Atropine sulfate - description of the drug, instructions for use, reviews. Medicinal guide geotar Atropine dispensing from pharmacies

Atropine sulfate (atropine)

Composition and form of release of the drug

1 ml - ampoules (10) - packs of cardboard.

pharmachologic effect

Blocker of m-cholinergic receptors, is a natural tertiary amine. It is believed that it binds to the same extent with m 1 -, m 2 - and m 3 - subtypes of muscarinic receptors. It affects both central and peripheral m-cholinergic receptors.

Reduces the secretion of salivary, gastric, bronchial, sweat glands. Reduces smooth muscle tone internal organs(including bronchi, organs digestive system, urethra, Bladder), reduces gastrointestinal motility. Virtually no effect on the secretion of bile and pancreas. Causes mydriasis, accommodation paralysis, reduces the secretion of lacrimal fluid.

In average therapeutic doses, atropine has a moderate stimulating effect on the central nervous system and a delayed but prolonged sedative effect. The central anticholinergic effect explains the ability of atropine to eliminate tremor in Parkinson's disease. In toxic doses, atropine causes agitation, agitation, hallucinations, coma.

Atropine reduces the tone of the vagus nerve, which leads to an increase in heart rate (with a slight change in blood pressure), an increase in conductivity in the bundle of His.

In therapeutic doses, atropine does not have a significant effect on peripheral vessels, but vasodilation is observed with an overdose.

At topical application in ophthalmology, the maximum expansion of the pupil occurs after 30-40 minutes and disappears after 7-10 days. Mydriasis caused by atropine is not eliminated by the instillation of cholinomimetic drugs.

Pharmacokinetics

It is well absorbed from the gastrointestinal tract or through the conjunctival membrane. After systemic administration, it is widely distributed in the body. Penetrates through the BBB. A significant concentration in the central nervous system is achieved within 0.5-1 h. Moderate protein binding.

T 1/2 is 2 hours. Excreted in the urine; about 60% - unchanged, the rest - in the form of hydrolysis and conjugation products.

Indications

Systemic use: spasm of smooth muscle organs of the gastrointestinal tract, bile ducts, bronchi; peptic ulcer and duodenum, acute pancreatitis, hypersalivation (parkinsonism, poisoning with heavy metal salts, during dental interventions), irritable bowel syndrome, intestinal colic, renal colic, bronchitis with hypersecretion, bronchospasm, laryngospasm (prevention); premedication before surgical operations; AV blockade, bradycardia; poisoning with m-cholinomimetics and anticholinesterase substances (reversible and irreversible action); x-ray examination of the gastrointestinal tract (if necessary, reduce the tone of the stomach and intestines).

Topical application in ophthalmology: to study the fundus, to dilate the pupil and achieve accommodation paralysis in order to determine the true refraction of the eye; for the treatment of iritis, iridocyclitis, choroiditis, keratitis, embolism and spasm of the central retinal artery and some eye injuries.

Contraindications

Hypersensitivity to atropine.

Dosage

Inside - 300 mcg every 4-6 hours.

To eliminate bradycardia in / in adults - 0.5-1 mg, if necessary, after 5 minutes, the introduction can be repeated; children - 10 mcg / kg.

For the purpose of premedication in / m adults - 400-600 mcg 45-60 minutes before anesthesia; children - 10 mcg / kg 45-60 minutes before anesthesia.

When applied topically in ophthalmology, 1-2 drops of a 1% solution are instilled (in children, a solution of a lower concentration is used) into the diseased eye, the frequency of use is up to 3 times with an interval of 5-6 hours, depending on the indications. In some cases, a 0.1% solution is administered subconjunctivally 0.2-0.5 ml or parabulbarno - 0.3-0.5 ml. By electrophoresis, a 0.5% solution from the anode is injected through the eyelids or eye bath.

Side effects

With systemic use: dry mouth, tachycardia, constipation, difficulty urinating, mydriasis, photophobia, accommodation paralysis, dizziness, impaired tactile perception.

When applied topically in ophthalmology: hyperemia of the skin of the eyelids, hyperemia and edema of the conjunctiva of the eyelids and eyeball, photophobia, dry mouth, tachycardia.

drug interaction

With simultaneous ingestion with those containing aluminum or calcium carbonate, the absorption of atropine from the gastrointestinal tract decreases.

With simultaneous use with anticholinergic agents and agents with anticholinergic activity, the anticholinergic effect is enhanced.

With simultaneous use with atropine, it is possible to slow down the absorption of mexiletine, reduce the absorption of nitrofurantoin and its excretion by the kidneys. Probably increased therapeutic and side effects of nitrofurantoin.

With simultaneous use with phenylephrine, an increase in blood pressure is possible.

Under the influence of guanethidine, a decrease in the hyposecretory effect of atropine is possible.

Nitrates increase the likelihood of an increase intraocular pressure.

Procainamide enhances the anticholinergic effect of atropine.

Atropine reduces the concentration of levodopa in plasma.

special instructions

Use with caution in patients with medical conditions of cardio-vascular system in which an increase in heart rate may be undesirable: atrial fibrillation, tachycardia, chronic insufficiency, ischemic heart disease, mitral stenosis, arterial hypertension, acute bleeding; with thyrotoxicosis (possibly increased tachycardia); at elevated temperature (may still increase due to suppression of the activity of the sweat glands); with reflux esophagitis, hiatal hernia, combined with reflux esophagitis (decrease in motility of the esophagus and stomach and relaxation of the lower esophageal sphincter can slow gastric emptying and increase gastroesophageal reflux through the sphincter with impaired function); in diseases of the gastrointestinal tract, accompanied by obstruction - achalasia of the esophagus, pyloric stenosis (possible decrease in motility and tone, leading to obstruction and retention of stomach contents), intestinal atony in elderly patients or debilitated patients (obstruction may develop), paralytic ileus; with an increase in intraocular pressure - closed-angle (mydriatic effect, leading to an increase in intraocular pressure, can cause an acute attack) and open-angle glaucoma (mydriatic effect can cause some increase in intraocular pressure; therapy may need to be adjusted); with ulcerative colitis (high doses can inhibit intestinal motility, increasing the likelihood paralytic ileus intestines, in addition, the manifestation or exacerbation of such a severe complication as toxic megacolon is possible); with dry mouth (long-term use may cause a further increase in the severity of xerostomia); with liver failure (decreased metabolism) and kidney failure(risk of side effects due to reduced excretion); at chronic diseases lungs, especially in young children and debilitated patients (a decrease in bronchial secretion can lead to thickening of the secret and the formation of plugs in the bronchi); with myasthenia gravis (the condition may worsen due to inhibition of the action of acetylcholine); prostatic hypertrophy without obstruction urinary tract, urinary retention or a predisposition to it or diseases accompanied by obstruction of the urinary tract (including the bladder neck due to prostatic hypertrophy); with gestosis (possibly increased arterial hypertension); brain damage in children, cerebral palsy, Down's disease (the reaction to anticholinergics increases).

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

With subconjunctival or parabulbar administration of atropine, the patient should be given a tablet under the tongue to reduce tachycardia.

Influence on the ability to manage vehicles and mechanisms

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

Pregnancy and lactation

Atropine crosses the placental barrier. Adequate and strictly controlled clinical research The safety of atropine during pregnancy has not been evaluated.

With intravenous administration during pregnancy or shortly before childbirth, tachycardia in the fetus may develop.

Atropine is found in breast milk in trace concentrations.

Use with caution in liver failure (decreased metabolism).

Use in the elderly

Use with caution in patients with diseases of the cardiovascular system, in which an increase in heart rate may be undesirable; with intestinal atony in elderly or debilitated patients (obstruction is possible), with prostatic hypertrophy without urinary tract obstruction, urinary retention or a predisposition to it, or diseases accompanied by obstruction of the urinary tract (including the bladder neck due to prostatic hypertrophy glands).

Pharmacological.

The mechanism of action is due to the selective blockade of M-cholinergic receptors by atropine (to a lesser extent affects H-cholinergic receptors), as a result of which M-cholinergic receptors become insensitive to acetylcholine, which is formed in the region of the endings of postganglionic parasympathetic neurons. The ability of atropine to bind to cholinergic receptors is explained by the presence of a fragment in its molecule, which makes it related to the molecule of the endogenous ligand, acetylcholine. Atropine sulfate reduces the secretion of salivary, bronchial, gastric and sweat glands, increases the viscosity of bronchial secretions, inhibits the activity of cilia ciliated epithelium bronchi, thereby reducing mucociliary transport, accelerates heart contraction, increases AV conduction, reduces the tone of smooth muscle organs, reduces the amount and total acidity of gastric juice (especially with the predominance of cholinergic regulation of secretion), reduces basal and nocturnal secretion of gastric juice, to a lesser extent reduces stimulated secretion, Vira Eno dilates the pupil (in this case, an increase in intraocular pressure is possible). Penetrating through the blood-brain barrier, atropine in therapeutic doses excites the respiratory center.

Pharmacokinetics.

After intravenous administration The maximum effect appears after 2-4 minutes. Atropine sulfate is rapidly absorbed into the bloodstream from the injection site. It is rapidly distributed in the body, penetrates the blood-brain, placental barrier and into breast milk. In the blood, atropine is 50% protein bound, its volume of distribution is about 3 l/kg. After administration, the concentration of atropine in the blood plasma decreases in two stages. The first stage is fast - the half-life is 2:00. During this time, approximately 80% of the administered dose of atropine is excreted in the urine. The second stage - the rest of the drug is excreted in the urine - the half-life is 13-36 hours. Atropine is metabolized in the liver by enzymatic hydrolysis, approximately 50% of the dose is excreted by the kidneys unchanged.

Indications

As a symptomatic remedy for peptic ulcer of the stomach and duodenum, pylorospasm, acute pancreatitis, cholelithiasis, cholecystitis, spasms of the intestines, urinary tract, bronchial asthma, bradycardia, as a result of an increase in the tone of the vagus nerve, to reduce the secretion of salivary, gastric, bronchial, sometimes sweat glands, to conduct an x-ray examination of the digestive system (decrease in tone and motor activity of organs).

The drug is also used before anesthesia, surgery and during surgery as a means of preventing broncho and laryngospasms, reduces the secretion of glands, reflex reactions and side effects due to stimulation of the vagus nerve. As a specific antidote for poisoning with cholinomimetic compounds and anticholinesterase (including organophosphorus) substances.

Contraindications

Hypersensitivity to the components of the drug. Diseases of the cardiovascular system, in which an increase in heart rate may be undesirable: atrial fibrillation, tachycardia, chronic heart failure, ischemic disease heart, mitral stenosis, severe arterial hypertension. Acute bleeding. thyrotoxicosis. hyperthermia syndrome. Diseases of the digestive system, accompanied by obstruction (achalasia of the esophagus, pyloric stenosis, intestinal atony). Glaucoma. Liver and kidney failure. myasthenia gravis gravity. Urinary retention or predisposition to it. Brain damage.

Interaction with other medicinal products and other forms of interaction

When using atropine sulfate with MAO inhibitors, cardiac arrhythmias occur, with quinidine, novocainamide, a summation of the anticholinergic effect is observed. When taken orally together with preparations of lily of the valley, with tannin, a physical and chemical interaction is observed, which leads to a mutual weakening of the effects.

Atropine sulfate reduces the duration and depth of action of narcotic drugs, weakens the analgesic effect of opiates.

With simultaneous use with diphenhydramine or diprazine, the effect of atropine is enhanced, with nitrates, haloperidol, GCS for systemic use - the likelihood of an increase in intraocular pressure increases, with sertraline - the depressive effect of both drugs increases, with spironolactone, minoxidil - the effect of spironolactone and minoxidil decreases, with penicillins - the effect of both drugs is enhanced, with nizatidine - the effect of nizatidine is enhanced, ketoconazole - the absorption of ketoconazole decreases, with ascorbic acid and attapulgite - the effect of atropine decreases, with pilocarpine - the effect of pilocarpine in the treatment of glaucoma decreases, with oxprenolone - the antihypertensive effect of the drug decreases. Under the action of oktadine, it is possible to reduce the hyposecretory action of atropine, which weakens the action of M-cholinomimetics and anticholinesterase agents. When used simultaneously with sulfa drugs increases the risk of kidney damage, preparations containing potassium - the formation of intestinal ulcers is possible, with non-steroidal anti-inflammatory drugs - the risk of gastric ulcers and bleeding.

The action of atropine sulfate can be enhanced with the simultaneous use of other drugs with antimuscarinic effect (M-anticholinergics, antispasmodics, amantadine, some antihistamines, drugs of the group of butyrophenones, phenothiazines, dispiramides, quinidine, tricyclic antidepressants, non-selective monoamine reuptake inhibitors). Inhibition of peristalsis by atropine may alter the absorption of other drugs.

Application features

Use with caution in patients with prostatic hypertrophy without urinary tract obstruction, with Down's disease, with cerebral palsy, reflux esophagitis, hiatal hernia, combined with reflux esophagitis, ulcerative colitis, megacolon, patients with xerostomia, elderly patients or debilitated patients, with chronic lung diseases without reversible obstruction, with chronic lung diseases that occur with low production of thick sputum, which is difficult to separate, especially in young children and debilitated patients, with autonomic (autonomous) neuropathy.

Use during pregnancy or lactation

The drug is contraindicated during pregnancy.

The use of atropine sulfate during breastfeeding is contraindicated due to the risk of developing toxic effects on the child.

The ability to influence the reaction rate when driving vehicles or operating other mechanisms

Considering the possibility of such adverse reactions, as dizziness, hallucinations, disturbance of accommodation, when using the drug, you should refrain from driving vehicles or other mechanisms.

Dosage and administration

Atropine sulfate is administered subcutaneously, intramuscularly, intravenously. With induction anesthesia in order to reduce the risk of vagus suppression of the heart rate and reduce the secretion of the salivary and bronchial glands - 0.3-0.6 mg under the skin or 30-60 minutes before anesthesia in combination with morphine (10 mg of morphine sulfate) - 1:00 before anesthesia. In case of poisoning with anticholinesterase drugs, atropine sulfate is administered intramuscularly at a dose of 2 mg every 20-30 minutes until redness and dryness of the skin, dilated pupils and the appearance of tachycardia, and normalization of breathing occur. In moderate and severe poisoning, atropine can be administered for two days (until signs of "reatropinization" appear).

For children, the highest single dose is:

• up to 6 months - 0.02 mg
• aged 6 months to 1 year - 0.05 mg
• at the age of 1 to 2 years - 0.2 mg
• at the age of 3 to 4 years - 0.25 mg
• at the age of 5 to 6 years - 0.3 mg
• at the age of 7 to 9 years - 0.4 mg
• at the age of 10 to 14 years - 0.5 mg.

Higher doses for adults subcutaneously: single - 1 mg, daily - 3 mg.

Adverse reactions

Side effect The drug is associated mainly with the M-anticholinergic effect of atropine.

From the digestive system: dry mouth, thirst, impaired taste sensations, dysphagia, decreased intestinal motility to atony, decreased tone of the biliary tract and gallbladder.

From the urinary system: difficulty and urinary retention.

From the side of the cardiovascular system: tachycardia, arrhythmia, including extrasystole, myocardial ischemia, facial flushing, sensation of hot flashes.

From the nervous system: headache, dizziness, nervousness, insomnia.

From the side of the organ of vision: dilated pupils, photophobia, accommodation paralysis, increased intraocular pressure, visual impairment.

From the side respiratory system: decrease in secretory activity and tone of the bronchi, which leads to the formation of viscous sputum, hard to cough.

From the side of the skin: rash, urticaria, exfoliative dermatitis.

Manufacturer

LLC "Kharkovskoe pharmaceutical company"Health of the people".

Pharmacodynamics.
Atropine sulfate - blocker of m-cholinergic receptors, binds to m1 -, m2 - and m3 - subtypes of muscarinic receptors. Affects both central and peripheral m-cholinergic receptors. To a lesser extent, it affects n-cholinergic receptors. It dilates the pupil, impedes the outflow of intraocular fluid, increases intraocular pressure, causes accommodation paralysis. The pupil, dilated with atropine, does not narrow during the instillation of cholinomimetic agents. The maximum mydriasis occurs in 30-40 minutes and persists for 7-10 days.
The systemic effect of atropine is due to the blockade of choline receptors and includes inhibition of the secretion of salivary, gastric, bronchial, sweat glands, pancreas, increased heart rate, decreased tone of smooth muscle organs (bronchial tree, abdominal organs, etc.).
Penetrating through the blood-brain barrier, atropine affects the central nervous system, in toxic doses causes motor and mental disorders, convulsions, hallucinatory phenomena, respiratory paralysis.
Pharmacokinetics
Atopine sulfate is well absorbed through the conjunctiva, as well as in gastrointestinal tract when swallowing eye drops that have entered the nasopharynx through the lacrimal canal. Atropine has a volume of distribution of 1-6 l / kg, 50% binds to plasma proteins. Plasma clearance is 8 ml / min / kg. Atropine crosses the blood-brain barrier and the placenta; traces of atropine are determined in breast milk. Metabolized in the liver, excreted by the kidneys unchanged (30-50%) and as metabolites.

Indications for use

Locally in ophthalmology: used as a mydriatic and cycloplegic agent for diagnostic or therapeutic purposes, for cycloplegia and mydriasis as part of complex therapy inflammatory diseases iris and uveal tract.

Dosage and administration

Assign 1 drop per conjunctival sac, pupillary dilation develops after 40 minutes. If necessary, it is possible to prescribe 1 drop into the conjunctival sac 2 times a day with an interval between doses of at least 5-6 hours. The dosage regimen and duration of use are determined by the doctor.

Side effect

local action: hyperemia of the skin of the eyelids, hyperemia and edema of the conjunctiva, eyelids and eyeball, photophobia, mydriasis, accommodation paralysis, increased intraocular pressure.
Systemic action: dry mouth, tachycardia, nausea, vomiting, intestinal atony, constipation, urinary retention, bladder atony, headache, dizziness, agitation, confusion, hallucinations, ataxia, impaired tactile perception, decreased bronchial secretion.
Allergic reactions may develop, including skin rash, contact dermatitis, anaphylactic shock.
In the event of adverse reactions, including those not listed in the instructions for use, it is necessary to stop using the drug and consult a doctor.

Contraindications

Hypersensitivity to atropine sulfate and excipients. Angle-closure glaucoma and patients with risk factors for angle-closure glaucoma. Anterior and posterior synechiae, keratoconus. Childhood up to 7 years old.

Carefully

Arrhythmias, chronic heart failure, ischemic heart disease, mitral stenosis, reflux esophagitis, hepatic and / or renal failure, severe urinary retention with prostatic hyperplasia, intestinal atony, obstructive bowel disease, paralytic ileus, toxic megacolon, ulcerative colitis, hiatal hernia apertures of the diaphragm, hyperthermia, arterial hypertension, hyperthyroidism, age over 40 years (risk of undiagnosed glaucoma), myasthenia gravis.

Overdose

In case of an overdose, systemic anticholinergic effects may develop: cardiovascular disorders, disorders of the central nervous system and other disorders (see section "Side effects").
Treatment is symptomatic.

Precautionary measures

Wash your hands before and after instilling the drug. Do not touch the dropper to the eyelids or any other surface. Before instillation of eye drops, it is necessary to tilt your head back, pull the lower eyelid down, look up. After instillation of eye drops, it is recommended to close the eye and lightly press a finger into the projection area of ​​the lacrimal sac at the inner corner of the eye for 1-2 minutes. When the drug is introduced into the conjunctival sac in the form of drops, it is necessary to compress the area of ​​the lacrimal ducts in order to avoid the solution entering the lacrimal canal and being absorbed. In ophthalmic practice, Atropine sulfate should be used primarily with therapeutic purpose, and with diagnostic - it is better to use mydriatics of less prolonged action.
The drug is limited to use at elevated body temperature (possible decrease in the activity of sweat glands), children with brain damage, cerebral palsy, patients with Down's syndrome (the reaction to m-anticholinergics increases).
Pupil dilation can provoke an acute attack of glaucoma in patients with risk factors for glaucoma, persons over 60 years of age, hyperopic patients who are predisposed to glaucoma due to the fact that they have a shallow anterior chamber.
Patients should be warned about the decrease in visual acuity after instillation of eye drops, as well as photophobia and the need to protect the eyes from bright light.
Application Data contact lenses during the use of Atropine sulfate are absent.

Pregnancy and lactation

The safety of use during pregnancy and lactation has not been established. Prescribing a drug during pregnancy and lactation is possible only according to absolute indications, if the doctor has determined that the expected benefit to the mother outweighs the potential risk to the fetus / child.

Pediatrics

For children under 7 years of age, atropine sulfate is prescribed in lower concentrations (0.125%, 0.25%, 0.5%).

The ability to influence the reaction rate when driving vehicles or working with other mechanisms

During the period of treatment, one should refrain from driving vehicles and engaging in other potentially hazardous activities that require increased concentration of attention, speed of psychomotor reactions and clarity of vision.

A warning

And other additional components, depending on the release form.

Release form

Atropine sulfate is produced in the form of an injection solution, packed in 1 ml ampoules, and eye drops in 5 ml dropper bottles.

pharmachologic effect

The drug is characterized mydriatic And antispasmodic action, as well as the ability to block M-cholinergic receptors.

Pharmacodynamics and pharmacokinetics

The main pharmacological property of atropine is that it is able to fully block M-cholinergic receptors. A slightly weaker substance can also act on H-cholinergic receptors. Therefore, it is considered a non-selective blocker of M-cholinergic receptors.

After the introduction of atropine into the body, there is a decrease in the secretion of salivary, bronchial, gastric, sweat and pancreas, heart contractions become more frequent, and the tone of smooth muscle organs decreases. The strongest effect of atropine is manifested with a high tone of the vagus nerve, but in any case, its mechanism of action is quite complex.

The use of atropine leads to a strong expansion of the pupils, depending on the degree of relaxation of the fibers of the circular muscle in the region of the iris innervated by parasympathetic fibers. Along with the expansion of the pupil due to a violation of the outflow of fluid from the chamber, intraocular pressure may increase. At the same time, relaxation of the ciliary muscles of the ciliary body of the eye leads to paralysis of accommodation, which is a violation of visual perception.

Indications for use

The main indications for the appointment of Atropine sulfate are:

• pylorospasms;
• the need to reduce the secretion of the salivary, gastric and bronchial glands;
• bradycardia;
• spasms of the intestines and urinary tract;
• pain caused by spasms of smooth muscles, as part of complex therapy.

Also, atropine can be used in anesthetic practice before anesthesia and surgery, which helps prevent the development of bronchospasm and laryngospasm, limit the secretion of the salivary and bronchial glands, reduce other reflex reactions and adverse events caused by excitation of the vagus nerve, and so on.

In ophthalmology, atropine is used when it is necessary to dilate the pupil for a diagnostic examination of the eye, to identify true refraction, and other things. In addition, the drug is used to treat:

• irita - inflammation of the iris of the eyes;
• - simultaneous inflammation of the iris and cornea of ​​​​the eyes;
• - inflammation of the cornea and some eye injuries.

Due to the relaxation of the muscles of the eye, functional rest is ensured and the elimination of a number of pathologies is accelerated.

Contraindications

• - increased intraocular pressure;
• severe urinary incontinence .

Side effects

When using Atropine sulfate, dry mouth, dilated pupils, , violation of accommodation, and urinary problems.

Instructions for Atropine sulfate (Method and dosage)

According to the instructions for use of Atropine sulfate, the drug can be used different ways: taken orally, parenterally and topically. Quite often it is administered by injection: by injection into a vein, muscle or under the skin. In this case, the dosage of the drug is set by the attending physician, taking into account the type, complexity of the disease and the characteristics of the patient's body.

In ophthalmic practice, eye drops concentration 0.5-0.1% active ingredient. Therapeutic dosage is 1-2 drops to instillation 2-6 times a day. Particularly severe cases are supplemented by laying 1% atropine ointment on the eyelids in the evenings.

Overdose

In case of overdose, severe dryness may occur in oral cavity, burning sensation, difficulty swallowing, severe photophobia, redness and peeling skin, fever, rash, nausea, vomiting, tachycardia and arterial hypertension.

The drug can have effects on the nervous system, with anxiety, confusion, agitation, and delirium often developing, as well as excessive and stupor. Such conditions often end in death, which can lead to cardiovascular or respiratory failure.

In especially severe cases, the introduction is recommended, prescribe . All this time it is necessary to constantly monitor the patency respiratory tract. Inhalation with oxygen or carbon dioxide will help prevent the development of respiratory failure.

Simultaneous use with antacids, which contain Al3 + or Ca2 +, leads to a decrease in the absorption of the active ingredient from the gastrointestinal tract. Combination with tricyclic antidepressants, , Phenothiazine, Quinidine , antihistamines and other drugs with m-anticholinergic properties often increase the manifestation of systemic undesirable effects. Some nitrates cause an increase in intraocular pressure, while atropine sometimes changes absorption

**** Veropharm, JSC Dalchimpharm OJSC MOSCOW End Z-d Moscow endocrine plant

Country of origin

Russia Ukraine

Product group

Digestive tract and metabolism

Anticholinergic medicines

Release form

• 10 ampoules of 1 ml in a carton pack 10 ampoules of 1 ml

Description of the dosage form

• Colorless clear liquid. Injection

pharmachologic effect

An alkaloid contained in plants of the nightshade family, a blocker of M-cholinergic receptors, binds equally to the m1-, m2- and m3-subtypes of muscarinic receptors. It affects both central and peripheral M-cholinergic receptors. It also acts (although much weaker) on n-cholinergic receptors. Interferes with the stimulating action of acetylcholine; reduces the secretion of salivary, gastric, bronchial, lacrimal, sweat glands, pancreas. Reduces the tone of the muscles of internal organs (bronchi, gastrointestinal tract, bile ducts and gallbladder, urethra, bladder); causes tachycardia, improves AV conduction. Reduces the motility of the gastrointestinal tract, practically does not affect the secretion of bile. It dilates the pupils, impedes the outflow of intraocular fluid, increases intraocular pressure, causes accommodation paralysis. In average therapeutic doses, it has a stimulating effect on the central nervous system and a delayed, but prolonged sedative effect; excites respiration (large doses - respiratory paralysis). It excites the cerebral cortex (in high doses), in toxic doses causes agitation, agitation, hallucinations, coma. Reduces the tone of the vagus nerve, which leads to an increase in heart rate (with a slight change in blood pressure) and a slight increase in conductivity in the bundle of His. The action is more pronounced with an initially increased tone of the vagus nerve. After intravenous administration, the maximum effect appears after 2-4 minutes, after oral intake(in the form of drops) - after 30 minutes.

Pharmacokinetics

After intravenous administration, the maximum effect appears after 2-4 minutes, after oral administration (in the form of drops) - after 30 minutes. Passes through the BBB. In the blood, atropine is 50% protein bound, its volume of distribution is about 3 l/kg. After intravenous administration, the concentration of atropine in the blood plasma decreases in 2 stages. The first is fast, characterized by a half-life of 2 hours. During this time, about 80% of the administered dose of atropine is excreted in the urine. The rest of it is excreted in the urine with a half-life of 13-36 hours. Atropine is metabolized in the liver, about 50% of the dose is excreted by the kidneys unchanged.

Special conditions

Use with caution in patients with diseases of the cardiovascular system, in which an increase in heart rate may be undesirable: atrial fibrillation, tachycardia, chronic heart failure, ischemic heart disease, mitral stenosis, arterial hypertension, acute bleeding; with thyrotoxicosis (possibly increased tachycardia); at elevated temperature (may still increase due to suppression of the activity of the sweat glands); with reflux esophagitis, hiatal hernia, combined with reflux esophagitis (decrease in motility of the esophagus and stomach and relaxation of the lower esophageal sphincter can slow gastric emptying and increase gastroesophageal reflux through the sphincter with impaired function); in diseases of the gastrointestinal tract, accompanied by obstruction - achalasia of the esophagus, pyloric stenosis (possible decrease in motility and tone, leading to obstruction and retention of stomach contents), intestinal atony in elderly patients or debilitated patients (obstruction may develop), paralytic ileus; with an increase in intraocular pressure - closed-angle (mydriatic effect, leading to an increase in intraocular pressure, can cause an acute attack) and open-angle glaucoma (mydriatic effect can cause some increase in intraocular pressure; therapy may need to be adjusted); with nonspecific ulcerative colitis (high doses can inhibit intestinal motility, increasing the likelihood of paralytic ileus, in addition, the manifestation or exacerbation of such a severe complication as toxic megacolon is possible); with dry mouth (long-term use may cause a further increase in the severity of xerostomia); with liver failure (decreased metabolism) and renal failure (risk of side effects due to reduced excretion); in chronic lung diseases, especially in young children and debilitated patients (a decrease in bronchial secretion can lead to thickening of secretions and the formation of plugs in the bronchi); with myasthenia gravis (the condition may worsen due to inhibition of the action of acetylcholine); prostatic hypertrophy without urinary tract obstruction, urinary retention or a predisposition to it, or diseases accompanied by urinary tract obstruction (including the bladder neck due to prostatic hypertrophy); with gestosis (possibly increased arterial hypertension); brain damage in children, cerebral palsy, Down's disease (the reaction to anticholinergics increases). Between taking atropine and antacids containing aluminum or calcium carbonate, the interval should be at least 1 hour. With subconjunctival or parabulbar administration of atropine, the patient should be given a validol tablet under the tongue to reduce tachycardia. Influence on the ability to drive vehicles and control mechanisms

Composition

• atropine sulfate 1 mg; excipients: 0.1 M hydrochloric acid, water for injection 1 ml of solution contains 1 mg or 0.5 mg of atropine sulfate. Excipients: hydrochloric acid, water for injection.

Atropine sulfate indications for use

• As symptomatic remedy, with peptic ulcer of the stomach and duodenum, pylorospasm, acute pancreatitis, cholelithiasis, cholecystitis, spasms of the intestines, urinary tract, bronchial asthma, bradycardia as a result of an increase in the tone of the vagus nerve, to reduce the secretion of salivary, gastric, bronchial, and sometimes sweat glands, for X-ray examination of the digestive tract (decrease in tone and motor activity of organs). The drug is also used before anesthesia and surgery and during surgery as a remedy that prevents broncho- and laryngospasms, reduces glandular secretion, reflex reactions and side effects caused by excitation of the vagus nerve. In addition, Atropine sulfate is a specific antidote for poisoning with cholinomimetic compounds and anticholinesterase (including organophosphorus) substances.

Atropine sulfate contraindications

• Hypersensitivity to the drug. Glaucoma, organic lesions of the heart and blood vessels, prostate hypertrophy, kidney disease, exhaustion of the body. Pregnancy and lactation. With caution appoint it to the elderly.

Atropine sulfate dosage

• 0.1% 1 mg/ml

Atropine sulfate side effects

• The side effect of the drug is mainly due to the m-anticholinergic effect of atropine. In large doses, the drug can lead to respiratory paralysis, cause severe anxiety, mental and motor agitation, dizziness, convulsions, hallucinations, disturbance of accommodation up to paralysis, a pronounced increase in intraocular pressure; dry mouth, palpitations (tachycardia), difficulty urinating, intestinal atony; violation of heat transfer, a decrease in sweating, which is of particular importance for the elimination of hyperthermia.

drug interaction

Weakens the action of m-cholinomimetics and anticholinesterase agents. Diphenhydramine or promethazine - enhancing the action of atropine. Nitrates increase the likelihood of increased intraocular pressure. Procainamide - increased anticholinergic action. Under the influence of guanethidine, a decrease in the hyposecretory effect of atropine is possible.

Overdose

Symptoms. Dryness of the mucous membrane of the oral cavity and nasopharynx, impaired swallowing and speech, dry skin, hyperthermia, mydriasis, etc. (see section "Side effect); motor and speech excitement, memory impairment, hallucinations, psychosis. Treatment. Anticholinesterase and sedatives.

Storage conditions

• keep away from children
• store in a place protected from light

Information provided