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1、Chapter 11 Drugs for Psychiatric Disorders【Learning points】Section 1 Antipsychotics Mechanism:(1)Anti-dopamine D2 receptors in the midbrain-limb lobe and midbrain-cortex pathways(2)Anti 5-HT2 receptor Classification:Divided into phenothiazines,thioxanthenes,butyrylbenzenes and others.(1)Phenothiazin
2、es 1.Chlorpromazine【Pharmacological action and mechanism】(1)The antipsychotic effect can quickly control excitement and restlessness,and can restore the patients sanity,emotional stability,and self-care.The mechanism of action is related to blocking the dopamine D2 receptor in the midbrain-limb lobe
3、 and midbrain-cortex pathway.(2)Antiemetic effect,which is caused by blocking the D2 receptor of the emetic chemosensory zone(CTZ)in small doses;high dose directly inhibits the vomiting center But it is not effective for vomiting caused by stimulation of the vestibule.(3)The effect on body temperatu
4、re regulation,inhibiting the body temperature regulation center,making body temperature regulation malfunction,and the body temperature rises and falls with the change of the ambient temperature.With the cooperation of physical cooling,the body temperature can be reduced to below normal.(4)Action on
5、 autonomic nerves,blocking alpha adrenergic receptors-blood pressure drop,M choline receptors-dry mouth,constipation,blurred vision.(5)Effect on endocrine:hypothalamus releases prolactin inhibitory factor(PIF)prolactin(PRL)breast enlargement,gonadotropin(GNRH)follicle stimulating hormone(FSH),lutein
6、izing hormone LH),corticotropin,growth hormone.【Clinical application】(1)The curative effect of type I schizophrenia,which is mainly based on psychomotor excitement and hallucination delusions,is good,and the curative effect is poor for type II schizophrenia.It is also used to treat mania.(2)It is ef
7、fective for vomiting caused by various diseases and drugs,and stubborn hiccups are effective,so it cannot be used to treat motion sickness.(3)The combined use of dilbutin and promethazine is used in hypothermic anesthesia and artificial hibernation therapy.【Adverse reactions】(1)Common:Alpha receptor
8、 blocking effect:It can cause orthostatic hypotension and cannot be rescued by epinephrine.Block M receptor:dry mouth,constipation,blurred vision,increased intraocular pressure,tachycardia and other atropine-like effects.Glaucoma patients are disabled.(2)Extrapyramidal reactions:blocking the substan
9、tia nigra-striatal pathway D2 receptors,weakening the DA function in the striatum,and enhancing the function of ACh to cause extrapyramidal reactions,including Parkinsons syndrome,acute Dystonia and akathisia,another type of extrapyramidal reaction-delayed dyskinesia may be related to the long-term
10、use of drugs to cause up-regulation of dopamine receptors,anti-DA drugs can reduce this response.(3)Endocrine system reaction:D2 receptors that block the nodule-funnel pathway can cause endocrine disorders,causing breast enlargement and lactation,delayed ovulation,slowed growth,and sexual dysfunctio
11、n.(4)Mental disorders,convulsions and epilepsy.(5)Allergic reactions.(6)Acute poisoning.2.Others Clozapine:commonly used atypical antipsychotics Features:Strong antipsychotic effect,can improve the positive and negative symptoms of mental illness,and it is still effective in cases where other drugs
12、are ineffective,and takes effect quickly.There are few extrapyramidal reactions,nor endocrine disorders.Risperidone:blocking the D2 receptor and 5-HT2A receptor,is the second generation of atypical antipsychotics Section 2 Anti-manic depression drugs Lithium carbonate:(1)It has a significant effect
13、on the manic author.It can inhibit the release of NA and DA in the brain and promote its reuptake,reduce the concentration of NA in the synaptic space and resist mania.(2)Overdose can cause lithium salt poisoning,and the blood lithium concentration of the drug users should be monitored to exceed 2mo
14、l/l,that is,the symptoms of poisoning appear.Intravenous drip of saline can accelerate the excretion of lithium.Section 3.Depressive drugs(1)TCAs Imipramine(Mipamine)【Pharmacological action】(1)Features:Continuous medication for 2 to 3 weeks can show obvious antidepressant effect.It has M receptor bl
15、ocking effect on cardiovascular,causing orthostatic hypotension,tachycardia and arrhythmia.(2)The mechanism of action may be related to inhibiting the reuptake of NA and 5-HT by the presynaptic membrane,increasing the concentration of intersynaptic transmitters,and promoting the function of synaptic
16、 transmission.【Clinical Application】Mainly used in the treatment of various types of depression,treatment of enuresis,anxiety and phobia.Other tricyclic drugs are desipramine,amitriptyline,and doxepin.(2)NA uptake inhibitors Maprotiline:It is a broad-spectrum antidepressant,which mainly inhibits NA
17、reuptake.It has the characteristics of quick effect and little side effects.(3)5-HT reuptake inhibitors Fluoxetine:a selective 5-HT reuptake inhibitor,which has little effect on other transmitters and receptors,retains the similar curative effect as tricyclic antidepressants,overcomes many adverse reactions,treats depression,neurotic Bulimia.Paroxetine,sertraline,trazodone,etc.