Drugs that excite the central nervous system. Analeptics. Antidepressants.

Analeptics (analeptica - revitalizing agents) are called medicinal substances, which stimulate vital centers medulla oblongata- respiratory and vasomotor. IN large doses analeptics can stimulate other parts of the central nervous system and cause convulsions. For this reason, analeptics are sometimes called convulsive poisons.

Bemegride, Niketamide, camphor, sulfocamphocaine, and caffeine are used as analeptics.

Analeptics differ in their mechanism of action. Some drugs (bemegride, camphor) directly stimulate the respiratory and vasomotor centers. They are direct acting drugs. A number of analeptics carry out their action reflexively. The reflex analeptics cititon (0.15% solution of cytisine) and lobelia excite N-cholinergic receptors in the sinocarotid zone; from these receptors, impulses travel along afferent pathways to the medulla oblongata and stimulate the respiratory and vasomotor centers. These drugs are ineffective in suppressing the reflex excitability of the respiratory center with anesthetics and narcotic-type hypnotics (for example, barbiturates). Lobelia and cytisine can stimulate breathing in cases of newborn asphyxia and carbon monoxide poisoning. The drugs are administered intravenously. Niketamide has a mixed effect (direct and reflex).

Bemegrid(ahypnone) is a highly active analeptic of synthetic origin. It has a stimulating effect on breathing and blood circulation, exhibiting antagonism to hypnotics (especially barbiturates) and anesthetics.

The drug is administered intravenously for mild barbiturate poisoning (for severe barbiturate poisoning, bemegride is not very effective), as well as to speed up recovery from anesthesia in the postoperative period. In case of overdose, bemegride causes convulsions.

Niketamide(cordiamin) - 25% solution of nicotinic acid diethylamide - refers to analeptics mixed type action (direct and reflexive at the same time). On the one hand, niketamide has an analeptic effect, directly stimulating the respiratory and vasomotor centers, especially when their tone is reduced. On the other hand, its analeptic effect is complemented by a reflex effect - from the chemoreceptors of the carotid glomeruli.

Indications for the use of the drug are circulatory disorders, decreased vascular tone and weakened breathing in patients with infectious diseases, collapse and asphyxia (including asphyxia of newborns), states of shock. Niketamide is used orally (in drops) or parenterally, 15-40 drops are taken orally 2-3 times a day 30-40 minutes before meals, with a sufficient amount of liquid.

The drug is well absorbed from the gastrointestinal tract and from places parenteral administration, causes pain at the injection site. As side effects muscle twitching, anxiety, vomiting, and arrhythmias are noted. In case of an overdose of the drug, tonic-clonic convulsions occur. Contraindicated in cases of predisposition to convulsive reactions or epilepsy.

Camphor- a compound obtained from the camphor tree (dextrorotatory isomer) or from fir oil(levorotatory isomer). Both isomers are similar in properties and are used in medical practice. Camphor has a resorptive and locally irritating effect.

Oil solution camphor is injected under the skin. By the nature of its resorptive effect, camphor is a typical analeptic: it stimulates the respiratory and vasomotor centers.

Camphor stimulates the activity of the heart, increasing the sensitivity of the myocardium to stimulating influence sympathetic innervation and the action of adrenaline.

With the resorptive effect of camphor, its expectorant properties appear: secreted partially by the bronchial glands, camphor stimulates their secretion.

Camphor is used to reduce blood pressure, respiratory depression, to stimulate cardiac activity. When camphor is administered subcutaneously, painful infiltrates may occur at the injection sites.

At local application camphor in the form of ointments, oil and alcohol solutions use its irritating properties. Due to these properties, camphor can have a distracting effect on joint, muscle, and neuralgic pain. Camphor solutions are used to treat the skin to prevent bedsores.

Sulfocamphocaine is a complex compound consisting of sulfocamphoric acid and novocaine. The drug is similar in action to camphor, but unlike it, it dissolves in water and is quickly absorbed when administered subcutaneously and intramuscularly (it does not cause the formation of infiltrates). The drug is used for depression of the respiratory and vasomotor centers (for infectious diseases, cardiogenic shock etc.).

The drug has positive influence on pulmonary ventilation, improves pulmonary blood flow and myocardial function.

Caffeine- alkaloid; found in tea leaves, coffee seeds, cocoa, cola nuts. Its chemical structure is trimethylxanthine. Caffeine differs from other analeptics in that it has not only analeptic, but also psychostimulant properties.

The psychostimulant properties of caffeine are manifested in the fact that caffeine increases mental and physical performance, reduces the feeling of fatigue and the need for sleep. The effects of caffeine depend on the type nervous activity; In some people, caffeine in large doses enhances inhibition processes.

As an analeptic, caffeine is administered parenterally. The analeptic effect of caffeine is manifested by stimulation of the respiratory and vasomotor centers. By stimulating the respiratory center, caffeine increases the frequency and volume of breathing. By stimulating the vasomotor center, caffeine enhances the stimulating effect of sympathetic innervation on the heart and blood vessels.

Caffeine also has a direct effect on the heart and blood vessels - it increases the frequency and strength of heart contractions and dilates blood vessels.

The mechanism of the stimulating effect of caffeine on the heart is associated with its ability to 1) inhibit cardiomyocyte phosphodiesterase, 2) stimulate ryanodine receptors.

By inhibiting cardiomyocyte phosphodiesterase, caffeine prevents the inactivation of cAMP; cAMP activates protein kinase, which promotes phosphorylation (activation) of Ca 2+ channels of the cell membrane; Ca 2+ entry into cardiomyocytes increases.

The cardiotonic effect of caffeine is also explained by the activation of Ca 2+ channels (ryanodine receptors) in the membrane of the sarcoplasmic reticulum of cardiomyocytes. At the same time, the release of Ca 2+ from the sarcoplasmic reticulum increases and the level of cytoplasmic Ca 2+ increases.

Ca 2+ ions bind troponin C and thus prevent the inhibitory effect of the troponin-tropomyosin complex on the interaction of actin and myosin.

The vasodilatory effects of caffeine are associated with inhibition of phosphodiesterases and increased levels of cAMP and cGMP in smooth muscle vessels. In this case, cAMP- and cGMP-dependent protein kinases are activated, which leads to a decrease in the level of Ca 2+ and the activity of myosin light chain kinase in the cytoplasm of smooth muscles.

The effect of caffeine on blood pressure depends on your blood pressure level. With a significant decrease in blood pressure (shock, collapse), the central effect of caffeine predominates - blood pressure rises. Caffeine does not change normal blood pressure (the central effect of caffeine is balanced by a direct vasodilator effect).

By blocking the receptors of adenosine, which has bronchoconstrictor properties, and also due to the inhibition of phosphodiesterase, caffeine relaxes the smooth muscles of the bronchi and can prevent bronchospasm. Theophylline (dimethylxanthine), the active principle of aminophylline, has more pronounced bronchodilator properties.

Systematic consumption of caffeine, as well as large quantities of tea and coffee, can lead to neuropsychiatric disorders; It is possible to develop a dependence on caffeine.

Caffeine has weak diuretic properties.

Caffeine is used for conditions accompanied by respiratory and circulatory depression. In combination with non-narcotic analgesics and other drugs (for example, as part of the tablets “Coffetamine”, “Ietamine”, “Pyramein”, “Pentalgin”, etc.), caffeine is used for migraines and headaches of other origins.

Caffeine has low toxicity, but in large doses it can cause agitation. , insomnia, nausea. Caffeine should not be prescribed to persons suffering from insomnia or increased mental excitability.

Caffeine is contraindicated in arterial hypertension, atherosclerosis, heart diseases,

4.3.3.2.Antidepressants(thymoanaleptics)

Antidepressants– medications used to treat depression.

Depression(from lat. depression - suppression, oppression) is a mental disorder, the main manifestation of which is pathologically low mood. It is expressed in different ways - from feelings of boredom and sadness to anhedonia (decreased ability to experience pleasure), feelings of hopelessness, social and psychological impasse. Patients develop pessimism in assessing their abilities, thoughts about their own inferiority and worthlessness, and the idea of ​​guilt before others. Suicide attempts are common.

The most developed biochemical theory of the occurrence of depression. According to this theory, in this disease there is a pathologically reduced level of the monoamines norepinephrine (NA) and serotonin (5-hydroxytryptamine - 5-HT) in the brain, and the sensitivity of the receptors that perceive the effects of these neurotransmitters is reduced. In other words, the development of depression is associated with disruption of serotonergic and noradrenergic transmission in brain synapses.

It has been established that drugs that increase the content of monoamines (NA and serotonin) in the brain have an antidepressant effect.

Antidepressants primarily affect pathologically low mood (depressive affect). They do not cause mood enhancement in healthy people.

Antidepressants differ in their mechanism of action and are divided into the following groups:

Classification of antidepressants by mechanism of action

Analeptic drugs (from the Greek analeptikos - restorative, strengthening) mean a group of drugs that primarily stimulate the vital centers of the medulla oblongata - vascular and respiratory. In large doses, these drugs can excite the motor areas of the brain and cause seizures.

In therapeutic doses, analeptics are used to weaken vascular tone, for respiratory depression, for infectious diseases, in the postoperative period, etc.

Currently, the group of analeptics according to the localization of action can be divided into three subgroups:

1) Drugs that directly, directly activate (I revive

breathing center:

Bemegrid;

Etimizole.

2) Means that reflexively stimulate the breathing center:

Cititon;

Lobelin.

3) Means of mixed type of action, having both direct and

reflex action:

Cordiamine;

Camphor;

Corazol;

Carbon dioxide.

Bemegridum (in amp. 10 ml of 0.5% solution) is a specific antagonist of barbiturates and has a “revitalizing” effect in case of intoxication caused by drugs of this group. The drug reduces the toxicity of barbiturates, relieves respiratory and circulatory depression. The drug also stimulates the central nervous system, so it is effective not only for barbiturate poisoning.

Bemegride is used for acute poisoning barbiturates, to restore breathing upon recovery from anesthesia (ether, fluorotane, etc.), to remove the patient from a severe hypoxic state. The drug is administered intravenously, slowly until breathing and blood pressure are restored,

Side effects: nausea, vomiting, convulsions.

Among direct-acting analeptics, the drug etimizol occupies a special place.

Etimizole (Aethimizolum; in the table, 0, 1; in amps, 3 and 5 ml of 1% solution). The drug activates reticular formation brain stem, increases the activity of neurons in the respiratory center, enhances the adrenocorticotropic function of the pituitary gland. The latter leads to the release of additional portions of glucocorticoids. At the same time, the drug differs from bemegride in its mild inhibitory effect on the cerebral cortex (sedative effect), improves short-term memory, promotes mental work. Due to the fact that the drug promotes the release of glucocorticoid hormones, it has a secondary anti-inflammatory effect.

Indications for use. Etimizole is used as an analeptic, a respiratory stimulant in cases of poisoning with morphine, non-narcotic analgesics, in the recovery period after anesthesia, and in pulmonary atelectasis. In psychiatry, it is used for its sedative effect in anxiety states. Given its anti-inflammatory effect, it is prescribed for the treatment of patients with polyarthritis and bronchial asthma, and also as an antiallergic agent.

Side effects: nausea, dyspepsia.

Reflex-acting stimulants are N-cholinomimetics. These are the drugs cititon and lobeline. They excite H-cholinergic receptors in the sinocarotid zone, from where afferent impulses enter the medulla oblongata, thereby increasing the activity of neurons in the respiratory center. These remedies act for a short time, within a few minutes. Clinically, breathing becomes more frequent and deep, and blood pressure increases. The drugs are administered only intravenously. Used for only one indication - for carbon monoxide poisoning.

In mixed-type agents, the central effect (direct stimulation of the respiratory center) is supplemented by a stimulating effect on the chemoreceptors of the carotid glomerulus (reflex component). These are, as stated above, cordiamine and carbon dioxide. IN medical practice carbogen is used: a mixture of gases - carbon dioxide (5-7%) and oxygen (93-95%). Prescribed in the form of inhalations, which increase breathing volume by 5-8 times.

Carbogen is used for overdose of general anesthetics, carbon monoxide poisoning, and asphyxia of newborns.

The drug cordiamine is used as a respiratory stimulant - a neogalenic drug (prescribed as an official one, but representing a 25% solution of diethylamide nicotinic acid). The effect of the drug is realized by stimulation of the respiratory and vasomotor centers.

Prescribed for heart failure, shock, asphyxia, intoxication.

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• Introduction
• Antitussives
• Expectorants
• Combination drugs
• Bibliography

Introduction

Respiratory analeptics are substances that directly or reflexively stimulate the respiratory and vasomotor centers.

Analeptic drugs (from the Greek analeptikos - restorative, strengthening) mean a group of drugs that stimulate, first of all, the vital centers of the medulla oblongata - vasomotor and respiratory. In large doses, these drugs can excite the motor areas of the brain and cause seizures.

In therapeutic doses, analeptics are used to weaken vascular tone, for respiratory depression, for infectious diseases, in the postoperative period, etc.

Analeptics (analeptics)

Currently, the group of analeptics according to the localization of action can be divided into three subgroups:

1) Drugs that directly, directly, activate the respiratory center (revitalizing):

bemegrid;

etimizol.

2) Means that reflexively stimulate the breathing center:

cititon;

lobeline.

3) Mixed-type agents that have both direct and reflex effects: - cordiamine;

camphor;

corazol;

carbon dioxide.

BEMEGRIDUM (in amp. 10 ml of 0.5% solution) is a specific antagonist of barbiturates and has a “revitalizing” effect in case of intoxication caused by drugs of this group. The drug reduces the toxicity of barbiturates, their inhibition of respiration and blood circulation. The drug also stimulates the central nervous system, therefore it is effective not only in case of poisoning with barbiturates, but also with other drugs that completely depress the functions of the central nervous system. Bemegride is used for acute poisoning with barbiturates, to restore breathing upon recovery from anesthesia (ether, fluorotane, etc.), to remove the patient from a severe hypoxic state. The drug is administered intravenously, slowly until breathing, blood pressure, and pulse are restored. Side effects: nausea, vomiting, convulsions. Among direct-acting analeptics, the drug etimizol occupies a special place.

ETIMIZOL (Aethimizolum; in the table 0, 1; in amp. 3 and 5 ml of 1% solution). The drug activates the reticular formation of the brain stem, increases the activity of neurons in the respiratory center, and enhances the adrenocorticotropic function of the pituitary gland. The latter leads to the release of additional portions of glucocorticoids. At the same time, the drug differs from bemegride in its mild inhibitory effect on the cerebral cortex (sedative effect), improves short-term memory, and promotes mental performance. Due to the fact that the drug promotes the release of glucocorticoid hormones, it has a secondary anti-inflammatory and bronchodilator effect.

Indications for use: etimizol is used as an analeptic, a respiratory stimulant in morphine poisoning, non-narcotic analgesics, in the recovery period after anesthesia, with lung atelectasis. In psychiatry, it is used for its sedative effect in anxiety states. Considering the anti-inflammatory effect of the drug, it is prescribed in the treatment of patients with polyarthritis and bronchial asthma, and also as an antiallergic agent.

Side effects: nausea, dyspepsia.

Reflex-acting stimulants are N-cholinomimetics. These are the drugs CYTITON and LOBELIN. They excite H-cholinergic receptors in the sinocarotid zone, from where afferent impulses enter the medulla oblongata, thereby increasing the activity of neurons in the respiratory center. These remedies act for a short time, within a few minutes. Clinically, breathing becomes more frequent and deep, and blood pressure increases. The drugs are administered only intravenously. Used for only one indication - for carbon monoxide poisoning.

For drugs with a mixed type of action (subgroup III), the central effect (direct stimulation of the respiratory center) is supplemented by a stimulating effect on the chemoreceptors of the carotid glomerulus (reflex component). These are, as stated above, CORDIAMINE and CARBON DIOXIDE. In medical practice, carbogen is used: a mixture of gases - carbon dioxide (5-7%) and oxygen (93-95%). Prescribed in the form of inhalations, which increase breathing volume by 5-8 times.

Carbogen is used for overdose of general anesthetics, carbon monoxide poisoning, and asphyxia of newborns.

As a respiratory stimulant, the drug CORDIAMINE is used - a neogalenic drug (prescribed as an official drug, but is a 25% solution of nicotinic acid diethylamide). The effect of the drug is realized by stimulating the respiratory and vascular centers, which will result in deepening breathing and improving blood circulation, and raising blood pressure.

Prescribed for heart failure, shock, asphyxia, intoxication (intravenous or intramuscular routes of administration), for cardiac weakness, fainting states(drops in mouth).

Antitussives

Drugs in this group suppress cough - a protective mechanism for removing contents from the bronchi. The use of antitussive drugs is advisable when the cough is ineffective (unproductive) or even contributes to retrograde movement secretion deep into the lungs ( Chronical bronchitis, emphysema, cystic fibrosis, as well as reflex cough).

Based on the predominant component of the mechanism of action, two groups of antitussives are distinguished:

1. Centrally acting drugs - narcotic analgesics (codeine, morphine, ethylmorphine hydrochloride - dionine).

2. Drugs of peripheral action (libexin, tusuprex, glaucine hydrochloride - glauvent).

CODEINE (Codeinum) is a drug of central action, an opium alkaloid, a phenanthrene derivative. It has a pronounced antitussive effect, a weak analgesic effect, and causes drug dependence.

Codeine is available as a base and also as codeine phosphate. Codeine is part of a number of combination drugs: Bekhterev's mixture, Codterpin tablets, panadeine, solpadeine (Sterling Health SV), etc.

Ankylosing spondylitis mixture contains an infusion of adonis, sodium bromide and codeine.

Codterpine contains codeine and an expectorant (terpine hydrate or sodium bicarbonate).

MORPHINE - narcotic analgesic, opium alkaloid, phenanthrene group. It has a stronger antitussive effect than codeine, but is rarely used in this regard, as it depresses the respiratory center and causes drug addiction. Used only for health reasons, when the cough becomes life-threatening patient (heart attack or lung injury, organ surgery chest, festering tuberculoma, etc.).

Antitussives with a predominantly peripheral effect include the following drugs:

LIBEXIN (Libexinum; tablets 0, 1) is a synthetic drug prescribed one tablet 3-4 times a day. The drug acts predominantly peripherally, but there is also a central component.

The mechanism of action of libexin is associated with:

with a slight anesthetic effect on the mucous membrane of the upper respiratory tract and facilitating the separation of sputum,

with a slight bronchodilator effect.

The drug does not affect the central nervous system. The antitussive effect is inferior to codeine, but does not cause the development of drug dependence. Effective for tracheitis, bronchitis, influenza, pleurisy, pneumonia, bronchial asthma, emphysema.

respiratory analeptic antiallergic expectorant

Side effects include excessive anesthesia of the mucous membranes.

A similar drug is GLAUCINE, an alkaloid from the yellow mace plant (Glaucium flavum). The drug is available in tablets of 0, 1. The action is to suppress the cough center, sedative effect on the central nervous system. Glaucine also weakens spasm of bronchial smooth muscles during bronchitis. The drug is prescribed to suppress cough in tracheitis, pharyngitis, acute bronchitis, whooping cough. When used, respiratory depression, delayed secretion from the bronchi and expectoration of sputum are noted. A moderate decrease in blood pressure is possible, since the drug has an alpha-adrenergic blocking effect. Therefore, glaucine is not prescribed to persons suffering from hypotension and persons with myocardial infarction.

TUSUPREX (Tusuprex; tablets of 0.01 and 0.02; syrup of 0.01 in 1 ml) is a drug that primarily acts on the cough center without suppressing the respiratory center. Used to relieve cough attacks in diseases of the lungs and upper respiratory tract.

FALIMINT (Falimint; tablets 0.025) - has a weak local anesthetic effect and a good disinfectant effect on the mucous membrane of the oral cavity and nasopharynx, reducing, during inflammation, the phenomenon of irritation of the mucous membranes, the occurrence of reflexes, including cough ones.

All these remedies are prescribed for dry nonproductive cough. If the mucous membrane of the bronchi is dry, if the secretion of the bronchial glands is viscous and thick, cough can be reduced by increasing the secretion of the glands of the mucous membrane of the bronchi, as well as by diluting the secretion, and for this purpose expectorants are prescribed.

Expectorants

Currently there are quite a lot of these funds. They have different mechanisms actions and application points.

According to the primary mechanism of action, expectorants are divided into expectorant stimulants and mucolytic agents (secretolytics).

Classification of expectorants

1. Medicines that stimulate expectoration:

a) reflex action (preparations of thermopsis, marshmallow, licorice, thyme, anise, ipecac, istoda, preparations of plantain leaf, bogulnik herb, coltsfoot, terpene hydrate, sodium benzoate, various essential oils, etc.);

b) direct resorptive action (sodium and potassium iodide, ammonium chloride, sodium bicarbonate, etc.).

2. Mucolytic agents (secretolytics):

a) non-enzymatic (acetylcysteine, methylcysteine, bromhexine);

b) enzymatic (trypsin, chymotrypsin, ribonuclease, deoxyribonuclease).

Expectorants of direct (resorptive) action after oral administration are absorbed, enter the blood and are delivered to the bronchi, where they are secreted by the mucous membrane, stimulate the secretion of the bronchial glands, entering the sputum, dilute it and facilitate its separation. Strengthens bronchial peristalsis. Ammonium chloride and sodium bicarbonate preparations alkalize the contents of the bronchi, which promotes thinning and better discharge of sputum.

Contained in herbal preparations reflex action of alkaloids (in thermopsis - saponins), when administered orally, cause irritation of the receptors of the gastric mucosa and duodenum. At the same time, the secretion of the bronchial glands increases reflexively (via the vagus nerve). Increased bronchial peristalsis, increased activity ciliated epithelium(stimulation of mucociliary transport occurs). The sputum becomes more abundant, thinner, with less protein, and it becomes easier to cough up.

MUKALTIN ​​- a preparation of Althea root is also characterized enveloping effect. Licorice root and its preparation - chest elixir - have an anti-inflammatory effect. Plants thyme, anise, and pine buds contain essential oils that have a reflex effect.

Enzymatic mucolytic agents, preparations of proteolytic enzymes, disrupt peptide bonds in the molecule of sputum proteins (crystalline TRYPSIN and CHYMOTRYPSIN), cause depolymerization of nucleic acids (deoxyribonuclease, ribonuclease), reducing the viscosity of sputum.

BROMHEXINE (Bromhexinum; tab. 0.008) - a non-enzymatic mucolytic agent (secretolytic) leads to depolymerization and liquefaction of mucoproteins and mucopolysaccharide fibers of sputum, thus having a mucolytic effect. The expectorant effect of the drug is also pronounced. Bromhexine increases surfactant synthesis and has a weak antitussive effect.

Other drugs in this group thin the sputum by breaking the disulfide bonds of mucopolysaccharides, thereby reducing the viscosity of the sputum and promoting its better discharge. This group includes ACETYL - and METHYL CYSTEINE (when taking acetylcysteine, bronchospasm may increase). Prescribe 2-5 ml of a 20% solution for 3-4 inhalations per day or wash the trachea and bronchi; intramuscular use is possible.

Expectorants are used for inflammatory diseases upper respiratory tract and complex therapy(together with antibiotics, bronchodilators, etc.) patients with pneumonia, pulmonary tuberculosis, bronchiectasis, bronchial asthma (with increased sputum viscosity, accession purulent infection). In addition, the prescription of these drugs for the prevention of postoperative complications after surgical interventions on the respiratory system and post-intratracheal anesthesia is justified.

Classification of drugs used for bronchial asthma

1. Bronchodilators:

a) neurotropic; b) myotropic.

2. Combined drugs (Ditek, Berodual).

3. Antiallergic drugs.

One of the components complex treatment bronchial asthma are bronchodilators - drugs that dilate the bronchi, since the main component of bronchial asthma is broncho-obstructive syndrome (BOS). BOS is understood as a condition accompanied by periodically occurring attacks of expiratory dyspnea due to bronchospasm, impaired bronchial obstruction and secretion of the bronchial glands. Bronchodilators are used to relieve and prevent bronchospasms.

Neurotropic bronchodilators (adrenergic agents)

A number of different groups of drugs can be used as bronchodilators. One of these is the group of beta-2 adrenergic agonists, which includes both non-selective and selective drugs.

The following drugs are widely used among non-selective beta-agonists for bronchospasms:

ADRENALINE, affecting alpha, beta (beta-1 and beta-2) adrenergic receptors. Typically, adrenaline is used to relieve an attack of bronchial asthma (0.3-0.4 ml of adrenaline subcutaneously). With this method of administration, the drug acts quite quickly and effectively, but does not last long. - EPHEDRINE - alpha-, beta-adrenomimetic of indirect type of action. It is less active than adrenaline, but lasts longer. It is used for both therapeutic (relief of bronchospasm by parenteral administration of the drug) and prophylactic (in tablet form) purposes.

ISADRINE, which is usually used to relieve bronchospasm. For this purpose, the drug is prescribed by inhalation. For prophylaxis, a tablet dosage form of isadrin can be used. The drug, non-selectively acting on beta-adrenergic receptors, stimulates beta-1-adrenergic receptors, resulting in increased heart rate and increased heart rate.

More pronounced tropism for adrenergic receptors bronchial tree has a beta-adrenergic agonist ORCIPRENALINE (alupent, asthmapent; tablets of 0.01 and 0.02; syrup 10 mg per tablespoon; inhaler for 400 doses of 0.75 mg). In terms of bronchodilator activity it is not inferior to isadrin, but has a longer duration of action. The drug is prescribed orally and inhaled, as well as parenterally subcutaneously, intramuscularly, intravenously (slowly). The effect develops after 10-60 minutes and lasts about 3-5 hours. Side effects include tachycardia and tremor.

Among selective beta-adrenergic agonists, agents that stimulate beta-2 adrenergic receptors of the bronchi are of interest:

SALBUTAMOL (duration of effect - 4-6 hours);

FENOTEROL (Berotec; inhaler for 300 doses of 0.2 mg) is the drug of choice, the effect lasts 7-8 hours.

The entire listed group of drugs that affect beta-adrenergic receptors is united by the commonality of their mechanisms of action, that is, pharmacodynamics. Therapeutic effect adrenergic agonists are associated with their effect on adenylate cyclase, under the influence of which cAMP is formed in the cell, which closes calcium channel in the membrane and thereby inhibiting the entry of calcium into the cell, or even promoting its excretion. An increase in intracellular cAMP and a decrease in intracellular calcium entails relaxation of bronchial smooth muscle fibers, as well as inhibition of the release of histamine, serotonin, leukotrienes and other biologically active substances from mast cells and basophils.

To prevent bronchospasms (night attacks of bronchial asthma), long-acting (retarded) beta-adrenergic agonists are produced: salmeterol (Servent), formoterol, bigolterol, etc.

Neurotropic bronchodilators (cholinergics)

Drugs that block the cholinergic innervation of the bronchi, in particular M-anticholinergic blockers, or atropine-like drugs, also have bronchodilator properties. As bronchodilators, they are weaker than adrenergic agonists and at the same time thicken bronchial secretions. The most commonly used drugs in this group are ATROPINE, ATROVENT, METACINE, and PLATIFYLLINE. In this case, the bronchodilator effect is associated with a decrease in cGMP content.

Myotropic bronchodilators

The bronchodilator effect can be achieved using myotropic drugs. Among the myotropic antispasmodics, papaverine and no-shpa are used, but more often, in order to relieve bronchospasm, EUPHYLLIN (Euphyllinum; in tablets of 0.15; in amp. 1 ml of 24% solution for intramuscular administration and in amp. 10 ml of 2.4% solution for injection into a vein). The latter is currently the main myotropic drug for bronchial asthma. It is a theophylline derivative. In addition to the pronounced bronchodilator effect, it also reduces pressure in the pulmonary circulation, improves blood flow in the heart, kidneys, and brain. A moderate diuretic effect is noted. Eufillin has a stimulating effect on the central nervous system. Used in tablets orally for chronic treatment bronchial asthma. May in this case cause dyspepsia. Intramuscular administration the drug is painful. The intravenous route of administration is used for bronchospasm and status asthmaticus. In this case, dizziness, palpitations, and decreased blood pressure are possible.

For prophylactic purposes, long-acting theophylline preparations are used (under the control of the concentration of theophylline in saliva):

I generation: theophylline, diprophylline;

II generation: theotard, teopek, rotafil;

III generation: Teonova, Unifil, Armophylline, Euphylong, etc.

Combination drugs

IN Lately Dual-action drugs: BERODUAL and DITEK are widely used as bronchospasmolytics.

The composition of berodual includes:

beta-2-adrenergic agonist - FENOTEROL;

M-anticholinergic agent - ipratropium bromide (ATROVENT).

The purpose of the combination is to create a complex, the components of which have different structures at their points of application and act through different mechanisms, but are synergistic in their bronchodilator effect.

Ditek contains:

beta-2-adrenergic agonist - FENOTEROL (Berotec), which has a bronchodilator effect;

antiallergic drug - CROMOLIN SODIUM (intal), which inhibits the development of an allergic reaction of HNT.

Thus, ditek allows you to combine two therapeutic principles: prevention and relief of attacks of bronchial asthma.

Antiallergic drugs

In the treatment of patients with bronchial asthma, in addition to true bronchodilators, antiallergic drugs are widely used. These include, first of all, glucocorticoid hormones, which, having the ability to stabilize the membrane of mast cells and their granules, have a bronchodilator effect, as well as an anti-inflammatory effect, which, in general, also has a positive effect. Most often, PREDNISOONE, TRIAMCINOLONE, METHYLPREDNISOLONE, BECLOMETASONE are used for this purpose (this drug is characterized by a slight systemic effect).

Of great importance is CROMOLIN-SODIUM (INTAL), a synthetic drug whose effect is that it reduces the entry of calcium ions into mast cells and stabilizes their membrane. In addition, under the influence of intal, the excitability of bronchial myocytes decreases, and the membranes of these cells become denser. All this generally prevents the process of degranulation of mast cells and the release of spasmogenic compounds from them (histamine, leukotrienes, etc. BAS). Intal is available in the form of a white powder in capsules containing 20 mg of active ingredient. The drug is inhaled 4 times a day using a spinhaler inhaler. The duration of action of the drug is about 5 hours. Dependence on this drug does not develop. Intal is prescribed exclusively for prophylactic purposes. Intal treatment is usually carried out for 3-4 weeks. If the patient's well-being improves daily dose reduce to 1-2 capsules. Side effects: irritation of the nasal mucosa, throat, dry mouth, cough.

KETOTIFEN (zaditen) is another, but newer, antiallergic drug, the mechanism of action is similar to Intal, but in a more convenient dosage form. The drug prevents the degranulation of mast cells and inhibits the release of mediators of allergic inflammation from them. Zaditen has weak antihistamine properties, has a direct antispasmodic effect on the walls of the bronchi and is effective both in atopic bronchial asthma and in asthma of infectious-allergic origin. Maximum effect appears within a few weeks from the start of therapy. Prescribe 1 mg 2 times a day. Side effects include only drowsiness. Overall, this is an effective oral drug.

Means used for acute edema lungs

Pulmonary edema can develop when various diseases of cardio-vascular system, with damage to the lungs by chemical substances, with a number of infectious diseases, diseases of the liver, kidneys, and cerebral edema. Naturally, treatment of patients with pulmonary edema should be carried out taking into account the nosological form of the underlying disease. However, the principles of pathogenetic pharmacotherapy of pulmonary edema are the same.

I. With high blood pressure (with hypertension) primarily the following groups of drugs are used:

1. Ganglioblockers (pentamine, hygronium, benzohexonium)

2. Alpha adrenergic blockers (aminazine, phentolamine, diprazine).

3. Vasodilators myotropic type of action (aminophylline, sodium nitroprusside).

Under the influence of these drugs, blood pressure is normalized, which means hemodynamics, the efficiency of the heart increases, and the pressure in the pulmonary circulation decreases.

4. Diuretics (furosemide or Lasix, mannitol, urea).

III. For certain types of pulmonary edema, for example left ventricular failure, the following is used:

5. Cardiac glycosides (strophanthin, corglycone).

6. Narcotic analgesics (morphine, fentanyl, thalamonal).

The use of these drugs is due to a decrease in the excitability of the respiratory center under the influence of narcotic analgesics. In addition, these drugs, by dilating peripheral vessels, reduce venous return of blood to the heart. Blood redistribution occurs, which reduces blood pressure in the pulmonary circulation.

IV. When the alveoli swell and foam forms in them, antifoam agents are used. The latter include

ETHYL ALCOHOL, the vapors of which are inhaled along with oxygen through a nasal catheter or through a mask. Ethyl alcohol irritates the mucous membranes, which is its side effect. The best defoamer is a silicone compound with surface-active properties, namely ANTIFOMSILAN. The drug has a rapid defoaming effect and does not irritate the mucous membranes. It is administered by inhalation in the form of an aerosol of an alcohol solution with oxygen.

Finally, for pulmonary edema of any origin, preparations of glucocorticoid hormones in injectable dosage form are also used. When administering prednisolone and its analogues intravenously, they rely primarily on the membrane-stabilizing effect of hormones. In addition, the latter sharply increase the sensitivity of adrenergic receptors to catecholamines (permissive effect), which is also important for the anti-edematous effect.

Bibliography

1. http://max.1gb.ru

2. http://www.pharmacological.ru

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Analeptics. Medicines that affect the functions of the respiratory system.

Medicines that affect the functions of the respiratory system are divided into the following groups:

1. Respiratory analeptics;
2. expectorants;
3. antitussives;
4. drugs used for bronchial asthma;
5. drugs used for pulmonary edema.

Respiratory analeptics- these are substances that directly or reflexively stimulate the respiratory and vasomotor centers.

Classification of respiratory analeptics .

1. Direct acting drugs:.

• bemegrid;
• etimizol;
• caffeine.

2. Reflex-action drugs (n-cholinomimetics):

• lobeline;
• cititon.

3. Mixed-action drugs.

• cordiamine;
• camphor;
• sulphocamphocaine.

Mechanism of action of analeptics.

Direct acting drugs directly increase the excitability of the cells of the respiratory center. Etimizole inhibits phosphodiesterase, which leads to an increase in the amount of cAMP, an increase in the release of calcium ions from the endoplasmic reticulum, and this in turn leads to stimulation of the process of glycogenolysis and an increase in the metabolism of neurons in the respiratory center. N-cholinomimetics activate the chromaffin cells of the carotid glomeruli and reflexively (along the Hering nerve) stimulate the respiratory center of the medulla oblongata, as a result of which the frequency and depth of respiratory movements increases.

Pharmacodynamics.

• The stimulating effect on breathing is most pronounced under conditions of suppression of the functions of the respiratory center and a decrease in its reactivity to physiological stimuli (CO2). Restoration of external respiration functions is usually unstable. Repeated administration may cause convulsive reactions.
• Stimulates the vasomotor center. The tone of resistive and capacitive vessels increases, which leads to an increase in venous blood return and an increase in blood pressure. This effect is most pronounced in camphor and cordiamine.
• The anti-drug effect is manifested in a temporary weakening of the depth of depression of the central nervous system, clarification of consciousness and improved coordination of movement. Drugs are indicated if depression does not reach the level of anesthesia. The most pronounced effect is found in bemegride and corazole.

Indications for use.

1. Exacerbation chronic diseases lungs, accompanied by symptoms of hypercapnia, drowsiness, loss of cough;
2. respiratory arrest in premature newborns (Etimizol is used);
3. hypoventilation of the lungs in case of poisoning with drugs that depress the central nervous system, carbon monoxide, during drowning, in postoperative period;
4. collapsed state;
5. cerebrovascular accident (fainting);
6. weakening of cardiac activity in older people.

1. Expectorants– this is a group of drugs that promote the removal of sputum.

Classification.

1. Bronchosecretory agents:

• Reflex agents:
  • thermopsis grass;
  • marshmallow root;
  • tricolor violet herb;
  • mucaltin;
  • terpinhydrate.
• Resorptive agents:
  • potassium iodide;
  • sodium bicarbonate.

2. Direct action expectorants (mucolytics):

• Preparations of proteolytic enzymes:
  • trypsin crystalline;
  • chymotrypsin.
• Synthetic drugs:
  • acetylcysteine.
• Drugs that stimulate surfactant synthesis:

bromhexine; ambroxol (lazolvan).

Pharmacodynamics

• Reduce the viscosity of sputum and improve its separation;
• increase the activity of the epithelium of the bronchial mucosa;
• reduce the amount of infection;
• improve gas exchange by enhancing bronchial drainage;
• weaken inflammatory reactions;
• reduce irritation of the sensitive endings of the mucous membranes.

Mechanisms of action of expectorants.

• Reflex-action drugs contain alkaloids and saponins, which irritate the gastric mucosa. As a result, the impulse is transmitted to the nuclei vagus nerve, and from them through efferent fibers to the smooth muscles and secretory cells of the respiratory tract, which leads to increased secretion of the bronchial glands, improved peristalsis of the bronchioles, and increased activity of the ciliated epithelium. Increasing the volume of secretion reduces irritation of the mucous membrane and helps reduce the inflammatory process.
• Resorptive drugs are administered orally and are secreted by the bronchial glands, which helps thin the sputum and reduce its viscosity. Activate the motor activity of the epithelium of bronchioles. They also have an antimicrobial effect.
• Mucolytics dissolve the protein and nucleic components of pus, fibrin deposits, promote the separation of especially dense mucous sputum that is fused to the surface. Proteolytic enzymes: break protein bonds in sputum components.
• Synthetic drugs (acetylcysteine): is a donor of SH - groups that break the disulfide bonds of sputum mucopolysaccharides, cause depolymerization of sputum and reduce its viscosity.
• Agents that stimulate surfactant synthesis: increase the number and secretory activity of epithelial lysosomes, which leads to an increase in the release of enzymes that hydrolyze protein molecules. They increase secretion of secretions by the bronchial glands. By improving the synthesis of surfactant, gas exchange is normalized.

1. Antitussives – This is a group of drugs that reduce the excitability of the cough center and reduce coughing.

Classification.

1. Centrally acting agents that depress the cough center:

• narcotic analgesics:
  • codeine;
  • morphine hydrochloride.
• Non-narcotic drugs:
  • glaucine (glauvent).

2. Peripheral action:

- libexin.

Indications for use.

Prolonged dry cough in chronic inflammatory diseases of the respiratory tract (dry non-productive cough). In this case, the drugs should eliminate overirritation of the cough center and their use should not impair the drainage of the respiratory tract. These drugs are not used for productive cough. Codeine phosphate.

• Long-term use reduces pulmonary ventilation, therefore it is contraindicated in children under 6 months;
• depresses the respiratory center;
• causes drug dependence.

Glaucine.

• Its action is based on selective inhibition of the cough center;
• does not depress breathing;
• does not inhibit sputum production;
• does not cause drug dependence.

Libexin.

• It has local anesthetic properties, blocks the sensitive endings of cough reflexogenic zones;
• has an antispasmodic effect;
• does not cause addiction;
• does not depress breathing.

4. Medicines used for bronchial asthma.

Classification.

1. Bronchodilators (bronchodilators):

• m – anticholinergics:
• atropine;
• metacin;
• ipratropium bromide.

• Adrenergic agonists:

a , b - adrenergic agonists:

• adrenaline hydrochloride;
• ephedrine hydrochloride.

b - adrenergic agonists:

• isadrin;
• orciprenaline sulfate (alupent).

b 2 – adrenergic agonists:

• salbutamol;
• fenoterol;
• terbutamine.

• Agents that inhibit mast cell degranulation: phosphodiesterase inhibitors:
  • theophylline;
  • aminophylline.

2. Drugs that affect allergy mediators:

• Glucocorticoids:
  • prednisolone;
  • beclomethasone.

Eufillin.

• Inhibits phosphodiesterase activity;
• blocks adenosine receptors;
• stimulates the release of adrenaline.

Pharmacodynamics.

• Reduces pressure in the pulmonary circulation;
  • improves blood flow in the heart, kidneys, central nervous system;
  • has a moderate diuretic effect.

Features of use in bronchial asthma. Eufillin is used as basic therapy. Capable of developing cumulation, which sometimes leads to disruption heart rate, and in high doses the development of convulsions and a collaptoid state is possible.

5. Drugs used for pulmonary edema. Classification.

1. Drugs that reduce pressure in the pulmonary capillaries:

• Agents that dilate capacitance vessels:
  • ganglion blockers (hygronium, benzohexonium);
  • nitrates (sodium nitroprusside).
• Fast acting diuretics:
  • furosemide (Lasix);
  • ethacrynic acid.

2. Means that restore impaired gas exchange(antifoaming):

• ethanol;
• antifomsilan.

3. Agents that reduce the permeability of the blood-alveolar barrier:

• glucocorticoids;
• antihistamines (H1 blockers).

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The human body can become very weak and lose resistance to infections as a result of the development of diseases. This interferes with the normal functioning of all systems and leads to disruptions in the body’s supply useful substances. To restore all functions and return to the body vitality, was developed special group medicines, which is called analeptics. However, in addition to therapeutic effect, such drugs have many quite serious contraindications, which greatly limits their use in therapeutic practice.

Analeptics are medications whose main purpose is to stimulate and restore brain function.

How do they work?

For the most part, these medications act on the medulla oblongata, which is responsible for respiratory function and blood circulation. There are also analeptic drugs that can stimulate other areas of the brain. Active elements force receptors to react vigorously to substances that enter the body or are produced by it itself.

If you take more than the prescribed dose, you need to take into account that the substances contained in analeptics can affect a person’s motor functions, which, in turn, can lead to convulsions.

What kind of means are these?

Analeptics are a group of drugs, the sequence of effects of which on the brain and central nervous system is not fully understood and studied. Until recently, they were used quite widely, but are now fading into the background, as more modern and safe analogues have entered the pharmaceutical market. Experts often criticize analeptics for the high likelihood of side effects such as hypoxia and convulsions.

Classification of analeptics

Most often you can find a classification of analeptics according to the effect that their use has on the respiratory center of the brain:

1. Direct stimulants or respiratory analeptics. They act directly on the neurons of the brain, namely the respiratory center. These include “Caffeine”, “Strychnine”, “Bemegride”, “Securinine”, etc.
2. N-cholinomimetics. They have a reflex effect, stimulating the corresponding receptors in the central nervous system. These include “Cytisin”, “Lobelin” and others.
3. Analeptic drugs with complex effects, combining the two previous types. The most common among them are “Cordiamin” and “Camphor”.

The most popular drugs

The pharmaceutical market offers a wide selection of drugs of this type. pharmacological group, however, the following are the most popular and widespread:

How do they work?

Analeptics are a special group of drugs. It was already said above that medicine has not fully studied the processes of their influence on the human brain and central nervous system. The only obvious fact is their opposite effect: in some patients they stimulate the functioning of certain areas of the brain, while in others, on the contrary, they depress. However, the main task of these medications is to facilitate neural connections and activate the transmission of nerve impulses between them.

The action of analeptics actually extends to all areas of the brain and central nervous system. Depending on the type of drug taken, the effect occurs in relation to the medulla oblongata, cerebral cortex, etc. The effect is approximately as follows: after administration, the analeptic excites the area nervous system, for which he is responsible, which makes the neurons in it more sensitive. Thus, the sensitivity of the selected area of ​​the brain to substances that irritate it also increases. As a result, breathing normalizes and blood pressure increases. Despite the fact that each analeptic stimulates a different part of the brain, the process of influence itself is approximately the same.

Hidden influence

In addition to the obvious effects, analeptic drugs can also affect the body in other ways:

1. Increased vascular resistance.
2. Suppression of the effect of taking narcotic drugs, capable of suppressing the psyche.
3. Suppressing the effect of taking sleeping pills.

Analeptics: indications for use

1. Therapy of asphyxia in newborn infants. This type of treatment has already faded into the background, as other methods have appeared without the use of synthetic drugs.
2. Drug intoxication, sleeping pills, as well as ethyl alcohol and alcoholic beverages.
3. Depressive state after the use of anesthesia in a patient.
4. Cardiovascular failure.
5. IN exceptional cases These drugs are used to treat impotence, paralysis and paresis, as they stimulate muscle activity.
6. Sometimes neuroleptics are also prescribed to patients with hearing and vision pathologies.

Popular analeptics

Although many experts criticize the drugs, some of them remain quite popular. Some of them should be considered.

"Etimizole". Main active substance The drug is a caffeine molecule in which the pyrimidine ring is broken. It mainly affects the area of ​​the respiratory center of the brain without affecting the vasomotor area, which eliminates the occurrence of seizures while taking the drug. In addition, Etimizol is able to elevate mood and stimulate memory function. Thanks to its intake, hypothalamic secretion increases, which allows the body to produce more corticotropin, which is a releasing hormone.

Given medicine It can also perform a regenerative function, affecting damaged areas of the gastric mucosa, and increase protein production. The drug extremely rarely causes side effects.

What other analeptics exist in pharmacology?

"Camphor". It belongs to the terpene group of ketones and appears as hexagonal crystals of a translucent white hue. Except positive effect on respiratory functions, the drug creates an antiarrhythmic effect and normalizes the heartbeat. In addition, while taking Camphor, the heart's need for oxygen saturation increases due to vasodilation. Opposite of expanding coronary arteries V abdominal cavity, the blood vessels of the heart narrow when taking the drug. Due to this, a whole range of necessary for the body substances such as glycogen, creatine phosphate, etc. The use of analeptics must be justified.

Most often used to stimulate the central nervous system in order to increase the physical and mental performance of a person. "Caffeine-sodium benzoate". This drug has an antisedative effect, reducing fatigue and drowsiness. Mostly active substance affects the vasomotor and respiratory centers of the human brain. Caffeine has a positive effect on the functioning of the heart, namely, it increases heart rate and increases striking force. Promotes vasodilation not only of the brain, but also of the kidneys, heart and other organs. This is the most optimal choice for the treatment of drug intoxication, vascular spasms and cardiovascular failure.

Action " Cordiamine"Similar to the previous ones. It affects the vasomotor and respiratory centers of the brain. The effect is closest to that of Caffeine. It differs in that it can be prescribed to relieve symptoms of asphyxia, vascular collapse, as well as in the complex treatment of diseases of infectious origin.

"Bemegrid"- a drug that has a targeted effect. It is chosen if the influence should be exerted only on respiratory function, but not on vascular system. Used in the following cases:

1. Minor intoxication.
2. Overdose of drugs that can suppress the central nervous system.
3. Recovery from anesthesia.

Conclusion

Analeptics are drugs that are quite widely used to solve various problems aimed at improving the patient's condition. They are still often prescribed by doctors to restore respiratory function and initiate recovery processes throughout the body. Some of them are gradually being replaced by more modern and safer analogues. However, analeptics still play a significant role in the treatment of patients with different diagnoses, and the situation is unlikely to change dramatically in the near future.