dc.creatorViviani, Paula
dc.creatorLifschitz, Adrian Luis
dc.creatorLuque, Sonia Elisabet
dc.creatorLloberas, Maria Mercedes
dc.creatorMaté, María Laura
dc.creatorCardozo, Patricia Alejandra
dc.creatorLanusse, Carlos Edmundo
dc.creatorVirkel, Guillermo Leon
dc.date.accessioned2020-05-11T14:24:49Z
dc.date.accessioned2022-10-15T03:29:02Z
dc.date.available2020-05-11T14:24:49Z
dc.date.available2022-10-15T03:29:02Z
dc.date.created2020-05-11T14:24:49Z
dc.date.issued2019-09
dc.identifierViviani, Paula; Lifschitz, Adrian Luis; Luque, Sonia Elisabet; Lloberas, Maria Mercedes; Maté, María Laura; et al.; Pharmacologic interaction between oxfendazole and triclabendazole: In vitro biotransformation and systemic exposure in sheep; Academic Press Inc Elsevier Science; Experimental Parasitology; 204; 9-2019
dc.identifier0014-4894
dc.identifierhttp://hdl.handle.net/11336/104738
dc.identifier1090-2449
dc.identifierCONICET Digital
dc.identifierCONICET
dc.identifier.urihttps://repositorioslatinoamericanos.uchile.cl/handle/2250/4340174
dc.description.abstractThe aim of the current work was to evaluate a potential pharmacokinetic interaction between the flukicide triclabendazole (TCBZ) and the broad-spectrum benzimidazole (BZD) anthelmintic oxfendazole (OFZ) in sheep. To this end, both an in vitro assay in microsomal fractions and an in vivo trial in lambs parasitized with Haemonchus contortus resistant to OFZ and its reduced derivative fenbendazole (FBZ) were carried out. Sheep microsomal fractions were incubated together with OFZ, FBZ, TCBZ, or a combination of either FBZ and TCBZ or OFZ and TCBZ. OFZ production was significantly diminished upon coincubation of FBZ and TCBZ, whereas neither FBZ nor OFZ affected the S-oxidation of TCBZ towards its sulfoxide and sulfone metabolites. For the in vivo trial, lambs were treated with OFZ (Vermox® oral drench at a single dose of 5 mg/kg PO), TCBZ (Fasinex® oral drench at a single dose of 12 mg/kg PO) or both compounds at a single dose of 5 (Vermox®) and 12 mg/kg (Fasinex®) PO. Blood samples were taken to quantify drug and metabolite concentrations, and pharmacokinetic parameters were calculated by means of non-compartmental analysis. Results showed that the pharmacokinetic parameters of active molecules and metabolites were not significantly altered upon coadministration. The sole exception was the increase in the mean residence time (MRT) of OFZ and FBZ sulfone upon coadministration, with no significant changes in the remaining pharmacokinetic parameters. This research is a further contribution to the study of metabolic drug-drug interactions that may affect anthelmintic efficacies in ruminants.
dc.languageeng
dc.publisherAcademic Press Inc Elsevier Science
dc.relationinfo:eu-repo/semantics/altIdentifier/url/https://www.sciencedirect.com/science/article/pii/S0014489419300529
dc.relationinfo:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.1016/j.exppara.2019.107718
dc.rightshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.rightsinfo:eu-repo/semantics/restrictedAccess
dc.subjectDRUG-DRUG INTERACTIONS
dc.subjectFENBENDAZOLE (PUBCHEM CID: 3334)
dc.subjectFENBENDAZOLE SULFONE (PUBCHEM CID: 162136)
dc.subjectMICROSOMAL FRACTIONS
dc.subjectOXFENDAZOLE
dc.subjectOXFENDAZOLE (PUBCHEM CID: 40854)
dc.subjectOXIBENDAZOLE (PUBCHEM CID: 4622)
dc.subjectPHARMACOKINETIC ASSESSMENT
dc.subjectRUMINANTS
dc.subjectTRICLABENDAZOLE
dc.subjectTRICLABENDAZOLE (PUBCHEM CID: 50248)
dc.subjectTRICLABENDAZOLE SULFONE (PUBCHEM CID: 10340439)
dc.subjectTRICLABENDAZOLE SULFOXIDE (PUBCHEM CID: 127657)
dc.titlePharmacologic interaction between oxfendazole and triclabendazole: In vitro biotransformation and systemic exposure in sheep
dc.typeinfo:eu-repo/semantics/article
dc.typeinfo:ar-repo/semantics/artículo
dc.typeinfo:eu-repo/semantics/publishedVersion


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