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dc.contributor.authorMcKellar, Quintin
dc.contributor.authorGokbulut, C.
dc.contributor.authorMuzandu, K.
dc.contributor.authorBenchaoui, H.
dc.date.accessioned2013-05-07T12:25:01Z
dc.date.available2013-05-07T12:25:01Z
dc.date.issued2002-11
dc.identifier.citationMcKellar , Q , Gokbulut , C , Muzandu , K & Benchaoui , H 2002 , ' Fenbendazole pharmacokinetics, metabolism, and potentiation in horses ' , Drug Metabolism and Disposition , vol. 30 , no. 11 , pp. 1230-1239 . https://doi.org/10.1124/dmd.30.11.1230
dc.identifier.issn1521-009X
dc.identifier.otherPURE: 1409915
dc.identifier.otherPURE UUID: f0188b5c-203b-4d6e-b883-895a078c1980
dc.identifier.otherBibtex: urn:9cb6f699fc3f607c2bef00abc88c995f
dc.identifier.otherScopus: 0036842030
dc.identifier.urihttp://hdl.handle.net/2299/10631
dc.description.abstractThe present study was designed to describe the pharmacokinetics and fecal excretion of fenbendazole (FBZ) and fenbendazole sulphoxide (FBZSO) and their metabolites in horses, to investigate the effects which concurrent feeding has on the absorption and pharmacokinetics of FBZ, and to determine the effect of coadministration of the metabolic inhibitor piperonyl-butoxide on the in vivo pharmacokinetics and in vitro liver microsomal metabolism of sulfide and sulfoxide benzimidazoles. The effect of piperonyl-butoxide on the enantiomeric genesis of the sulfoxide moiety was also investigated. Following administration of FBZSO and FBZ, the fenbendazole sulphone metabolite predominated in plasma, and the C-max and area under the plasma curve (AUC) values for each moiety were larger (P < 0.001) following FBZSO than FBZ. In feces the administered parent molecule predominated. The combined AUC for active benzimidazole moieties following oral administration of FBZ (10 mg/kg) in horses was almost 4 times as high in unfed horses (2.19 &mu;g.h/ml) than in fed horses (0.59 &mu;g.h/ml), and coadministration of piperonyl-butoxide significantly increased the AUC and C-max of active moieties following intravenous administration of FBZSO and oral administration of FBZ. When FBZSO was administered i.v. as a racemate, the first enantiomer of oxfendazole (FBZSO-1) predominated in plasma, however, following coadministration with piperonyl-butoxide, the second enantiomer of oxfendazole (FBZSO-2) predominated for 10 h. Piperonyl-butoxide significantly reduced the oxidative metabolism of FBZSO and FBZ in equine liver microsomes and altered the ratio of enantiomers FBZSO-1/FBZSO-2 from >4:1 to 1:1. It is concluded that in horses efficacy of FBZSO and FBZ could be improved by administration to unfed animals and coadministration with piperonyl-butoxide.en
dc.format.extent10
dc.language.isoeng
dc.relation.ispartofDrug Metabolism and Disposition
dc.subjectORGANIC-SOLVENTS
dc.subjectOXFENDAZOLE
dc.subjectSHEEP
dc.subjectALBENDAZOLE
dc.subjectABSORPTION
dc.subjectTRACT
dc.titleFenbendazole pharmacokinetics, metabolism, and potentiation in horsesen
dc.contributor.institutionOffice of the Vice-Chancellor
dc.contributor.institutionVeterinary Science
dc.contributor.institutionGeography, Environment and Agriculture
dc.description.statusPeer reviewed
dcterms.dateAccepted2002-11
rioxxterms.versionofrecordhttps://doi.org/10.1124/dmd.30.11.1230
rioxxterms.typeJournal Article/Review
herts.preservation.rarelyaccessedtrue


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