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Beta2-Agonist Doping Control and Optical Isomer Challenges.
Sports Med. 2016 Dec; 46(12):1787-1795.SM

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.

Authors+Show Affiliations

School of Medicine, University of Tasmania, Private Bag 26, Hobart, TAS, 7001, Australia. glenn.jacobson@utas.edu.au.School of Pharmacy, University of Otago, Dunedin, New Zealand.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

27164986

Citation

Jacobson, Glenn A., and J Paul Fawcett. "Beta2-Agonist Doping Control and Optical Isomer Challenges." Sports Medicine (Auckland, N.Z.), vol. 46, no. 12, 2016, pp. 1787-1795.
Jacobson GA, Fawcett JP. Beta2-Agonist Doping Control and Optical Isomer Challenges. Sports Med. 2016;46(12):1787-1795.
Jacobson, G. A., & Fawcett, J. P. (2016). Beta2-Agonist Doping Control and Optical Isomer Challenges. Sports Medicine (Auckland, N.Z.), 46(12), 1787-1795. https://doi.org/10.1007/s40279-016-0547-4
Jacobson GA, Fawcett JP. Beta2-Agonist Doping Control and Optical Isomer Challenges. Sports Med. 2016;46(12):1787-1795. PubMed PMID: 27164986.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Beta2-Agonist Doping Control and Optical Isomer Challenges. AU - Jacobson,Glenn A, AU - Fawcett,J Paul, PY - 2016/5/12/pubmed PY - 2018/5/4/medline PY - 2016/5/12/entrez SP - 1787 EP - 1795 JF - Sports medicine (Auckland, N.Z.) JO - Sports Med VL - 46 IS - 12 N2 - 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. SN - 1179-2035 UR - https://www.unboundmedicine.com/medline/citation/27164986/Beta2_Agonist_Doping_Control_and_Optical_Isomer_Challenges_ L2 - https://dx.doi.org/10.1007/s40279-016-0547-4 DB - PRIME DP - Unbound Medicine ER -