Cholinesterase reactivators: drugs, mechanism of action. Antidote for organophosphate poisoning

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Cholinesterase reactivators: drugs, mechanism of action. Antidote for organophosphate poisoning
Cholinesterase reactivators: drugs, mechanism of action. Antidote for organophosphate poisoning

Video: Cholinesterase reactivators: drugs, mechanism of action. Antidote for organophosphate poisoning

Video: Cholinesterase reactivators: drugs, mechanism of action. Antidote for organophosphate poisoning
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Cholinesterase reactivators are antidotes that help relieve organophosphate (OP) poisoning. Toxic compounds containing phosphorus include chemical warfare agents such as sarin, tabun. However, it is possible to get intoxication with such chemical compounds in peacetime. On the basis of FOS, many means have been created to combat harmful insects ("Dichlorvos", "Thiophos", "Chlorophos"), as well as some eye drops ("Armin", "Phosfakol"). Similar compounds are also used in industry in the production of plastics and varnishes. In case of accidental ingestion of such substances into the body, severe poisoning occurs. And then cholinesterase reactivators come to the rescue.

How do FOS work on the body?

A group is formed in the human bodyenzymes - cholinesterase. They play an important role in metabolic processes and the functioning of the nervous system. Phosphorus organic compounds, getting into the body, inhibit the activity of these enzymes. Acetylcholine begins to accumulate in the tissues. An excess of this substance leads to the following symptoms of intoxication:

  • increased salivation;
  • noisy breathing with wheezing due to phlegm in the bronchi;
  • constricted pupils;
  • convulsions;
  • cyanosis of the skin;
  • muscle paralysis;
  • high BP;
  • "chemical" breath odor;
  • excessive sweating.

FOS act on the body as a nerve poison. Intoxication with such substances is extremely dangerous. Possible death due to paralysis of the respiratory muscles. In the photo below you can see a sharp narrowing of the pupils in case of poisoning with FOS.

cholinesterase reactivators
cholinesterase reactivators

How do cholinesterase reactivators work?

In case of FOS poisoning, cholinesterase reactivating drugs act as an antidote. This means that they are antidotes for toxic phosphorus compounds. They can be used in the treatment of poisoning. They are able to quickly neutralize the poison and remove signs of intoxication.

the antidote is
the antidote is

The mechanism of action of cholinesterase reactivators lies in their ability to restore the activity of enzymes. The composition of such drugs contains a group of molecules -NOH, which interacts with blocked acetylcholinesterase. As a result, links betweenFOS molecules and an enzyme. Thus, the activity of cholinesterase is completely restored under the action of the antidote. This leads to the gradual disappearance of the symptoms of intoxication.

drugs for poisoning
drugs for poisoning

Types of drugs

The following medicines belong to the group of cholinesterase reactivators:

  • "Dipiroxime".
  • "Dietixim".
  • "Alloxim".
  • "Carboxyme".
  • "Isonitrosin".

The indication for their use is organophosphate poisoning. However, blocking of cholinesterase also occurs during intoxication with drugs from the group of cholinomimetics. The above drugs in case of poisoning by other means are ineffective. They only work against FOS.

cholinesterase reactivators drugs
cholinesterase reactivators drugs

There are no contraindications to the use of cholinesterase reactivators.

Drug descriptions

FOS antidotes are available as injectable solutions. These are fast acting drugs. Cholinesterase reactivators begin to unblock enzymes 15-30 minutes after administration. "Isonitrozin" is a more effective drug. It is able to stop the damage to the central nervous system caused by FOS. "Dipiroxime" does not penetrate the brain. For this reason, the drug is only able to neutralize the poison, but to a lesser extent affects the symptoms of intoxication.

Recommended dosage

Drugs in case of poisoning must be administeredas soon as possible when early symptoms appear. They are effective only in the first hours after the poison enters the body. Their dosage depends on the severity of intoxication:

  1. At the initial signs of poisoning, 2-3 ml of atropine solution (0.1%) and FOS antidotes are injected under the skin, their dosage is determined by the instructions for use of each drug. If the manifestations of intoxication do not disappear, then the introduction of cholinesterase and atropine reactivators is repeated.
  2. In severe poisoning, 3 ml of atropine and FOS antidotes are injected into a vein. Atropine is administered every 5 minutes until wheezing disappears and the amount of mucus in the respiratory organs decreases. Injections are stopped when dry mouth appears and pupils dilate. These are signs of the effects of atropine on the body. If necessary, enzyme reactivators are administered again.
cholinesterase reactivators mechanism of action
cholinesterase reactivators mechanism of action

On the second day after poisoning, drugs are not administered. This can lead to the development of side effects and re-exacerbation of the symptoms of intoxication. During antidote therapy, it is necessary to control the level of cholinesterase activity. Usually, 2-3 days after the start of therapy, enzymatic function begins to recover. A week later, cholinesterase activity doubles.

Side effects

FOS antidotes are strictly prescription drugs. They not only cannot be taken without the appointment of a specialist, but should not be used at home. These drugs can only be used in a hospital under supervision.doctor. They are exclusively for hospital treatment of organophosphate poisoning.

Both remedies have severe side effects. They can cause a drop in blood pressure, tachycardia, and impaired liver function. A severe condition called "cholinergic arousal" may develop with restlessness, delusions, and hallucinations.

If a person accidentally swallowed an organophosphorus substance, it is necessary to call a doctor as soon as possible and provide first aid to the victim. The patient's stomach is washed with a solution of potassium permanganate and activated charcoal is given. If the substance enters the body through the respiratory system, you need to take the person to fresh air and rinse the nasal passages. If the poison is on the skin, then it must be washed off with soap and water.

Further assistance will be provided to the patient in the hospital, only under the supervision of a doctor can therapy be carried out using antidotes. This means that it is impossible to completely remove the signs of FOS poisoning at home. It must be remembered that antidotes are effective only in the first hours after intoxication. The sooner an ambulance is called, the greater the chances for successful treatment and recovery.

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