An antipsychotic is a special drug that is used for various mental disorders. As a rule, such drugs are used to treat neurotic syndromes, psychoses, and the medication can also be used for hallucinations. In addition, antipsychotic drugs are prescribed to prevent the main manifestations of a person's mental illness.

The main effects of the considered drugs

The effects of neuroleptics are multifaceted. The main pharmacological feature is a kind of calming effect, which is characterized by a decrease in response to external stimuli, a weakening of affective tension and psychomotor agitation, suppression of fear, and a decrease in aggressiveness. Antipsychotic drugs can suppress hallucinations, delusions and other psychopathological symptoms, have a therapeutic effect in patients suffering from schizophrenia and other psychosomatic ailments.

Certain drugs of this group have antiemetic activity, this effect of neuroleptics is achieved due to selective inhibition of chemoreceptor trigger (trigger) areas of the medulla oblongata. Some neuroleptics can have a sedative or activating (energizing) effect. A number of these funds are characterized by elements of normothymic and antidepressant action.

The pharmacological properties of various antipsychotic drugs are expressed to varying degrees. The combination of the main antipsychotic effect and other properties determines the profile of their impact and indications for use.

How do neuroleptics work?

Antipsychotics are drugs that depress the brain. The action of these drugs is also associated with the effect on the occurrence and conduction of excitation in various parts of the central and peripheral nervous system. Today, the most studied effect of neuroleptics is the effect on mediator processes in the brain. Scientists have accumulated enough data on the effects of these drugs on adrenergic, serotonergic, dopaminergic, cholinergic, GABAergic and other neurotransmitter processes, which include the effect on the neuropeptide systems of the brain. Particularly much attention has recently been paid to the process of interaction between dopamine brain structures and neuroleptics. With the inhibition of the mediator activity of dopamine, the main side effect of these drugs manifests itself, the so-called neuroleptic syndrome develops, which is characterized by extrapyramidal disorders, for example, such as involuntary muscle contraction, akathisia (restlessness), parkinsonism (tremor, muscle stiffness), motor restlessness, fever . This effect is achieved due to the blocking effect of neuroleptics on the subcortical formations of the brain, where a large number of receptors that are sensitive to dopamine are localized.

The manifested side effects of neuroleptics are a reason for correcting treatment and prescribing special correctors (drugs "Akineton", "Cyclodol").

Pharmacodynamics

An antipsychotic is a drug that, by acting on central dopamine receptors, provokes some endocrine disorders, including stimulation of lactation under their influence. When neuroleptics block the dopamine receptors of the pituitary gland, the secretion of prolactin increases. By acting on the hypothalamus, these drugs prevent the secretion of growth hormone and corticotropin.

Antipsychotics are drugs that have a relatively short half-life in the body and after a single administration they have a short effect. Scientists have created special preparations with a longer action (Moditen-Depot, Geloperidol Decanoate, Piportil L4, Clopixol-Depot). Often neuroleptics are combined with each other: in the first half of the day they take a stimulating drug, in the second - a sedative. In order to stop the affective-delusional syndrome, it is recommended to take antidepressants and antipsychotics in combination.

Indications for use

Antipsychotics are prescribed primarily for the treatment of nosogenic paranoid reactions (sensitive reactions) and in chronic somatoform pain disorder.

Rules for prescribing these drugs

Treatment with antipsychotics begins with the appointment of an average therapeutic dose, then the effect is evaluated and a decision is made on the need to change the dose. The dosage of antipsychotics is quickly increased to a certain value, which is subsequently gradually reduced by 3-5 times, and the therapy becomes anti-relapse, supportive. Change the prescribed amount of the drug strictly on an individual basis. Maintenance doses are switched after the desired therapeutic effect is achieved. It is more expedient to carry out anti-relapse therapy with drugs that have a prolonged action. The route of administration of psychotropic drugs is of great importance. At the initial stage of treatment, parenteral administration is recommended, in which the relief of symptoms occurs faster (intravenous jet, intravenous drip, intramuscular). Further, it is preferable to take antipsychotics orally. A list of the most effective drugs will be given below.

The drug "Propazine"

This tool has a sedative effect, reduces anxiety and motor activity. The drug is used for borderline disorders in patients with, if there are anxiety, phobic disorders, obsessions. Take the medicine inside 2-3 times a day, 25 mg, if necessary - the dose can be increased to 100-150 mg per day. When using small doses, the development of manifestations of parkinsonism, as a rule, is not observed.

The drug "Etaperazine"

The drug has an antipsychotic activating effect and affects syndromes that are characterized by lethargy, lethargy, apathy. In addition, the drug "Etaperazine" is used to treat neurosis, accompanied by tension, fear, anxiety. The daily dose of the drug is 20 mg.

Means "Triftazin"

The drug has a noticeable anti-delusional effect, stops hallucinatory disorders. The drug has a moderate stimulating (energizing) effect. It can be used in the treatment of atypical depressive states with the phenomenon of obsession. For the treatment of somatoform disorders, the drug "Triftazin" is combined with antidepressants and tranquilizers. The dosage of the drug is 20-25 mg per day.

The drug "Teralen"

The drug has antihistamine and neuroleptic activity. The drug "Teralen" is a mild sedative and has a positive effect on synestopathic-hypochondriac signs of the borderline register, with psychosomatic symptoms that develop against the background of infectious, somatogenic, vascular manifestations, with neurovegetative pathologies. It is widely used in gerontological practice and pediatrics. Recommended for use in allergic diseases and skin itching. The drug is taken orally at 10-40 mg per day, intramuscularly used in the form of a 0.5% solution.

Means "Tiridazine"

The drug has an antipsychotic effect with a calming effect, without causing lethargy and lethargy. Also, the drug has a moderate thymoleptic effect. The drug shows the greatest effectiveness in emotional disorders, which are characterized by tension, fear, excitement. In the treatment of borderline conditions, 40-100 mg of the drug is used per day. With such phenomena as neurasthenia, increased irritability, anxiety, neurogenic functional gastrointestinal and cardiovascular disorders, take the medicine 2-3 times a day, 5-10-25 mg. With premenstrual nervous disorder - 1-2 times a day, 25 mg.

The drug "Chlorprothixen"

The drug has an antipsychotic and sedative effect, enhances the effect of sleeping pills. A medication is used for psychoneurotic conditions characterized by fears, anxieties. The use of the drug is indicated for neurosis, including against the background of a variety of somatic ailments, in case of sleep disturbance, skin itching, subdepressive states. The dose of the drug is 5-10-15 mg, take the medicine after meals, 3-4 times a day.

The drug "Flyuanksol"

This remedy has an antidepressant, activating, anxiolytic effect. In the treatment of depressive, apathetic conditions take 0.5-3 mg of medication per day. For the treatment of psychosomatic disorders with subdepression, asthenia, hypochondriacal manifestations, the daily dose is 3 mg. Fluanxol does not cause daytime sleepiness and does not affect attention.

Means "Eglonil"

The drug has a regulatory effect on the central nervous system, has a moderate antipsychotic activity, which is combined with some stimulating and antidepressant effects. It is used in conditions that are characterized by lethargy, lethargy, anergy. It is used in patients with somatoform, somatized disorders on the background of subdepressive mood and in skin ailments accompanied by itching. This medication is especially indicated for use in patients who have a latent form of depression, senestopathic disorders. It is also recommended to use the drug "Eglonil" for depression with pronounced sensations such as dizziness and migraines. The tool also has a cytoprotective effect on the gastric mucosa, so it is used to treat conditions such as gastritis, duodenal ulcer and gastric ulcer, irritable bowel syndrome, Crohn's disease. The recommended dose of the drug is 50-100 mg per day, the daily dose, if necessary, can be increased to 150-200 mg. The drug can be taken in combination with sedative antidepressants.

Side effects of neuroleptics

Like any other medication, antipsychotics also have negative sides, the reviews of those who used such drugs indicate the possible development of undesirable effects. Long-term or incorrect use of these drugs can cause the following effects:

All movements are accelerated, a person moves for no reason in different directions, usually at high speed. You can get rid of calm down, find a comfortable position only after taking psychotropic drugs.

There is a constant movement of the eyeballs, facial muscles and various parts of the body, grimacing.

Due to damage to the muscles of the face, its features change. A “skewed” face may never return to its normal state, it may remain with a person until the end of his life.

As a result of intensive therapy with antipsychotics and depression of the nervous system, severe depression develops, which significantly affects the effectiveness of treatment.

An antipsychotic is a drug that has a direct effect on the gastrointestinal tract, therefore, during treatment with this medication, discomfort in the stomach and dry mouth may be felt.

Such substances that are part of neuroleptics, such as thioxanthene and phenothiazine, negatively affect human vision.

Atypical antipsychotics

These drugs act more on serotonin receptors than dopamine receptors. Therefore, their anti-anxiety and calming effect is more pronounced than antipsychotic. Unlike typical antipsychotics, they affect brain function to a lesser extent.

Consider the main atypical antipsychotics.

Medication "Sulpiride"

This drug is used to treat conditions such as somatized mental disorders, hypochondriacal, senestopathic syndromes. The drug has an activating effect of action.

The drug "Solian"

The action of this remedy is similar to the previous drug. It is used in conditions with hypobulia, apathetic manifestations, with the aim of stopping

Means "Clozapine"

The drug has a pronounced sedative effect, but does not cause depression. The drug is used in the treatment of catatonic and hallucinatory-delusional syndromes.

Means "Olanzalin"

The drug is used for psychotic disorders and catatonic syndrome. With prolonged use of this medication, obesity may develop.

The drug "Risperidone"

This atypical remedy is used most widely. The drug has an elective effect in relation to hallucinatory-delusional symptoms, catatonic symptoms, obsessive-compulsive states.

Means "Rispolept-consta"

This is a long-acting medication that ensures the stabilization of the well-being of patients. Also, the tool shows high efficiency in relation to acute endogenous genesis.

Medication "Quetiapine"

This drug, like other atypical antipsychotics, acts on both dopamine and serotonin receptors. It is used for paranoid, manic excitement. The drug has an antidepressant and moderately pronounced stimulating effect.

The drug "Ziprasidone"

The agent affects dopamine D-2 receptors, 5-HT-2 receptors, and also blocks the reuptake of norepinephrine and serotonin. This determines its effectiveness in the treatment of acute hallucinatory-delusional, as well as affective disorders. The use of the drug is contraindicated in arrhythmia and the presence of pathologies cardiovascular systems s.

Means "Aripiprazole"

The drug is used for all types of psychotic disorders. The drug contributes to the restoration of cognitive functions in the treatment of schizophrenia.

Means "Sertindol"

The drug is used for sluggish-apathetic conditions, the drug improves cognitive functions, has antidepressant activity. Sertindol is used with caution in cardiovascular pathologies - it can provoke arrhythmia.

The drug "Invega"

The drug prevents exacerbation of catatonic, hallucinatory-delusional, psychotic symptoms in patients with schizophrenia.

Side effects of atypical antipsychotics

The action of drugs such as Clozapine, Olanzapine, Risperidone, Ariprazol is accompanied by the phenomenon of neurolepsy and significant changes in the endocrine system, which can cause weight gain, the development of bulimia, and an increase in the level of certain hormones (prolactin). In the treatment of the drug "Clozapine" agranulocytosis may also occur. Taking Quetiapine often causes drowsiness, headaches, increased levels of hepatic transaminases, and weight gain.

It is worth noting that today scientists have accumulated enough information indicating that the superiority of atypical antipsychotics over typical ones is not so significant. And their reception is prescribed when, with the use of typical antipsychotics, a significant improvement in the patient's condition is not observed.

Antipsychotic withdrawal syndrome

Like any other drug with psychoactive properties, antipsychotic drugs cause a strong psychological and physical addiction. Abrupt withdrawal of the drug can provoke the development of severe aggression, depression. The person becomes too impatient, whiny. There may also be signs of a disease for which antipsychotics were used.

From a physiological point of view, the manifestations during the abolition of neuroleptics are similar to the symptoms during the abolition of drugs: a person is tormented by painful sensations in the bones, he suffers from headaches, insomnia. Nausea, diarrhea and other intestinal disorders may develop.

Psychological dependence does not allow a person to refuse to use these means, because he is tormented by the fear of returning to a gloomy, depressive life.

How to stop taking antipsychotics without disturbing the normal state of health? First of all, you should know that it is contraindicated to use antipsychotics without a doctor's prescription. Only an experienced specialist is able to adequately assess the patient's condition and prescribe the necessary treatment. Also, the doctor will give recommendations on reducing the dose of the medication consumed. The dosage of the drug should be reduced gradually, without causing a strong feeling of discomfort. Further, the specialist prescribes antidepressants that will support the patient's emotional state and will prevent the development of depression.

An antipsychotic is a medication that allows you to normalize a person's mental state. However, in order to avoid the development of side effects, be sure to follow the doctor's recommendations and do not self-medicate. Be healthy!

To date, very few people know anything about psychiatry, and, moreover, this topic is considered taboo in society.

While we are all surrounded people suffering from mental disorders.

One part of them is unaware of this, and the other is being treated, being under outpatient supervision by doctors who regularly prescribe powerful drugs which help to live normally in society. One type of such drug is neuroleptics.

Who prescribes antidepressants? Learn about it from ours.

What drugs are in this class?

Antipsychotics - what is it?

First of all, this class of drugs includes drugs intended for the treatment of various psychosis and other severe mental disorders.

These include a number of derivatives of phenothiazine, butyrophenone and diphenylbutylpiperidine.

Render very fast soothing effect, which complements the reduced response to external stimuli.

If the patient has or, then these symptoms are neutralized after taking the drug.

In Russian psychiatric realities, antipsychotics prescribed for almost all mental illnesses whatever etymology they may be. However, hallucinations are the most important indicator, since, first of all, the patient must be calmed down.

Mechanism of action

What are they for and how do they work? All antipsychotic drugs known to date have a similar mode of action in which the transmission of nerve impulses decreases in those parts of the brain where dopamine acts as a link.

That is, dopamine receptors themselves are blocked, and psychosis recedes. There are 4 main ways to block dopamine receptors:

Modern drugs are aimed at blockade of hormones not the entire dopamine series, but only certain receptors.

This approach allows you to get rid of most of the side effects and more competently deal with the disease.

What is an antipsychotic effect?

The effect is the effect that a neuroleptic has on the brain and general state sick.

That is, it is the removal of all actual psychotic symptoms that observed in the patient at the time of exacerbation.

In the event of psychosis or other mental disorders, such as an antipsychotic, for example, will help relieve symptoms and improve the general condition of the patient.

This must be done not only for health, but also for the safety of the person himself, so that he cannot harm himself and those around him, because often deliriums and other acute conditions are accompanied by hallucinations.

Indications and contraindications

The main reasons for the appointment are acute conditions in which the patient may be. Usually this hallucinations or delusions whatever they are caused by.

Anyway, here is a list of the main indications:

• schizophrenia;
• neurological disorders;
• dissociative disorders;
• affective insanity ();
• psychopathy;
• mania;
• alcoholic and narcotic delirium;
• apathy;

You should be careful with contraindications, because there is great risk of harm your health or someone close to you.

For example, almost all antipsychotics banned for glaucoma because it is possible to simply lose sight.

Contraindications:

• angle-closure glaucoma;
• prostate adenoma;
• porphyria;
• parkinsonism;
• diseases of the liver and kidneys;
• damage to the heart and blood vessels;
• acute fever;
• poisoning with drugs that depress the central nervous system;
• coma;
• pregnancy;
• lactation.

Classification

In the typology, 2 large groups are distinguished, which differ from each other in the mechanism of action. In fact, these are drugs of the old and new type.

Typical antipsychotics:

Atypical antipsychotics:

• clozapine;
• sulpiride;
• olanzapine;
• aripiprazole;
• risperidone.

In addition, "small" antipsychotics can be singled out as a separate group, since they do not fit into any of the above groups.

Their key difference is that they are, in fact, behavior correctors. have sedative and anti-anxiety effects. They do not help to cope with hallucinations and delusions, but fully complement therapy for anxiety disorders.

Usually antipsychotics are distributed in the form of tablets or ampoules for injection. On the this moment the only drug in the form of drops is presented on the market - Neuleptyl.

It belongs to the "typical" antipsychotics, and the convenient form of release is ideal for patients with an impaired swallowing reflex and who do not tolerate injections.

List of the most popular in alphabetical order

List of antipsychotics alphabetically:

Speaking about the power of antipsychotics, 2 drugs collide in the struggle for the title of the most potent - these are Clozapine (atypical group) and Thioproperazine (typical group). If the first has a powerful sedative effect, then the second is antipsychotic.

Speaking about the power of exposure, doctors distinguish another classification - clinical:

1. Strong Action: Amisulpride, Fluanxol, Haloperidol, Seroquel, Ziprasidone.
2. Medium action: Clozapine, Quetiapine, Sulpiride, Clopixol.
3. Weak action: Truxal, Tizercin, Floropipamide, Promethazine.
4. Prolonged action: Fluanxol Depot, Fluphenazine Decanoate (Dapotum, Liogen Depot).

Names of the best new generation drugs without side effects

Despite the rapid development of modern medicine, The pharmaceutical industry is practically in a dead end., since there are almost no "breakthrough" drugs on the market for psychotropic drugs that would be radically different from the previous ones.

However, there are several drugs that have been withdrawn unwanted side effects, which often accompany the use of neuroleptics.

These drugs almost no side effects:

• Abilify (aripiprazole);
• fluphenazine;
• Quetiapine;
• Fluanxol;
• Levomepromazine;
• Zeldox.

Leave without a doctor's prescription

There are very few antipsychotic drugs that dispensed without a prescription.

At the moment, the release of such drugs is very tightly controlled by the state as part of the fight against drugs.

This is controlled by the "List of narcotic drugs, psychotropic substances and their precursors subject to control in Russian Federation" from 1998.

Purchase or possession of drugs without a valid prescription from this list punishable under Article 228 of the Criminal Code of the Russian Federation.

However, there are medicines that can be bought without a prescription.

This Etaperazine, Paliperidone and Chlorprothixene.

Despite the free sale of these drugs in pharmacies, we would not recommend that you self-medicate, but consult with a specialist.

Harm

The prescription of such drugs should be strictly controlled and ensured by professional doctors, since antipsychotics, like any drugs, can harm the body. Especially when it comes to the human brain.

Antipsychotics have many opponents. Indeed, if the drug is prescribed in the wrong dosage or for some reason does not suit the patient, the patient's state of health obviously get worse.

The main harm that is done to the body comes from side effects, which, in fact, become independent diseases that were caused by taking antipsychotics. These are parkinsonism, depression, epilepsy, infertility, heart attack, jaundice and stroke.

In addition, the patient's brain experiences very serious stress in the "withdrawal syndrome" when, at the direction of the attending physician, the medication is stopped.

The effect of neuroleptics on the body is in many ways similar to narcotic, especially dependencies.

In case of failure from the drug, a person may experience emotional instability, depression, diarrhea, sleep disturbances, and body aches.

Like any drug group, antipsychotics have both opponents and defenders.

Anyway, can't do without their use., because they have not been demonstrating their effectiveness for the first decade. And thanks to the development of pharmacology, the side effects of drugs are reduced or disappear completely.

And finally: never self-medicate, take care of your nerves and your loved ones!

Briefly about the side effects of neuroleptics:

Antipsychotics (neuroleptics) ) have a calming, inhibitory and even depressing effect on the nervous system,

especially actively acting on the state of excitation (affective disorders), delirium, hallucinations, mental automatisms and other manifestations of psychosis. By chemical structure, they are derivatives of phenothiazine, thioxanthene, butyrophenone, etc. Antipsychotics are also divided into typical and atypical. Typical Antipsychotics are broad-spectrum drugs that affect all brain structures in which dopamine, norepinephrine, acetylcholine, and serotonin are mediators. This breadth of exposure will create a large number of side effects. Atypical neuroleptics do not show a pronounced inhibitory effect on the central nervous system.

Classification of neuroleptics

• 1. Typical antipsychotics.
• 1.1. Phenothiazine derivatives:
  • aliphatic derivatives: levomepromazine("Tizercin"), chlorpromazine("Aminazin"), alimemazine("Teraligen");
  • piperazine derivatives: perphenazine("Etaperazine"), trifluoperazine("Triftazin"), fluphenazine("Moditen Depot"), thioproperazine("Mazeptil");
  • piperidine derivatives: periciazine("Neuleptil"), thioridazine("Sonapax").
• 1.2. Butyrophenone derivatives: haloperidol, droperidol.
• 1.3. Indole derivatives: ziprasidone("Zeldox") sertindole("Serdolekg").
• 1.4. Thioxanthene derivatives: zuclopenthixol("Klopiksol"), flupentixol("Fluanxol"), chlorprothixene("Truksal"), zuclopenthixol("Klopiksol").
• 2. Atypical antipsychotics: quetiapine("Quentiax"), clozapine("Azaleptin", "Leponeks"), olanzapine("Zyprexa"), amisulpride("Solian"), sulpiride("Eglonil"), risperidone("Rispolept"), aripiprazole("Zilaksera").

The neurochemical mechanism of action of neuroleptics is associated with their interaction with dopamine brain structures. The effects of the dopaminergic system in normal and pathological conditions are shown in Fig. 4.13. The action of neuroleptics on the dopaminergic system of the brain causes antipsychotic activity, and the inhibition of central noradrenergic receptors (in particular, in the reticular formation) causes predominantly a sedative effect and hypotensive effects.

There are neuroleptics, the antipsychotic action of which is accompanied by a sedative (aliphatic derivatives of phenothiazine, etc.) action. Other antipsychotics are distinguished by an activating (energizing) effect (piperazine derivatives of phenothiazine). These and other pharmacological properties of different antipsychotic drugs are expressed to varying degrees.

Neuroleptic (calming) effect, accompanied by a decrease in reactions to external stimuli, a weakening of psychomotor arousal and affective tension, suppression of fear, a decrease in aggressiveness. The ability to suppress delusions, hallucinations, automatism and other psychopathological syndromes has a therapeutic effect in patients with schizophrenia and other mental illnesses.

Rice. 4.13.

In psychiatry, antipsychotics are effective in the treatment of a wide range of conditions, ranging from the short-term treatment of acute psychotic disorder, agitation in delirium and dementia, to the long-term treatment of chronic psychotic disorders such as schizophrenia. Atypical antipsychotics have largely replaced in clinical practice relatively outdated drugs of the phenothiazines, thioxanthenes and butyrophenones groups.

Antipsychotics in small doses are prescribed for non-psychotic diseases accompanied by agitation.

Let us consider in more detail the above neuroleptics.

Chlorpromazine("Aminazin") - the first drug of neuroleptic action, it gives a general antipsychotic effect, is able to stop the hallucinatory-paranoid (delusional) syndrome, as well as manic arousal. With prolonged use, it can cause depression, parkinson-like disorders. The strength of the antipsychotic action of chlorpromazine in the conditional scale for evaluating neuroleptics is taken as one point (1.0). This allows comparison with other antipsychotics.

Levomepromazine("Tizercin") has a more pronounced anti-anxiety effect compared to chlorpromazine, is used to treat affective-delusional disorders, in small doses it has a hypnotic effect and is used in the treatment of neuroses.

Alimemazine synthesized later than other phenothiazine neuroleptics of the aliphatic series. Currently produced in Russia under the name "teraligen". It has a very mild sedative effect, combined with a slight activating effect. Stops the manifestations of the vegetative psychosyndrome, fears, anxiety, hypochondriacal and senestopathic disorders of a neurotic nature, is indicated for sleep disorders and allergic reactions. Unlike chlorpromazine, it does not act on delirium and hallucinations.

Thioridazine("Sonapax") was synthesized in order to obtain a drug that, having the properties of aminazine, would not cause severe drowsiness and would not give extrapyramidal complications. Selective antipsychotic action is manifested in a state of anxiety, fear, with obsessions. The drug has some activating effect.

Periciazine("Nsulsptil") detects a narrow spectrum of psychotropic activity aimed at stopping psychopathic manifestations with excitability, irritability.

Piperazine derivative of phenothiazine thioproperazine("Mazheptil") has a very powerful incisive (breaking psychosis) action. Mazeptil is usually prescribed when treatment with other neuroleptics has no effect. In small doses, mazeptil helps well in the treatment of obsessive-compulsive disorders with complex rituals.

Haloperidol- the most powerful neuroleptic, which has a wide spectrum of action. Stops all types of excitation (catatonic, manic, delusional) faster than triftazin, and more effectively eliminates hallucinatory and pseudo-hallucinatory manifestations. It is indicated for the treatment of patients with the presence of mental automatisms. In small doses, it is widely used to treat neurosis-like disorders (hypochondriac syndromes, senestopathy). The drug is used in the form of tablets, solution for intramuscular injection, in drops.

"Haloperidol-decanoate" is a long-acting drug for the treatment of delusional and hallucinatory-delusional states. Haloperidol, like mazheptil, causes pronounced side effects with stiffness, tremor, and a high risk of developing neuroleptic malignant syndrome (NMS).

Chlorprothixene("Truxal") - a neuroleptic with a sedative effect, has an anti-anxiety effect, is effective in the treatment of hypochondriacal and senestoiatic disorders (the patient is looking for signs of various diseases and is hypersensitive to pain).

Sulpiride("Eglonil") - the first drug of atypical structure, synthesized in 1968. It does not have pronounced side effects of action, it is widely used to treat mental disorders against the background of somatic diseases, with hypochondriacal syndromes, it has an activating effect of action.

Clozapine("Leponex", "Azaleptin") does not have extrapyramidal side effects, reveals a pronounced sedative effect, but unlike chlorpromazine does not cause depression. Complications in the form of agranulocytosis are known.

Olanzapine("Zyprexa") is used to treat psychotic (hallucinatory-delusional) disorders. A negative property is the development of obesity with prolonged use.

Risperidone("Rispolept", "speridan") is the most widely used antipsychotic from the group of atypical drugs. It has a general interrupting effect on psychosis, as well as an elective effect on hallucinatory-delusional symptoms, obsessive-compulsive states. Risperidone, like olanzapine, causes a number of adverse complications in the endocrine and cardiovascular systems, which in some cases requires discontinuation of treatment. Risperidone, like all antipsychotics, the list of which is increasing every year, can cause neuroleptic complications up to NMS. Small doses of risperidone are used to treat obsessive-compulsive disorders, persistent phobias. Rispolept-consta is a long-acting drug that provides long-term stabilization of the condition of patients and relieves acute syndromes in schizophrenia.

Quetiapine("Quentiax"), like other atypical antipsychotics, has a tropism for both dopamine and serotonin receptors. It is used to treat hallucinatory, paranoid syndromes, manic arousal. Registered as a drug with antidepressant and moderately pronounced stimulating activity.

Aripiprazole("Zilaksera") is used to treat all types of psychotic disorders, it has a positive effect on the restoration of cognitive (cognitive) functions in the treatment of schizophrenia.

indole derivative sertindole("Serdolect") in terms of antipsychotic activity is comparable to haloperidol, it is also indicated for the treatment of sluggish conditions, improving cognitive functions, and has antidepressant activity. Sertindole should be used with caution when indicating cardiovascular pathology, it can cause arrhythmias.

Recently, clinical materials have been accumulating, indicating that atypical antipsychotics do not have a significant superiority over typical ones and are prescribed in cases where typical antipsychotics do not lead to a significant improvement in the condition of patients. The benefits and risks of modern and traditional antipsychotics are presented in Table. 4.7.

The main indication for neuroleptics is treatment psychoses (schizophrenia, manic-depressive psychosis, delirium tremens). Hallucinations, arousal respond well to treatment with neuroleptics. Apathy, social isolation are less effectively removed by antipsychotic drugs.

According to the severity of the general antipsychotic effect, antipsychotics are divided into highly potent– chlorpromazine, trifluoperazine, thioridazine, haloperidol, pimozide, penfluridol, fluphenazine; moderate strength antipsychotics (perphenazine) And low potency- flupentixol, sulygiride.

Table 4.7

Benefits and risks of modern and traditional antipsychotics

Characteristic	Modern antipsychotics						Traditional antipsychotics by power*
	Aripiprazole	Clozapine	Olanzapine	Kvetnapin	Risperidone	ziprasidone		Moderate action
Efficiency in terms
Positive symptoms**
negative symptoms
exacerbations
Side effects
Anticholinergics
Repolarization of the heart
hypotension
Hyperprolactinemia
Type 2 diabetes
Sexual dysfunctions
Weight gain

Notes. EPS - extrapyramidal symptoms (dystonia, bradykinesia, tremor, akathisia, dyskinesia). MNS - neuroleptic malignant syndrome (fever, delirium, unstable vital functions, muscle rigidity of varying degrees). Benefits or risks: ++++ - very high, +++ - high, ++ - moderate, + - low, 0 - insignificant, ? - poorly defined. *Examples of powerful traditional drugs are flupentixol (fluanxol), fluphenazine (modigen depot), haloperidol; medium power - zuclopenthixol (clopixol), weak - chlorpromazine and thioridazine. **Risk of exacerbation decreased after 1 year when compared with placebo. Unavailable data from long-term comparative studies with other antipsychotics. *** Akathisia can also occur with the use of modern antipsychotics.

Antipsychotics have anticonvulsant activity. Drugs help reduce body temperature.

A variety of side effects of antipsychotics can be combined into the main side effects associated with the action on the CNS and peripheral undesirable effects of action.

Main side effects: drowsiness, extrapyramidal symptoms, impaired thermoregulation. Extrapyramidal symptoms include impaired coordination - ataxia, akinesia - lack of movement, slow movements. These side effects, like the main effect, are associated with an effect on the level of dopamine in the brain. A decrease in dopamine leads to the phenomena of drug parkinsonism (extrapyramidal disorders similar to parkinsonism). At the same time, patients have muscle stiffness, tremors of varying severity, hypersalivation, the appearance of oral hyperkinesias, etc. the number of receptors sensitive to dopamine.

The influence on central dopamine receptors explains the mechanism of some endocrine disorders caused by neuroleptics, including the stimulation of lactation. By blocking the dopamine receptors of the pituitary gland, antipsychotics increase the secretion of prolactin. Acting on the hypothalamus, antipsychotics also inhibit the secretion of corticotropin and growth hormone.

The main side effects form the neuroleptic syndrome (NS). The leading symptoms of NS are extrapyramidal disorders with a predominance of either hypo- or hyperkinetic disorders.

Hypokinetic disorders include drug-induced parkinsonism with increased muscle tone, rigidity, stiffness and slowness of movements and speech. Hyperkinetic disturbances include tremor, hyperkinesis. Dyskinesias are also observed quite often and can be hypo- and hyperkinetic in nature. They are localized in the mouth and are manifested by spasms of the muscles of the pharynx, tongue, larynx. In some cases, signs of restlessness, motor restlessness are expressed.

Autonomic disorders are expressed in the form of hypotension, sweating, visual disturbances, dysuric disorders. There are also phenomena of agranulocytosis, leukopenia, disturbances of accommodation, urinary retention.

Malignant neuroseptic syndrome (ZPS) is a rare but life-threatening complication of antipsychotic therapy, accompanied by fever, muscle rigidity, autonomic disorders. This condition can lead to kidney failure and death.

Risk factors for NMS can be early age, physical exhaustion, concomitant diseases. The frequency of NMS is 0.5–1%.

The main undesirable effects of the action also include an increase in appetite and an increase in body weight, a violation of the endocrine function. Chlorpromazine, thioridazine have a photosensitizing effect.

Unwanted effects of action atypical antipsychotics clozapine, risperidone, aripeprazole are accompanied by symptoms of neurolepsy, significant changes in the state of the endocrine system, which causes an increase in body weight, bulimia, an increase in the level of certain hormones (prolactin, etc.), very rarely, but symptoms of MNS can be observed. In the treatment of clozapine there is a risk of epileptic seizures and agranulocytosis. The use of seroquel (quetiapine) leads to drowsiness, headache, increased levels of hepatic transaminases and weight gain. Features of the action of some antipsychotics are presented in table. 4.8.

Table 4.8

Features of the action of some antipsychotics

Note. high - high activity; cf - moderately pronounced activity; bottom - low activity.

Peripheral side effects are expressed in the occurrence of orthostatic hypotension (decrease blood pressure when moving from a horizontal position to vertical position). Hepatotoxicity and jaundice, bone marrow depression, photosensitivity, dry mouth, and blurred vision are possible.

A psychotropic drug intended to treat psychotic disorders is called an antipsychotic (also antipsychotic or antipsychotic). What is it and how does it work? Let's figure it out.

Antipsychotic. What it is? History and characteristics

Antipsychotics in medicine appeared relatively recently. Prior to their discovery, the most commonly used drugs for the treatment of psychosis were herbal preparations (eg, henbane, belladonna, opiates), intravenous calcium, bromides, and narcotic sleep.

In the early 1950s, antihistamines or lithium salts began to be used for these purposes.

One of the very first antipsychotics was chlorpromazine (or chlorpromazine), which until then was considered a common antihistamine. It has been widely used since 1953, mainly as or as antipsychotics (for schizophrenia).

The next neuroleptic was the alkaloid reserpine, but soon gave way to other, more effective drugs because it didn't really work.

In early 1958, other first-generation antipsychotics appeared: trifluoperazine (triftazine), haloperidol, thioproperazine, and others.

The term "neuroleptic" was proposed in 1967 (when the classification of psychotropic drugs of the first generation was created) and it referred to drugs not only having an antipsychotic effect, but also capable of causing neurological disorders (akatasia, neuroleptic parkinsonism, various dystonic reactions and others). Typically, these disorders were caused by substances such as chlorpromazine, haloperidol and triftazin. Moreover, their treatment is almost always accompanied by unpleasant side effects: depression, anxiety, severe fear, emotional indifference.

Previously, antipsychotics could also be called "great tranquilizers", so antipsychotics and tranquilizers are one and the same. Why? Because they also cause pronounced sedative, hypnotic and tranquilizing-anti-anxiety effects, as well as a rather specific state of indifference (ataraxia). Now this name in relation to neuroleptics is not applied.

All antipsychotics can be divided into typical and atypical. We have partially described typical antipsychotics, now we will consider an atypical antipsychotic. a group of softer drugs. They do not act as strongly on the body as typical ones. They belong to the new generation of neuroleptics. The advantage of atypical antipsychotics is that they have less effect on dopamine receptors.

Antipsychotics: indications

All antipsychotics have one main property - an effective effect on productive symptoms (hallucinations, delusions, pseudohallucinations, illusions, behavioral disorders, mania, aggressiveness and arousal). In addition, antipsychotics (mostly atypical) may be prescribed to treat depressive or deficient symptoms (autism, emotional flattening, desocialization, etc.). However, their effectiveness in relation to the treatment of deficient symptoms is a big question. Experts suggest that antipsychotics can only eliminate secondary symptoms.

Atypical neuroleptics, whose mechanism of action is weaker than typical ones, are also used to treat bipolar disorder.

The American Psychiatric Association prohibits the use of antipsychotics to treat the psychological and behavioral symptoms of dementia. Also, they should not be used for insomnia.

It is unacceptable to be treated with two or more antipsychotic drugs at the same time. And remember that neuroleptics are used to treat serious diseases, it is not recommended to take them just like that.

Main effects and mechanisms of action

Modern neuroleptics have one common mechanism of antipsychotic action, because they are able to reduce the transmission of nerve impulses only in those brain systems in which dopamine transmits impulses. Let's take a closer look at these systems and the effect of antipsychotics on them.

• mesolimbic pathway. A decrease in transmission in this pathway occurs when taking any antipsychotic drug, since it means the removal of productive symptoms (for example, hallucinations, delusions, etc.)
• mesocortical pathway. Here, a decrease in the transmission of impulses leads to the manifestation of symptoms of schizophrenia (there are such negative disorders as apathy, desocialization, poverty of speech, smoothing of affect, anhedonia) and cognitive impairment (attention deficit, impaired memory function, etc.). The use of typical antipsychotics, especially long-term use, leads to an increase in negative disorders, as well as serious impairment of brain functions. Cancellation of antipsychotics in this case will not help anything.
• Nigrostriatal path. Blockade of dopamine receptors in this case usually leads to the side effects typical of antipsychotics (akathisia, parkinsonism, dystonia, salivation, dyskinesia, trismus of the jaws, etc.). These side effects are observed in 60% of cases.
• Tuberoinfundibular pathway (transmission of impulses between the limbic system and the pituitary gland). Blocking the receptors leads to an increase in the hormone prolactin. Against this background, a huge number of other side effects are formed, such as gynecomastia, galactorrhea, sexual dysfunction, infertility pathology, and even a pituitary tumor.

Typical neuroleptics have a greater effect on dopamine receptors; atypical ones affect serotonin with other neurotransmitters (substances that transmit nerve impulses). Because of this, atypical antipsychotics are less likely to cause hyperprolactinemia, neuroleptic depression, as well as neurocognitive deficits and negative symptoms.

Signs of blockade of α 1 -adrenergic receptors are a decrease in blood pressure, orthostatic hypotension, the development of dizziness, the appearance of drowsiness.

With the blockade of H 1 -histamine receptors, hypotension appears, the need for carbohydrates and weight gain, as well as sedation, increase.

If blockade of acetylcholine receptors occurs, the following side effects appear: constipation, dry mouth, tachycardia, increased intraocular pressure and disturbances of accommodation. Confusion and drowsiness may also occur.

Western researchers have proven that there is a connection between antipsychotics (new antipsychotics or old ones, typical or atypical, it doesn't matter) and sudden cardiac death.

Also, when treated with antipsychotics, the risk of stroke and myocardial infarction is significantly increased. This is due to the fact that psychotic drugs affect lipid metabolism. Taking antipsychotics can also trigger type 2 diabetes. The chances of getting serious complications increase with combined treatment with typical and atypical antipsychotics.

Typical neuroleptics can provoke epileptic seizures, as they lower the threshold for convulsive readiness.

Most antipsychotics (mainly phenothiazine antipsychotics) have a large hepatotoxic effect, and can even cause the development of cholestatic jaundice.

Treatment with antipsychotics in the elderly can increase the risk of pneumonia by 60%.

The cognitive effect of neuroleptics

Conducted open studies have shown that atypical antipsychotics are slightly more effective than typical ones in the treatment of neurocognitive insufficiency. However, there is no convincing evidence of any effect on neurocognitive impairment. Atypical neuroleptics, whose mechanism of action is slightly different from the typical ones, are often tested.

In one of the clinical studies, physicians compared the effects of risperidone and haloperidol at low doses. During the study, no significant differences were found in the readings. Haloperidol at low doses has also been shown to have a positive effect on neurocognitive performance.

Thus, the question of the impact of first or second generation antipsychotics on the cognitive sphere is still controversial.

Classification of antipsychotics

It has already been mentioned above that antipsychotics are divided into typical and atypical.

Typical antipsychotics include:

1. Sedative antipsychotics (having an inhibitory effect after use): promazine, levomepromazine, chlorpromazine, alimemazine, chlorprothixene, periciazine and others.
2. Incisive antipsychotics (have a powerful global antipsychotic effect): fluphenazine, trifluoperazine, thioproperazine, pipothiazine, zuclopenthixol, and haloperidol.
3. Disinhibiting (have an activating, disinhibitory effect): carbidine, sulpiride and others.

Atypical antipsychotics include substances such as aripiprazole, sertindole, ziprasidone, amisulpride, quetiapine, risperidone, olanzapine, and clozapine.

There is another classification of antipsychotics, according to which they distinguish:

1. Phenothiazines, as well as other tricyclic derivatives. Among them there are such types:

   ● neuroleptics with a simple aliphatic bond (levomepromazine, alimemazine, promazine, chlorpromazine), powerfully block acetylcholine receptors and adrenoreceptors, have a pronounced sedative effect and can cause extrapyramidal disorders;
   ● antipsychotics with a piperidine core (thioridazine, pipothiazine, periciazine), which have a moderate antipsychotic effect and mild neudocrine and extrapyramidal side effects;
   ● Antipsychotics with a piperazine core (fluphenazine, prochlorperazine, perphenazine, thioproperazine, frenolone, trifluoperazine) are able to block dopamine receptors, and also have little effect on acetylcholine and adrenoreceptors.

2. All thioxanthene derivatives (chlorprothixene, flupentixol, zuclopenthixol), whose action is similar to that of phenothiazines.
3. Substituted benzamides (tiapride, sultopride, sulpiride, amisulpride), the action of which is also similar to phenothiazine antipsychotics.
4. All derivatives of butyrophenone (trifluperidol, droperidol, haloperiodol, benperidol).
5. Dibenzodiazapine and its derivatives (olanzapine, clozapine, quetiapine).
6. Benzisoxazole and its derivatives (risperidone).
7. Benzisothiazolylpiperazine and its derivatives (ziprasidone).
8. Indole and its derivatives (sertindole, dicarbine).
9. Piperazinylquinolinone (aripiprazole).

Of all the above, it is possible to single out available antipsychotics - drugs sold without prescription in pharmacies, and a group of antipsychotics that are sold strictly according to the doctor's prescription.

Interactions of neuroleptics with other drugs

Most often, these symptoms appear when the antipsychotic is withdrawn (this is also called has several varieties: hypersensitivity psychosis, unmasked dyskinesia (or recoil dyskinesia), cholinergic "recoil" syndrome, etc.

To prevent this syndrome, treatment with antipsychotics must be completed gradually, gradually reducing the dose.

When taking antipsychotics in high doses, such side effect as neuroleptic deficit syndrome. According to anecdotal evidence, this effect occurs in 80% of patients taking typical antipsychotics.

Structural changes in the brain with prolonged use

According to placebo-controlled studies of macaques, which were given normal doses of olanzapine or haloperidol for two years, the volume and weight of the brain from taking antipsychotics decreases by an average of 8-11%. This is due to a decrease in the volume of white and gray matter. Recovery after neuroleptics is impossible.

After the publication of the results, researchers were accused of not testing the effects of antipsychotics on animals before entering the pharmaceutical market, and that they pose a danger to humans.

One of the researchers, Nancy Andreasen, is sure that the decrease in the volume of gray matter and the use of antipsychotics in general negatively affect the human body and lead to atrophy of the prefrontal cortex. On the other hand, she also noted that antipsychotics are an important medicine that can cure many ailments, but they should be taken only in very small quantities.

In 2010, researchers J. Leo and J. Monkrieff published a review of research based on magnetic resonance imaging of the brain. The study was carried out to compare brain changes in patients taking antipsychotics and patients not taking them.

In 14 out of 26 cases (in patients taking antipsychotics), a decrease in brain volume, gray and white matter volume was observed.

Of the 21 cases (in patients who did not take antipsychotics or took them, but in small doses), none showed any changes.

In 2011, the same researcher Nancy Andreasen published the results of a study in which she found changes in brain volume in 211 patients who had been taking antipsychotics for quite a long time (more than 7 years). At the same time, the larger the dose of drugs, the more significantly the volume of the brain decreased.

Development of new drugs

At the moment, new antipsychotics are being developed that would not affect receptors. One group of researchers claimed that cannabidiol, a component of cannabis, has an antipsychotic effect. So it is possible that soon we will see this substance on the shelves of pharmacies.

Conclusion

We hope no one has any questions left about what a neuroleptic is. What is it, what is its mechanism of action and the consequences of taking it, we discussed above. It remains only to add that no matter what the level of medicine in the modern world, not a single substance can be fully studied. And the trick can be expected from anything, and even more so from such complex drugs as antipsychotics.

In recent years, cases of treatment of depression with antipsychotics have become more frequent. Out of ignorance of the dangers of this drug, people make things worse for themselves. Antipsychotics should never be used for any purpose other than their intended use. And what effect these drugs produce on the brain is out of the question.

That is why antipsychotics - drugs available for purchase without prescriptions, should be used with caution (and only if you are 100% sure that you need it), and even better not to use at all without a doctor's prescription.