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Título
Ivermectin reduces secretion of meloxicam into milk by inhibition of ABCG2 transporter 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. (2023). Ivermectin reduces secretion of meloxicam into milk by inhibition of ABCG2 transporter in sheep. Research in Veterinary Science
Editorial
Elsevier
Fecha
2023
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 mice. In vitro meloxicam
transport assays in ovine ABCG2-transduced cells have shown that meloxicam is a
substrate of ovine ABCG2 and that ivermectin is an efficient inhibitor of in vitro transport
of meloxicam mediated by ovine ABCG2. 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). A significantly lower
concentration of meloxicam in milk was detected when ivermectin was coadministered,
revealing a major role of ABCG2 in the secretion into milk of meloxicam and a relevant
drug-drug interaction affecting this process. These results will contribute to the
understanding of the potential factors that modulate the transfer of anti-inflammatory
drugs into milk, opening their potential use in lactating ruminants, and the effect of drug
coadministration on the presence of milk residues of these compounds.
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