β-adrenoceptor antagonists repeatedly described in the literature.

Key words Propranolol; stereoselectivity chirality enantiomers isomers 

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Copyright information

© Springer-Verlag Berlin Heidelberg 1996

Authors and Affiliations

  • K. Stoschitzky
    • 2
  • M. Schumacher
    • 2
  • G. Stark
    • 2
  • H.-P. Dimai
    • 2
  • R. Stauber
    • 2
  • P. Stoschitzky
    • 2
  • G. J. Krejs
    • 2
  • W. Klein
    • 2
  • W. Lindner
    • 1
  1. 1.Institute of Pharmaceutical Chemistry, Karl Franzens University, Graz, AustriaAT
  2. 2.Department of Medicine, Karl Franzens University, Auenbruggerplatz 15, A-8036 Graz, AustriaAT

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