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dc.contributor.authorBenchaoui, H. A.
dc.contributor.authorMcKellar, Quintin
dc.date.accessioned2013-06-26T15:01:53Z
dc.date.available2013-06-26T15:01:53Z
dc.date.issued1996-07
dc.identifier.citationBenchaoui , H A & McKellar , Q 1996 , ' Interaction between fenbendazole and piperonyl butoxide : pharmacokinetic and pharmacodynamic implications ' Journal of Pharmacy and Pharmacology , vol. 48 , no. 7 , pp. 753-759 . https://doi.org/10.1111/j.2042-7158.1996.tb03965.x
dc.identifier.issn2042-7158
dc.identifier.otherPURE: 1426615
dc.identifier.otherPURE UUID: 200ab068-c78b-45bd-9a4a-6a428cf08ea0
dc.identifier.otherBibtex: urn:afaba1d1519f8f5399e9481f23a1203f
dc.identifier.otherScopus: 0029809394
dc.identifier.urihttp://hdl.handle.net/2299/10965
dc.description.abstractThe effect of the cytochrome P450 inhibitor, piperonyl butoxide on the pharmacokinetics and anthelmintic efficacy of the benzimidazole compound fenbendazole was studied in sheep and goats. Pretreatment of goats with the inhibitor caused a greater than three-fold increase in the relative bioavailability of fenbendazole and fenbendazole sulphoxide. A pharmacokinetic dose titration study was carried out in sheep with fenbendazole (5 mg kg(-1)) and piperonyl butoxide administered orally at 0, 15, 31, 63, 125 and 250 mg kg(-1). The AUC of fenbendazole and the sulphoxide were significantly increased when fenbendazole was co-admimstered with piperonyl butoxide at dose rates equal to or higher than 31 mg kg(-1). Peak plasma concentrations (C-max) and mean residence time (MRT) were also significantly increased. The efficacy of the combination was assessed in sheep against two species of benzimidazole-resistant abomasal nematodes; Ostertagia circumcincta and Haemonchus contortus. The percentage reduction in the total number of O. circumcincta worms was 7.9% (fenbendazole) and 97.8% (fenbendazole-piperonyl butoxide). For H. contortus, the percentage reduction was 84.8% (fenbendazole) and 99.0% (fenbendazole-piperonyl butoxide). The in-vitro S-oxidation of fenbendazole and fenbendazole sulphoxide was studied using microsomal preparations from rat liver. Piperonyl butoxide inhibited significantly the sulphoxidation and sulphonation of fenbendazole. It was concluded that piperonyl butoxide inhibited the oxidative conversion of fenbendazole into inactive metabolites and this resulted in a potentiated anthelmintic action.en
dc.format.extent7
dc.language.isoeng
dc.relation.ispartofJournal of Pharmacy and Pharmacology
dc.subjectRAT-LIVER MICROSOMES
dc.subjectSHEEP
dc.subjectALBENDAZOLE
dc.subjectDISPOSITION
dc.subjectSULFOXIDATION
dc.subjectMETABOLITES
dc.subjectOXFENDAZOLE
dc.subjectCATTLE
dc.subjectCYTOCHROME-P-450
dc.subjectMETHIMAZOLE
dc.titleInteraction between fenbendazole and piperonyl butoxide : pharmacokinetic and pharmacodynamic implicationsen
dc.contributor.institutionOffice of the Vice-Chancellor
dc.contributor.institutionVeterinary Science
dc.contributor.institutionGeography, Environment and Agriculture
dc.description.statusPeer reviewed
rioxxterms.versionofrecordhttps://doi.org/10.1111/j.2042-7158.1996.tb03965.x
rioxxterms.typeJournal Article/Review
herts.preservation.rarelyaccessedtrue
herts.rights.accesstyperestrictedAccess


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