The sensitivity of H-cholinergic receptors to the action of drugs is different, which also manifests itself with blockade of H-cholinergic receptors. Medicines of one group block H-cholinergic receptors of the autonomic ganglia, sinocarotid zone, and adrenal medulla - ganglion blockers; another group - block H-cholinergic receptors at neuromuscular synapses - peripherally acting muscle relaxants or curare-like drugs.

GANGLION BLOCKERS

By blocking H-cholinergic receptors of the sympathetic and parasympathetic autonomic ganglia, drugs in this group cause a number of characteristic changes:

Ganglion blockers dilate blood vessels and reduce blood pressure, which is due to the blockade of sympathetic ganglia and the elimination of sympathetic vasoconstrictor impulses;

Ganglion blockers reduce the release of adrenaline by blocking H-cholinergic receptors in the adrenal medulla;

Ganglion blockers reduce impulses to the vasomotor center from the carotid glomerulus, blocking H-cholinergic receptors in the carotid sinocarotid zone; these properties of ganglion blockers are used to treat hypertension, however, it should be borne in mind that this may cause a sharp drop in blood pressure, especially when changing body position - orthostatic collapse (therefore, after taking ganglion blockers, you should be in a horizontal position for 2-3 hours); dilation of the vessels of the lower extremities and improvement of their blood supply make it possible to use ganglion blockers also for the treatment of diseases accompanied by peripheral circulatory disorders (obliterating endarteritis, etc.); They are also used for pulmonary and cerebral edema, as well as for controlled hypotension during operations to reduce blood loss (short-acting ganglion blockers);

Ganglion blockers reduce the tone of smooth muscles of internal organs and reduce the secretion of glands, including glands of the gastrointestinal tract; this allows them to be used for the treatment of gastric and duodenal ulcers, hyperacid gastritis, etc.;

Ganglioblockers have (some ganglioblockers) a stimulating effect on the muscles of the uterus (for example, pachycarpine increases the tone of the muscles of the uterus and also reduces blood pressure, which is used during childbirth, especially in the case of high blood pressure in women in labor);

Ganglion blockers reduce the effect of sympathetic innervation on organs; used in surgical practice as premedications prescribed before surgery in combination with other drugs.

Due to side effects (orthostatic collapse, intestinal and bladder atony, dry mouth, impaired accommodation, development of addiction), ganglion blockers are currently used as inpatient therapy.

SHORT-ACTING GANGLION BLOCKERS

IMEKHIN- used for controlled hypotension, for pulmonary and cerebral edema, to relieve a hypertensive crisis. Imekhin is administered intravenously as a 0.01% solution of the drug in a 5% glucose solution or isotonic sodium chloride solution. Side effects when using imekhin: allergic reactions. Imequin should not be administered in the same syringe with barbiturates. Imekhin release form: ampoules of 1 ml and 2 ml of 1% solution. List B.

An example of a recipe for imekhin in Latin:

Rp.: Sol. Imechini 1% 1 ml

D.t. d. N. 6 in ampull.

S. Dilute 1 ml of 1% solution in 100 ml of 5% glucose solution and administer intravenously 90-120 drops per day

HYGRONIUM(pharmacological analogues: trepirium iodide) - used for controlled hypotension in the form of a 0.1% solution for nephropathy in pregnant women, eclampsia. Hygronium is used to relieve a hypertensive crisis. Side effects of hygronium: a sharp decrease in blood pressure. Hygronium release form: 10 ml ampoules containing 0.1 g of drug powder. List B.

Example of a recipe for hygronia in Latin:

Rp.: Hygronii 0.1

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

S. Dissolve the contents of the ampoule in an isotonic sodium chloride solution and administer intravenously.

LONG-ACTING GANGLION BLOCKERS

BENZOHEXONIUM(pharmacological analogues: hexamethonium benzosulfonate) - used for the treatment of hypertension, relief of hypertensive crises, spasm of peripheral vessels, gastric and duodenal ulcers, bronchial asthma. Benzohexonium is administered orally, subcutaneously, intramuscularly. Side effects when using benzohexonium: orthostatic collapse, mydriasis, bladder atony. Contraindications to the use of benzohexonium: arterial hypotension, liver and kidney dysfunction. Release form of benzohexonium: tablets of 0.1 g and ampoules of 1 ml of 2.5% solution. List B.

Example of a benzohexonium recipe in Latin:

Rp.: Tab. Benzohexonii 0.1 N. 20

D.S. 1 tablet 3 times a day.

Rp.: Sol. Benzohexonii 2.5% 1 ml

D.t. d. N. 6 in ampull.

S. 1 ml intramuscularly 1 time per day.

PENTAMINE(pharmacological analogues: Azamethonium bromide) - indications for use, side effects and contraindications for use are the same as for benzohexonium. Pentamine release form: ampoules of 1 ml of 5% solution. List B.

Example of a pentamin recipe in Latin:

Rp.: Sol. Pentamini 5% 1 ml

D.t. d. N. 6 in ampull.

S. 0.5 ml intramuscularly, gradually increasing the dose to 1 ml 2-3 times a day.

DIMECOLINE(pharmacological analogues: dimecoline iodide) - is close in action to benzohexonium. Dimecoline has the same indications for use, side effects and contraindications. Caution is required when combined with nitroglycerin, the effect of which is potentiated by dimecoline. Dimecoline release form: tablets of 0.025 g. List B.

Example of a recipe for dimecoline in Latin:

Rp.: Tab. Dimecolini 0.025 N. 50

D.S. 1 tablet 2 times a day, gradually increasing the dose to 2 tablets 2 times a day.

PACHYCARPINE HYDRIOIDIDE- used for spasms of peripheral vessels, to stimulate labor and reduce bleeding in the postnatal period. Pachycarpine hydroiodide is prescribed orally, subcutaneously, intramuscularly. Pachycarpine hydroiodide is contraindicated during pregnancy, severe hypotension, liver and kidney diseases. Release form pachycarpine hydroiodide: tablets 0.1 g; ampoules of 2 ml of 3% solution. Pachycarpine hydroiodide is available only with a doctor's prescription! List B.

Example of a recipe for pachycarpine hydroiodide in Latin:

Rp.: Tab. Pachycarpini hydroiodidi 0.1 N. 12

D.S. 1 tablet 2 times a day.

Rp.: Sol. Pachycarpini hydroiodidi 3% 2 ml

D.t. d. N. 10 in ampull. S. 2-4 ml intramuscularly 1 time per day.

CAMPHONIUS(pharmacological analogues: trimethidine methosulfate) - gives a pronounced ganglion-blocking effect. Camphonium is prescribed orally and parenterally (subcutaneously, intramuscularly). Indications for use, side effects and contraindications are typical for ganglion blockers. Kamphonium release form: powder; tablets 0.01 g; ampoules of 1 ml of 1% solution. List B.

Example of a camphonium recipe in Latin:

Rp.: Tab. Camphonii 0.01 N. 20

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

Rp.: Sol. Camphonii 1% 1 ml

D.t. d. N. 10 in ampull. S. 1 ml intramuscularly 1-2 times a day.

QUATERON- the action is close to benzohexonium. Quateron has the same indications for use, side effects and contraindications. Quateron is sometimes used to treat angina pectoris. Release form of quateron: powder and tablets of 0.02 g. List B.

Example of a quaterone recipe in Latin:

Rp.: Tab. Quateroni 0.02 N. 25

D.S. 1-2 tablets 3-5 times a day.

PYRYLENE(pharmacological analogues: pempidine tosylate) - used in the same cases as benzohexonium, has the same contraindications and side effects. Pyrylene release form: tablets of 0.005 g. List B.

Example of a pyrylene recipe in Latin:

Rp.: Tab. Pirileni 0.005 N. 20

D.S. 1-2 tablets 3-4 times a day.

TEMEKHIN- has indications for use, contraindications, side effects characteristic of ganglion blockers of this group. Tamekhin release form: tablets0.001 g each. List B.

Example of a tamehin recipe in Latin:

Rp.: Tab. Temechini 0.001 N. 50

D.S. 1 tablet 2-4 times a day.

Federal Agency for Education

State educational institution of higher professional education

Kola branch of Petrozavodsk State University

University department

Test

Discipline: "Clinical pharmacology"

Ganglioblockers. Curare-like remedies

4th year students (group M/2004 - 5)

correspondence department

Revvo Olga Nikolaevna

Teacher:

Evstigneeva Antonina Petrovna

Apatity 2007

Introduction

1. Ganglioblockers

1.1 Mechanism of action and main pharmacodynamic effects

1.2 Pharmacokinetics

1.3 Indications and dosage regimen

1.4 Contraindications and side effects

2. Curare-like agents

2.1 Mechanism of action and main pharmacodynamic effects

2.2 Indications for the use of curare-like drugs

2.3 Pharmacokinetics and dosage regimen of drugs

2.4 Contraindications and side effects

Conclusion

List of used literature

Introduction

Ganglion blockers and curare-like drugs belong to one large group of drugs that affect efferent innervation, but they are completely different drugs in their effect on the human body.

Ganglion-blocking substances have the ability to block n-cholinergic receptors of the autonomic nerve ganglia and, therefore, inhibit the transmission of nervous excitation from preganglionic to postganglionic fibers of the autonomic nerves. Modern ganglion blockers inhibit or completely turn off the conduction of nerve impulses in the sympathetic and parasympathetic nodes, sinocarotid glomerulus and chromaffin tissue of the adrenal glands, which leads to temporary artificial denervation of internal organs and a change in their function. However, different drugs may have different activities in relation to different groups of ganglia. The first ganglion blocker to receive practical use in medicine in the early 50s was hexamethonium (hexonium). Then a number of other ganglion blockers were obtained; some of them, like hexamethonium, are quaternary ammonium compounds, and some are tertiary amines.

Curare-like drugs used in medicine to relax skeletal muscles, mainly during surgical operations. The effect of these drugs is associated with their specific effect on cholinergic receptors in the area of ​​motor nerve endings. Curare is a mixture of condensed extracts from South American plants of the species Strychnos (S.toxifera, etc.) and Chondodendron (Ch. tomentosum, Ch. Platyphyllum, etc.); has long been used by the local population as arrow poison. A wound from a poisoned arrow causes immobilization of the animal or death as a result of asphyxia caused by the cessation of contractions of the respiratory muscles. In 1935, it was established that the main active ingredient of “pipe” curare and Chondodendrontomentosum is the alkaloid d-tubocurarine. d-Tubocurarine has found application in medicine as a skeletal muscle relaxant (peripheral muscle relaxant).

The purpose of the work is to study the pharmacological properties of the presented groups of drugs, as well as the possibility of using them in practical medicine.

1. Ganglioblockers

1.1 Mechanism of action and main pharmacodynamic effects

Ganglion blockers competitively block n-cholinergic receptors and inhibit the transmission of nerve impulses in the ganglia of the sympathetic and parasympathetic nerves. Some drugs (benzohexonium, pentamine, pyrylene, dimecoline) block the sympathetic and parasympathetic ganglia to almost the same extent, others act predominantly on the parasympathetic ganglia (quaterone). In large doses, these substances can block n-cholinergic receptors at neuromuscular synapses and the central nervous system. By interrupting the transmission of nerve impulses through the autonomic nerve nodes, ganglion blockers change the functions of organs supplied with autonomic innervation. In this case, a decrease in blood pressure occurs, which is associated primarily with a decrease in the flow of vasoconstrictor impulses to the blood vessels and the expansion of the peripheral vascular bed (primarily arterioles). Inhibition of the conduction of impulses along cholinergic nerve fibers leads to impaired accommodation, dilation of the bronchi, decreased motility of the gastrointestinal tract, inhibition of gland secretion, increased heart rate, and decreased bladder tone. Inhibition of chromaffin tissue of the adrenal glands leads to a decrease in the release of adrenergic substances and a weakening of reflex pressor reactions.

Some ganglion blockers (pachycarpine, dimecoline) have a direct stimulating effect on the contractile activity of the uterus. Pachycarpine hydrochloride increases the tone and enhances contractions of the myometrium, without causing, unlike pituitrin, an increase in blood pressure, and therefore pachycarpine can be prescribed for weak labor in women in labor with concomitant hypertension.

1.2 Pharmacokinetics

According to their chemical structure, ganglion blockers are divided into quaternary ammonium compounds(benzohexonium, pentamine, dimecoline, hygronium, camphonium, imekhin) and tertiary amines(pachycarpine, pyrylene, etc.). Their main difference is that tertiary amines are better absorbed from the gastrointestinal tract. Quaternary compounds are less absorbed and penetrate the blood-brain barrier poorly, but they are more active when administered parenterally. Based on the duration of action, ganglion blockers are divided into fast-, medium- and long-acting ganglion blockers. To medications fast action include trimetophan camsilate, hygronium, imequin (from 4 to 30 minutes). Average duration actions of pentamine, benzohexonium, quateron - from 2 to 6 - 8 hours. The following have a long duration of action (10–12 hours or more): pachycarpine, camphonium, and dimecoline.

At intravenous administration Ganglioblockers their effect begins after 2 - 3 minutes, the maximum effect occurs after 5 - 10 minutes with the introduction of hygronium, trimetophan, imekhin and after 30 - 60 minutes with the introduction of pentamine, benzohexonium, dimecoline.

At intramuscular and subcutaneous administration the drugs begin to act after 15–20 minutes, and the maximum effect occurs after 30–60 minutes (pentamine, benzohexonium, quaterone, dimecoline, temekhin, pachycarpine, camphonium).

Some ganglion-blocking substances (benzohexonium, quaterone, pyrylene, dimecoline, temekhin, pachycarpine, camphonium) are used to take inside. With this method of administration, their effect begins 30–60 minutes after administration, and the maximum effect is achieved after 1–2 hours.

1.3 Indications and dosage regimen

Short-acting drugs(trimethophan camsilate, hygronium, imekhin) are used mainly in anesthesiology for controlled hypotension and the prevention of autonomic reflexes associated with surgery (in particular, during neurosurgical operations). Brain surgery reduces the risk of brain edema. Correct use of ganglion blocking agents usually reduces the risk of shock and facilitates the postoperative period. In addition, the use of ganglion blockers during general anesthesia reduces the required amount of the narcotic substance. Sometimes they are used to relieve severe hypertensive crises, as well as in obstetric practice for the treatment of nephropathy in pregnant women and eclampsia.

Medium- and long-acting drugs(benzohexonium, dimecoline, pyrylene, temekhin, camphonium) are used orally (rarely) for the treatment of hypertension, toxicosis of pregnancy. For the treatment of hypertensive crises, pulmonary edema against the background of a hypertensive crisis, eclampsia, pentamine, benzohexonium, dimecoline, temekhin, and camphonium are administered parenterally.

Initially, ganglion blockers were widely used for diseases associated with disorders of nervous regulation, when reducing the flow of nerve impulses to the organs could give the desired therapeutic effect. These include arterial hypertension, peripheral vascular spasms (endarteritis, intermittent claudication, etc.), diencephalic syndrome, causalgia, gastric and duodenal ulcers, bronchial asthma, hyperhidrosis, etc. For gastric and duodenal ulcers, chronic cholecystitis , chronic colitis, oral administration of benzohexonium, pyrylene, dimecoline, temekhin, quateron, camphonium is indicated. For spasms of peripheral vessels, pentamine, benzohexonium, and dimecoline are used parenterally. For causalgia, ganglionitis, and sympathalgia, long-acting ganglion blockers were prescribed - pyrylene, dimecoline, temekhin.

Over time, however, it became clear that the use of ganglion blockers is not always quite effective and is often accompanied by side effects: orthostatic hypotension, tachycardia, intestinal and bladder atony, etc. In connection with the advent of new, more effective and selectively acting drugs, the use of ganglion blockers for arterial hypertension and peptic ulcers of the stomach and duodenum has become more limited.

Medium-duration and long-acting drugs are prescribed both parenterally and orally.

Pentamin (Pentaminum) belongs to list B. Available in ampoules of 1 and 2 ml of 5% solution. To achieve a therapeutic effect, it can be administered in the form of a 5% solution 2 – 3 times a day intramuscularly, intravenously, intravenously. In case of hypertensive crises, pulmonary edema, cerebral edema, 0.2 - 0.3 ml or more than 5% solution diluted in 20 ml of isotonic sodium chloride solution or 5% glucose solution is injected into a vein. Administration is carried out slowly, under the control of blood pressure and general condition. There is considerable experience in the effective use of pentamin also for spasms of peripheral vessels, spasms of the intestines and biliary tract, renal colic, bronchial asthma (relief of acute attacks), eclampsia, and causalgia. In urological practice, pentamin is used during cystoscopy in men to facilitate passage of the cystoscope through the urethra. For spasms of peripheral vessels and other diseases, start with the introduction of 1 ml of a 5% solution and then increase the dose to 1.5 - 2 ml 2 - 3 times a day. Higher doses for adults: single 0.15 g (3 ml of 5% pentamine solution), daily 0.45 g (9 ml of 5% pentamine solution)

There are tertiary ganglion blockers: pachycarpine [an alkaloid from the plant Sophora pachycarpa], pyrylene, and quaternary ones - benzohexonium, pentamin, hygronium, quaterone, camphonium, etc.

Ganglion blocking drugs list and their action

Drugs in this group disrupt the conduction of impulses through the autonomic ganglia, while quaterone, camphonium and pyrylene have some advantage on the parasympathetic ganglia. Hygronium has a short duration of action.

Ganglion blockers mechanism of action of drugs

By disrupting the conduction of excitation through the sympathetic ganglia, ganglion blockers reduce the tone of the smooth muscles of the precapillary sphincters, arterioles and venules. As a result, they improve microcirculation in tissues, which is used in the treatment of patients with various forms of shock, infectious toxicosis, burn disease, pneumonia, etc. They increase the deposition of blood in capacitive vessels (veins), which reduces the return of blood to the heart (i.e. preload), and improve its working conditions, especially in acute heart failure. They also lower blood pressure, which facilitates the ejection of blood from the heart into the arterial bed (reduce afterload). Ganglion blockers are prescribed to children for hypertensive crises, cerebral edema, left ventricular failure leading to pulmonary edema, for controlled hypotension during operations on tissues with abundant blood supply.

In children under 3 years of age, ganglion blockers lower blood pressure less than in older children. This is due to the preserved autonomous functioning of the neurons of the corresponding ganglia, which are less dependent on sympathetic neurons. Microcirculation at this age is improved by ganglion blockers in the same way as in other age periods.

Blocking the ganglia of the parasympathetic system leads to a decrease in the secretion of gastric juice, contractions of the intestines and stomach. This is used in the treatment of hyperacid gastritis and peptic ulcers in children.

Ganglion blockers indications for use

The use of ganglion blockers causes a number of complications. The most dangerous of them is orthostatic collapse, i.e. a drop in blood pressure when a person moves from a horizontal to a vertical position. This complication is the result of inhibition of impulses in the sympathetic pathways to the veins. It usually occurs in children over 3 years of age, especially in adolescents. Camphonium, pyrylene and quaterone are less likely to cause this complication. In addition to orthostatic phenomena, ganglion blockers reduce the acidity of gastric juice, cause atonic constipation, urinary retention (the latter contributes to the development of cystitis).

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Azamethonium bromide is a ganglion blocker; it is an ammonium biquaternary compound.

What is the mechanism of action of the ganglion blocker?

The ganglion blocker Azamethonium bromide has a hypotensive effect on the body and also promotes vasodilation, that is, it has a so-called venodilating effect.

As a result of the use of this substance, n-cholinergic receptors are blocked, after which the transmission of nervous excitation is inhibited. The sensitivity of the autonomic ganglia to the stimulating action of certain cholinergic stimuli, for example, cytisine, acetylcholine, nicotine, and lobeline, is suppressed.

By interrupting the conduction of impulses, ganglion blockers affect the function of organs with autonomic innervation. As a result, a decrease in blood pressure occurs, this is associated with a decrease in vasoconstrictor impulses to the vessels and with the dilation of arterioles.

Inhibition of impulses along nerve fibers leads to a change in accommodation, to dilation of the bronchi, the secretory function of the glands is inhibited, the motility of the digestive tract organs decreases, in addition, tachycardia increases, and the tone of the bladder decreases.

In high dosages, Azamethonium bromide can block receptors in skeletal muscles and the nervous system.

What are the indications for use of the ganglion blocker?

There are a number of conditions when Azamethonium bromide is indicated for use, I will list them:

Diseases that are caused by spasm of peripheral vessels, including endarteritis, as well as intermittent claudication;
Azamethonium bromide is part of a combination treatment for cerebral edema, in the presence of a hypertensive crisis, as well as for pulmonary edema;
It is also used in anesthesiological practice to carry out a controlled decrease in blood pressure.

In addition, it is also used in urological practice, for example, for cystoscopy in men to facilitate the advancement of the cystoscope directly through the urethra.

What are the contraindications for use of the ganglion blocker?

Among the contraindications, the following conditions can be noted: angle-closure glaucoma, myocardial infarction in the acute phase, the presence of severe low blood pressure, shock.

In addition, Azamethonium bromide is contraindicated for use in cases of impaired liver or kidney function, certain degenerative diseases of the nervous system, pheochromocytoma, as well as hypersensitivity to the active substance.

What is the use and dosage of the ganglion blocker?

Azamethonium bromide is used intramuscularly, as well as as an intravenous injection. The dose is determined by the doctor individually depending on the indications and clinical situation.

The maximum dosage will be as follows: for intramuscular administration, a single dose corresponds to 150 mg, and the daily dose should not exceed 450 mg. When used together, ganglion blockers can enhance the medicinal effects of adrenergic agonists.

Anticholinesterase drugs are considered ganglion blocker antagonists. When used simultaneously with antidepressants, the hypotensive effect of Azamethonium bromide is reduced.

There is no information on the safety of using Azamethonium bromide during lactation and pregnancy.

What are the side effects of the ganglion blocker?

From the cardiovascular system: an increase in heart rate is noted, orthostatic collapse may occur, as reflex mechanisms that maintain blood pressure levels will be inhibited.

Changes in the urinary system are also possible if Azamethonium bromide is used in large doses for a long time, in particular, atony of the bladder will occur, and anuria may also occur.

From the digestive system: the patient may notice dry mouth; if the use was carried out over a long period, then intestinal atony is possible, which can lead to paralytic obstruction.

From the nervous system: dizziness and general weakness are possible. On the part of the organ of vision: dilation of the pupils, paresis of accommodation, as well as redness of the sclera.

special instructions

Azamethonium bromide is prescribed with caution for bronchial asthma, in the presence of atony of the bladder and intestines, for thrombosis, thrombophlebitis, for some degenerative diseases of the nervous system, in addition, the use is limited in old age.

Treatment with ganglion blockers is recommended to be carried out under the direct supervision of a qualified doctor. To prevent the development of orthostatic collapse, it is necessary to place the patient in a horizontal position before administering Azamethonium bromide, and also after the injection, the patient must be in a supine position for at least one hour.

If there is a history of open-angle glaucoma, intraocular pressure may decrease, this is due to a sharp decrease in aqueous humor, which occurs under the influence of ganglion blockers.

Preparations containing Azamethonium bromide

Pentamine in solution for intravenous and intramuscular administration, as well as in powder.

Conclusion

We talked about the parameters that describe Azamethonium bromide (ganglionic blocker): indications for use, side effects, mechanism of action, overdose. Azamethonium bromide is recommended to be used only after preliminary consultation with a specialist, and you must adhere to exactly the dosage recommended by the treating doctor.

Be healthy!

Mechanism of action: block H-ChRs of the sympathetic and parasympathetic ganglia, the adrenal medulla and the carotid glomerulus.

According to their chemical structure, ganglion blockers are divided into:

Quaternary ammonium compounds: benzohexonium, pentamine, dimecoline, hygronium.

Tertiary amines: pachycarpine, pyrylene.

According to the duration of action, ganglion blockers are divided into:

Long-acting ganglion blockers (6-10 hours or more): benzohexonium (hexonium), dimecoline, pyrylene (pempidine tonsilate).

When the sympathetic and parasympathetic ganglia are blocked, the flow of impulses from the central nervous system to peripheral tissues decreases, which leads to a decrease in vascular tone, intestinal motility, production of exocrine glands, etc.

Medium-acting ganlioblockers (4-6 hours): pentamine (azamethonium).

Short-acting ganglion blockers (10-15 minutes): hygronium, arfonade.

Indications for the use of ganglion blockers:

Edema of the lungs, brain (pyrylene, pentamine).

Controlled hypotension in anesthesiology (hygrony).

Eclampsia, causalgia (pentamine, pachycarpine).

Relief of hypertensive crises (pentamine, benzohexonium).

Peptic ulcer of the stomach and duodenum (benzohexonium, pyrylene).

Obliterating endarteritis, spasm of peripheral vessels (pyrylene, pachycarpine, benzohexonium, pentamine).

Toxicosis of pregnancy (pyrylene).

Rodostimulation (pachycarpine).

Spasm of the intestines and biliary tract, renal colic (pentamine).

Baby Features: Children are prescribed only for hypertensive crises, edema of the brain, lungs, and left ventricular failure.

Side effects:

Constipation, bloating, intestinal atony (myasthenic syndrome) and bladder (urinary retention).

Tachycardia.

General weakness, dizziness.

Dry mouth.

Visual impairment.

Thrombosis.

Muscle relaxants (MR)

Antidepolarizing Mixed Depolarizing

Pipecuronium bromide Dioxonium Dithiline

(arduan), pancuronium

bromide, atrocurium

(traquarium), mevacu-

riy (mevacron).

Mechanism of action of anti-depolarizing MRs: block H-ChRs of skeletal muscles and compete with ACh for interaction with receptors.

Mechanism of action of depolarizing MRs: first, skeletal muscle H-AChRs are briefly activated (cholinomimetic phase). As a result, depolarization of the receptor membrane occurs, accompanied by fibrillation of skeletal muscles with loss of K. Depolarization is then replaced by loss of sensitivity of the receptor to ACh - desensitization. It is considered as a consequence of changes in the conformation of the receptor and the inhibitory effect of K on K-Na-ATPase, which delays the repolarization of the postsynaptic membrane and the restoration of its response to incoming impulses.

Mechanism of action of mixed MR: first induces a depolarizing phase and then acts as an anti-depolarizing MR. In the second phase, prozerin weakens the effect of dioxonium. During anesthesia with ether and fluorothane, the effect of dioxonium increases. See Figure 4.

Fig.5. Mechanism of action of muscle relaxants.

Indications for use:

Anesthesiology: tracheal intubation, endoscopic procedures (ditilin, dioxonium).

Reposition of bones in case of fracture, reduction of dislocations (vecuronium bromide, pancuronium bromide).

Treatment of tetanus, convulsive conditions (alcuronium chloride, dithiline).

Immobilization of the eyeball (ditilin).

Side effects:

Respiratory depression.

Muscle postoperative pain.

Cardiac arrhythmias.

Bronchospasm.

Hypokalemia.

Hyperhidrosis.

Increased intraocular pressure.

Neuromuscular block.

Children's features: children of the first years of life are highly sensitive to antidepolarizing muscle relaxants, this is due to a small supply of ACh in presynaptic endings. When excitation arrives, less ACh is released into the synaptic cleft. But the effect of using these drugs disappears faster than in adults. Most often used in anesthesiology.