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Exercise increases plasma concentrations of (R)- and (S)-propranolol (1996)

Stoschitzky, K. ; Schumacher, M. ; Stark, G. ; [et al.]

Springer

European journal of clinical pharmacology 50 (1996), S. 339-342

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ISSN: 1432-1041

Keywords: Key words Propranolol; stereoselectivity ; chirality ; enantiomers ; isomers

Source: Springer Online Journal Archives 1860-2000

Topics: Chemistry and Pharmacology , Medicine

Notes: 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.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/s002280050119

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Pharmacokinetic data of propranolol enantiomers in a comparative human study with (S)- and (R,S)-propranolol (1989)

Lindner, W. ; Rath, M. ; Stoschitzky, K. ; [et al.]

New York, NY [u.a.] : Wiley-Blackwell

Chirality 1 (1989), S. 10-13

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ISSN: 0899-0042

Keywords: (S)-, (R,S)-propranolol ; pharmacokinetic ; human study ; Chemistry ; Organic Chemistry

Source: Wiley InterScience Backfile Collection 1832-2000

Topics: Chemistry and Pharmacology

Notes: The pharmacokinetics of (S)-propranolol were compared after the oral administration of a 40 mg dose of the pure enantiomer and an 80 mg dose of a racemic mixture of (R,S)-propranolol. The results of this study indicate that the bioavailability of (S)-propranolol, as expressed by the mean area uner the concentration-time curve (AUC) and maximum serum concentration, is lower after 40mg of the optically pure drug than after the racemic drug.

Additional Material: 2 Ill.