Analeptics mechanism of action. Analeptic drugs. Carbogen is used for overdose of general anesthetics, carbon monoxide poisoning, and asphyxia of newborns.

Analepsis - restorative, revitalizing effect. Analeptics are emergency drugs. They are antagonists of anesthesia, hypnotics and other drugs that depress the central nervous system, and, mainly, this group of drugs acts on the centers of the medulla oblongata: it stimulates the suppressed respiratory and vasomotor center, thereby restoring impaired respiratory and circulatory functions.

Pharmacomarketing

Classification and drugs

Depending on the dose analeptics can affect various parts of the central nervous system, so they are divided into:

With a predominant effect in small doses on the cerebral cortex, in large doses on the medulla oblongata, in toxic doses on the spinal cord (caffeine)

With a predominant effect on the medulla oblongata, but in high doses they stimulate the cerebral cortex (bemegride, niketamide, sulfocamphocaine, etimizol)

With a predominant effect on the spinal cord; in large doses they act on the medulla oblongata and cerebral cortex (strychnine).

mechanism of action

Some analeptics directly excite the vital centers of the medulla oblongata and, according to the mechanism of action, belong to the analeptics of the first group - direct action (bemegrkd, egimizole, caffeine).

The second group of analeptics reflexively (through the carotid sinus) excites the centers of the medulla oblongata (cytisine, lobeline).

Third group - along with the direct effect, it also causes a reflex effect from the chemoreceptors of the blood vessels to the vital centers of the medulla oblongata (sulfocamphocaine, camphor, carbon dioxide, nichamide). Analeptics also stimulate the motor areas of the brain and interneurons of the spinal cord. (Fig.9.)

Strychnine blocks the action of amino acid neurotransmitters (mainly glycine), which play the role of inhibitory factors in the transmission of excitation in postsynaptic nerve endings in the spinal cord, and facilitate the conduction of excitation in interneuron synapses of the spinal cord.

Rice. 9

Mechanism of action bemegrida, niketamide- inhibition of GABA-A receptors.

Pharmacological

The most characteristic feature of drugs in this group is their stimulating effect on the centers of the medulla oblongata. With the introduction of analeptics, especially against the background of previous suppression, an increase in the depth and frequency of breathing is noted. At the same time, analeptics stimulate the vasomotor center with the respiratory center. In practice, this manifests itself in an increase in the tone of peripheral vessels, a decrease in the deposition of blood in the organs and an increase in its venous return to the heart, as a result of which the work of the heart improves again. Apart from camphor, sulfocamphocaine and caffeine, drugs in this group do not have a direct effect on the contractile properties of the myocardium and its conduction system.

The effect of anapeptics is not limited to the influence on the centers of the medulla oblongata.

In the pharmacodynamics of anapeptics, central (on the central nervous system) and peripheral effects (direct effects on blood vessels and the heart) are distinguished.

Bemegride and cordiamine stimulate the central nervous system, have an “awakening effect” against the background of suppression of the nervous system with large doses of sleeping pills, narcotic analgesics, alcohol and anesthetic substances, which manifests itself in a decrease in the depth of anesthesia and a shortening of its duration, restoration of sternal and other reflexes.

Analeptics increase AT (bemegride, niketamide, sulfocamphocaine), stimulate respiration (all analeptics), are antagonists of hypnotics (bemegride), narcotic drugs (bemegride, sulfocamphocaine, etimizol) increase myocardial contractility (niketamide, camphor, caffeine, sulfocamphocaine) stimulate the reflex function of the spinal cord brain, increase the tone of skeletal and non-muscular muscles, visual acuity, taste, smell, hearing, board (strychnine).

Activate the adrenocorticotropic function of the pituitary gland and are endowed with antispasmodic, anti-inflammatory and antiallergic effects (etimizole) in large doses cause convulsive effects (all analeptics).

Indications for use and interchangeability

1. Acute poisoning with sleeping pills and narcotic drugs (bemegride sulfocamphocaine, etimizol, caffeine sodium benzoate, niketamide).

2. Acute and chronic circulatory disorders (niketamide, cytisine, caffeine sodium benzoate).

3. Shock, collapse, asphyxia (niketamide, sulfocamphocaine, etimizol, cytisine, caffeine sodium benzoate).

4. Acute and chronic heart failure (sulfocamphocaine, camphor, caffeine sodium benzoate).

5. Functional impairment of vision, hearing, smell, paresis, paralysis, gastric atony (strychnine).

6. For seizure therapy (bemegride).

Side effect

1. Increased excitability of the central nervous system, anxiety, insomnia, hypertension, epilepsy, increased convulsive readiness. With prolonged use, addiction and dyspeptic symptoms are possible (bemegride, etimizol).

2. After administration camphor solutions an infiltrate may occur under the skin (Oleg), to accelerate the resorption of which physiotherapeutic procedures are used.

3. Reduced arterial blood flow due to novocaine, which is part of sulfocamphocaine, skeletal muscle rigidity, difficulty breathing (strychnine).

4. When using niketamide Possible vomiting, cardiac arrhythmia, pain at the injection site.

Contraindications

Sulfocamphocaine contraindicated in case of idiosyncrasy to novocaine, Niketamide - in case of a tendency to convulsive reactions, Bemegride - in case of psychomotor agitation.

Strychnine Contraindicated for hypertension, bronchial asthma, angina pectoris, atherosclerosis, acute and chronic nephritis, hepatitis, tendency to convulsive reactions, pregnancy, Graves' disease.

Application cytisine Contraindicated in case of exacerbation of gastric and duodenal ulcers, organic diseases of the cardiovascular system.

Pharmacosafety

Analeptics incompatible with adrenergic blockers, antiarrhythmic drugs, MAO inhibitors, streptomycin.

Niketamide incompatible with camphor.

Analeptic action niketamide decreases under the influence of sodium para aminosalicylate, ftivazid, phenothiazine derivatives.

In cases of severe depression of the central nervous system, analeptics are used in large doses.

High concentrations bemegrida are quickly formed in the blood only when administered intravenously.

Injections bemegrida can be combined with the administration of mezatone, caffeine and other cardiovascular drugs.

Care must be taken when administering sulfocamphocaine patients with low blood pressure .

Caffeine And strychnine Not prescribed to children under two years of age. Caffeine is part of Askofen, citramon, caffeine.

After meals, take etimizol before meals - niketamide.

Comparative characteristics of drugs

Caffeine - an alkaloid, belongs to xanthine derivatives. The latter are formed in the body, are part of the cell and are products of its metabolism. It is characterized by a large breadth of therapeutic action, relatively rapid destruction in the body and the absence of accumulation with long-term use. Caffeine is trimethylxanthine. Theobromine and theophylline - dimethylxanthine differ from each other in the position of methyl radicals. Despite the chemical similarity, caffeine, theobromine and theophylline differ from each other mainly in that dimethylxanthine is characterized by peripheral vasodilating, antispasmodic, and diuretic effects.

The effect of caffeine on the cortex: relieves drowsiness, fatigue, increases mental performance, causes a cheerful mood, that is, stimulates mental activity, improves memory, thinking, perception of external impressions, reduces the number of errors.

For the analeptic effects of caffeine, higher doses are required, especially in conditions of a sharp decrease in the functions of the respiratory and vasomotor centers. As an analeptic, caffeine is significantly inferior to cordiamine and bemegride. This effect of caffeine on the nervous system is called central, but there is a peripheral effect - directly on the blood vessels - dilating. This is especially true for the vessels of the brain, skeletal muscles, kidneys, and heart. The effect depends on the dose, the state of blood circulation: AT does not change under the influence of caffeine if it is normal; increases if it was decreased. The vessels of the abdominal cavity narrow. When caffeine affects the heart, the coronary vessels dilate, the force of contractions increases, and cardiac conduction improves.

Bemegrid - respiratory analeptic with resorptive central action. It is especially effective for poisoning with narcotic drugs and barbiturates.

Etimaol - respiratory analeptic, combines the properties of a respiratory analeptic and a tranquilizer. It has a central, resorptive effect. Since etimizol stimulates the adrenocorticotropic function of the pituitary gland, it is used as an anti-inflammatory and hypoallergenic substance. In addition, for bronchial asthma it has a moderate antispasmodic effect.

Strychnine - an alkaloid from the seeds of chilibukha (emetic nut), has a local, resorptive and reflex effect. The local effect is associated with a bitter taste and irritation of the tongue receptors, increasing appetite. The resorptive effect is associated with its effect on the central nervous system. Strychnine stimulates the reflex function of the spinal cord. The medulla oblongata is more sensitive to strychnine than the cortex, but at doses close to toxic. The drug stimulates the respiratory and vasomotor centers. In the cerebral cortex, it increases the activity of the analyzers of vision, hearing, taste, and smell. Under the influence of strychnine, the field of vision, visual acuity, and shade analysis increase.

Strychnine is characterized by a small breadth of therapeutic action. The main symptoms of poisoning are observed from the spinal cord. It is a reflex convulsive poison. Convulsions occupy a central place. Under the influence of toxic doses, the process of reciprocal inhibition of antagonist muscles is disrupted. Therefore, the poser takes the Opisthotonus pose (head thrown back, back arched, limbs outstretched, sardonic smile).

The cause of death is the cessation of breathing at the stage of maximum inspiration.

Niketamide directly and reflexively excites vital centers through the chemoreceptors of the carotid glomeruli. It has no direct effect on the heart and blood vessels. With deep anesthesia it is not very effective and even enhances anesthesia. Due to the fact that niketamide is a derivative of nicotinic acid, it has a weak antipellagric effect.

Camphor - oxidation product of borneol alcohol. The synthetic levorotatory isomer camphor, which is extracted from fir oil, is also used. Natural camphor (right-handed) is part of the essential oil of the camphor tree. Racemic camphor (from turpentine) is used for external use.

Camphor has local, resorptive and reflex effects, central and peripheral.

Local effect: irritates the skin (feeling of cold, heat, redness, reduction of pain), which is used for inflammation of the middle ear, rheumatism, arthritis, muscle pain, gout, in dermatology. Locally, camphor acts as a weak antiseptic and anti-inflammatory agent.

Camphor enhances metabolic processes in the heart muscle, dilates coronary vessels, and increases the sensitivity of the heart to the effects of adrenaline. Due to the reflex and direct action, camphor excites the vasomotor and respiratory centers of the medulla oblongata, especially when they are suppressed; camphor has a calming effect in neuroses. Excreted in the urine, it suppresses microflora and improves urination.

Sulfocamphocaine - a drug close to camphor, but faster in action. It dissolves well in water. You can enter.

Carbon dioxide - a natural stimulant of respiration and blood circulation, found in the air (0.03%). It is as important for breathing as oxygen, because it stimulates the respiratory center. The latter carbon dioxide excites directly and reflexively from the chemoreceptors of blood vessels. The first mechanism is of leading importance. Carbon dioxide has local, resorptive and reflex effects.

Local effect: in small doses causes tissue irritation, in large doses - their necrosis. Used in dermatology to remove warts and treat leprosy. Drinks containing carbon dioxide cause moderate hyperemia of the gastric mucosa, increase the secretion of gastric glands, and improve absorption from the intestine. Carbon dioxide baths lead to reflex changes in the activity of the cardiovascular system and metabolism.

When prescribing CO 2, you must always remember that if there is no effect of CO 2 within 5-8 minutes, then it will no longer be there.

Cytiton (0.15% solution of cytisine alkaloid) - a reflex stimulator of the respiratory center, excites H-cholinergic receptors of the carotid glomeruli, therefore, according to the mechanism of action, it is a cholinomimegic. Cytisine increases AT (stimulates H-cholinergic receptors of the sympathetic nodes and adrenal glands) and can be used for shock and collapse. The drug is injected into a vein slowly. Cytisine is part of Tabex tablets, which are used to quit smoking. When using them, an unpleasant sensation occurs. Excites the breathing center for a short time - in “pushes”.

Thus, according to the strength of the stimulating effect, these drugs are arranged in the following sequence:

On the respiratory center CO 2 - bemegride - Niketamide, camphor;

For the vasomotor center: niketamide - bemegride - camphor;

For the “awakening” effect: bemegride - niketamide.

list of drugs

Analeptics include medications that help restore respiratory function, the activity of the cardiovascular system, and have a stimulating effect on the vital centers of the medulla oblongata - respiratory and vasomotor. Analeptics stimulate other parts of the central nervous system to a lesser extent: the cerebral cortex, subcortical centers, and the spinal cord. The stimulating effect of analeptics (revitalizing effect) manifests itself especially clearly when respiratory functions and the activity of the cardiovascular system are depressed, including those resulting from the use of central nervous system depressants (anesthetics, hypnotics).

Analeptics include bemegride, camphor, cordiamine, etimizol, etc. Caffeine, which has a psychostimulating effect, is also analeptic, as well as lobelia, cititon and other drugs with a reflex mechanism of action, mainly stimulating the respiratory center due to the stimulation of H-cholinergic receptors in the carotid sinocarotid zone.

BEMEGRID- the most powerful analeptic. Bemegride is used to stimulate breathing and blood circulation, to recover from a state of anesthesia, in case of an overdose of narcotic drugs; recommended for poisoning with barbiturates and other sleeping pills. The dosage of bemegride is strictly individual depending on the patient’s condition. Side effects when using bemegride: vomiting, convulsions. Bemegride is contraindicated if you are prone to seizures. Release form: ampoules of 10 ml of 0.5 solution. List B.

An example of a recipe for bemegride in Latin:

Rp.: Sol. Bemegridi 0.5% 10 ml

D.t. d. N. 10 in ampull.

S. Administer 2-5 ml intravenously to non-anesthetized patients; 5-10 ml - in case of poisoning with sleeping pills, for recovery from anesthesia.

ETIMIZOL- has a pronounced stimulating effect on the respiratory center, is used as a respiratory stimulant (under anesthesia, etc.). Etimizole improves short-term memory and increases mental performance. Etimizole stimulates the pituitary-adrenal system, and therefore has an anti-inflammatory, anti-allergic effect. Etimizol is used for polyarthritis, bronchial asthma, etc. The accumulation of cAMP in tissues plays a role in the mechanism of action of etimizol. Side effects when using etimizol: nausea, dyspepsia, anxiety, sleep disturbances, dizziness. Etimizole is contraindicated in diseases accompanied by central nervous system stimulation. Etimizole is prescribed orally and parenterally (intramuscularly, slowly intravenously). Release form of etimizol: tablets of 0.1 g and ampoules of 3 ml of 1.5% solution. List B.

Example of a recipe for etimizol in Latin:

Rp.: Sol. Aethimizoli 1.5% 3 ml

D.t. d. N. 10 in ampull.

S. 3-5 ml intramuscularly.

Rp.: Tab. Aethimizoli 0.1 N. 50

D.S. 1 tablet 2-3 times a day.

CORDIAMINE- official 25% solution of nicotinic acid diethylamide, stimulates the respiratory and vasomotor centers. Cordiamine is used for heart failure (improves blood circulation), shock, asphyxia, poisoning, infectious diseases (to improve the function of the cardiovascular system and respiration). Cordiamine is prescribed orally and intravenously slowly (for poisoning, shock), subcutaneously, intramuscularly. Cordiamine release form: 15 ml bottle and 1 ml and 2 ml ampoules. List B.

Example of a cordiamin recipe in Latin:

Rp.: Cordiamini 15 ml

D.S. 20-25 drops 2-3 times a day.

Rp.: Cordiamini 1 ml

D.t. d. N. 10 in ampull.

S. 1 ml subcutaneously 1-2 times a day.

MIKOREN- has a powerful stimulating effect on the respiratory center in case of respiratory failure of central and peripheral origin. Mykoren is used for poisoning with drugs that depress the central nervous system (hypnotics, anesthetics, alcohol, etc.), asphyxia of newborns. Mykoren is administered intravenously 0.3-0.5 ml; in emergency cases (coma, respiratory arrest, poisoning) - 3-4 ml (maximum - 10 ml), and then, if necessary, administered at a rate of 3-9 ml/hour in isotonic sodium chloride solution or dextran. Side effects of mycorene: transient paresthesia, agitation, rarely - vomiting, convulsions. Release form of mycorene: ampoules of 1.5 ml of 15% solution (containing 225 mg of mycorene). Foreign drug.

CAMPHOR- stimulates the respiratory and vasomotor centers, and also acts directly on the heart, normalizing metabolic processes in the myocardium. It is also possible that there is a reflex effect on the centers of the medulla oblongata due to the irritating effect of camphor. Camphor has a longer lasting effect than previous drugs. Camphor is used for various infectious diseases, poisonings accompanied by respiratory depression and the functions of the cardiovascular system, for arterial hypotension, collapse, and in the complex therapy of acute and chronic heart failure. Side effects when using camphor: embolism when the oil solution gets into the lumen of the vessel, skin reaction (rash), agitation, convulsions. Camphor is contraindicated in diseases characterized by central nervous system excitation and convulsions. Camphor release form: powder; ampoules of 1 ml and 2 ml of 20% oil solution; bottles of 30 ml of 10% camphor oil and bottles of 40 ml and 80 ml of camphor alcohol.

Example of a camphor recipe in Latin:

Rp.: Sol. Camphorae oleosae 20% pro injectionibus 2 ml

D.t. d. N. 10 in ampull.

Rp.: Camphorae tritae 0.1 Sacchari 0.2

M.f. pulv.

D.t. d. N. 10 in charta cerata.

S. 1 powder 3 times a day.

Rp.: Camphorae tritae 2.0

T-rae Valerianae 20 ml

M.D.S. 20 drops 3 times a day (in hot water after meals).

Rp.: Spiritus camphorati 80 ml

D.S. For rubbing.

SULPHOCAMPHOCAINE- a complex compound of sulfocamphoric acid and novocaine. Sulphocamphocaine is used for acute cardiac and respiratory failure; its action is similar to camphor. This drug (sulfocamphocaine) is not prescribed for hypersensitivity to novocaine and great care is taken when administered to patients with arterial hypotension (due to the possible hypotensive effect of novocaine). Sulphocamphocaine is administered intramuscularly, slowly intravenously and subcutaneously. Release form sulfocamphocaine: ampoules of 2 ml of 10% solution.

Example of a recipe for sulfocamphocaine in Latin:

Rp.: Sol. Sulfocamphocaini 10% 2 ml

D.t. d. N. 10 in ampull.

S. 2 ml under the skin 2-3 times a day.

CARBON DIOXIDE- has a direct stimulating effect on the centers of the medulla oblongata and a reflex effect through the receptors of the sinocorotid zone. Carbon dioxide is formed in the process of metabolism and is a physiological stimulant of the respiratory center; It also stimulates the vasomotor center, causing constriction of peripheral vessels and increasing blood pressure. To stimulate breathing, a mixture of carbon dioxide (5-7%) and oxygen (93-95%), called carbogen, is used. Carbogen is used for overdose of anesthesia, carbon monoxide poisoning, asphyxia of newborns, etc. If after 5-7 minutes from the start of inhalation with carbogen there is no effect, then the administration of carbon dioxide should be stopped, since otherwise more severe respiratory depression may occur. Carbon dioxide is also used in balneology (in medicinal baths) for diseases of the cardiovascular system, dermatology (treatment with “carbon dioxide snow” of warts, neurodermatitis, lupus erythematosus, etc.). Carbonated drinks containing carbon dioxide are used to enhance secretory activity and motility of the gastrointestinal tract.

Breathing stimulants are also lobeline And cititon(see N-hom nomimetics).

Bemegrid (Agypton, Ethymid)

Group affiliation

Mechanism of action

Pharmacological effects

· Analeptic.

· Awakening.

Recipe

Rp.: Sol. Bemegridi 0.5% - 10 ml

D.t.d. No. 5 in amp.

S. 10 ml intravenously slowly 1 time per day.

Indications

· Mild poisoning with barbiturates, narcotic sleeping pills, anesthetics.

Contraindications

· Psychomotor agitation.

Side effects

· Nausea.

· Convulsions.

· Muscle twitching.

Caffeine sodium benzoate

Group affiliation

· Analeptic, direct stimulator of neurons of the respiratory center.

Mechanism of action

· Increases the excitability of the respiratory and vasomotor centers of the medulla oblongata.

· Exhibits antagonism with the inhibitory transmitters of the central nervous system (GABA).

Pharmacological effects:

· Cardiotonic.

· Psychostimulating.

· Analeptic.

· Awakening.

Recipes

Rp.: Sol. Coffeini natrio-benzoatis 10% - 1 ml

D.t.d. No. 10 in amp.

S. 1 ml subcutaneously 2 times a day.

Rp.: Tab. Coffeini natrio-benzoatis 0.1 No. 10

D.S. 1 tablet 2 times a day in the morning.

Indications

· Infectious diseases accompanied by inhibition of the function of the central nervous system, cardiovascular and respiratory systems.

· Poisoning with drugs and other poisons that depress the central nervous system.

· Migraine.

· Decreased mental and physical performance.

· Elimination of drowsiness.

· Enuresis in children.

· Hypotension.

Contraindications

· Increased excitability.

· Insomnia.

· Arterial hypertension.

· Atherosclerosis.

· Organic diseases of the cardiovascular system.

· Senile age.

· Glaucoma.

· Convulsions.

Side effects

· Excitement.

· Insomnia.

· Arrhythmia.

· Increased blood pressure.

Sulfocamphocaine (Sulfocamphoric acid + Procaine)

Group affiliation

· Analeptic of mixed type of action (direct and reflex).

Mechanism of action

· Increases the excitability of the respiratory and vasomotor centers of the medulla oblongata.

· Reflexively stimulates the chemoreceptors of the carotid glomeruli.

Pharmacological effects

· Improves pulmonary blood flow, ventilation and myocardial function.

Recipe

Rp.: Sol. Sulfocamphocaini 10% - 2 ml

D.t.d. No. 10 in amp.

S. 2 ml subcutaneously 2 times a day.

Indications

· Inhibition of the respiratory and vasomotor centers.

Contraindications

· Idiosyncrasy to procaine (novocaine).

· Pregnancy.

· Convulsions.

Side effects

· Reduced blood pressure.

· Allergic reactions.

Etimizole

Group affiliation

· Analeptic of direct action.

· Alveolar surfactant donor.

Mechanism of action

· An antagonist of adenosine, in this case cAMP accumulates, which inhibits the release of lysosomal enzymes - the cells are not destroyed and retain their function.

Pharmacological effects

· Analeptic.

· Sedative (on the cortex).

Recipe

Rp.: Tab. Aethimizoli 0.1 No. 10

D.S. 1 tablet 3 times a day.

Rp.: Sol. Aethimizoli 1% - 3 ml

D.t.d. No. 5 in amp.

S. 3 ml intramuscularly.

Indications

· Rupture of a cerebral aneurysm.

· Pulmonary atelectasis.

· Asphyxia of newborns.

Contraindications

· Psychomotor agitation.

REMEDIES AFFECTING EXECUTIVE BODIES

Antiatherosclerotic agents

1. Drugs that reduce the absorption of cholesterol and bile acids from the intestine (“sequestrants” of bile acids): - cholestyramine (questran, colestipol); - guar resin (guarem).

For respiratory depression, respiratory stimulants are used to stimulate the respiratory and vasomotor centers of the medulla oblongata. Since they restore vital functions (breathing and circulation), they are called analeptics, which means revitalizing agents.

Stimulation of the breathing center leads to an increase in pulmonary ventilation and gas exchange, an increase in oxygen content and a decrease in carbon dioxide in the blood, an increase in oxygen delivery to tissues and the removal of metabolic products, stimulation of redox processes and normalization of the acid-base state. Stimulation of the vasomotor center causes an increase in vascular tone, vascular resistance and blood pressure, improves hemodynamics. Some analeptics (caffeine, camphor, cordiamine) have a direct effect on the heart. The effects manifest themselves mainly against the background of respiratory and circulatory depression.

Most analeptics in large doses can cause convulsions. The difference between respiratory stimulating doses and convulsive doses is relatively small. Convulsions also affect the respiratory muscles, which is accompanied by respiratory and gas exchange disorders, increased stress on the heart and the risk of arrhythmias. A sharp increase in the need of neurons for oxygen with insufficient oxygen delivery leads to hypoxia and the development of degenerative processes in the central nervous system. Analeptics are antagonists of anesthetics, hypnotics, alcohol, narcotic analgesics and provide "awakening" an effect that is manifested by a decrease in the depth and duration of anesthesia and sleep, restoration of reflexes, muscle tone and consciousness. However, this effect is expressed only when large doses are used. Therefore, they should be prescribed in doses sufficient to restore breathing, circulation and some reflexes with mild to moderate depression of these functions. Antagonism between analeptics and CNS depressants double-sided Therefore, in case of an overdose of analeptics and the occurrence of convulsions, anesthesia and sleeping pills are used.

MD analeptics are associated with an increase in neuronal excitability, improvement in the function of the reflex apparatus, a reduction in the latent period and an increase in reflex responses. The stimulating effect is most pronounced against the background of life-threatening depression of the central nervous system.

According to the direction of action, analeptics are divided into 3 groups: 1) direct action on the respiratory center (bemegride, etimizol, caffeine, strychnine); 2) mixed action(cordiamin, camphor, carbon dioxide); 3) reflex actions(lobeline, cititon); Although they have general properties, individual drugs differ in their main and side effects. The choice of drugs depends on the cause of respiratory depression and the nature of the disorders.

Bemegrid used mainly for poisoning with barbiturates and anesthetics, for rapid recovery from anesthesia, as well as for respiratory and circulatory depression caused by other reasons. it is administered intravenously slowly, 5-10 ml of 0.5% solution every 3-5 minutes. until breathing, circulation and reflexes are restored. If convulsive muscle twitching occurs, administration should be stopped.

Etimizole occupies a special position, since, along with excitation of the centers of the medulla oblongata, it has a depressing effect on the cerebral cortex. Therefore, it does not give an “awakening” effect in case of poisoning with anesthetics and hypnotics. It combines the properties of an analeptic and a tranquilizer, as it can even enhance the hypnotic effect. It is used primarily for poisoning with narcotic analgesics, and also in psychiatry as a sedative. Etimizole stimulates the hypothalamus and the production of adrenocorticotropic hormone from the pituitary gland, which is accompanied by stimulation of the adrenal cortex and an increase in the content of corticosteroids in the blood, resulting in anti-inflammatory and antiallergic effects. Therefore, etimizol can be used in the treatment of bronchial asthma and inflammatory processes.

Caffeine described in detail in the lecture on “psychostimulants”. The analeptic effect occurs with pareitheral application of sufficient doses that stimulate the centers of the medulla oblongata. As an analeptic, caffeine is weaker than bemegride, but unlike it, it has a pronounced cardiotonic effect, and therefore has a more significant effect on blood circulation. It is prescribed mainly for alcohol poisoning and a combination of acute respiratory failure and cardiac failure.

Strychnine - an alkaloid from the seeds of the chilibuha, or “vomit nut,” native to tropical areas of Asia and Africa. It stimulates all parts of the central nervous system: enhances the functional activity of the cortex, sensory organs, centers of the medulla oblongata, and spinal cord. This is manifested by improved vision, taste, hearing, tactile sensitivity, muscle tone, heart function and metabolism. Thus, strychnine has a general tonic effect. Strychnine MD is associated with a weakening of postsynaptic inhibition, the mediator of which is glycine. The direct effect on the centers of the medulla oblongata is weaker than that of bemegride, but strychnine increases their sensitivity to physiological stimuli, resulting in an increase in the volume of pulmonary ventilation, an increase in blood pressure and increased vasoconstrictor reflexes. Excitation of the vagal center leads to a slowdown in the heart rate. The spinal cord is most sensitive to strychnine. Even in small doses, strychnine increases the reflex excitability of the spinal cord, which is manifested by increased reflex reactions, increased tone of skeletal and smooth muscles. The weakening of postsynaptic inhibition leads to easier interneuronal transmission of impulses, acceleration of central reflex reactions and increased irradiation of excitation to the central nervous system. At the same time, conjugate (reciprocal) inhibition weakens and the tone of the antagonist muscles increases.

Strychnine has a small breadth of therapeutic action and can accumulate, so an overdose can easily be caused. At poisoning Strychnine sharply increases reflex excitability and develops tetanic convulsions that occur in response to any irritation. After several attacks of convulsions, paralysis of the central nervous system may occur. Treatment: administration of drugs that depress the central nervous system (fluorotane, sodium thiopental, chloral hydrate, sibazone, sodium hydroxybutyrate), muscle relaxants, gastric lavage with potassium permanganate solution, activated charcoal and a saline laxative orally, complete rest.

Strychnine is used as general tonic PM with functional impairment of vision and hearing, with intestinal atony and myasthenia, with sexual impotence of a functional nature, as an analeptic to stimulate breathing and blood circulation. It is contraindicated for hypertension, atherosclerosis, angina pectoris, bronchial asthma, liver and kidney diseases, epilepsy and children under 2 years of age.

Analeptics of mixed action stimulate the respiratory center directly and reflexively through the chemoreceptors of the sinocarotid zone. Cordiamine stimulates breathing and blood circulation. Increased blood pressure and improved blood circulation are associated with a direct effect on the vasoconstrictor center and the heart, especially in heart failure. It is prescribed orally and parenterally for weakened breathing and circulation caused by intoxication, infectious diseases, shock, etc.

Camphor - bicyclic ketone of the terpene series, is part of the essential oils of camphor laurel, camphor basil, etc. Synthetic camphor is also used. Camphor is well absorbed and partially oxidized. Oxidation products combine with glucuronic acid and are excreted by the kidneys. Part of the camphor is excreted through the respiratory tract. Locally has an irritating and antiseptic effect. Stimulates the centers of the medulla oblongata directly and reflexively. It acts slowly, but lasts longer than other analeptics. Camphor increases blood pressure by constricting the blood vessels of the abdominal organs, while dilating the blood vessels of the brain, lungs and heart. The tone of the venous vessels increases, which leads to an increase in venous return to the heart. The different effects of camphor on blood vessels are associated with a stimulating effect on the vasomotor center and a direct dilating effect on the walls of blood vessels. When the heart is depressed by various poisons, camphor has a direct stimulating and detoxifying effect on the myocardium. The cardiotonic effect is due to the sympathomimetic effect and activation of oxidative phosphorylation. In large doses, camphor stimulates the cerebral cortex, especially motor areas, increases reflex excitability of the spinal cord and can cause clonic-tonic convulsions. Camphor enhances the secretion of bronchial glands, thins sputum and improves its secretion, stimulates the secretion of bile and sweat glands. It dissolves poorly in water, but well in oil and alcohol. Therefore, it is used in the form of solutions in oil subcutaneously to improve breathing and blood circulation in case of poisoning and infectious diseases. Prescribed locally in the form of ointments, rubbing in for inflammatory processes, for itching, for the prevention of bedsores, etc. Contraindicated in patients prone to seizures.

Carbon dioxide is a physiological regulator of respiration and blood circulation. It acts directly and reflexively on the respiratory center. Inhalation of 3% CO 2 increases ventilation of the lungs by 2 times, and inhalation of 7.5% increases ventilation by 5-10 times. The maximum effect develops after 5-6 minutes. Inhalation of large concentrations of CO 2 (over 10%) causes severe acidosis, violent shortness of breath, convulsions and respiratory paralysis. Excitation of the vasomotor center leads to an increase in peripheral vascular tone and an increase in blood pressure. At the same time, the vessels of the lungs, heart, muscles and brain expand. The dilation is due to a direct effect on vascular smooth muscle.

Carbon dioxide apply to stimulate breathing in case of poisoning with anesthesia, carbon monoxide, hydrogen sulfide, asphyxia of newborns, in diseases accompanied by weakened breathing, for the prevention of pulmonary atelectasis after anesthesia, etc. It can be used only in the absence of pronounced hypercapnia, since a further increase in the concentration of CO 2 in the blood can cause paralysis of the respiratory center. If after 5-8 minutes. after the start of CO 2 inhalation, breathing does not improve, it must be stopped. Use a mixture of CO 2 (5-7%) with oxygen (93-95%) - carbogen.

Cititon And lobeline stimulate the respiratory center reflexively due to stimulation of the chemoreceptors of the carotid glomeruli. With intravenous administration, a strong and rapid effect develops, but short-term (2-3 minutes). In some cases, especially with reflex cessation of breathing, they can contribute to a stable restoration of breathing and blood circulation. In case of poisoning with anesthetics and hypnotics, these drugs are not very effective.

Analeptic drugs include nalorphine, bemegride, cordiamine, corazol, lobeline, prozerin, cititon, tensilon, sugamin.

NALORPHINE. This analeptic drug is an antagonist of morphine and other opioid analgesics. Synonyms: Lethidron, Nalorphini, Naline. In terms of its chemical structure, antorphine is close to morphine, differing in that the nitrogen atom has an allylic group instead of a methyl group.

Weakens or removes the effects of morphine, fentanyl, promedol, isopromedol, such as respiratory depression, vomiting, hypotension, cardiac arrest. Reduces the hyperglycemic reaction after administration of morphine. In people who have not received morphine, antorphine in clinical doses does not affect breathing or blood circulation. Quite often after its administration, especially after large doses, miosis, increased sweating, drowsiness, nausea or visual hallucinations are observed.

The mechanism of action of nalorphine: it accelerates the removal of morphine from the body 100 times, inhibits the formation of the pituitary antidiuretic factor, which is stimulated by morphine.

It is used as an antidote to morphine and opioid analgesics when there is severe respiratory depression with these drugs, as well as other signs of poisoning, overdose. It is also indicated for asphyxia of newborns, if during childbirth the woman in labor received a large amount of analgesics.

In case of respiratory depression, signs of overdose with barbiturates, ether, cyclopropane and chronic morphinism, antorphine is ineffective. Its use can cause an attack of withdrawal (anxiety, melancholy, vomiting, severe weakness, and sometimes agitation that occurs when a morphine user abstains from morphine).

Single single adult dose 5-10 mg. If there is no effect, repeat the same dose after 8-10 minutes. To obtain an effect, up to 50 mg of antorphine can be administered. The effectiveness of the drug is determined mainly by its effect on breathing. Within seconds after the administration of nalorphine, breathing evens out and becomes quite deep.

For newborns, nalorphine is administered into the umbilical vein at a dose of 5 mg. If there is no effect, the drug injections are repeated. As a prophylactic measure, women in labor who have received large doses of analgesics are administered 10-20 mg intramuscularly 10-12 minutes before the onset of labor.

BEMEGRID(MEGIMID). This analeptic drug is a barbiturate antagonist and a respiratory stimulant. White powder with a melting point of 124-125°. Dissolves in 200 volumes of water. Stimulates the central nervous system, significantly reduces depression of the nervous system caused by barbiturates (hexenal, sodium thiopental, luminal). To a lesser extent, it reduces central nervous system depression caused by ether and some other drugs.

Significantly weakens the depth of barbituric anesthesia and accelerates awakening. Indicated when it is desirable to stop barbiturate anesthesia, to speed up awakening after it, as well as after combined anesthesia with the use of barbiturates and other narcotic substances, in case of barbiturate poisoning. The appearance of cramps in the limbs (should be distinguished from movements associated with awakening) is a signal to stop administering bemegride.

The effectiveness of the drug depends on the depth of anesthesia and the degree of barbiturate poisoning. Depending on the initial condition of the patient in which the drug was administered, it causes the appearance or strengthening of eye reflexes, deepening of breathing, movements of the head and limbs, and restoration of consciousness. Bemegride does not cause serious side effects. Changes in pulse and respiration, sometimes observed after its administration, are associated with the beginning awakening of patients.

CORAZOL. Respiratory analeptic, stimulant of the cardiovascular and central nervous systems. Synonyms: Apgiazol, Cardiazol, Centrazol, Pentamethazolum. Crystalline white powder. Melting point 60°. For clinical use, this analeptic drug is available in tablets, powder, and ampoules. Most often, a solution of corazol is used and it is administered intramuscularly or intravenously.

In terms of pharmacological action, corazol is close to camphor and caffeine. However, due to its good solubility and absorption, its effect occurs faster and for less duration.

It is used when there is a drop in cardiac activity, weakening of breathing associated with depression of the respiratory center during prolonged awakening after anesthesia, in case of poisoning with drugs or analgesics.

In case of prolonged awakening and drug overdose, Corazol is administered intravenously, 200-300 mg, slowly, 1 ml per minute, can be driped with a glucose solution or with blood. For long-term action, the same dose of the analeptic drug can be administered intramuscularly. To stimulate cardiac activity, corazol is administered intravenously, 1-2 ml of a 10% solution.

CORDIAMINE. Respiratory analeptic, stimulant of the central nervous and cardiovascular systems. Synonyms: Anacardon, Cardiamidum, Coramin, Cowitol. Specific gravity 1.023; mix well with water and alcohol. For clinical use it is available in ampoules of 1-2 ml. In its pharmacological action it is very close to corazol. Indications for use and dosages are the same as Corazole.

LOBELIN. An analeptic drug, a respiratory stimulant. In clinical medicine, a 1% solution of lobeline hydrochloride in 1 ml ampoules is used. Although the drug is a respiratory analeptic, it does not speed up awakening and does not stimulate the cardiovascular system. The action is short-term. Used for depression, reflex cessation of breathing. The most effective is intravenous administration of 10 mg. It is necessary to administer slowly, 1 ml per minute, since rapid administration may cause cardiovascular changes.

PROZERIN. An analeptic drug that inhibits the enzyme cholinesterase. This analeptic is used as an antagonist of muscle relaxants. Synonyms: Eustigmin, Myostegmin, Neostegmini, Prostigmin. Available in tablets, powder, eye drops, 1 ml ampoules for intravenous, intramuscular or subcutaneous administration.

Weakens and sometimes completely interrupts the effect of non-depolarizing muscle relaxants or depolarizing relaxants.

The antagonistic effect of this analeptic drug on muscle relaxants is based mainly on the fact that prozerin inhibits the production of cholinesterase. As a result, acetylcholine quickly accumulates, which displaces muscle relaxants from the end plate receptors and makes it possible for excitation to transfer from the nerve ending to the muscle and, consequently, muscle contraction. The so-called direct, immediate effect of proserin on the muscle fiber, which improves the muscle’s response to stimulation, is less pronounced.

The use of prozerin as an antidote to muscle relaxants is indicated when muscle weakness is observed after the end of the action of non-depolarizing muscle relaxants, a weakening of the respiratory amplitude after non-depolarizing muscle relaxants, a change in the action of depolarizing relaxants (causing a non-depolarizing block, weakening of muscle tone or breathing).

Proserin should not be used to stop the action of relaxants when breathing is completely absent, since the concentration of relaxants is high and excessively large doses of proserin will be required, which themselves can cause a neuromuscular block. In addition, if there is a high concentration of relaxants in the blood after the effect of proserine wears off, complete muscle relaxation (recurarization) may occur again.

Method of application: first, 0.5 mg of atropine is administered intravenously. If after the administration of atropine the pulse quickens or remains unchanged, then 2 minutes after atropine, 2 mg of proserine is administered intravenously. When the effect after the first dose is insufficient, a similar dose is re-administered after 3 minutes. A total of 5 mg of proserine can be administered in 20 minutes. Usually, 2 minutes after the administration of the analeptic drug, restoration of muscle activity is observed, the strength of movement of the limbs appears or sharply increases, and the respiratory amplitude increases. Prozerin enhances the effect of depolarizing relaxants such as ditilin. However, when ditilin causes excessively prolonged relaxation and there are no apparent reasons for this (hyperventilation, severe exhaustion and dehydration of the patient), one can assume the presence of a “double block” and use proserin to weaken it. In practice, if 30 minutes after the last administration of ditilin (if it was administered several times) there is still muscle relaxation, spontaneous breathing is weakened and muscle activity is restored gradually, as happens when using non-depolarizing relaxants, we can assume that ditilin acts like non-depolarizing relaxants.

The administration of relatively large doses of proserin, which are used to relieve the effect of muscle relaxants, can cause increased salivation, provoke laryngospasm or bronchospasm, bradycardia up to cardiac arrest. Therefore, prozerin should not be used in patients with asthma or diseases. To prevent bradycardia, it is necessary to administer atropine before using prozerin and be sure to make sure that the drug does not cause the so-called vagotonic effect (pulse reduction). In addition, the most reliable preventive measure to prevent bradycardia and arrhythmia is to maintain the necessary pulmonary ventilation (if necessary, artificial respiration) for the entire time that proserin is in effect.

After the administration of proserin, the patient should be monitored for 45-60 minutes, since after the end of the effect of proserin, recurarization may occur with a sufficient concentration of relaxants in the blood.

TENSILON(edrophonium). This is an analeptic drug, an antagonist of non-depolarizing relaxants. In contrast, proserin mainly has a direct direct effect on the muscle, increasing the amplitude of the end plate potential and promoting muscle contraction.

An important feature of Tensilone is its short duration of action. So, 5-8 minutes after the administration of Tensilon, its effect completely ends. Such a short duration of action makes it possible to use it to find out whether there is a “double block” after the use of ditilin: if, against the background of the action of ditilin, the administration of tensilin increases relaxation, therefore, there is a depolarizing effect usual for a relaxant and proserin and tensilin should not be used. Diagnostic administration of Tensilon will not be dangerous, since its effect will quickly end. If tenzilon has reduced the relaxation caused by ditilin, then proserin can be safely administered, since it is clear that there is a non-depolarizing blockade.

Tenzilon is administered intravenously, a single dose of 5-10 mg. 0.5 mg of atropine is also administered intravenously.

CITITON. An analeptic respiratory drug, it is a solution of the alkaloid cytisine. Transparent liquid. A 0.15% solution in 1 ml ampoules is used.

The indication for the use of cititon is reflex respiratory depression, weakening of respiratory and cardiovascular activity in case of drug overdose. In these cases, 1 ml is usually administered intravenously.

Cititon slightly increases blood pressure, so the administration of this analeptic drug is indicated for a drop in cardiovascular activity; it is contraindicated for hypertension and atherosclerosis.