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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%). CONCLUSIONS 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.
K Stoschitzky, and
M Schumacher, and
G Stark, and
H P Dimai, and
R Stauber, and
P Stoschitzky, and
G J Krejs, and
W Klein, and
W Lindner
March 2002,
Cardiovascular drugs and therapy,
K Stoschitzky, and
M Schumacher, and
G Stark, and
H P Dimai, and
R Stauber, and
P Stoschitzky, and
G J Krejs, and
W Klein, and
W Lindner
April 1992,
Clinical pharmacology and therapeutics,
K Stoschitzky, and
M Schumacher, and
G Stark, and
H P Dimai, and
R Stauber, and
P Stoschitzky, and
G J Krejs, and
W Klein, and
W Lindner
June 2003,
Journal of clinical pharmacy and therapeutics,
K Stoschitzky, and
M Schumacher, and
G Stark, and
H P Dimai, and
R Stauber, and
P Stoschitzky, and
G J Krejs, and
W Klein, and
W Lindner
April 1980,
Biological psychiatry,
K Stoschitzky, and
M Schumacher, and
G Stark, and
H P Dimai, and
R Stauber, and
P Stoschitzky, and
G J Krejs, and
W Klein, and
W Lindner
April 1981,
Life sciences,
K Stoschitzky, and
M Schumacher, and
G Stark, and
H P Dimai, and
R Stauber, and
P Stoschitzky, and
G J Krejs, and
W Klein, and
W Lindner
December 1981,
Drug intelligence & clinical pharmacy,
K Stoschitzky, and
M Schumacher, and
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H P Dimai, and
R Stauber, and
P Stoschitzky, and
G J Krejs, and
W Klein, and
W Lindner
December 2013,
Drug and alcohol dependence,
K Stoschitzky, and
M Schumacher, and
G Stark, and
H P Dimai, and
R Stauber, and
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G J Krejs, and
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W Lindner
November 2007,
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences,
K Stoschitzky, and
M Schumacher, and
G Stark, and
H P Dimai, and
R Stauber, and
P Stoschitzky, and
G J Krejs, and
W Klein, and
W Lindner
January 1989,
Chirality,
K Stoschitzky, and
M Schumacher, and
G Stark, and
H P Dimai, and
R Stauber, and
P Stoschitzky, and
G J Krejs, and
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W Lindner
December 1994,
Journal of pharmaceutical and biomedical analysis,
