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British journal of sports medicine1976; 10(3); 116-123; doi: 10.1136/bjsm.10.3.116

Excretion and metabolism of nikethamide in the horse.

Abstract: It is well known that nikethamide (N,N-diethylnicotinamide, CoramineR) is metabolized very rapidly to nicotinamide. Hence, there is difficulty in proving that nikethamide has been used as a doping substance because nicotinamide is a normal physiological metabolite in the organism as well as a vitamin preparation. However, an intermediate metabolite (N-ethylnicotinamide) was found by us in the urine of horses treated with CoramineR. This was characterized by gas chromatography/mass spectrometry, and synthesized and identified as being N-ethylnicotinamide. The excretion and metabolism of nikethamide after intramuscular injection in the horse was followed using quantitative gas chromatography of urine extracts over a period of several hours and the results of these experiments are reported. Changes in urinary pH had no significant effect upon either the metabolism or rate of excretion of the drug.
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Publication Date: 1976-10-01 PubMed ID: 11864PubMed Central: PMC1859729DOI: 10.1136/bjsm.10.3.116Google Scholar: Lookup
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  • Journal Article

Summary

This research summary has been generated with artificial intelligence and may contain errors and omissions. Refer to the original study to confirm details provided. Submit correction.

This study investigates how a horse’s body processes a drug called nikethamide, paying special attention to one of the metabolites (N-ethylnicotinamide) that could be used to identify instances of doping in horses since nikethamide is often metabolised to a compound that naturally occurs in the body (nicotinamide).

Objective of the Research

  • The main objective of this study was to understand the metabolism and excretion of nikethamide (N,N-diethylnicotinamide, CoramineR) in horses. It is a challenge to detect nikethamide use as a doping substance in organisms as it is rapidly metabolized to nicotinamide, a regular physiological metabolite present in animals and also used as a vitamin supplement.

Discovery of an Intermediate Metabolite

  • The researchers discovered an intermediate metabolite, N-ethylnicotinamide, in the urine of horses treated with CoramineR. This was a significant development because the presence of this metabolite could suggest the use of nikethamide.
  • The identification was done using gas chromatography/mass spectrometry, and it was synthesized and discerned to be N-ethylnicotinamide.

Study Methodology and Results

  • The researchers studied the metabolism and excretion of nikethamide following an intramuscular injection in horses using quantitative gas chromatography of urine extracts.
  • This study was conducted over several hours to accurately understand the drug’s metabolism and excretion rates.
  • The findings showed that changes in urinary pH had no significant influence on the drug’s metabolism or excretion rate.

Implications of the Study

  • The results of this research could substantially assist anti-doping bodies. If the presence of N-ethylnicotinamide can be linked definitively to the usage of nikethamide, it could make detection of doping using nikethamide more reliable and more manageable.
  • In conclusion, this study provides a new method for detecting nikethamide in doping cases, making it less likely for such cases to go unnoticed.

Cite This Article

APA
Delbeke FT, Debackere M. (1976). Excretion and metabolism of nikethamide in the horse. Br J Sports Med, 10(3), 116-123. https://doi.org/10.1136/bjsm.10.3.116

Publication

British journal of sports medicine
ISSN: 0306-3674
NlmUniqueID: 0432520
Country: England
Language: English
Volume: 10
Issue: 3
Pages: 116-123

Researcher Affiliations

Delbeke, F T
    Debackere, M

      MeSH Terms

      • Ammonium Chloride / pharmacology
      • Animals
      • Female
      • Horses / urine
      • Hydrogen-Ion Concentration
      • Niacinamide / analogs & derivatives
      • Niacinamide / urine
      • Nikethamide / urine

      References

      This article includes 10 references
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      9. Debackere M, Laruelle L. Isolation, detection and identification of some alkaloids or alkaloid-like substances in biological specimens from horses with special reference to doping.. J Chromatogr 1968 Jun 4;35(2):234-47.
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      Citations

      This article has been cited 0 times.
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