MindMap Gallery Sedational hypnosis and anti-anxiety drugs
Explore the mysteries of sedation, hypnosis and anti-anxiety! From iV infusion NaHCO3 to Chapter 14, we reveal how BDZ relies on GABA to play its role and its outstanding performance in anxiety and insomnia treatment. Barbiturates, benzodiazepine BDZs and zopiclones have their own characteristics, but BDZs have become the first clinical choice for their fewer adverse reactions. As a BDZ receptor antagonist, flumasinib provides key support for the rescue of poisoning. From slow-wave sleep to heterogeneous sleep, these drugs accurately regulate the sleep phase and bring peace to patients. However, contraindications such as severe pulmonary insufficiency remind us to safely explore the secrets of sedation, hypnosis and anti-anxiety!
Edited at 2025-03-10 15:20:28Rumi: 10 dimensions of spiritual awakening. When you stop looking for yourself, you will find the entire universe because what you are looking for is also looking for you. Anything you do persevere every day can open a door to the depths of your spirit. In silence, I slipped into the secret realm, and I enjoyed everything to observe the magic around me, and didn't make any noise. Why do you like to crawl when you are born with wings? The soul has its own ears and can hear things that the mind cannot understand. Seek inward for the answer to everything, everything in the universe is in you. Lovers do not end up meeting somewhere, and there is no parting in this world. A wound is where light enters your heart.
Chronic heart failure is not just a problem of the speed of heart rate! It is caused by the decrease in myocardial contraction and diastolic function, which leads to insufficient cardiac output, which in turn causes congestion in the pulmonary circulation and congestion in the systemic circulation. From causes, inducement to compensation mechanisms, the pathophysiological processes of heart failure are complex and diverse. By controlling edema, reducing the heart's front and afterload, improving cardiac comfort function, and preventing and treating basic causes, we can effectively respond to this challenge. Only by understanding the mechanisms and clinical manifestations of heart failure and mastering prevention and treatment strategies can we better protect heart health.
Ischemia-reperfusion injury is a phenomenon that cellular function and metabolic disorders and structural damage will worsen after organs or tissues restore blood supply. Its main mechanisms include increased free radical generation, calcium overload, and the role of microvascular and leukocytes. The heart and brain are common damaged organs, manifested as changes in myocardial metabolism and ultrastructural changes, decreased cardiac function, etc. Prevention and control measures include removing free radicals, reducing calcium overload, improving metabolism and controlling reperfusion conditions, such as low sodium, low temperature, low pressure, etc. Understanding these mechanisms can help develop effective treatment options and alleviate ischemic injury.
Rumi: 10 dimensions of spiritual awakening. When you stop looking for yourself, you will find the entire universe because what you are looking for is also looking for you. Anything you do persevere every day can open a door to the depths of your spirit. In silence, I slipped into the secret realm, and I enjoyed everything to observe the magic around me, and didn't make any noise. Why do you like to crawl when you are born with wings? The soul has its own ears and can hear things that the mind cannot understand. Seek inward for the answer to everything, everything in the universe is in you. Lovers do not end up meeting somewhere, and there is no parting in this world. A wound is where light enters your heart.
Chronic heart failure is not just a problem of the speed of heart rate! It is caused by the decrease in myocardial contraction and diastolic function, which leads to insufficient cardiac output, which in turn causes congestion in the pulmonary circulation and congestion in the systemic circulation. From causes, inducement to compensation mechanisms, the pathophysiological processes of heart failure are complex and diverse. By controlling edema, reducing the heart's front and afterload, improving cardiac comfort function, and preventing and treating basic causes, we can effectively respond to this challenge. Only by understanding the mechanisms and clinical manifestations of heart failure and mastering prevention and treatment strategies can we better protect heart health.
Ischemia-reperfusion injury is a phenomenon that cellular function and metabolic disorders and structural damage will worsen after organs or tissues restore blood supply. Its main mechanisms include increased free radical generation, calcium overload, and the role of microvascular and leukocytes. The heart and brain are common damaged organs, manifested as changes in myocardial metabolism and ultrastructural changes, decreased cardiac function, etc. Prevention and control measures include removing free radicals, reducing calcium overload, improving metabolism and controlling reperfusion conditions, such as low sodium, low temperature, low pressure, etc. Understanding these mechanisms can help develop effective treatment options and alleviate ischemic injury.
Chapter 14: Sedational Hypnosis and Anti-Anxiety Medicine
Basic concepts
Sedational Hypnosis
Refers to drugs that have selective inhibitory effects on the central nervous system and can cause sedation and hypnosis
Hypnosis pills
The drug that causes approximately physiological sleep is called hypnosis
Small doses only cause quiet or lethargy
It is manifested as sedation
Hypnosis is manifested in large doses
There is no obvious boundary between the two, but the degree of effect is different
Anti-anxiety drugs
Refers to drugs that can relieve anxiety and other symptoms such as excitement and anxiety and corresponding physical symptoms
Sleeping phase
Slow wave sleep/non-rapid eye movement sleep
The gradual loss of consciousness, a slight drop in blood pressure, a slower heart rate and breathing, a shrinking pupil, a decrease in body temperature and metabolic rate, a decrease in urine volume, an increase in gastric juice, a decrease in saliva secretion, and an enhanced sweating function, which gradually eliminates fatigue and restores energy.
Disparate sleep/rapid eye movement sleep
When the brain is in a heterogeneous sleep, the EEG presents fast-frequency and low-voltage radio waves, which is a bit like the brain waves when awake. Some agitated reactions will occur, such as increased activity of the autonomic nervous system, frequent rapid eye movements, accelerated heart rate and breathing, increased blood pressure, increased cerebral blood flow and oxygen consumption, male penis erection, facial and finger (toe) muscles twitch from time to time when turning over, etc. People will also dream.
Three commonly used categories
Benzodiazepine BDZs
Currently the most commonly used sedative hypnosis/anti-anxiety drugs in clinical practice
Chemical structure
Benzodiazepines are produced by substitution of different groups
main
Diazepam/Andine
effect
main
Anti-anxiety
It is less than the sedation dose
High selectivity and can eliminate anxiety in small doses that do not affect central activity
Can eliminate anxiety and symptoms such as gastrointestinal disorders or insomnia caused by it
advantage
Long-lasting effect
Long duration
Not easy to generate dependencies
e.g. "Little mouse reactive fight experiment"
Sedation and hypnosis
Shorten sleep time and prolong sleep time
Effects on sleep phases
Shorten rapid eye movement and deep sleep
Compared with barbiturates, its effect of shortening rapid eye movement sleep is weaker → The "rebound" phenomenon is mild after stopping the drug
Anticonvulsive and anti-epileptic
iV (intravenous injection) is the first choice for the treatment of status epilepsy
Treatment of tetanus/drug poisoning/convulsion caused by high fever in children
Central muscle relaxation
This effect is more prominent in iV
use
Muscle ankle in cerebrovascular accident or spinal cord injury
Relieve muscle spasms caused by joint lesions, lumbar muscle strain, and endoscopy
The central muscle relaxation effect of clonazepam is the most obvious
It can occur without causing sedation dose
mechanism
There is a diazepam binding site-BDZ receptor in the brain, and its distribution is consistent with the GABA (A) receptor distribution
When GABA (A) receptor is excited, open with Cl-channel → Cl-influence makes membrane potential hyperpolarized → Postsynaptic inhibitory effect
BDZs bind to GABA to the same "GABA(A) receptor•Cl-channel complex"
Increase the affinity of GABA with binding sites →accelerate the open frequency of Cl-channel, thereby increasing the postsynaptic inhibition effect
The effect of BDZ is the effect of GABA
Diazepam binds to inhibitor DBI/anxiety peptide
Also known as "BDZ's reverse phase agonist"
mechanism
BDI binding at the binding site of GABA(A) receptor and BDZ
And its effect is the opposite of BDZ
Inhibit GABA Open Cl Channel → Cause Anxiety and Convulsion
In vivo process
Good absorption
High plasma protein binding rate
Converted into active metabolites through liver drug enzymes with long half-life
Long-lasting effect
Pay attention to the accumulation of drugs and their active metabolites in the body when taking continuous medication.
Adverse reactions
Lethargy, fatigue, dizziness
Influences skillful operation and driving safety
The iV speed is too fast to suppress respiration and circulation functions
Use caution in the elderly and those with low cardiopulmonary function
Long-term medication can create dependence
Symptoms of withdrawal from sudden stopping medication: insomnia, excitement, anxiety, tremor and even convulsions
Stop the medicine gradually
Excessive acute poisoning
Causes motor dysfunction, delirium, coma and respiratory depression
Not life-threatening
However, drinking alcohol or other central inhibitors during diazepam use can aggravate the symptoms of poisoning and lead to death
Chlorazole/Limianning
Features
The T1/2 of its active metabolite is very long, 60h
Have savings after long use
For
Anxiety
Neuroscience
Insomnia
Control of symptoms after drinking, etc.
Fluzepam
Its active metabolite T1/2 is longer
40-100h
Long-acting drugs
Taboos
People with liver and renal insufficiency, women and children
Nitazepam
effect
Except for insomnia
Can also treat epilepsy
Especially for infant spasm and myoclonus seizures
Clonazepam
Main applications
Treatment of epilepsy and convulsions
One of the strongest anti-epileptic drugs
iV treatment for persistent epilepsy
Triazolam
Sedation and hypnosis are significant
Strong titer and fast metabolism in BDZs
Quick effect
Strong
Very little accumulation
Eszolam/Shuanle
Midazolam/Sleeping
For
Insomnia
anxiety
Pre-ansthesia medication
BDZ receptor antagonist—Flumacinib
mechanism
Compete with BDZs to bind to BDZ receptors
The effect of antagonizing DBI
Features
Good oral absorption, but the first pass effect is obvious
F is only 20%
Usually iV administration
Clinical application
Mainly used for central deep inhibition caused by excessive BDZs
Barbiturate
There are many adverse reactions, and they have gradually been replaced by BDZs
Representative medicine
Long-term effect
Phenobarbital
The lowest fat-soluble
Slow absorption
Slow onset
Long duration
Mainly excreted through the kidneys
Weak acidic drugs
Alkalitic blood, urine →
iV instillation of NaHCO3
Increased polarity, reduced absorption
Accelerate excretion
Rescue measures for poisoning
Medium effect
Isomal Barbital
Short-term effect
Scobarbito
Ultra short-term effect
Sulfur
The highest fat-soluble
Fast absorption
Quickly take effect
Short duration
Quickly enter the brain and then quickly distribute it to the whole body (especially fat tissue), so the blood drug concentration is rapidly reduced
All four types of fat-soluble other drugs are high → easy to pass through the blood-brain barrier and play a role in the center
The higher the fat solubility → the shorter the effect
Pharmacological effects
Features
Barbiturates have significant dose-dependent
As the dose increases, the degree and range of central inhibition gradually increase
Sedation → Hypnosis → Anticonvulsive → Anesthesia → Until the life center is paralyzed and death
Hypnosis effect
Shorten the sleep time and reduce the number of awakenings
For sleep
Shortening of rapid eye movement sleep is more obvious than BDZs
Therefore, the rebound phenomenon is more obvious after long-term use and stopping the medicine
Mechanism of action
Binding with "GABA (A) receptor • Cl-channel complex" → promoting GABA binding to receptor → prolonging Cl-opening time, Cl-influx ↑ → membrane potential hyperpolarization → excitability ↓
Inhibition of Na channels at anesthesia concentration → not easy to depolarize
Selective inhibition of brainstem reticular structure upward activation system under sedative hypnosis dose → reduce cortical excitability
Clinical application
Sedation and hypnosis
Mainly used as a companion
Antagonizes the central excitation effect of amyophylate and ephedrine
Enhance the efficacy of analgesics
Anti-convulsion
Convulsions caused by high fever, tetanus, eclampsia, and drug poisoning in children
Anti-epileptic
Larger dose
Anesthesia and pre-ansthesia medication
It is mainly used to perform anesthesia and induce anesthesia with ultra-short speed.
Adverse reactions
As a hypnotic drug, there is also a "hangover" phenomenon
Occasionally allergic reactions
e.g. Exfoliating dermatitis
It is an inducer of liver enzymes
Accelerate your own metabolism
Accelerate the metabolism of other drugs
Contraindicated for those with severe pulmonary insufficiency, bronchial asthma, and respiratory depression caused by craniocerebral injury
Other categories
Chloraldehyde Hydrated
Chemical structure
Hydrate of trichloroacetaldehyde
Features
Quick oral absorption
But oral irritation is high (penetrating odor and corrosive bitter taste)
It can easily cause nausea and vomiting
Generally diluted into 10% solution, and administered with anal enema
Must be diluted, the original concentration will cause poisoning
Long duration
6-8h
Strong hypnosis
Go to sleep about 15 minutes
Mild effect
No hangover
Clinical application
Mainly used for intractable insomnia
Large doses-anticonvulsive
Things to note
Be sure to dilute the enema, the original concentration will cause poisoning
Otherwise, it will cause damage to the heart, liver, kidneys, etc.
After a long period of use of the medication, it may develop tolerance and addiction.
Buspirone
A new type of anti-anxiety drug
Compared with BDZs
No hypnosis, anticonvulsive and central muscle relaxation
Pharmacological effects
Mainly used for anti-anxiety
It takes one week to develop a stable anti-anxiety effect
mechanism
No direct relationship with GABA
It is a partial agonist of the 5-HT (1A) receptor
Zopiclon
Chemical structure is not BDZs, but
Basically consistent
It has sedation, hypnosis, anti-anxiety and anti-convulsive, muscle relaxation
The mechanism of action is basically the same
It is just that the binding site that binds to the "GABA(A) receptor•Cl-channel complex" is different from that of BDZs
Hypnotic Characteristics
Fast sleep, shorten the latent period of sleep
Extend sleep time
Mildly reduce rapid eye movement sleep time
There is basically no rebate after stopping the drug
Significantly increase deep sleep
Better for hypnosis medication
Contraindications
Contraindicated during breastfeeding, use with caution for those with poor liver and kidney function.