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1、第18章,抗精神失常药,药学系药理教研室,1,谢谢观赏,2019-6-29,Chapter 18,Antipsychotic disorders drugs,Zhu xiaoguang,2,谢谢观赏,2019-6-29,objecter,掌握 氯丙嗪的药理作用、作用机制、临床应用与主要不良反应等。熟悉 抗精神失常药的概念和分类; 其他抗精神病药的作用特点; 碳酸锂、米帕明的药理作用特点。了解 精神失常的概念、分型.,3,谢谢观赏,2019-6-29,Why ?,4,谢谢观赏,2019-6-29,神经兮兮,神经稀稀,神经搭错,5,谢谢观赏,2019-6-29,Neuropathy,psychop
2、athy,note,（神经病）,（精神病）,6,谢谢观赏,2019-6-29,Introduction,1、Concept,Psychotic disorders,various reason severe mental disorders .,7,谢谢观赏,2019-6-29,2、classification,1、schizophrenia 精神分裂症2、mania-depressive disorder 躁狂抑郁症 3、anxiety 焦虑症4、 others,8,谢谢观赏,2019-6-29,1）the most familiar, 2）inpatient 6070%;3）thought
3、 and behavior -cloven(分裂)4） limbic system (边缘系统) DA function.,Schizophrenia ( I type, II type ),9,谢谢观赏,2019-6-29,Mania-depressive disorder,mania,5-HT ,NA ,NA ,1） Mania-depressive,2）,depression,5-HT ,10,谢谢观赏,2019-6-29,3、anxiety,焦虑症,4、 others,青春期、 周期性、 更年期,11,谢谢观赏,2019-6-29,10月10日是世界精神卫生日,健康体魄,+,健康心理,
4、美好人生,12,谢谢观赏,2019-6-29,Classification of drugs,Antipsychotic drugs chlorpromazineAntimanic drugs lithium carbonateAntidepressants imipramineAnxiolytics diazepam,氯丙嗪,碳酸锂,米帕明,地西泮,13,谢谢观赏,2019-6-29,1 Antipsychotic Drugs,吩噻嗪类：chlorpromazine硫杂蒽类： chlorprothixene丁酰苯类： haloperidol其他类： sulpiride，clozapine,1
5、4,谢谢观赏,2019-6-29,chlorpromazine, CPZ 氯丙嗪 （wintermin 冬眠灵）, pharmacokinetics 1、po. slow and irregular, F variable , im. absorb quickly ； 2、pass BBB easily, distribution is wide (in brain higher) ; 3、metabolize mainly in liver ; 4、elimination： kidney.,15,谢谢观赏,2019-6-29,chlorpromazine, actions uses I. C
6、NS 1、Antipsychotic effects (抗精神病作用) characteristics 1) long use, cant produce tolerance ; 2) symptomatic treatment (对症治疗); 3) the onset of effect is slow ( 6W-6M).,16,谢谢观赏,2019-6-29,mechanism,four important dopaminergic pathways: 1) mesolimbic pathway 中脑边缘系统 2) mesocortical pathway 中脑皮质通路 3) nigrost
7、riatal pathway 黑质纹状体通路 4) tubero-infundibular pathway 结节漏斗通路,CPZ,() D2-R antipsychotic effects,17,谢谢观赏,2019-6-29,Clinical uses,sychotic disorder ： 1）schizophrenia- first choice; 2）other psychotic states: manic states; delirium (谵妄)states. no effect on depression.,( I typeII type ),18,谢谢观赏,2019-6-29,
8、2、Antiemetic effects (镇吐作用),Antiemetic effect is strong;But no effect on motion sickness. (晕动性呕吐),CPZ,low dosage,CTZ（催吐化学感受区）,(+),vomiting center,large dosage,vomit,chemoreceptor trigger zone,19,谢谢观赏,2019-6-29, nausea and vomit induced by uremia(尿毒症), cancer, pregnant toxemia(妊娠毒血症), radiation(辐射) a
9、nd some drugs. stubborn hiccup 顽固性呃逆,Clinical uses,20,谢谢观赏,2019-6-29,3、influence of temperature regulation,characteristics:1) temperature,normal person and patients with fever;,2) action correlative with environmental temperature (环境温度);,3） produce fever , dispel fever(散热).,21,谢谢观赏,2019-6-29,Clinica
10、l uses,1）hypothermal anesthesia 低温麻醉 2）artificial hibernation 人工冬眠 CPZ + pethidine(哌替啶) + promethazine (异丙嗪),hibernation mixture,22,谢谢观赏,2019-6-29,配合物理降温使体温降至34以下 机体进入“冬眠”状态。BMR，对各种病理刺激的反应性，组织对缺氧的耐受力 。,mostly used for 严重感染、中毒性休克、高热惊厥、甲状腺危象等辅助治疗。,人工冬眠,23,谢谢观赏,2019-6-29,4、 the effects of CNS depressan
11、ts,e.g. general anaesthetics, sedative-hypnotics, analgesics(镇痛药), alcohol, ,24,谢谢观赏,2019-6-29,II. autonomic nerve system,1、cardiovascular,(-) - R(-)血管运动中枢dilate the blood vessel directly,BP,orthostatic hypotension 体位性低血压,adrenaline reversal,cannot use in the hypertension:tolerance,2、(-) M R dry mou
12、th, constipation(便秘), blurred vision (视力模糊),25,谢谢观赏,2019-6-29,III. endocrine system,CPZ (-) D2-R (tubero-infundibular pathway) prolactin inhibitory factor (催乳素释放抑制因子) ; the secretion of growth hormone; the secretion of GnRH (促性腺激素); the secretion of ACTH ; ,（内分泌系统）,26,谢谢观赏,2019-6-29,adverse reaction
13、s,1、 common adverse reaction 1) CNS, 2) M-R , 3) -R : BP , orthostatic hypotension 4) local irritative(刺激性).,27,谢谢观赏,2019-6-29,2. extrapyramidal system reactions 锥体外系反应,1) parkinsonism 帕金森综合征 2) acute dystonia 急性肌张力障碍 3) akathisia 静坐不能 4) tardive dyskinesia 迟发性运动障碍,中枢抗胆碱药,CPZ () nigrostriatal pathwa
14、y D2-R,28,谢谢观赏,2019-6-29,3.allergic reactions 4.acute toxication po. large dose: 12 g / time， clinical symptoms： narcoma ，Bp shock， （麻醉性昏睡） cardiac damage, arrhythmia contraindications p.160,29,谢谢观赏,2019-6-29,brief summary,CPZ blocking,中脑-皮质通路D2-R中脑-边缘叶通路D2-R,抗精神病作用,黑质-纹状体通路DA-R,锥体外系反应,结节-漏斗通路DA-R,影
15、响内分泌,30,谢谢观赏,2019-6-29,other antipsychotic drugs p.161-163,硫杂蒽类 tardan 泰尔登 丁酰苯类 haloperidol 氟哌啶醇 其他口服长效类 penfluridol 五氟利多 sulpiride 舒必利 clozapine 氯氮平 risperidone 利培酮,31,谢谢观赏,2019-6-29,2 Antimanic drugs,lithium carbonate 碳酸锂 characteristics 1.absorbed well；wide distribution ； 2. Na+ enhance the excre
16、tion of Li+ ; incept Na+ renal discharge Li+ 3. onset of effect is slow, individual variation（个体差异）;,32,谢谢观赏,2019-6-29,4. mechanism is complex; p.1645. mania and the manic state of schizophrenia clinical first choice;6. adverse reaction safe margin is narrow; common adverse reaction acute toxication
17、: CNS() coma, death . withdrawal, treatment: iv. 0.9% NaCl,TDM important !,33,谢谢观赏,2019-6-29,3 Antidepressant drugs,Imipramine 米帕明（丙咪嗪） characteristics 1. po.absorbed well；wide distribution ； 2.Antidepressant selectivity high; action slow; normal-CNS() depressed-uplift (情绪高涨),34,谢谢观赏,2019-6-29,. mec
18、hanism： inhibit the reuptake of NA、5-HT in the brain. 4. Clinical uses: different types of depression, enuresis(遗尿症), anxiety and phobia(恐怖症).5. Adverse reactions: M-R (), CNS symptom drug interaction p.165,35,谢谢观赏,2019-6-29,Other drugs p.166-170,amitriptyline 阿米替林 maprotiline 马普替林 mianserin 米安色林 ,36,谢谢观赏,2019-6-29,1.Describe the actions and uses of CPZ.2. Please explain the effects and adverse reactions of CPZ by receptor theory.3. List the name used for mania or depressive.,questions,37,谢谢观赏,2019-6-29,38,谢谢观赏,2019-6-29,
