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Beta2-agonist doping control and optical isomer challenges
journal contribution
posted on 2023-05-18, 19:40 authored by Glenn JacobsonGlenn Jacobson, Fawcett, JPThe 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.
History
Publication title
Sports MedicineVolume
46Issue
12Pagination
1787-1795ISSN
0112-1642Department/School
School of Pharmacy and PharmacologyPublisher
Adis International LtdPlace of publication
New ZealandRights statement
Copyright 2016 Springer International Publishing SwitzerlandRepository Status
- Restricted