MindMap Gallery Pharmacology—antipsychotic drugs
This is a mind map about 18 - antipsychotic drugs, which mainly includes antischizophrenia drugs/neuroleptics, antidepressant drugs, etc.
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antipsychotic drugs
insane
Schizophrenia, mania, depression, anxiety
antischizophrenia drugs / neuroleptics
Schizophrenia
Incoordination between thinking, emotion, and behavior, separation of mental activities from reality
Type I (mainly positive symptoms): delusions, hallucinations, abnormal behavior
Type II (mainly negative symptoms): apathy, lack of initiative
mechanism
Type I is mostly DA hyperactivity, so most drugs are multi-DA receptor antagonists.
1. Block the central DA receptors in the mesencephalic-limbic pathway and mesencephalic-cortical pathway
2. Block 5-HT receptors: clozapine
Phenothiazines
Dimethylamines
Chlorpromazine-Hibernating Spirit
Intramuscular injection; individualize dosage
Pharmacological effects
CNS
Anti-schizophrenia
Depresses the central nervous system (neuroleptic effect)
Significant control of activity, mania, and induction of sleep
Unlike barbiturates, large doses do not cause anesthesia
Oral administration to normal people: Quietness, reduced activity, apathy, decreased concentration Schizophrenia patients: quickly control excitement and agitation, eliminate hallucinations and delusions in large doses
By antagonizing limbic and cortical D2 receptors Long-term use will antagonize D2 in the nigrostriatal body and cause extrapyramidal reactions.
Suppress vomiting
A small dose blocks the emetic chemoreceptor center in the oblongata → antagonizes the DA receptor agonist apomorphine
High-dose blockade inhibits the vomiting center
But does not combat vomiting (motion sickness) caused by vestibular stimulation Effective for stubborn hiccups
thermoregulation
Inhibiting the hypothalamic thermoregulatory center leads to body temperature failure, which can not only reduce high temperature, but also reduce normal body temperature.
Body temperature changes with changes in the external environment
autonomic nerve
Block alpha adrenergic receptors
Dilates blood vessels and lowers blood pressure, but has many side effects and is not used to treat HBP
Epinephrine's pressor-reversing to antihypertensive effect
The antihypertensive effect caused by chlorpromazine cannot be treated with epinephrine
Blocks M-choline receptors
Large doses can block M receptors and have atropine-like effects
endocrine
DA receptors that block the nodule-infundibular pathway
Reduce the release of prolactin inhibitory factor from the hypothalamus → increase prolactin
Inhibits the secretion of gonadotropin-releasing hormone, reducing the release of follicle-stimulating hormone and luteinizing hormone, causing reduced ovulation
Inhibition of pituitary growth hormone secretion: treatment of gigantism
Clinical application
Schizophrenia
Type I schizophrenia (mainly psychomotor excitement, hallucinations and delusions)
acute patients
It cannot be cured, long-term medication, lifelong treatment
Vomiting and refractory vomiting
Diseases such as cancer and radiation sickness
Drugs such as tetracycline and digitalis
Hypothermia anesthesia and artificial hibernation
Chlorpromazine, promethazine, pethidine = hibernation mixture
hypothermic anesthesia
artificial hibernation
Adjuvant treatment for severe trauma, febrile convulsions, thyroid storm, pregnancy-induced hypertension, central hyperthermia, septic shock, etc.
Adverse reactions
General adverse reactions
Central depression symptoms: lethargy, apathy, drowsiness, fatigue
M receptor blocking effect: blurred vision, nasal congestion, dry mouth, constipation
Alpha receptor blockade symptoms: BP decrease, orthostatic hypotension, palpitations, etc.
It is highly irritating and cannot be injected subcutaneously. It can be injected deep into the muscle.
Intravenous administration is prone to thrombophlebitis
extrapyramidal reaction
anticholinergic relief
Parkinson's syndrome: increased muscle tone, dull facial expression, slow movement, muscle tremors, salivation → antagonizes D2 receptors
Akathisia: restless and wandering → weakened striatal DA function
Acute dystonia: forced mouth opening, tongue thrusting, torticollis, breathing difficulties, dysphagia → enhanced ACh function
Long-term use→Tardive dyskinesia TD
Clozapine treatment
Mechanism: DA receptors are antagonized for a long time, and receptor sensitivity increases or feedback promotes DA release.
Involuntary orofacial sucking, tongue licking, chewing and other stereotyped movements as well as generalized choreoathetosis
The incidence rate is higher among middle-aged and elderly patients and patients with organic brain diseases
Central anticholinergic drugs lose their effect and aggravate symptoms. Antidopamine drugs can reduce this reaction.
mental disorder
Disorder of consciousness, lethargy, apathy, excitement, restlessness - discontinuation of medication
Convulsions and epilepsy
focal or generalized convulsions
EEG epileptiform discharges
Patients with a history of convulsions, epilepsy and organic brain lesions should use medication with caution
allergic reaction
Rash, contact dermatitis
cardiovascular system response
Orthostatic hypotension, sustained hypotensive shock, more common in the elderly with AS and HBP Abnormal ECG, arrhythmia
endocrine system response
Breast enlargement, lactation, cessation of menstruation, growth inhibition in children, sexual dysfunction
acute poisoning
Lethargy, blood pressure drops to shock levels, and myocardial damage occurs
drug interactions
Collaboration
Enhance other centrally acting drugs: sedative-hypnotics, analgesics, antihistamines, ethanol
inhibition
Dopamine precursors such as levodopa
Piperazines
perphenazine
Piperidines
thioridazine
Thiaxanthenes
Chlorprothixol
Treat anxiety and depression
flupenthixol
Butyrophenones
haloperidol
droperidol
Nerve block analgesia: Intravenous injection with the strong analgesic drug fentanyl can produce a special anesthetic state for the patient
pimote
other
Penfluridol
Sulpiride
atypical antischizophrenia drugs
clozapine
Selective D4 subtype receptor blocker, the drug of choice for refractory schizophrenia
Few extrapyramidal reactions and mild endocrine disorders
Serious adverse reactions include agranulocytosis, and white blood cell count examinations are required during medication.
Olanzapine
Quetiapine
Risperidone
ziprasidone
Aripiprazole
antimanic drugs
Elevated mood, irritability, hyperactivity, and loss of control over thinking and speech
Lithium carbonate
Oral absorption
The safety range is narrow, there are many adverse reactions, and it is easy to be poisoned: intravenous injection of NS accelerates li excretion
Clinical application
No impact on normal people
Mania, manic depression
schizophrenia agitation
antidepressants
Abnormal mood (apathy, pessimism, low self-esteem) and abnormal behavior (less movement, less speech, lack of response to surrounding things, etc.), which are often accompanied by low appetite, insomnia and autonomic nervous system symptoms
Pathogenesis
Low function of monoaminergic nerves (5-HT nerves and NE nerves) in the brain
Non-selective NA/5-HT reuptake inhibitors [Tricyclic antidepressants (TCAs)]
Imipramine (imipramine)
oral
Pharmacological effects
CNS
normal person
Quietness, drowsiness, slight drop in blood pressure, dizziness, and dizziness. These symptoms may worsen after several days of continuous use, and may even lead to inattention and decreased thinking ability.
depression patients
Invigorating, slow onset of effect 2-3w
PNS
Therapeutic amounts block M-choline receptors
Blurred vision, dry mouth, constipation, urinary retention
cardiovascular nerves
Decreased blood pressure, causing arrhythmia
Contraindicated for cardiovascular patients
Clinical application
depression
Endogenous depression and menopausal depression are more effective,
Anxiety and Phobias
enuresis
child
Adverse reactions
Prostate patients and glaucoma patients are prohibited from using
anticholinergic effects
Dry mouth, constipation, blurred vision, difficulty urinating, blurred vision, tachycardia
Drowsiness, fatigue, dizziness, orthostatic hypotension and muscle tremors
Large doses can cause cardiac conduction block and arrhythmia
Occasionally epilepsy
granulocytopenia
Toxic liver damage
medicine interactions
Binding to Hb can be reduced by competition with phenylbutazone, phenytoin, Aspirin, and scopolamine
Combined use with MAOI may cause BP elevation, high fever, and convulsions.
Enhance the effect of central nervous system depressants
Amitriptyline
clomipramine
doxepin
NA reuptake inhibitors
Desipramine (desimipramine)
maprotiline
nortriptyline
Reboxetine
venfaracin, duloxetine
5-HT reuptake inhibitors
Fluoxetine (Prozac)
Clinical application
Various types of depression
obsessive-compulsive disorder
bulimia nervosa
Strong selectivity: does not block a, M, 5-HT, H-R, can be used by patients with prostatic hypertrophy and glaucoma Does not impair mental and motor functions and has no sedative effect Little impact on autonomic nervous system and cardiovascular system, high safety Long half-life
Paroxetine
Sertraline
other
trazodone, mirtazapine
Mianshelin
Moclobemide