RT info:eu-repo/semantics/article
T1 Ivermectin reduces secretion of meloxicam into milk by inhibition of ABCG2 transporter in sheep
A1 Blanco Paniagua, Esther
A1 García Lino, Alba María
A1 Álvarez Fernández, Laura
A1 Álvarez de Felipe, Ana Isabel
A1 Merino Peláez, Gracia
A2 Fisiologia
K1 Fisiología
K1 ABCG2
K1 Ivermectin
K1 Meloxicam
K1 Milk
K1 Sheep
AB [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.
PB Elsevier
LK https://hdl.handle.net/10612/17412
UL https://hdl.handle.net/10612/17412
NO 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
DS BULERIA. Repositorio Institucional de la Universidad de León
RD 01-jun-2024