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antipsychotic
Xinjiang medical university teaching plan home page
Item code: 16
Course Name Clinical Course of Pharmacology Specialty
Lecturer Hu Jian plans to spend 2 hours as a professional undergraduate.
Written by associate professor of professional and technical titles in September 2003.
Chapter Name Chapter 16 Time of Use of Antipsychotic Drugs
Academic goal
And requirements
To master the function, main clinical application and main adverse reactions of chlorpromazine, the representative drug of phenothiazine, and to be familiar with its mechanism of action. To understand the characteristics of perphenazine, chlorpromazine, haloperidol, imipramine and lithium carbonate.
Key and Difficult Points 1 Main Physiological Functions of Dopamine (DA) System in Brain II. Theory of hyperactivity of DA nervous system in schizophrenia III. 4. The relationship between chlorpromazine receptor blocking effect and clinical application and main adverse reactions. Theory of sodium 5- hydroxytryptamine disorder in manic depression. Characteristics of imipramine, lithium carbonate and other drugs.
course content
Update status
not have
Teaching methods and organizational teaching methods: explain the key points and difficulties with CAI courseware, and then summarize them with blackboard writing. The terminology is in English.
Organizational arrangement:
Methods: Arrange two classes: 1. The main physiological function of dopamine (DA) system in brain and the theory of hyperactivity of DA nervous system in schizophrenia (10 min).
2. The relationship between chlorpromazine receptor blocking effect and clinical application and major adverse reactions (50 minutes).
3. The theory of manic depression caused by 3.NA.5-HT disorder and the characteristics, pharmacology and clinical application of drugs such as imipramine and lithium carbonate (40 minutes).
Self-made electronic handouts and courseware by teaching means
Basic Textbooks and Reference Books Basic Textbooks: Fundamentals of Medical Pharmacology 5th Edition
Reference book: Pharmacology (seven-year program) Fundamentals of Pharmacology and Drug Treatment &; Clinical pharmacology
Collective lesson preparation introduces the core content in detail according to the requirements of the syllabus.
Signature of Audit Opinion of Director of Teaching and Research Section:
Chapter XVI Antipsychotic Drugs
Teaching objectives and requirements:
1. To master the function, main clinical application and main adverse reactions of chlorpromazine, the representative drug of phenothiazine, and to be familiar with its mechanism of action.
2. Understand the characteristics of perphenazine, chlorpromazine, haloperidol, imipramine, lithium carbonate and other drugs.
Key points and difficulties:
1. Main physiological functions of dopamine system in brain
2. Schizophrenia nervous system function theory.
3. The relationship between chlorpromazine receptor blocking effect and clinical application and main adverse reactions.
4. The theory of 5- hydroxytryptamine disorder in manic depression
5. Characteristics of imipramine, lithium carbonate and other drugs
Mental disorder is caused by many reasons, and it is a disease with abnormal psychological activities such as cognition, emotion, consciousness and behavior.
Drugs for the treatment of mental disorders are divided into:
1. Antischizophrenia drugs,
2. Antimanic and antidepressant drugs
3. Anti-anxiety drugs.
First, antipsychotic drugs (antipsychotics):
Mainly used to treat schizophrenia and mania. According to the chemical structure, it can be divided into phenothiazine, thiaanthracene, butyl benzene and so on.
Main physiological functions of dopamine (DA) system in (1) brain
1. Regulation of motor function of extrapyramidal system: substantia nigra-striatum DA pathway
2. Related to mental activities: DA pathways in midbrain-cerebral cortex and midbrain-limbic system.
3. Regulating the secretion of some hormones in pituitary gland: Nodule-infundibulum DA pathway
4. Participate in central vomiting reaction: DA system in medulla oblongata
(2) Pathogenesis: The function of DA system in brain is too strong.
Chlorpromazine (dongming)
(1) mechanism of action
1. Blocking DA receptor; Blocking DA receptors in different parts of the brain can not only produce antipsychotic or antiemetic effects, but also produce extrapyramidal adverse reactions.
2. Blocking α receptor
3. Blocking M receptor
(2), pharmacological action
1. Effects related to blocking dopamine receptor (D2)
① Antipsychotic effect ② Antiemetic effect ③ Endocrine system ④ Extrapyramidal system.
2. Effects related to blocking α receptor
① Sedative effect ② Reversing the pressor effect of adrenaline.
3. Effects related to blocking M receptor: dry mouth, constipation and blurred vision.
4. Others: ① Inhibition of thermoregulatory center; ② Inhibition of vascular motor center; ③ Strengthen the function of central depressants.
(3) Clinical application
1. Antipsychotic drugs have a good effect on type I schizophrenia with psychomotor excitement and hallucination (positive symptoms), but have a poor effect on type II schizophrenia (negative symptoms such as apathy and poor thinking). It is also used to treat mania. Can quickly control excitement, restlessness, continue to use drugs, can make patients regain their senses, emotional stability, and take care of themselves. Its mechanism is related to blocking dopamine D2 receptor in midbrain-limbic lobe and midbrain-cortex pathway.
2. The antiemetic effect is effective for vomiting caused by many diseases and drugs, which is caused by blocking D2 receptor in vomiting chemosensory area (CTZ). High dose can directly inhibit vomiting center. But it has no effect on vomiting caused by vestibular stimulation, so it cannot be used to treat motion sickness.
3. The effect of artificial hibernation on thermoregulation inhibits the thermoregulation center, making thermoregulation ineffective, and the body temperature rises and falls with the change of environmental temperature. With the cooperation of physical cooling, the body temperature can drop below normal. Used for hypothermia anesthesia and artificial hibernation therapy. Combine dolantin and promethazine.
4. Strengthening the role of central depressants can enhance the role of anesthetics, sedatives, hypnotics, painkillers and ethanol.
(4) Adverse reactions
Chlorpromazine can also block dopaminergic nerve pathways in other parts of the brain, and also block α receptor and M receptor of autonomic nervous system, which is mainly related to some adverse reactions.
1. General adverse reactions: ① lethargy, fatigue and apathy (blocking DA receptor); ② Dry mouth, constipation and blurred vision (blocking M receptor); ③ Nasal congestion and decreased blood pressure (blocking α receptor); ④ Breast enlargement and amenorrhea (endocrine).
2. Extrapyramidal system reaction: It is the most common side effect, such as blocking D2 receptor of substantia nigra-striatum pathway, weakening DA function in striatum and enhancing ACh function, which causes extrapyramidal system reaction. There are four types:
(1) Parkinson's syndrome (Parkinson's disease), (more common in middle-aged and elderly people)
(2) akathisia can be relieved by reducing the dosage or using central anticholinergic drugs. (Young people are more common)
③ Acute dystonia
④ tardive dyskinesia may be related to the up-regulation of dopamine receptor caused by long-term medication, and anti-DA drugs can alleviate this reaction.
The first three reactions can be alleviated by Antan, and the fourth reaction can be aggravated by anticholinergic drugs.
Step 3: Allergy
4. Acute poisoning; Acute poisoning can occur if a very large dose of chlorpromazine (1 ~ 2g) is swallowed at one time. Symptomatic treatment should be given immediately
Other anti-schizophrenia drugs: Fluperphenazine, Triflurazzine (phenothiazine), Telden (thiaanthracene), Flupentine (butylbenzene), penfluridol, Sulpiride, Clozapine, Risperidone, etc.
Summary:
1. Schizophrenia patients have increased dopaminergic nerve activity in the limbic system, which can be caused by increased D2-like receptors, increased D2-like dopamine sensitivity, excessive dopamine production or slow elimination.
2. Classical anti-schizophrenia drugs have therapeutic effects by competitively blocking dopamine receptors, which is atypical.
Antischizophrenia drugs block serotonin receptors.
3. Antischizophrenia drugs are mainly used to treat schizophrenia and manic symptoms of other mental diseases.
It also has curative effect.
4. Anti-schizophrenia drugs have no radical effect, but can maintain the normal function of patients with support.
Second, antipsychotic drugs
Manic depression is a kind of psychosis characterized by abnormal high or low emotional activity.
Etiology: unknown. It is believed that it is related to the imbalance of monoamine function in the brain. 5-HT deficiency with hyperna is mania; 5-HT deficiency with NA deficiency is characterized by depression.
Antimanic drugs (antimanic drugs)
Nerve lithium
The therapeutic dose has no effect on the mental activity of normal people, but it has a significant effect on manic episode. Its mechanism may be to inhibit the release of NA and DA in the brain, promote their uptake, and reduce the concentration of neurotransmitters in synaptic cleft (related to inhibiting the dephosphorylation of IP3 and reducing PIP2). There are many adverse reactions, and the blood drug concentration is more than 2mmol/L, which causes poisoning.
Antidepressants (antidepressants)
Imimipramine is the main representative of tricyclic drugs commonly used.
Ingram (Ingram)
(A), pharmacological action and clinical application
Central nervous system: It has inhibitory effects on normal people, such as drowsiness and decreased thinking ability, but it has antidepressant effects on depressed people, such as high mood and uplifting spirit. Its mechanism may be related to inhibiting the reuptake of NA and 5-HT by neurons, increasing the concentration of neurotransmitters in synaptic cleft and promoting synaptic transmission function. Mainly used to treat various types of depression.
Anticholinergic effect: blocking M receptor
Cardiovascular system: hypotension, arrhythmia, etc. It may be related to the inhibition of myocardial NA reabsorption.
(2) Adverse reactions: Atropine-like effects, prostatic hypertrophy and glaucoma are prohibited. Postural hypotension and tachycardia.
The selective 5-HT reuptake inhibitor of fluvoxamine has little effect on other transmitters and receptors, retains the similar curative effect as tricyclic antidepressants, and overcomes many adverse reactions.
Maprotiline selective sodium reuptake inhibitor has little effect on 5-HT.
Moclobemide selective MAO-A inhibitor can reduce 5-HT and NA metabolism.
Third, anti-anxiety drugs.
Benzodiazepines are commonly used.
Buspirone is a partial agonist of selective 5-HT 1A receptor, which can reduce the release of 5-HT and reduce the neurological function of 5-HT, thus treating anxiety disorder. There are few adverse reactions and no obvious drug dependence.
Summary:
1. All antidepressants used in clinic directly or indirectly enhance the function of norepinephrine and/or serotonin in the brain.
2. Both tricyclic and polycyclic antidepressants block the reabsorption of norepinephrine and/or serotonin, and enhance related neurological functions. They all have similar therapeutic effects, and the choice of drugs depends on the tolerance to adverse reactions and the duration of drug action.
3. Selective serotonin reuptake inhibitors are a new generation of antidepressants. Compared with tricyclic drugs, their serotonin reuptake inhibitors
Choline is less toxic to the heart.
Thinking about the problem:
1. Briefly describe the effect of chlorpromazine on receptor and its relationship with pharmacological action and adverse reactions.
2. What are the adverse reactions of chlorpromazine? What are the countermeasures?
3. What is the difference between atypical antipsychotics and chlorpromazine?
4. The pharmacological action and application of tricyclic antidepressants.
References:
1. Fundamentals of medical pharmacology
2. Learn medicine in Jizhou
3. Pharmacological progress fund for new concepts such as antipsychotics (2000) 1~9. Science Press Basic and Clinical Pharmacology People's Health Publishing House