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Chapter 6 Antipsychotic drugs

Chapter 6 Antipsychotic drugs. Jining Medical College School of Mental Health Zhai Jinguo. Main Points. Grasp ： Therapeutic indications of antipsychotics Common side effects and treatment Clinical treatment methods

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Chapter 6 Antipsychotic drugs

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  1. Chapter 6Antipsychotic drugs Jining Medical College School of Mental Health Zhai Jinguo

  2. Main Points • Grasp： Therapeutic indications of antipsychotics Common side effects and treatment Clinical treatment methods • Familar：The pharmacological effects of different antipsychotics • Understand ：Classificationof antipsychotics

  3. Classification of psychopharmaca • Antipsychotics • Antidepressants • Antimanic drugs (Mood stabilizers) • Antianxiety drugs (anxiolytics) • Psychostimulants • Hypnotics • Nootropic drugs

  4. New Words • Antipsychotic drugs/agents Antipsychotics 抗精神病药 • neuroleptics 神经阻滞剂 • Typical antipsychotics 典型抗精神病药 • Atypical antipsychotics 非典型抗精神病药 • Potency 效价 • Extrapyramidal syndrome(EPS) 锥体外系反应 • Hyperprolactinemia 高催乳素血症 • Acute dystonia 急性肌张力障碍 • Akathisia 静坐不能 • Parkinsonism 类帕金森症 • Tardive dyskinesia (TD) 迟发性运动障碍 • Neuroleptic Malignant Syndrome(NMS)恶性综合征

  5. New Words • Clozapine 氯氮平 • Risperidone 利培酮 • Olanzapine 奥氮平 • Quetiapine 喹硫平 • Ziprasidone 齐拉西酮 • Aripiprazole 阿立派唑 • Sertindole 舍吲哚 • Perospirone 哌罗匹隆 • Chlorpromazine 氯丙嗪 • Haloperidol 氟哌啶醇 • Perphenazine 奋乃静 • Thioridazine 硫利达嗪 • Sulpiride 舒必利

  6. New Words • psychopathology • hallucination • delusion • apathy • withdrawal • schizophrenia • bipolar disorder • Pharmacodynamics 药效动力学 • Pharmacokinetics药代动力学

  7. New Words • dopamine • dopaminergic • serotonin • Serotonergic • muscarine毒蕈碱 • muscarinic毒蕈碱的 • epinephrine肾上腺素/ adrenaline • adrenergic肾上腺素能的 • norepinephrine去甲肾上腺素 • histamine组胺 • histaminergic组胺能的 • antagonist • agonist • enzyme

  8. New Words • Phenothiazines 酚噻嗪类 Chlorpromazine • benzamides 苯酰胺类 sulpiride • butyrophenones 丁酰苯类haloperidol • dibenzoxazepines 二苯氧氮平类 (loxapine) • dihydroindolones二氢吲哚酮类(molindone ) • diphenylbutylpiperidines 二苯丁基哌啶类(pimozide)

  9. Definition • Antipsychotics are mainly given to control symptoms of schizophrenia and other kinds of psychosis. • 抗精神病药（antipsychotic drugs）主要用于治疗精神分裂症和其他具有精神病性症状的精神障碍。这类药物，在通常治疗剂量时，不影响意识和智能，能有效地控制精神病患者的精神运动性兴奋、幻觉妄想、敌对情绪、思维障碍和奇特行为等精神症状。除此之外，尤其新一代药物还可以改善动力低下和社会退缩等精神分裂症的阴性症状。

  10. History of antipsychotics

  11. History of antipsychotics • 20世纪50年代初: Chlorpromazine Rhone-Poulenc-Specia实验室 France • 1958:保罗·杨森 Haloperidol • 1958瑞士clozapine，1972年在瑞士和奥地利上市 • 20世纪70年代:sulpiride • 20世纪90年代:Risperidone，Quetiapine，Ziprasidone • 2002年11月FDA批准aripiprazole

  12. History of antipsychotics in America 电休克等 奥氮平 喹硫平 氯丙嗪 阿立哌唑 氟奋乃静 利培酮 氯氮平 甲硫达嗪 齐拉西酮 氟哌啶醇 氯氮平 1950 1960 1970 1980 1990 2000 2002

  13. The Classification of Antipsychotic Drugs • Antipsychotic drugs have been classified into typical or first-generation antipsychotics and atypical or Second-generation antipsychotics. • Typical antipsychotic drugs are those which produce extrapyramidal side-effects at clinically effective doses in the majority of patients. • Atypical antipsychotic drugs are those with a significantly lower propensity to produce extrapyramidal side-effects at clinically effective doses.

  14. Classificationby Pharmacological effects

  15. New Classificationof Antipsychotics Maguire G. Journal of Clinical Psychiatry. 2002. 63 (Suppl 4): 56-62.

  16. M1 1 H1 conventional antipsychotic drug D2 First-generation antipsychotics

  17. Stahl S M, Essential Psychopharmacology (2000) pure D2 blocker

  18. 5HT2A D2 Second-generation antipsychotics SDA

  19. 5HT1A 1 M1 H1 5HT2A D1 5HT2C D3 5HT3 clozapine 5HT6 D4 D2 5HT7 Multi-acting receptor targeted agents

  20. 1 M1 H1 5HT2A D1 5HT2C D3 5HT3 olanzapine 5HT6 D4 D2 Stahl S M, Essential Psychopharmacology (2000) Multi-acting receptor targeted agents

  21. 1 H1 5HT2A 2 quetiapine 5HT6 D2 5HT7 Stahl S M, Essential Psychopharmacology (2000) Multi-acting receptor targeted agents

  22. Classification of typical antipsychotic drugs according to potency • Low-potency agents are those in which the usual dose range in schizophrenia is equal to or greater than 200 mg/day. e.g. chlorpromazine, sulpiride 镇静作用强、抗胆碱能作用明显、对心血管和肝脏毒性较大、锥体外 系副作用较小、治疗剂量较大。 • High-potency agents are those in which the dose range is between 2 and 120 mg/day . e.g. haloperidol, perphenazine 镇静作用较弱、对心血管和肝脏毒性小、锥体外系副作用较大、治疗 剂量较小。

  23. Classificationby chemical structure

  24. 吩噻嗪类 丁酰苯类 硫杂蒽类 二苯二氮卓类 苯甲酰胺类

  25. According to pharmacological action • Serotonin-dopamine antagonists, SDAs: Risperidone, ziprasidone, sertindole • Multi-acting receptor targeted agents: MARTAs，clozapine, olanzapine, quetiapine, zotepine • Selective D2/D３receptors antagnists: amisulpride，remoxipride • D2、5-HT1A受体部分激动剂和5-HT2A受体拮抗剂: aripiprazole

  26. Pharmacodynamics药效动力学Pharmacokinetics药代动力学

  27. Pharmacological mechanism of antipsychotics • DA receptor blocker role • 5-HT receptor blocker role • 1 receptor blocker role • M1 cholinergic receptor blocker role • H1 histamine receptor blocker role Theraputic effects Side effects

  28. M1 1 H1 First-generation antipsychotics D2 Stahl S M, Essential Psychopharmacology (2000) 11-7

  29. 5HT2A D2 Second-generation antipsychotics

  30. 5HT1A 1 M1 H1 5HT2A 2 D1 5HT2C D3 5HT3 clozapine 5HT6 D4 D2 5HT7 multi-acting receptor targeted agents，MARTAs

  31. 1 M1 H1 5HT2A D1 5HT2C D3 5HT3 olanzapine 5HT6 D4 D2

  32. 1 H1 5HT2A 2 quetiapine 5HT6 D2 5HT7 Stahl S M, Essential Psychopharmacology (2000) 11-41

  33. Dopamine Pathways Basal Ganglia Nucleus accumbens a Substantia nigra c b hypothalamus d Tegmentum

  34. 大脑的多巴胺能递质系统 基底核 黑质纹状体通路 中脑皮质通路 黑质 中脑边缘通路 下丘脑 被盖区 结节漏斗通路

  35. Dopamine Pathways a. Nigrostriatal Pathway（黑质-纹状体通路）: EPS b. Mesolimbic Pathway（中脑-边缘通路）： 阳性症状 c. Mesocortical Pathway（中脑-皮层通路）： 阴性症状 心境症状 认知症状 d. Tubero Infundibular Pathway（结节-漏斗通路）：催乳素 J Clin Psych 1998(16) (monograph)

  36. EPS Stahl S M, Essential Psychopharmacology (2000) Nigrostriatal pathway （黑质-纹状体通路）

  37. Blockade of receptors in the nigrostriatal dopamine pathway causes them to up-regulate This up-regulation may lead to tardive dyskinesia Stahl S M, Essential Psychopharmacology (2000)

  38. Mesolimbic Pathway （中脑-边缘通路） mesolimbic overactivity = positive symptoms of psychosis Stahl S M, Essential Psychopharmacology (2000)

  39. Stahl S M, Essential Psychopharmacology (2000) primary dopamine deficiency Mesocortical Pathway （中脑-皮层通路） D2 receptor blockade increase in negative symptoms secondary dopamine deficiency

  40. Prolactin levels rise Tuberoinfundibular pathway （结节-漏斗通路）

  41. 预防EPS • 黑质纹状体通路 • 促进多巴胺释放 改善认知 改善 抑郁 症状 • 中脑皮质通路 • 促进多巴胺释放 保留 抗精神病 作用 • 中脑边缘通路 • 多巴胺释放不受影响 5-HT receptor blocker role 非典型抗精神病药物是5-HT2A受体的拮抗剂

  42. M1 INSERTED blurred vision constipation LAXATIVE dry mouth drowsiness Stahl S M, Essential Psychopharmacology (2000)

  43. H1 INSERTED drowsiness weight gain Stahl S M, Essential Psychopharmacology (2000)

  44. 1 INSERTED decreased blood pressure dizziness drowsiness Stahl S M, Essential Psychopharmacology (2000)

  45. 抗精神病药物的受体结合及临床作用 Adapted from: Richelson e. J Clin Psychiatry 1996; 57(suppl 11): 4-11. Pickar D. Lancet 1995; 345:557-562

  46. Therapeutical effect of antipsychotics • Antipsychotic action Positive symptoms Negative symptoms Cognitive symptoms Affective symptoms • Non-specific sedation • Prevent recurrence and relapse

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