...
首页> 外文期刊>Journal of applied toxicology >Prophylactic administration of non-organophosphate cholinesterase inhibitors before acute exposure to organophosphates: assessment using terbufos sulfone
【24h】

Prophylactic administration of non-organophosphate cholinesterase inhibitors before acute exposure to organophosphates: assessment using terbufos sulfone

机译:非有机磷酸胆碱酯酶抑制剂的预防施用在急性暴露于有机磷酸盐之前:使用Terbufos砜评估

获取原文
获取原文并翻译 | 示例
           

摘要

Poisoning with organophosphorus compounds (OPCs) poses a serious threat worldwide. OPC-induced mortality can be significantly reduced by prophylactic administration of reversible acetylcholinesterase (AChE) inhibitors. The only American Food and Drug Administration (FDA)-approved substance for such pre-treatment (to soman exposure) is presently pyridostigmine, although its efficacy is controversial. In search for more efficacious and broad-spectrum alternatives, we have assessed in vivo the mortality-reducing efficacy of a group of five compounds with known AChE inhibitory activity (pyridostigmine, physostigmine, ranitidine, tacrine and K-27), when given in equitoxic dosage (25% of LD01) 30 min before exposure to the OPC terbufos sulfone. Protection was quantified in rats by determining the relative risk of death (RR) using Cox analysis, with RR = 1 for animals given only terbufos sulfone, but no pre-treatment. All tested AChE inhibitors reduced terbufos sulfone-induced mortality significantly (p <= 0.05) as compared with the non-treatment group (RR = 1: terbufos sulfone only). Best in vivo protection from terbufos sulfone-induced mortality was achieved, when K-27 was given before terbufos sulfone exposure (RR = 0.06), which was significantly (P <= 0.05) superior to the pre-treatment with all other tested compounds, for example tacrine (RR = 0.21), pyridostigmine (RR = 0.28), physostigmine (RR = 0.29) and ranitidine (RR = 0.33). The differences in efficacy between tacrine, pyridostigmine, physostigmine and ranitidine were not statistically significant. Prophylactic administration of an oxime (such as K-27) in case of imminent OPC exposure may be a viable option. Copyright (C) 2013 John Wiley & Sons, Ltd.
机译:有机磷化合物(OPCS)中毒在全世界造成严重威胁。通过预防可逆乙酰胆碱酯酶(ACHE)抑制剂,可以显着降低OPC诱导的死亡率。唯一的美国食品和药物管理局(FDA) - 用于此类预处理(对Soman暴露)的批准物质是目前吡哆啶的,尽管其疗效是有争议的。在寻求更多有效和广谱的替代方案中,我们在舍士毒性给出时,我们已经评估了一组具有已知疼痛抑制活性的五种化合物(Pyridostigmine,Shateostigmine,Ranitidine,Tacrine和K-27)的死亡率降低的疗效在暴露于OPC Terbufos砜之前30分钟的剂量(LD01的25%)。通过确定使用COX分析的死亡(RR)的相对风险来定量保护,只有仅给予Terbufos砜的动物,但没有预处理。所有测试的ACHE抑制剂明显降低了Terbufos砜诱导的死亡率(P <= 0.05)与非处理基团相比(仅限RR = 1:Terbufos砜)相比。达到砜砜诱导的死亡率的最佳体内保护,当在Terbufos砜暴露之前给予K-27(RR = 0.06),这显着(p <= 0.05)优于与所有其他测试化合物的预处理,例如,Tacrine(RR = 0.21),吡啶甾啶(RR = 0.28),辐射术(RR = 0.29)和ranitidine(RR = 0.33)。鸡尾酒,吡吡甲基葡萄球菌,火虫和雷尼啶之间有效性的差异在统计学上没有统计学意义。在迫在眉睫的OPC暴露的情况下,预防肟(例如K-27)的施用可能是可行的选择。版权所有(c)2013 John Wiley&Sons,Ltd。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱:kefu@zhangqiaokeyan.com

京公网安备:11010802029741号 ICP备案号:京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有
  • 客服微信

  • 服务号