Matsubara T, Horikoshi I
J Pharmacobiodyn. 1983 Oct;6(10):699-707. doi: 10.1248/bpb1978.6.699.
We investigated antidotal effects of nine drugs against acute fenitrothion poisoning in rats. The antidotal effects were evaluated by a relief from toxic signs, an increased survival ratio and a prolonged surviving time. In the poisoning with approximate LD50 fenitrothion (500 mg/kg), oximes such as 2-PAM (2-pyridine aldoxime methiodide) and TPMM (1-(methyl morphorinium)-3-(4-hydroxyiminomethylpyridinium) propane dibromide), diphenhydramine and parasympatholytics such as atropine, scopolamine and biperiden significantly increased survival ratio and/or prolonged surviving time. These effective drugs did not sufficiently depress the toxic signs, except that the parasympatholytics markedly blocked salivation, miosis and motor ataxia. In contrast, reduced glutathione and central depressants such as diazepam and phenobarbital made the poisoning serious. In the poisoning with 100% lethal dose of fenitrothion (800 mg/kg), the parasympatholytics were more effective than 2-PAM and diphenhydramine, and they elevated the survival ratio up to 20-40%. The best therapy against the severe poisoning with 100% lethal dose of fenitrothion was confirmed to be the repeated and combined treatment with atropine and 2-PAM as established in parathion poisoning, resulting in 90% survival ratio and considerable alleviation from the toxic signs.
我们研究了九种药物对大鼠急性杀螟硫磷中毒的解毒作用。通过观察中毒症状的缓解情况、存活率的提高以及存活时间的延长来评估解毒效果。在用近似半数致死量的杀螟硫磷（500毫克/千克）进行中毒实验时，肟类药物如2-吡啶醛肟甲基碘（2-PAM）和1-(甲基吗啡啉)-3-(4-羟基亚胺甲基吡啶)丙烷二溴化物（TPMM）、苯海拉明以及副交感神经阻滞剂如阿托品、东莨菪碱和安克痉显著提高了存活率和/或延长了存活时间。除了副交感神经阻滞剂明显抑制流涎、瞳孔缩小和运动性共济失调外，这些有效药物并未充分减轻中毒症状。相比之下，还原型谷胱甘肽以及中枢抑制剂如地西泮和苯巴比妥则使中毒情况加重。在用100%致死剂量的杀螟硫磷（800毫克/千克）进行中毒实验时，副交感神经阻滞剂比2-PAM和苯海拉明更有效，它们将存活率提高到了20%-40%。事实证明，针对100%致死剂量杀螟硫磷严重中毒的最佳治疗方法是按照对硫磷中毒所确立的那样，重复联合使用阿托品和2-PAM进行治疗，从而使存活率达到90%，并使中毒症状得到显著缓解。
