Perfil farmacocinético e eficácia contra Ctenocephalides felis felis e Rhipicephalus sanguineus do fipronil administrado pela via oral em cães

Detalhes bibliográficos
Autor(a) principal: Santos, Gabriela Carmelinda Martins dos
Data de Publicação: 2021
Tipo de documento: Tese
Idioma: por
Título da fonte: Biblioteca Digital de Teses e Dissertações da UFRRJ
Texto Completo: https://rima.ufrrj.br/jspui/handle/20.500.14407/9791
Resumo: O fipronil (FIP) é um ectoparasiticida da classe dos fenilpirazóis, usado na medicina veterinária sob a forma tópica. Apoiado pelas evidências da exposição humana não controlada ao FIP e aos danos ambientais causados a partir das formulações disponíveis no mercado, o seu uso como um fármaco para administração oral tem-se tornado promissor. Nesse estudo, a eficácia do FIP contra a pulga Ctenocephalides felis felis e o carrapato Rhipicephalus sanguineus e a sua farmacocinética e a do seu principal metabólito ativo, a fipronil-sulfona (SULF), foram avaliadas após a administração oral de comprimidos em três diferentes doses (2, 4 e 6 mg/kg) em cães da raça Beagle, em um único tratamento. Nas doses de 4 mg/kg (AUC0-t= 442,39 ± 137,35 µg/mL*h) e 6 mg/kg (AUC0-t= 421,32 ± 102,84 µg/mL*h), foi possível observar percentuais de eficácia médios de 100 e 99% para a pulga e de 95 e 98% para o carrapato, respectivamente, 48h após o tratamento. Nas três doses testadas nesse estudo, o FIP apresentou perfil de rápida absorção e metabolização e lenta eliminação. Os valores de Cmax (β = 0,7653) e AUC0-t (β = 0,3209) não aumentaram proporcionalmente com o aumento da dose. As CE90 estimadas para FIP + SULF foram de 1,30 µg/mL para C. felis felis e 2,16 µg/mL para R. sanguineus. A correlação dos dados farmacocinéticos e de eficácia do FIP deste estudo demonstrou o seu potencial para ser administrado via oral na forma de comprimidos para o controle de ectoparasitas em cães, encorajando o desenvolvimento de uma nova formulação, como uma alternativa mais segura para os animais, seres humanos e o meio ambiente, alinhado ao conceito de Saúde Única.
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spelling Santos, Gabriela Carmelinda Martins dosCid, Yara Peluso055.357.316-09http://lattes.cnpq.br/0788912635109182Scott, Fabio Barbour001.382.167-97Cid, Yara PelusoAzevedo, Thais Ribeiro CorreiaCortes, Wellington da SilvaKlafke, Guilherme MarcondesSarcinelli, Michelle Alvares082.988.956-65http://lattes.cnpq.br/27171411390325802023-12-21T18:44:24Z2023-12-21T18:44:24Z2021-08-27SANTOS, Gabriela Carmelinda Martins dos. Perfil farmacocinético e eficácia contra Ctenocephalides felis felis e Rhipicephalus sanguineus do fipronil administrado pela via oral em cães. 2021. 77 f. Tese (Doutorado em Ciências Veterinárias, Biotecnologia e Inovação Tecnológica em Medicina Veterinária) - Instituto de Veterinária, Departamento de Parasitologia Animal, Universidade Federal Rural do Rio de Janeiro, Seropédica, RJ, 2021.https://rima.ufrrj.br/jspui/handle/20.500.14407/9791O fipronil (FIP) é um ectoparasiticida da classe dos fenilpirazóis, usado na medicina veterinária sob a forma tópica. Apoiado pelas evidências da exposição humana não controlada ao FIP e aos danos ambientais causados a partir das formulações disponíveis no mercado, o seu uso como um fármaco para administração oral tem-se tornado promissor. Nesse estudo, a eficácia do FIP contra a pulga Ctenocephalides felis felis e o carrapato Rhipicephalus sanguineus e a sua farmacocinética e a do seu principal metabólito ativo, a fipronil-sulfona (SULF), foram avaliadas após a administração oral de comprimidos em três diferentes doses (2, 4 e 6 mg/kg) em cães da raça Beagle, em um único tratamento. Nas doses de 4 mg/kg (AUC0-t= 442,39 ± 137,35 µg/mL*h) e 6 mg/kg (AUC0-t= 421,32 ± 102,84 µg/mL*h), foi possível observar percentuais de eficácia médios de 100 e 99% para a pulga e de 95 e 98% para o carrapato, respectivamente, 48h após o tratamento. Nas três doses testadas nesse estudo, o FIP apresentou perfil de rápida absorção e metabolização e lenta eliminação. Os valores de Cmax (β = 0,7653) e AUC0-t (β = 0,3209) não aumentaram proporcionalmente com o aumento da dose. As CE90 estimadas para FIP + SULF foram de 1,30 µg/mL para C. felis felis e 2,16 µg/mL para R. sanguineus. A correlação dos dados farmacocinéticos e de eficácia do FIP deste estudo demonstrou o seu potencial para ser administrado via oral na forma de comprimidos para o controle de ectoparasitas em cães, encorajando o desenvolvimento de uma nova formulação, como uma alternativa mais segura para os animais, seres humanos e o meio ambiente, alinhado ao conceito de Saúde Única.CAPES - Coordenação de Aperfeiçoamento de Pessoal de Nível SuperiorFipronil (FIP) is an ectoparasiticide of the phenylpyrazole class, used in veterinary medicine in topical form. Supported by evidence of uncontrolled human exposure to FIP and environmental damage caused by commercially available formulations, its use as a medicine for oral administration has become promising. In this study, the effectiveness of FIP against the flea Ctenocephalides felis felis and the tick Rhipicephalus sanguineus and its pharmacokinetics and its main active metabolite, fipronil sulfone (SULF), were evaluated after oral administration of tablets in three different doses (2, 4 and 6 mg/kg) in Beagle dogs, in a single treatment. At doses of 4 mg/kg (AUC0-t= 442.39 ± 137.35 µg/mL*h) and 6 mg/kg (AUC0-t= 421.32 ± 102.84 µg/mL*h), it was possible to observe mean efficacy percentages of 100 and 99% for the flea and 95 and 98% for the tick, respectively, 48h after treatment. In the three doses tested in this study, FIP showed a profile of rapid absorption and metabolism and slow elimination. The values of Cmax (β = 0.7653) and AUC0-t (β = 0.3209) did not increase proportionally with increasing dose. The estimated EC90 for FIP + SULF was 1.30 µg/mL for C. felis felis and 2.16 µg/mL for R. sanguineus. The correlation of the FIP pharmacokinetic and efficacy data demonstrated its potential to be administered orally in the form of tablets for the control of ectoparasites in dogs, as a safer alternative for animals, humans and environment, aligned with the One Health concept.application/pdfporUniversidade Federal Rural do Rio de JaneiroPrograma de Pós-Graduação em Ciências VeterináriasUFRRJBrasilInstituto de VeterináriaFenilpirazóisOralFarmacocinéticaDoseEficáciaEctoparasitosPhenylpyrazolesPharmacokineticsEfficacyEctoparasitesMedicina VeterináriaPerfil farmacocinético e eficácia contra Ctenocephalides felis felis e Rhipicephalus sanguineus do fipronil administrado pela via oral em cãesPharmacokinetic profile and efficacy against Ctenocephalides felis felis and Rhipicephalus sanguineus of fipronil administered orally in dogsinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/doctoralThesisABINPET. Associação Brasileira da Indústria de Produtos para Animais de Estimação. 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dc.title.por.fl_str_mv Perfil farmacocinético e eficácia contra Ctenocephalides felis felis e Rhipicephalus sanguineus do fipronil administrado pela via oral em cães
dc.title.alternative.eng.fl_str_mv Pharmacokinetic profile and efficacy against Ctenocephalides felis felis and Rhipicephalus sanguineus of fipronil administered orally in dogs
title Perfil farmacocinético e eficácia contra Ctenocephalides felis felis e Rhipicephalus sanguineus do fipronil administrado pela via oral em cães
spellingShingle Perfil farmacocinético e eficácia contra Ctenocephalides felis felis e Rhipicephalus sanguineus do fipronil administrado pela via oral em cães
Santos, Gabriela Carmelinda Martins dos
Fenilpirazóis
Oral
Farmacocinética
Dose
Eficácia
Ectoparasitos
Phenylpyrazoles
Pharmacokinetics
Efficacy
Ectoparasites
Medicina Veterinária
title_short Perfil farmacocinético e eficácia contra Ctenocephalides felis felis e Rhipicephalus sanguineus do fipronil administrado pela via oral em cães
title_full Perfil farmacocinético e eficácia contra Ctenocephalides felis felis e Rhipicephalus sanguineus do fipronil administrado pela via oral em cães
title_fullStr Perfil farmacocinético e eficácia contra Ctenocephalides felis felis e Rhipicephalus sanguineus do fipronil administrado pela via oral em cães
title_full_unstemmed Perfil farmacocinético e eficácia contra Ctenocephalides felis felis e Rhipicephalus sanguineus do fipronil administrado pela via oral em cães
title_sort Perfil farmacocinético e eficácia contra Ctenocephalides felis felis e Rhipicephalus sanguineus do fipronil administrado pela via oral em cães
author Santos, Gabriela Carmelinda Martins dos
author_facet Santos, Gabriela Carmelinda Martins dos
author_role author
dc.contributor.author.fl_str_mv Santos, Gabriela Carmelinda Martins dos
dc.contributor.advisor1.fl_str_mv Cid, Yara Peluso
dc.contributor.advisor1ID.fl_str_mv 055.357.316-09
dc.contributor.advisor1Lattes.fl_str_mv http://lattes.cnpq.br/0788912635109182
dc.contributor.advisor-co1.fl_str_mv Scott, Fabio Barbour
dc.contributor.advisor-co1ID.fl_str_mv 001.382.167-97
dc.contributor.referee1.fl_str_mv Cid, Yara Peluso
dc.contributor.referee2.fl_str_mv Azevedo, Thais Ribeiro Correia
dc.contributor.referee3.fl_str_mv Cortes, Wellington da Silva
dc.contributor.referee4.fl_str_mv Klafke, Guilherme Marcondes
dc.contributor.referee5.fl_str_mv Sarcinelli, Michelle Alvares
dc.contributor.authorID.fl_str_mv 082.988.956-65
dc.contributor.authorLattes.fl_str_mv http://lattes.cnpq.br/2717141139032580
contributor_str_mv Cid, Yara Peluso
Scott, Fabio Barbour
Cid, Yara Peluso
Azevedo, Thais Ribeiro Correia
Cortes, Wellington da Silva
Klafke, Guilherme Marcondes
Sarcinelli, Michelle Alvares
dc.subject.por.fl_str_mv Fenilpirazóis
Oral
Farmacocinética
Dose
Eficácia
Ectoparasitos
topic Fenilpirazóis
Oral
Farmacocinética
Dose
Eficácia
Ectoparasitos
Phenylpyrazoles
Pharmacokinetics
Efficacy
Ectoparasites
Medicina Veterinária
dc.subject.eng.fl_str_mv Phenylpyrazoles
Pharmacokinetics
Efficacy
Ectoparasites
dc.subject.cnpq.fl_str_mv Medicina Veterinária
description O fipronil (FIP) é um ectoparasiticida da classe dos fenilpirazóis, usado na medicina veterinária sob a forma tópica. Apoiado pelas evidências da exposição humana não controlada ao FIP e aos danos ambientais causados a partir das formulações disponíveis no mercado, o seu uso como um fármaco para administração oral tem-se tornado promissor. Nesse estudo, a eficácia do FIP contra a pulga Ctenocephalides felis felis e o carrapato Rhipicephalus sanguineus e a sua farmacocinética e a do seu principal metabólito ativo, a fipronil-sulfona (SULF), foram avaliadas após a administração oral de comprimidos em três diferentes doses (2, 4 e 6 mg/kg) em cães da raça Beagle, em um único tratamento. Nas doses de 4 mg/kg (AUC0-t= 442,39 ± 137,35 µg/mL*h) e 6 mg/kg (AUC0-t= 421,32 ± 102,84 µg/mL*h), foi possível observar percentuais de eficácia médios de 100 e 99% para a pulga e de 95 e 98% para o carrapato, respectivamente, 48h após o tratamento. Nas três doses testadas nesse estudo, o FIP apresentou perfil de rápida absorção e metabolização e lenta eliminação. Os valores de Cmax (β = 0,7653) e AUC0-t (β = 0,3209) não aumentaram proporcionalmente com o aumento da dose. As CE90 estimadas para FIP + SULF foram de 1,30 µg/mL para C. felis felis e 2,16 µg/mL para R. sanguineus. A correlação dos dados farmacocinéticos e de eficácia do FIP deste estudo demonstrou o seu potencial para ser administrado via oral na forma de comprimidos para o controle de ectoparasitas em cães, encorajando o desenvolvimento de uma nova formulação, como uma alternativa mais segura para os animais, seres humanos e o meio ambiente, alinhado ao conceito de Saúde Única.
publishDate 2021
dc.date.issued.fl_str_mv 2021-08-27
dc.date.accessioned.fl_str_mv 2023-12-21T18:44:24Z
dc.date.available.fl_str_mv 2023-12-21T18:44:24Z
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
dc.type.driver.fl_str_mv info:eu-repo/semantics/doctoralThesis
format doctoralThesis
status_str publishedVersion
dc.identifier.citation.fl_str_mv SANTOS, Gabriela Carmelinda Martins dos. Perfil farmacocinético e eficácia contra Ctenocephalides felis felis e Rhipicephalus sanguineus do fipronil administrado pela via oral em cães. 2021. 77 f. Tese (Doutorado em Ciências Veterinárias, Biotecnologia e Inovação Tecnológica em Medicina Veterinária) - Instituto de Veterinária, Departamento de Parasitologia Animal, Universidade Federal Rural do Rio de Janeiro, Seropédica, RJ, 2021.
dc.identifier.uri.fl_str_mv https://rima.ufrrj.br/jspui/handle/20.500.14407/9791
identifier_str_mv SANTOS, Gabriela Carmelinda Martins dos. Perfil farmacocinético e eficácia contra Ctenocephalides felis felis e Rhipicephalus sanguineus do fipronil administrado pela via oral em cães. 2021. 77 f. Tese (Doutorado em Ciências Veterinárias, Biotecnologia e Inovação Tecnológica em Medicina Veterinária) - Instituto de Veterinária, Departamento de Parasitologia Animal, Universidade Federal Rural do Rio de Janeiro, Seropédica, RJ, 2021.
url https://rima.ufrrj.br/jspui/handle/20.500.14407/9791
dc.language.iso.fl_str_mv por
language por
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