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Urinary excretion of pentoxifylline and its metabolites by standardbred mares.

Abstract: The urinary excretion of a sustained-release formulation of pentoxifylline was studied in the horse after the oral administration of 4.0 grams of Trental tablets. Urine samples were collected for 24 hours after dosing and analyzed for pentoxifylline and its metabolites using high-performance liquid chromatography coupled with an ultraviolet detector. Six metabolites of pentoxifylline were identified in horse urine in addition to less than 0.2% of unchanged drug. Concomitant use of gas chromatography/mass spectrometry allowed for the elucidation of the chemical structures of the metabolites. Metabolism of pentoxifylline yields one demethylated derivative, four hydroxylated metabolites and a conjugate of one of the hydroxymetabolites as urine products. The demethylated derivative, 3-methyl-1-(5-oxohexyl)-xanthine, was found to be the predominant metabolite in the urine.
Publication Date: 1989-04-01 PubMed ID: 2713780PubMed Central: PMC1255539
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  • Journal Article
  • Research Support
  • Non-U.S. Gov't

Summary

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The research paper discusses a study on how horses eliminate pentoxifylline, a drug usually used to improve blood flow, through their urine. The study examines the various metabolites formed in the process.

Research Method and Procedure

  • The research was conducted on standardbred mares who were orally administered a sustained-release formulation of Pentoxifylline in the form of 4.0 grams of Trental tablets.
  • Urine samples were collected from the horses for a full day post-drug administration.
  • These samples were then analyzed for pentoxifylline and its various metabolites. This was accomplished using a high-performance liquid chromatography system, which was coupled with an ultraviolet detector.

Identification of Metabolites and Unchanged Drug

  • The research revealed that there were six different metabolites of pentoxifylline identified in the Urine. This was in addition to less than 0.2% of the unchanged drug being excreted.
  • The concomitant use of gas chromatography/mass spectrometry allowed the researchers to determine the exact chemical structures of these metabolites.

Metabolism of Pentoxifylline

  • The metabolism of the drug yielded one demethylated derivative, four hydroxylated metabolites and a conjugate of one of the hydroxy metabolites as urine products.
  • The majority of the drug metabolized into the predominant demethylated derivative, known as 3-methyl-1-(5-oxohexyl)-xanthine.

Conclusion

  • The detailed analysis shown in this paper indicates that a substantial part of orally administered pentoxifylline is metabolized before excretion in a horse’s system, with very little of the unchanged drug being excreted.
  • Understanding these breakdown pathways has implications for drug detection, dosage, as well as potential toxicity in horses.

Cite This Article

APA
Kwong EC, Chen FC, Young LM. (1989). Urinary excretion of pentoxifylline and its metabolites by standardbred mares. Can J Vet Res, 53(2), 147-153.

Publication

ISSN: 0830-9000
NlmUniqueID: 8607793
Country: Canada
Language: English
Volume: 53
Issue: 2
Pages: 147-153

Researcher Affiliations

Kwong, E C
  • CanTest Ltd., Vancouver, British Columbia.
Chen, F C
    Young, L M

      MeSH Terms

      • Animals
      • Chromatography, High Pressure Liquid
      • Delayed-Action Preparations
      • Female
      • Horses / urine
      • Pentoxifylline / analogs & derivatives
      • Pentoxifylline / metabolism
      • Pentoxifylline / pharmacokinetics
      • Pentoxifylline / urine
      • Theobromine / analogs & derivatives
      • Time Factors

      References

      This article includes 14 references
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      Citations

      This article has been cited 2 times.
      1. Uney K, Tras B, Corum O, Yildiz R, Maden M. Pharmacokinetics of pentoxifylline and its 5-hydroxyhexyl metabolite following intravenous administration in cattle. Trop Anim Health Prod 2019 Feb;51(2):435-441.
        doi: 10.1007/s11250-018-1710-8pubmed: 30219998google scholar: lookup
      2. Weiss DJ, Geor RJ, Burris SM, Smith CM 2nd. Effects of pentoxifylline on equine neutrophil function and flow properties. Can J Vet Res 1992 Oct;56(4):313-7.
        pubmed: 1335832