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阿托品和梭曼对麻醉豚鼠体内肟HLö 7二甲磺酸盐药代动力学的影响。

Effects of atropine and soman on the pharmacokinetics of the oxime HLö 7 dimethanesulfonate in anesthetized guinea-pigs.

作者信息

Worek F, Klimmek R, Szinicz L

机构信息

Institut für Pharmakologie und Toxikologie, Sanitätsakademie der Bundeswehr, Garching, Germany.

出版信息

Drug Chem Toxicol. 1995 May-Aug;18(2-3):137-49. doi: 10.3109/01480549509014317.

Abstract

The respiratory and circulatory effects and the pharmacokinetics of the bispyridinium dioxime HLö 7 (30 mumol/kg) were investigated in guinea-pigs in combination with atropine (28.8 mumol/kg) or with atropine plus soman (0.44 mumol/kg = 5 x LD50). The pharmacokinetics and pharmacodynamics were studied in separate groups of animals. HLö 7 had only minor effects on circulation and respiration. HLö 7 plus atropine caused a transient, pronounced fall of blood pressure, tachycardia, and respiratory stimulation. The soman-induced bradycardia was completely restored by the antidotes, while respiration improved within a few minutes with the respiratory rate becoming stabilized at 50% of baseline. Plasma half-time (60-70 min), plasma clearance (6-7 ml.kg-1.min-1) and apparent volume of distribution (0.5-0.6 l/kg) of HLö 7 did not differ between the groups, i.e. atropine and soman did not affect the kinetics of the oxime.

摘要

在豚鼠中研究了双吡啶二肟HLö 7(30微摩尔/千克)与阿托品(28.8微摩尔/千克)或阿托品加梭曼(0.44微摩尔/千克 = 5倍半数致死量)联合使用时的呼吸和循环效应以及药代动力学。在不同组的动物中研究了药代动力学和药效学。HLö 7对循环和呼吸仅有轻微影响。HLö 7加阿托品导致血压短暂、显著下降、心动过速和呼吸刺激。解毒剂完全恢复了梭曼诱导的心动过缓,而呼吸在几分钟内有所改善,呼吸频率稳定在基线的50%。HLö 7的血浆半衰期(60 - 70分钟)、血浆清除率(6 - 7毫升·千克⁻¹·分钟⁻¹)和表观分布容积(0.5 - 0.6升/千克)在各实验组之间没有差异,即阿托品和梭曼不影响肟的动力学。

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