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Journal of the American Veterinary Medical Association2024; 262(12); 1632-1638; doi: 10.2460/javma.23.06.0340

Detection of levamisole and its metabolites in horses after oral levamisole administration over seven days.

Abstract: Levamisole is a regulated substance sometimes administered to racehorses to treat equine protozoal myelitis. Metabolites include compound II, aminorex, and pemoline. Aminorex and pemoline are Horseracing Integrity and Safety Authority-banned substances. Previous studies have examined single doses of the drug. This study examined the disposition of levamisole after 7 days of dosing. Methods: 6 healthy Thoroughbred geldings. Methods: Horses were treated with 500 mg (approx 0.91 to 1 mg/kg) of compounded levamisole hydrochloride paste PO every 12 hours for a total of 13 doses over 7 days. Serum and urine samples were analyzed for levamisole and its metabolites over a 28-day period. Results: The terminal half-life of levamisole in serum was variable between horses. Following the last dose of levamisole on day 7, serum levamisole levels took 3 to 14 days (days 10 to 21) to fall below the limit of detection (LOD) in 5 of 6 horses. Serum from 1 horse remained over LOD on the last testing day (day 28). In urine, following the final dose (day 7), levamisole was below LOD on day 13 (6 days after final dose) and aminorex was below LOD on day 10 (3 days after final dose). Compound II was above LOD in 4 of 5 horses sampled on the last sampling day (day 28). Conclusions: Levamisole and its metabolites can be detected for variable lengths of time in horses, with detection lasting for days to weeks following multiple doses. This study supports the Racing Medication and Testing Consortium Advisory on levamisole, which suggests that clearance sample testing should be conducted on treated horses to verify elimination of levamisole and its metabolites.
Publication Date: 2024-09-13 PubMed ID: 39270716DOI: 10.2460/javma.23.06.0340Google Scholar: Lookup
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Summary

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This research article explores the detection rates of levamisole and its byproducts in horses after the administration of multiple oral doses over a week. The findings suggest variations in the clearance of the drug and its metabolites, emphasizing the need for clearance sample testing for treated horses.

Research Study Methodology

  • The study subjects were six healthy Thoroughbred geldings that were administered levamisole, a controlled substance used to treat protozoal myelitis in horses.
  • Each horse received 500mg of compounded levamisole hydrochloride paste orally every 12 hours, making a total of 13 doses over a period of one week.
  • Serum and urine samples from the horses were analyzed over 28 days after the final levamisole dosage. The analyses focused on the detection of levamisole and its metabolites, including compound II, aminorex, and pemoline. Notably, aminorex and pemoline are prohibited substances under the Horseracing Integrity and Safety Authority rules.

Research Study Findings

  • The half-life of levamisole in serum was inconsistent amongst the horses. Post the final dosage, it took 3 to 14 days for the serum levamisole levels of 5 out of the 6 horses to fall beneath the limit of detection (LOD).
  • One horse’s serum consistently tested above the LOD for levamisole until the last testing day (day 28).
  • In urine samples, it took 6 days after the final dose for levamisole to fall below LOD, and 3 days for aminorex.
  • On the last sample collection day, compound II was still detectable in urine samples of 4 out of the 5 horses. This suggests a longer detection time for this particular metabolite.

Research Conclusions

  • The study proved that levamisole and its metabolites could be detected in horses for variable lengths of time. In some cases, detection lasted for weeks following the administration of multiple doses.
  • The insights gained from this study align with the Racing Medication and Testing Consortium Advisory’s recommendations to conduct clearance sample testing on treated horses. This will ensure the elimination of levamisole and its metabolites from the horses’ system.

Cite This Article

APA
Adam E, Scollay M, Howard B, Taormina J, Hartmann P, Knych H. (2024). Detection of levamisole and its metabolites in horses after oral levamisole administration over seven days. J Am Vet Med Assoc, 262(12), 1632-1638. https://doi.org/10.2460/javma.23.06.0340

Publication

ISSN: 1943-569X
NlmUniqueID: 7503067
Country: United States
Language: English
Volume: 262
Issue: 12
Pages: 1632-1638

Researcher Affiliations

Adam, Emma
  • 1Maxwell H. Gluck Equine Research Center, Martin-Gatton College of Agriculture, Food and Environment, University of Kentucky, Lexington, KY.
Scollay, Mary
  • 2Racing Medication and Testing Consortium, Lexington, KY.
Howard, Bruce
  • 3Kentucky Horse Racing Commission, Lexington, KY.
Taormina, John
  • 3Kentucky Horse Racing Commission, Lexington, KY.
Hartmann, Petra
  • 4Industrial Laboratories, Wheat Ridge, CO.
Knych, Heather
  • 5Kenneth L. Maddy Equine Analytical Pharmacology Laboratory, School of Veterinary Medicine, University of California-Davis, Davis, CA.

MeSH Terms

  • Animals
  • Levamisole / administration & dosage
  • Levamisole / pharmacokinetics
  • Levamisole / urine
  • Horses
  • Male
  • Administration, Oral
  • Half-Life
  • Antinematodal Agents / administration & dosage
  • Antinematodal Agents / pharmacokinetics
  • Antinematodal Agents / urine

Citations

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