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Xenobiotica; the fate of foreign compounds in biological systems1989; 19(1); 97-100; doi: 10.3109/00498258909034681

Comparative microsomal oxidation of febantel and its metabolite fenbendazole in various animal species.

Abstract: A comparison has been made of the in vitro metabolism of febantel (FBT) with that of one of its pharmacologically active metabolites fenbendazole (FBZ) using microsomal preparations from liver of sheep, calf, horse, pig, rat, chicken and trout. The oxidation of FBT to the corresponding sulphoxide appeared to be far more rapid with the exception of the trout, than a similar reaction with FBZ. Indeed FBT was further metabolized in several species by cyclization and further oxidation. This observation could have toxicological significance in view of the greater tetratogenic effects of the metabolite oxfendazole. Reaction rates were most rapid in pigs and sheep.
Publication Date: 1989-01-01 PubMed ID: 2756722DOI: 10.3109/00498258909034681Google Scholar: Lookup
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  • Comparative Study
  • Journal Article
  • Research Support
  • Non-U.S. Gov't

Summary

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This research paper primarily examines how febantel and one of its active metabolites, fenbendazole, are metabolized by several animal species. The scientists find that the rate of this metabolic process varies between species, and this could potentially have significant toxicological implications.

Overview of the Research

  • The study focuses on the in vitro metabolism (chemical transformations that a compound undergoes inside an organism) of febantel (FBT) and its pharmacologically active metabolite fenbendazole (FBZ).
  • The researchers used liver microsomal preparations from various animal species, including sheep, calf, horse, pig, rat, chicken, and trout.

Metabolic Findings

  • They found that the oxidation of FBT to the corresponding sulphoxide occurs at a much faster rate compared to a similar reaction with FBZ in all the tested species, except trout.
  • Interestingly, FBT was also metabolized further through a process called cyclization and additional oxidation steps in several species.

Toxicological Considerations

  • These metabolic observations are important from a toxicological point of view. This importance arises because the metabolite oxfendazole, which is created in the process, has been found to have higher teratogenic effects.
  • Teratogenic effects refer to the capability of a compound to cause birth defects or developmental malformations.

Variability Among Species

  • The research observed that reaction rates varied over different species; pigs and sheep displayed the most rapid rates of reaction.
  • This suggests that the metabolism of febantel and fenbendazole might be species-dependent, which could influence the efficacy, safety and recommended dosage of these compounds in different species.

Cite This Article

APA
Montesissa C, Stracciari JM, Fadini L, Beretta C. (1989). Comparative microsomal oxidation of febantel and its metabolite fenbendazole in various animal species. Xenobiotica, 19(1), 97-100. https://doi.org/10.3109/00498258909034681

Publication

ISSN: 0049-8254
NlmUniqueID: 1306665
Country: England
Language: English
Volume: 19
Issue: 1
Pages: 97-100

Researcher Affiliations

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

        MeSH Terms

        • Animals
        • Anthelmintics / metabolism
        • Benzimidazoles / metabolism
        • Cattle
        • Chickens
        • Female
        • Fenbendazole / metabolism
        • Guanidines / metabolism
        • Horses
        • In Vitro Techniques
        • Male
        • Microsomes, Liver / metabolism
        • Oxidation-Reduction
        • Rats
        • Rats, Inbred Strains
        • Sheep
        • Species Specificity
        • Swine
        • Trout

        Citations

        This article has been cited 3 times.
        1. Ichinose P, Miró MV, Larsen K, Lanusse C, Lifschitz A, Virkel G. Medication with fenbendazole in feed: plasma concentrations and effects on hepatic xenobiotic metabolizing enzymes in swine.. Vet Res Commun 2023 Jun;47(2):803-815.
          doi: 10.1007/s11259-022-10041-6pubmed: 36542192google scholar: lookup
        2. Wu Z, Lee D, Joo J, Shin JH, Kang W, Oh S, Lee DY, Lee SJ, Yea SS, Lee HS, Lee T, Liu KH. CYP2J2 and CYP2C19 are the major enzymes responsible for metabolism of albendazole and fenbendazole in human liver microsomes and recombinant P450 assay systems.. Antimicrob Agents Chemother 2013 Nov;57(11):5448-56.
          doi: 10.1128/AAC.00843-13pubmed: 23959307google scholar: lookup
        3. 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