Cholinolytics anticholinergics. Anticholinergic (anticholinergic) drugs, acting mainly in the field of peripheral M-cholinergic systems. From the history of anticholinergics

- taking anticholinergic drugs (cyclodol, diphenhydramine, atropine, solutan) to achieve a state of euphoria. It is usually episodic or periodic, often observed in polydrug addiction and polytoxicomania. Less common is regular mono use. The drugs cause delirious disorders of consciousness with delusions, visual hallucinations, psychomotor agitation and disorientation in the surrounding reality. Perhaps the development of mental and physical dependence. With prolonged abuse of anticholinergics, the functions of the heart and lungs are disturbed, an organic lesion of the central nervous system develops.

General information

Abuse of anticholinergics - regular, periodic or episodic use of anticholinergics to achieve a state of euphoria. It occurs predominantly among adolescents and young adults. Drugs are usually taken for recreational purposes (in the process of some specific social activity). Abuse of anticholinergics is often combined with other drug addictions and substance abuse. The development of dependence is possible even with irregular intake of anticholinergic drugs.

The first place in prevalence is occupied by the use of cyclodol. This psychoactive substance is often taken in conjunction with other narcotic and toxic drugs: tranquilizers, diphenhydramine, alcohol, barbiturates, hashish. The use of antihistamines and Datura as a separate form of abuse is rare these days. Atropine-containing and antihistamines are usually combined with alcoholic beverages. Diphenhydramine is used as a means to prolong euphoria in opium addiction. Treatment for abuse of anticholinergics is carried out by specialists in the field of narcology.

Cholinolytics

Cholinolytic agents are a large group of synthetic drugs and herbal preparations that have the ability to block acetylcholine receptors. This group includes some medicines for the treatment of parkinsonism (trihexyphenidyl), antihistamines (diphenhydramine, promethazine) and tropane alkaloids (hyoscyamine, scopolamine and atropine), which are found in dope, scopolia, mandrake, henbane, belladonna and other plants.

Cholinolytics "attach" to acetylcholine receptors and do not allow them to interact with acetylcholine. As a result, the functions of the parasympathetic nervous system are largely blocked, and sympathetic effects predominate. Various drugs from the group of anticholinergics act on different types of receptors. When taking atropine-containing drugs, peripheral receptors are blocked, when using antihistamines - central receptors, when taking antiparkinsonian drugs - both central and peripheral receptors.

The abuse of anticholinergics is due to the ability of drugs to cause mental disorders when the therapeutic dose is exceeded. With the simultaneous use of 3-4 therapeutic doses, severe disorders of consciousness are usually absent, there is an increase in mood, fragmentary visual and auditory hallucinations. With a further increase in the dose, a delirious syndrome develops, which includes delirium, extensive visual and auditory hallucinations, disorientation in the surrounding world, and psychomotor agitation. Self-orientation is preserved.

The most common anticholinergic used as a narcotic drug is cyclodol. Less common is the abuse of diphenhydramine, atropine-containing plants (datura, henbane) and taren (aprofen) - a drug used to stimulate labor, eliminate spasms in cholecystitis, spastic colitis, hepatic and renal colic, peptic ulcer and some vascular diseases.

Abuse of Datura, Diphenhydramine and Taren

Datura is a wild plant whose seeds contain scopolamine, atropine and other alkaloids. To achieve euphoria, the seeds are consumed orally. When taking 10-15 seeds, muscle relaxation, a feeling of warmth, dizziness and an uplift in mood occur. Sometimes the intoxication resembles the euphoria of hashishism. There may be dyspeptic symptoms, increased heart rate, noise, a feeling of fullness or squeezing in the head. Intoxication persists for several hours, and then gives way to headache, weakness and fatigue. Unsharply expressed violations of coordination of movements are often noted.

With the use of large doses of dope, the development of delirium-type psychosis is possible. "Goofy" behavior, motor agitation, and body schema disorders are observed, accompanied by facial flushing, fever, tachycardia, BP fluctuations, and pupillary dilation. The duration of psychosis is up to 1 day. In the next few days, anxiety, unmotivated fears, fussiness and sleep disturbances may persist.

Isolated abuse of the anticholinergic diphenhydramine is rare. Usually the drug is taken simultaneously with alcohol to enhance and modify intoxication. Perhaps the combined abuse of an anticholinergic and an opiate drug (most often heroin) - in this case, diphenhydramine is used to prolong narcotic euphoria. With an overdose of the drug, psychoses develop, manifested by hallucinations, delusions, psychomotor agitation and disorders of consciousness.

The illegal use of taren is due to its ability to cause hallucinations. The drug is taken in doses several times higher than therapeutic. When used, a delirious disorder of consciousness occurs in combination with vivid auditory, visual and tactile hallucinations. After leaving the state of intoxication, patients retain fragmentary memories of their own experiences. There is no mental and physical dependence when taking taren, addiction does not occur.

Cyclodol and addiction development

Cyclodol (parkan, parkopan, romaparkin, artan) is an antiparkinsonian drug included in the list of essential medicines. It is used to eliminate the side effects of drugs from the group of neuroleptics. In patients suffering from parkinsonism, cyclodol reduces trembling of the extremities, hypersalivation and sweating. Influences bradykinesia and rigidity. In an antisocial teenage environment, it is seen as an inexpensive means to achieve unusual euphoria.

Patients suffering from cyclodol addiction take cyclodol tablets. To achieve a state of euphoria at the initial stage, 2-4 tablets are usually sufficient, sometimes narcotic effects occur when using a therapeutic dose. At risk of anticholinergic abuse are adolescents with addictive behavior who practice taking various psychoactive substances in order to obtain unusual sensations. Group episodic or occasional use prevails, with most adolescents choosing cyclodol purposefully to obtain hallucinogenic effects.

Less often, the reason for admission in the initial stages is the need to "keep up with others." In some cases, there is a systematic single use. When taken alone, severe addiction develops more often than when consumed in groups. Abuse of the anticholinergic cyclodol is often found in other substance abuse and in polydrug addiction. The drug is taken as a means to eliminate withdrawal symptoms in the absence of the usual drug or is used to enhance the effects of the main narcotic substance.

Adolescents with no experience with other psychoactive substances usually start with 4-6 pills. More "experienced" patients, configured to receive hallucinatory effects, immediately take 8-10 tablets. After the first use, unpleasant sensations are possible: fear, anxiety and nausea. If the abuse of the anticholinergic continues, these sensations disappear after a few doses. Adolescents usually gather in a group and take cyclodol 1-2 times a week. After 1.5-2 months, post-narcotic effects occur, euphoria is replaced by depression and internal tension. This indicates the development of mental dependence.

With the abuse of an anticholinergic, tolerance gradually increases. After some time, hallucinations when taking 8-10 tablets disappear, and patients gradually increase the dose to 20-30 tablets. After 1-1.5 years after the start of use, physical dependence occurs. Withdrawal syndrome develops, accompanied by internal tension, anxiety and a feeling of mental distress. Against the background of a progressive decrease in mood, vegetative and somatic symptoms occur: trembling of the whole body, stiffness of movements, a pronounced increase in muscle tone, muscle twitching. Weakness, irritability and progressive dysphoria, combined with a pathological craving for cyclodol, push patients to further anticholinergic abuse.

Symptoms of dependence on cyclodol

In intoxication with the abuse of the anticholinergic cyclodol, 4 phases are distinguished. The first phase (euphoric) begins half an hour after consumption and is accompanied by an increase in mood, optimism, a tendency to see everything in pink. All negative experiences become insignificant. Patients are mobile, sociable, scattered and inconsistent, they chat with other members of the group, laugh, dance and sing.

After another half an hour, the phase of narrowed consciousness begins. Patients "withdraw into themselves", stop communicating and immerse themselves in their own experiences. Possible derealization, depersonalization, violations of the body scheme (parts of the body seem alien) and the perception of surrounding objects (objects change shape, the relationship between objects is violated). Thinking is slowed down, it is difficult for patients to contact others, follow someone else's thoughts and answer questions, however, if necessary (for example, when contacting parents or policemen), they can concentrate for a short time and return to reality.

After 2-3 hours, the phase of narrowed consciousness either ends or passes into the phase of hallucinations. Patients no longer navigate in time and place. The environment seems to them distorted, unusual. Initially, fragmentary hallucinations appear: individual sounds, calls or clicks, circles or dots before the eyes. After some time, there are developed scene-like hallucinations of fantastic content. Hallucinations can be both positive and terrible, but patients do not feel fear, even when they see scenes of cruelty or severed limbs.

With the abuse of an anticholinergic, the mood of patients changes depending on the content of hallucinations. At the end of intoxication, patients often compare the seen pictures with cartoons. Against the background of the use of cyclodol, negative hallucinations often occur. It seems to patients that some objects (for example, a cigarette in their hand) either appear or disappear. An external examination of patients reveals tachycardia, increased blood pressure, impaired coordination of movements and dilated pupils. The eyes are cloudy, the skin and mucous membranes are dry and pale.

Abuse of an anticholinergic may be accompanied by the development of acute psychotic conditions. In case of an overdose, acute psychosis is possible, accompanied by impaired consciousness. At the initial stage, there are fragmentary visual hallucinations: small animals, objects, insects. Then the hallucinations become extended, scene-like, threatening. Delusional disorders join. Delirious disturbances of consciousness are supplemented by psychomotor agitation.

Already at the initial stages of abuse of the anticholinergic, the activity of the central nervous system is disrupted. With regular intake of cyclodol for six months or more, patients are found to have a slowdown in thinking, deterioration in cognitive functions, difficulty in trying to concentrate and memory impairment. Characteristic vegetative and neurological disorders are observed: muscle tone is increased, twitching of individual muscles and trembling of the fingers are noted. The face becomes pale, against the background of general pallor, a "pattern" in the form of a butterfly is clearly visible on the cheeks.

With the abuse of an anticholinergic for 1-1.5 years or more, an abstinence syndrome develops. The first manifestations of abstinence become noticeable a day after the last intake of cyclodol. Patients feel dissatisfaction and inner tension. A feeling of general unhappiness grows, the level of anxiety increases. Against the background of a progressive deterioration in mood, weakness and apathy occur. Employability is declining. Muscle tone increases, movements become constrained, the face acquires a mask-like appearance, trembling of the torso and limbs is noted. Patients suffering from anticholinergic abuse complain of back pain. Withdrawal symptoms persist for 1-2 weeks, and then are replaced by severe asthenia.

Treatment and prognosis for cyclodol addiction

The prognosis for abuse of an anticholinergic depends on the level of motivation of the patient, the severity and duration of the disease. With proper complex treatment in the initial stages of the disease, many patients manage to finally get rid of addiction. Prognostically unfavorable are cases of constant prolonged abuse, accompanied by an organic lesion of the central nervous system, thinking disorders and a decrease in criticism of one's condition. In severe cases, the outcome may be organic dementia, disorders of the respiratory and cardiovascular systems.

Cholinolytics are substances that have the ability to block or weaken the effects of acetylcholine, which is responsible for the appearance of an excited state of the nervous system. Anticholinergic compounds are able to act on various structures of the body, and therefore they are conditionally divided into atropine-like substances, central, curare-like, ganglion-blocking.

Description

In clinical practice, these compounds are of great importance due to their ability to influence the reflex regulation of body structures.

The most common anticholinergics are alkaloids, which include platifillin, scopolamine, atropine and preparations based on belladonna, dope, henbane (can be used in combination and independently). They are of natural origin.

Currently, synthetic substances are also widely used. They contain compounds that can significantly enhance the effect of anticholinergics.

Preparations based on these substances are easy to use in practice, and the number of negative reactions provoked by them is significantly reduced. Most anticholinergics can also have antispasmodic and analgesic effects. The group of such medicines has features that are also inherent in some anticholinergics of local anesthetic and antihistamine action. These include diphenhydramine, diprazine.

Below is a list of anticholinergic drugs.

All anticholinergics in their chemical structure are very diverse. In addition, taking into account the ability to block different types of effects of acetylcholine, it is customary to subdivide them into M-anticholinergics and N-anticholinergics.

M-cholinolytics

M-cholinolytics are:

  1. Alkaloids, including scopolamine, platifillin, atropine.
  2. Cholinolytics of plant origin. These include: ragwort, dope, henbane, belladonna.
  3. Anticholinergics of semi-synthetic origin, for example, homatropin.
  4. Cholinolytics of synthetic origin. Among them: chlorosil, spasmolytin, propantelin, metacin, pirenzepine, ipratropium bromide, aprofen, arpenal.

The action of M-cholinolytics

M-cholinolytics, blocking M-cholinergic receptors, prevent the interaction of the acetylcholine mediator with them. Reduce or eliminate the effects of irritation of cholinergic (parasympathetic) nerves and the action of substances with M-cholinomimetic activity.

M-anticholinergic preparations are used in the following situations:

  1. Acute poisoning with cholinomimetic, anticholinesterase poison.
  2. Parkinsonism, other pathologies of the central nervous system.
  3. Eye injury, iridocyclitis, iritis. In this case, m-cholinolytics are used to relax the eye muscles.
  4. Spasms of organs with smooth muscle layers (pylorospasm, hepatic, renal colic).
  5. Ulcerative lesions of the duodenum, stomach.
  6. Vagotonic bradycardia.
  7. Violation of intra-atrial, atrioventricular conduction.
  8. Preoperative premedication (to prevent laryngospasm, bronchospasm, hypersalivation).
  9. Bronchospasm.

In addition, M-cholinolytics are used in diagnostic studies, for example, to dilate the pupil during the examination of the fundus, during X-ray examination of the gastrointestinal tract.

Contraindications

The main contraindications that prevent the use of anticholinergic drugs are:

  1. Hypertrophic changes in the prostate gland, atonic conditions of the bladder.
  2. Atonic constipation.
  3. Asthmatic status.
  4. Glaucoma in any form.

Central anticholinergics, which include scopolamine, spasmolytin, aprofen, arpenal, are contraindicated for use by persons whose activities require concentration of attention and speed of reactions and are associated with the management of complex mechanisms and vehicles.

N-cholinolytics

All N-cholinolytics are drugs that are conventionally divided into two main groups: ganglioblocking and curare-like.

Ganglioblocking anticholinergics are able to block n-cholinergic receptors located in the ganglia. These include: fubromegan, temekhin, pyrilene, pentamin, pahikarpin, kvateron, camphonium, imekhin, dimecolin, gigronium, benzohexonium.

Ganglion blocking anticholinergics are used, as a rule, as antihypertensive and vasodilators in the following cases:

  1. Spasms of peripheral vessels (obliterating endarteritis, Raynaud's disease).
  2. In order to relieve crises of a hypertensive nature.
  3. To control hypotensive conditions.
  4. For the purpose of therapy of ulcerative lesions of the duodenum, stomach.
  5. For the purpose of symptomatic treatment of arterial hypertension.

Negative reactions

Against the background of the use of ganglioblocking anticholinergics, some negative reactions may develop, and therefore their use is limited. With the use of ganglioblockers, the following may develop:

  1. orthostatic hypotension.
  2. Decreased venous pressure.
  3. Accommodation disorder.
  4. Dryness in the mouth.
  5. Pupil dilation.

Among the main contraindications that prevent the use of ganglioblockers, the following should be noted:

  1. Thrombosis.
  2. Renal, hepatic lesions.
  3. Acute myocardial infarction.
  4. Arterial hypotension.
  5. Glaucoma in closed-angle form.

Curare-like anticholinergics

Curare-like anticholinergics are able to block H-cholinergic receptors, which are located in the neuromuscular synapses of the skeletal muscles. These include: tubocurarine chloride, mellitin, dithylin, dioxonium.

Curare-like anticholinergics are used, mainly in the field of anesthesiology to relax skeletal muscles:

  1. With reposition of bone fragments, reduction of dislocations.
  2. during endoscopic procedures.
  3. During surgical interventions.

In addition, they are often used as an element of the complex treatment of tetanus. Melliktin-based preparations are often used to reduce muscle tone in neurological pathologies, accompanied by a disorder of motor function, an increase in skeletal muscle tone.

Against the background of the use of curare-like anticholinergics, the following negative symptoms may develop:

  1. Depolarizing curare-like anticholinergics are capable of provoking skeletal muscle soreness.
  2. Ditilin preparations can increase intraocular pressure and increase blood pressure, which in turn provokes cardiac arrhythmias.
  3. Under the influence of tubocurarine chloride preparations, a decrease in the level of blood pressure, the development of laryngospasm, bronchospasm can be observed.

In what cases should they not be used?

The main contraindications to the use of curare-like substances are the following pathologies and physiological conditions:

  1. Breast age.
  2. Glaucoma.
  3. Violations of the hepatic, renal functionality.
  4. Myasthenia.

It is important to exercise caution when prescribing curare-like anticholinergics to patients suffering from cachexia, anemia, as well as those who are pregnant or elderly.

Why are anticholinergics prescribed?

Currently, this list of anticholinergics (drugs of all groups) is widely used in various medical fields. The classification of their use is as follows:

  1. Application in therapeutic practice, when there is a need to treat pathologies accompanied by spasms in smooth muscle structures. The most relevant drugs in this area are those that combine myotropic and neurotropic effects, as well as those that have a selective antispasmodic effect.
  2. Use for the treatment of ulcerative lesions of the duodenum, stomach. In this area, it would be advisable to use anticholinergics with antispasmodic activity that can inhibit the production of gastric juice.
  3. Use in functional disorders of the nervous system. Cholinolytics are widely used for the treatment of parkinsonian conditions, Parkinson's disease.
  4. Use in psychiatric practice as tranquilizers.
  5. Application in the field of anesthesiology. Cholinolytic substances can enhance the effectiveness of sleeping pills and narcotic drugs.
  6. Use as a prophylactic to prevent sea and air sickness.
  7. Use as an antidote if the body is intoxicated with poisons.

Overdose of anticholinergics

With prolonged use, the degree of exposure to anticholinergics may decrease. Due to this feature of substances, experts recommend periodic replacement of drugs.

In some cases, against the background of the use of drugs, a side effect of a toxic nature may develop. This happens, most often, if the patient has an individual sensitivity to the substance, or exceeds the recommended dosage. Intoxication with anticholinergics is manifested by the following symptoms:

  1. Wrong accommodation.
  2. Dryness of the mucous membranes in the oral region.
  3. Tachycardia.

When using central anticholinergics, an overdose is accompanied by the occurrence of violations of the functionality of the National Assembly:

  1. hallucinations.
  2. Headache feeling.
  3. Dizziness.
  4. Pain in the head.

When treating with anticholinergics, it is important for the patient to follow the dosages recommended by the specialist and take into account the individual characteristics of his own body. Even a slight overdose of substances leads to the development of tachycardia and severe dry mouth. At the onset of intoxication, prozerin should be administered intravenously to the patient. The most serious contraindication to their use is glaucoma.

Substances in this group include:

Blocking M-cholinergic receptors (M-cholinergic blockers),

N-cholinergic receptors of autonomic ganglia (ganglioblockers) - blocking N-cholinergic receptors of skeletal muscles (curare-like drugs)

1. M-anticholinergics (m-anticholinergics). General characteristics, mechanism of action, main pharmacological effects.

M 1 - receptors are located: in the neurons of the central nervous system; sympathetic postganglionic cell bodies; in many presynaptic regions.

M 2 – receptors are located in the heart: SA node; atrial AV node; ventricles.

M 3 - receptors are located: in smooth muscles; in most exocrine glands, vascular endothelium (extrasynaptic, lie freely).

M-anticholinergics (M-cholinolytics or muscarinic antagonists) block M-cholinergic receptors localized on the cell membrane of effector organs, and thus prevent their interaction with acetylcholine.

Since M-cholinergic receptors are located in organs and tissues that receive parasympathetic innervation, its influence is eliminated and effects are caused that are opposite to the effects of excitation of the parasympathetic nervous system:

1) dilate the pupils of the eyes;

2) cause accommodation paralysis;

3) increase heart rate;

4) facilitate atrioventricular conduction;

5) reduce the tone of smooth muscles of the bronchi, gastrointestinal tract, bladder;

6) reduce the secretion of salivary, bronchial, digestive, sweat glands.

All M-cholinergic blockers are contraindicated in glaucoma!

The most well-known drug in this group is atropine, so the whole group is often called the atropine group, or atropine-like drugs.

1.1.Classification:

1.1.1. Natural alkaloids:atropine and hyoscine hydrobromide (scopolamine)

Atropine sulfate– racemic mixture of d, l-hyoscyamine.

L-hyoscyamine is an alkaloid of a number of plants of the nightshade family: belladonna (Atropa belladonnae), dope (Datura stramonium), henbane (Hyosciamus niger). It is impossible to isolate l-hyoscyamine in its pure form, because it undergoes spontaneous racemization to d-hyoscyamine.

Pharmacological activity possesses only l-hyoscyamine, which blocks M-cholinergic receptors 100 times stronger than d-hyoscyamine. At the molecular level, the formation of inositol triphosphate (IP3) vM is prevented 1 - , M 3 -effector cells or lowers cAMP in M 2 cardiac effectors.

Atropine has a high selectivity for muscarinic receptors: it blocks all types of M-cholinergic receptors (M 1 -M 5 ). The sensitivity of the receptors is not the same hence the doses will be different. The power of influence on nicotinic receptors is much less: in clinical use, its effect on non-scarinic receptors is usually not detected.

The effectiveness of antimuscarinic drugs varies depending on the localization of the organ:

    most sensitive- salivary, bronchial and sweat glands;

    average sensitivity – autonomous effectors of smooth muscles and heart;

    least sensitive - secretory parietal cells of the stomach (secretion of HCl).

In most tissues, antimuscarinic substances are more active in blocking the effects of exogenously administered cholinergic agonists than endogenous acetylcholine.

Blockade of muscarinic receptors is reversible and competitive: removed by increasing the concentration of ACH or muscarinic agonists (in case of poisoning, you have to increase the dose for competition and blockade in small doses can be removed by high concentrations of acetylcholine or equivalent muscarinic agonists.

Pharmacokinetics: Atropine is well absorbed by almost any route of administration. When instilled into the eyes, it penetrates well through the cornea of ​​the eye into the fluid of the anterior chamber, as well as through the blood-brain barrier into the central nervous system. Approximately 50% of atropine is metabolized, the rest is excreted unchanged in the urine. The elimination half-life is 3-4 hours.

Pharmacological effects of atropine:

1. Effect on the eye. When applied topically, the following effects develop:

        midriaz(Greek amydros - dark, obscure) - pupil dilation, because M-cholinergic receptors are blocked m. sphincter pupillae and the muscle stops responding to parasympathetic impulses. Against this background, the influence of sympathetic nerves on m. dilatator pupillae. The contraction of this muscle causes the pupil to dilate. Blockade m. sphincter pupillae is so pronounced that the pupil stops responding to light (the pupillary reflex disappears), photophobia occurs.

        Paralysis accommodation. Under the influence of atropine, the receptors of the ciliary body are blocked, and it ceases to respond to impulses from the parasympathetic nerves. Since M-cholinergic receptors are blocked, there is no activation of phospholipase C and the synthesis of IP 3 and DAG in the cell is suspended. The lack of these messengers leads to a decrease in the level of Ca 2+ ions in the cytoplasm and muscle contraction does not develop. The ciliary muscles relax (cycloplegia), while it flattens and stretches the ligament of Zinn. Zinn ligament fibers stretch the lens capsule and make it less convex. The eye is set to the far vision point. Arises micropsia (objects appear smaller) and blurred vision.

        In people with a shallow anterior chamber or latent glaucoma there is an increase in intraocular pressure, since with the expansion of the pupil, the iris thickens, and the angle of the anterior chamber closes. As a result, the lymphatic fissures of the fountain spaces are compressed and the outflow of intraocular fluid decreases.

The effect on the eye after a single instillation lasts for 7-12 days.

2. Respiratory organs. The secretory cells of the bronchial glands receive vagal parasympathetic innervation. Under the influence of atropine, the blockade of M-cholinergic receptors of the bronchial glands occurs, their secretion decreases. At the same time, the secretion of the laryngeal and tracheal glands decreases. This can lead to a hoarse voice and a scratchy throat.

Muscarinic receptors are located in the smooth muscle cells of the large bronchi. Under the influence of atropine, the receptors are blocked, and the contraction of the smooth muscle cell does not develop - the bronchodilating effect of atropine is manifested. In healthy people, the bronchodilatory effect of atropine is weakly expressed, however, in diseases of the respiratory tract and in the elderly, the ability of atropine to expand the bronchi increases dramatically.

A significant disadvantage of atropine is that under its influence the motor activity of the ciliary epithelium of the bronchi decreases. Against the background of a decrease in the secretion of glands, this leads to the fact that mucociliary clearance drops sharply - the ability of the cells of the respiratory tract to remove pollutants (dust particles) coming with the air flow.

3. Digestive organs. Blockade of M-cholinergic receptors in the cells of exocrine digestive glands leads to a decrease in their secretion. The antisecretory effect of atropine is more pronounced in the upper gastrointestinal tract. The secretion of the salivary glands decreases, patients often report dry mouth. Gastric secretion is inhibited only when using significantly higher doses of atropine.

It is believed that atropine: a) blocks the effect of postganglionic fibers of the vagus nerve not only directly on the secretory cells of the stomach, but also on the endocrine G- and H-cells of the mucosa (which secrete, respectively, gastrin and histamine - hormones that stimulate gastric secretion). The blockade is carried out by shielding the active centers of M 3 cholinergic receptors on all these cells.

The mediator acetylcholine is no longer able to activate the endocrine and parietal cells of the stomach. Pirenzepine - blocks the presynaptic M 1 -cholinergic receptors of the vagus nerve fibers and disrupts the release of acetylcholine, which is necessary to stimulate secretion.

b) blockade of only basal (on an empty stomach) secretion of gastric juice. Stimulated juice secretion (i.e., secretion in response to food) does not decrease. Pancreatic and intestinal secretions are practically insensitive to the action of atropine. This is due to the fact that a significant part of the control of the secretion of intestinal juice falls on the system of non-cholinergic neurons of the metasympathetic nervous system (serotonin and opioid neurons) and the humoral system of the intestine.

c) blockade of M-cholinergic receptors of smooth muscles of the gastrointestinal tract and their relaxation. Gastrointestinal motility is reduced. There is an effect on the motility of all parts of the gastrointestinal tract, as well as on the smooth muscles of the biliary tract. When taken regularly, the effect does not last more than 1-3 days. This is due to the fact that non-cholinergic neurons of the metasympathetic system compensate for the shutdown of vagal influences on the intestine.

4. Genitourinary system: blockade of M-cholinergic receptors of the smooth muscles of the urethra and bladder, which causes their relaxation and slows down the emptying of the bladder. In late pregnancy, M-cholinergic receptors are blocked in the region of the smooth muscles of the cervix, which contributes to their relaxation.

31. M-cholinolytics

The drugs of this group block the transmission of excitation in m-cholinergic receptors, making them insensitive to the mediator acetylcholine, resulting in effects opposite to the action of parasympathetic innervation and m-cholinomimetics.

M-anticholinergics (drugs of the atropine group) suppress the secretion of the salivary, sweat, bronchial, gastric and intestinal glands. The secretion of gastric juice decreases, but the production of hydrochloric acid, the secretion of bile and pancreatic enzymes decrease slightly. They dilate the bronchi, reduce the tone and peristalsis of the intestines, relax the bile ducts, reduce the tone and cause relaxation of the ureters, especially with their spasm. Under the action of m-cholinergic blockers on the cardiovascular system, tachycardia, increased heart rate, increased cardiac output, improved conduction and automatism, and a slight increase in blood pressure occur. When introduced into the cavity, the conjunctiva causes pupil dilation (mydriasis), an increase in intraocular pressure, accommodation paralysis and dryness of the cornea. According to the chemical structure, m-cholinergic blockers are divided into tertiary and quaternary ammonium compounds. Quaternary amines (matacin, chlorosyl, propanteline bromide, furbromegane, ipratropium bromide, troventol) penetrate poorly through the blood-brain barrier and show only a peripheral anticholinergic effect.

Atropine sulfate (Atropini sulfas).

It has m-anticholinergic activity. Blocks m-cholinergic systems of the body.

Application: peptic ulcer of the stomach and duodenum, vasospasm of internal organs, bronchial asthma, in ophthalmology - to dilate the pupil.

Method of application: administered orally at 0.00025-0.001 g 2-3 times a day, s / c at 0.25-1 ml of a 0.1% solution, in ophthalmology - 1-2 drops of a 1% solution. V. R. D. - 0.001, V. S. D. - 0.003.

Side effects: dry mouth, tachycardia, blurred vision, intestinal atony, difficulty urinating.

Contraindications: glaucoma.

Release form: ampoules of 1 ml of 0.1% solution No. 10, eye drops (1% solution) of 5 ml, powder. List A.

Metacin (Methacinum).

Synthetic m-anticholinergic, superior in activity to atropine.

Use, side effects, contraindications: the same as for atropine.

Method of application: administered orally at 0.002-0.004 g 2-3 times a day, parenterally at 0.5-2 ml of a 0.1% solution.

Release form: tablets of 0.002 No. 10, ampoules of 1 ml of a 0.1% solution No. 10. Combined preparations containing m-cholinolytics: bellataminal, bellaspon, belloid, besalol, bellalgin. Assign 1 tablet 2-3 times a day for intestinal spasms, increased acidity of gastric juice and others; suppositories (betiol and anuzol) are used for hemorrhoids and rectal fissures.

From the book Pharmacology: lecture notes author

6. N-cholinolytics A group of drugs that selectively block n-cholinergic receptors of the autonomic ganglia, the carotid sinus zone and the adrenal medulla is called ganglioblockers, and a group that blocks n-cholinergic receptors of neuromuscular synapses is called

From the book Pharmacology author Valeria Nikolaevna Malevannaya

31. M-cholinolytics The drugs of this group block the transmission of excitation in m-cholinergic receptors, making them insensitive to the mediator acetylcholine, resulting in effects that are opposite to the action of parasympathetic innervation and

From the author's book

32. N-cholinolytics A group of drugs that selectively block n-cholinergic receptors of autonomic ganglia, the carotid sinus zone and the adrenal medulla is called ganglioblockers, and a group that blocks n-cholinergic receptors of neuromuscular synapses is called

Anticholinergic (anticholinergic) drugs

See also bellazone, hyoscyamine, hyoscine, ipratropium bromide, dinezin, meclozine, norakine, oxitropium bromide, pirenzepin, tropacin, cyclodol, etpenal.

According to the modern classification, anticholinergic drugs are divided into atropine group alkaloids (atropine sulfate, henbane leaves, homatropine hydrobromide, dope leaves, belladonna preparations, scopolamine, platifillin hydrotartrate) and synthetic anticholinergics (aprofen, arpenal, ipratropium bromide, metacin, prifinium bromide, propanteline bromide , spasmolitin, troventol).

APROFEN (Apropheniun)

Pharmachologic effect. It has a pronounced peripheral and central anticholinergic effect.

Indications for use. Endarteritis (inflammation of the inner lining of the artery), angiospasms (vasospasms), weakness of labor, spastic dyskinesia (impaired mobility) of the gastrointestinal tract, peptic ulcer of the stomach and duodenum, spastic colitis (inflammation of the large intestine, characterized by its sharp contractions), cholecystitis (inflammation of the gallbladder).

Method of application and dose. Inside after eating 0.025 g 2-4 times a day; subcutaneously or intramuscularly - 0.5-1 ml of a 1% solution. Higher doses for adults: inside single - 0.03 g, daily - 0.1 g; under the skin and intramuscularly: single - 0.02 g, daily - 0.06 g.

Side effect. Dry mouth, disturbances of accommodation (impaired visual perception), dizziness, feeling of intoxication, weakness, drowsiness.

Contraindications. Glaucoma (increased intraocular pressure).

Release form. Tablets of 0.025 g in a package of 10 pieces; ampoules of 1 ml of 1% solution in a package of 10 pieces.

Storage conditions.

ARPENAL (Arpenalum)

Pharmachologic effect. It has a blocking effect on H- and M-cholinergic structures.

Indications for use. Peptic ulcer of the stomach and duodenum, pylorospasm (spasm of the muscles of the pylorus of the stomach), cholelithiasis, renal and hepatic colic, bronchial asthma, parkinsonism, etc.

Method of application and dose. Inside, 0.05-0.1 g 2-4 times a day. The course of treatment is 3-4 weeks.

Side effect. Dizziness, headache, feeling of intoxication, dry mouth, disturbance of accommodation (impaired visual perception).

Contraindications. Glaucoma (increased intraocular pressure).

Release form. Tablets of 0.05 g in a package of 50 pieces.

Storage conditions.

Atropine sulfate (Atropini sulfas)

Synonyms: Atropine sulfate, Atromed.

Pharmachologic effect. The main pharmacological feature of atropine sulfate is its ability to block M-cholinergic receptors; it also acts (although much weaker) on H-cholinergic receptors. Thus, atropine sulfate refers to non-selective blockers of M-cholinergic receptors.

The introduction of atropine into the body is accompanied by a decrease in the secretion of the salivary, gastric, bronchial, sweat glands, pancreas, an increase in heart rate (due to a decrease in the inhibitory effect on the heart of the vagus nerve), a decrease in the tone of smooth muscle organs (bronchi, abdominal organs, etc.). The action of atropine is more pronounced with increased tone of the vagus nerve.

Under the influence of atropine, a strong dilation of the pupils occurs. The mydriatic effect (dilation of the pupils) depends on the relaxation of the fibers of the circular muscle of the iris, which is innervated by parasympathetic fibers. Simultaneously with the expansion of the pupil due to a violation of the outflow of fluid from the chambers, an increase in intraocular pressure is possible.

Relaxation of the ciliary muscle of the ciliary body of the eye leads to paralysis of accommodation (impaired visual perception).

Indications for use. Atropine is used for peptic ulcer of the stomach and duodenum, pylorospasm (spasm of the muscles of the pylorus of the stomach), cholelithiasis, with spasms of the intestines and urinary tract, bronchial asthma, to reduce the secretion of the salivary, gastric and bronchial glands, with bradycardia (rare pulse), which developed in as a result of increased vagal tone.

For pain associated with spasms of smooth muscles, atropine is often administered together with analgesics (painkillers) (analgin, promedol, morphine, etc., 256, 255).

In anesthesia practice, atropine is used before anesthesia and surgery and during surgery to prevent broncho- and laryngospasm (sharp narrowing of the lumen of the bronchi and larynx), limit the secretion of the salivary and bronchial glands and reduce other reflex reactions and side effects associated with excitation of the vagus nerve.

Atropine is also used in X-ray examination of the gastrointestinal tract, if necessary, to reduce the tone and motor activity of the stomach and intestines.

In connection with the ability to reduce the secretion of sweat glands, atropine is sometimes used for excessive sweating.

Atropine is an effective antidote (antidote) for poisoning with cholinomimetic and anticholinesterase substances, including FOS (organophosphorus substances); It is used in acute poisoning with FOS, usually in combination with cholinesterase reactivators.

In ophthalmic practice, atropine is used to dilate the pupil for diagnostic purposes (to examine the fundus, determine the true refraction, etc.), as well as for therapeutic purposes in acute diseases: with iritis (inflammation of the iris), iridocyclitis (combined inflammation of the cornea and iris). membranes of the eye), keratitis (inflammation of the cornea), etc., as well as eye injuries. The relaxation of the muscles of the eye caused by atropine contributes to its functional rest and accelerates the elimination of the pathological process.

Method of application and dose. Apply atropine inside (before meals), parenterally (bypassing the digestive tract) and topically (in the form of eye drops). Inside prescribed for adults in powders, tablets and solutions (0.1%), 0.00025 g (0.25 mg) -0.0005 g (0.5 mg) -0.001 g (1 mg) per reception 1-2 times in a day. Under the skin, intramuscularly and intravenously, 0.00025-0.0005-0.001 g (0.25-0.5-1 ml of a 0.1% solution) is injected.

Children are prescribed, depending on age, 0.00005 g (0.05 mg) -0.0005 g (0.5 mg) per reception.

In the case of using atropine for the treatment of gastric ulcer and duodenal ulcer, the drug is prescribed orally, selecting the dose individually (usually until a slight dry mouth appears). Depending on the sensitivity to atropine, the dose may correspond to 6-8-10-12-15 drops of a 0.1% solution per dose 2-3 times a day. Assign 30-40 minutes before meals or one hour after meals. In cases of exacerbation of the disease, atropine is administered first in the form of subcutaneous injections.

In ophthalmic practice, 0.5-0.1% solutions (eye drops) are used. With a therapeutic purpose, 1-2 drops are prescribed 2-6 times a day. In severe cases, 1% atropine ointment is applied in the evening over the edges of the eyelids. Apply also eye drops with atropine.

For therapeutic purposes, it is advisable to use atropine as a long-acting mydriatic (pupil dilating) agent; for diagnostic purposes, it is more expedient to use less long-acting mydriatic agents. Atropine causes the maximum expansion of the pupil in 30-40 minutes after installation (instillation); the effect lasts up to 7-10 days. Accommodation paralysis (impaired visual perception) occurs after 1-3 hours and lasts up to 8-12 days. At the same time, homatropin causes maximum mydriasis after 40-60 minutes; Mydriatic effect and paralysis of accommodation persist for 1-2 days. The mydriatic effect with the use of platyfillin lasts 5-6 hours.

In case of poisoning with cholinomimetics and anticholinesterase substances, a 0.1% solution of atropine is injected into a vein, preferably together with cholinesterase reactivators.

With bronchospasm (a sharp narrowing of the lumen of the bronchi), atropine can be used in the form of a fine aerosol (0.25 ml of a 0.1% solution is inhaled for 2-3 minutes).

Side effect. Dry mouth, dilated pupils, disturbance of accommodation (impaired visual perception), atony (loss of tone) of the intestine, dizziness, tachycardia (rapid heartbeat), difficulty urinating.

Contraindications. Glaucoma (increased intraocular pressure), severe urination disorders with adenoma (benign tumor) of the prostate gland.

Release form. Powder; ampoules of 1 ml of a 0.1% solution in a package of 10 pieces; 1% solution (eye drops) in 5 ml vials; eye films of 0.0016 g in a package of 30 pieces.

Storage conditions.

Atropine sulfate is also part of the preparations neoephrodal, perfillon, solutan, spasmoveralgin, tulle.

BLACKED LEAVES (Folia Hyoscyami)

Basal and stem leaves of a wild-growing and cultivated biennial herbaceous plant of black henbane (Hyoscyamus niger) fam. nightshade (Solanaceae). Contain at least 0.05% alkaloids of the atropine group (hyoscyamine, scopolamine, etc.).

Pharmachologic effect. They have an analgesic and antispasmodic (relieving spasms) effect.

Indications for use. As an anti-spasmodic and analgesic (instead of belladonna extract).

Method of application and dose. They have limited use in the form of an extract. In powders, pills and potions (0.02-0.05 g per dose).

Higher doses for adults: single - 0.4 g, daily - 1.2 g.

Release form. Powder.

Storage conditions. List B. In a dry place.

BLEACHED OIL (Oleum Hyoscyami)

Indications for use. With neuralgia (pain that spreads along the nerve), myositis (muscle inflammation), rheumatoid arthritis (an infectious-allergic disease from the group of collagenoses, characterized by chronic progressive inflammation of the joints).

Method of application and dose. Used externally for rubbing.

Release form. In vials of 25 g.

Storage conditions.

Bleached oil is also part of the preparations capsin, saliment.

HOMATROPINE HYDROBROMIDE (Homatropini hydrobromidum)

Synonyms: Homatropin hydrobromide.

Pharmachologic effect. Similar to atropine, but less active and its action is shorter.

Indications for use. In ophthalmology, for dilating the pupil and as a means of causing paralysis of accommodation (when examining the fundus).

Method of application and dose. Use 0.25-1% aqueous solution (eye drops). Pupil dilation occurs quickly and disappears after 10-20 hours.

Side effects and contraindications. The same as with the use of atropine sulfate.

Release form. Powder; 0.25% solution in 5 ml vials.

Storage conditions. List A. In a dark place.

DURMANALISTYA (Folia Datura stramonii)

Leaves of a herbaceous wild-growing and cultivated annual plant Datura ordinary (Datura stramonium L), fam. nightshade (Solanaceae), containing alkaloids of the atropine group.

Pharmachologic effect. Coincides mainly with the properties of atropine.

Indications for use. Bronchial asthma.

Method of application and dose. They are rarely used on their own. Inhale the smoke generated by burning 1/2 teaspoon of powder or smoke a cigarette containing Datura leaf powder. Higher doses for adults: single - 0.2 g, daily - 0.6 g.

Side effects and contraindications. See Atropine.

Release form. In a package of 100 g.

Storage conditions. List B. In a dry place.

Dope Oil (Oleum Stramonii)

Indications for use. With neuralgia (pain that spreads along the nerve), rheumatism.

Method of application and dose. Used externally for rubbing.

Release form. In vials of 25 ml.

Storage conditions. List B. In a cool place.

Datura oil is also part of the complex turpentine liniment.

BEAUTY DRUGS

Belladonna is a perennial cultivated herbaceous plant (Belladonna) (Atropa Belladonnae L.) family. Nightshade (Solanaceae).

The plant contains alkaloids of the atropine group (hyoscyamine, scopolamine, apoatropine, etc.). The content of alkaloids in the leaves (in terms of hyoscyamine) must be at least 0.3% according to the requirements of the State Pharmacopoeia; when the content of alkaloids is more than 0.3% for the preparation of dosage forms, the leaves are taken in a correspondingly smaller amount.

Pharmacological properties of belladonna coincide mainly with the properties of atropine.

On the basis of belladonna herbal raw materials, a number of medicines are made:

DRAGEE "BELLOID" (Belloid)

Indications for use. Taken with increased irritability, insomnia, autonomic dystonia, Meniere's syndrome, neurogenic disorders associated with menstrual irregularities, hyperthyroidism (thyroid disease).

Method of application and dose. 1-2 tablets (pellets) 3 times a day.

Side effect. In some cases, dry mouth, nausea, vomiting, diarrhea.

Contraindications. Same as for Bellataminal tablets.

Release form. Dragee in a package of 50 pieces. The composition of one dragee: 0.3 mg of ergotoxin, 0.1 mg of belladonna alkaloids (belladonna) and 0.03 g of butylethylbarbituric acid.

Storage conditions. List B. In a dark place.

BEAM LEAVES (Folia Atropae Belladonnae)

Collected in the phase of the beginning of budding before mass fruiting, the leaves of a perennial cultivated herbaceous plant of belladonna (belladonna) - Atropa belladonna L., fam. nightshade -Solanaceae.

Pharmachologic effect. The pharmacological properties of belladonna coincide mainly with the properties of atropine.

Indications for use. Preparations of belladonna (extracts, tinctures) are used as antispasmodic (relieving spasms) and painkillers for stomach ulcers, gallstones and other diseases accompanied by spasms of the smooth muscles of the abdominal organs, with bradycardia (rare pulse) due to overexcitation of the vagus nerve.

Method of application and dose. Inside in the form of tincture 5-10 drops.

Side effect. Dry mouth, dizziness, disturbance of accommodation (impaired visual perception), tachycardia (rapid heartbeat).

Contraindications. Contraindicated in glaucoma (increased intraocular pressure).

Storage conditions. List B. In a dry, dark place.

Release form. In boxes.

Storage conditions. List B. In a dry, dark place.

Belladonnae Tincture (Tinctura Belladonnae)

Prepared from belladonna leaves (1:10) in 40% alcohol; contains 0.027-0.033% alkaloids.

Indications for use. It is used as an antispasmodic (relieving spasms) and analgesic for gastric ulcer, cholelithiasis and other diseases accompanied by spasms of the smooth muscles of the abdominal organs, with bradycardia (rare pulse) due to overexcitation of the vagus nerve.

Method of application and dose. Adults: 5-10 drops per reception; children 1-5 drops per reception, depending on age.

Higher doses for adults: single - 0.5 ml (23 drops), daily - 1.5 ml (70 drops).

Release form. In vials of 10 ml.

Storage conditions. List B. At room temperature, protected from light.

BELLATAMINAL TABLETS (Tabulettae "Bellataminalum")

Pharmachologic effect. Combined drug, the action of which is due to the properties of its constituent components. Reduces the excitability of the central and peripheral adrenergic and cholinergic systems of the body, has a calming effect on the central nervous system.

Indications for use. Applied with increased irritability, insomnia, menopausal neuroses, neurodermatitis (skin diseases caused by dysfunction of the central nervous system), autonomic dystonia.

Method of application and dose. Assign 1 tablet 2-3 times a day (after meals).

Side effect. Dry mouth, dizziness.

Contraindications. Due to the content of ergotamine, which can cause contraction of the uterus and blood vessels, tablets are contraindicated during pregnancy and childbirth, with spasms (sharp narrowing of the lumen) of the vessels of the heart and peripheral vessels, in advanced stages of atherosclerosis. Also contraindicated in glaucoma (increased intraocular pressure).

Release form. Coated tablets containing: belladonna alkaloids - 0.0001 g (0.1 mg), phenobarbital - 0.02 g (20 mg), ergotamine tartrate - 0.0003 g (0.3 mg).

Storage conditions. List B. In a dark place.

The belladonna is also included in the preparations of antastman, bellergal, valerian, Poland, belladonna tincture, valerian, wormwood, belladonna and peppermint tincture, Zelenin drops, anti-asthma collection, candles "anuzol", candles "betiol", solutan, tablets "becarbon", Bellalgin tablets, Bepasal tablets, Besalol tablets, gastric tablets with belladonna extract, theofedrin, theofedrin N, thick belladonna extract, dry belladonna extract.

METACIN (Methacinuni)

Synonyms: Metacin iodide.

Pharmachologic effect. Active M-anticholinergic agent, selectively acting peripheral anticholinergic.

Indications for use. Diseases accompanied by spasms of smooth muscles (peptic ulcer of the stomach and duodenum, chronic gastritis, renal and hepatic colic, etc.), in anesthesiology to reduce the secretion of the salivary and bronchial glands, etc.

Method of application and dose. Inside, 0.002-0.004 g 2-3 times a day, parenterally (bypassing the digestive tract) - 0.5-2 ml of a 0.1% solution.

The highest single dose for adults when taken orally - 0.005 g, daily - 0.015 g, single parenteral - 0.002 g, daily - 0.006 g.

Side effect. In case of an overdose, dry mouth, constipation, difficulty urinating.

Contraindications. Glaucoma (increased intraocular pressure), hypertrophy (increase in volume) of the prostate gland.

Release form. Tablets of 0.002 g in a package of 10 pieces; ampoules of 1 ml of a 0.1% solution in a package of 10 pieces.

Storage conditions. List A. In a dark place.

PLATIFILLINA HYDROTARTRATE (Platyphyllini hydrotartras)

Tartar rock salt of the alkaloid contained in the broad-leaved ragwort (Senecio platyphyllus).

Pharmachologic effect. It has a predominantly M-anticholinergic, as well as a vasodilating and calming effect.

Indications for use. Spasms of smooth muscles of the abdominal organs, peptic ulcer of the stomach and duodenum, bronchial asthma, hypertension (persistent rise in blood pressure), colic (intestinal, renal, hepatic), etc.; in ophthalmology for pupil dilation.

Method of application and dose. Inside, 0.0025-0.005 g 2-3 times a day, subcutaneously - 1-2 ml of a 0.2% solution. In eye practice, a 1% solution is used for diagnosis, a 2% solution for therapeutic purposes.

Higher doses for adults inside and under the skin: single - 0.01 g, daily -0.03 g.

Side effect. Dry mouth, disturbance of accommodation (impaired visual perception), palpitations, difficulty urinating.

Contraindications. Glaucoma (increased intraocular pressure). Organic diseases of the liver and kidneys.

Release form. Powder; tablets of 0.005 g in a package of 10 pieces; ampoules of 1 ml of a 0.2% solution in a package of 10 pieces.

Storage conditions. List A. In a dark place.

TABLETS "PALYUFIN" (Tabulettae "Palunnum")

Pharmachologic effect. Combined drug - antispasmodic (relieving spasms) and anticholinergic agent.

Indications for use. The same as for platifillin.

Method of application and dose.

Side effects and contraindications are the same as for platifillin.

Release form. Composition tablets: platyfillin hydrotartrate - 0.005 g, phenobarbital and papaverine hydrochloride - 0.12 g each.

Storage conditions. List A. In a dry place.

TEPAFILLIN TABLETS (Tabulettae "ThepaphyUinum")

Pharmachologic effect. Combined drug - antispasmodic (relieving spasms), anticholinergic, vasodilator.

Indications for use. The same as for platifillin.

Method of application and dose. Assign 1 tablet 2-3 times a day.

Side effects and contraindications are the same as for platifillin.

Release form. Composition tablets: platyfillin hydrotartrate - 0.003 g, papaverine hydrochloride and phenobarbital - 0.03 g each, theobromine - 0.25 g.

Storage conditions. List A. In a dry place.

Prifinium bromide (Prifinium bromide)

Synonyms: Riabal for children.

Pharmachologic effect. Anticholinergic agent, acting mainly on the M-cholinergic receptors of the digestive tract. Reduces the secretion (release) of hydrochloric acid and reduces the peptic (secretory) activity of gastric juice. Reduces exocrine activity (secretion of digestive juices) of the pancreas. Reduces the tone of the smooth muscles of the gastrointestinal tract, promotes gastric emptying, has a corrective effect in case of increased motor (motor) activity of the digestive tract.

Indications for use. Vomiting: common in infants and children; with acute gastroenteritis (inflammation of the mucous membranes of the stomach and small intestine); in febrile conditions (a sharp increase in body temperature); with intracranial hypertension (increased intracranial pressure); with radiation therapy; with drug intolerance. Abdominal pain syndrome (abdominal pain): functional diseases of the colon, accompanied or not accompanied by obstruction and bloating; spasms of smooth muscles of the gastrointestinal tract of a psychogenic nature; as an addition to the etiological (affecting the immediate cause of the disease) treatment of diseases of the gastrointestinal tract.

Method of application and dose. The solution of the drug is intended for oral administration only. The average daily dose is 1 mg/kg body weight of the child. When determining the daily dose, it should be taken into account that one pipette filled to the red line contains a dose of 2 mg (0.4 ml). The frequency of administration of the drug - 3 times a day.

Side effect. Dry mouth, dilated pupils, disturbance of accommodation (impaired visual perception), drowsiness

Contraindications. Increased intraocular pressure, urinary tract dysfunction, manifested in urinary retention.

Release form. Solution for oral administration in 50 ml vials with a 0.4 ml pipette. (50 ml of solution contains 0.25 g of prifinium bromide; in a filled pipette - 0.002 g).

Storage conditions. List B. In a cool, dark place.

PROPANTELIN BROMIDE (Propantheline bromide)

Synonyms: Pro-Bantin, Aklobrom, Bropantil, Ketaman, Lenigastril, Mefatelin, Neo Gastrosedal, Pantelin, Progastron, Propantel, Spaztil, Suprantil, etc.

Pharmachologic effect. It has a peripheral anticholinergic and antispasmodic (relieving spasms) effect.

Indications for use. It is used for functional gastrointestinal disorders, peptic ulcer of the stomach and duodenum, spasms of the ureter and bladder, etc.

Method of application and dose. Assign inside 1-2 tablets (15-30 mg) 2-3 times a day.

Side effects and contraindications are the same as for metacin.

Release form. Tablets of 0.015 g (15 mg) in glass tubes of 20 pieces.

Storage conditions. List A. In a dark place.

SCOPOLAMINE (Scopolamine)

Synonyms: Scopolamine hydrobromide, Hyoscine hydrobromide.

Pharmachologic effect. Close to atropine in its effect on peripheral cholinergic systems. Like atropine, it causes dilated pupils, paralysis of accommodation (impaired visual perception), increased heart rate, relaxation of smooth muscles, and a decrease in the secretion of the digestive and sweat glands.

It also has a central anticholinergic effect. Usually causes a sedative (calming) effect: reduces physical activity, may have a hypnotic effect. A characteristic property of scopolamine is the amnesia (memory loss) it causes.

Indications for use. They are sometimes used in psychiatric practice as a sedative, in neurological practice for the treatment of parkinsonism, in surgical practice, together with analgesics (morphine, promedol, 256), to prepare for anesthesia, sometimes as an antiemetic and sedative for sea and air sickness, and also for iritis (inflammation of the iris), iridocyclitis (combined inflammation of the cornea and iris) and for diagnostic purposes to dilate the pupils instead of atropine.

Method of application and dose. Assign scopolamine inside (usually in solutions) and under the skin in single doses of 0.00025-0.0005 g (0.25-0.5 mg) or 0.5-1 ml of a 0.05% solution. In eye practice (to dilate the pupil and paralysis of accommodation), a 0.25% aqueous solution (1-2 drops in the eye 2 times a day) or a 0.25% ointment is used.

Higher doses for adults inside and under the skin: single - 0.0005 g, daily -0.0015 g.

In ophthalmic practice, along with a 0.25% aqueous solution, a prolonged (long-acting) drug is used - a solution of scopolamine hydrobromide 0.25%.

Contraindications. Contraindications are the same as for the appointment of atropine. It is necessary to take into account a very wide difference in individual sensitivity to scopolamine: relatively often, ordinary doses do not cause sedation, but arousal, hallucinations (delusions, visions that acquire the character of reality) and other side effects.

Release form. Powder; 0.05% solution in 1 ml ampoules; 0.25% solution with methylcellulose in vials of 5 and 10 ml.

Storage conditions. List A. In a well-closed container and protected from light.

TABLETS "AERON" (Tabulettae "Aeronum")

Pharmachologic effect. Combined drug, the action of which is associated with the peculiarities of the pharmacological properties of its components - scopolamine and hyosiamine.

Indications for use. Aeron tablets are used to prevent and treat sea and air sickness, as well as to prevent and relieve (relieve attacks of Meniere's disease. Sometimes they are used to reduce tear and salivation during plastic surgery on the face and during operations on the upper respiratory tract.

Method of application and dose. In case of air and seasickness, tablets are prescribed orally: prophylactically, 30-60 minutes before departure, take 1-2 tablets, and later, if necessary, after 6 hours, one more tablet. If Aeron was not used prophylactically, then at the first sensations of the disease (nausea, dizziness, headache) take 1-2 tablets, then give one tablet 2 times a day.

Higher doses for adults: single - 2 tablets, daily - 4 tablets.

In rare cases, with persistent vomiting, instead of Aeron, suppositories containing as much camphorate scopolamine and hyoscyamine can be prescribed as they are contained in one Aeron tablet.

In Meniere's disease, 1 tablet is prescribed 2-3 times a day. For surgical interventions on the face 20-30 minutes before surgery, 2 tablets are prescribed immediately and after surgery, 1 tablet 2 times a day for the first 2 days.

Side effect. When using aeron, thirst, dry mouth and throat are possible. Drinking and caffeine are prescribed to alleviate this condition.

Contraindications. Do not prescribe to patients with glaucoma (increased intraocular pressure).

Release form. Tablets of 0.0005 g in a package of 10 pieces. Ingredients: scopolamine camphorate - 0.0001 g and hyoscyamine camphorate - 0.0004 g.

Storage conditions. List B. In a dark place.

SPASMOLITIC (Spasmolytinum)

Synonyms: Difacil, Adifenin, Trazentin, Vagospasmil, Vegantin.

Pharmachologic effect. It has peripheral M-anticholinergic activity; in addition, it has a blocking effect on N-cholinergic systems. Has antispasmodic activity: relaxes smooth muscles of internal organs and blood vessels; also causes local anesthesia (loss of sensation at the injection site).

Indications for use. It is used for pylorospasm (spasm of the pyloric muscles of the stomach), spastic colic, cholelithiasis, renal colic, peptic ulcer of the stomach and duodenum, for angina pectoris, endarteritis (inflammation of the inner lining of the arteries), as well as for neuralgia (pain spreading along the nerve), neuritis (inflammation of the nerve), radiculitis. There is evidence of the effectiveness of the drug in itching dermatoses (skin diseases), as well as migraines.

Method of application and dose. Assign inside after eating 0.05-0.1 g 2-3-4 times a day. The course of treatment is 3-4 weeks.

Side effect. When using an antispasmodic (as well as other anticholinergics), the dose should be individually selected. In case of an overdose, dizziness, headache, a feeling of intoxication (due to the central action), dry mouth (due to the peripheral anticholinergic effect), and disturbance of accommodation (impaired visual perception) may appear.

Having an irritating effect on the gastric mucosa, the antispasmodic can cause dyspeptic symptoms (digestive disorders).

The feeling of intoxication or dizziness can be prevented or relieved by the appointment of caffeine: 0.1-0.2 g of sodium caffeine benzoate orally or 1 ml of a 20% solution under the skin.

Contraindications. Contraindicated in glaucoma (increased intraocular pressure).

Antispasmodic and drugs close to it (arpenal, etc.) should not be taken before and during work by drivers of transport and other persons whose profession requires a quick mental and physical reaction.

Release form. Powder.

Storage conditions. List B. In a dry, dark place.

TROVENTOL (Troventolum)

Synonyms: Truvent.

Pharmachologic effect. It is an anticholinergic substance, acting mainly on M-cholinergic receptors. Compared with atropine, the effect of troventol on the cholinergic receptors of the bronchial muscles is stronger and longer with a less pronounced effect on the cholinergic receptors of other organs (heart, intestines, salivary glands). Troventol does not penetrate the blood-brain barrier (the barrier between blood and brain tissue). The selective action of troventol determines its advantages over atropine as a bronchodilator and its better tolerability.

Indications for use. Troventol as a very active bronchodilator (expanding the lumen of the bronchi) is used for chronic obstructive bronchitis (inflammation of the bronchi, combined with impaired air passage through them), bronchospasm (sharp narrowing of the lumen of the bronchi) in chronic pneumonia, with bronchospasm associated with colds (including number in elderly patients).

Troventol is most effective in bronchospasm caused by hyperactivity of the cholinergic system, when adrenomimetics (see Orciprenaline) and methylxanthines (see Theophylline) are not effective enough.

Method of application and dose. Troventol is used in the form of inhalation from aerosol cans. There are cylinders with two dosages: 12.5 and 25 mg per cylinder. Each time you press the valve of the balloon with 12.5 mg, a single dose of troventol 40 mcg (0.04 mg) is released, and when you press the valve of the balloon with 25 mg - 80 mcg (0.08 mg).

The prophylactic and therapeutic dose of the drug can vary in different patients from 40 to 160 mcg. The daily dose is 120 and 480 mcg, respectively.

Start with the appointment of 40 mcg, i.e. one breath when you press the valve of the balloon with 12.5 mg. If the effect is insufficient, two breaths (two clicks) are produced, i.e., a single dose is increased to 80 mcg. Depending on the clinical effect and tolerability of the drug, a single dose is increased to 80-160 mcg, while for convenience, a balloon with 25 mg of troventol is used (1-2 clicks). With a sufficient effect from a single dose of 40 mcg, continue to use a balloon with 12.5 mg of troventol.

Inhalations are repeated every 4-6 hours.

Side effect. Troventol inhalations are usually well tolerated, however, due to the anticholinergic effect, dry mouth, sore throat, and slight disturbances in accommodation (impaired visual perception) are possible. If necessary, in these cases, reduce the dose or increase the intervals between inhalations, and with severe side effects, temporarily stop inhalation.

Contraindications. Glaucoma (increased intraocular pressure); pregnancy.

Release form. Aerosol aluminum cans with a capacity of 21 g containing troventol 12.5 or 25 mg.

Storage conditions. List A. In a place protected from heat and direct sunlight at a temperature not exceeding +30 ° C.

TROPICAMIDE (Tropicamide)

Synonyms: Midrum.

Pharmachologic effect. Refers to mydriatic (pupil dilating) means. It blocks M-cholinergic receptors of the sphincter of the iris and ciliary muscle (structural formations of the eye), causing mydriasis (pupil dilation) and accommodation paralysis (disorder of the motor function of the ciliary muscle of the eye, accompanied by impaired visual perception). The action of the drug comes quickly, is relatively short. The tendency to increase intraocular pressure is less pronounced than with atropine. The expansion of the pupils is observed 5-10 minutes after the use of the drug; maximum mydriasis and cycloplegia (accommodation paralysis) are noted after 20–45 minutes and persist for 1–2 hours. The initial pupillary width is restored after 6 hours. side effects due to the systemic action of the drug.

Indications for use. For diagnostic purposes, if necessary, mydriasis and cycloplegia, including when examining the fundus and determining refraction (refractive power of the eye). With hypersensitivity to other drugs that dilate the pupil (atropine, scopolamine, 95). As part of the complex therapy of inflammatory processes and bruising of adhesions - fusion of eye tissues with surrounding tissues).

Method of application and dose. For diagnostic purposes, 0.5% or 1% solutions are used in a single dose of 1-2 drops according to the scheme, depending on the type of study. When using a 0.5% solution of the drug, the optimal time to study the refraction of the eye is 25-40 minutes, 1% solution - 25-50 minutes. For treatment, a 0.5% solution is used up to 6 times a day.

Eye drops are instilled into the lower conjunctival sac (the cavity between the posterior surface of the lower eyelid and the anterior surface of the eyeball). To reduce the resorptive effect of the drug (the effect of the drug, which manifests itself after its absorption into the blood), light pressure on the area of ​​​​the lacrimal sacs is recommended for 2-3 minutes after instillation. Soft contact lenses should not be worn during treatment. Cold compresses are recommended to eliminate hyperthermia (fever).

Side effect. When using high doses of the drug, an increase in intraocular pressure (an attack of glaucoma), accommodation disorders (impaired visual perception), photophobia (photophobia) are possible. Possible systemic effects (more often in children): headache, psychopathic reactions, tachycardia (rapid heartbeat), lowering blood pressure, collapse (a sharp drop in blood pressure), hyperthermia (fever), transient burning sensation, dry mouth, allergic reactions .

Contraindications. Glaucoma, especially angle-closure. Hypersensitivity to the components of the drug.

Release form. Eye drops (0.5%) in a 10 ml dropper bottle; eye drops (0.5% and 1%) in 10 ml vials.

Storage conditions. In a cool place.

Similar posts