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J Vet Pharmacol Ther. 2019 Sep;42(5):548-555. doi: 10.1111/jvp.12798. Epub 2019 Jul 22.

In vitro and in vivo effects of chlorpyrifos and cypermethrin on blood cholinesterases in sheep.

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Laboratorio de Ecotoxicología y Biología Celular, Facultad de Ciencias Veterinarias, UNCPBA, Tandil, Argentina.
Laboratorio de Farmacología, Centro de Investigación Veterinaria de Tandil (CIVETAN-CIC-CONICET), Facultad de Ciencias Veterinarias, UNCPBA, Tandil, Argentina.


The combination of the organophosphate (OP) chlorpyrifos (CPF) and the pyrethroid cypermethrin (CPM) is commonly marketed as pour-on formulations for the control of sheep lice, ked, and blowflies. CPF irreversibly inhibits acetylcholinesterases (AChE), while pyrethroids are not AChE inhibitors. However, combinations of pyrethroids with OPs showed a highly synergistic effect on AChE inhibition. Thus, the aim of the current work was to evaluate in vitro and in vivo the inhibitory potency of both pesticides, alone and in combination with AChE and butyrylcholinesterase (BChE) activities in sheep blood. In vitro, IC50 values were similar after CPF or CPF plus CPM incubations. The pour-on coadministration of recommended doses of CPF and CPM did not cause a significant inhibition of AChE and BChE in sheep blood. Only slight percentages of inhibition of their catalytic activities were observed when both drugs were given at 4-fold higher dose rates. The lower systemic availability of topical administration of OPs in sheep may help to explain the lower degree of inhibition of blood AChE and BChE in vivo. The results emerged from this research are a further contribution to the knowledge of the risks of implementing higher dosage regimens of OPs-containing antiparasitic formulations.


acetylcholinesterase; butyrylcholinesterase; chlorpyrifos; cypermethrin; organophosphates

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