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Título
Ivermectin inhibits ovine ABCG2-mediated in vitro transport of meloxicam and reduces its secretion into milk in sheep
Autor
Facultad/Centro
Área de conocimiento
Título de la revista
Research in Veterinary Science
Cita Bibliográfica
Blanco-Paniagua, E., Garcia-Lino, A. M., Alvarez-Fernández, L., Alvarez, A. I., & Merino, G. (2022). Ivermectin inhibits ovine ABCG2-mediated in vitro transport of meloxicam and reduces its secretion into milk in sheep. Research in Veterinary Science, 153, 88-91. https://doi.org/10.1016/J.RVSC.2022.10.019
Editorial
Elsevier
Fecha
2022
ISSN
0034-5288
Resumen
[EN] The ATP-binding cassette transporter G2 (ABCG2) is an efflux protein involved
in the bioavailability and secretion into milk of several compounds including anti
inflammatory drugs. The aim of this work was to determine the effect in sheep of an
ABCG2 inhibitor, such as the macrocyclic lactone ivermectin, on the secretion into milk
of meloxicam, a non-steroidal anti-inflammatory drug widely used in veterinary
medicine, and recently reported as an ABCG2 substrate. In vitro meloxicam transport
assays in ovine ABCG2-transduced cells have shown that ivermectin is an efficient
inhibitor of in vitro transport of meloxicam mediated by ovine ABCG2, with a 75%
inhibition in the transport ratio (24.85 ± 4.62 in controls vs 6.31 ± 1.37 in presence of
ivermectin). In addition, the role of ovine ABCG2 in secretion into milk of meloxicam
was corroborated using Assaf lactating sheep coadministered with ivermectin. Animals
were administered subcutaneously with meloxicam (0.5 mg/kg) with or without
ivermectin (0.2 mg/kg). No difference in plasma pharmacokinetic parameters was found
between treatments. In the case of milk, a significant reduction in the area under
concentration-time curve (AUC) (3.92 ± 0.66 vs 2.26 ± 1.52 vs μg·h/mL) and the AUC
milk-to-plasma ratio (0.17 ± 0.03 vs 0.09 ± 0.06) was reported for ivermectin-treated
animals compared to controls.
Materia
Palabras clave
Peer review
SI
ID proyecto
- info:eu-repo/grantAgreement/MINECO/Programa Estatal de I+D+I Orientada a los Retos de la Sociedad/AGL2015-65626-R
- info:eu-repo/grantAgreement/AEI/Programa Estatal de I+D+i Orientada a los Retos de la Sociedad/RTI2018-100903-B-I00
URI
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