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Dr. Ji-qun Cai
Department of Pharmacology;Chapter 14
Sedatives, hypnotics and Anxiolytics
镇静催眠药和抗焦虑药;定义( Definitions )
镇静药:
降低人体的活动(度),抑制激动和兴奋,使人
趋向于平静。
催眠药:
产生困倦感, 加速进入睡眠,并能保持近似生
理的睡眠状态。
抗焦虑药:
解除患者焦虑、不安、兴奋和紧张 。
;睡眠的各个阶段Stages of Sleep;Stages of Sleep;Four Stages of Sleep;生物节律 Circadian Rhythms;;;What is the difference between Stage 1 Emergent Stage 1?
Only emergent stage 1 is there REM ?
REM sleep also called paradoxical 非常规 sleep (paradox that subjects slept while EEGs suggested wakefulness)
Stages 2, 3, 4 together (slow-wave sleep)
Stages 3 4 (delta sleep)
;Progression of EEG stages changes during typical nights sleep
Each cycle approximately 90 minutes long
As night progresses less time spent in stages 3 4 (more in REM sleep)
Brief periods of wakefulness--normally forgotten in the morning ;REM Sleep and Dreaming;Why Do We Sleep?;Why Do We Sleep?;REM Sleep and Dreaming;睡眠紊乱Sleep Disorders;Sleep Disorders ;Sleep Disorders;Night terrors – mostly occur in children, tend to go away with age. Child sits up in bed, screaming, unresponsive to stimuli. Usually occur in NREM sleep, unlike nightmares, which occur during REM.
Sleepwalking – person gets up and wanders about. Mostly seen in children and declines with age. Also occurs during NREM sleep.;镇静催眠药的历史
;镇静催眠药的分类;14.1苯二氮卓类; 3,抗惊厥抗癫痫:
可有效拮抗印防已毒素、荷包牡丹碱等的致惊厥作用。临床可用于治疗破伤风等疾病引起的惊厥,癫痫大发作的首选药物。;作用机理 ;药名;苯二氮卓类衍生物的药动学Pharmacokinetics
1 口服吸收良好
F =55---100
2 与血浆蛋白结合率为 77-99%
3 在体内部分药物可以产生活性代谢产物:
Flurezepam desalkylflurazepam
脱烷基西泮
(a long acting active metabolite);不良反应 Side effects:
1 一般来说安全 usually safe
excessive hypersomnias ataxia
(嗜睡) 共济失调
2 iv too fast cause CNS depression
3 addiction 成瘾;BDZ Receptor Antagonist
苯二氮卓受体结抗剂; 巴比妥类 Barbiturates weak acid
分类 Classification:
Drug t ?( h)
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