Budesonide use and misuse in sports: Elimination profiles of budesonide and metabolites after intranasal, high-dose inhaled and oral administrations

Budesonide use and misuse in sports: Elimination profiles of budesonide and metabolites after intranasal, high-dose inhaled and oral administrations / Sergi Coll, Núria Monfort, Xavier Matabosch, Katerina Papakonstantinou, Clara Pérez-Mañá, Julian A. Mateus, Rosa Ventura. - (Drug Testing and Analysis 12 (2020) 5 (May); p. 629-636)

  • PMID: 31306564
  • DOI: 10.1002/dta.2678


Abstract

Budesonide (BUD) is a glucocorticoid (GC) widely used in therapeutics. In sports, the World Anti-doping Agency (WADA) controls the use of GCs, and WADA-accredited laboratories use a reporting level of 30 ng/mL for 6β-hydroxy-budesonide (6βOHBUD) to detect the systemic administration of BUD. In the present work, we examined the urinary excretion profile of 6βOHBUD, BUD, and 16α-hydroxy-prednisolone (16αOHPRED) after intranasal (INT), inhaled (INH) (at high doses) and oral administrations in male and female volunteers. BUD was administered to healthy volunteers using INT route (256 μg/day for three days, n = 4 males and 4 females), INH route (800 μg/day for three days, n = 4 males and 4 females, and 1600 μg/day for three days, n = 4 males) or oral route (3 mg, n = 8 females). Urine samples were collected before and after administration at different time periods, and were analyzed by liquid chromatography-tandem mass spectrometry. 6βOHBUD and BUD concentrations were very low after INT treatment (0.0-7.1 and 0.0-8.1 ng/mL, respectively), and higher after INH treatments (0.0-35.4 and 0.0-48.3 ng/mL, respectively). For 16αOHPRED, elevated concentrations were detected after INT and INH treatments (2.6-66.4 and 3.4-426.5 ng/mL, respectively). Concentrations obtained following oral administration were higher than after therapeutic administrations (2.8-80.6, 1.5-36.1, and 10.4-532.2 ng/mL for 6βOHBUD, BUD, and 16αOHPRED, respectively). After all administrations, concentrations were higher in males than in females. Results demonstrated that 6βOHBUD is the best discriminatory marker and a reporting level of 40 ng/mL was found to be the best criterion to distinguish allowed from forbidden administrations of BUD.

Parameters

Science
Study
Date
2 December 2019
People
Coll, Sergi
Matabosch, Xavier
Mateus, Julian A.
Monfort, N.
Papakonstantinou, Katerina
Pérez-Mañá, Clara
Ventura, Rosa
Country
Spain
Language
English
Other organisations
Institut d'Investigació en Ciencies de la Salut Germans Trias i Pujol (IGTP) - The Institute for Health Science Research Germans Trias i Pujol
Institut Hospital de Mar d'Investigacions Mèdiques (IMIM) - Hospital del Mar Medical Research Institute
Universitat Autònoma de Barcelona (UAB) - Autonomous University of BarcelonaUniversitat Autònoma de Barcelona
Universitat Pompeu Fabra (UPF) - Pompeu Fabra University
Doping classes
S9. Glucocorticosteroids
Substances
Budesonide
Document type
Pdf file
Date generated
15 March 2021
Category
  • Legal Source
  • Education
  • Science
  • Statistics
  • History
Country & language
  • Country
  • Language
Other filters
  • ADRV
  • Legal Terms
  • Sport/IFs
  • Other organisations
  • Laboratories
  • Analytical aspects
  • Doping classes
  • Substances
  • Medical terms
  • Various
  • Version
  • Document category
  • Document type
Publication period
Origin