Data/hora: 11/05/2024 17:31:47

Biblioteca(s): | Embrapa Caprinos e Ovinos.
Data corrente: | 29/09/2008
Data da última atualização: | 08/07/2021
Autoria: | LANUSSE, C.; BALLENT, M. LIFCHITZ, A.
Afiliação: | Laboratorio de Farmacología, Facultad de Ciencias Veterinarias, Universidad Nacional del Centro. Campus Universitario, (7000) Tandil, Argentina.
Título: | Modulation of cellular drug efflux: impact on antiparasitic therapy.
Ano de publicação: | 2008
Fonte/Imprenta: | In: CONGRESSO BRASILEIRO DE PARASITOLOGIA VETERINÁRIA, 15.; SEMINÁRIO DE PARASITOLOGIA VETERINÁRIA DOS PAÍSES DO MERCOSUL, 2., 2008, Curitiba. Programa e resumos. Curitiba: UFPR: Universidade Estadual de Londrina, 2008. 12 f. 1 CD-ROM.
Idioma: | Inglês
Conteúdo: | The progress achieved on the comprehension of the relationship among disposition kinetics, tissue distribution and the patterns of drug uptake/metabolism by different target parasites has greatly contributed to optimize parasite control in livestock. In vivo and in vitro studies have demonstrated that P-glicoprotein (P-gp) functions as an energy dependent efflux pump for many chemotherapeutic compounds, including some antiparasitic drugs. At the intestinal level, P-gp can actively transport a wide range of structurally diverse compounds out of the cell, pumping them back into the intestinal lumen. Therefore, P-gp may be involved both in limiting enteric absorption and facilitating intestinal secretion of different compounds, being an important determinant of drug systemic bioavailability. Different pharmacological approaches to delay the P-gp-mediated bile/intestinal secretions and to extend the plasma-intestine recycling time of the macrocyclic lactones (ivermectin, moxidectin) are currently being investigated. Their implications on the efficacy against resistant nematodes are under evaluation and some preliminary results are promissory.  On the other hand, some novel reported data reveal that a number of different P-gp´s are over-expressed in resistant Haemonchus contortus, and an enhanced drug efflux mechanism may be involved in the resistance of Fasciola hepatica to triclabendazole. Overall, the involvement of the efflux-transport protein P-gp (and perhaps other drug transporters) on both the pharmacokinetic disposition (host) and resistance mechanisms (target parasites) to different anthelmintic chemical groups, is described in the current article. Further work in the field is required to assess the practical pharmaco-parasitological implication of the chemical modulation of these cell efflux pump systems.
Palavras-Chave: | antiparasitic compounds; cellular efflux; Drug transport systems; P-glycoprotein.
Categoria do assunto: | H Saúde e Patologia
Registro original: | Embrapa Caprinos e Ovinos (CNPC)
Exemplares: | CNPC - (21275-1) - ADD - PC - DD - CD 00190 -  -  - DIS