Mechanism of action of atropine

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Mechanism of action of atropine
Mechanism of action of atropine

Video: Mechanism of action of atropine

Video: Mechanism of action of atropine
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Atropine is a very well-known naturally occurring alkaloid (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 just to eat belladonna berries, common in our area.

belladonna extract
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 identify poisoning and how to deal with it.

Dangerous alkaloid

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

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

vegetable poison
vegetable poison

Description

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

The chemical structure of the alkaloid classifies it as a crystalline powder. This substance is amorphous, colorless and odorless. It has two isomers. Hyoscyamine is a levorotary, which is more active than atropine. It is hyoscyamine that is part of the composition of plants, but when chemically released, it turns into atropine.

Mechanism of action

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

release form
release form

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

Different effects are observed depending on the area of exposure to the substance:

  1. Relaxation of smooth muscle cells - observed in the gastrointestinal tract, bronchi, bladder. This effect is due to the inhibition of impulses of the parasympathetic nervous system.
  2. Reduction of secretory activity of endocrine glands, including bronchial, digestive, sweat, salivary, lacrimal. The suppressive effect of atropine in these cases is due to the blockade of the sympatheticnervous system (lacrimal, sweat) and parasympathetic (bronchial, digestive).
  3. Mydriasis or dilated pupils. Being antagonists, the radial and circular muscles of the iris of the eye balance each other. The orbicular 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 pupil dilation.
  4. Paralysis of accommodation. The relaxing effect of atropine on the ciliary muscle of the eye causes the lens to flatten, resulting in farsightedness.
  5. The increase in heart rate occurs due to the inhibition of parasympathetic action on the sinoatrial node. Sometimes bradycardia (reduced heart rate) may precede an increase in heart rate, which is caused by stimulation of the vagal centers.
  6. A large dosage of a substance affects the vessels of the human body: they expand, and the skin turns red. Small doses of atropine do nothing to dilate blood vessels, but may interfere with other vasodilating drugs.

Indications for the use of atropine

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

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

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

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

Indications for the use of atropine in other branches of medicine:

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

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

ampoule of atropine
ampoule of atropine

Dosage and methods of administration

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

use of atropine
use of atropine

Intramuscular, intravenous and subcutaneous - the same dosage, only up to two times a day.

Eye drops should be instilled in the following order: 1-2 drops three times a day. To dilate 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 manifestations of atropine poisoning depends on its nature - accidental or purposeful. Usually, people get poisoned after accidentally eating fruits of the nightshade family.

Signs of an overdose

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, first of all, the structure of the brain (psychosis, hallucinations, impaired coordination), only then the lungs and heart suffer.

atropine drops
atropine drops

Atropine overdose symptoms:

  • redness of mucous membranes;
  • dry mouth;
  • reduce sweating;
  • palpitations, arrhythmia;
  • vomiting, nausea;
  • limb tremor;
  • visual impairment;
  • skin redness;
  • breathing;
  • constipation;
  • difficulty swallowing, hoarseness;
  • convulsions.

All of the above symptoms appear whenunintentional overdose.

Targeted plant poisoning has more severe symptoms:

  • hallucinations;
  • unconscious;
  • coma;
  • paralysis of respiratory muscles;
  • low heart rate, ventricular fibrillation or atrial fibrillation.

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

If counted in belladonna berries, then 4-6 pieces can cause death in a child, which occurs no earlier than five hours after the use of plant poison.

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

How to save a poisoned person?

Poisoning with vegetable poison is treated primarily by gastric lavage with water, saline laxative solutions (magnesium sulfate) or potassium permanganate. It is necessary to immediately give the one who has poisoned the antidote of atropine. Among them: a solution of aminostigmine one percent (2 mg), a solution of galantimin half a percent (drug "Nivalin" - 2 mg).

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

More about how antidotes work

Aminostigmine helps to quickly restore consciousness, eliminate psychomotor agitation andhallucinations. 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. Based on it, drugs (eye drops) are created and used in ophthalmology as a means to reduce intraocular pressure. By dilating the pupil, atropine can cause glaucoma. Inside the eyeball, increased pressure can lead to retinal detachment. In cases of poisoning by plants or preparations containing atropine, pilocarpine must be administered immediately 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 product every 30 minutes;
  • the next six hours you need to drip 1 drop per hour;
  • then one drop a day every seven hours (until high intraocular pressure subsides).

Price of medicines

"Atropine" in the form of tablets and ampoules is an affordable drug in any pharmacy, but it is issued strictly by prescription. In a pharmacy, pharmacists may require a prescription from a doctor with exact dosages. The release form 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 fluctuates around 20 rubles.

Reviews

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

atropine sulfate for eyes
atropine sulfate for eyes

However, it should be borne in mind that afterits use disrupts the function of vision (for a maximum of two days). Atropine has been reported by some people to cause eye pain due to increased intraocular pressure. At the moment, there are a number of analogues with a more effective and safe effect. Many buyers claim that atropine is an outdated medication. 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 become ill: the skin and eyes turn red. In such cases, immediate medical attention is needed.

Summing up

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

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

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

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