What is atropine. Medicinal reference book geotar

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Atropine
Anticholinergics (M-anticholinergics)

Release form

Solution d / in. 0.05%, 0.1%
Tab. 0.5 mg

Mechanism of action

Atropine binds strongly to muscarinic cholinergic receptors and blocks them, preventing the stimulating effect of acetylcholine. Atropine interacts with both central and peripheral M-cholinergic receptors.

Main Effects

■ Reduces the secretion of salivary, gastric, bronchial, lacrimal and sweat glands.
■ Reduces the tone of the muscles of internal organs (bronchi, gastrointestinal tract, bile ducts and gallbladder, urethra, bladder), increases the tone of the sphincters; reduces the tone of the vagus nerve, which causes tachycardia, improves conduction in the heart muscle.
■ Causes paralysis of accommodation, dilates the pupil, impedes the outflow of intraocular fluid, which increases intraocular pressure.
■ It has a stimulating effect on the central nervous system, in toxic doses causes agitation, agitation, hallucinations, coma.

The maximum effect is manifested in 2-4 minutes after i / v administration, after ingestion in the form of drops - after 30 minutes.

Pharmacokinetics

Well absorbed from the gastrointestinal tract. It is widely distributed throughout the organs and tissues of the body, passes through the BBB, the placenta, penetrates into breast milk. It is found in significant concentrations in the central nervous system 0.5-1 hour after administration. Communication with plasma proteins - 18%.

Metabolized in the liver by enzymatic hydrolysis. It is excreted by the kidneys unchanged (50%), in the form of hydrolysis and conjugation products. T1 / 2 - 2 hours.

Indications

■ Premedication before surgery (in combination with anxiolytics, analgesics, antihistamines).
■ Hypersalivation (during dental interventions).
■ Peptic ulcer of the stomach and duodenum, pylorospasm, cholelithiasis.
■ Spasms of the intestines and urinary tract.
■ Bronchial asthma, bronchitis with hyperproduction of mucus.
■ Bradyarrhythmia.

Dosage and administration

Atropine is used orally, parenterally (s / c, i / v, i / m) and topically.

Inside: before meals - powders, tablets, solution. To eliminate bradycardia in adults - 0.5-1 mg IV, if necessary, after 5 minutes, the introduction is repeated; children - 10 mcg / kg. For premedication, adults are prescribed 0.4–0.6 mg intramuscularly 45–60 minutes before anesthesia; children - 0.01 mg / kg. To reduce salivation - inside adults 0.025-1 mg before intervention.

Contraindications

■ Hypersensitivity.
■ Glaucoma.
■ Obstructive bowel and urinary tract diseases.
■ Paralytic ileus.
■ Toxic megacolon.
■ Ulcerative colitis.
■ Hernia of the esophageal opening of the diaphragm.

Precautions, therapy control

Between taking atropine and antacid drugs containing aluminum or calcium, the interval should be at least 1 hour.

Atropine should not be abruptly discontinued, tk. there may be symptoms similar to the "withdrawal" syndrome.

During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration, speed of psychomotor reactions and good vision.

Prescribe with caution:
■ in chronic heart failure, coronary heart disease;
■ with atrial fibrillation, tachycardia;
■ with mitral stenosis;
■ with arterial hypertension;
■ in case of acute bleeding;
■ with thyrotoxicosis;
■ with liver failure (decreased metabolism);
■ with intestinal atony in elderly patients or debilitated patients (obstruction is possible);
■ with renal failure;
■ in chronic lung diseases, especially in young children and debilitated patients;
■ with prostatic hypertrophy;
■ with cerebral palsy;
■ with Down's disease (reaction to anticholinergic drugs is increased);
■ patients with fever;
■ patients with dry mouth;
■ during pregnancy;
■ during lactation;
■ in the elderly and senile age.

Side effects

System effects:
■ xerostomia, thirst;
■ intestinal atony;
■ constipation;
■ atony of the bladder;
■ urinary retention;
■ mydriasis, increased intraocular pressure;
■ accommodation paralysis;
■ tachycardia;
■ headache;
■ dizziness;
■ insomnia, excitation of the central nervous system;
■ violation of tactile perception;
■ dysphagia.

Interaction

Synonyms

Atropine (Russia)

G.M. Barer, E.V. Zoryan

Atropine is a drug used to create a drug ( extension) long-term action (the effect lasts up to 10 days).

Composition, release form

Atropine - 1% eye drops solution, contains:

• Active ingredients: atropine sulfate - 10 mg;
• Excipients: sodium chloride, sodium disulfite, water.

Package. The bottles supplied with a cover dispenser - 5 and 10 ml.

pharmachologic effect

Atropine is a naturally occurring alkaloid derived from plants in the nightshade family. Its action is the expansion of the pupil, associated with inhibition of the outflow of intraocular fluid and an increase in intraocular pressure, which leads to paralysis. Such paralysis, without a therapeutic effect, can significantly reduce near visual acuity. Therefore, it is very difficult to work with papers, drive a car or complex mechanisms under the influence of atropine.

The effect of exposure to a 1% solution of atropine occurs within 30-40 minutes. after applying eye drops. The duration of action of the drug is approximately four days, then the functions of the eye are gradually restored. The maximum exposure time is 10 days, after which the pupil can again naturally expand and contract.

Absorption of the drug occurs through the conjunctiva of the eye (outer shell). Relaxation, fixing, ciliary muscle and its displacement into the anterior chamber begins in parallel with the cessation of the outflow of intraocular fluid from there. The result of this process is an increase in intraocular pressure, therefore, in patients with certain types of Atropine, it can cause an exacerbation.
Treatment with atropine should be carried out in a specialized medical institution, under the control of intraocular pressure.

Indications for use

Atropine solution is prescribed to dilate the pupil, which is necessary for detailed diagnosis, as well as the treatment of certain eye diseases. However, it is used to achieve accommodation paralysis, in which the pupil of the eye cannot constrict, and the eye is not able to change the focal length. Such paralysis is the main condition for thorough research, with the identification of true or false, as well as the treatment of certain intraocular diseases.

Atropine is also used to create rest, which is mandatory for a number of eye pathologies: inflammatory processes, arterial spasms, injuries, as well as a tendency to thrombosis in the vessels of the organ of vision. Atropine relaxes the muscles of the eye, and the restoration of normal functions is greatly accelerated.

Dosage and administration

Atropine solution is instilled into the affected eye 1 or 2 drops, up to 3 times daily. The intervals between instillations do not exceed 6 hours. Children are not prescribed a solution of the drug, the percentage of which is higher than 0.5.

Attention! When administering the drug under the conjunctiva, it is recommended to press the inner lower corner of the eye in the region of the point with your finger, which will close its access to the systemic circulation, significantly reducing the risk of atropine side effects.

Contraindications

• Hypersensitivity;
• Diagnosed or suspected angle-closure or narrow-angle glaucoma;
• Synechia;
• Younger children's age.

Atropine is used with caution in women during pregnancy, lactation, and in patients over 40 years of age. To prescribe the drug in patients with severe arrhythmias, arterial hypertension, or other pathologies of the cardiovascular system, a consultation with a cardiologist is necessary. For the use of Atropine, potentially dangerous conditions are also diseases of the gastrointestinal tract, liver, urinary organs, thyroid gland, fever.

Side effects

• conjunctiva and skin, .
• Dry mouth, headaches, dizziness, anxiety, restlessness, palpitations, impaired skin sensitivity.

If any of the described signs appear, the drug should be immediately discontinued.

Overdose

An overdose of Atropine is expressed in an increase in the manifestations of side effects, which requires immediate discontinuation of the drug and seeking help from a medical institution.

Interaction with other tools

The simultaneous use of Atropine and other drugs with anticholinergic action leads to an increase in its effect.

Storage conditions and special instructions

The simultaneous use of Atropine and drugs with anticholinergic activity causes an increase in its action. Its simultaneous appointment with phenylephrine can cause an increase in blood pressure. Under the influence of nitrates, the likelihood of an increase in intraocular pressure increases. Under the influence of guanethidine, the hyposecretory effect of atropine is reduced.
During treatment with Atropine, it is worth refusing to drive vehicles and engage in any kind of activity that requires the speed of psychomotor reactions and high visual acuity.

The pupils dilated under the action of the drug let in more light, which harms the retina. Therefore, during treatment with Atropine, it is necessary to use sunglasses during the day.

The drug is not prescribed to users, for the duration of treatment they must be replaced with glasses. If necessary, put on lenses, it is better to do this 1 hour after the instillation of Atropine, or use the drug only in the evening, having already removed the lenses.

To store the drug, a dark place should be chosen, away from children. After a three-year shelf life, the vial must be disposed of, even if it has not yet been opened.

Atropine eye drops have many serious, life-threatening side effects. Therefore, its independent use, especially the introduction of the drug for the first time, is absolutely unacceptable. In our ophthalmological center, in order to prevent undesirable consequences, the instillations of the drug are carried out only under medical supervision in a special treatment room, where there is a set of emergency aid needed in an emergency.

Atropine's analogs

Analogues of Atropine are drugs Midriacil, Cyclomed, Irifrin.

The price of the drug

Atropine price in online stores in Russia: 42 rubles.

Atropine (Atropine) is a well-known drug that has a natural origin - found in some plants. Despite its active use in medicine, atropine is a dangerous substance - it is easy for them to get poisoned, especially for children. To do this, you need to eat belladonna berries that grow everywhere.

So, what is atropine, how does it work and where is it used? How to determine poisoning with it and what to do about it? What antidotes exist? Let's figure it out.

Atropine is a dangerous alkaloid

What is atropine? This substance belongs to the group of alkaloids. Alkaloids are called heterocyclic bases containing a nitrogenous group, present in some plants and exhibiting biological activity. In other words, alkaloids are compounds that can somehow affect a living organism. Several alkaloids may be present in one plant.

Such an alkaloid is found in belladonna (Belladonna), henbane, dope, scopolia and other plants of the nightshade family. Atropine (lat. atropinum) is a natural poison, but in small doses it is used for medical purposes.

According to the chemical structure, atropine belongs to crystalline powders. It is amorphous, colorless, odorless. The substance has two isomers. The levorotatory is called hyoscyamine, which is much more active than atropine. It is hyoscyamine that is found in plants. But this substance is unstable and when chemically released, it turns into atropine.

The mechanism of action of atropine

This alkaloid disrupts the conduction of a nerve impulse by blocking receptors. That is, it competes with the natural substance of the body (acetylcholine) in the ability to bind to sensitive endings along the path of the impulse. There are several types of sensitive endings: M and H. Atropine blocks only M receptors.

The mechanism of action of atropine is that it binds to specific formations of the nerve cell instead of acetylcholine. Accordingly, the transmission of the nerve impulse is blocked. Depending on which organ system it acts on, atropine causes different effects.

Where is atropine used?

There are 2 drugs, the main active ingredient of which is belladonna alkaloid:

• "Atropine" - tablets;
• "Atropine sulfate" - 0.1% injection and 1% eye drops.

The drug is widely used in clinical practice. The use of atropine is practiced in gastroenterology. He is appointed:

• with ulcers of the duodenum and stomach in order to suppress gastric secretion;
• spasm of the pyloric sphincter of the stomach to relax it;
• cholelithiasis and inflammation of the gallbladder in order to expand the ducts and drain stagnant bile;
• with spasms of the intestines;

In other branches of medicine, atropine is used:

• with spasms of the bladder;
• bronchial asthma, as a means of eliminating bronchospasm;
• to reduce the secretion of glands: salivary, sweat, lacrimal;
• with a slowing of the pulse associated with the tone of the vagus (must be prescribed carefully, since there may be a short-term increase in bradycardia);
• in anesthesiology for sedation and anesthesia, during surgery, intubation, to eliminate laryngospasm and bronchospasm, reduce salivation;
• with radiography of the stomach to reduce its tone during the study;
• with increased sweating.

What else is atropine used for? This drug is an antidote for poisoning with organophosphorus compounds, including poisons, an overdose of cholinomimetic and anticholinesterase drugs. In addition, atropine is used in ophthalmology as a drug that dilates the pupil in the study of the fundus.

Overdose and poisoning

Atropine can be used intramuscularly, by mouth, intravenously, subcutaneously, or as eye drops. Orally, it is prescribed from 0.25 to 1 mg 1-3 times a day. This variation in dosage is due to the individuality of each organism and the amount of the drug should be selected individually. Intravenously, intramuscularly, subcutaneously in the same dosage, but 1-2 times a day. Atropine in the form of eye drops is instilled 1-2 drops 3 times a day. To expand the pupil for research - 1-2 drops 1-2 times. The maximum single dose of atropine is 1 mg, the maximum daily dose is 3 mg.

Atropine poisoning can be accidental or purposeful. The severity of manifestations depends on this. Basically, poisoning occurs when the fruits of the nightshade family are accidentally consumed. Children are in the main risk group.

Overdose symptoms

The toxic effect of atropine begins to appear 40-60 minutes after ingestion. Depending on the dose, mild, moderate and severe degrees of poisoning are distinguished. First of all, the substance affects the structures of the brain, causing psychosis, impaired coordination, hallucinations. Then the heart and lungs suffer.

An overdose of atropine is detected by the following symptoms:

Such symptoms may occur with unintentional overdose.

Targeted poisoning has more serious symptoms:

The lethal dose of atropine is 100-150 mg or 1-1.5 mg per 1 kg of body weight. Children have a lower dose. In terms of belladonna berries - 3-6 pieces can cause death in a child. Death usually occurs no earlier than 5 hours after poisoning.

The consequences of poisoning can be not only death. With a long stay in a coma, irreversible organic changes in the brain can occur, leading to impaired intelligence and memory.

Antidote

Treatment of poisoning begins with gastric lavage with water, potassium permanganate or saline laxative solutions. Immediately you need to give the poisoned antidote atropine. It could be:

• 0.1% solution of aminostigmine 2 mg;
• 0.05% solution of galantamine (drug "Nivalin") 2 mg.

The administration of the antidote should be repeated after 90 minutes. The more severe the poisoning, the less interval the antidote is administered. In a severe case, it can be administered every 15 minutes.

Aminostigmine quickly restores consciousness, eliminates psychomotor agitation and hallucinations. It is used not only for the treatment of overdose, but also for the prevention of recurrence of coma.

There is another atropine antagonist - the alkaloid pilocarpine. Preparations based on it (eye drops) are used in ophthalmology to reduce intraocular pressure. Atropine, dilating the pupil, can cause glaucoma. With a strong increase in pressure inside the eye, retinal detachment can occur. Therefore, in case of poisoning with plants or preparations containing atropine, pilocarpine should be administered immediately according to the following scheme:

• every 15 minutes, 1 drop in each eye for an hour;
• the next 2-3 hours drip 1 drop in 30 minutes;
• then 4-6 hours - drop by drop every hour;
• then 3-6 times a day drop by drop until high intraocular pressure is relieved.

Let's summarize. Atropine is a plant alkaloid from the nightshade family. It is an anticholinergic drug widely used in medicine. It is used in gastroenterology, pulmonology, cardiology, ophthalmology, anesthesiology, toxicology, urology. A serious overdose of this drug can occur if nightshade berries or large amounts of the drug are ingested accidentally. The clinic of poisoning depends on the accepted dose. Death occurs from taking 100 mg of atropine. There are specific antidotes that need to be taken immediately - these are aminostigmine and galantamine. They are administered intravenously repeatedly. The consequences of atropine poisoning can be coma, impaired intelligence and memory.

The composition of the drug contains the main substance atropine sulfate and additional components depending on its shape.

Release form

The main form of release of Atropine: injection solution and eye drops. The solution is packaged in 1 ml ampoules, and eye drops in 5 ml dropper bottles.

pharmachologic effect

The drug has cholinolytic action capable of blocking M-cholinergic receptors.

Pharmacodynamics and pharmacokinetics

Atropine is an alkaloid that is also found in some plants, such as belladonna, dope, henbane and others. In medicine, a substance called is used. It should be noted that the release form of this component is a granular or crystalline powder of white color, odorless. It is easily soluble in water or ethanol, shows resistance to chloroform and ether.

The pharmacological group, which includes this drug, is anticholinergic. The mechanism of action includes the blocking of m-cholinergic receptors.

The use of this substance leads to amidriasis, accommodation paralysis, increased intraocular pressure, and xerostomia. Inhibition of the secretion of bronchial, sweat and other glands was also noted. Relaxation occurs in the smooth muscles of the bronchi, bile or urinary organs, gastrointestinal tract, that is, the substance acts as an antagonist and exhibits an antispasmodic effect.

In high doses, excitation of the nervous system is possible. When Atropine is administered intravenously, the manifestation of the maximum effect is noted after 2-4 minutes, and if eye drops are used, then after 30 minutes.

Combination with antacids containing Al3+ or Ca2+ may reduce the absorption of the main substance from the gastrointestinal tract. Some tricyclic antidepressants , phenothiazines , Quinidine, antihistamines and other drugs with m-anticholinergic features can enhance the development of systemic undesirable effects.

Nitrates can cause an increase in intraocular pressure, and Atropine can change absorption parameters and Meksiletina .

special instructions

The use of atropine for distal AV block with wide QRS complexes is ineffective and is generally not recommended.

When the solution is dripped into the conjunctival sac, the lower lacrimal punctum should be gently pressed to avoid droplets entering the nasopharynx. Conducting subconjunctival or parabulbar injection is recommended with simultaneous administration in order to reduce tachycardia.

Terms of sale

On prescription.

Storage conditions

To store any form of the drug, a dark, cool place is required that is inaccessible to children.

Shelf life

For injection solution - 5 years, for eye drops - 3 years.

Atropine's analogs

Coincidence in the ATX code of the 4th level:

Main analogues: , and .

Atropine is an anticholinergic and antispasmodic.

The active substance of this drug is Atropine, which is a poisonous alkaloid that is found in the leaves and seeds of plants of the nightshade family, such as henbane, belladonna, dope. The main chemical feature of Atropine is its ability to block the M-cholinergic systems of the body, which are located in the heart muscle, smooth muscle organs, the central nervous system and secretory glands. As a result of this blocking, M-cholinergic receptors become insensitive to the mediator of nerve impulses (acetylcholine).

The use of Atropine helps to reduce the secretory function of the glands, relax the tone of smooth muscle organs, dilate the pupil, increase intraocular pressure and paralysis of accommodation (the ability of the eye to change focal length). Acceleration and excitation of cardiac activity after the use of Atropine is explained by its ability to remove the inhibitory effects of the vagus nerve. The effect of Atropine on the central nervous system occurs in the form of stimulation of the respiratory center, and when using toxic doses, motor and mental excitation (convulsions, visual hallucinations) is possible.

Atropine quickly penetrates into the bloodstream from the site of application, and then is distributed in the body in a short time. The maximum effect of the drug after intravenous administration occurs after 2-4 minutes, after oral administration - after half an hour. Plasma protein binding occurs by 18%. The drug is able to pass through the placental and blood-brain barriers. Excreted by the kidneys, excreted in the urine both in the form of metabolites and unchanged. Traces of the drug can be found in breast milk.

Indications for the use of Atropine

This drug is actively used to treat the following diseases:

• spasm of the bile ducts, smooth muscle organs of the gastrointestinal tract;
• acute pancreatitis, peptic ulcer of the stomach and duodenum;
• renal colic, intestinal colic, irritable bowel syndrome;
• laryngospasm, bronchospasm, bronchitis with hypersecretion, bronchial asthma;
• urinary incontinence due to increased excitability of the muscles of the bladder;
• pulmonary bleeding;
• poisoning with asphyxiants, morphine, cholinomimetic substances, poisonous mushrooms (fly agaric), anticholinesterase drugs.

According to the instructions, Atropine can be used as a premedication before surgical operations, as well as during radiological examinations of the intestine.

In ophthalmology, Atropine drops are used to expand the pupil of the eye and achieve accommodation paralysis to examine the fundus and determine the true refraction of the eye. Atropine drops are also used to create functional rest in case of inflammatory diseases and eye injuries.

How to use Atropine

According to the instructions, Atropine can be used orally, administered intravenously, intramuscularly, under the skin. With these methods of administration, depending on the intended effect, the doctor prescribes a single dose, which usually corresponds to 0.25 - 1 mg or the same number of milliliters and is taken once or twice a day.

With induction anesthesia, Atropine (0.3-0.6 mg) is applied intramuscularly or under the skin half an hour - an hour before anesthesia, and in combination with morphine - 60 minutes before anesthesia.

The use of Atropine in case of poisoning with anticholinergic drugs occurs at 2 mg as an intramuscular injection every half hour.

The maximum single dose of the drug should not exceed 2 mg, and the daily dose should not exceed 3 mg. For children, the daily dose of Atropine is prescribed in two doses and should not exceed 0.02 mg (for children under 6 months), 0.05 mg (6 months - 1 year), 0.2 mg (1-2 years), 0 .25 mg (3-4 years), 0.3 mg (5-6 years), 0.4 mg (7-9 years), 0.5 mg (10-14 years).

In ophthalmology, Atropine drops, ointment or solution are used. 1-2 drops of 1% (adults), 0.5%, 0.25%, 0.125% (children) solution are instilled into the diseased eye, or 1% ointment is placed over the edge of the eyelid. Atropine drops and ointment should be applied no more than three times a day with 5-6 hour intervals. In some cases, the drug in the form of a 1% solution is administered subconjunctivally (instilled into the eye) at a dose of 0.2-0.5% or parabulbarno (injection under the eyeball) - 0.3-0.5 ml.

Side effects

The instructions for Atropine indicate the following negative effects that can be triggered by the use of this drug:

• dizziness, insomnia, headache, euphoria, confusion, impaired tactile perception;
• ventricular tachycardia, ventricular fibrillation, aggravation of myocardial infarction due to excessive tachycardia, sinus tachycardia;
• constipation, xerostomia;
• urinary retention, intestinal and bladder atony, photophobia, fever;
• increased intraocular pressure, development of conjunctivitis, conjunctival hyperemia and edema, accommodation paralysis, mydriasis.

Contraindications to the use of Atropine

This drug is not prescribed for hypersensitivity to it, as well as keratoconus, angle-closure glaucoma, open-angle glaucoma,

The instructions for Atropine indicate a number of diseases in which the appointment of this drug should occur with extreme caution:

Diseases of the cardiovascular system, in which an increase in the number of heart contractions is undesirable;

Increased body temperature;

Reflux esophagitis or associated hiatal hernia;

Diseases of the gastrointestinal tract, which are accompanied by obstruction;

Intestinal atony, especially in debilitated or elderly patients;

Diseases with increased intraocular pressure;

Nonspecific ulcerative colitis;

Liver failure;

dry mouth;

kidney failure;

Chronic lung diseases;

myasthenia;

Diseases that accompany obstruction of the urinary tract;

Down's disease, cerebral palsy, brain damage in children;

Synechia of the iris and age over 40 years - in ophthalmology.

Pregnancy and lactation are also a reason for the careful appointment of Atropine.

Additional Information

The shelf life of Atropine is 5 years, the manufacturer indicates the end date of use on the package. The drug should be stored in a dark place out of the reach of children.

Atropine sulfate

Atropine sulfate is an analogue of Atropine, in this regard, the characteristics of Atropine sulfate correspond to the characteristics of Atropine. Preparations Atropine sulfate and Atropine should be taken only as prescribed by a doctor and under his constant supervision.

Sincerely,