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Biochemical pharmacology1987; 36(19); 3107-3114; doi: 10.1016/0006-2952(87)90619-8

In vitro febantel transformation by sheep and cattle ruminal fluids and metabolism by hepatic subcellular fractions from different animal species.

Abstract: Febantel and one of its main metabolites, febantel sulphoxide, are chemically modified to only a slight extent when incubated in vitro with sheep and cattle ruminal fluids; other major metabolites, fenbendazole and oxfendazole, are respectively, oxidized to oxfendazole and reduced to fenbendazole. Febantel is negligibly metabolized by hepatic cytosol fractions but microsome preparations effect more extensive metabolic transformations. Important differences in this respect were found between microsome preparations from rat, horse, pig, cattle, sheep, chicken and trout livers.
Publication Date: 1987-10-01 PubMed ID: 3663228DOI: 10.1016/0006-2952(87)90619-8Google Scholar: Lookup
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  • Journal Article

Summary

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The research article explores how the drug Febantel is metabolized differently by different animal species both in the digestive system (using sheep and cattle ruminal fluids) and at the liver-cell level.

Study Overview

  • The researchers used in vitro methods, meaning they performed their studies outside a living organism, likely in a laboratory dish or a test tube.
  • The substance under examination was Febantel, a broad-spectrum anthelmintic drug commonly used in veterinary medicine to treat parasites.
  • In addition to Febantel, the scientists were also interested in two of its primary metabolites (chemicals produced as the body breaks the drug down), febantel sulphoxide, fenbendazole, and oxfendazole.

Metabolism in Ruminal Fluids

  • The first part of the research involved assessing how Febantel and its metabolites are transformed in the ruminal fluids (fermentation liquid in the first stomach) of sheep and cattle.
  • During this phase of the experiment, it was discovered that Febantel and febantel sulphoxide weren’t significantly altered when incubated in the rumen fluids.
  • On the other hand, fenbendazole and oxfendazole were chemically transformed, with fenbendazole being oxidized to oxfendazole, and oxfendazole being reduced to fenbendazole.

Metabolism in Hepatic Subcellular Fractions

  • In the second part of the investigation, the researchers turned their attention to how Febantel is metabolized in the liver, using hepatic cytosol fractions (fluid portion of liver cells) and microsome preparations (small vesicles within liver cells).
  • The researchers found that the hepatic cytosol fractions barely metabolized Febantel, whereas the microsomes brought about substantial metabolic transformations.
  • The team detected significant differences in the metabolism of Febantel by microsomes extracted from different animal species. These species included rats, horses, pigs, cows, sheep, chickens, and trout.
  • Although the original abstract didn’t provide specific differences between the studied species, this observation underlines the fact that different animals can metabolize the same compounds in diverse ways, likely due to differences in their enzyme systems and metabolic pathways.

Significance of the Research

  • The study’s findings contribute valuable data to the understanding of how Febantel is metabolized in different animals, information that could affect its dosing, effectiveness, and potential side effects in those animals.
  • This knowledge could potentially serve to create better, species-specific treatments for parasitic infections.

Cite This Article

APA
Beretta C, Fadini L, Stracciari JM, Montesissa C. (1987). In vitro febantel transformation by sheep and cattle ruminal fluids and metabolism by hepatic subcellular fractions from different animal species. Biochem Pharmacol, 36(19), 3107-3114. https://doi.org/10.1016/0006-2952(87)90619-8

Publication

ISSN: 0006-2952
NlmUniqueID: 0101032
Country: England
Language: English
Volume: 36
Issue: 19
Pages: 3107-3114

Researcher Affiliations

Beretta, C
  • Institute of Veterinary Pharmacology and Toxicology, University of Milan, Italy.
Fadini, L
    Stracciari, J M
      Montesissa, C

        MeSH Terms

        • Animals
        • Anthelmintics / metabolism
        • Benzimidazoles / metabolism
        • Biotransformation
        • Cattle
        • Chickens
        • Cytosol / metabolism
        • Female
        • Fenbendazole / metabolism
        • Guanidines / metabolism
        • Horses
        • Liver / metabolism
        • Male
        • Microsomes, Liver / metabolism
        • Rats
        • Rats, Inbred Strains
        • Rumen / metabolism
        • Sheep
        • Species Specificity
        • Swine
        • Trout

        Citations

        This article has been cited 2 times.
        1. Imperiale F, Lanusse C. The Pattern of Blood-Milk Exchange for Antiparasitic Drugs in Dairy Ruminants.. Animals (Basel) 2021 Sep 22;11(10).
          doi: 10.3390/ani11102758pubmed: 34679780google scholar: lookup
        2. Lanusse CE, Nare B, Gascon LH, Prichard RK. Bioconversion of netobimin pro-drug by gastrointestinal fluids of ruminants.. Eur J Drug Metab Pharmacokinet 1992 Apr-Jun;17(2):121-8.
          doi: 10.1007/BF03188780pubmed: 1425810google scholar: lookup