Ichikawa S, Goto T, Umetsu N
Naruto Research Center, Otsuka Chemical Co., Ltd., Tokushima, Japan.
J Toxicol Sci. 1995 May;20(2):143-8. doi: 10.2131/jts.20.143.
The antidotal action of atropine sulfate and 2-pyridine aldoxime methiodide (2-PAM) against poisoning attributable to the new procarbamate insecticide benfuracarb [(ethyl N-[2,3-dihydro-2,2-dimethylbenzofuran-7-yloxycarbonyl (methyl) aminothio]-N-isopropyl-beta-alaninate] was compared utilizing rats as our experimental model. Both the intraperitoneal and oral administrations of these antidotes were examined after five, ten, fifteen and thirty minutes exposure periods, following treatment with benfuracarb at dose levels approximating LD50 and LD100. The results obtained demonstrate that both the intraperitoneal and oral administrations of atropine sulfate blocked or significantly reduced the toxic effects of benfuracarb and protected the animals from death. The intraperitoneal administration route appears to be more effective than was the oral route. In addition, the administration of atropine sulfate after the shorter period (up to 15 minutes), following exposure to benfuracarb, improved antidotal action, particularly with the LD100 dose of benfuracarb. It is suggested that atropine sulfate antagonizes benfuracarb poisoning by blocking acetylcholine (ACh) receptors, as many other carbamate insecticides, since benfuracarb was an in vivo cholinesterase (ChE) inhibitor and the toxic effect of benfuracarb was reduced by atropine sulfate. 2-PAM, however, did not significantly block or reduce the toxic effects of benfuracarb.
以大鼠作为实验模型,比较了硫酸阿托品和碘解磷定(2 - PAM)对新型氨基甲酸酯类杀虫剂丙硫克百威[(乙基N - [2,3 - 二氢 - 2,2 - 二甲基苯并呋喃 - 7 - 基氧基羰基(甲基)氨基硫代] - N - 异丙基 - β - 丙氨酸酯]中毒的解毒作用。在用接近半数致死量(LD50)和致死量100(LD100)的丙硫克百威处理后,分别在暴露5、10、15和30分钟后检查了这些解毒剂的腹腔注射和口服给药情况。所得结果表明,硫酸阿托品的腹腔注射和口服给药均能阻断或显著降低丙硫克百威的毒性作用,并保护动物免于死亡。腹腔给药途径似乎比口服途径更有效。此外,在接触丙硫克百威后的较短时间(长达15分钟)内给予硫酸阿托品,可增强解毒作用,尤其是在丙硫克百威LD100剂量时。由于丙硫克百威是一种体内胆碱酯酶(ChE)抑制剂,且硫酸阿托品可降低丙硫克百威的毒性作用,因此提示硫酸阿托品与许多其他氨基甲酸酯类杀虫剂一样,通过阻断乙酰胆碱(ACh)受体来拮抗丙硫克百威中毒。然而,2 - PAM并未显著阻断或降低丙硫克百威的毒性作用。