Pharmacological assessment of netobimin as a potential anthelmintic for use in horses: Plasma disposition, faecal excretion and efficacy

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dc.contributor.authorGökbulut, Cengiz
dc.contributor.authorYıldırım, Funda
dc.contributor.authorMcKellar, Quintin A.
dc.contributor.buuauthorÇırak, Veli Yilgör
dc.contributor.buuauthorŞenlik, Bayram
dc.contributor.departmentUludağ Üniversitesi/Veteriner Fakültesi/Parazitoloji Anabilim Dalı.tr_TR
dc.contributor.orcid0000-0003-2964-2245tr_TR
dc.contributor.scopusid6602404057tr_TR
dc.contributor.scopusid9332720500tr_TR
dc.date.accessioned2022-01-24T08:26:59Z
dc.date.available2022-01-24T08:26:59Z
dc.date.issued2009-06
dc.description.abstractThis study aimed to determine the plasma disposition and faecal excretion of netobimin (NTB) and its respective metabolites as well as the efficacy against strongyles in horses following oral administration. Netobimin (10 mg/kg) was administered orally to 8 horses. Blood and faecal samples were collected from 1 to 120 h post-treatment and analysed by high performance liquid chromatography (HPLC). Using a chiral phase-based HPLC, plasma disposition of ABZSO enantiomers produced was also determined. Faecal strongly egg counts (EPG) were performed by a modified McMaster's technique before and after the treatment. Neither NTB nor ABZ were present and only albendazole sulphoxide (ABZSO) and sulphone metabolites (ABZSO(2)) were detected in the plasma samples. Maximum plasma concentration of ABZSO (0.53 +/- 0.14 mu g/ml) and ABZSO(2) (0.36 +/- 0.09 mu g/ml) were observed at (t(max)) 10.50 and 19.50 h, respectively following administration of NTB. The area under the curve (AUC) of the two metabolites was similar to each other. Netobimin was not detected, and ABZ was predominant in faecal samples. The maximum plasma concentration (C(max)) of (-)ABZSO was significantly higher than (+)ABZSO, but the area under the curves (AUCs) of the enantiomer were not significantly different each other in plasma samples. The enantiomers of ABZSO were close to racemate in the faecal samples analyzed. Netobimin reduced the EPG by 100%, 100%, 77%, 80% and 75% 2, 4, 6, 8 and 10 weeks post-treatment, respectively. The specific behaviour of the two enantiomers probably reflects different enantioselectivity of the enzymatic systems of the liver which are responsible for sulphoxidation and sulphonation of ABZ. Considering the pharmacokinetic and efficacy parameters NTB could be used as an anthelmintic in horses.en_US
dc.identifier.citationGökbulut, C. vd. (2009). "Pharmacological assessment of netobimin as a potential anthelmintic for use in horses: Plasma disposition, faecal excretion and efficacy". Research in Veterinary Science, 86(3), 514-520.en_US
dc.identifier.endpage520tr_TR
dc.identifier.issn0034-5288
dc.identifier.issue3tr_TR
dc.identifier.pubmed19022462tr_TR
dc.identifier.scopus2-s2.0-64449084573tr_TR
dc.identifier.startpage514tr_TR
dc.identifier.urihttps://doi.org/10.1016/j.rvsc.2008.10.001
dc.identifier.urihttps://www.sciencedirect.com/science/article/pii/S0034528808002178
dc.identifier.urihttp://hdl.handle.net/11452/24245
dc.identifier.volume86tr_TR
dc.identifier.wos000266122900024tr_TR
dc.indexed.pubmedPubmeden_US
dc.indexed.scopusScopusen_US
dc.indexed.wosSCIEen_US
dc.language.isoenen_US
dc.publisherElsevieren_US
dc.relation.collaborationSanayitr_TR
dc.relation.collaborationYurt dışıtr_TR
dc.relation.collaborationYurt içitr_TR
dc.relation.journalResearch in Veterinary Scienceen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergitr_TR
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectAlbendazoleen_US
dc.subjectAlbendazole sulphoxideen_US
dc.subjectEfficacyen_US
dc.subjectEnantiomersen_US
dc.subjectHorseen_US
dc.subjectNetobiminen_US
dc.subjectPharmacokineticsen_US
dc.subjectStrongylesen_US
dc.subjectAcquired gastrointestinal nematodesen_US
dc.subjectAlbendazole-sulfoxide enantiomersen_US
dc.subjectBenzimidazole anthelminticsen_US
dc.subjectHaemonchus-contortusen_US
dc.subjectCritical testsen_US
dc.subjectSheepen_US
dc.subjectMetabolitesen_US
dc.subjectFenbendazoleen_US
dc.subjectPharmacokineticsen_US
dc.subjectResistanceen_US
dc.subjectVeterinary sciencesen_US
dc.subjectEquidaeen_US
dc.subjectStrongylesen_US
dc.subject.emtreeAlbendazoleen_US
dc.subject.emtreeAlbendazole sulfoxideen_US
dc.subject.emtreeDrug metaboliteen_US
dc.subject.emtreeNetobiminen_US
dc.subject.emtreeSulfoneen_US
dc.subject.emtreeAnimal experimenten_US
dc.subject.emtreeArea under the curveen_US
dc.subject.emtreeArticleen_US
dc.subject.emtreeControlled studyen_US
dc.subject.emtreeDrug blood levelen_US
dc.subject.emtreeDrug efficacyen_US
dc.subject.emtreeDrug excretionen_US
dc.subject.emtreeDrug feces levelen_US
dc.subject.emtreeDrug half lifeen_US
dc.subject.emtreeDrug metabolismen_US
dc.subject.emtreeDrug structureen_US
dc.subject.emtreeEnantiomeren_US
dc.subject.emtreeHorse diseaseen_US
dc.subject.emtreeMaximum plasma concentrationen_US
dc.subject.emtreeNematodeen_US
dc.subject.emtreeNonhumanen_US
dc.subject.emtreeRacemic mixtureen_US
dc.subject.emtreeStrongyle infectionen_US
dc.subject.emtreeSulfoxidationen_US
dc.subject.emtreeTime to maximum plasma concentrationen_US
dc.subject.meshAlbendazoleen_US
dc.subject.meshAnimalsen_US
dc.subject.meshAnthelminticsen_US
dc.subject.meshCalibrationen_US
dc.subject.meshFecesen_US
dc.subject.meshGuanidinesen_US
dc.subject.meshHelminthiasisen_US
dc.subject.meshHorse diseasesen_US
dc.subject.meshHorsesen_US
dc.subject.meshIntestinal absorptionen_US
dc.subject.meshSulfonesen_US
dc.subject.meshTissue distributionen_US
dc.subject.scopusAlbendazole; Fasciola Hepatica; Anthelmintic Agenten_US
dc.subject.wosVeterinary sciencesen_US
dc.titlePharmacological assessment of netobimin as a potential anthelmintic for use in horses: Plasma disposition, faecal excretion and efficacyen_US
dc.typeArticle
dc.wos.quartileQ2en_US

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