论文部分内容阅读
以小鼠戊巴比妥钠睡眠时间,戊巴比妥钠在小鼠体内消失速率及大鼠肝切片对戊巴比妥钠的代谢为指标观察了几种药物对戊巴比妥钠转化的影响。按对戊巴比妥钠睡眠时间的影响,可将这些药物分为三类:甲类包括密尔通,苯妥英钠,苯海拉明,氨基比林,氯丁醇,氯丙嗪及3′-甲基奶油黄等已知的药物转化酶刺激剂,给这些药物后48小时,小鼠戊巴比妥钠睡眠时间缩短,但在给药后1小时睡眠时间延长。由于给这些药后1小时戊巴比妥钠在体内的消失延缓,以及当温孵液中含有6.6—17.0×10~(-4)M 时明显抑制大鼠肝切片对戊巴比妥钠的代谢,故这些药物延长睡眠时间的原因,至少部分由于抑制催眠药的生物转化。乙类药物只延长睡眠时间而不随后使之缩短,包括丙嗪,美沙酮,E605,安他布斯,PT-22,2-甲基奶油黄,奶油黄,牛胱胺,AET 及氮芥类化合物。其中美沙酮,E605,安他布斯及2-甲基奶油黄都经进一步证明能抑制戊巴比妥的转化,新恩比兴在给药后第3天有抑制作用,唯丙嗪并不延缓戊巴比妥钠在小鼠体内的消失。丙类包括阿司匹林,DFP,6-MP 及 8-氮杂鸟扁便嘌呤等,既不在给药后早期显著延长睡眠时间,也不在后期缩短睡眠时间。上述结果表明:凡药酶刺激剂,在给予动物的早期,必表现出对药酶的抑制作用;但药酶抑制剂在给予动物后晚期,对药酶不一定都有刺激作用。
The effects of sodium pentobarbital sodium on the sleep time of mice, the disappearance rate of sodium pentobarbital in mice and the metabolism of pentobarbital sodium in rat liver slices were observed. influences. These drugs are classified into three categories according to their effect on the sleep time of pentobarbital sodium: Group A includes Milliton, phenytoin sodium, diphenhydramine, aminopyrine, chlorobutanol, chlorpromazine and 3 ’ - Methyl Butyryl Yellow and other known drug-converting enzyme stimulants. After 48 hours of administration of these drugs, the mice were shortened by pentobarbital sodium, but the sleep time was prolonged by 1 hour after administration. Due to the delay in vivo elimination of pentobarbital sodium in one hour after the administration of these drugs and the significant inhibition of rat liver sections to sodium pentobarbital when containing 6.6-17.0 x 10 ~ (-4) M in warm incubation solution Metabolism, so the reason these drugs extend sleep time is at least partly due to the inhibition of the biotransformation of hypnotics. Class B drugs only prolonged sleep without subsequent shortening, including mesalamine, methadone, E605, amphetamines, PT-22, 2-methyl butagreen, cream yellow, cysteamine, AET and nitrogen mustards Compound. Among them, methadone, E605, Anabesi and 2-methyl Butyral were further proved to inhibit the conversion of pentobarbital, nembutir inhibition at 3 days after administration, Pentobarbital sodium in mice disappeared. Category C includes aspirin, DFP, 6-MP, and 8-azapyridine and purpurin, which neither significantly prolong or significantly reduce the amount of sleep in the early post-dose period. The above results show that: All drug enzyme stimulants, in the early administration of animals, will show the inhibition of drug enzymes; but drug enzyme inhibitors late in the administration of animals, the enzyme does not necessarily have a stimulating effect.