MindMap Gallery Pharmacology-Antipsychiatric Drugs Mind Map
An article about pharmacology - a mind map of antipsychotic drugs, with a detailed introduction and comprehensive description. I hope it will be helpful to those who are interested!
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antipsychotic drugs
antischizophrenia drugs
Classification (symptoms)
Type I
Mainly positive symptoms (hallucinations and delusions)
Type II
Mainly negative symptoms (apathy, lack of initiative)
Classic antischizophrenia drugs
Phenothiazines
Chlorpromazine
internal processes
The brain concentration is greater than the plasma concentration. It is mainly excreted through liver metabolism and kidneys. It is highly fat-soluble and easily accumulated in adipose tissue. The individual dosage varies greatly.
mechanism
Mainly antagonizes dopamine in the limbic system of the brain, and can also antagonize alpha receptors and M receptors
Pharmacological effects
Central Nervous System
1. Anti-schizophrenia effect
Mesolimbic and mesencephalocortical
2. Antiemetic effect
The emetic chemoreceptive area in the brain oblongata cannot combat vomiting (motion sickness) caused by vestibular stimulation, but is effective for intractable hiccups.
3. Body temperature regulation
It can not only lower the body temperature of those with fever, but also lower the normal body temperature.
autonomic nervous system
alpha receptor blocking effect
It inhibits the vasomotor center and directly dilates blood vessels. Chlorpromazine can reverse the pressor effect of epinephrine.
M receptor blocking effect
Large doses can cause dry mouth, constipation, and blurred vision
Effects on the endocrine system
Blocks D2 receptors in the subthalamic nodule-infundibulum pathway
Increase prolactin secretion (breast enlargement and lactation suppression)
Suppression of gonadotropins (menstrual disorders, delayed ovulation)
inhibit glucocorticoids
Suppresses pituitary growth hormone (treats gigantism)
Clinical application
Treat mental illness
Type I schizophrenia, especially acute
Effective for those with excitement and delusions associated with mania and other mental illnesses. Ineffective for type II
Antiemetic and intractable hiccups
All kinds of vomiting but motion sickness vomiting is not effective
Hypothermic anesthesia and artificial hibernation
Hibernation mixture (chlorpromazine, promethazine, pethidine)
Artificial hibernation (lowering body temperature, basal metabolism, tissue oxygen consumption)
Used for severe trauma, septic shock, febrile convulsions
Adverse reactions
Common reactions
CNS depression: lethargy, apathy, weakness, etc.
M receptor blockade: blurred vision, less sweating, dry mouth, constipation, difficulty urinating
Alpha receptor blockade: nasal congestion, orthostatic BP↓, heart rate↑
Correction of chlorpromazine-induced hypotension: norepinephrine
extrapyramidal reaction
acute extrapyramidal movement disorder
Parkinson's disease is the most common
akathisia
acute dystonia
Reason: Blocking the substantia nigra-striatal D2R Prevention and treatment: discontinue medication and use trihexyphenidyl
Tardive dyskinesia (involuntary stereotyped movements of mouth, tongue and cheeks)
Psychosis, convulsions, epilepsy
Allergic reactions: liver damage, jaundice, granulocytopenia, anemia
Cardiovascular and Endocrine: BP↓; Endocrine Disorders
Acute poisoning: lethargy, BP↓→shock, myocardial damage
Other phenothiazines
Perphenazine, Fluphenazine, Trifluoperazine
Features
1. Strong antipsychotic and antiemetic effects; strong extrapyramidal adverse reactions
2. Weak sedative and antihypertensive effects
Thiaxanthenes
Chlorprothixol
Features
1. Has anti-anxiety and anti-depressant effects
2. Mild adverse reactions
use
Suitable for obsessive-compulsive states or anxiety, depression, schizophrenia and menopausal depression.
Flupentixol
Anti-schizophrenic effects similar to chlorpromazine, also used to treat depression or depression with anxiety
Sedation is weak but extrapyramidal reactions are common, contraindicated in patients with mania
Butyrophenones
haloperidol
Features
1. Strong antipsychotic effects, antiemetic effects, and extrapyramidal reactions
2. Weak sedative and antihypertensive effects
use
Commonly used for various types of schizophrenia and mania, and also suitable for antiemetics and persistent hiccups
droperidol
Features
Loss of pain, trance, indifference to the environment
use
Minor surgery, pre-anesthetic medication, controlling aggressive behavior of mental patients
pimozide
Features
The difluorobenzene derivative of droperidol has good anti-hallucination and delusion effects
use
It is clinically used to treat schizophrenia, mania and Tourette syndrome, and is contraindicated for heart disease.
Other antischizophrenia drugs
Penfluridol
It has a strong extrapyramidal system and has a strong anti-schizophrenia effect. It can also be used as an antiemetic but has a weak sedative effect. It is suitable for acute and chronic schizophrenia, especially for chronic patients. It lasts for a long time.
Sulpiride
Midbrain-limbic system D2 receptor, highly effective in catatonic schizophrenia, effective quickly, known as drug electroshock
atypical antischizophrenia drugs
clozapine
Fast, strong, D4-R blocking, effective for both positive and negative symptoms
There are almost no extrapyramidal adverse reactions, and it has antihistamine, anticholinergic, and anti-α adrenergic effects.
Adverse reactions
Decreased granule C (female > male)
Risperidone
Anti-5-HT>Anti-D2
Suitable for first-episode acute and chronic patients
It has a therapeutic effect on the cognitive function and secondary depression of schizophrenia, with mild adverse reactions.
ziprasidone
The fifth atypical anti-schizophrenia drug launched globally
Currently the only atypical antischizophrenia drug that inhibits NA and 5-HT reuptake.
Aripiprazole
It has a two-way regulatory effect on the DA nervous system and is responsible for the stability of DA transmitters.
Treating various types of schizophrenia
Mechanism
1. Anti-schizophrenia drugs
(1) Block dopamine receptors in the midbrain-limbic system and midbrain-cortex system
Only the theory of DA system hyperactivity in the mesencephalic-limbic pathway and mesocortical pathway has been widely recognized
(2) Block 5-HT receptors
2. Antimanic Drugs
3. Antidepressants (mainly based on monoamine theory)
(1) Non-selective inhibition of norepinephrine (NA) and 5-hydroxytryptamine (5-HT) reuptake
(2) Selectively inhibit NA reuptake
(3) Selectively inhibit 5-HT reuptake
(4) Inhibit monoamine oxidase
(5) Block presynaptic α2 adrenergic receptors and increase NA release
There are four DA pathways in the brain
1. Midbrain-limbic system pathway DA-R: function related to emotion regulation
2. Midbrain-cortical system pathway DA-R: functions related to thinking, feeling, understanding, etc.
3. Nodule infundibulum is related to endocrine function
Hypothalamic hormone secretion, oblongata vomiting chemoreceptor area, body temperature center
4. Substantia nigra-striatum is related to extrapyramidal function
ADHD, Parkinson's disease
Drug Classification
antischizophrenia drugs
Classic antischizophrenia drugs
Atypical antischizophrenia drugs (clear advantages over classics)
It is well tolerated and has good compliance, with rare adverse reactions including extrapyramidal reactions and hyperprolactinemia.
Most negative symptoms are stronger than classic ones
antimanic drugs
antidepressants
anti-anxiety medications
Cardiovascular and liver damage are mild and reserved for use
The most common adverse reactions of chlorpromazine in the treatment of schizophrenia
This class of drugs is recommended as first-line treatment for patients with first-episode schizophrenia
Clinically used to enhance the effect of analgesics, such as when used in combination with fentanyl
Ineffective against depression and may even worsen it
The nitrogen atom at position 10 of the phenothiazine ring is replaced by a carbon atom