The salmeterol anomaly and the need for a urine threshold
journal contributionposted on 2023-05-20, 14:04 authored by Glenn JacobsonGlenn Jacobson, Hostrup, M
Salmeterol is a long acting beta2-agonist (LABA) widely used for treatment of airways disease. There is evidence that beta2-agonists, including salmeterol, have the potential for performance enhancing effects when delivered at supratherapeutic doses. For this reason, all beta2-agonists are currently on the Prohibited List issued by the World Anti-Doping Agency (WADA) regardless of dosing route with some exemptions for inhaled salbutamol, formoterol, and salmeterol when used at therapeutic inhaled doses. For 2020, salmeterol use is permitted up to a therapeutic dosing threshold of 200 μg daily, but unlike salbutamol and formoterol, there is an anomaly; currently there is no urine threshold to control for supratherapeutic dosing beyond this dosing threshold. Salmeterol, however, is reportable as an Adverse Analytical Finding (AAF) at levels above 10 ng/ml. Complicating matters is that following inhalation, salmeterol parent drug is present at relatively low levels compared to other beta2-agonists due to rapid metabolism to the metabolite, alpha-hydroxysalmeterol, which is typically present at higher levels than parent drug. Moreover, peak parent drug levels following permitted therapeutic dosing are below the minimum required performance level (MRPL) of 10 ng/ml for salmeterol (50% of the MRPL that analytical laboratories are required to meet for non-threshold beta2-agonists), hence the presence of salmeterol may be unreported. For consistency, a urine threshold should be introduced for salmeterol as matter of priority, to balance the needs of athletes that use salmeterol therapeutically up to the agreed dosing threshold, with the need to control supratherapeutic dosing for doping intentions and athlete harm minimisation.
Publication titleDrug Testing and Analysis
Department/SchoolSchool of Pharmacy and Pharmacology
PublisherJohn Wiley & Sons
Place of publicationUnited Kingdom
Rights statementCopyright 2020 John Wiley & Sons, Ltd. This is the peer reviewed version of the following article, which has been published in final form at http://dx.doi.org/10.1002/dta.2810. This article may be used for non-commercial purposes in accordance with Wiley Terms and Conditions for Use of Self-Archived Versions.