Involvement of P-glycoprotein on ivermectin kinetic behaviour in sheep: itraconazole-mediated changes on gastrointestinal disposition

Autores
Ballent, Mariana; Lifschitz, Adrian Luis; Virkel, Guillermo Leon; Sallovitz, Juan Manuel; Lanusse, Carlos Edmundo
Año de publicación
2007
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
Different pharmacological approaches have been used in an attempt to increased drug systemic availability of anthelmintic drugs. The comparative effect of the itraconazole (ITZ)-mediated modulation of P-glycoprotein (P-gp) activity on the in vivo kinetic behaviour of ivermectin (IVM) administered by intravenous (IV) and intraruminal (IR) routes to sheep was assessed in the current work. Corriedale sheep received IVM (50 µg/kg) by the intravenous (IV) route either alone (Group A) or co-administered with the P-gp modulator ITZ (100 mg orally three times every 12 h) (Group B). Animals in Groups C and D were intraruminally (IR) treated with IVM (50 µg/kg) alone or co-administered with ITZ (100 mg orally three times every 12 h), respectively. Jugular blood and gastrointestinal tissue samples (only of the IVM IR treated animals) were collected. The samples were analyzed by HPLC using fluorescence detection. The plasma disposition of IVM given intravenously was unaffected by the presence of ITZ. However, the co-administration with ITZ resulted in markedly higher IVM plasma concentration profiles compared to the control group. Likewise, the presence of ITZ enhanced the IVM concentration profiles in the gastrointestinal mucosal tissues. An ITZ-induced reduction on the P-gp efflux activity at the intestinal lining may have accounted for the greater absorption and enhanced systemic availability observed for IVM in the intraruminally-treated animals.
Fil: Ballent, Mariana. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencias Veterinarias. Departamento de Fisiopatología; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Tandil; Argentina
Fil: Lifschitz, Adrian Luis. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencias Veterinarias. Departamento de Fisiopatología; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Tandil; Argentina
Fil: Virkel, Guillermo Leon. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencias Veterinarias. Departamento de Fisiopatología; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Tandil; Argentina
Fil: Sallovitz, Juan Manuel. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencias Veterinarias. Departamento de Fisiopatología; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Tandil; Argentina
Fil: Lanusse, Carlos Edmundo. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Tandil; Argentina. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencias Veterinarias. Departamento de Fisiopatología; Argentina
Materia
IVERMECTIN
ITRACONAZOLE
INTERACTION
P-GLYCOPROTEIN
Nivel de accesibilidad
acceso abierto
Condiciones de uso
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
Repositorio
CONICET Digital (CONICET)
Institución
Consejo Nacional de Investigaciones Científicas y Técnicas
OAI Identificador
oai:ri.conicet.gov.ar:11336/112015

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network_name_str CONICET Digital (CONICET)
spelling Involvement of P-glycoprotein on ivermectin kinetic behaviour in sheep: itraconazole-mediated changes on gastrointestinal dispositionBallent, MarianaLifschitz, Adrian LuisVirkel, Guillermo LeonSallovitz, Juan ManuelLanusse, Carlos EdmundoIVERMECTINITRACONAZOLEINTERACTIONP-GLYCOPROTEINhttps://purl.org/becyt/ford/4.3https://purl.org/becyt/ford/4Different pharmacological approaches have been used in an attempt to increased drug systemic availability of anthelmintic drugs. The comparative effect of the itraconazole (ITZ)-mediated modulation of P-glycoprotein (P-gp) activity on the in vivo kinetic behaviour of ivermectin (IVM) administered by intravenous (IV) and intraruminal (IR) routes to sheep was assessed in the current work. Corriedale sheep received IVM (50 µg/kg) by the intravenous (IV) route either alone (Group A) or co-administered with the P-gp modulator ITZ (100 mg orally three times every 12 h) (Group B). Animals in Groups C and D were intraruminally (IR) treated with IVM (50 µg/kg) alone or co-administered with ITZ (100 mg orally three times every 12 h), respectively. Jugular blood and gastrointestinal tissue samples (only of the IVM IR treated animals) were collected. The samples were analyzed by HPLC using fluorescence detection. The plasma disposition of IVM given intravenously was unaffected by the presence of ITZ. However, the co-administration with ITZ resulted in markedly higher IVM plasma concentration profiles compared to the control group. Likewise, the presence of ITZ enhanced the IVM concentration profiles in the gastrointestinal mucosal tissues. An ITZ-induced reduction on the P-gp efflux activity at the intestinal lining may have accounted for the greater absorption and enhanced systemic availability observed for IVM in the intraruminally-treated animals.Fil: Ballent, Mariana. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencias Veterinarias. Departamento de Fisiopatología; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Tandil; ArgentinaFil: Lifschitz, Adrian Luis. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencias Veterinarias. Departamento de Fisiopatología; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Tandil; ArgentinaFil: Virkel, Guillermo Leon. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencias Veterinarias. Departamento de Fisiopatología; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Tandil; ArgentinaFil: Sallovitz, Juan Manuel. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencias Veterinarias. Departamento de Fisiopatología; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Tandil; ArgentinaFil: Lanusse, Carlos Edmundo. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Tandil; Argentina. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencias Veterinarias. Departamento de Fisiopatología; ArgentinaWiley Blackwell Publishing, Inc2007-06info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfapplication/pdfapplication/pdfapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/112015Ballent, Mariana; Lifschitz, Adrian Luis; Virkel, Guillermo Leon; Sallovitz, Juan Manuel; Lanusse, Carlos Edmundo; Involvement of P-glycoprotein on ivermectin kinetic behaviour in sheep: itraconazole-mediated changes on gastrointestinal disposition; Wiley Blackwell Publishing, Inc; Journal of Veterinary Pharmacology and Therapeutics; 30; 3; 6-2007; 242-2480140-7783CONICET DigitalCONICETenginfo:eu-repo/semantics/altIdentifier/url/https://onlinelibrary.wiley.com/doi/abs/10.1111/j.1365-2885.2007.00848.xinfo:eu-repo/semantics/altIdentifier/doi/10.1111/j.1365-2885.2007.00848.xinfo:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-09-29T10:46:13Zoai:ri.conicet.gov.ar:11336/112015instacron:CONICETInstitucionalhttp://ri.conicet.gov.ar/Organismo científico-tecnológicoNo correspondehttp://ri.conicet.gov.ar/oai/requestdasensio@conicet.gov.ar; lcarlino@conicet.gov.arArgentinaNo correspondeNo correspondeNo correspondeopendoar:34982025-09-29 10:46:13.3CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv Involvement of P-glycoprotein on ivermectin kinetic behaviour in sheep: itraconazole-mediated changes on gastrointestinal disposition
title Involvement of P-glycoprotein on ivermectin kinetic behaviour in sheep: itraconazole-mediated changes on gastrointestinal disposition
spellingShingle Involvement of P-glycoprotein on ivermectin kinetic behaviour in sheep: itraconazole-mediated changes on gastrointestinal disposition
Ballent, Mariana
IVERMECTIN
ITRACONAZOLE
INTERACTION
P-GLYCOPROTEIN
title_short Involvement of P-glycoprotein on ivermectin kinetic behaviour in sheep: itraconazole-mediated changes on gastrointestinal disposition
title_full Involvement of P-glycoprotein on ivermectin kinetic behaviour in sheep: itraconazole-mediated changes on gastrointestinal disposition
title_fullStr Involvement of P-glycoprotein on ivermectin kinetic behaviour in sheep: itraconazole-mediated changes on gastrointestinal disposition
title_full_unstemmed Involvement of P-glycoprotein on ivermectin kinetic behaviour in sheep: itraconazole-mediated changes on gastrointestinal disposition
title_sort Involvement of P-glycoprotein on ivermectin kinetic behaviour in sheep: itraconazole-mediated changes on gastrointestinal disposition
dc.creator.none.fl_str_mv Ballent, Mariana
Lifschitz, Adrian Luis
Virkel, Guillermo Leon
Sallovitz, Juan Manuel
Lanusse, Carlos Edmundo
author Ballent, Mariana
author_facet Ballent, Mariana
Lifschitz, Adrian Luis
Virkel, Guillermo Leon
Sallovitz, Juan Manuel
Lanusse, Carlos Edmundo
author_role author
author2 Lifschitz, Adrian Luis
Virkel, Guillermo Leon
Sallovitz, Juan Manuel
Lanusse, Carlos Edmundo
author2_role author
author
author
author
dc.subject.none.fl_str_mv IVERMECTIN
ITRACONAZOLE
INTERACTION
P-GLYCOPROTEIN
topic IVERMECTIN
ITRACONAZOLE
INTERACTION
P-GLYCOPROTEIN
purl_subject.fl_str_mv https://purl.org/becyt/ford/4.3
https://purl.org/becyt/ford/4
dc.description.none.fl_txt_mv Different pharmacological approaches have been used in an attempt to increased drug systemic availability of anthelmintic drugs. The comparative effect of the itraconazole (ITZ)-mediated modulation of P-glycoprotein (P-gp) activity on the in vivo kinetic behaviour of ivermectin (IVM) administered by intravenous (IV) and intraruminal (IR) routes to sheep was assessed in the current work. Corriedale sheep received IVM (50 µg/kg) by the intravenous (IV) route either alone (Group A) or co-administered with the P-gp modulator ITZ (100 mg orally three times every 12 h) (Group B). Animals in Groups C and D were intraruminally (IR) treated with IVM (50 µg/kg) alone or co-administered with ITZ (100 mg orally three times every 12 h), respectively. Jugular blood and gastrointestinal tissue samples (only of the IVM IR treated animals) were collected. The samples were analyzed by HPLC using fluorescence detection. The plasma disposition of IVM given intravenously was unaffected by the presence of ITZ. However, the co-administration with ITZ resulted in markedly higher IVM plasma concentration profiles compared to the control group. Likewise, the presence of ITZ enhanced the IVM concentration profiles in the gastrointestinal mucosal tissues. An ITZ-induced reduction on the P-gp efflux activity at the intestinal lining may have accounted for the greater absorption and enhanced systemic availability observed for IVM in the intraruminally-treated animals.
Fil: Ballent, Mariana. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencias Veterinarias. Departamento de Fisiopatología; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Tandil; Argentina
Fil: Lifschitz, Adrian Luis. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencias Veterinarias. Departamento de Fisiopatología; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Tandil; Argentina
Fil: Virkel, Guillermo Leon. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencias Veterinarias. Departamento de Fisiopatología; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Tandil; Argentina
Fil: Sallovitz, Juan Manuel. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencias Veterinarias. Departamento de Fisiopatología; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Tandil; Argentina
Fil: Lanusse, Carlos Edmundo. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Tandil; Argentina. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencias Veterinarias. Departamento de Fisiopatología; Argentina
description Different pharmacological approaches have been used in an attempt to increased drug systemic availability of anthelmintic drugs. The comparative effect of the itraconazole (ITZ)-mediated modulation of P-glycoprotein (P-gp) activity on the in vivo kinetic behaviour of ivermectin (IVM) administered by intravenous (IV) and intraruminal (IR) routes to sheep was assessed in the current work. Corriedale sheep received IVM (50 µg/kg) by the intravenous (IV) route either alone (Group A) or co-administered with the P-gp modulator ITZ (100 mg orally three times every 12 h) (Group B). Animals in Groups C and D were intraruminally (IR) treated with IVM (50 µg/kg) alone or co-administered with ITZ (100 mg orally three times every 12 h), respectively. Jugular blood and gastrointestinal tissue samples (only of the IVM IR treated animals) were collected. The samples were analyzed by HPLC using fluorescence detection. The plasma disposition of IVM given intravenously was unaffected by the presence of ITZ. However, the co-administration with ITZ resulted in markedly higher IVM plasma concentration profiles compared to the control group. Likewise, the presence of ITZ enhanced the IVM concentration profiles in the gastrointestinal mucosal tissues. An ITZ-induced reduction on the P-gp efflux activity at the intestinal lining may have accounted for the greater absorption and enhanced systemic availability observed for IVM in the intraruminally-treated animals.
publishDate 2007
dc.date.none.fl_str_mv 2007-06
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
http://purl.org/coar/resource_type/c_6501
info:ar-repo/semantics/articulo
format article
status_str publishedVersion
dc.identifier.none.fl_str_mv http://hdl.handle.net/11336/112015
Ballent, Mariana; Lifschitz, Adrian Luis; Virkel, Guillermo Leon; Sallovitz, Juan Manuel; Lanusse, Carlos Edmundo; Involvement of P-glycoprotein on ivermectin kinetic behaviour in sheep: itraconazole-mediated changes on gastrointestinal disposition; Wiley Blackwell Publishing, Inc; Journal of Veterinary Pharmacology and Therapeutics; 30; 3; 6-2007; 242-248
0140-7783
CONICET Digital
CONICET
url http://hdl.handle.net/11336/112015
identifier_str_mv Ballent, Mariana; Lifschitz, Adrian Luis; Virkel, Guillermo Leon; Sallovitz, Juan Manuel; Lanusse, Carlos Edmundo; Involvement of P-glycoprotein on ivermectin kinetic behaviour in sheep: itraconazole-mediated changes on gastrointestinal disposition; Wiley Blackwell Publishing, Inc; Journal of Veterinary Pharmacology and Therapeutics; 30; 3; 6-2007; 242-248
0140-7783
CONICET Digital
CONICET
dc.language.none.fl_str_mv eng
language eng
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dc.publisher.none.fl_str_mv Wiley Blackwell Publishing, Inc
publisher.none.fl_str_mv Wiley Blackwell Publishing, Inc
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repository.mail.fl_str_mv dasensio@conicet.gov.ar; lcarlino@conicet.gov.ar
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