Atropine method of administration. The use of atropine

Atropine is a drug that is widely used in medicine. It is produced on a plant basis. But, despite its natural origin, this medicine is quite dangerous. Atropine, or atropine sulfate, is an alkaloid and helps block m-cholinergic receptors.

Dosage form and main components

Atropine can be found in pharmacies in various forms.

  • Powder - 0.5 mg.
  • Tablets - 0.5 mg.
  • Solution intended for oral administration - 10 ml.
  • The solution released for injection in ampoules and syrettas - 1 ml.
  • Atropine sulfate drops, intended for the treatment of diseases of the organs of vision (1%), in the form of a solution, released in 5 ml vials.
  • Eye ointment 1%.
  • Films for the eyes. Each bottle contains 30 of them.

The main active substance of the drug is atropine sulfate. The secondary components are: hydrochloric acid, water for injection.

1 ml of eye drops contains 10 mg of the main substance, 1 ml of injection solution - 1 mg.

The effect of the drug on the body

Atropine sulfate has an anticholinergic effect, that is, it helps to disrupt the supply of a nerve impulse by blocking m-cholinergic receptors. The effective mechanism is aimed at a bunch of atropine sulfate not with acetylcholine, but with specific formations of the neuron. In this regard, the conduction of a nerve impulse is blocked. Atropine has such effects depending on which disease the fight is directed at:

  • Promotes muscle relaxation, that is, Atropine solution is an antispasmodic agent. A similar effect is noted in the gastrointestinal tract, bronchi, urinary and biliary organs.
  • Reduces the activity of the secretion of the external glands. This includes: bronchial, sweat, salivary, digestive glands.
  • It paralyzes accommodation (the ability of the organ of vision to clearly perceive objects located at different distances).
  • It has an effect on blood vessels, that is, promotes their expansion, but only if a significant dose is used.





The agent is also actively used in anesthesiology before or during surgery in order to reduce the secretion of bronchial and salivary glands, weaken reflexes, and prevent laryngospasm.

Additional properties of the drug

In addition, the use of Atropine is advisable before performing an X-ray examination of the intestines and stomach. A medicine is used for poisoning with organophosphorus compounds (sarin, chlorophos, karbofos). Atropine in this case acts as an antidote.

Pharmacological properties of Atropine

Atropine is found in some plants. Most of this substance is present in belladonna, henbane and dope. It is a fine-crystalline powder that has neither odor nor color. The substance dissolves quickly in water, alcohol, is resistant to ether and chloroform.

If the solution is injected subcutaneously, the effect is achieved after 2–4 minutes, after using the drops, the effect of the agent is observed after half an hour. In large doses, the drug leads to excitation of the nervous system.

Indications for use

Atropine solution is widely used in clinical practice. Here are the main indications for the use of the drug.

  • Ulcerative lesions of the stomach and duodenum. The main purpose of the drug is to suppress the secretory function of organs.
  • Contraction of the pylorus in order to relax it.
  • Cholelithiasis (cholelithiasis), an inflammatory process in the organ. The main purpose of the drug is to expand the ducts for the passage of stagnant bile.
  • Pancreatitis in an acute stage.
  • Intestinal, hepatic, biliary colic.
  • Bronchial asthma - in order to eliminate bronchospasm.
  • Suppression of bronchial secretion, as well as salivary, sweat, lacrimal.
  • Bronchitis with hypersecretion, bronchospasm.
  • Hypersalivation - excessive salivation.
  • Poisoning of the body with organophosphorus compounds.
  • The need to dilate the pupil to examine the fundus.
  • Providing functional rest of the organ of vision in the event of an inflammatory process or injury.








Application rules and optimal dosages for various diseases

The agent with atropine can be taken orally, injected subcutaneously, into a vein, muscles. In each individual case, a certain dosage and course of treatment is established.

So, in case of ulcerative lesions of the stomach and duodenum, 0.25-1 mg should be taken. This is the daily dosage for adults, which is divided into 3 doses. As for children, the dose of the drug should be reduced to 0.05–0.5 mg per day and divided into 1–2 doses.

The maximum daily dosage of Atropine should not be more than three mg. If intravenous, subcutaneous, intramuscular administration is required, then the highest dosage in this case is 0.25–1 mg and is divided into 1–2 injections.

Drops of Atropine sulfate for the treatment of eye diseases are injected into the organs of vision in 1-2 drops. The frequency of drug administration is 3 times a day. Eye ointment is applied for the eyelids 1 (if necessary, 2 times) a day.

Contraindications

It is forbidden to use the drug in any form for the following pathologies:

  • closed-angle and open-angle glaucoma;
  • synechiae of the iris;
  • if there is a narrow angle between the cornea and the iris;
  • keratoconus (thinning of the cornea);
  • intolerance to atropine sulfate;
  • hypertrophy of the prostate;
  • kidney disease;
  • cachexia.






There are also a number of restrictions that prohibit the use of the drug. It:

  • vascular and heart disease;
  • high body temperature;
  • diseases and hernias of internal organs;
  • reflux esophagitis;
  • ulcerative colitis is nonspecific.





The contraindication of the drug also includes children under 7 years of age.

Side effects of the drug

The use of Atropine in various diseases can cause undesirable effects. These include:

  • headache;
  • sleep disturbance, insomnia;
  • dizziness;
  • euphoria, hallucination;
  • confusion of consciousness;
  • strong pupil dilation;
  • accommodation paralysis;
  • violation of tactile perception;
  • photophobia;
  • if you use drops of atropine sulfate, then in rare cases, there may be hyperemia of the eyeball, edema of the conjunctiva, irritation and swelling of the eyelids;
  • tachycardia;
  • dry mouth;
  • constipation;
  • difficulty urinating;
  • increased intraocular pressure;
  • fever;
  • aggravation of myocardial ischemia.










Overdose when using Atropine

If you exceed the dose of the medicine, then the person will feel the following symptoms:



An overdose of Atropine primarily affects the state of the nervous system. In this case, the person will feel: confusion, tremors of the limbs, anxiety, unreasonable fear, hallucinations and delirium, drowsiness and stupor. If you do not take action in time, it can result in death caused by vascular, heart or respiratory failure.

Incompatibility of Atropine

It is undesirable to use such drugs together with Atropine:

  • tricyclic antidepressants;
  • phenothiazines;
  • antihistamines;
  • nitrates.

special instructions

When using the product, you should be careful for people whose work is associated with complex mechanisms and driving vehicles.With any illness, it is not allowed to take pregnant women and nursing mothers. The fact is that the main active substance of the drug penetrates the placenta and breast milk, which can lead to the development of a toxic effect on the child.

Atropine Sulfate (or simply Atropine) is mydriatic and antispasmodic produced in various dosage forms. Such a variety can allow the drug to be used as directed in any convenient form - tablets or injection solutions. Substances of the chemical structure of the agent belong to the group of alkaloids and are found mainly in the nightshade plant families. Belladonna (or belladonna) is one of the most famous of their representatives.

Composition of the preparation developed from chemical and synthetic compounds in factories using special technologies. Atropine Sulfate belongs to the pharmacological group of anticholinergics, adjusted for the blockade of M-cholinergic receptors. The drug is used primarily to relieve tension in smooth muscle tissue and spastic conditions. The drug has found application in the prevention and treatment of ophthalmic diseases.

Atropine indications: for use

Atropine is used for a wide variety of purposes. The full range of directions for the use of the product is indicated in the instructions, which can be found in each package.

Conditions in which the drug is prescribed:

  • Gastric pylorus spasm
  • Stomach or intestinal ulcer
  • Colic due to gallstones
  • Intestinal, renal, or biliary colic
  • Inflammatory processes in the pancreas and gallbladder
  • All forms of bradycardia
  • Irritable bowel syndrome
  • Bronchospasm caused by an allergic or asthmatic condition.

Atropine is often used before surgery using anesthesia. This is done to reduce salivation.

For X-ray diagnostics of the gastrointestinal tract, the drug is also used. Since the drug reduces the efficiency of the skin glands, it is also used for the pathology of sweating. As an antidote, the medication is applicable for poisoning with some poisons.

Ophthalmologists use a drug for mydriasis, that is, a special effect of dilating the pupil. This is done in order to gain access to the fundus of the patient and perform the necessary manipulations and diagnostics. It is also used to treat inflammation and diseases of the cornea and iris of the eye. After an injury or an operation on the eyeball, Atropine drops relax the eye muscles to the required state and helps to achieve a speedy recovery, providing them with complete peace.

Since the drug is subject to quantitative accounting in pharmacies, it is impossible to buy it without a doctor's prescription. In the absence of contraindications to the components of Atropine, the doctor may prescribe this medicine, which is part of the group of poisonous and narcotic drugs (group A).

Atropine sulfate

The presented drug can be used for inhalation for problems of bronchial spasms, injected intramuscularly and intravenously, taken orally and as a fine aerosol.

Injection 0.1% is injected twice a day. If you take the solution inside, then once a day is enough, also 0.1%. If it is necessary to use Atropine aerosol, the dosage is discussed in advance with the attending physician and, as a rule, is the same 0.1% solution. Used by required amount times, usually 3-5 minutes before getting rid of the attack.

Atropine eye drops

For ophthalmic use Atropine ophthalmic solution can be purchased in pharmacies with a dosage of 5 ml of a 1% solution. In case of inflammation and damage to the eye, for favorable conditions, ophthalmologists prescribe to use drops 5-6 times a day, 1-2 doses in each eye. In such cases, medriasis lasts about a week and occurs within half an hour after using the drops.

If the patient turns to an ophthalmologist to diagnose, the duration of medriasis is regulated by the dose of the drug, and this effect lasts no more than two days. Some manufacturers produce eye films, gels, and ointments that contain a base substance.

Mechanism of action of Atropine

M-cholinergic receptors are actively blocked by the special ability of Atropine, which underlies its mechanism of action. These receptors are found predominantly in smooth muscle tissues in the region of the endings of parasympathetic nerve fibers. The specific mechanism of action of the drug provokes the following pharmacological effects:

  • Increases heart rate
  • Causes pupil dilation
  • Normalizes the patency of nerve impulses of the heart muscle
  • Inhibits the production of secretions of sweat, salivary, digestive and bronchial glands
  • Relaxes the smooth muscles of the gastrointestinal tract, bronchi and urinary system

Such a wide range of rather serious effects in pharmacology increases the likelihood of side effects from the drug, and also explains the rather long list of contraindications to the use of the drug.

Atropine contraindications

Medication instruction says about all kinds of situations when the drug can cause irreparable damage to health, so it must be used with some caution or completely excluded from the complex treatment.

Contraindications:

  • Keratoconus
  • Bowel obstruction
  • Age up to 7 years
  • Kidney pathology
  • Abnormal heart rhythm
  • Rapid or decreased heart rate
  • Organic or pathological disorders of the heart muscle
  • Allergy to the drug
  • Individual intolerance to one or more components of the drug
  • Reflux - esophagitis
  • Small intestine paralysis
  • Prostate adenoma causing urinary disorders
  • Glaucoma (is a contraindication to Atropine drops, powders, solutions and tablets)

In case of an overdose or non-observance of the rules for using the drug, as well as in case of hypersensitivity of the body to the drug, the following can be expected side effects:

  • allergic reaction
  • tachycardia
  • visual impairment
  • headache
  • dry mouth
  • dizziness
  • urination problems

Only the attending physician, on the basis of the diagnostics and analyzes carried out, can prescribe use of the drug Atropine, in order to avoid the negative consequences of the uncontrolled use of the medicine.

Atropine tablets

A fairly widely used form of release of Atropine is tablets. They are prescribed to reduce the secretion of digestive enzymes in complex treatment of ulcers intestines and stomach.

Dosage of Atropine tablets- 0.5 mg. They are taken half an hour before a meal or 1-2 hours after it. The dose is compiled by the attending physician individually for each patient. The main guideline of the gastroenterologist in the selection of the dosage is the symptom of dry mouth of the patient based on the intake of Atropine tablets. This symptomatology indicates that a further increase in the dose of the drug is fraught with stronger negative effects.

Overdose atropine

If you use the drug uncontrollably, there is poisoning against the background of an overdose, which is shown by the following symptoms:

  • Constipation
  • Vomiting and nausea
  • Redness of the mucous membranes and their dryness
  • Arrhythmia or tachycardia
  • Increased breathing
  • Trembling limbs
  • Swallowing reflex disorder, hoarseness
  • Excitation of muscle tissue
  • Loss of consciousness
  • Convulsions

In case of deliberate poisoning with a drug or in cases of severe overdose of the drug, the patient can expect a fatal one caused by paralysis of the respiratory muscles. In order to avoid such rare situations, you can buy a medicine only by presenting an appropriate document at the pharmacy, which officially allows the pharmacist to sell the drug.

Atropine reviews

The pharmacological effect of the drug outweighs the problems from its overdose or misuse, therefore, positive reviews are still more numerous, although they are diluted with adverse consequences and corresponding reviews.

Since this drug has been replaced by more modern and effective drugs with a much smaller spectrum of side effects, the reviews of specialists about it are also ambiguous.

Atropine analogues

Atromed is considered to be a complete analogue of Atropine on a composite basis, but it has a relative drawback - the form of release is exclusively in eye drops, therefore, the agent is not suitable for other therapeutic areas. To replace Atropine, you can use belladonna extracts or tinctures, but subject to prior agreement of the treatment with your doctor.

The following drugs have a completely different composition, but a similar pharmacological effect:

  • Darifenacin
  • Platyphyllin
  • Cyclodol
  • Pirenzepine

Atropine during pregnancy

In such a fragile situation as pregnancy, it is advisable to avoid taking Atropine or use it exclusively when urgently needed and under the strict supervision of the attending physician. There are cases when the active substances of the drug penetrated the placenta barrier, causing serious ailments and violations of the course of pregnancy.

When the solution for injection is administered intravenously, Atropine to a pregnant woman can provoke pathologies of the development of the fetus while still in the womb. During lactation, the drug can be used, but also with caution, since trace concentrations of the substance can penetrate into breast milk.

Atropine drops for children

With extreme caution, it is allowed to use Atropine in the treatment of children from 7 years of age. With cerebral palsy, cerebral palsy and downism, the use of the drug is possible, but it is worth considering the more powerful reaction of the child's body to drugs of this pharmacological group.

If the drug must be used on a child with periodic or chronic diseases of the upper and lower respiratory tract, it is advisable to do this in a hospital under the strict supervision of specialists. The same recommendations apply to children weakened from various diseases. Doctors should monitor the concentration of bronchial secretions in order to avoid an increase in density and viscosity, and then blockage of the bronchial passages.

special instructions

When taking atropine in any of the prescribed ways, in order to avoid the possible development of tachycardia, you can put the pill under the tongue. For almost every indication, there is a number of contraindications- this should also not be forgotten.

If during the period of treatment the patient needs to drive vehicles or use increased concentration of attention, one should be extremely careful in dosage and administration.

Atropine price

It is not difficult to get Atropine in a pharmacy with a doctor's prescription. Also, recently it has become incredibly convenient to buy drugs in online pharmacies... This method eliminates unnecessary queues and saves a lot of time. Price for Atropine is not a decisive factor in choosing a purchase method, since both in a regular pharmacy and on the Internet you can buy a package of medicine for 40-50 rubles.

The drug Atropine lowers the tone of the internal muscles of the bronchi, stomach and bladder. It is prescribed to reduce the secretion of the salivary, sweat and bronchial glands. You need to know in what dosage the medicine is taken, and what side effects it has on the body.

The main task of Atropine is to block the M-cholinergic receptors. The drug will reduce the secretion of saliva in bronchial diseases. Also, Atropine will increase heart rate for a therapeutic effect. The medicine can reduce the tone in the bronchi and in the abdominal cavity. If the patient has an overestimated vagus nerve tone, then Atropine will act even more strongly. The medicine affects the dilation of the pupil in the eye. This occurs at the moment of relaxation of the muscles in the membrane of the eye.

Doctors prescribe Atropine as symptomatic therapy for such diseases:

  • Stomach ulcer;
  • Duodenal problems;
  • Acute pancreatitis;
  • At the time of pylorospasm;
  • For the treatment of gallstone disease;
  • Cholecystitis treatment;
  • Severe cramps in the intestines;
  • Urinary tract problems;
  • Severe attacks of bronchial asthma;
  • To increase the tone of the nerve with bradycardia;
  • To reduce the tone of organ activity during x-rays.

Also, the doctor may prescribe injections with a drug for the following purposes:

  1. Before the introduction of anesthesia at the time of the operation;
  2. To relieve bronchial spasms during surgery;
  3. To reduce the secretion of the gland;
  4. Removal of a reflex reaction;
  5. It is prescribed as an antidote for overdose with cholinomimetic drugs.

In some cases, the use of Atropine is dangerous to the patient's health. Doctors prohibit the drug in such situations:

  • Severe allergy to any component in the composition;
  • Heart problems;
  • The onset of atrial fibrillation;
  • Tachycardia attacks;
  • Insufficiency in the work of the heart;
  • Ischemic attacks;
  • Dangerous with mitral stenosis;
  • Not prescribed for severe stage of arterial hypertension;
  • If the patient has any bleeding;
  • The drug is dangerous for thyrotoxicosis;
  • It is not prescribed for hyperthermic syndrome;
  • If the patient has stomach problems;
  • Dangerous with glaucoma;
  • It is not prescribed for problems with the kidneys and liver;
  • If the patient has frequent urinary retention;
  • Dangerous in case of serious brain damage.

If you use the drug in specific cases, it can cause complications and harm the body. Be sure to get tested to use Atropine correctly.

You need to know with which drugs Atropine is incompatible or may cause side effects. Here is a complete list of drug combinations:

  • The use together with MAO inhibitors leads to a change in the rhythm in the heart;
  • The use of Atropine with Quinidine causes an increase in the anticholinergic action;
  • If taken together with tannin, it will weaken the effect of both substances;
  • Atropine will reduce the analgesic effect of all opiates;
  • The drug reduces the duration of action from narcotic drugs;
  • Parallel reception of diphenhydramine enhances the effect of Atropine;
  • The use of haloperidol increases the pressure inside the eye;
  • Application together with sertraline will cause feelings of depression and oppression;
  • Taking penicillin leads to an increase in the action of both drugs;
  • If Atropine is used together with ketoconazole, its absorption into the bloodstream will decrease.

Also, experts have identified a number of other interactions that you need to pay attention to before taking:

  1. Attapulgite will reduce the therapeutic effect of Atropine;
  2. The medicine will, when taken in parallel, reduce the therapeutic effect of Pilocarpine;
  3. When using octadine, the effect of Atropine is reduced;
  4. If the medicine is used together with sulfa drugs, a big problem with the kidneys and liver may begin;
  5. Parallel administration with potassium preparations leads to stomach ulcers. It can also cause bleeding;
  6. The effect of the drug Atropine is enhanced by taking antidepressants, Amantadine and Phenothiazine;
  7. Any other medicines will be absorbed and effective more slowly after taking Atropine.

If the patient is taking other drugs for therapy, he needs to adjust the dosage or temporarily suspend treatment. This should be decided only by the attending physician.

Doctors have identified a number of diseases in which Atropine is prescribed with great care. In this case, the doctor must monitor the patient's condition and adjust the dosage. Here is a list of the main diseases in which the drug can harm:

  • Cerebral palsy in children;
  • Problems with urination;
  • Down's disease;
  • With hernias in the digestive area;
  • Any stage of ulcerative colitis;
  • At the moment of the megacolony;
  • Caution for dosage in elderly patients;
  • With an advanced stage of lung disease;
  • For children with autonomic neuropathy.

Patients with such diseases must necessarily monitor their health after using Atropine and inform their doctor.

Doctors do not allow pregnant women to use Atropine at any time. Also, do not use the drug while breastfeeding. Scientists have proven that toxic substances can get to a child through milk. This will lead to severe allergies and health complications.

Driving during treatment

Remember that Atropine causes the side effects of dizziness and mild hallucinations. That is why it is worth refraining from driving until the end of therapy. Doctors also advise patients not to work with mechanisms that require a lot of concentration.

Atropine can be administered intramuscularly, intravenously and subcutaneously. To reduce the heart rate and reduce the bronchial glands, doctors prescribe 0.5 mg of the drug in the form of a subcutaneous injection. It should be applied one hour before anesthesia along with morphine.

In case of severe poisoning with cholinomimetic substances, use the drug, 2 mg by intramuscular injection. It is necessary to enter Atropine every half hour. It is necessary to stop the administration of the drug after redness of the skin or with an attack of tachycardia. For severe poisoning, use the drug for 1-2 weeks.

The maximum dose for an adult is 3 mg per day. You can enter 1 mg of Atropine at a time. For children, an individual dosage is selected by the attending physician. It depends on the age and weight of the baby, as well as on the stage of the disease. The dosage for elderly patients should be used with caution.

If a person develops side effects, the doctor should reduce the dose of Atropine or reduce the frequency of injections.

If too much drug is injected into a patient, complications and health problems can develop. The first signs of an overdose are displayed in the following symptoms:

  1. A strong feeling of nausea, vomiting;
  2. The patient's blood pressure drops;
  3. Tremor occurs;
  4. The person feels overexcited;
  5. Severe cramps
  6. It is difficult to fall asleep at night;
  7. Hallucinations may begin;
  8. The patient becomes nervous and irritable;
  9. Hyperthermia occurs;
  10. The process of oppression in the nervous system;
  11. Decrease in activity in the respiratory zone.

As soon as the patient feels such symptoms, he should immediately stop using Atropine and go to the hospital. Doctors are required to quickly flush the stomach and introduce cholinomimetic agents into the body. With a symptom of hyperthermia, you need to wipe the patient with wet towels and prescribe antipyretic drugs.

If a person feels overexcited and fearful, the doctor will prescribe thiopental injections. You can also take Physostigmine. If glaucoma is detected, the patient should drip Pilocarpine into the eye sac. At this point, you can give an injection with Proserin 3 times a day. The patient can leave the hospital only after all unpleasant symptoms have passed.

Adverse drug reactions

In the instructions for use, you can see all the side effects of the drug. Usually complications arise with individual intolerance to the drug or with an overestimated dosage for use.

Where do they arise?Side effects
Side effects like this can start in the stomachFeeling of dry mouth;
Intense thirst;
Changes in taste when eating;
Problems with motility in the intestines;
Decreased tone in bile;
The onset of dysphagia;
Problems with urination.
Such complications can begin in the heart zone.Tachycardia attacks;
Severe arrhythmia;
An attack of ischemic disorder;
The patient's face turns red;
There is a feeling of rush of blood to the body.
Such side effects are observed in the nervous system.Severe headache attacks;
The patient is dizzy;
Feelings of nervousness and fear arise;
It is difficult for a person to fall asleep at night.
Such complications can begin in vision.The patient's pupils will dilate;
Photophobia occurs;
Accommodation paralysis;
Pressure rises inside the eye;
The clarity of vision is rapidly declining.
The respiratory system has these side effects.The tone of the bronchi decreases;
The phlegm becomes more viscous;
It is difficult for the patient to clear his throat.
The following side effects are observed on the skin:Red rash on the body;
The appearance of urticaria;
Manifestation of exfoliative dermatitis;
Severe allergy to the composition of the drug.
Other side effects of the drugThe patient begins to sweat less;
The skin at the injection site becomes dry;
Dysarthria occurs;
The skin may turn red due to the sensitivity to the composition.

If any side effects are found, the injection must be stopped. The doctor must determine the cause of this reaction. It may be necessary to reduce the dosage or replace Atropine with a similar agent.

Store the drug only in its original packaging. It is important to keep the ampoules at a temperature of no more than +25 degrees and at least +15 degrees. Never put Atropine in the refrigerator. It is important that children cannot get the medicine and take it internally. The shelf life of ampoules is no more than 3 years from the date of production. It is forbidden to inject if Atropine is expired.

Drug price

Atropine can now be purchased in ampoules at any pharmacy. Some pharmacists will require a prescription from a doctor with an accurate dosage. The average price for a drug is from 70 to 90 rubles. For this cost, you can purchase 1 ampoule of a 0.1 percent solution.

Composition and release form of the drug

1 ml - ampoules (10) - cardboard boxes.
1 ml - ampoules (5) - contoured plastic packaging (1) - cardboard packs.
1 ml - ampoules (5) - contoured cell packs (1) - cardboard packs.

pharmachologic effect

Blocker of m-cholinergic receptors, is a natural tertiary amine. It is believed that atropine binds equally to the m 1, m 2 and m 3 subtypes of muscarinic receptors. 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, 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 moderate therapeutic doses, atropine has a moderate stimulating effect on the central nervous system and a delayed but long-term sedative effect. The central anticholinergic effect explains the ability of atropine to eliminate tremors in Parkinson's disease. In toxic doses, atropine 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), an increase in conduction in the His bundle.

In therapeutic doses, atropine has no significant effect on peripheral vessels, but in case of an overdose, vasodilation is observed.

When applied topically in ophthalmology, the maximum dilation of the pupil occurs in 30-40 minutes and disappears after 7-10 days. Mydriasis caused by atropine is not eliminated by 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 the BBB. A significant concentration in the central nervous system is achieved within 0.5-1 hours. The protein binding is moderate.

T 1/2 is 2 hours. It is 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 surgery; AV block, bradycardia; poisoning with m-cholinomimetics and anticholinesterase substances (reversible and irreversible action); X-ray examination of the gastrointestinal tract (if necessary, to reduce the tone of the stomach and intestines).

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

For the purpose of intramuscular premedication for 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 application is up to 3 times with an interval of 5-6 hours, depending on the indications. In some cases, a 0.1% solution is injected subconjunctivally 0.2-0.5 ml or parabulbarly - 0.3-0.5 ml. Using the electrophoresis method through the eyelids or an eye bath, a 0.5% solution is injected from the anode.

Side effects

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

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

Drug interactions

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

When used simultaneously 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, decrease the absorption of nitrofurantoin and its excretion by the kidneys. Probably an increase in the 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 action 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 the blood 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, coronary artery disease, mitral stenosis, arterial hypertension, acute bleeding; with thyrotoxicosis (possibly increased tachycardia); at elevated temperatures (may increase further due to suppression of the activity of sweat glands); with reflux esophagitis, hernia of the esophageal opening of the diaphragm, combined with reflux esophagitis (decreased motility of the esophagus and stomach and relaxation of the lower esophageal sphincter can slow down 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 (possibly decreased motility and tone, leading to obstruction and retention of stomach contents), intestinal atony in elderly patients or debilitated patients (obstruction may develop), paralytic intestinal obstruction; with an increase in intraocular pressure - angle-closure (the mydriatic effect, leading to an increase in intraocular pressure, can cause an acute attack) and open-angle glaucoma (the mydriatic effect may cause a slight increase in intraocular pressure; correction of therapy may be required); with nonspecific ulcerative colitis (high doses can inhibit intestinal motility, increasing the likelihood of paralytic intestinal obstruction, in addition, the manifestation or exacerbation of such a severe complication as toxic megacolon is possible); with dry mouth (prolonged use may further increase the severity of xerostomia); with liver failure (decreased metabolism) and renal failure (risk of side effects due to reduced excretion); with 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 congestion 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 predisposition to it, or diseases accompanied by urinary tract obstruction (including bladder neck due to prostatic hypertrophy); with gestosis (possibly increased arterial hypertension); brain damage in children, cerebral palsy, Down's disease (the reaction to anticholinergic drugs increases).

The interval should be at least 1 hour between atropine and antacids containing aluminum or calcium carbonate.

With subconjunctival or parabulbar administration of atropine, the patient must be given a pill under the tongue in order to reduce tachycardia.

Influence on the ability to drive vehicles and mechanisms

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

Pregnancy and lactation

Atropine crosses the placental barrier. Adequate and strictly controlled clinical studies of the safety of atropine use during pregnancy have not been conducted.

With intravenous administration during pregnancy or shortly before childbirth, the development of tachycardia in the fetus is possible.

Atropine is found in human 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 may develop), with prostatic hypertrophy without urinary tract obstruction, urinary retention or 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 the H-cholinergic receptors), as a result of which M-cholinergic receptors become insensitive to acetylcholine, which is formed in the area 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 gives it an affinity with the endogenous ligand molecule, acetylcholine. Atropine sulfate reduces the secretion of 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 the stimulated secretion, vira eno dilates the pupil (with a possible increase in intraocular pressure). Penetrating through the blood-brain barrier, atropine in therapeutic doses stimulates 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 quickly distributed in the body, penetrates the blood-brain, placental barrier and into breast milk. In the blood, atropine binds to proteins by 50%, 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 gastric ulcer and duodenal ulcer, 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 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 laryngospasm, reduces glandular secretion, reflex reactions and side effects caused by excitation of the vagus nerve. As a specific antidote for poisoning with cholinomimetic compounds and anticholinesterase (including organophosphate) 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. Hyperthermic syndrome. Diseases of the digestive system, accompanied by obstruction (achalasia of the esophagus, pyloric stenosis, intestinal atony). Glaucoma. Hepatic and renal failure. Myasthenia gravis gravis... Retention of urine or a predisposition to it. Brain damage.

Interaction with other medicinal products and other forms of interaction

When atropine sulfate is used with MAO 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.

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

With simultaneous use with diphenhydramine or diprazine, the effect of atropine increases, with nitrates, haloperidol, GCS for systemic use - the likelihood of increased 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 is reduced, with ascorbic acid and attapulgite - the effect of atropine is reduced, with pilocarpine - the effect of pilocarpine in the treatment of glaucoma is reduced, with oxprenolone - the antihypertensive effect of the drug decreases. Under the action of octadine, it is possible to reduce the hyposecretory action of atropine, which weakens the action of M-cholinomimetics and anticholinesterase agents. With simultaneous use with sulfonamide drugs, the risk of kidney damage increases, drugs containing potassium - the formation of intestinal ulcers is possible, with nonsteroidal anti-inflammatory drugs - the risk of stomach ulcers and bleeding.

The effect of atropine sulfate can be enhanced with the simultaneous use of other drugs with an antimuscarinic effect (M-anticholinergics, antispasmodics, amantadine, some antihistamines, drugs of the group of butyrophenones, phenothiazines, dispiramidives, quinidine, tricyclic antidepressants, non-selective uptake inhibitors of monoamine inhibitors). The inhibition of peristalsis under the action of atropine can lead to a change in the absorption of other drugs.

Application features

Use with caution in patients with prostatic hypertrophy without urinary tract obstruction, with Down's disease, with infantile cerebral palsy, reflux esophagitis, hiatal hernia, combined with reflux esophagitis, ulcerative colitis, elderly patients, patients with Xer or debilitated patients, with chronic lung diseases without reversible obstruction, with chronic lung diseases occurring with low production of thick sputum, which is difficult to separate, especially in young children and debilitated patients, with autonomic (autonomic) 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 or driving other mechanisms

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

Method of administration and dosage

Atropine sulfate is administered subcutaneously, intramuscularly, intravenously. With induction of anesthesia in order to reduce the risk of inhibition of the heart rate by the vagus 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 morphine sulfate) - at 1:00 am before anesthesia. In case of poisoning with anticholinesterase drugs atropine sulfate, inject 2 mg intramuscularly every 20-30 minutes until redness and dryness of the skin occurs, pupil dilation and tachycardia appear, and normalization of breathing. In moderate to severe poisoning, atropine can be administered within two days (until signs of "re-atropinization" appear).

For children, the highest single dose is:

  • up to 6 months - 0.02 mg
  • at the age from 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 associated with the M-anticholinergic effect of atropine.

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

From the urinary system: difficulty and retention of urination.

On the part of the cardiovascular system: tachycardia, arrhythmia, including extrasystole, myocardial ischemia, facial redness, hot flashes.

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

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

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

On the part of the skin: rash, urticaria, exfoliative dermatitis.

Manufacturer

LLC "Kharkiv Pharmaceutical Enterprise" People's Health ".