论文部分内容阅读
力可拉敏季铵化后,对外周胆碱能效应器的作用约增强10倍,但对小鼠,家兔和猫的急性毒性作用却是明显减弱。季铵力可拉敏的治疗指数比叔胺力可拉敏大28倍,比加兰他敏大10倍,比新斯的明大22.4倍。它对血压、呼吸的影响也比叔胺力可拉敏弱,故其治疗安全范围最大。叔胺力可拉敏对家兔自发脑电活动有明显影响,能使脑电产生类似于惊醒反应的低幅快波。大剂量季铵力可拉敏亦无此作用。给猫侧脑室内注射季铵与叔胺力可拉敏后,外观行为变化类似,表明季铵化后,不易通过血脑屏障到达中枢神经系统。季铵力可拉敏抑制胆碱酯酶作用比叔胺稍强,但对横纹肌的作用增强10倍,两者之间无平行关系。新斯的明对猫慢性去神经支配腓肠肌有直接兴奋作用,力可拉敏、加兰他敏则均无此作用,提示它们加强横纹肌颤搐的作用机理有别。
Ricramidal quaternization, the role of peripheral cholinergic effect increased about 10-fold, but on mice, rabbits and cats acute toxicity was significantly weakened. The therapeutic index of quaternary ammonium potenable was 28 times larger than that of tertiary amine, 10 times larger than galantamine and 22.4 times larger than neostigmine. Its impact on blood pressure and respiration is also weaker than that of tertiary amines, so the safe range of treatment is the largest. Tertiary amine force can pull sensitive to spontaneous EEG activity in rabbits have a significant effect, can make the brain electrical shock similar to the slow wave response. High-dose quaternary ammonium pull-sensitive also does not have this effect. After intravenous administration of quaternary ammonium and tertiary amikacin to cats, the changes in appearance behavior were similar, indicating that it is not easy to reach the central nervous system through the blood-brain barrier after quaternization. Quaternary ammonium potenable to inhibit the role of cholinesterase slightly stronger than the tertiary amine, but the role of striated muscle enhanced 10-fold, no parallel relationship between the two. Neostigmine had a direct excitatory effect on the chronic denervation of the gastrocnemius muscle of cats, and no effect was observed on levamisole and galantamine, suggesting that their mechanism of action to strengthen the rhabdomyolus twitch is different.