Analeptics. medicines
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; it differs 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.
The article was prepared and edited by: surgeon
Department of Pharmacology
Lectures on the course “Pharmacology”
Topic: Drugs affecting respiratory function
Assoc. ON THE. Anisimova
In the treatment of acute and chronic respiratory diseases, which are widespread in medical practice, drugs from various groups can be used, including antimicrobial, antiallergic and other antiviral.
In this topic, we will consider groups of substances that affect the functions of the respiratory apparatus:
1. Breathing stimulants;
2. Bronchodilators;
3. Expectorants;
4. Antitussives.
I. Respiratory stimulants (Respiratory analeptics)
Respiratory function is regulated by the respiratory center (medulla oblongata). The activity of the respiratory center depends on the content of carbon dioxide in the blood, which stimulates the respiratory center directly (directly) and reflexively (through the receptors of the carotid glomerulus).
Causes of respiratory arrest:
a) mechanical blockage of the respiratory tract (foreign body);
b) relaxation of the respiratory muscles (muscle relaxants);
c) direct inhibitory effect on the respiratory center of chemical substances (anesthetics, opioid analgesics, hypnotics and other substances that depress the central nervous system).
Breathing stimulants are substances that stimulate the respiratory center. Some means stimulate the center directly, others reflexively. As a result, the frequency and depth of breathing increases.
Substances of direct (central) action.
They have a direct stimulating effect on the respiratory center of the medulla oblongata (see the topic “Analeptics”). The main drug is etimizol . Etimizole differs from other analeptics:
a) a more pronounced effect on the respiratory center and a lesser effect on the vasomotor;
b) longer action – intravenous, intramuscular – the effect lasts for several hours;
c) fewer complications (less tendency to depletion of function).
Caffeine, camphor, cordiamine, sulfocamphocaine.
Substances of reflex action.
Cititon, lobeline – stimulate the respiratory center reflexively due to the activation of N-XP of the carotid glomerulus. They are effective only in cases where the reflex excitability of the respiratory center is preserved. Administered intravenously, the duration of action is several minutes.
The drug can be used as a respiratory stimulant carbogen (a mixture of 5-7% CO 2 and 93-95% O 2) by inhalation.
Contraindications:
Asphyxia of newborns;
Respiratory depression due to poisoning with substances that depress the central nervous system, CO, after injuries, operations, anesthesia;
Restoring breathing after drowning, muscle relaxants, etc.
Currently, breathing stimulants are rarely used (especially reflex ones). They are used if there are no other technical possibilities. And more often they resort to the help of an artificial respiration apparatus.
The introduction of an analeptic gives a temporary gain in time, which is necessary to eliminate the causes of the disorder. Sometimes this time is enough (asphyxia, drowning). But in case of poisoning or injury, a long-term effect is required. And after analeptics, after a while the effect wears off and the respiratory function weakens. Repeated injections →PbD + weakening of respiratory function.
II. Bronchodilators
These are substances that are used to eliminate bronchospasms, as they dilate the bronchi. Used for bronchospastic conditions (BSS).
BSS associated with increased bronchial tone can occur in various diseases of the respiratory tract: chronic bronchitis, chronic pneumonia, some lung diseases (emphysema); in case of poisoning with certain substances, inhalation of vapors or gases. Bronchospasm can be caused by drugs, chemotherapy, V-AB, reserpine, salicylates, tubocurarine, morphine...
Bronchodilators are used in the complex treatment of bronchial asthma (attacks of suffocation due to bronchospasm; infectious-allergic and non-infectious-allergic (atopic) forms are distinguished).
Substances from various groups have the ability to expand the bronchi:
β 2 -AM (α,β-AM),
Myotropic antispasmodics,
Various means.
Bronchodilators are usually used by inhalation: aerosols and other dosage forms (capsules or disks + special devices). But they can be used enterally and parenterally (tablets, syrups, ampoules).
1. Widely used adrenomimetics , which influence β 2 -AR , the activity of the sympathetic nervous system increases, there is a decrease in smooth muscle tone and dilation of the bronchi (+ ↓ release of spasmogenic substances from mast cells, since ↓ Ca ++ and no degranulation).
Selective β 2 -AMs are of greatest practical importance:
Salbutamil (Ventolin),
Fenoterol (Berotek),
Terbutaline (Bricanil).
Less selectivity: Orciprenaline sulfate (asthmopent, alupent).
PC: relief and prevention of bronchial asthma attacks - 3-4 times a day.
When used inhalation in the form of aerosols, as a rule, there are no side effects. But in high doses (orally), headaches, dizziness, and tachycardia may occur.
With long-term treatment with β 2 -AM, addiction may develop, since the sensitivity of β 2 -AR decreases and the therapeutic effect is weakened.
Complex preparations: “Berodual”, “Ditek”, “Intal plus”.
Non-selective AMs can be used to eliminate bronchospasm, but they have many side effects:
Izadrin – β 1 β 2 -AR – effect on the heart, central nervous system; solution / inhalation; pills; aerosols;
Adrenalin - α,β-AM – ampoules (relief of attacks);
Ephedrine - α,β-AM – ampoules, tablets, combined aerosols.
PbD: blood pressure, heart rate, central nervous system.
Drugs that excite the central nervous system. Analeptics. Antidepressants.
Analeptics (analeptica - revitalizing agents) are medicinal substances that stimulate the vital centers of the 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 of mixed type of action (direct and reflex 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), shock conditions. 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 sites of parenteral administration, causing pain at the injection site. Side effects include muscle twitching, anxiety, vomiting, and arrhythmias. 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 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.
An oily solution of 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 the stimulating influence of 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, and to stimulate cardiac activity. When camphor is administered subcutaneously, painful infiltrates may occur at the injection sites.
When camphor is applied topically in the form of ointments, oil and alcohol solutions, its irritating properties are used. 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 a positive effect 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 effect of caffeine depends on the type of 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 disease,
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
The breathing process is known to be regulated by the respiratory center located in the medulla oblongata. The activity of the respiratory center depends on the concentration of carbon dioxide (CO₂) in the blood. The latter affects the respiratory center directly and reflexively, stimulating the receptors of the sinocarotid zone.
The pathology of the respiratory system is very diverse. Respiratory arrest is life-threatening, occurring mainly as a result of depression of the respiratory center (poisoning with alcohol, carbon monoxide, sleeping pills, asphyxia of newborns). In this situation apply respiratory stimulants, or respiratory analeptics- drugs that enhance breathing.
Breathing stimulants are substances that affect the respiratory center, resulting in an increase in the frequency and depth of breathing. Therapeutic doses of these drugs are usually close to convulsive doses, which significantly limits their use.
Prescription of respiratory analeptics should be avoided for coronary heart disease, hypertension, epilepsy (due to the risk of developing seizures). It is not recommended to use respiratory stimulants if hypoxemia is not accompanied by hypercapnia, in case of neurological diseases and pathology of the muscular system, or in case of drug overdose.
Classification of respiratory analeptics
❶ Central acting agents: bemegrid; caffeine; etimizol.
Mechanism of action These drugs look like this:
direct stimulation of the respiratory center ➜ flow of nerve impulses along the efferent (descending) part of the reflex arc to the respiratory muscles ➜ increased contractile activity of the respiratory muscles: diaphragm, intercostal and abdominal muscles.
❷ Reflex agents: lobeline; cititon.
Mechanism of action: stimulation of N-cholinergic receptors of the carotid sinus, increased impulses along the afferent (ascending) part of the reflex arc ➜ excitation of the respiratory center ➜ flow of nerve impulses along the efferent (descending) part of the reflex arc to the respiratory muscles ➜ increased contractile activity of the respiratory muscles ➜ increased volume of the chest, stretching of the bronchi ➜ The pressure in the bronchi becomes lower than atmospheric pressure, which leads to the entry of air into the bronchi.
This class of respiratory stimulants is used quite rarely due to low efficiency (mainly for drowning and asphyxia of newborns).
❸ Mixed action agents: niketamide (cordiamin).
Mechanism of action This drug includes a direct and reflex effect on the respiratory center.
Sources:
1. Lectures on pharmacology for higher medical and pharmaceutical education / V.M. Bryukhanov, Ya.F. Zverev, V.V. Lampatov, A.Yu. Zharikov, O.S. Talalaeva - Barnaul: Spektr Publishing House, 2014.
2. Pharmacology with formulation / Gaevy M.D., Petrov V.I., Gaevaya L.M., Davydov V.S., - M.: ICC March, 2007.
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 anesthetics, 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).
