Cholinolytics (also known as cholinolytic and anticholinergic drugs) are a large group of substances with various uses. Their common feature is the mechanism of action of blocking the neurotransmitter acetylcholine. Therefore, drugs of this nature will have similar side effects. In what diseases are cholinolytics used? What are the disadvantages of taking these substances?

Allcholinolyticsexhibit activities opposite to acetylcholine. This name covers a diverse group of substances.

The group of cholinolytics functions under many other names. This can sometimes be confusing when reading the information about the drug. Other terms are:

  • anticholinergics
  • parasympatykolityki
  • cholinolytic drugs
  • anticholinergic drugs
  • muscarinic receptor antagonists

Drugs, poisons and drugs belong to the group of cholinolytics. All these chemical compounds have a common mechanism of action.

It may seem disturbing that a therapeutic preparation that we buy in a pharmacy affects the body in a similar way to a lethal poison. However, don't worry about it.

The safety of the drug depends on its dose. Even inconspicuous vitamin C, if eaten enough of it, can seriously damage the kidneys.

Due to the fact that cholinolytics have stimulating properties towards the central nervous system, they are used as drugs as well as drugs in neurodegenerative diseases.

The effect of anticholinergic therapeutic preparations on the brain is strong, therefore their use requires great caution.

A toxic reaction known as acute anticholinergic syndrome may occur after large amounts of the anticholinergic drug have been ingested. This can happen accidentally by a patient's mistake. Drugs of this nature are also deliberately overdosed, as their high dose can bring you into a state of narcotic intoxication.

Cholinolytics - indications

Cholinolytics are used in the treatment of various and unrelated diseases. We can list the following diseases in which the properties are usedthese drugs:

  • dizziness, including those related to motion sickness
  • gastrointestinal disorders: ulcers, diarrhea, pyloric spasm, diverticulitis, ulcerative colitis, nausea and vomiting
  • urogenital disorders: cystitis, urethritis and prostatitis.
  • insomnia
  • respiratory system disorders: asthma, chronic bronchitis and chronic obstructive pulmonary disease
  • sinus bradycardia
  • Parkinson's disease
  • poisoning with substances belonging to the group of sympathomimetics, e.g. organophosphate pesticides. Cholinolytics have opposite properties to sympathomimetics and therefore act as an antidote.

Substances with cholinolytic properties are also used in diagnostics and anesthesiology. Atropine, belonging to this group, is used in ophthalmology to dilate the pupil before the examination.

Most cholinolytics block the production of saliva by the salivary glands and are somewhat sedative. Both of these properties are beneficial when preparing a patient for a surgical procedure.

Cholinolytics - sample medications

Atropine- is used in ophthalmology to dilate the pupil of the eye. It is also used as an antidote in cases of poisoning with organophosphorus pesticides. It is administered in the spastic states of the gastrointestinal tract, ureters and bile ducts. Due to the fact that it inhibits bronchospasm and secretory activity in the respiratory tract, it is used in anesthesiology.

This substance belongs to the tropane alkaloids and occurs naturally in plants, e.g. in wolfberry ( Atropa belladonna ) and datura ( Datura stramonium). Often there is poisoning with these plants. The hry has blueberries that can be eaten by a child.

Both plants are used for narcotic purposes, which can also lead to life-threatening conditions.

Scopolamine- just like atropine, it is a substance found in plants. It has a depressant effect on the central nervous system, causing drowsiness and dementia. In the past, it was used in the treatment of asthma. Currently, a derivative of this substance, i.e. N-butylscollamine bromide, is used more often in medicine. It has antiemetic properties.

Trihexyphenidyl ,prydinol ,biperiden- used in the treatment of Parkinson's disease. They reduce muscle stiffness and tremorsbodies involved in this disease.

Ipratropium bromide- is a substance used in the treatment of bronchial asthma. The drug is administered topically into the bronchi to dilate them and prevent spasms.

Pirenzepine- an organic chemical compound used in peptic ulcer disease.

Cholinolytics - the mechanism of action of cholinolytic substances

Cholinolytics block the activity of the neurotransmitter acetylcholine in nerve synapses. These substances inhibit the flow of nerve impulses in the parasympathetic system.

Parasympathetic conductivity is responsible for bringing the body into a state of rest and digesting food. Acetylcholine stimulation of receptors in nerve synapses results in:

  • miosis
  • increased salivation
  • bronchoconstriction
  • dilatation of blood vessels
  • drop in blood pressure
  • intensification of peristalsis in the digestive tract

Since anticholinergics block the activity of acetylcholine, they act to inhibit the parasympathetic system. As a result, substances from this group will be:

  • dilate pupils - which is used in ophthalmology
  • reduce salivation - this reaction is, on the one hand, troublesome. undesirable cholinolytics, on the other hand, it is used in anesthesiology
  • dilate the bronchial tubes - this reaction is used to treat asthma
  • inhibit intestinal peristalsis and the secretion of digestive juices - therefore cholinolytics are used in the treatment of digestive system disorders

Due to the place of action in the nervous system, cholinolytics can be divided into:

  • antimuscarinic drugs
  • coil blockers
  • neuromuscular blockers

Drugs with the opposite mechanism of action to cholinolytics are parasympathomimetics. The latter antagonist group of drugs can therefore be used as an antidote in the case of poisoning with cholinolytic substances.

Cholinolytics - side effects

Although cholinolytics are used in many different diseases that are independent of each other, the side effects in the whole group are similar. The typical inconveniences associated with taking these medications are:

  • dilated pupils
  • slow bowel movement
  • dry mouth
  • dry mucous membranes
  • hallucinations
  • psychomotor agitation
  • delirium
  • low fever

The same body reactions to cholinolytics for somemedical situations can be beneficial, while for others they can be bothersome side effects. An example of this is the inhibition of saliva secretion that is usually uncomfortable for patients with dry mouth.

In anesthesiology, this property of anticholinergics is useful and is used to prepare the patient for surgery.

Poisoning with cholinolytics

The state of intoxication with cholinolytic substances is called an acute anticholinergic syndrome. It is a reversible condition. Symptoms pass when the cholinolytic is expelled from the body.

The state of poisoning with these substances leads to intense reactions from the central nervous system. The characteristic symptoms are:

  • hallucinations
  • entanglement
  • psychomotor agitation

In addition, peripheral reactions such as dry mucous membranes and dilation of the pupils appear. The condition is rarely described as pleasant, but cases of intentional narcotic overdose of cholinolytics are frequent. The usual antidote is physostigmine, which increases the concentration of acetylcholine in the body by blocking its breakdown. However, this substance is recommended for use only in life-threatening situations.

This is due to the fact that the use of physostigmine can lead to serious side effects such as:

  • convulsions
  • vomiting
  • bradycardia
  • excess saliva production

In many cases, the antidote can make the body worse.

Cholinolytic poisoning usually occurs after ingesting drugs or poisonous plants.

Plant cholinolytic substances

Compounds with cholinolytic activity are characteristic of plants from the familySolanaceae .

The substances found in them are anticholinergic tropane alkaloids such as scopolamine, atropine and hyoscyamine. Examples of plants containing cholinolytics are:

  • Atropa belladonnaL. - hryvnia wolfberry
  • Datura stramoniumL. - Datura Dziedzierzawa
  • Hyoscyamus nigerL. - black hen

These plants are, on the one hand, dangerous poisons, and on the other hand, they can be used for the production of effective drugs.

About the authorSara Janowska, MA in pharmacyPhD student of interdisciplinary doctoral studies in the field of pharmaceutical and biomedical sciences at the Medical University of Lublin and the Institute of Biotechnology in Białystok.in Lublin with a specialization in herbal medicine. She obtained a master's degree defending a thesis in the field of pharmaceutical botany on the antioxidant properties of extracts obtained from twenty species of mosses. Currently, in his research work, he deals with the synthesis of new anti-cancer substances and the study of their properties on cancer cell lines. For two years she worked as a master of pharmacy in an open pharmacy.

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