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Beta2-agonist doping control and optical isomer challenges

Citation

Jacobson, GA and Fawcett, JP, Beta2-agonist doping control and optical isomer challenges, Sports Medicine, 46, (12) pp. 1787-1795. ISSN 0112-1642 (2016) [Refereed Article]

Copyright Statement

Copyright 2016 Springer International Publishing Switzerland

DOI: doi:10.1007/s40279-016-0547-4

Abstract

The World Anti-Doping Agency (WADA) currently allows therapeutic use of the beta2-agonists salbutamol, formoterol and salmeterol when delivered via inhalation despite some evidence suggesting these anti-asthma drugs may be performance enhancing. Beta2-agonists are usually administered as 50:50 racemic mixtures of two enantiomers (non-superimposable mirror images), one of which demonstrates significant beta2-adrenoceptor-mediated bronchodilation while the other appears to have little or no pharmacological activity. For salbutamol and formoterol, urine thresholds have been adopted to limit supratherapeutic dosing and to discriminate between inhaled (permitted) and oral (prohibited) use. However, chiral switches have led to the availability of enantiopure (active enantiomer only) preparations of salbutamol and formoterol, which effectively doubles their urine thresholds and provides a means for athletes to take supratherapeutic doses for doping purposes. Given the availability of these enantiopure beta2-agonists, the analysis of these drugs using enantioselective assays should now become routine. For salmeterol, there is currently only a therapeutic dose threshold and adoption of a urinary threshold should be a high priority for doping control.

Item Details

Item Type:Refereed Article
Keywords:beta2-agonist, doping, asthma, pharmacokinetics
Research Division:Medical and Health Sciences
Research Group:Pharmacology and Pharmaceutical Sciences
Research Field:Pharmaceutical Sciences
Objective Division:Health
Objective Group:Other Health
Objective Field:Health not elsewhere classified
Author:Jacobson, GA (Dr Glenn Jacobson)
ID Code:109142
Year Published:2016
Web of Science® Times Cited:2
Deposited By:Pharmacy
Deposited On:2016-05-27
Last Modified:2017-11-07
Downloads:0

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