The mechanism of action of atropine

Atropine is a substance that is a very famous alkaloid with a natural origin (a component of some plants). And, although it is quite actively used in medicine, it belongs to dangerous toxic substances (children are at risk). It is enough to eat belladonna berries common in our area.

belladonna extract

Further in the article you will learn about the use and effect of atropine on the human body, as well as how to determine poisoning and how to deal with it.

Dangerous alkaloid

So what is atropine? This substance belongs to the group of alkaloids. The term alkaloid means a heterocyclic base containing a nitrogenous group and exhibiting biological activity in some plants. Simply put, these are compounds that can act one way or another on a living organism. One plant may contain several alkaloids.

Plants containing atropine: henbane, datura, belladonna (belladonna), scopolia and other species from the nightshade family.

plant poison

Description

The substance is a natural poison, however, the use of a small dosage of atropine is widespread in the medical field.

The chemical structure of the alkaloid classifies it as crystalline powders. This substance is amorphous, colorless and odorless. He has two isomers. Hyoscyamine is a levorotatory, which is more active in comparison with atropine. It is hyoscyamine that is part of plants, but when it is chemically excreted, it turns into atropine.

Mechanism of action

The alkaloid in question interferes with the conduction of a nerve impulse by blocking receptors. It turns out that he is a competitor of the body's natural substance (acetylcholine), in the ability to bind to sensitive endings during the pulse. Sensitive endings are of two types: H and M. Only the latter is blocked by a dangerous alkaloid.

release form

The mechanism of action of atropine is that instead of acetylcholine it binds to specific formations of nerve cells.

Various effects are observed depending on the zone of exposure of the substance:

  1. Relaxation of smooth muscle cells - is noted in the gastrointestinal tract, bronchi, bladder. This effect is due to inhibition of impulses of the parasympathetic nervous system.
  2. Reduction of secretory activity of endocrine glands, including bronchial, digestive, sweat, salivary, lacrimal. The suppressing effect of atropine in these cases is explained by blockade of the sympathetic nervous system (lacrimal, sweat) and parasympathetic (bronchial, digestive).
  3. Mydriasis or dilated pupils. Being antagonists, the radial and circular muscles of the iris balance each other. The circular muscle of the iris relaxes due to the binding of atropine to M3-cholinergic receptors, and the action of the radial muscle predominates, it is tense, which leads to the expansion of the pupil.
  4. Paralysis of accommodation. The relaxing effect of atropine on the ciliary muscle of the eye leads to flattening of the lens, which causes hyperopia.
  5. Increased heart rate occurs due to inhibition of parasympathetic effects on the sinoatrial node. Sometimes bradycardia (the heart rate decreases) may precede an increase in the heart rate, which is caused by stimulation of the vagus centers.
  6. A large dosage of the substance affects the vessels of the human body: they expand, and the skin turns red. Small doses of atropine do not contribute to vasodilation, but may interfere with the action of other drugs aimed at vasodilation.

Indications for use of atropine

At the moment, there are three forms of release of the drug, the active substance of which is the belladonna alkaloid:

  1. Atropine in the form of tablets.
  2. "Atropine sulfate" - a one percent solution of atropine for injection in ampoules of 1 ml.
  3. "Atropine sulfate" - one percent eye drops in 5 ml plastic dropper bottles.

This drug is widely used in clinical practice. It is prescribed for gastroenterological purposes:

  • relaxing effect with cramps of the pyloric sphincter of the stomach;
  • suppression of gastric secretion in ulcers of the stomach and duodenum;
  • drainage of stagnant bile and expansion of the ducts with gallstone disease and inflammation of the gallbladder.

Indications for use of atropine in other branches of medicine:

  • with bronchial asthma (eliminates bronchospasm);
  • to reduce the secretion of sweat, lacrimal, salivary glands;
  • with spasms of the bladder;
  • with a decrease in heart rate associated with vagal tone (carefully, may cause a short-term increase in bradycardia);
  • with increased sweating;
  • for sedation and anesthesia in anesthesiology, during intubation, operations to eliminate bronchospasm and laryngospasm, to reduce salivation;
  • to reduce gastric tone during radiography.

Where else is atropine used? It is an antidote if the body is poisoned with organophosphorus compounds / poisons, it is also used in case of an overdose of anticholinesterase and cholinomimetic drugs. In addition, the form of release of atropine in ampoules is used in ophthalmology to expand the pupil in studies of the fundus.

atropine ampoule

Dosage and Administration

Atropine is administered orally, intravenously and intramuscularly, in the form of eye drops or subcutaneously. According to the recommendation and medical reviews, Atropine tablets are prescribed from 0.25 to 1 mg up to three times a day. Dosage variation is determined by an individual approach in the preparation of the prescription for each individual patient.

use of atropine

Intramuscularly, intravenously and subcutaneously - a similar dosage, only up to two times a day.

Eye drops should be instilled in the following order: 1-2 drops three times a day. For the expansion of the pupil for research purposes - two drops 1-2 times. The dose of atropine at one time should not exceed 1 mg, per day - no more than 3 mg.

The severity of the manifestations of atropine poisoning depends on its nature - accidental or targeted. Usually people get poisoned after accidentally consuming fruits from the nightshade family.

Overdose Signs

45-60 minutes after taking the drug, the toxic effect of atropine begins to appear. According to the dosage, the degree of poisoning can be mild, moderate or severe. The substance affects primarily the structure of the brain (psychosis, hallucinations, impaired coordination), only then the lungs and heart suffer.

atropine drops

Symptoms of an atropine overdose:

  • redness of the mucous membranes;
  • dry mouth
  • sweating reduction;
  • palpitations, arrhythmia;
  • vomiting, nausea;
  • tremor of limbs;
  • visual impairment;
  • redness of the skin;
  • rapid breathing;
  • constipation
  • difficulty swallowing, hoarseness;
  • cramps.

All of the above symptoms appear with an unintentional overdose.

Targeted poisoning with plant poison has more serious symptoms:

  • hallucinations;
  • unconsciousness;
  • coma;
  • paralysis of the respiratory muscles;
  • decreased heart rate, ventricular or atrial fibrillation.

The registered lethal dosage of atropine ranges between 100-150 mg or 1-1.5 mg per kilogram of body weight.

If you count in belladonna berries, then 4-6 pieces can cause a child to die, which occurs no earlier than five hours after consuming plant poison.

There may be other consequences. If a person has been in a coma for a long time, memory and intelligence may atrophy due to irreversible organic changes in the brain.

How to save the poisoned?

Poisoning with plant poison is treated, first of all, by washing the stomach with water, saline laxatives (magnesium sulfate) or potassium permanganate. It is necessary to immediately give the one who poisoned the antidote of atropine. Among them: a solution of aminostigmine one percent (2 mg), a solution of galantimine half percent (drug "Nivalin" - 2 mg).

The introduction should be repeated after 90 minutes. The stronger the poisoning, the shorter the interval between antidote doses. The most severe cases require the introduction of funds every 15 minutes.

More on the effects of antidotes

Aminostigmine helps to quickly restore consciousness, eliminate psychomotor agitation and hallucinations. It is used not only in cases of overdose, it is often used to prevent recurrence of coma.

Another atropine antagonist is the alkaloid pilocarpine. On its basis, drugs (eye drops) are created that are used in ophthalmology as a means to reduce intraocular pressure. Expanding the pupil, atropine can cause glaucoma. Inside the eyeball, elevated pressure can lead to retinal detachment. In cases of poisoning by plants or preparations containing atropine, it is necessary to immediately introduce pilocarpine according to the following scheme:

  • for an hour, 1 drop in each eye every 15 minutes;
  • in the next two hours you need to drip 1 drop of the drug in 30 minutes;
  • the next six hours, you need to drip 1 drop per hour;
  • then one drop should be dripped per day every seven hours (until the high intraocular pressure drops).

Medication price

Atropine in the form of tablets and ampoules is an affordable drug in any pharmacy, however it is issued strictly according to the prescription. At the pharmacy, pharmacists may require the appointment of a doctor with exact dosages. The form of release in ampoules costs 70-90 rubles (the cost of one ampoule of a one percent solution) depending on the region. The price of Atropine in the form of tablets varies around 20 rubles.

Reviews

As they say, those who have tried the action of atropine on themselves, it can be used to completely relax the eyes.

atropine sulfate for eyes

However, it should be borne in mind that after its use the visual function is violated (for a maximum of two days). As some people note, as a result of the use of atropine, pain in the eyes appeared, the cause of which was increased intraocular pressure. At the moment, there are a number of analog drugs with a more effective and safe effect. Many buyers claim that atropine is an obsolete medicine. Others agree with this opinion, but are in favor of the drug, since it performs its function properly and, in comparison with the latest innovations, is much more reliable. And the price of atropine is relatively small. According to recent reviews, atropine can cause an allergic reaction. Some children feel bad: their skin and eyes turn red. In such cases, immediate medical attention is needed.

Summarizing

Atropine, as mentioned earlier, is an alkaloid of plants in the nightshade family.

This anticholinergic drug is widely used in medicine. It is used in toxicology, gastroenterology, pulmonology, ophthalmology, anesthesiology, cardiology.

A severe overdose of atropine can occur with the use of belladonna or a large amount of the drug. The degree of poisoning depends on the amount of substance taken. 100 mg of atropine is fatal. Aminostigmine and galantamine are specific antidotes that must be taken immediately (administered repeatedly intravenously). Coma, impaired memory and intelligence - all these are consequences of atropine poisoning.


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