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Journal of pharmaceutical and biomedical analysis2004; 35(1); 107-116; doi: 10.1016/j.jpba.2003.12.007

Determination of xylazine and its metabolites by GC-MS in equine urine for doping analysis.

Abstract: Xylazine and its main metabolites were detected in equine urine after a single-dose intravenous administration of 0.98 and 1.01 mg/kg body weight xylazine, respectively, in two horses, in order to be used for equine doping control routine analysis. The urine levels of the parent drug and its metabolites were determined using gas chromatography-mass spectrometry (GC-MS). Xylazine is metabolised rapidly, down to a concentration level of about 1.0 microg/ml after 1-3h administration. Seven metabolites were identified in urine. 4-Hydroxy-xylazine, the major metabolite, could be traced for 25 h and it is regarded as the long-term metabolite of xylazine in horse. 2,6-Dimethylaniline was, for the first time, reported as metabolite in equine.
Publication Date: 2004-03-20 PubMed ID: 15030885DOI: 10.1016/j.jpba.2003.12.007Google Scholar: Lookup
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  • Journal Article

Summary

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This research explored the detection of xylazine and its metabolites in horse urine for doping control, using a method called gas chromatography-mass spectrometry (GC-MS). The substance xylazine was quickly metabolized following injection, and the main metabolite could be traced for up to 25 hours.

Detailed Explanation of the Research

  • The study investigated the detection and analysis of xylazine and its metabolites in equine urine. Xylazine is a drug used in veterinary medicine for sedation, analgesia, and muscle relaxation. In the context of horse racing, its use can be considered doping. Detecting the presence of this substance in an equine urine sample is thus important for maintaining the integrity of competitions.
  • For the purpose of this study, two horses were intravenously administered with a single dose of xylazine at each of two different weights (0.98 and 1.01 mg/kg). The urine concentrations of xylazine and its metabolites were then determined and analyzed with a technique called gas chromatography-mass spectrometry (GC-MS). This method is widely used in doping control analysis for its reliability and accuracy.
  • The research findings revealed that xylazine was rapidly metabolized in the horse’s body, reaching a concentration level of about 1.0 microgram/ml after 1-3 hours of administration. This means that the substance is eliminated from the body rather quickly, making its detection a time-sensitive matter.
  • Seven metabolites of xylazine were identified in the urine samples. The chief metabolite, known as 4-Hydroxy-xylazine, could be traced for up to 25 hours after administration. This makes it the longer-lasting metabolite of xylazine in horses and can be essential for detection during doping control.
  • Of significant note is the detection of 2,6-Dimethylaniline as a metabolite of xylazine in the equine for the first time. Additional research may be required to better understand the implications of this novel finding.

Cite This Article

APA
Spyridaki MH, Lyris E, Georgoulakis I, Kouretas D, Konstantinidou M, Georgakopoulos CG. (2004). Determination of xylazine and its metabolites by GC-MS in equine urine for doping analysis. J Pharm Biomed Anal, 35(1), 107-116. https://doi.org/10.1016/j.jpba.2003.12.007

Publication

ISSN: 0731-7085
NlmUniqueID: 8309336
Country: England
Language: English
Volume: 35
Issue: 1
Pages: 107-116

Researcher Affiliations

Spyridaki, M-H
  • Doping Control Laboratory of Athens, Olympic Athletic Center of Athens, Kifissias 37, 15123 Maroussi, Greece.
Lyris, E
    Georgoulakis, I
      Kouretas, D
        Konstantinidou, M
          Georgakopoulos, C G

            MeSH Terms

            • Adrenergic alpha-Agonists / metabolism
            • Adrenergic alpha-Agonists / urine
            • Animals
            • Doping in Sports
            • Female
            • Gas Chromatography-Mass Spectrometry
            • Horses / urine
            • Injections, Intravenous
            • Molecular Structure
            • Xylazine / metabolism
            • Xylazine / urine

            Citations

            This article has been cited 3 times.
            1. Saisahas K, Soleh A, Promsuwan K, Saichanapan J, Phonchai A, Sadiq NSM, Teoh WK, Chang KH, Abdullah AFL, Limbut W. Nanocoral-like Polyaniline-Modified Graphene-Based Electrochemical Paper-Based Analytical Device for a Portable Electrochemical Sensor for Xylazine Detection.. ACS Omega 2022 Apr 26;7(16):13913-13924.
              doi: 10.1021/acsomega.2c00295pubmed: 35559175google scholar: lookup
            2. Yuan M, Breitkopf SB, Asara JM. Serial-omics characterization of equine urine.. PLoS One 2017;12(10):e0186258.
              doi: 10.1371/journal.pone.0186258pubmed: 29028822google scholar: lookup
            3. Chen H, Wang H, Chen Y, Zhang H. Liquid chromatography-tandem mass spectrometry analysis of anisodamine and its phase I and II metabolites in rat urine.. J Chromatogr B Analyt Technol Biomed Life Sci 2005 Sep 25;824(1-2):21-9.
              doi: 10.1016/j.jchromb.2005.07.036pubmed: 16095983google scholar: lookup