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1、Chapter 10 Sedative-Hypnotic【Learning points】1.Introduction to sedative hypnotics 1.Definition of sedative hypnotics 2.The sleep phase is non-rapid eye movement sleep(NREMS)and rapid eye movement sleep(REMS).3.Traditional sedative hypnotics Sedation occurs with increasing dose hypnosis drowsiness an
2、ticonvulsions anesthesia respiratory paralysis death.2.Benzodiazepines【Pharmacological action and clinical application】1.Anti-anxiety effect,small doses have good anti-anxiety effect,and diazepam is used for anxiety caused by various reasons.2.The sedative and hypnotic effect has little effect on RE
3、MS,and the compensatory rebound is less after withdrawal.3.Anticonvulsant effect,diazepam is the drug of choice for the status of epilepsy.4.Central muscle relaxation.5.Other temporary memory loss【Mechanism】The distribution of BDZ(benzodiazepine binding site)is cortex,and the limbic system is the mo
4、st dense,which is consistent with the GABAA receptor.1.Enhance GABAergic nerve transmission function and synaptic inhibition effect.2.Enhance the combination of GABA and GABAA receptors.3.The combination of benzodiazepine and BDZ promotes the binding of GABA and GABAA receptors,which increases the f
5、requency of Cl-channel opening and GABA-dependent effects.【In vivo process】Triazolam absorbs fastest;but the metabolites of most drugs are still active.【Adverse reactions】Large doses occasionally cause ataxia;excessive acute poisoning can cause coma and respiratory depression;intravenous injection h
6、as inhibitory effects on the cardiovascular;there is a certain tolerance,rebound and withdrawal reactions occur after withdrawal.【Special effect antidote】Flumazenil(BDZ blocker)3.Barbiturates【Clinical application】Such drugs need to be used until the sedative dose shows anxiolytic effect.Medium and l
7、ong-acting phenobarbital and pentobarbital are used to control the status of epilepsy,and ultra-short-acting thiopental sodium is used for intravenous anesthesia during minor surgery or endoscopy.【Mechanism】Prolonging the opening time of GABA-mediated chloride channels and increasing Cl-influx will
8、shorten REMS sleep,which is independent of GABA and can simulate the role of GABA.【Adverse reactions】Drug enzyme induction can accelerate the metabolism of other drugs and affect the efficacy of the drug.Stopping drugs is prone to rebound.4.Other sedative hypnotics Chloraldehyde hydrate:does not sho
9、rten REMS sleep,it is irritating to the stomach;it is used for patients with intractable insomnia or poor effect on other hypnotic drugs.Meprobamate(Mianertong),Grummet,and methaqualone:sedative and hypnotic effect,can be addictive after long-term use Buspirone:anti-anxiety effect,no sedation,muscle relaxation and anti-convulsant effect.Zolpidem,Zopiclone,Zaleplon:New non-benzodiazepine sedative hypnotic drugs.Addiction comparison:benzodiazepines Zopiclone Zolpidem Zaleplon.