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And other additional components, depending on the form of release.

Release form

Atropine sulfate is available in the form of a solution for injection, packaged in 1 ml ampoules, and eye drops in 5 ml dropper bottles.

pharmachologic effect

The drug is characterized by 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. The substance can also have a somewhat weaker effect on H-cholinergic receptors. Therefore, it is considered a non-selective M-cholinergic receptor blocker.

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 effect of atropine is strongest when the tone of the vagus nerve is high, but in any case its mechanism of action is quite complex.

The use of atropine leads to a strong dilation of the pupils, depending on the degree of relaxation of the fibers of the orbicularis muscle in the area of ​​the iris, innervated by parasympathetic fibers. Along with the dilation of the pupil, intraocular pressure may increase due to impaired outflow of fluid from the chamber. In this case, 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 use 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.

Atropine can also be used in anesthesiological practice before anesthesia and surgery, which helps prevent the development of broncho- and laryngospasms, 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 to conduct a diagnostic examination of the eye, determine true refraction, and so on. In addition, the drug is used to treat:

• iritis – inflammation of the iris;
• – simultaneous inflammation of the iris and cornea of ​​the eyes;
• – inflammation of the cornea and some eye injuries.

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

Contraindications

• – increased intraocular pressure;
• severe urination problems with .

Side effects

When using Atropine sulfate, dry mouth, dilated pupils, , disturbance of accommodation, and problems with urination.

Instructions for Atropine sulfate (Method and dosage)

According to the instructions for use of Atropine sulfate, the drug can be used in different ways: taken orally, parenterally and locally. 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 established 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 with a concentration of 0.5-0.1% of the active substance are used. The therapeutic dosage is 1-2 drops instilled 2-6 times a day. Particularly severe cases are supplemented by applying 1% atropine ointment to the eyelids in the evenings.

Overdose

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

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

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

Simultaneous use with antacids that contain Al3+ or Ca2+ leads to a decrease in the absorption of the active component 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 alters absorption

Atropine sulfate (Atropini sulfas)

pharmachologic effect

The main pharmacological feature of atropine sulfate is its ability to block M-cholinergic receptors; it also acts (albeit much weaker) on H-cholinergic receptors. Thus, atropine sulfate is a non-selective blocker 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, increased heart rate (due to a decrease in the inhibitory effect of the vagus nerve on the heart), and a decrease in the tone of smooth muscle organs (bronchi, abdominal organs, etc.). The effect of atropine is more pronounced with increased tone of the vagus nerve.
Under the influence of atropine, the pupils are greatly dilated. The mydriatic effect (pupil dilation) depends on the relaxation of the fibers of the circular muscle of the iris, which is innervated by parasympathetic fibers. Simultaneously with the dilation 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 gastric and duodenal ulcers, pylorospasm (spasm of the muscles of the pylorus), cholelithiasis, spasms of the intestines and urinary tract, bronchial asthma, to reduce the secretion of the salivary, gastric and bronchial glands, for bradycardia (rare pulse) that has developed in as a result of increased tone of the vagus nerve.
For pain associated with smooth muscle spasms, atropine is often administered together with analgesics (painkillers) (analgin, promedol, morphine, etc., 256, 255).
In anesthesiological 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 for X-ray examination of the gastrointestinal tract if necessary to reduce the tone and motor activity of the stomach and intestines.
Due to its ability to reduce the secretion of sweat glands, atropine is sometimes used to treat excessive sweating.
Atropine is an effective antidote (antidote) for poisoning with cholinomimetic and anticholinesterase substances, including FOS (organophosphorus substances); used for 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 of the eye, determine true refraction, etc.), as well as for therapeutic purposes in acute diseases: 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 eye muscles caused by atropine promotes its functional rest and accelerates the elimination of the pathological process.

Mode of application

Atropine is used orally (before meals), parenterally (bypassing the digestive tract) and topically (in the form of eye drops). Orally prescribed for adults in powders, tablets and solutions (0.1%) at 0.00025 g (0.25 mg) - 0.0005 g (0.5 mg) - 0.001 g (1 mg) per dose 1-2 times in a day. 0.00025-0.0005-0.001 g (0.25-0.5-1 ml of 0.1% solution) is injected intramuscularly and intravenously under the skin.
Depending on age, children are prescribed 0.00005 g (0.05 mg) - 0.0005 g (0.5 mg) per dose.
In the case of using atropine for the treatment of gastric and duodenal ulcers, the drug is prescribed orally, selecting the dose individually (usually until mild dry mouth appears). Depending on sensitivity to atropine, the dose may correspond to 6-8-10-12-15 drops of a 0.1% solution taken 2-3 times a day. Prescribed 30-40 minutes before meals or an hour after meals. In cases of exacerbation of the disease, atropine is first administered in the form of subcutaneous injections.
In ophthalmic practice, 0.5-0.1% solutions (eye drops) are used. For therapeutic purposes, 1-2 drops are prescribed 2-6 times a day. In severe cases, apply 1% atropine ointment behind the edges of the eyelids in the evening. Atropine eye drops are also used.
For medicinal purposes, it is advisable to use atropine as a long-acting mydriatic (pupil dilating) agent; For diagnostic purposes, it is more advisable to use shorter-acting mydriatic drugs. Atropine causes maximum pupil dilation 30-40 minutes after installation (instillation); the effect lasts up to 7-10 days. Paralysis of accommodation (impaired visual perception) occurs within 1-3 hours and lasts up to 8-12 days. At the same time, homatropine causes maximum mydriasis after 40-60 minutes; The mydriatic effect and paralysis of accommodation last 1-2 days. The mydriatic effect when using platyphylline 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.
For bronchospasms (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 effects

Dry mouth, dilated pupils, impaired accommodation (impaired visual perception), atony (loss of tone) of the intestines, dizziness, tachycardia (rapid heartbeat), difficulty urinating. Attention!
Description of the drug " Atropine sulfate"on this page is a simplified and expanded version of the official instructions for use. Before purchasing or using the drug, you should consult your doctor and read the instructions approved by the manufacturer.
Information about the drug is provided for informational purposes only and should not be used as a guide to self-medication. Only a doctor can decide to prescribe the drug, as well as determine the dose and methods of its use.

Atropine sulfate

International nonproprietary name

Dosage form

Solution for injection 1mg/ml, 1ml

Compound

1 ml of solution contains

active substance - atropine sulfate 1.0 mg,

Excipients: 0.1 M hydrochloric acid, water for injection.

Description

Transparent colorless liquid

Pharmacotherapeutic group

Preparations for the treatment of functional intestinal disorders. Belladonna and its derivatives. Belladonna alkaloids, tertiary amines. Atropine.

ATX code A03B A01

Pharmacological properties

Pharmacokinetics

When administered intravenously, the maximum effect appears after 2-4 minutes. 18% binds to blood plasma proteins. Metabolized in the liver. Passes through the blood-brain barrier and is found in breast milk in trace amounts. Excreted by the kidneys, 50% of the dose unchanged.

Pharmacodynamics

Anticholinergic agent. Belladonna alkaloid, blocks m-cholinergic receptors of smooth muscles, cardiac muscle, sinoatrial and atrioventricular nodes, endocrine glands and the central nervous system.

Has anticholinergic dose-dependent effects:

In smaller doses - inhibits the secretion of the salivary and bronchial glands, sweating, accommodation of the eye, dilates the pupil, increases intraocular pressure and heart rate;

In large doses, it reduces the contractility of the gastrointestinal tract (including the biliary tract and bladder), urinary tract and bronchial smooth muscles, suppresses gastric secretion, and stimulates the central nervous system.

Thanks to its central anticholinergic effect, it can eliminate tremor in Parkinson's disease. In toxic doses it causes agitation, agitation, hallucinations, and coma. Atropine reduces the tone of the vagus nerve, which leads to an increase in heart rate with a slight change in blood pressure and to an increase in conductivity in the His bundle. In therapeutic doses it does not have a significant effect on peripheral vessels; in case of overdose, vasodilation is observed. It is an effective antidote for poisoning with cholinomimetic and anticholinesterase substances.

Indications for use

For gastric and duodenal ulcers, intestinal spasms, acute pancreatitis, for X-ray examination of the gastrointestinal tract (decreased tone and motor activity of organs)

Pylorospasm

Gallstone disease, cholecystitis

Bronchial asthma

Bradycardia as a consequence of increased vagal tone

Decreased secretion of salivary, gastric, bronchial, and sometimes sweat glands.

The drug is also used before anesthesia and surgery and during surgery as a means that prevents broncho- and laryngospasms, reduces glandular secretion, reflex reactions and side effects caused by stimulation of the vagus nerve. In addition, Atropine sulfate is a specific antidote for poisoning with cholinomimetic compounds and anticholinesterase (including organophosphorus) substances.

Directions for use and doses

Atropine sulfate is administered subcutaneously, intramuscularly, intravenously, orally. In case of poisoning with cholinomimetics and anticholinesterase substances, a 0.1% solution of Atropine sulfate is administered intravenously, guided by antidote treatment regimens for these intoxications, taking into account the use of atropine together with cholinesterase reactivators.

Orally, adults are prescribed the drug 4-13 drops of a 0.1% solution 1-2 times a day before meals or 1 hour after it. 0.5-1 ml of a 0.1% solution is administered subcutaneously, intramuscularly and intravenously.

Higher doses for adults orally and subcutaneously: single - 0.001 g, daily - 0.003 g. Children in the first 3 months of life are especially sensitive to atropine. Atropine is prescribed to children in the following single doses per 1 kg of body weight: newborns and infants - 0.018 mg (0.018 ml of 0.1% solution); from 1 to 5 years - 0.016 mg (0.016 ml of 0.1% solution); from 6 to 10 years - 0.014 mg (0.014 ml of 0.1% solution); from 11 to 14 years - 0.012 mg (0.012 ml of 0.1% solution). The duration of the course of treatment is determined by the doctor.

Side effects

Often

Dry mouth, nose and/or skin

Decreased sweating

Mydriasis, paralysis of accommodation

Tachycardia

Atony of the intestines and urinary tract, constipation

Headache, dizziness, mental and motor agitation, memory loss (in elderly patients)

Rarely

Allergic reactions

Orthostatic hypotension

Increased eye pressure

Difficulty urinating, urinary retention

Drowsiness

Nausea, vomiting

Impaired tactile perception

Hallucinations

Contraindications

hypersensitivity

angle-closure glaucoma (mydriatic effect, leading to increased intraocular pressure, can cause an acute attack)

tachyarrhythmias

severe congestive heart failure

cardiac ischemia

mitral stenosis

reflux esophagitis

hiatal hernia

pyloric stenosis (possibly decreased motility and tone, leading to obstruction and retention of gastric contents)

liver failure

renal failure

intestinal atony

obstructive bowel disease

paralytic ileus

toxic megacolon

nonspecific ulcerative colitis

xerostomia (long-term use may cause further reduction in salivation)

myasthenia gravis (condition may worsen due to inhibition of acetylcholine action)

urinary retention or predisposition to it, or diseases,

accompanied by obstruction of the urinary tract (including the bladder neck due to prostatic hypertrophy)

Down's disease

cerebral palsy (response to anticholinergics increases)

period of pregnancy and lactation.

Drug interactions

When using Atropine sulfate with monoamine oxidase inhibitors, cardiac arrhythmias occur; with quinidine, novocainamide, a summation of the anticholinergic effect is observed. When taken orally together with lily of the valley preparations, a physicochemical interaction is observed with tannin, which leads to a mutual weakening of the effects.

special instructions

For pain caused by smooth muscle spasm, the drug is often administered with analgesics (promedol, morphine, analgin, etc.). With extreme caution, the drug is prescribed to patients with severe hyperthermia, open-angle glaucoma, chronic heart failure, arterial hypertension, chronic pulmonary disease, acute blood loss, hyperthyroidism, and old age.

Features of the effect of the drug on the ability to drive a vehicle or potentially dangerous mechanisms

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

Overdose

In cases of overdose, the most pronounced side effect occurs.

Treatment: symptomatic.

Release form and packaging

1 ml of the drug is placed in glass ampoules.

10 ampoules, along with instructions for medical use in the state and Russian languages ​​and a scarifier or ceramic cutting disc, are placed in a cardboard pack.

A drug Atropine sulfate reduces the secretion of salivary and other glands, causes tachycardia, improves atrioventricular conduction, reduces the tone of smooth muscle organs, significantly dilates the pupils (with a possible increase in intraocular pressure), causes paralysis of accommodation. The mechanism of action is due to the selective blockade of atropine-cholinergic receptors (to a lesser extent affects n-cholinergic receptors), as a result of which the latter become insensitive to acetylcholine, which is formed in the area of ​​​​the endings of postganglionic parasympathetic nerves. Maximum mydriasis occurs after 30 - 40 minutes and persists for 7 - 10 days , paralysis of accommodation, respectively, after 1 - 3 hours and persists for 8 - 12 days.
The systemic effect of atropine is due to its anticholinergic (cholinolytic) effect and includes inhibition of the secretion of salivary, gastric, bronchial, sweat glands, pancreas, increased heart rate (the inhibitory effect of the n.vagus on the heart decreases), decreased tone of smooth muscle organs (bronchial tree, abdominal organs and etc.).
Penetrating the blood-brain barrier, atropine affects the central nervous system. The drug reduces muscle tone and tremor in patients with parkinsonism (central anticholinergic effect); in therapeutic doses, atropine stimulates the respiratory center; large doses of atropine cause motor and mental disorders, convulsions, hallucinatory phenomena, and respiratory paralysis.

Indications for use

Apply Atropine sulfate with 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) developed as a result of increased vagus nerve tone.
For pain associated with smooth muscle spasms, atropine is often administered together with analgesics (painkillers) (analgin, promedol, morphine, etc., 256, 255).
In anesthesiological 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 for X-ray examination of the gastrointestinal tract if necessary to reduce the tone and motor activity of the stomach and intestines.
Due to its ability to reduce the secretion of sweat glands, atropine is sometimes used to treat excessive sweating.
Atropine is an effective antidote (antidote) for poisoning with cholinomimetic and anticholinesterase substances, including FOS (organophosphorus substances); used for 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 of the eye, determine true refraction, etc.), as well as for therapeutic purposes in acute diseases: 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 eye muscles caused by atropine promotes its functional rest and accelerates the elimination of the pathological process.

Mode of application

Apply Atropine sulfate orally (before meals), parenterally (bypassing the digestive tract) and locally (in the form of eye drops). Orally prescribed for adults in powders, tablets and solutions (0.1%) at 0.00025 g (0.25 mg) - 0.0005 g (0.5 mg) - 0.001 g (1 mg) per dose 1-2 times in a day. 0.00025-0.0005-0.001 g (0.25-0.5-1 ml of 0.1% solution) is injected intramuscularly and intravenously under the skin.
Depending on age, children are prescribed 0.00005 g (0.05 mg) - 0.0005 g (0.5 mg) per dose.
In the case of using atropine for the treatment of gastric and duodenal ulcers, the drug is prescribed orally, selecting the dose individually (usually until mild dry mouth appears). Depending on sensitivity to atropine, the dose may correspond to 6-8-10-12-15 drops of a 0.1% solution taken 2-3 times a day. Prescribed 30-40 minutes before meals or an hour after meals. In cases of exacerbation of the disease, atropine is first administered in the form of subcutaneous injections.
In ophthalmic practice, 0.5-0.1% solutions (eye drops) are used. For therapeutic purposes, 1-2 drops are prescribed 2-6 times a day. In severe cases, apply 1% atropine ointment behind the edges of the eyelids in the evening. Atropine eye drops are also used.
For medicinal purposes, it is advisable to use atropine as a long-acting mydriatic (pupil dilating) agent; For diagnostic purposes, it is more advisable to use shorter-acting mydriatic drugs. Atropine causes maximum pupil dilation 30-40 minutes after installation (instillation); the effect lasts up to 7-10 days. Paralysis of accommodation (impaired visual perception) occurs within 1-3 hours and lasts up to 8-12 days. At the same time, homatropine causes maximum mydriasis after 40-60 minutes; The mydriatic effect and paralysis of accommodation last 1-2 days. The mydriatic effect when using platyphylline 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.
For bronchospasms (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 effects

Of the side effects from using the drug Atropine sulfate may occur: dry mouth, dilated pupils, impaired accommodation (impaired visual perception), atony (loss of tone) of the intestines, dizziness, tachycardia (rapid heartbeat), difficulty urinating.

Contraindications

:
Contraindications to the use of the drug Atropine sulfate are: glaucoma (increased intraocular pressure), severe urination disorders due to adenoma (benign tumor) of the prostate gland.

Pregnancy

:
During pregnancy the drug Atropine sulfate prescribed only in case of emergency. When using atropine during lactation, you should stop breastfeeding, as the drug passes into breast milk and can cause respiratory depression and drowsiness in the child.

Interaction with other drugs

When using Atropine sulfate with monoamine oxidase inhibitors, heart rhythm disturbances occur; with quinine, novocainamide, a summation of the anticholinergic effect is observed.

Overdose

:
In case of drug overdose Atropine sulfate it is possible to increase the side effects and development of systemic effects of atropine: tachycardia, dry mucous membranes, constipation, urinary retention, the occurrence or intensification of symptoms of bronchial obstruction, decreased sweating, the appearance of hyperthermia, especially in children, the development of motor and mental disorders.
Treatment: intravenous administration of physostigmine 0.5-2 mg (no more than 5 mg/day) at a rate of no more than 1 mg per minute or neostigmine methyl sulfate intravenously 0.5-2 mg or intramuscularly 0.5-1 mg every 2-3 hours.

Storage conditions

List A. In a place protected from light.

Release form

A drug Atropine sulfate Available in the form of: powder; tablets 0.5 mg; oral solution 10 ml; solution in ampoules of 1 ml; solution in syringe tubes of 1 ml; eye drops - solution in 5 ml bottles; eye ointment; eye films.

Compound

:
1 ml solution Atropine sulfate contains:
active substance - atropine sulfate 0.05 g,
excipients: sodium chloride, sodium metabisulfite, water for injection.

Atropine sulfate: instructions for use and reviews

Atropine sulfate is an M-anticholinergic blocker with antispasmodic and mydriatic effects. Reduces the tone of smooth muscle organs (urinary tract, abdominal organs, bronchi, uterus), reduces the secretion of the pancreas, bronchial, gastric, sweat and salivary glands, increases intraocular pressure, causes paralysis of accommodation, increases heart rate.

Release form and composition

Dosage form - injection solution 0.05% and 0.1%: colorless transparent liquid [1 ml in ampoules, 10 ampoules in a cardboard box complete with an ampoule knife or scarifier (when using ampoules with break points, rings and notches knife may not be available for opening); 5 ampoules in blister packs, 1 or 2 packs in a cardboard box; Each pack also contains instructions for the use of Atropine sulfate].

Active substance: atropine sulfate, 0.5 or 1 mg in 1 ml of solution.

Auxiliary components: water for injection, hydrochloric acid.

Pharmacological properties

Pharmacodynamics

Atropine is a blocker of m-cholinergic receptors, a natural tertiary amine. It is believed that the substance binds to the m 1 -, m 2 - and m 3 -subtypes of muscarinic receptors to the same extent. It has an effect on central and peripheral m-cholinergic receptors.

The main effects of atropine:

• decreased secretion of gastric, salivary, sweat, bronchial glands;
• decreased tone of smooth muscles of internal organs (including bronchi, digestive system organs, urethra, bladder);
• decreased motility of the gastrointestinal tract;
• decreased secretion of tear fluid.

In addition, atropine promotes the development of mydriasis, paralysis of accommodation, and has virtually no effect on the secretion of bile and pancreas.

When used in average therapeutic doses, atropine has a moderate stimulating effect on the central nervous system and has a delayed but lasting sedative effect.

The ability of atropine to eliminate tremor in Parkinson's disease is explained by its central anticholinergic effect. In toxic doses, the substance can lead to agitation, agitation, hallucinations, and coma.

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

When used in therapeutic doses, atropine does not significantly affect peripheral vessels, but with an overdose, vasodilation is observed.

Pharmacokinetics

Atropine is widely distributed in the body. Metabolism occurs in the liver by enzymatic hydrolysis. Binds to plasma proteins at a level of 18%.

Penetrates through the blood-brain barrier, the placenta and into breast milk. After 0.5–1 hour it is found in the central nervous system in significant concentrations. The half-life is 2 hours.

It is excreted by the kidneys unchanged and in the form of hydrolysis and conjugation products in approximately the same ratio.

Indications for use

0.05% and 0.1% solution of Atropine sulfate is used in the following cases:

• spasms of the bronchi, urinary tract, intestines, gallbladder and bile ducts;
• bronchitis with hyperproduction of mucus;
• bronchial asthma;
• cholelithiasis;
• acute pancreatitis;
• cholecystitis;
• exacerbation of peptic ulcer of the stomach and duodenum;
• pylorospasm;
• atrioventricular block;
• bradyarrhythmias that developed as a result of increased tone of the vagus nerve (including bradycardia);
• hypersalivation (parkinsonism, poisoning with heavy metal salts);
• poisoning with anticholinesterase and cholinomimetic (including organophosphorus) drugs;
• laryngospasm (for prevention);
• premedication before surgical operations (to prevent laryngo- and bronchospasm, reduce vagal cardiac reflexes and secretion of salivary and bronchial glands);
• X-ray examinations of the gastrointestinal tract.

Contraindications

• intestinal atony;
• reflux esophagitis;
• obstructive bowel diseases;
• hiatal hernia;
• nonspecific ulcerative colitis;
• toxic megacolon;
• paralytic ileus;
• liver and/or kidney failure;
• prostatic hyperplasia;
• mitral stenosis;
• tachyarrhythmias;
• cardiac ischemia;
• severe congestive heart failure;
• obstructive urinary tract diseases;
• angle-closure glaucoma or predisposition to it;
• myasthenia gravis;
• pregnancy complicated by gestosis;
• breastfeeding period;
• hypersensitivity to the components of Atropine sulfate.

Carefully:

• hyperthyroidism;
• arterial hypertension;
• hyperthermia;
• pregnancy;
• age over 40 years (due to the risk of undiagnosed glaucoma).

Atropine sulfate, instructions for use: method and dosage

Atropine sulfate is administered subcutaneously (SC), intravenously (IV) or intramuscularly (IM).

• relief of renal and hepatic colic, acute pain due to pancreatitis, gastric and duodenal ulcers, etc.: IM or SC in a dose of 0.25–1 mg of atropine sulfate (0.25–1 ml solution) ;
• bradycardia: 0.5-1 mg intravenously, if necessary, another dose is administered after 5 minutes;
• premedication: IM at a dose of 0.4–0.6 mg 45–60 minutes before anesthesia;
• poisoning with anticholinesterase drugs or m-cholinostimulants: IV 1.4 ml of 0.1% solution of Atropine sulfate, usually in combination with cholinesterase reactivators.

For children, the dose of atropine is 0.01 mg per kilogram of body weight.

Side effects

• headache, dizziness;
• dry mouth, constipation;
• atony of the intestines and bladder;
• tachycardia;
• increased intraocular pressure, mydriasis, photophobia, paralysis of accommodation;
• difficulty urinating;
• violation of tactile perception.

Overdose

Main symptoms: dry mucous membrane of the nasopharynx and oral cavity, impaired speech and swallowing, hyperthermia, dry skin, mydriasis, memory impairment, psychosis, hallucinations, speech and motor agitation.

Therapy: use of anticholinesterase and sedatives.

special instructions

Atropine sulfate penetrates the placental barrier. Adequate and strictly controlled clinical studies on the safety of the drug during pregnancy have not been conducted. If the drug is administered intravenously to a pregnant woman shortly before birth, the fetus may develop tachycardia.

Impact on the ability to drive vehicles and complex mechanisms

During treatment, it is advised to refrain from driving a car and performing any work related to the speed of reactions and increased attention.

Use during pregnancy and lactation

If it is necessary to use Atropine sulfate during pregnancy, it must be taken into account that the active substance penetrates the planetary barrier.

During pregnancy complicated by gestosis, the drug is contraindicated (due to the risk of increased blood pressure).

For women who are breastfeeding, drug therapy is contraindicated.

For impaired renal function

Atropine sulfate is contraindicated for use in renal failure.

For liver dysfunction

Atropine sulfate is contraindicated for use in liver failure.

Use in old age

In patients over 40 years of age, the use of the drug requires caution, which is associated with the risk of undiagnosed glaucoma.

Drug interactions

The drug weakens the effect of anticholinesterase drugs and m-cholinomimetics.

Promethazine and diphenhydramine enhance the effect of atropine, guanethidine can reduce its hyposecretory effect.

With simultaneous use of nitrates, the risk of increased intraocular pressure increases.

In case of combined use with procainamide, an increase in anticholinergic effect is observed.

Analogs

Analogs of Atropine sulfate are Atropine, Atropine Nova.

Terms and conditions of storage

Store in a place protected from light, out of reach of children, at a temperature of 2–30 °C.

Shelf life – 5 years.