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Identification of lidocaine and its metabolites in post-administration equine urine by ELISA and MS/MS.

Abstract: Lidocaine is a local anesthetic drug that is widely used in equine medicine. It has the advantage of giving good local anesthesia and a longer duration of action than procaine. Although approved for use in horses in training by the American Association of Equine Practitioners (AAEP), lidocaine is also an Association of Racing Commissioners International (ARCI) Class 2 drug and its detection in forensic samples can result in significant penalties. Lidocaine was observed as a monoprotonated ion at m/z 235 by ESI+ MS/MS (electrospray ionization-positive ion mode) analysis. The base peak ion at m/z 86, representing the postulated methylenediethylamino fragment [CH2N(CH2CH3)2]+, was characteristic of lidocaine and 3-hydroxylidocaine in both ESI+ and EI (electron impact-positive ion mode) mass spectrometry. In addition, we identified an ion at m/z 427 as the principal parent ion of the ion at m/z 86, consistent with the presence of a protonated analog of 3-hydroxylidocaine-glucuronide. We also sought to establish post-administration ELISA-based 'detection times' for lidocaine and lidocaine-related compounds in urine following single subcutaneous injections of various doses (10, 40, 400 mg). Our findings suggest relatively long ELISA based 'detection times' for lidocaine following higher doses of this drug.
Publication Date: 2000-12-07 PubMed ID: 11106996
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  • Journal Article
  • Research Support
  • Non-U.S. Gov't

Summary

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This research discusses how lidocaine, a local anesthetic used in horse medicine, was identified in equine urine following administration. It also explores the detection times for lidocaine and associated compounds following different dosages in an attempt to enhance testing protocols.

What Lidocaine Is

  • Lidocaine is a local anesthetic often used in equine medicine, and it provides a longer-lasting effect than another anesthetic called procaine.
  • While the American Association of Equine Practitioners (AAEP) authorizes its use, it is classified as a Class 2 drug by the Association of Racing Commissioners International (ARCI). If lidocaine is discovered in racing horses, this could lead to major penalties.

Methodology and Discovery

  • Researchers found lidocaine as a monoprotonated ion at m/z 235 during their ESI+ MS/MS (Electrospray Ionization-Positive Ion Mode) analysis.
  • They recognized a base peak ion at m/z 86, which represented the proposed methylenediethylamino fragment [CH2N(CH2CH3)2]+, as a signature of lidocaine and 3-hydroxylidocaine in both ESI+ and EI (Electron Impact-Positive Ion Mode) mass spectrometry examinations.
  • Also, they pinpointed an ion at m/z 427 as the primary parent ion of the ion at m/z 86, which is in line with the existence of a protonated analog of 3-hydroxylidocaine-glucuronide.

Establishing Detection Times

  • Afterward, the team worked to set post-administration ELISA-based (Enzyme-Linked Immunosorbent Assay) ‘detection times’ for lidocaine and related compounds in urine samples after single subcutaneous injections of various doses (10, 40, 400 mg).
  • It was observed that higher doses of lidocaine resulted in longer ELISA-based detection times, indicating the drug’s presence could be detected over an extended period when larger amounts were administered.

Significance of the Study

  • This research aids in the identification of lidocaine in equine urine following administration, which could help in ensuring fair practices in horse racing.
  • Furthermore, setting detection times would contribute to developing more effective testing protocols for lidocaine and similar substances, refining the drug testing process in the equine sports industry.

Cite This Article

APA
Dirikolu L, Lehner AF, Karpiesiuk W, Harkins JD, Woods WE, Carter WG, Boyles J, Fisher M, Tobin T. (2000). Identification of lidocaine and its metabolites in post-administration equine urine by ELISA and MS/MS. J Vet Pharmacol Ther, 23(4), 215-222.

Publication

ISSN: 0140-7783
NlmUniqueID: 7910920
Country: England
Language: English
Volume: 23
Issue: 4
Pages: 215-222

Researcher Affiliations

Dirikolu, L
  • Maxwell H. Gluck Equine Research Center and the Department of Veterinary Science, University of Kentucky, Lexington 40506, USA.
Lehner, A F
    Karpiesiuk, W
      Harkins, J D
        Woods, W E
          Carter, W G
            Boyles, J
              Fisher, M
                Tobin, T

                  MeSH Terms

                  • Anesthetics, Local / administration & dosage
                  • Anesthetics, Local / pharmacokinetics
                  • Anesthetics, Local / urine
                  • Animals
                  • Dose-Response Relationship, Drug
                  • Enzyme-Linked Immunosorbent Assay / standards
                  • Enzyme-Linked Immunosorbent Assay / veterinary
                  • Female
                  • Horses / metabolism
                  • Injections, Subcutaneous / veterinary
                  • Lidocaine / administration & dosage
                  • Lidocaine / pharmacokinetics
                  • Lidocaine / urine
                  • Mass Spectrometry / standards
                  • Mass Spectrometry / veterinary
                  • Substance Abuse Detection / veterinary

                  Citations

                  This article has been cited 1 times.
                  1. Wang Y, Ou-Yang QG, Huang WL, Huang HL, Zhuang XL, Lin QM, Zeng DL. Investigation of the Inhibitory Effect of Simvastatin on the Metabolism of Lidocaine Both in vitro and in vivo. Drug Des Devel Ther 2020;14:1739-1747.
                    doi: 10.2147/DDDT.S241022pubmed: 32440099google scholar: lookup