Medizinische Universität Graz - Research portal
Selected Publication:
Stoschitzky, K; Schumacher, M; Stark, G; Dimai, HP; Stauber, R; Stoschitzky, P; Krejs, GJ; Klein, W; Lindner, W.
Exercise increases plasma concentrations of (R)- and (S)-propranolol.
Eur J Clin Pharmacol. 1996; 50(4):339-342
Doi: 10.1007/s002280050119
Web of Science
PubMed
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- Leading authors Med Uni Graz
- Stoschitzky Kurt
- Co-authors Med Uni Graz
- Dimai Hans Peter
- Krejs Günter Josef
- Schumacher Martin
- Stauber Rudolf
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- 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.
- Find related publications in this database (using NLM MeSH Indexing)
- Adrenergic beta-Antagonists - blood
- Adult -
- Aged -
- Analysis of Variance -
- Blood Pressure - drug effects
- Exercise - physiology
- Female -
- Heart Rate - drug effects
- Humans -
- Male -
- Middle Aged -
- Molecular Conformation -
- Propranolol - blood
- Stereoisomerism -
- Find related publications in this database (Keywords)
- Propranolol
- Stereoselectivity
- Chirality
- Enantiomers
- Isomers