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抗胆碱药与胆碱酯酶复活剂在急性有机磷中毒治疗中的作用及相互作用

Actions and interactions of cholinolytics and cholinesterase reactivators in the treatment of acute organophosphorus toxicity.

作者信息

Das Gupta S, Ghosh A K, Chowdhri B L, Asthana S N, Batra B S

机构信息

Division of Pharmacology, Defence Research & Development Establishment, Gwalior, India.

出版信息

Drug Chem Toxicol. 1991;14(3):283-91. doi: 10.3109/01480549109002190.

DOI:10.3109/01480549109002190
PMID:1935707
Abstract

Different drug combinations consisting of cholinolytic and a cholinesterase (ChE) reactivator provide greater therapeutic efficacy in acute organophosphorus (OP) poisoning in mice than when used alone. Maximum protection, as determined by a shift of the LD50 for the two OP agents, was observed with the cholinolytic benactyzine. A protection index (P.I.) of 42 was obtained when benactyzine was given along with obidoxime in diisopropylphosphorofluoridate (DFP) intoxication. With the more toxic OP agent soman (o-pinacolylmethylphosphonofluoridate), the same cholinolytic only offered a maximum P.I. of 3.2 when administered with HS-6, another bispyridinium ChE reactivator. This beneficial effect of benactyzine is possibly due to its greater antimuscarinic effect in the central nervous system than atropine or dexetimide.

摘要

与单独使用相比,由抗胆碱药和胆碱酯酶(ChE)复活剂组成的不同药物组合在小鼠急性有机磷(OP)中毒中具有更高的治疗效果。通过两种OP剂的半数致死量(LD50)的变化确定,抗胆碱药苯那辛可提供最大保护。在二异丙基氟磷酸酯(DFP)中毒时,苯那辛与氯解磷定一起使用时,保护指数(P.I.)为42。对于毒性更强的OP剂梭曼(邻频哪基甲基膦酰氟),当与另一种双吡啶鎓ChE复活剂HS-6一起给药时,相同的抗胆碱药仅提供最大P.I.为3.2。苯那辛的这种有益作用可能是由于其在中枢神经系统中的抗毒蕈碱作用比阿托品或右苯丙胺更强。

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