抗凝血灭鼠剂大隆和鼠得克的生物学效果评价

大隆(brodifacoum)和鼠得克(difenacoum)是1975-1976年新发展的第二代抗凝血灭鼠剂,化学名称分别为3-(3-(对溴联苯基)-1,2,3,4-四氢化萘基)-4-羟基香豆素和3-(3-联苯基-1,2,3,4-四氢化萘基)-4羟基香豆素。这一类抗凝血灭鼠剂有2个突出的特性:(1)能杀灭抗药性鼠种,指对杀鼠灵(warfarin)产生抗药的鼠种,(2)兼有急性和慢性灭鼠剂的优点,单剂量对多种鼠类都有防制效果。这样不仅可以解决鼠类对杀鼠灵的抗药问题,而且可以节约灭鼠用粮和人力,有可能使抗凝血灭鼠剂推广用于防制野鼠。根据全国除四害规划安排,军事医学科学院微生物流行病研究所于1979年合成了这2种灭鼠剂样品,供全国新药协作组15个单位进行生物学效果评价。本文为部份试验结果。

THE BIOLOGICAL EVALUATION OF BRODIFACOUM AND DIFENACOUM

Biological evaluation of second generation anticoagulants, brodifacoum and difenacoum, was carried out in 1980-1981. The samples of these anticoagulants were synthesized by Institute of Microbiology and Epidemiology Academy of Military Medical Sciences.Determinations of acute ( single dose ) and chronic( 5 consecutive daily doses ) oral toxicities were performed on Rattus norvegicus, R. flavipectus, Mus musculus, R, losea, Apodemus chevrieri, Cricetus triion, Microtus brandti, Meriones unguicula-tus, Citellus dauricus and Ochotona curzonise, etc.Meriones unguiculatus and Citellus dauricus are very sensitive to brodifacoum. The values of LD₅₀ are as low as 0.003mg/kg and 0.093mg/kg respectively. Cricetus triton and Microtus brandti are very resistant to difenacoum. The values of LD₅₀ are as high as 112.4mg/kg and 29.96mg/kg respectively.