The use of ganglion blockers in medicine. Ganglioblockers. Mechanism of action. Pharmacological effects. Indications for use. Side effects

This is a group of substances that selectively block H-ChRs of the autonomic ganglia, sinocarotid zone and adrenal medulla.

Blocking both sympathetic and parasympathetic ganglia, Gbl actually eliminate the influence of the VNS on organs and tissues.

Sympathetic ganglion blockade under the influence of GBL is especially noticeably reflected in the tone peripheral vessels, especially arterioles - they dilate, which leads to lower blood pressure . This valuable property of GBL is used in the treatment of hypertension and the elimination of spasms of peripheral vessels. However, blockade of the sympathetic ganglia, carotid sinuses and adrenal medulla disrupts the physiological regulation of vascular tone and can lead to a sharp drop in blood pressure and loss of consciousness (collapse), especially with a rapid transition from a horizontal to a vertical position ( orthostatic collapse). Therefore, after administration of GBL, patients are recommended to stay in bed for 1.5 - 2 hours.

By blocking the parasympathetic ganglia, GBL decrease smooth muscle tone V internal organs (gastrointestinal tract, bladder, etc.) and reduce secretion digestive glands . This property of GBL is used in the treatment of peptic ulcer and duodenal ulcer, smooth muscle spasms internal organs. However, with prolonged administration of GBL, this can lead to intestinal dysfunction (atony, constipation).

Mechanism of action: GBL are capable of binding the mediator acetylcholine. In this case, the flow of impulses from the central nervous system to the executive organs is interrupted in the ganglia and the following pharmacological effects are observed:

Vasodilation, decreased blood pressure

Decreased tone of smooth muscles of internal organs (spasmolytic effect)

Decreased secretion of salivary, digestive, sweat, bronchial glands

Anti-edema effect

Anti-shock effect.

Indications for use of GBL:

GB, hypertensive (hypertensive) crises

Obliterating endarteritis (intermittent claudication) and other peripheral circulatory disorders

Peptic ulcer and duodenum

To prevent cerebral edema and pulmonary edema

For controlled hypotension to reduce bleeding from blood vessels during operations on the heart and blood vessels, during thyroidectomy, mastectomy, etc.

Side effects:

Orthostatic collapse.

Intestinal atony and constipation up to paralytic intestinal obstruction.

Dry skin and mucous membranes.

There may be mydriasis, disturbance of accommodation, dysarthria, dysphagia, urinary retention.

At long-term use addiction develops, which requires increasing doses.

Based on their duration, ganlioblockers are divided into two subgroups:

Long-lasting:benzohexonium(duration of action 3 - 4 hours), pyrylene(duration of action 12 hours), pentamine(acts somewhat shorter than benzohexonium), pachycarpine. They are used for diseases of internal organs associated with nervous regulation disorders. These drugs must meet the following requirements: high activity at in different ways introduction; long duration of action; low toxicity and no side effects.

Short acting:hygronium(10 – 15 minutes), imekhin(arfonade). Used in surgical practice for controlled hypotension. Administered intravenously; the effect occurs quickly, and after cessation of administration, the blood pressure level quickly (after 10–15 minutes) returns to its original level.

BENZOHEXONIUM,Benzohexonium, list “B”, 0.3 inside

White synthetic crystalline powder, salty-bitter taste, highly soluble in water, sensitive to light. The main action of benzohexonium is hypotensive effect In addition, it relaxes smooth muscles, reduces gland secretion, lowers metabolic processes, and can lower body temperature; inhibits the function of the pituitary gland.

Applicable:

1. for spasms of peripheral vessels (endarteritis, intermittent claudication).

2. to relieve hypertensive crises (rarely in hypertension),

3. for the treatment of peptic ulcer (ulcer and duodenal ulcer)

4. for bronchospasms

5. for controlled hypotension (IV)

6. when preparing patients for operations on thyroid gland, since, by inhibiting the pituitary gland, it eliminates the influence of the pituitary gland on the thyroid gland. Mainly used in hospitals.

FV – ampoules of 1 ml of 2.5% solution, tablets of 0.1.

PYRYLENE,Pirilenum, list “B”, 0.005

It is slightly inferior in activity to benzogexonium, but superior in duration of action. Used: for obliterating endarteritis, for gastrointestinal ulcers, for toxicosis of pregnant women, for hypertension in combination with other drugs. Penetrates through the BBB and has a blocking effect on central cholinergic receptors. It is better absorbed when administered orally.

FV – tablets of 0.005.

Contraindications to the use of benzohexonium and pyrylene.

1. Severe atherosclerosis.

2. For intestinal atony, Bladder.

3. In case of dysfunction of the liver and kidneys.

4. For glaucoma, because may increase intraocular pressure.

PENTAMINE,Pentaminum, list “B”, VRD 3 ml 5% solution i.m.

It has a wider application: in anesthesiology (for controlled hypotension), effective in hypertensive crises, spasms of peripheral vessels; for renal, hepatic and intestinal colic, for relief acute attacks BA, with pulmonary and cerebral edema, with ulcerative gastric ulcer and duodenal ulcer.

FV: 5% solution in amps of 1 and 2 ml.

HYGRONIUM,Hygronium, list "B".

It has a short-term ganglion-blocking effect, and therefore is convenient for use in anesthesiology for controlled hypotension. It is administered intravenously in the form of a 0.1% solution.

PAKHIKARPIN,Pachycarpinihydroiodiumlist “B”, 0.2 orally, 5 ml of 3% solution s.c.

- salt of the alkaloid pachycarpine, found in the Sophora thick-fruited plant. Blocks ganglia without prior stimulation, reduces the sensitivity of adrenal tissue and receptors of the carotid glomeruli of the sinocarotid zone. Applicable:

1. for weakness labor activity, because increases the tone of the uterus and enhances its contractions.

2. with muscular dystrophy, 3. with spasms of peripheral vessels, with circulatory disorders in the lower extremities.

Contraindications: Pregnant women, with severe heart pathology, as well as with liver and kidney diseases.

FV – tablets 0.1; in ampoules of 2 ml of 3% solution.

Benzohexonium(Benzohexonium). Synonym: Hexamethonium benzosulfonate (Hexamethoni i benzosnlfonas).

pharmachologic effect : blocks N-cholinergic receptors of the sympathetic and parasympathetic ganglia. It has a vasodilator, antispasmodic and antisecretory effect.

Reduces motor skills gastrointestinal tract, reduces systemic arterial pressure, increases the depositing capacity of veins. Because the drug reduces venous return to the heart and reduces afterload, it increases cardiac output.

Indications: used for hypertensive crises, including those accompanied by left ventricular failure and cerebral hemorrhages. Used for spasms of peripheral vessels during endarteritis, severe attacks bronchial asthma, not eliminated by other drugs (beta-agonists, methylxanthines, M-anticholinergics). Also used for renal and hepatic colic. In anesthesiology it is used for controlled hypotension.

Mode of application: during a hypertensive crisis, 0.5-1 ml of a 2.5% solution (12.5-25 mg of substance) is administered subcutaneously or intramuscularly. For controlled hypotension, 1 - 1.5 ml of a 2.5% solution is prescribed intravenously over 2 minutes.

If necessary, the injection is repeated. For the rest Indications m is prescribed orally before meals, 0.1 g 3-6 times a day. Maximum doses for adults when taken orally they are: single - 0.3 g, daily - 0.9 g; for subcutaneous administration: single dose - 0.75 g, daily dose - 0.3 g of the drug.

Side effect : Possible orthostatic collapse. To prevent this phenomenon, after the administration of benzohexonium, the patient must maintain a horizontal body position for 2 hours. Atony of the intestines and bladder, mydriasis, impaired accommodation, increased intraocular pressure. With prolonged use, the effect of the drug decreases.

Contraindications: hypotension, acute heart attack myocardium, thrombosis cerebral arteries, pheochromocytoma, closed form glaucoma, as well as severe violations liver and kidney functions. : severe hypotension that occurs with an overdose of benzohexonium can be eliminated by the administration of norepinephrine or mesatone.

Release form: tablets of 0.1 and 0.25 g; 2.5% solution in ampoules of 1 ml.

Storage conditions: list B.

Hygronia(Hygronium). Synonym: Trepirium iodide.

pharmachologic effect: is a ganglion blocker (see also Benzohexonium). Has a short-term effect. Indications: in anesthesiology used to produce controlled hypotension. Can be used for hypertensive crises.

Mode of application: for controlled hypotension, a 0.1% solution of the drug in isotonic sodium chloride solution is administered intravenously at a rate of 70-100 drops per minute until the required hypotensive effect is achieved. Then the drip rate is reduced to 30-40 drops per minute.

After cessation of administration, the initial blood pressure is restored within 10-15 minutes. In case of hypertensive crisis, 40-80 mg of the drug (0.04-0.08 g) is administered intravenously slowly in 15-20 ml isotonic solution sodium chloride for 7-10 minutes.

Side effect, Contraindications: see Benzohexonium.

Interaction with other drugs: in case of overdose and severe hypotension, norepinephrine or metazone is administered.

Release form: ampoules of 0.1 g of the drug. The solution is prepared immediately before administration.

Storage conditions: list B.

Pentamin(Pentaminum). Synonym: Azamethonium bromide (Azamethonii bromidum).

pharmachologic effect: see Benzohexonium.

Indications: used for hypertensive crises, spasms of peripheral vessels, spastic conditions of the intestines and biliary tract, renal colic, pulmonary edema and cerebral edema. In anesthesiology it is used for controlled hypotension.

Mode of application: for spastic conditions, 1 ml of a 5% solution is administered intramuscularly, then the dose can be increased to 1.5-2 ml 23 times a day. For hypertensive crisis, cerebral edema, pulmonary edema - 0.2-0.5 ml of a 5% solution intravenously. For controlled hypotension, 0.8-1.2 ml of a 5% solution is prescribed slowly intravenously, if necessary - up to 2.4-3.6 ml of the same solution.

Side effect, Contraindications: see Benzohexonium.

Interaction with other drugs: severe hypotension that occurs with an overdose of pentamine can be eliminated by the administration of norepinephrine or mesatone.

Release form: 5% solution in ampoules of 1 and 2 ml.

Storage conditions: List B.

Dentist's Guide to medicines
Edited by Honored Scientist of the Russian Federation, Academician of the Russian Academy of Medical Sciences, Professor Yu. D. Ignatov

In addition to the central nervous system, the human body also has one that controls the functioning of many internal organs. Relatively recently, scientists have derived new group chemicals called ganglion blockers. Drugs from this group can control the functioning of the autonomic nervous system and improve the patient’s condition in many diseases.

Basic information

Thanks to numerous nerve endings the autonomic system controls the activity of almost all internal organs (lungs, heart, intestines, etc.). The functioning of the autonomic nervous system itself is regulated by the brain. Broadcast nerve impulses carried out thanks to special chemicals. In some clinical cases It may be necessary to block the transmission of nerve impulses, that is, to stop the production of these substances. Ganglioblockers can solve this problem.

Drugs can be short-, medium- and long-acting. Such drugs are used in anesthesiology, for therapy complex cases toxicosis of pregnant women, hypertension. However, the action of ganglion blockers is not always effective and may be accompanied by side effects. Therefore, it is strictly forbidden to use such medications without consulting a doctor. Most drugs are not available in pharmacies without a prescription.

"Gigronium"

The drug is available in powder form for the preparation of a solution. The medication is administered by injection intravenously or intramuscularly. You can’t just buy Gigroniy at a pharmacy. The prescription must be written by the attending physician. Thanks to its ganglion-blocking effect medicine used in anesthesiology when it is necessary to control the patient's blood pressure. In addition, the drug is used in obstetric practice. With its help it is possible to stop attacks of eclampsia.

"Gigronium" has a number of contraindications. These may include thrombosis, hypotension, acute stage myocardial infarction, renal or liver failure. In old age (after 65 years), the medication is used with caution. Some patients may develop hypersensitivity.

The ganglion-blocking effect is observed within 5 minutes after intravenous administration of the drug and persists for 15-20 minutes. This is sufficient for short-term blood pressure control (with simple surgical interventions).

"Azamethonium bromide"

The drug is a potent ganglion blocker. Active ingredient selectively blocks vegetative nerve receptors. Azamethonium bromide is widely used for hypertensive crises, bronchial asthma, pulmonary and cerebral edema. With the help of the drug, it is possible to control blood pressure in anesthesiology and normalize the condition of pregnant patients suffering from eclampsia.

The medication is used in the form of injections (intramuscular or intravenous). Exact dosage determined by the doctor in accordance with the patient’s disease, individual characteristics body. In this case, contraindications must be taken into account. These include the following conditions: angle-closure glaucoma, central nervous system, kidney and liver disorders, acute period myocardial infarction. The medicine is used with caution in elderly people, as well as in patients suffering from bronchial asthma and thrombophlebitis.

"Gangleron"

By blocking vegetative impulses, the drug has an anesthetic and antispasmodic effect. For gastric ulcers and duodenum The drug "Gangleron" is widely used. The instructions indicate that the drug can also be prescribed for angina pectoris and impaired mobility of the gastrointestinal tract. The medicine is administered intramuscularly or subcutaneously. The dosage is determined by the doctor.

The medication has its contraindications, like other ganglion blockers. Drugs of this type are not used for arterial hypotension, if there is degenerative changes in the central nervous system. IN in rare cases Hypersensitivity to the active ingredient may develop. Under no circumstances should the medicine be administered intravenously. This can lead to a sharp decrease in blood pressure.

"Benzohexonium"

The remedy is considered one of the most popular in the treatment arterial hypertension. Allows you to quickly stop a hypertensive crisis "Benzohexonium". Instructions for use indicate that the drug can also be prescribed for chronic gastritis, some forms of bronchial asthma, gastric and duodenal ulcers. Benzohexonium tablets are used to treat mild pathologies. The instructions for use indicate that the drug is also available in the form of an injection solution.

The medicine is used to lower blood pressure in surgical practice (anesthetic effect). In this case, the drug is used in the form of a solution and is administered intravenously. For the treatment of stomach diseases, a solution for intramuscular administration can be used.

Taking the wrong medication can lead to side effects (weakness, dizziness, dry mouth). Deterioration in health is associated with sharp decline blood pressure. It is recommended to use the drug in a hospital setting, where the patient can receive timely assistance in case of collapse.

"Pentamine"

The medicine has a pronounced hypotensive effect. The drug Pentamin is widely used for hypertensive crises. The instructions indicate that it is produced in the form of a solution for intramuscular or intravenous injections. The active ingredient is azomethonium bromide.

The medication is used in a hospital setting and can be prescribed for the following pathological processes: cerebral edema, pulmonary edema, sharp increase blood pressure, acute attacks of bronchial asthma, intestinal spasms, renal colic. To create controlled hypotension, Pentamin can also be used in anesthesiology. The instructions indicate that the medicine is available only by prescription.

The drug has the same contraindications as other ganglion blockers. These are myocardial infarction, hypotension, thrombophlebitis, and angle-closure glaucoma.

"Imekhin"

The medicine produces pronounced hypotensive effect, like other ganglion blockers. Drugs from this group are widely used in surgical practice, as well as to relieve hypertensive crises. However, remove high blood pressure This medicine will not work at home. The medication is used exclusively under the supervision of a physician. The drug "Imekhin" is also used to treat cerebral and pulmonary edema and relieve acute attacks of bronchial asthma.

The drug has many side effects. One of them is which is characterized by a sharp decrease in blood pressure when changing body position (from vertical to horizontal). In addition, during therapy the patient may complain of dry mouth, general weakness, frequent dizziness.

"Temekhin"

This ganglion blocking agent is available in tablet form. The medicine is prescribed for Raynaud's syndrome, gastric and duodenal ulcers, and arterial hypertension. The active ingredient produces a pronounced analgesic effect. It is recommended to take the tablets after meals. The dosage and duration of therapy are determined by the doctor.

Contraindications include the acute period of myocardial infarction, hypotension, liver and kidney damage, and angle-closure glaucoma. The medication is not suitable for self-medication. You can purchase tablets only with a doctor's prescription.

Bottom line

Ganglion blocking agents are indispensable in many areas of medicine. However, the use of drugs from this group should be strictly controlled by a specialist. Overdose can lead to serious side effects, up to fatal outcome. Therefore, ganglion blockers are used in hospitalization or emergency care. medical care. You cannot use such drugs on your own, even after carefully studying the instructions.

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There are 2 main groups of substances that block H-cholinergic receptors: ganglion blockers and muscle relaxants.

Ganglioblockers - This medicinal substances, interrupting the transmission of excitation in the autonomic ganglia. They do not affect the synthesis and release of acetylcholine.

Mechanism of action ganglion blockers consist in blocking H-cholinergic receptors in a competitive manner, as a result of which these receptors of the postsynaptic membranes are shielded from acetylcholine, and the conformation of the receptors does not occur. As a result, the activity of the SH group of the transport ATPase decreases, and ultimately the development of an action potential does not occur.

By chemical structure allocate:

1. Quaternary ganglion blockers: the nitrogen atom of these substances has 4 chemical bonds through carbon. Due to this structure, they are poorly absorbed from the gastrointestinal tract (they are effective only when parenteral administration) and do not penetrate the BBB. Drugs in this group include benzohexonium, pentamine, dimecoline, hygronium, camphonium, and arfonade.

2. Non-quaternary (pyrylene, pachycarpine hydroiodide, ganglerone, temechin): the nitrogen atom has 2 or 3 chemical bonds through carbon. Drugs of this group are well absorbed and pass well through the BBB. They can be used both orally and parenterally.

Based on the duration of action, ganglion blockers are divided into drugs:

1. Short-acting: hygronium, arfonade - act for 20-30 minutes;

2. Medium duration actions: benzohexonium, pentamine, dimecoline - duration of action is 2-4 hours;

3. Long-lasting: pachycarpine hydroiodide, pyrylene are effective for 6-12 hours.

Ganglion blockers do not act directly on executive bodies, they only cause autonomic denervation. At the same time, the sensitivity of peripheral receptors to acetylcholine and norepinephrine increases.

The main effects of ganglion blockers:

1. Dilation of arterioles, venules, small veins, which leads to a decrease in blood pressure. The blood, under its own weight, is redistributed into the vessels of the mesentery and the lower half of the body, and the filling of the pulmonary circulation and the pressure in it decreases. Blood flow in the kidneys and urine filtration are also reduced. As a result of a decrease in central venous pressure and the return of blood to the heart, cardiac outflow is reduced by 15-20%. This reduces the load on the left ventricle. Ganglion blockers do not have a direct effect on the heart, although they cause a decrease in cardiovascular reflexes, including pathological ones during trauma, shock, and myocardial infarction. Blockade of H-cholinergic receptors medulla adrenal glands leads to inhibition of the release of norepinephrine, which helps lower blood pressure and reduce vascular reflexes to various influences.

2. Blockade of H-cholinergic receptors of the carotid glomeruli reduces reflex stimulation of the respiratory and vasomotor centers.

3. Blockade of the parasympathetic ganglia leads to weakened motility and secretion of the gastrointestinal tract. Therefore, ganglion blockers have been used in the past for peptic ulcers. For the same reason, long-term use of ganglion blockers for hypertension may lead to constipation.

4. Blockade of the parasympathetic ganglia also leads to pupil dilation and weakening of the secretion of the salivary and lacrimal glands.

5. Some ganglion blockers (Pachycarpin) stimulate labor and are used during obstetrics.

Mechanism of blood pressure reduction from ganglion blockers:

1. block of H-receptors of sympathetic ganglia

2. block of H-receptors of the adrenal cortex => adrenalin

3. block of H-receptors of the pituitary gland => vasopressin

4. H-receptor block skeletal muscles=> vascular tension

5. block of H-receptors of the carotid sinus => tone SDC

Main indications: hypertensive crises, usually severe or complicated, spasms of peripheral vessels (endarteritis, Raynaud's disease), artificial hypotension during surgical interventions, peptic ulcer (oral intake as reserve drugs), with weakness of labor, with acute edema of the lungs and brain.

Complications: orthostatic collapse, intestinal atony, constipation, urinary retention, dry mouth, blurred vision, dizziness.

Contraindicated ganglion blockers for hypotension of various origins, cerebral hemorrhages, liver and kidney dysfunction.

Ganglion blockers are derivatives of either quaternary nitrogen - hexamethonium bromide (benzohexonium) , Azamethonium bromide (pentamine), Trepirium iodide (hygronium), or tertiary - pachycarpine hydroiodide. pempidine(pyrylene). All quaternary amines are poorly absorbed in the gastrointestinal tract and do not pass into the central nervous system, while tertiary amines - are easily resorbed in the intestine and penetrate the blood-brain barrier.

The mechanism of their action is associated with the blockade of H-cholinergic receptors of the ganglia and the adrenal medulla (evolutionarily - the ganglion). The conduction of impulses to the organs through the sympathetic and parasympathetic nerves(pharmacological denervation of organs), the sympathetic and parasympathetic influence on organs and tissues decreases. The tone of blood vessels (arterioles and venules) is mainly determined by the sympathetic nervous system and endogenous adrenaline produced by chromaffin cells of the adrenal gland. Blockade of the sympathetic ganglia and adrenal medulla reduces the amount of norepinephrine (in synapses) and adrenaline (in the blood), blood vessels dilate (both arterioles and venules) - blood pressure drops. Ganglion blockers dilate peripheral vessels, improve blood supply and microcirculation in the extremities (indicated for spasm of peripheral vessels).

The function of the heart, smooth muscles, gastrointestinal tract, bladder, and glandular secretions are generally maintained parasympathetic system. Blockade of intramural parasympathetic ganglia inhibits the stimulating effect vagus nerve and reduces contractions of the smooth muscles of internal organs (gastrointestinal tract, bladder, bronchi, etc.), that is, it gives a pronounced antispasmodic effect. For the same reason, the secretion of glands (salivary, gastrointestinal tract) decreases, heart contractions become more frequent, and paralysis of accommodation develops.

Indications for use:

1. Hypertensive crises. For this purpose, pentamine and benzohexonium are used.

2. Edema of the lungs and brain due to high blood pressure. Ganglion blockers dilate peripheral vessels (both arterioles and venules), blood is deposited in the periphery, its flow to the “right” heart is reduced and the pulmonary circulation is unloaded, hydrostatic pressure in the vessels of the lungs and brain decreases. The expansion of venules helps to reduce the venous return of blood to the heart, which improves its working conditions.

3. Controlled hypotension. Artificial hypotension is used for exsanguination surgical field during surgical interventions on the heart, cerebral vessels (the risk of cerebral edema is reduced), pelvic organs, dental operations (on tissues with abundant blood supply). Ganglion blockers dilate peripheral vessels, and blood is deposited in the periphery, which leads to a decrease in bleeding in the surgical field. At the same time, ganglionic blockers prevent the development of negative autonomic reactions to organs and blood vessels during surgical interventions. For controlled hypotension, drugs are mainly used short acting(hydronium, imekhin - administered intravenously).

4. Treatment of peripheral vascular spasms (endarteritis, Raynaud's disease).

5. Peptic ulcer stomach and duodenum. Ganglion blockers reduce secretion gastric juice and relax the smooth muscles of the stomach and intestines, creating functional peace of the ulcerated mucosa.

In addition, ganglion blockers are sometimes used as bronchodilators (as one of the components of treatment), apachycarpine, which stimulates contractile activity of the uterus, with weak labor.

Unfortunately, the use of ganglion blockers often leads to severe complications:

1) orthostatic collaptoid state ( sharp drop blood pressure when a person moves from a horizontal to a vertical position). Depositing blood in the vessels of the limbs and organs reduces systemic blood pressure in the vessels of the brain. When the position of the body changes due to gravity, the blood is redistributed - it goes to the underlying areas of the body, the brain bleeds, and the patient loses consciousness. For prophylaxis, it is recommended to stay in a room for 1.5-2 hours after administration of the drug. horizontal position(lie);

2) atony of the intestine (up to obstruction) and bladder. Due to the blockade of the parasympathetic ganglia, expressed antispasmodic effect motor and secretory functions gastrointestinal tract, and constipation develops. Decreased bladder contractility can lead to urinary retention.

In addition, the use of ganglion blockers may be accompanied by photophobia (dilated pupils), visual impairment (accommodative paralysis), dry mouth, and tachycardia.