Medicinal reference book geotar. How to use atropine sulfate for pancreatitis? Application in pediatric practice

Atropine sulfate belongs to the category of antispasmodics with mydriatic action. The drug affects the smooth muscle tissue of the internal organs and reduces their tone. Due to the use of the drug, spasms of the urinary and digestive systems are eliminated, the heart rate increases and the secretion of the pancreas decreases.

Indications for the appointment of Atropine sulfate include peptic ulcer, gastritis, bronchial asthma, gallbladder pathology, acute pancreatitis, cholecystitis and other diseases accompanied by pain. It is possible to identify some pathologies in which the use of the drug is prohibited only by a comprehensive examination. This nuance excludes the use of Atropine sulfate on its own.

1. Instructions for use

The instructions for the medication contain complete information about its composition, the principle of exposure to the body and indications for use. Pathological processes included in the list of contraindications are displayed in a separate paragraph. Additionally, the manufacturer notes special instructions, the nuances of the drug interaction of the drug and possible side effects. Some instructions are duplicated on a cardboard box. The dosage regimen and the scheme of application of Atropine sulfate can be adjusted by the doctor and differ from the recommendations described by the manufacturer.

pharmachologic effect

The main pharmacological feature of Atropine sulfate is a non-selective blocking of M-cholinergic receptors, as well as an effect on H-cholinergic receptors, but much weaker. The effect of Atropine on the body is expressed in a decrease in the secretion of the gastric, pancreatic, bronchial, sweat, salivary glands, the tone of smooth muscles on the internal organs decreases. Due to the reduced action of the vagus nerve on the heart, the heart rate increases.

Atropine is able to greatly expand the pupils, which is regulated by the innervation of parasympathetic fibers that relax the iris muscle. Along with the expansion of the pupil, the outflow of fluid from the chambers is disturbed, due to which the intraocular pressure may increase.

A relaxed ciliary muscle of the ciliary body causes paralysis of accommodation (visual perception is disturbed). The action on the central nervous system is expressed in the excitation of the respiratory center, as well as a decrease in muscle tension and trembling in parkinsonism.

The drug is broken down by the liver. The dose taken after 2 hours is excreted by the kidneys by 80%, and the rest in the same way within 12-36 hours. About 60% of the active substance is excreted in its original form, the rest is in the form of conjugation and hydrolysis products.

Indications for use

The drug is used as a symptomatic treatment for the following disorders and pathologies:

Mode of application

Atropine sulfate is used as follows:

• Tablets and solutions are taken orally 1-3 r. per day. Therapeutic dose is prescribed in the range of 0.025-0.05-0.1 mg;
• Intravenous solution is administered in exceptional cases, such as poisoning with cholinomimetics - 0.5-1.0 ml of 0.1% solution;
• Subcutaneously - 0.25-1 ml of solution, concentration 0.1%.

Eye drops and atropine ointment:

• 1% solution is instilled in 1-2 drops (children are prescribed a lower concentration). The procedure is carried out up to 3 times in the interval up to 6 hours, depending on the doctor's prescription;
• Ointment 0.5-1% is placed on the edges of the eyelids;
• With electrophoresis of the eyelids - 0.5% solution.

Release form, composition

The drug, which includes the active component of atropine sulfate, is produced in the following forms:

• Tablets or powder;
• Solution 0.1% in amp. 1 ml;
• Eye drops;
• Ointment for the eyes.

Interaction with other drugs

Atropine sulfate interacts with other drugs as follows:

• Reduces the duration and depth of action of narcotic substances, reduces the analgesic effect of opiates;
• When used with novocainamide and quinine, the anticholinergic effect is summed up;
• Together with MAO inhibitors, it can provoke cardiac tachycardia and arrhythmia.

2. Side effects

The drug can cause the following side effects:

• After systemic administration - constipation, mydriasis, tachycardia, dry mouth, difficulty urinating, accommodation paralysis, photophobia;
• After topical application by ophthalmologists (usually after a long one) - hyperemia and swelling of the eyeball, conjunctiva, dry mouth, hyperemia of the skin of the eyelids, tachycardia.

Overdose

In high doses, Atropine sulfate provokes serious side effects (from the nervous system and the general condition of the body). In case of an overdose, the risk of developing respiratory failure is increased. Regular excess of dosages can provoke a feverish state and disruption of the heart. In severe cases, death is possible.

Consequences of an overdose:

With a severe overdose, paralysis of the respiratory muscles can occur, leading to death, which happens only due to a targeted action. To prevent such situations, the medicine can be purchased only from a doctor on his recommendation.

Contraindications

The tool is contraindicated for use in the following cases:

• With intolerance to Atropine;
• With suspicion of glaucoma and glaucoma;
• With prostate adenoma and severe urination disorders;
• With paralysis or intestinal obstruction;
• With palpitations or heart rhythm disorders.

During pregnancy

The drug during pregnancy is prescribed only when absolutely necessary, and is not prescribed for lactation. Atropine is able to pass through the placental barrier and passes into breast milk in trace concentrations.

The use of the drug during pregnancy and before childbirth can cause tachycardia in the fetus.

3. Special instructions

Influence on the ability to drive vehicles and control mechanisms

Side effects can cause a decrease in the speed of psychomotor reactions and concentration. Driving a car and dangerous mechanisms during the period of therapy is recommended to be excluded.

Pregnancy and lactation

Atropine sulfate is forbidden to use during pregnancy. Substances from its composition penetrate the placenta and can adversely affect the condition of the fetus. The drug relaxes smooth muscle tissues (including the uterus) and can provoke premature birth. Pregnant women have an increased risk of tachycardia as a result of the use of atropine sulfate. During the lactation period, the drug is prohibited (it is permissible to use it only with a temporary cessation of breastfeeding).

Application in pediatric practice

In pediatrics, Atropine sulfate is used according to indications. For children, the drug should be prescribed by a doctor (specific age restrictions are not indicated in the instructions).

For disorders of the kidneys

Atropine sulfate is used in the treatment of renal colic. With severe renal dysfunction, the drug is used with caution (adjustment of the dosing regimen may be required).

For disorders of the liver

Hepatic dysfunction is the basis for the careful use of Atropine sulfate. The decision to use the medication should be made by the doctor.

Terms of dispensing from pharmacies

A prescription is required.

4. Terms and conditions of storage

The unopened preparation is stored in the dark at t less than 25 ° C for the period indicated on the package.

5. Price

Depending on the location of the pharmacy network and the margin, the cost of Atropine sulfate is as follows:

1. Average price in Russia:

• Ampoules 1 ml 0.1% - from 11 to 30 rubles;
• H / c 1% 5 ml - from 31 to 52 rubles.

2. Average cost in Ukraine:

• Ampoules 1 ml 0.1% - from 18 to 22 UAH;
• H / c 1% 5 ml - from 12 to 22 UAH.

Video on the topic: How to properly instill in the eye

6. Analogs

A drug that has a similar active ingredient with Atropine is Atromed eye drops. Atropine can be replaced by belladonna extract, which is used only after consulting a doctor.

Structural analogues of Atropine sulfate are not produced, but there are drugs that have a similar pharmacological effect with it:

• Darifenacin;
• Cyclodol;

7. Reviews

Atropine Sulfate is a rather old drug, although it is used in the treatment, despite the existence of more effective means. Reviews about it on the network are rather ambiguous: patients highly appreciate the effectiveness of the remedy in relieving spasms and eye diseases, but at the same time there are negative opinions due to many side effects of the drug.

Atropine sulfate is used to relieve spasms of smooth muscles on internal organs, prevent spasms in the respiratory system, treat ulcers, and also in ophthalmology.

The drug is not available for free sale, and is dispensed only by prescription, as it is on list A (poisons and drugs) in pharmacies. It can only be prescribed by a doctor, taking into account contraindications and the patient's diagnosis.

8. Results

1. Atropine sulfate belongs to the category of blockers of central and peripheral m-cholinergic receptors (the drug has an antispasmodic effect, reduces the secretion of the salivary and sweat glands, affects the smooth muscle layer);
2. indications for the use of the drug are intestinal and renal colic, spasms of the digestive system, bronchospasm, cholelithiasis, pancreatitis during an exacerbation and other pathological processes accompanied by pain;
3. Atropine sulfate is used during the procedure for examining the fundus (with pathological processes of various origins);
4. it is not recommended to use the drug during pregnancy due to the risk of tachycardia and stimulation of labor;

Gastroenterologist, Therapist

The doctor conducts a general diagnosis of internal organs. Makes conclusions about disorders in the gastrointestinal tract based on the results of the examination and prescribes appropriate treatment. Among the diagnoses that the specialist deals with: stomach and duodenal ulcers, gastritis, dysbacteriosis, etc.

Atropine (or atropine sulfate) is an essential tool in the treatment of many aggravated diseases of the stomach, intestines, kidneys, etc. Atropine (lat. Atropinum sulfate) is an anticholotnergic alkaloid of a natural plant type. It is found in nightshade plants, as well as in intoxicating herbs. Before using it for its intended purpose, it is important to read the instructions from top to bottom and make sure that there are no contraindications. The discovery of atropine took place in the last century, which was preceded by numerous studies.

Description of Atropine sulfate and indications for use

Atropinum belongs to the pharmacological and therapeutic group of belladonna alkaloids and, as mentioned earlier, is of natural origin. The main substance (atropine) binds equally well to the M-1, M-2 and M-3 subtypes of muscarinic receptors. It has its clinical effect not only on the central, but also on the peripheral M-cholinergic receptors. Atropine also acts very weakly and inconspicuously on H-cholinergic receptors, and also becomes a strong obstacle to stimulating acetylcholine in general. As a result of such an action on acetylcholine, the secretion of all glands in the body decreases to the minimum permissible levels (this applies to salivary, sweat, gastric, lacrimal and broncho glands).

Atropinum affects the tone of the muscles of the internal organs, reducing them. This applies to the smooth muscle muscles of the biliary tract and bladder, bronchi, pancreas, stomach, urinary canal and bladder. In addition, atropine can cause severe/mild tachycardia, make aqueous humor more difficult to drain, dilate pupils, and cause accommodative paralysis. At medium-moderate doses, it can act like a drug, providing the patient with a delayed and prolonged sedative effect. This is due to the high ability of Atropinum to act on the central nervous system.

The absorption and action of the atropine-containing agent occurs very quickly, after which the substance goes to the system. blood flow and gives its therapeutic effect. The distribution of atropinum in the body also occurs surprisingly quickly, along with this, it crosses the placenta. barrier and mother's milk. It is also easy for the substance to penetrate the blood-brain barrier. For example, if we take into account an intravenously administered drug, then its maximum concentration in the blood is observed after a couple of minutes.

As a symptomatic therapy, Atropinum has the following indications for use:

• stomach ulcer;
• Ulcer of the 12th colon;
• Pylorospasm;
• Acute pancreatitis;
• Cholecystitis;
• Cholelithiasis;
• Intestinal spasms;
• Bronchial asthma;
• Ophthalmic diseases caused by declining visual acuity;
• Active-passive spasms in the urinary tract.

In addition, Atropine is prescribed before preoperative anesthesia, as well as during the continuation of surgery to prevent spasms in the respiratory system, as well as to reduce the secretion of excretory glands during this period. Atropinum is very effective as a fast-acting antidote when a person has been poisoned by the adverse effects of cholinomimetes and anticholinesterases.

Atropine is most actively used in psychiatric medicine. Here, a broadly effective remedy is used to treat psychoses - affective, catatonic, paranoid and many others. For this, atropinocomatous therapy was previously used, where higher doses of Atropinum were present. Since the 1970s, I have almost never used this treatment method against psychoses.

Atropinum is available as eye drops, tablets, injectable clear solution. The choice of one form or another depends on the general disease.

Application instruction of Atropine

Atropinum sulfat begins to be taken only after an appropriate recommendation - independent use of the drug is prohibited. The fact is that it has contraindications and side effects.

Eye drops

Here Atropine is used in diagnostic studies of the fundus for those purposes, to dilate the pupil for greater visibility and for the treatment of certain eye diseases.

For the treatment of eye diseases, children from 7 years old and adults are prescribed 1-2 drops in each affected eye from 2 to 6 times a day. The effect of the pupillary dilator depends on the type of pathology and can vary from 7 to 12 days.

In childhood, Atropinum sulfate should be used in the form of eye drops in low-concentrated doses - 0.125%, 0.25%, 0.50%.

A very well tolerated agent can sometimes cause adverse reactions and overdose (use in the maximum allowable doses). Symptoms of pronounced excesses of Atropinum dosing in this case may be globally occurring insomnia, convulsive states, hallucinations, irritability “out of the blue”, vomiting and nausea, a slightly significant drop in the arter. pressure, severely depressing the nervous and respiratory systems of the state. Overdose therapy should include properly performed gastric lavage in a hospital, as well as symptomatic treatment. In case of an overdose of Atropinum eye drops, physicians also administer cholinomimetics and anticholinesteretics to the patient parenterally.

injection solution

Atropinum is administered by injection in various ways - subcutaneously, intramuscularly and intravenously. With the introduction of preoperative anesthesia Atropine sulfate is administered intradermally in an amount of 0.3-0.6 mg or together with morphine in an amount of 10 mg one hour before anesthesia. If a person has been poisoned by anticholinesterases, then Atropinum is administered intramuscularly every half hour in an amount of 2 mg. The introduction of the drug is not stopped until the patient has an easily noticeable tachycardia with enlarged pupils, red-dry skin and normally stabilized breathing. If this kind of poisoning is severe, then Atropinum is administered for two days - as a rule, after a two-day period, a phenomenon such as "reatropinization" occurs.

The maximum acceptable dose (single) of the drug depends on the age of the patient:

• Up to 6 months - 0.02 mg;
• 6 months - 1 year - 0.05 mg;
• 1-2 years - 0.2 mg;
• 3-4 years - 0.25 mg;
• 5-6 years - 0.3 mg;
• 7-9 years - 0.4 mg;
• 10-14 years - 0.5 mg;
• Adults - single 1 mg, and daily - 3 mg.

Atropine sulfate is given with great caution to people who are in old age. Extremely sensitive to atropine are infants who are not yet 3 months old.

Pills

Atropinum tablet is prescribed for the treatment of gastrointestinal problems, where it is indispensably good and expected to reduce gastric secretions. As a rule, these tablets are used in combination with other anti-ulcer drugs.

Atropine-containing medicine is available in one active dosage option. Substances - 0.5 mg. Their reception is prescribed half an hour before breakfast / dinner / lunch or one hour after the end of the meal. The dosage of internally applicable solid tablets is determined by an individually tailored plan for each patient, however, it is considered optimal if he began to feel genuine desiccation in the oral cavity. In this case, it is better not to deal with an increase in the dosage of an atropine-containing agent in the form of tablets.

Do I need a prescription to buy Atropine?

Atropinum cannot be bought just like that - the pharmacy always requires its most accurate prescription from a specialized doctor. It is usually written in Latin letters, including the dosage and method of administration. The recipe for Atropine sulfate looks like this:

• Rep: Sol. Atropini sulfatis 0.05% - 1 ml.
• D.t. d. N 10 ampull.
• S. 1 ml subcutaneously.

Only a doctor should write this prescription, where he must also write the specific disease for which the medicine was prescribed. Due to the fact that Atropinum acts like a narcotic in long-term multi-dose use, the availability of a prescription is monitored very strictly.

Atropine eye drops

The composition of these eye drops necessarily contains such components as atropine sulfate (active substance), sodium metabisulfate, sodium chloride, specially prepared water. Drops have a water-like appearance - the same liquid and transparent, and their smell is slightly specific.

In addition to fundus research, Atropinum drops are also used to treat other diseases associated with visual functions. This applies to the complex-collective treatment of inflammatory eye diseases, injuries in the eye area, embolism, as well as spastic conditions in the central retinal artery.

Despite the fact that Atropinum is often used to diagnose eye problems, doctors strongly recommend choosing other drugs for this purpose. For diagnosis, mydriatics are usually chosen with a short therapeutic effect (pupillary dilation), which is no more than 1-2 days.

In order to reduce tachycardia from the drug, which can occur both with subconjunctival and parabulbar drops, in parallel with instillation of the eyes, the patient can put a validol tablet under the tongue. Using Atropinum drops in combination with other conjunctival drops, the interval between instillation procedures should be at least fifteen minutes.

The price of Atropine in pharmacies

As mentioned above, Atropinum sulfate can be bought at a pharmacy only after providing a prescription to a pharmacist. The cost of Atropine is average when compared with many other products of this type.

Sometimes online pharmacies have lower prices than standard ones. If it is supposed to transport the medicine to another city, then the difference may become opposite and the Internet tool will cost even more. But most often, buyers turn to such non-standard pharmacies for the reason that there is no such remedy in the usual one. When purchasing the described atropine-containing or any other remedy in such a pharmacy, you need to be as careful as possible so as not to get a fake instead of a medication.

Contraindications

The presence of serious/non-serious contraindications in a patient should be checked very well, since even one of them can lead to difficult-to-solve problems. We are talking about such necessarily-taken into account contraindications:

• Carrying a baby at any time and feeding, since atropinum freely penetrates through the placental protective barrier;
• Highly sensitive reactions to available components;
• Diseases of the cardiovascular system;
• Acute current bleeding;
• Gastrointestinal diseases accompanied by obstruction (pyloric stenosis, esophageal achalasia, etc.);
• Brain damage;
• thyrotoxicosis;
• Glaucoma;
• Liver and / and renal failure;
• Urinary retention or high risk of its occurrence.

Sometimes, strictly contraindicated phenomena, the patient is brought to know after the start of the treatment and rehabilitation course. Here, not a single negative phenomenon is overlooked - it should be urgently told to a specialist doctor who is aware of the history of meteorological pathology from "a" to "z".

Atropine sulfate

International non-proprietary 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

Clear colorless liquid

Pharmacotherapeutic group

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

ATX code A03B A01

Pharmacoboolean properties

Pharmacokinetics

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

Pharmacodynamics

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

It has anticholinergic dose-dependent effects:

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

In high 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 excites the central nervous system.

Due to the central anticholinergic action, it is able to eliminate tremor in Parkinson's disease. In toxic doses 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 and to an increase in conduction in the bundle of His. In therapeutic doses, it does not have a significant effect on peripheral vessels, with an overdose, vasodilation is observed. It is an effective antidote for poisoning with cholinomimetic and anticholinesterase substances.

Indications for use

With gastric ulcer and 12 duodenal ulcer, intestinal spasms, acute pancreatitis, for X-ray examination of the gastrointestinal tract (decrease in tone and motor activity of organs)

Pylorospasm

gallstone disease, cholecystitis

Bronchial asthma

Bradycardia due to increased vagal tone

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

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.

Dosage and administration

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 the antidote therapy regimens for these intoxications, taking into account the use of atropine together with cholinesterase reactivators.

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

Higher doses for adults inside and subcutaneously: single - 0.001 g, daily - 0.003 g. Children of 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 a 0.1% solution); from 1 to 5 years - 0.016 mg (0.016 ml of a 0.1% solution); from 6 to 10 years - 0.014 mg (0.014 ml of a 0.1% solution); from 11 to 14 years old - 0.012 mg (0.012 ml of a 0.1% solution). The duration of the course of treatment is determined by the doctor.

Side effects

Often

Dry mouth, nose and/or skin

Reduced sweating

Mydriasis, accommodation paralysis

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

Violation of 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 stomach contents)

liver failure

kidney failure

intestinal atony

obstructive bowel disease

paralytic ileus

toxic megacolon

nonspecific ulcerative colitis

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

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

urinary retention or predisposition to it, or diseases,

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

Down's disease

cerebral palsy (reaction 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 preparations of lily of the valley, with tannin, a physicochemical interaction is observed, which leads to a mutual weakening of the effects.

special instructions

With pain caused by spasm of smooth muscles, 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 lung disease, acute blood loss, hyperthyroidism, advanced age.

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

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

Overdose

In cases of overdose - the most pronounced side effect.

Treatment: symptomatic.

Release form and packaging

1 ml of the drug is placed in glass ampoules.

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

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 the tone of smooth muscles of internal organs (including bronchi, organs of the 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.

When applied topically 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 of the stomach and duodenum, acute pancreatitis, hypersalivation (parkinsonism, poisoning with salts of heavy metals, 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 sore 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 swelling of the conjunctiva of the eyelids and the 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 increased 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 diseases of the cardiovascular 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 (possible development of obstruction), 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 the secretion 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 tablet under the tongue to reduce tachycardia.

Influence on the ability to drive 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 studies of the safety of the use of atropine during pregnancy have not been conducted.

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 urinary tract obstruction (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 the salivary, bronchial, gastric and sweat glands, increases the viscosity of bronchial secretions, inhibits the activity of cilia of the ciliated epithelium of the bronchi, thereby reducing mucociliary transport, accelerates heart contraction, increases AV conduction, reduces the tone of smooth muscle organs, reduces the number and total acidity gastric juice (especially with the predominance of cholinergic regulation of secretion), reduces the basal and nocturnal secretion of gastric juice, to a lesser extent reduces stimulated secretion, vir 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, for 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 caused by excitation 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, coronary heart disease, 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. With simultaneous use with sulfanilamide drugs, the risk of kidney damage increases, with drugs 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, butyrophenones, phenothiazines, dispyramids, 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

Given the possibility of such adverse reactions as dizziness, hallucinations, disturbance of accommodation, when using the drug, you should refrain from driving vehicles or operating 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

The side effect of the drug is mainly due to 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 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 "Kharkov Pharmaceutical Enterprise" People's Health ".