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dc.contributorFacultad de Veterinariaes_ES
dc.contributor.authorGarcia-Lino, Alba M.
dc.contributor.authorGarcia-Mateos, Dafne
dc.contributor.authorAlvarez-Fernandez, Indira
dc.contributor.authorBlanco-Paniagua, Esther
dc.contributor.authorMedina, Juan M.
dc.contributor.authorMerino, Gracia
dc.contributor.authorAlvarez, Ana I.
dc.contributor.otherOtroses_ES
dc.date2021
dc.date.accessioned2021-07-14T12:08:01Z
dc.date.available2021-07-14T12:08:01Z
dc.identifier.issn0034-5288
dc.identifier.urihttp://hdl.handle.net/10612/13314
dc.description6 p.es_ES
dc.description.abstractTherapeutic outcome results of the coadministration of several drugs in veterinary medicine is affected by, among others, the relationship between drugs and ATP-binding cassette (ABC) transporters, such as ABCG2. ABCG2 is an efflux protein involved in the bioavailability and milk secretion of drugs. The aim of this work was to determine the role of eprinomectin, a macrocyclic lactone (ML) member of avermectin class, as inhibitor of ABCG2. The experiments were carried out through in vitro inhibition assays based on mitoxantrone accumulation and transport assays in ovine ABCG2 transduced cells using the antimicrobial drug danofloxacin and the anti-inflammatory drug meloxicam, both widely used in veterinary medicine and well known ABCG2 substrates. The inhibition results obtained showed that eprinomectin was an efficient in vitro ABCG2 inhibitor, tested in mitoxantrone accumulation assays. In addition, this ML decreased ovine ABCG2-mediated transport of danofloxacin and meloxicam. To evaluate the role of eprinomectin in systemic exposure of drugs, pharmacokinetic assays based on subcutaneous coadministration of eprinomectin with danofloxacin (1.25 mg/kg) or meloxicam (0.5 mg/kg) in sheep were performed obtaining a significant increase of systemic exposure of these drugs. Especially relevant was the increase of the systemic concentration of meloxicam, since coadministration with eprinomectin increased significantly the plasma concentration of meloxicam, obtaining an increase of AUC (0-72 h) value of more than 40%.es_ES
dc.languageenges_ES
dc.publisherElsevieres_ES
dc.subjectSanidad animales_ES
dc.subject.otherABCG2es_ES
dc.subject.otherDanofloxacines_ES
dc.subject.otherEprinomectines_ES
dc.subject.otherMacrocyclic lactonees_ES
dc.subject.otherMeloxicames_ES
dc.subject.otherSheepes_ES
dc.titleRole of eprinomectin as inhibitor of the ruminant ABCG2 transporter: Effects on plasma distribution of danofloxacin and meloxicam in sheepes_ES
dc.typeinfo:eu-repo/semantics/preprintes_ES
dc.identifier.doi10.1016/j.rvsc.2021.03.026
dc.rights.accessRightsinfo:eu-repo/semantics/openAccesses_ES
dc.journal.titleResearch in Veterinary Sciencees_ES
dc.volume.number136es_ES
dc.page.initial478es_ES
dc.page.final483es_ES
dc.type.hasVersioninfo:eu-repo/semantics/submittedVersiones_ES


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