Drugs affecting the central nervous system classification. Drugs affecting the central nervous system. Effect of opioids on the vomiting center

Means affecting the central nervous system.

Drugs for anesthesia.

Narcosis (narcosis - stupor, stunning) is a condition characterized by reversible CNS depression, manifested by loss of consciousness, loss of sensitivity (primarily pain), suppression of reflexes, and a decrease in skeletal muscle tone.

History of anesthesia. The discovery of anesthesia is associated with the discovery of the analgesic properties of ether. "Ether" is a word of Greek origin, which means "heavenly fire". As a substance, it was discovered in Spain in 1200. Lullius, and only in 1540 Paracelsus established the analgesic properties of this substance, and Cordus carried out its synthesis. Ether was synthesized again in 1730 by Frobenius.

Nitrous oxide was obtained by Priestley in 1772, and the English chemist Davy described its analgesic properties, and in 1945 the American physician Wells used it to extract teeth. In 1849, the Russian doctor S.K. Klikovich successfully used a mixture of nitrous oxide and oxygen to anesthetize childbirth.

The generally accepted date of birth of anesthesia is October 16, 1846, when the American dentist Morton publicly gave ether anesthesia to a patient during tooth extraction. He was awarded the prize of the Paris Academy of Sciences, many countries awarded him orders.

A.I. Pirogov made a great contribution to the study of anesthesia, who widely used anesthesia in the field, studied various methods of its administration. In 1947 his monograph was published.

In the future, many new drugs for anesthesia were found.

Classification of drugs for anesthesia

Means for inhalation Means for non-inhalation

anesthesia anesthesia

1.Volatile liquids 2. Gaseous 1. Short action

Ether for anesthesia - nitrous oxide - Propanidide

Fluorotan - Ketamine

2. Medium cont. actions

Thiopental - sodium

3. Long lasting

Sodium hydroxybutyrate

Means for inhalation anesthesia are administered through Airways(by inhalation).

Means for non-inhalation anesthesia are most often administered intravenously or intramuscularly.

During anesthesia, there are four stages(see ether anesthesia):

I stage of analgesia (3-5 minutes). First of all, the cerebral cortex is oppressed: pain sensitivity decreases, consciousness is gradually lost. Reflexes, muscle tone are preserved. Respiration, pulse, blood pressure are not changed, the pupils react to light.

II stage of excitation (20 min). According to the figurative expression of I.P. Pavlov, a “rebellion of the subcortex” arises. Sensitivity and consciousness are completely lost. At the same time, motor and speech excitation develops (the patient begins to sing, speak, scream, cry or laugh). Increased reflexes (cough, vomiting), muscle tone. Respiration, pulse quickened, blood pressure increased. Pupils dilated and unresponsive to light.

Stage III of surgical anesthesia is characterized by a lack of sensitivity, consciousness, suppression of reflexes, a decrease in muscle tone, other indicators decrease gradually.

IV stage of recovery (awakening) - 20-40 min.

The functions of the central nervous system are restored in the reverse order. After awakening, post-anesthetic sleep lasts several hours.

Means for anesthesia must meet the following requirements:

cause deep and prolonged anesthesia

have sufficient narcotic latitude

be well managed

cause rapid development and rapid recovery from anesthesia

cause no complications

application technique should be simple and convenient

be fire safe

Characteristics of means for inhalation anesthesia

Ether for anesthesia (Aether pro narcosi) - a liquid with a peculiar smell. Fire, explosive. Available in bottles of 100 ml and 150 ml.

Possesses high activity, wide range of action, easy to control, well relaxes skeletal muscles. Used for all types of operations.

The disadvantages are: slow induction into anesthesia, irritation of the mucous membranes of the respiratory tract, increased salivation and secretion of bronchial glands, which makes breathing difficult; long stage of excitation (10-20 min.), in which cough, vomiting, tachycardia, increased blood pressure are possible; in the stage of surgical anesthesia, a decrease in blood pressure, respiratory depression are possible; awakening is slow (20-40 min.), pneumonia, bronchitis may develop in the postoperative period, due to irritation of the mucous membranes of the respiratory tract with ether, sometimes nausea, vomiting.

To prevent complications before anesthesia, M-xb (atropine) should be administered.

Fluorotan(Phtorothanum, Narcotan) - a liquid with a peculiar odor in a 50 ml bottle does not burn, does not explode.

Characterized high activity (3-4 times greater than ether), the introduction of anesthesia is fast (after 3-5 minutes) without a stage of excitation, has a wide range of action, is easily controlled, well relaxes the skeletal muscles. Relatively little toxic, does not irritate the respiratory tract, inhibits the secretion of the salivary, bronchial glands. Awakening occurs in 3-5 minutes. after cessation of anesthesia. Nausea and vomiting are rare. Convenient for operations in children.

Disadvantages: bradycardia (prevented by atropine), arrhythmia, hypotension (mezaton is administered, and adrenaline and norepinephrine cannot be administered due to the increased sensitivity of the myocardium to them). Not recommended for cardiogenic shock. Synthesized in England, introduced into clinical practice in 1956.

Nitrous oxide colorless gas in cylinders of 5-12 liters. Does not ignite. It is used in a mixture with oxygen (80% nitrogen oxide + 20% O 2) to prevent hypoxia. In lower concentrations of nitrogen, nitrous oxide causes a superficial narcosis resembling intoxication (the former name is “laughing gas”).

Characteristically rapid onset of anesthesia with a short and unexpressed stage of excitation, large latitude of action, good controllability, rapid recovery from anesthesia, no side effects.

chief disadvantage is a low activity, therefore, to enhance the effect and obtain deep anesthesia, they are combined with other drugs.

Can be used for short-term interventions in traumatology, cardiology, dentistry, obstetrics.

Characteristics of funds for non-inhalation anesthesia

propanidide, ketamine, thiopental sodium are used mainly for induction anesthesia, for short-term operations, for burns, painful instrumental studies, biopsies, fractures, removal of drains, in dentistry, etc.

Sodium hydroxybutyrate used for induction and basic anesthesia in patients in a state of hypoxia, in the elderly and children.

Comparative characteristics of inhaled and non-inhaled anesthetics

Ethanol ( Spiritus acthylicus )

Transparent, volatile, flammable liquid with a characteristic odor. According to the effect on the central nervous system, 3 stages are distinguished: arousal, anesthesia, agonal.

Normal Excitation Narcosis Paralysis

condition

As an agent for anesthesia, alcohol is of little use, because. causes a long stage of excitation, and the period of anesthesia quickly passes into the agonal stage, i.e. it has a small scope.

In medical practice, the irritant and antimicrobial properties of alcohol are used. Alcohol 40% has a pronounced irritant effect and is used for rubbing the skin in the composition of liquids, such as Menovazin, for myositis, arthritis, neuritis, sciatica, and also for the prevention of bedsores. With the help of warming compresses for otitis, tonsillitis, bruises on the second day, in the event of infiltrates, etc.

Alcohol 70%, 96% has an antimicrobial effect and is used to treat instruments, etc. Previously, it was widely used as an antiseptic for treating the surgical field, the hands of medical staff.

As a solvent, alcohol is used to prepare solutions, tinctures, extracts.

Ingestion of alcohol is characterized initially by intoxication. The prolonged stage of arousal is manifested by euphoria, increased mood, excessive talkativeness, and sociability. Psychomotor

reactions are disturbed, behavior, self-control, and performance suffer. The coordination of movement is disturbed, the reaction slows down, unsteadiness of the gait appears. There is a feeling of warmth. The skin is red, sweating is increased, the pulse is frequent, blood pressure is increased. With an increase in the dose, signs of acute poisoning with ethyl alcohol appear. There is analgesia, drowsiness, impaired consciousness. The skin is pale or cyanotic, moist, cold (increased heat transfer), breathing is rare, shallow; the pulse is frequent, weak, blood pressure is lowered, muscle tone and reflexes are lowered. In severe poisoning, fecal and urinary incontinence is possible.

I Prevent absorption of alcohol in the gastrointestinal tract (see above)

II Purify the blood

III Symptomatic treatment:

Analeptics: caffeine, cordiamin, bemegrid, B vitamins (B 1 B 6), vitamin C intravenously or intramuscularly.

Chronic alcoholism and its treatment - see student abstracts

Lecture #23

Lecture topic: Sleeping pills. Anticonvulsants.

Sleeping pills that can cause a person to experience a state resembling physiological sleep. By the nature of the effect on the central nervous system, they belong to substances of an inhibitory effect.

As you know, sleep is absolutely necessary for a person. Prolonged insomnia leads to death sooner than starvation (after 4-6 days).

There are two phases in the sleep process; slow and REM sleep. The phase of "slow" sleep is characterized by a slowdown in brain activity. It accounts for 75-80% of all sleep time in an adult. The REM sleep phase is characterized by an increase in brain activity, it takes 20-25% of the total sleep time.

Hypnotics facilitate the onset of sleep, increase its duration, provide its depth.

The ratio of the stages of action of narcotic-type substances (scheme)

Means for anesthesia Excitation stage Anesthesia stage Agonal stage

Hypnotics Sleep stage Anesthesia stage Agonal stage

Ethyl alcohol Excitation stage Anesthesia stage Agonal stage

Classification of sleeping pills based on their chemical structure

1. Derivatives 2. Derivatives 3. Miscellaneous drugs

barbituric benzodiazepine chemical structure

acids - nitrazepam - zopiclone

- phenobarbital - rohypnol

In small doses, they have a sedative (soothing) effect, in medium doses they are hypnotic, and in large doses they are narcotic.

Indications for the use of hypnotics are various sleep disorders, which can be of three types:

1. violation of the process of falling asleep - "insomnia of the young", occurs in young people with overwork, neurosis, etc .; in this case, preparations of short and medium duration of action are recommended;

2. normal falling asleep, but quick awakening "insomnia of the elderly", occurs in elderly people with severe sclerosis of cerebral vessels; long-acting sleeping pills are recommended.

3. violation of the processes of falling asleep and sleep - occurs at any age in various neurotic conditions, sleep can be superficial, not bringing rest, long-acting hypnotics are recommended that inhibit the phase of "REM sleep"

Fenbarbitalo ( Phenobarbitalum)

Long acting barbiturate. Sleep comes in ½-1 hour, because. poorly soluble and slowly absorbed from the zh.k.t.; lasts about 8 hours. Facilitates falling asleep, but disrupts the phase structure of sleep. Only 35% is inactivated by the liver and with repeated doses cumulation is possible, which is manifested by aftereffects (weakness, depression, drowsiness, decreased ability to work). With prolonged use, addiction and addiction develop, with cancellation - the “withdrawal” syndrome.

Contraindications: severe liver and kidney disease.

Nitrazepam ( Nitrazepamum, Rededorm)

Sleep comes in 20-30 minutes, lasts 6-8 hours. Difference from phenobarbital: a) changes the structure of sleep to a lesser extent; b) has a wide breadth of therapeutic action; c) lower risk of developing drug dependence.

It is used for sleep disorders of various etiologies.

P.d.: in large doses - drowsiness, lethargy, headache.

Contraindications: myasthenia gravis, pregnancy.

Rohypnol (Rohypnol)

Release form: tablets of 0.001 and 0.002, solution in ampoules of 1 ml

It is prescribed just before bedtime. Accelerates the period of falling asleep, reduces the number of night awakenings

P.d: see nitrazepam

Zopiclone ( Jmovan )

Release form: tablets

Application: insomnia (poor sleep, nocturnal awakenings, early awakenings, chronic insomnia).

Contraindications: children under 15, pregnancy, lactating.

The sedative effect of hypnotics is used in small doses for the treatment of neurosis, angina pectoris, hypertension etc. Lowering the excitability of the motor centers of the brain, hypnotics (especially phenobarbital) have an anticonvulsant effect and are used to treat epilepsy.

All sleeping pills slow down reactions to external stimuli, so some categories of people (drivers, pilots, high-altitude workers, dispatchers, etc.) cannot take them during work, it is forbidden to take them with alcohol.

Acute drug poisoning

IN initial stage the victim complains of weakness, drowsiness, headache. In severe poisoning, there is loss of consciousness, respiratory depression, a drop in blood pressure, relaxation of skeletal muscles, the skin is pale, cold, moist, the pupils first narrow, then expand. Death occurs from paralysis of the respiratory center and cardiac arrest.

Help with poisoning: see ethyl alcohol poisoning.

Antiepileptic drugs

Epilepsia is a seizure. The drugs in this group prevent the onset of seizures in epilepsy.

1. big seizures are characterized by convulsions covering the whole body, against the background of loss of consciousness, after which a long sleep occurs.

2. small seizures are characterized by a short-term loss of consciousness without noticeable convulsions.

3. psychomotor seizures are manifested by impaired consciousness, motor and mental anxiety, inadequate actions.

Admission rules:

1. The drugs should be used regularly and for a long time, cessation can lead to a "withdrawal" syndrome, the dose is reduced gradually.

2. The drug should be prescribed individually, taking into account the form of the disease.

3. It should be remembered that drugs prevent epilepsy attacks, slow down the process of mental degradation, but do not cure the disease.

Diazepam (Seduxen) IV or IM 0.5%-2 ml is most often used to relieve status epilepticus

Antiparkinsonian drugs used to treat disease Parkinson's (trembling paralysis).

The disease is associated with damage to the substantia nigra of the brain. At the same time, the content of dopamine, which regulates the activity of motor neurons, decreases, cholinergic receptors are excited - the tone of skeletal muscles increases.

Symptoms: stiffness of movements, mincing gait, mask-like face, muscle rigidity, tremor.

Treatment of the disease can be aimed either at enhancing dopaminergic effects, or at reducing cholinergic ones.

Levodopa enters the brain, where it is converted to dopamine.

Release form: capsules of 0.25 and 0.5

Pd: nausea, vomiting, orthostatic collapse, arrhythmia.

Cycladol has a pronounced central and peripheral anticholinergic effect.

Release form: tablets of 0.002 List A

P.d.: dry mouth, disturbance of accommodation, tachycardia

In case of an overdose, motor and mental agitation, hallucinations are possible.

P.p.: glaucoma, pregnancy.

DRUGS AFFECTING THE CENTRAL NERVOUS SYSTEM

This group of drugs includes substances that change the functions of the central nervous system, having a direct effect on its various parts of the head or spinal cord.

According to the morphological structure of the CNS, it can be considered as a set of many neurons. Communication between neurons is provided by contact of their processes with the bodies or processes of other neurons. Such interneuronal contacts are called synapses.

The transmission of nerve impulses in the synapses of the central nervous system, as well as in the synapses of the peripheral nervous system, is carried out with the help of chemical transmitters of excitation - mediators. The role of mediators in the CNS synapses is performed by acetylcholine, norepinephrine, dopamine, serotonin, gamma-aminobutyric acid (GABA), etc.

Medicinal substances that affect the central nervous system change (stimulate or inhibit) the transmission of nerve impulses in synapses. The mechanisms of action of substances on the CNS synapses are different. Substances can excite or block receptors on which mediators act, affect the release of mediators or their inactivation.

Medicinal substances acting on the central nervous system are represented by the following groups:

) means for anesthesia;

) ethanol;

) sleeping pills;

a) antiepileptic drugs;

a) antiparkinsonian drugs;

) analgesics;

) psychotropic drugs(neuroleptics, antidepressants, lithium salts, anxiolytics, sedatives, psychostimulants, nootropics);

) analeptics.

Some of these drugs have a depressing effect on the central nervous system (anesthesia, hypnotics and antiepileptic drugs), others have a stimulating effect (analeptics, psychostimulants). Some groups of substances can cause both excitatory and depressant effects (for example, antidepressants).

1. Means for anesthesia

Narcosis is a reversible depression of the central nervous system, which is accompanied by loss of consciousness, loss of sensitivity, a decrease in reflex excitability and muscle tone. In this regard, during anesthesia, favorable conditions are created for surgical operations.

One of the first drugs for anesthesia was diethyl ether, first used for surgical operation W. Morton in 1846. Since 1847, the outstanding Russian surgeon N.I. Pirogov. Since 1868, nitrous oxide has been used in surgical practice, and since 1956, halothane has been used.

Means for anesthesia have a depressing effect on the transmission of nerve impulses in the synapses of the central nervous system. The sensitivity of the synapses of different parts of the central nervous system to anesthetic agents is not the same. First, the synapses of the reticular formation and the cerebral cortex are inhibited, and lastly, the respiratory and vasomotor centers medulla oblongata. In this regard, in the action of drugs for anesthesia, certain stages are distinguished, which replace each other as the dose of the drug increases.

So, in the action of diethyl ether, 4 stages are distinguished: I - the stage of analgesia; II - stage of excitation; III - stage of surgical anesthesia; IV - agonal stage.

The stage of analgesia is the loss of pain sensitivity while maintaining consciousness. Respiration, pulse, arterial pressure are little changed.

Excitation stage. Consciousness is completely lost. At the same time, some manifestations of nervous activity are intensified. Patients develop motor and speech excitation (they can scream, cry, sing). Muscle tone sharply increases, cough and gag reflexes increase (vomiting is possible). Respiration and pulse are quickened, blood pressure is increased. It is believed that excitation is associated with inhibition of inhibitory processes in the brain.

Stage of surgical anesthesia. The inhibitory effect of diethyl ether on the brain deepens and spreads to the spinal cord. The phenomena of excitation pass. Unconditioned reflexes are inhibited, muscle tone decreases. Breathing slows down, blood pressure stabilizes. At this stage, 4 levels are distinguished: 1) light anesthesia; 2) medium anesthesia; 3) deep anesthesia;) super-deep anesthesia.

At the end of anesthesia, the functions of the central nervous system are restored in the reverse order. Awakening after ether anesthesia occurs slowly (after 20-40 minutes) and is replaced by a long (several hours) post-anesthetic sleep.

agonal stage. With an overdose of diethyl ether, the respiratory and vasomotor centers are inhibited. Breathing becomes rare, superficial. The pulse is frequent, weak filling. Arterial pressure is sharply reduced. There is cyanosis of the skin and mucous membranes. The pupils are maximally dilated. Death occurs with symptoms of respiratory arrest and heart failure.

There are certain requirements for anesthetics. These funds must: 1) have a pronounced narcotic activity; 2) induce well-controlled anesthesia, i.e. allow you to quickly change the depth of anesthesia; 3) have sufficient narcotic latitude, i.e. a sufficiently large range between doses (concentrations) that cause surgical anesthesia, and doses in which substances depress breathing; 4) do not have a pronounced side effect.

Classification of drugs for anesthesia

1.Means for inhalation anesthesia

Volatile liquids

Fluorotan Enflurane Isoflurane Diethyl ether

Gaseous media

Nitrous oxide

2. Means for non-inhalation anesthesia

Sodium thiopental Propanidide Propofol Ketamine Hexenal Sodium hydroxybutyrate

Means for inhalation anesthesia

Preparations of this group (vapors of volatile liquids or gaseous substances) are introduced into the body by inhalation (inhalation). Inhalation anesthesia is usually carried out with the help of special anesthesia machines, which allow precise dosing of inhaled substances. In this case, vapors of volatile liquids or gaseous substances enter the respiratory tract through a special endotracheal tube inserted into the trachea through the glottis.

Inhalation anesthesia is easily controlled, as narcotic substances are rapidly absorbed and excreted through the respiratory tract.

Liquid volatile drugs for anesthesia

Halothane (halothane, fluotan) is a volatile non-flammable liquid. A highly active agent for anesthesia - anesthesia develops at low concentrations of a substance in the inhaled air. The stage of revival is short-term, without pronounced motor restlessness. It has a sufficient narcotic latitude. Does not irritate the respiratory tract. Awakening comes faster than the number of ether anesthesia.

Analgesia and muscle relaxation with the use of halothane are somewhat less pronounced than with ether anesthesia. Therefore, halothane is more often combined with nitrous oxide and curare-like agents.

Side effects of halothane: decrease in myocardial contractility, bradycardia, decreased blood pressure, myocardial sensitization to the action of adrenaline and norepinephrine (possible cardiac arrhythmias).

Due to possible hepatotoxic effects, halothane is not recommended for use in liver diseases.

Enflurane is similar in properties to halothane; less active, but acts faster. It has a more pronounced muscle relaxant effect. To a lesser extent, sensitizes the myocardium to adrenaline and norepinephrine.

Isoflurane is an isomer of enflurane. Less toxic.

Diethyl ether (ether for anesthesia) - active drug, which has a significant narcotic latitude. Causes pronounced analgesia and muscle relaxation. However, it has a number of negative properties.

Diethyl ether irritates the respiratory tract and therefore increases the secretion of the salivary and bronchial glands. May cause laryngospasm, reflex bradycardia, vomiting. It is characterized by a pronounced long stage of excitation. Ether vapors are highly flammable and form explosive mixtures with air. Currently, diethyl ether is rarely used for anesthesia.

Gaseous anesthetics

Nitrous oxide is a gas with low narcotic activity. In small concentrations, it causes a state resembling intoxication, which is why nitrous oxide used to be called "laughing gas".

Only at a concentration of 80% nitrous oxide causes superficial anesthesia with a fairly pronounced analgesia. To prevent hypoxia, anesthesiologists use a mixture containing 80% nitrous oxide and 20% oxygen (corresponding to the oxygen content in the air). Anesthesia occurs quickly, without a pronounced stage of excitation and is characterized by good controllability, but a small depth and lack of muscle relaxation. Awakening occurs in the first minutes after the cessation of inhalation. The aftereffect is practically absent. Side effects are not observed. Due to the low narcotic activity, nitrous oxide is usually combined with more active anesthetics, such as halothane.

Means for non-inhalation anesthesia

The drugs in this group are most often administered intravenously (intravenous anesthesia). Anesthesia develops in the first minutes after injection, without a pronounced stage of excitation and is characterized by low controllability.

Thiopental sodium is a derivative of barbituric acid. Released in vials in the form of a dry substance, which is dissolved before intravenous administration. After the introduction of anesthesia develops after 1-2 minutes and lasts 15-20 minutes. Awakening is replaced by post-anesthetic sleep. Analgesic effect and muscle relaxation are insignificant.

The drug is particularly suitable for induction anesthesia, i.e. introduction to the state of anesthesia without the stage of excitation. It is possible to use sodium thiopental for short-term surgical interventions, as well as for cupping convulsive conditions. Thiopental-sodium is contraindicated in violations of the liver and kidneys.

Sodium hydroxybutyrate has a long-term effect - synthetic analogue natural metabolite found in the CNS. It penetrates well through the blood-brain barrier. Renders gray hair

CNS drugs were among the first drugs discovered by our ancient ancestors and are still among the most commonly used drugs. Substances such as caffeine, nicotine, ethanol, are consumed very widely in the world, including in our country.

Anesthesia drugs State of anesthesia, or general anesthesia, usually includes loss of sensitivity, primarily pain (analgesia, anesthesia), loss of consciousness, inhibition of reflexes, relaxation of skeletal muscles and amnesia (memory loss).

Means for inhalation anesthesia ● Fluorotan - anesthesia occurs quickly (after 3-5 minutes), the stage of excitation is short, anesthesia is easily controlled. Side effects hypotension, bradycardia (increased vagal tone) and arrhythmia up to ventricular fibrillation and cardiac arrest, sometimes nausea, vomiting, headache; after prolonged anesthesia - slight hypothermia. Contraindications for use Fluorothane anesthesia is contraindicated in shock, collapse, severe heart damage, severe arrhythmias,. Composition and form of production: dark glass bottles of 50 ml, 200 ml and 250 ml ● Nitrous oxide (laughing gas) - a mixture of 80% nitrous oxide + 20% oxygen is used. The narcotic effect is insufficient, therefore, combined with halothane. It is also used for myocardial infarction or other conditions accompanied by severe pain(good analgesic effect). ● Xenon is a good but expensive drug. Does not enter chemical reaction with neurons, but temporarily alters their function in the transmission of pain signals. Of all the numerous anesthetics, xenon is closest to unraveling the theories of anesthesia. It is no coincidence that in the scientific world it is considered a tool for understanding the mechanisms of anesthesia.

Propofol is a fast-acting intravenous anesthetic for induction and maintenance of general anesthesia, as well as for sedation of patients during intensive care. General anesthesia occurs in 30-60 seconds. The duration of anesthesia is from 10 minutes to 1 hour. From anesthesia, the patient wakes up quickly and with a clear mind. The ability to open the eyes appears after 10 minutes. Application Induction anesthesia, maintenance of general anesthesia; sedation of patients during mechanical ventilation, surgical and diagnostic procedures. Contraindications Hypersensitivity, childhood: up to 1 month - for induction of anesthesia and maintenance of anesthesia, up to 16 years - to provide a sedative effect during intensive care. Side effects Decreased blood pressure, bradycardia, short-term respiratory arrest, shortness of breath; rarely - convulsions, during awakening - headache, nausea, vomiting, postoperative fever (rarely); local - pain at the injection site, rarely - phlebitis and vein thrombosis. Sodium oxybutyrate - Used in anesthesiology practice as a non-inhalation narcotic for anesthesia during non-cavitary low-traumatic operations with spontaneous breathing, also for induction and basic anesthesia in surgery, obstetrics and gynecology, especially in patients who are in a state of hypoxia; in pediatric surgery; during anesthesia in the elderly. in psychiatric and neurological practice sodium hydroxybutyrate is used in patients with neurotic and neurosis-like conditions, with intoxication and traumatic injuries of the central nervous system, with sleep disorders, with narcolepsy (to improve night sleep). There is evidence of the effectiveness of sodium oxybutyrate in trigeminal neuralgia.

+ Advantages of inhalation anesthesia - its good controllability and relative ease of anesthesia, - Disadvantages - prolonged entry into anesthesia and the presence of a stage of excitation. + Advantages of non-inhalation anesthesia - its rapid onset and the absence of a stage of excitation, - Disadvantage - poor controllability.

Stages of ether anesthesia 1. Stage of analgesia - pain sensitivity disappears, but the patient is conscious. 2. Stage of excitation 3. Stage of surgical anesthesia. It is due to the inhibition of most subcortical formations, with the exception of the respiratory and vasomotor center. 4. The agonal stage is the complete suppression of all departments of the central nervous system and without life-supporting measures, death quickly occurs. When the ether is canceled, all stages of anesthesia go in reverse order (the awakening stage), but, as a rule, faster and with less pronounced symptoms.

Ethyl alcohol - With a resorptive effect, ethyl alcohol manifests itself as a low-effective agent for anesthesia. At the same time, it has a number of features: there is no stage of analgesia, the stage of excitation is long and with the preservation of consciousness, pronounced disinhibition (speech, motor, sexual) is characteristic, the stage of anesthesia very quickly passes into the agonal stage. In medicine, ethyl alcohol is used topically as an antimicrobial agent (70%) and as an irritant in compresses (40-50%). The resorptive action of ethyl alcohol is rarely used, as a warming and as a supplier of easily digestible energy to malnourished patients. in small doses, ethyl alcohol has a mild sedative effect, increases appetite, and improves digestion. The constant intake of small doses of alcohol (up to 20 ml / day) significantly reduces the risk of myocardial infarction and the occurrence of angina attacks. This effect of alcohol is associated with lowering blood cholesterol levels and reducing blood clotting. However, with continued use high doses alcohol seriously disrupts the function of the central nervous system, a person loses the ability to self-criticism, commits antisocial acts. With a persistent addiction to alcohol, when it does not enter the body, a withdrawal syndrome develops - abstinence - in the form of delirium tremens.

Sleeping pills There are different classifications of sleeping pills, but in historical and practical terms they can be divided into three groups: 1. barbituric acid derivatives (barbiturates), 2. benzodiazepine derivatives, 3. sleeping pills of different chemical structure.

Barbiturates (derivatives of barbituric acid) Phenobarbital, barbital-sodium, etaminal-sodium, barbamil, etc. All barbiturates are characterized by a violation of the structure of sleep, an increase in the duration of slow sleep, which does not give satisfaction from sleep. All barbiturates are able to increase the activity of the antitoxic function of the liver, due to which addiction develops quite quickly. (Phenobarbital is sometimes used for this action to prevent possible poisoning by drugs metabolized in the liver.) More commonly used to treat epileptic seizures.

Benzodiazepine derivatives (BDA) BDA derivatives interact with benzodiazepine receptors. They are considered optimal hypnotics. Effective in sleep disorders associated with anxiety and emotional stress. sensitivity to GABA corresponding receptors inhibitory effect of GABA.

Benzodiazepines have a wide range pharmacological action, including anxiolytic, sedative, hypnotic, muscle relaxant, anticonvulsant, amnestic, etc. Drugs medium duration Actions: Nitrazepam. (It has a good sedative effect and at the same time a pronounced sleeping pill. Sleep occurs after taking nitrazepam after 20-45 minutes and lasts up to 8 hours. An important feature of the drug is that it practically does not disturb the normal phase structure of sleep. Long-acting drugs: Diazepam, Phenazepam, Zopiclone and Zolpidem are not BDA derivatives, but have an affinity for BDA.

An ideal hypnotic should induce sleep that is close in structure and duration to physiological sleep, have a short latent period (that is, the time from taking the drug to falling asleep), have no side and toxic effects, not cause addiction and addiction, and not have aftereffects (that is, pain, dizziness, feeling overwhelmed, depressed the next day). With all obviousness, it should be recognized that at present, none of the sleeping pills available in the arsenal of physicians fully satisfies these criteria. Moreover, almost all sleeping pills have one common negative property - the recoil syndrome. It means that when the drug is discontinued, insomnia not only reappears, but also becomes more pronounced. In addition, addiction and addiction develop to some extent to all sleeping pills. Therefore, long-term treatment of insomnia with sleeping pills (more than a week) is a medical mistake.

Anticonvulsants 1. Means symptomatic therapy: narcotic, sleeping pills, neuroleptics, tranquilizers, muscle relaxants. 2. Means for the treatment of epilepsy. 3. Drugs for the treatment of Parkinson's disease.

Parkinson's disease is caused by the progressive destruction and death of neurons that produce the neurotransmitter dopamine. THEREFORE, it is NECESSARY to fill the dopamine deficiency in the brain to inhibit central cholinergic influences. The precursors of dopamine - Levodopa - penetrates through the BBB into the basal ganglia and turns into dopamine there. Nakom, madopar, midantan. Means stimulating dopamine receptors. Bromocriptine (parlodel) - excites dopamine receptors. Central anticholinergics - Cyclodol. Tropacin.

Antiepileptic drugs Epilepsy - chronic illness, characterized by episodes of uncontrolled excitation of brain neurons that repeat from time to time. Depending on the cause that caused the pathological excitation of neurons and the localization of the focus of excitation in the brain, epileptic seizures can take many forms. Types of seizures 1) Generalized seizures Drugs Major seizures Carbamazepine, phenobarbital, diphenin, sodium valproate, lamotrigine. Epileptic status Diazepam, clonazepam. Minor epileptic seizures Ethosuccimide, clonazepam, sodium valproate, lamotrigine. Myoclonus - epilepsy Clonazepam, sodium valproate, lamotrigine. one) Partial convulsions Carbamazepine, clonazepam, diphenin, sodium valproate, lamotrigine

Difenin has a pronounced anticonvulsant effect. Difenin reduces the excitability of the motor centers of the brain in the absence of a hypnotic effect. Favorably affects the general condition of patients with epilepsy. Carbamazepine - Reduces the frequency of seizures, anxiety, depression, irritability and aggressiveness in patients with epilepsy. The effect on cognitive functions in patients with epilepsy is variable. Prevents the appearance of paroxysmal pain in neuralgia. Used for alcohol withdrawal syndrome: reduces increased nervous excitability, tremor, gait disturbances. It is used for the treatment of affective disorders as an antipsychotic and normothymic agent. Clonazepam - Clinical action manifested by a strong and prolonged anticonvulsant effect. It also has antiphobic, sedative (especially pronounced at the beginning of treatment), muscle relaxant and moderate hypnotic effect. Lamotrigine (lamiktal) - effective for various forms epilepsy. Inhibits the release of excitatory amino acids in the central nervous system. Diazepam is used to treat status epilepticus. Epilepsy has been treated for several years. This often leads to side effects: headache, nausea, appearance skin itching. Possible leukopenia and erythropenia, impaired liver and kidney function. Almost all antiepileptic drugs cause sedation, impair the ability to concentrate and slow down the speed of psychomotor reactions.

Psychotropic drugs Modern psychotropic substances interfere with the biochemical processes of brain tissue. 1. psychosedatives - have a calming effect on the central nervous system; 2. psychostimulants and antidepressants - have an exciting effect on the central nervous system; 3. nootropic substances - affecting the processes of thinking (noos - mind); 4. psychodysleptics, hallucinogens - disrupt the mental activity of a person. They are not drugs, but are used as intoxicants.

Psychosedatives Antipsychotics have a pronounced inhibitory effect on the nervous and mental activity of a person without disturbing consciousness. They have tranquilizing (calming) and antipsychotic effects.

Tranquilizers are drugs that reduce the feeling of fear, anxiety, restlessness, internal tension. They are often called anxiolytics (anxiosis - anxiety).

Sedatives Before the advent of tranquilizers, these were the means of treating neuroses. At present, due to low effectiveness, sedative drugs have practically lost their importance and are mainly of historical interest.

STIMULANTS Psychostimulants - increase mood, ability to perceive external stimuli, psychomotor activity. They reduce the feeling of fatigue, increase physical and mental performance(especially when tired), temporarily reduce the need for sleep.

. Nootropics - activate the higher integrative functions of the brain. Many nootropics have a pronounced antihypoxic activity. On the higher nervous activity of healthy animals and the psyche healthy person these drugs have no effect.

Drugs that improve cerebral circulation. Improving cerebral circulation action medicines manifested in increased blood flow and blood supply to the brain.

Analeptics. This medicines, which have a strong stimulating effect on the respiratory and vasomotor centers of the medulla oblongata directly (caffeine, camphor, bemegride), or by increasing their sensitivity (strychnine), which stimulates vital important features respiration and circulation. Some analeptics can, in addition, stimulate other parts of the central nervous system, which causes convulsions in case of overdose.

Antidepressants. - psychotropic drugs used primarily for the treatment of depression. In a depressed patient, they improve mood, reduce or relieve melancholy, lethargy, apathy, anxiety and emotional stress, increase mental activity, normalize the phase structure and duration of sleep, and appetite. Many antidepressants fail to improve mood in a non-depressed person

Magnesium sulfate has a multifaceted effect on the body. The drug reduces the excitability of the respiratory center, large doses of the product when administered parenterally (bypassing the digestive tract) can easily cause respiratory paralysis. Blood pressure is slightly reduced due to the general calming effect of the product; this effect is more pronounced in hypertension (persistent increase in blood pressure). When administered parenterally, magnesium sulfate has a calming effect on the central nervous system. Depending on the dose, a sedative (calming), hypnotic or narcotic effect may be observed. When taken orally, it is poorly absorbed and acts as a laxative.

Analgesics From the point of view of medicine, pain is: a kind of feeling, a kind unpleasant feeling; reaction to this sensation, which is characterized by a certain emotional coloring, reflex changes in the functions of internal organs, unconditioned motor reflexes, as well as volitional efforts aimed at getting rid of pain factor. an unpleasant sensory and emotional experience associated with real or perceived tissue damage, and at the same time the reaction of the body, mobilizing various functional systems to protect it from pathogens.

Pain sensations are perceived by special receptors - nociceptors, which are located at the ends of branched afferent fibers located in the skin, muscles, joint capsules, periosteum, internal organs etc. Causes of pain: ● inflammation ● endogenous substances (bradykinin, serotonin, histamine) ● prostaglandins (Prostaglandins are mediators with a pronounced physiological effect.) They increase the sensitivity of nociceptors to chemical and thermal stimuli.

Analgesics are drugs that, with a resorptive action, selectively suppress pain sensitivity. They do not depress consciousness and do not turn off other types of sensitivity. Allocate 1. narcotic (opioid) analgesics, 2. non-narcotic analgesics 3. mixed-action analgesics.

Narcotic analgesics include: phenanthrene opium alkaloids: Morphine Omnopon Codeine synthetic narcotic analgesics: Promedol Fentanyl

Narcotic analgesics. ● Act on opiate receptors, and there is a loss of pain sensitivity. Other types of sensitivity are not disturbed, moreover, hearing, vision and smell can be aggravated. ● Oppress respiratory center(reduce its sensitivity to carbon dioxide), especially in overdoses, and this is the main cause of death in acute morphine poisoning. ● Cause euphoria, Feelings of anxiety, fear, hunger disappear, imagination increases and self-control is eliminated, complete indifference to the environment appears. A person renounces reality for the duration of the drug, in the future he feels the need for repeated similar sensations and is drawn into dependence on the drug. ● stimulates the centers of the oculomotor nerves, which is manifested by severe miosis, and the vagus nerve - causes bradycardia. In addition, on the periphery, morphine increases the tone of the sphincters of the gastrointestinal tract, Bladder and bronchi. With prolonged use, tolerance develops to many of the effects of narcotic analgesics, with the exception of miosis and constipation.

Morphine overdose: Symptoms of acute and chronic overdose: cold clammy sweat, confusion, dizziness, drowsiness, decreased blood pressure, nervousness, fatigue, miosis, bradycardia, severe weakness, slow breathing difficulties, hypothermia, anxiety, dryness of the oral mucosa, delirious psychosis , intracranial hypertension(up to cerebrovascular accident), hallucinations, muscle rigidity, convulsions, in severe cases - loss of consciousness, respiratory arrest, coma. Specific antagonists of narcotic analgesics are opioid receptor antagonists naloxone and naltrexone, which are successfully used in acute poisoning morphine and its analogues.

SYNTHETIC NARCOTIC ANALGESICS Promedol - inferior to morphine in analgesic action, but does not have a spasmodic effect. A feature of the drug is its effect on the pregnant uterus - it helps to establish the correct rhythmic contractions of the uterus and accelerates delivery. Promedol is the drug of choice for labor pain relief, although it must be remembered that it can depress the fetal respiratory center to a certain extent, although less than morphine. Fentanyl is one of the most powerful analgesics, but has a short duration of effect (up to 30 minutes). It is often used in conjunction with the antipsychotic droperidol to achieve a special kind of general pain relief called neuroleptanalgesia. At the same time, the patient's analgesia is accompanied by the preservation of consciousness, but the absence of a sense of fear and anxiety, the development of indifference to surgical intervention. Used for short-term surgical interventions. Recently, a number of new synthetic drugs have appeared: Pentazocine, butorphanol, tramadol, etc.

Non-narcotic analgesics. Are characterized by: - ​​lack of narcotic action; - not effective for intense pain - indicated for pain caused by inflammation (arthritis, neuritis, myositis) There are 3 groups of non-narcotic analgesics: 1. derivatives salicylic acid(salicylates) - aspirin ( acetylsalicylic acid) 2. pyrazolone derivatives - analgin, butadione, 3. aniline derivatives - paracetamol.

Currently, in pharmacology, it is customary to single out another group of drugs, which is very close to non-narcotic analgesics. This group of drugs is referred to as non-steroidal anti-inflammatory drugs (NSAIDs), thus contrasting this group of drugs with steroidal (hormonal) anti-inflammatory drugs. NSAIDs include drugs of different chemical groups - indomethacin, voltaren, ibuprofen, etc. These drugs are mainly used as antirheumatic, antiarthritic drugs. They are several times superior to the anti-inflammatory activity of salicylates and pyrazolone derivatives.

INDICATIONS FOR THE USE OF NSAIDs 1. Rheumatic diseases It should be borne in mind that in rheumatoid arthritis, NSAIDs have only a symptomatic effect, without affecting the course of the disease. But the relief that NSAIDs bring to patients rheumatoid arthritis, so essential that none of them can do without these drugs. With large collagenoses (systemic lupus erythematosus, scleroderma, and others), NSAIDs are often ineffective. 2. Non-rheumatic diseases of the musculoskeletal system 3. Neurological diseases. Neuralgia, sciatica, sciatica, lumbago. 4. Renal, hepatic colic. five. Pain syndrome various etiologies, including headache and toothache, postoperative pain. 6. Fever (as a rule, at a body temperature above 38.5 ° C). 7. Prevention of arterial thrombosis. 8. Dysmenorrhea.

CONTRAINDICATIONS NSAIDs are contraindicated in erosive and ulcerative lesions of the gastrointestinal tract, especially in the acute stage, severe violations of the liver and kidneys, cytopenias, individual intolerance, pregnancy. If necessary, the safest (but not before childbirth!) Are small doses of aspirin. Indomethacin should not be prescribed on an outpatient basis to persons whose professions require increased attention.

To this group medicines include substances that alter the functions CNS, exerting a direct effect on its various departments - the brain, medulla oblongata or spinal cord.

According to the morphological structure CNS can be considered as a collection of many individual neurons (a neuron is a nerve cell with all its processes), the number of which in humans reaches 14 billion. Communication between neurons is ensured by contact of their processes with each other or with the bodies of nerve cells. Such interneuronal contacts are called synapses (sinapsis - connection, connection). The transmission of nerve impulses in the synapses of the central nervous system, as well as in the synapses of the peripheral nervous system, is carried out with the help of chemical transmitters of excitation - mediators. The role of mediators in the synapses of the central nervous system is performed by acetylcholine, norepinephrine, dopamine and other substances.

medicinal substances that affect the central nervous system, change (stimulate or inhibit) the transmission of nerve impulses in synapses. The mechanisms of action of substances on the CNS synapses are different. So, some substances can excite or block receptors in synapses, with which certain mediators interact.

Medicines, affecting the CNS, are usually classified according to their main effects. For example, substances that cause anesthesia are combined into a group of drugs for anesthesia, inducing sleep - into a group of sleeping pills, etc.

Drugs affecting the central nervous system

Means for anesthesia; Ethanol; sleeping pills; Antiepileptic drugs; Antiparkinsonian drugs; analgesics; Analeptics; Psychotropic drugs. Among these substances, there are drugs that have a depressing effect on most of the functions of the central nervous system. These substances include anesthetics, ethyl alcohol, hypnotics. Along with this, many substances (antiepileptics, antipsychotics, tranquilizers, sedatives) have a more selective inhibitory effect on the functions of the central nervous system.

In contrast to these substances, some drugs act on the central nervous system in a stimulating way (for example, analeptics, psychostimulants).

There are also substances that can have a depressing effect on some nerve centers and a stimulating effect on others. For example, narcotic analgesics inhibit the perception of pain, the respiratory center, the cough center, but stimulate the centers of the vagus and oculomotor centers.