Sedative-Hypnotic Drugs
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Sedative-Hypnotic Drugs. CHEN Zhong 陈 忠 Department of Pharmacology, College of Pharmaceutical Sciences, Zhejiang University 医学院科研楼 B402-420 , 88208228. 2013.6. Sedatives (镇静药): 能缓和激动,消除躁动,恢复安静情绪的药物. Hypnotics (催眠药): 能促进和维持近似生理睡眠的药物.

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Sedative-Hypnotic Drugs

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Sedative-Hypnotic Drugs

CHEN Zhong 陈 忠Department of Pharmacology, College of Pharmaceutical Sciences, Zhejiang



Sedatives (镇静药):


Hypnotics (催眠药):




  • is characterized by excessive, exaggerated anxiety and worry about everyday life events with no obvious reasons for worry;

  • can be extremely debilitating, having a serious impact on daily life.


  • 1-5%, more in old women;

  • trouble in falling asleep or too easily to be waken up;

  • can be primary or secondary;

  • harmful to daily life: excessive daytime sleepiness and a lack of energy, feel anxious, depressed, or irritable.

Several kinds of sleep deficits

  • 无法入睡

  • 浅睡、易醒

  • 早醒

  • 睡后焦虑、烦躁

  • 梦游

  • 嗜睡

  • 神经性睡眠障碍

What’s the mechanism?




stimulator pathway?

When should start drug treatment?

Why ethanol produce dual effect?

Stage 3 & 4, 统称为慢波睡眠

Molecular Neuropharmacology

A schematic drawing showing key components of the ascending reticular activating system (ARAS)

Circadian rhythm & Circadian control

SCN: suprachiasmatic nucleus


Sedative-Hypnotic Drugs

  • Benzodiazepines

    (BZ / BDZ, 苯二氮卓类)

  • Barbiturates (巴比妥类)

  • Others

A. Benzodiazepines


  • Oral absorption

  • Lipid solubility-dependent distribution, placental penetrability

  • Hepatic metabolism ---active metabolites

  • Urinary excretion

(5) Classification according to action duration


triazolam, laorazepam, oxazepam, etc

Medium and long-acting:

nitrazepam, chlordiazepoxide, flurazepam etc

A. Benzodiazepines

2. Mechanisms of actions

(1) Sites of action:mainly acts on limbic system and midbrain reticular formation.

(2) Interaction with GABAA receptor

Benzodiazepines bind to specific, high affinity sites on the cell membrane, which are separate from but adjacent to the receptor for -aminobutyric acid (GABA).

The binding of benzodiazepinesenhances the affinity of GABA receptor for this neurotransmitter, resulting in a more frequent opening of adjacent chloride channels.- coagonist

This in turn results inenhanced hyperpolarization(超极化)and further inhibition of neuronal firing.

Modulation mode of the central inhibitory transmitter GABA and the action sites of drugs

Action of the central inhibitory transmitter GABA on Cl- influx and the action sites of benzodiazepines (BDZs)

A. Benzodiazepines

Diazepam 地西泮(安定)






A. Benzodiazepines

1. Pharmacological effects and clinical uses

(1) Antianxiety

at small doses

acting on limbic system(边缘系统,杏仁核、海马)

(2) Sedative-hypnotic effects(作用于脑干)

at relatively larger doses, no anesthetic effect;

not remarkably affect on REM

used forinsomnia(失眠)andpreanesthetic medication



Stages 3 and 4 are deep sleep.

Growth hormone is released during these stages.

Stages 3

Slow wave sleep

A. Benzodiazepines

(3) Antiepileptic and anticonvulsant effects

Convulsion due various causes; status epilepticus(i.v.)

(4) Centrally acting muscle relaxant effect

Relaxing the spasticity of skeletal muscle, probably by increasing presynaptic inhibition in the spinal cord.

Used for the treatment of skeletal muscle spasms caused by central or peripheral diseases.

(5) Others

Amnesia (短暂性记忆缺失, i.v.)

Respiratory and CVS effects

A. Benzodiazepines

3. Adverse effects

(1) Central depression

Most common: drowsiness and confusion (potentiated by ethanol or other central depressants).

Ataxia (共济失调); cognitive impairment

Antagonized by BZ receptor antagonist flumazenil(氟马西尼)

(2) Tolerance and dependence

Withdrawal syndrome: central excitation

A. Benzodiazepines

(3) Others

local pain, respiratory and CVS reactions (i.v.)

teratogenic effects(致畸效应)

(4) Contraindications

Myasthenia gravis

Infants < 6 months

Pregnancy and lactation mothers

Elderly, heart/lung/liver/kidney dysfunction

A. Benzodiazepines

Other benzodiazepines

According to the metabolisms

  • Long-acting:

    diazepam, chlordiazepoxide (氯氮卓), flurazepam (氟西泮)

  • Intermediate-acting:

    Nitrozepam (硝西泮), flunitrozepam (氯硝西泮),

    oxazepam (奥沙西泮), estazolam (艾司唑仑)

  • Short-acting:triazolam (三唑仑)

B. Barbiturates

Phenobarbital 苯巴比妥

B. Barbiturates


  • Inducing hepatic enzymes

  • Alkalining urine: excretion 

  • 硫喷妥钠脂溶性极高,故易通过BBB,易发生再分布;

  • 苯巴比妥脂溶性低,不易在肝脏代谢;

  • 脂溶性高,血浆蛋白结合率高。

B. Barbiturates

2. Pharmacological effects and clinical uses

  • Sedative-hypnotic effects


    (2) Preanesthetic medication

    (3) Antiepileptic and anticonvulsant effects

B. Barbiturates

3. Adverse effects

(1) Central depression:including after effect (hangover “宿醉”)

(2) Tolerance and dependence:long-term uses

(3) Acute poisoning

supporting therapies

alkalizing urine


C. Others

  • Chloral hydrate 水合氯醛

    Sedative-hypnotic effects

    Anticonvulsant effect:usually used in children

  • Hydroxyzine 羟嗪(安泰乐)

  • Meprobamate 甲丙氨酯(眠尔通)

  • Buspirone丁螺环酮

  • Methaqualone安眠酮

C. Others

  • Antihistamines 抗组胺药

  • Ethanol 乙醇

  • Melatonin 褪黑素

In her circulation system:

8 % chloral hydrate (3% toxic level and 10% lethal level)

4.5 % Nembutal (pentobarbital)

(death level 1.5-4%)

In her stomach and duodenum:

No drug crystal found!




Central stimulants

  • Psychomotor stimulants

  • Respiratory center stimulants

A Psychomotor stimulants

Cortex stimulants

(mainly acting on cerebral cortex)

Xanthines:caffeine 咖啡因

Related drugs

Respiratory center stimulants

Direct stimulation:尼可刹米

Indirect stimulation (reflex)

Spinal cord stimulants:士的宁

A Psychomotor stimulants

Caffeine 咖啡因

A Psychomotor stimulants

1. Pharmacological effects

(1) Central stimulation

(2) CVS effects:cardiac stimulation, dilatation of vessels

(3) Relaxing smooth muscles:airways, GI

(4) Other effects:Gastric acid secretion, diuretic effect

(5) Mechanisms of action:inhibiting PDE- cAMP ;antagonizing A1 adenosine receptor & GABA receptor

A Psychomotor stimulants

2. Clinical uses

  • Central depression

  • Adjuvant of migraine (偏头痛) and antipyretic-analgesic drugs

    3. Adverse effects

  • Central excitation

  • Convulsion (overdose)

A Psychomotor stimulants

Methylphenidate 哌甲酯(利他灵)

  • used for central depression caused by drugs or diseases; mild depression;child hyperactivity; enuresis; etc.

    Meclofenoxate 甲氯芬酯(氯酯醒)

  • Adjuvant of central depressive diseases; enuresis; etc.

B Respiratory center stimulants

Nikethamide 尼可刹米

B Respiratory center stimulants

1. Pharmacological effects

  • Direct(respiratory centre)and indirect(reflex via chemoreceptor)stimulation

    2. Clinical uses

  • Respiratory failure

    3. Adverse effects

  • Elevation of BP, tachycardia, tremor, convulsion

B Respiratory center stimulants

Dimefline 二甲弗林 (回苏灵)

  • Direct stimulation


  • Indirect stimulation

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