Types of atypical antipsychotics
Neuroleptics are drugs for the treatment of various psychiatric pathologies and nervous system disorders that help:
- normalize human social behavior;
- stop coughing, nausea, vomiting;
- reduce body temperature;
- eliminate increased anxiety, insomnia;
- reduce vegetative reactions.
Previously used drugs to relieve the symptoms of schizophrenia and bipolar disorder completely blocked the metabolism of dopamine, causing a decrease in a person’s mental and physical activity. Atypical neuroleptics of the new generation, in contrast to their predecessors, have a milder effect and rarely provoke the appearance of adverse reactions in the body.
The classification of atypical antipsychotics is based on:
- The duration of the effect produced. In modern pharmacology, antipsychotics with rapid and prolonged action are produced.
- The severity of the clinical picture of treatment.
- The mechanism of action of the drug on dopamine nerve endings (the doctor can choose the appropriate therapy for the patient).
- Chemical composition of the drug. The synthetic formula of the drug is selected strictly individually, in order to reduce the possible unpleasant consequences of the treatment.
History[edit]
The term “neuroleptic” (ancient Greek νευρον - nerve, nervous system; ancient Greek ληψη - retention) has been declared obsolete, since neurolepsy is an undesirable side effect of antipsychotic drugs and in psychiatry they try not to remember this in vain. The term "neuroleptics" was proposed in 1967, during the development of the first classification of psychotropic drugs.
Even earlier, these substances were called “major tranquilizers”, or “ataractics”, for the pronounced sedative, hypnotic and tranquilizing-anti-anxiety effect caused by many antipsychotics, as well as a specific state of indifference to external stimuli (“ataracsia”). This name was considered even more inappropriate and disappeared from circulation earlier than the name “neuroleptics”, since not all antipsychotics have a sedative and hypnotic effect, and some of them, on the contrary, even have an activating, disinhibiting and energizing effect, especially noticeable in small doses .
The earliest representative of the group of typical antipsychotics, chlorpromazine-aminazine, began to be widely used in 1952. Also typical neuroleptics are the well-known trifluoperazine, thioridazine and, in general, all the so-called. “phenothiazines”, haloperidol and all butyrophenones, clopixol, flupenthixol and others.
The first of the atypical antipsychotics, clozapine (azaleptin), was developed in 1960; most other atypical antipsychotics were developed in the 1990s.
The effectiveness of new generation neuroleptics
New generation neuroleptics, without side effects that impair the mental functioning of the brain, have weak antipsychotic activity. They act on certain dopamine receptors in the brain. Unlike typical antipsychotics, the use of which leads to complete disorientation of a person, atypical antipsychotics act only in the limbic system.
They have low anti-dopamine properties and high sedative qualities:
- eliminate obvious and hidden symptoms of psychosis;
- calm, reduce anxiety, gag reflex;
- prevent the progression of human mental disorders;
- do not affect the pituitary gland, extrapyramidal system, hypothalamus;
- retain cognitive function in full.
Benefits of atypical antipsychotics
New generation neuroleptics without side effects for the subsequent socialization of a person’s personality have a number of advantages compared to typical antipsychotics:
- maintain the patient’s motor activity in full;
- do not reduce fertility, ovulation, potency;
- do not affect dopamine metabolism;
- are easily excreted from the human body;
- eliminate symptoms of acute and chronic mental disorders;
- support human mental functions;
- after treatment, they allow you to return to normal activities;
- are not addictive.
Pharmaceutical companies have developed a number of drugs approved for the treatment of psychosis in pregnant women and minor patients.
Structural changes in the brain[edit]
Placebo-controlled studies of three groups of macaques treated with haloperidol or olanzapine at therapeutic dosages for 17-27 months indicate a significant decrease in brain weight and volume due to antipsychotics, reaching 8-11% [12] and associated with a decrease in volumes of both gray, and white matter in a number of areas. The decrease in gray matter volume was caused predominantly by the loss of glial cells,[13] primarily astrocytes (up to 20% in the parietal region) and oligodendrocytes (up to 11%),[14] while an increase in the density of neurons was noted, the total number of which did not change . The publications were followed by accusations from pharmaceutical companies that the effects of their psychotropics were not properly tested in animal models before introducing these false drugs to the market[15].
Researcher Nancy Andreasen believes that accelerated loss of gray matter in patients receiving increased amounts of antipsychotic drugs indicates a negative effect. This position has drawn criticism from other researchers, including Fuller Tory.
Neuroleptics without side effects: a review of drugs
A new generation of antipsychotics that do not cause side effects prevents the development of mental pathology, preserving a person’s cognitive functions. Popular medicines:
Abilify
The drug is yellow-cream capsules of 10, 15, 30 mg. The active substance is aripiprazole.
The product has:
- highly dynamic in relation to D2, D3 receptors, nerve endings 3HT1a, 5HT2a;
- moderate effect on D4, 5HT7 receptors;
- does not stop muscarinic endings.
Prescribed for:
- sudden outbreaks of schizophrenia;
- long-term therapy of chronic sluggish decay of the thinking process;
- sudden onset bipolar disorder following a manual or mixed episode.
The medication is taken once, regardless of food consumption. The dosage is determined by the doctor individually for each patient.
Recommended treatment:
- Schizophrenia (acute attack, chronic course). In the first week, 10-15 mg/day is prescribed. After the condition improves, the daily dosage of the drug is reduced (to 10 mg).
- Bipolar disorder – 15-30 mg/day.
Abilify is instantly absorbed by the gastrointestinal tract. The highest concentration in the blood is observed 3-7 hours after taking the capsule. The positive effect of the drug is actively manifested from the 14th day after the start of therapy. Metabolized in the liver, completely excreted from the body with decay products.
The medication is not used in patients:
- having intolerance to any component of the drug;
- under 18 years of age.
Contraindicated for pregnant women and nursing mothers.
Abilify drug therapy should be used with caution in persons suffering from:
- cardiovascular pathologies;
- dysfunction of the gastrointestinal tract;
- endocrinological disorders;
- chronic diseases of the respiratory system;
- suicidal tendencies;
- renal, liver failure.
Correction of psychiatric pathologies in patients over 65 years of age does not require changing the standard dosage.
Fluphenazine
One of the best modern antipsychotics. Relieves nervous excitability, eliminates symptoms of psychiatric diseases and hallucinogenic disorders.
Components:
- fluphenazine decanoate;
- benzyl alcohol;
- sesame oil.
The drug is a suspension for i.m. injections are pale yellow, oily in nature.
Prescribed for the treatment of:
- acute schizophrenia;
- circular psychosis;
- hyperactivity;
- increased nervous excitability;
- disorders of the dynamics of mental functioning.
Demonstrates antipsychotic effects. Interferes with the functioning of D-receptors in the dopaminergic system of the brain.
Possesses:
- antiemetic effect - active against D2 endings, the vagus nerve in the gastrointestinal tract;
- hypotensive properties – releases the hypothalamus, pituitary hormones;
- enhancing effect on prolactin production;
- low expiramidal impact.
In the body, the active substances of Fluphenazine disintegrate, combining with plasma protein.
The course of treatment for the patient is selected individually, depending on the patient’s personal characteristics, type, and stage of nervous pathology.
Recommended dosage for adult patients:
- orally – 1 – 5 mg 2-3 times a day (total amount not more than 20 mg);
- IM injection – from 1.25 to 2.5 mg every 6-8 hours.
For minors, Fluphenazine is prescribed in the form of a “demo form” - 250-750 mg/kg (1-4 times a day). Maximum up to 100 mg. Treatment must be carried out in a course with an interval of 14 days.
The drug rarely causes addiction or the development of side pathologies.
Contraindicated for use by persons suffering from:
- loss of consciousness with complete cessation of respiratory activity;
- cerebrovascular disorder;
- pathologies of the heart and blood vessels;
- blood disease;
- depression;
- disruption of the liver and kidneys.
Not prescribed for the treatment of women expecting a baby and nursing mothers.
When taken together with antispasmodics, it can depress respiratory functions and the functioning of the central nervous system. Strengthens the effect of alcohol and psychotropic substances.
Quetiapine
The safest antipsychotic. Not addictive. The appearance of side effects occurs only when the maximum permissible amount of the drug taken daily is exceeded. In pharmacology, “Quetiapine” is presented as convex white capsules.
Components:
- quetiapine;
- polysorb;
- milk sugar;
- sodium carboxymethyl starch;
- povidone K-30;
- talc;
- magnesium salt;
- silicon dioxide cellulose.
Antipsychotic. It is most active in relation to 5HT2 serotonin endings, less so in relation to D1, D2 receptors. Does not cause an increase in prolactin levels. Has a strong antisiolytic effect. Blocks the antihistamine H1 receptor. Absorbed by the gastrointestinal tract. Combines with plasma proteins. Actively decomposes in the liver.
Prescribed for acute and chronic mental disorders of various etymologies with a strong anti-sociological orientation.
Mode of application:
- adults – 50 mg/day;
- elderly people – 25 mg once a day;
- persons suffering from chronic problems with the liver and kidneys – 25 mg.
Over time, the daily consumed dosage of Quetiapine increases (up to 700 mg).
It is prohibited to prescribe medication:
- persons suffering from hypersensitivity to the constituent components of the drug;
- small children;
- pregnant women;
- nursing mothers.
Fluanxol
Antipsychotic, available in the form:
- brown-yellow tablets, sugar-coated;
- liquids for intramuscular administration.
Thioxanthene derivative:
- reduces excitability and psychomotor activity;
- has a disinhibiting effect;
- reduces feelings of anxiety and fear;
- prevents the development of depression;
- weakens the activity of dopamine receptors (D1, D2).
The effectiveness of therapy depends on the dosage of the drug. The duration of action of the tablets is from 2 to 4 weeks.
Components:
- flupenthixol dihydrochloride;
- magnesium stearate;
- gelatin;
- lactose monohydrate.
Once in the body, the drug is broken down into cis-flupenthixol and capric acid. Excreted by the intestines.
The dosage is selected for each patient depending on the personal characteristics and stage of the disease.
Fluanxol is prescribed in amounts up to 3 mg/day. for elimination:
- depressive mental disorders accompanied by apathy;
- chronic neurological problems of an alarming nature;
- stressful conditions;
- psychosomatic disorders with asthenic reactions.
Prescribed in a course of 3 to 40 mg/day. patients suffering from:
- paranoia with delusions;
- hallucinatory syndrome;
- decreased mental activity;
- apathy, autism.
Dosage from 40 to 150 mg/day. suitable for cupping:
- psychiatric disorders;
- neurological and physiological dysfunctions that occur during the manifestation of withdrawal syndrome in persons suffering from alcohol dependence.
The maximum amount of approved medication is 150 mg/day. divided into 3 doses. For intramuscular injections - up to 200 ml with an interval of 2-4 weeks.
The medication is not used in persons suffering from:
- acute drug and alcohol intoxication;
- hyperthermia;
- parkinsonism;
- fever;
- allergic reactions to the components of the drug;
- kidney and liver dysfunction.
Fluanxol is contraindicated:
- patients with a history of toxic agranulocytosis;
- pregnant women;
- nursing mothers.
Triftazin
Medication for psychosis secondary to phenothiazine.
Used to combat:
- various psychotic disorders;
- neuroses accompanied by anxiety, fear;
- nausea (reduces the gag reflex).
Trifluoperazine, contained in a suspension for intramuscular injection, freezes postsynaptic mesolimbic D receptors located in the nervous system.
Demonstrates:
- decreased gag reflexes (due to elimination of the activity of the D2 receptor, the paired nerve of the gastrointestinal tract);
- alpha-adrenergic blocking activity;
- hypotensive effect.
Taking Triftazin slightly reduces the brain and labor activity of patients.
The dosage of the drug is prescribed individually:
- adults - 1-5 mg every 8-12 hours;
- children - 1 mg (2-3 injections per day).
Restrictions on use:
- deep fainting with loss of breath;
- depression;
- oncology;
- shortness of breath;
- shaking paralysis;
- renal dysfunction;
- the waiting period for the child;
- breast-feeding;
- epilepsy;
- peptic ulcer.
For the treatment of persons over 70 years of age, a reduced dosage is established.
Levomepromazine
The drug is available as tablets and a solution for intramuscular and intravenous administration. Phenothiazine derivative. Included in the list of vital and essential drugs.
Tizercin is a new generation antipsychotic with the active ingredient Levomepromazine
When a medication enters the body:
- carries out sedative, antipsychotic, antiemetic, hypotensive actions;
- suppresses depression without reducing a person’s brain and mental activity;
- increases the production of prolactin by the pituitary gland;
- merges with plasma protein (the highest concentration is shown after 1-3 hours);
- excreted by the intestines and kidneys.
The drug is indicated for:
- mental and motor disorders accompanied by severe excitability;
- circular psychosis;
- schizophrenia;
- senile dementia;
- seizures caused by psychotropic, alcohol addiction;
- depressive state accompanied by anxiety, restlessness;
- neurological problems;
- sleep disturbance;
- severe pain caused by inflammation of the triple nerve, herpes zoster, oncology;
- itchy dermatosis.
Dosage regimen:
- adults need to consume 25-50 mg;
- children are prescribed 15 mg/kg/day. for 2-3 times;
- injections – 24-50 mg.
The use of the drug is limited to persons suffering from:
- decompensation of myocardial dysfunction;
- essential hypertension;
- pathologies of the circulatory system;
- disorders of the kidneys and liver.
Pregnant women are prescribed the minimum dosage. By the time of delivery, the amount of the drug used is reduced in order to avoid the development of atropine-like effects in the newborn baby.
Levomepromazine should be administered with caution:
- children;
- To old people;
- cancer patients;
- persons suffering from Reye's syndrome, Parkinson's disease, chronic dysfunctions of the respiratory system;
- epileptic patients.
Links[edit]
- Main side effects of typical antipsychotics
- Recovery after psychopharmacotherapy
- Mechanism of action of antipsychotics (neuroleptics)
- Video of tardive dyskinesia
- Psychiatry
- Chlorpromazine equivalent
- Andrew CHETLEY. Problematic medications. Part 27 Psychotropic drugs
- Non-psychiatric ways to deal with depression
- Psychiatry and the pharmaceutical industry - in 100 words; David Healy; The British Journal of Psychiatry. 2009; 194:85
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- Sernyak MJ, Leslie DL, Alarcon RD, Losonczy MF, Rosenheck R (2002) Association of diabetes mellitus with use of atypical neuroleptics in the treatment of schizophrenia Pharmacotherapy
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- CATIE Comes To Surprising Conclusions, Schizophrenia Research Forum, 2005.
- Goldberg TE, Goldman RS, Burdick KE, Malhotra AK, Lencz T, Patel RC, Woerner MG, Schooler NR, Kane JM, Robinson DG (October 2007). “Cognitive improvement after treatment with second-generation antipsychotic medications in first-episode schizophrenia: is it a practice effect?”. Arch. Gen. Psychiatry 64(10):1115–22. DOI:10.1001/archpsyc.64.10.1115. PMID 17909123.
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Antipsychotics without side effects that can be bought without a prescription
New generation neuroleptics without side effects on the nervous and endocrine systems are widely used to eliminate neurological and psychotic disorders. The medicinal properties of the drugs are aimed at blocking dopamine receptors D1, D2, reducing increased excitability and anxiety.
This list of antipsychotics has a sedative effect and is used for depression and stress, and sleep problems:
- "Olanzapine" - reduces the action of neurons, pacifies the activity of the nerve pathways that control motor functions. Removes anxiety and negative manifestations of stress. Prescribed for depression, mental pathologies, and increased fear. Pregnant and lactating women, children under 18 years of age, and persons suffering from blood, liver, and kidney diseases should not take the drug.
- "Amisulpride" is an antipsychotic with a calming and antidepressant effect. Indicated for schizophrenia, mental pathologies accompanied by delusions, hallucinations, impaired thinking, and withdrawal.
- "Aprizol" - used to treat psychosis. Acts on dopamine and sedative receptors. Relaxes the nervous system. The maximum drug effect occurs 4-5 days after the start of therapy. Recommended for depressive disorders. May be dangerous for patients suffering from pathologies of the cardiovascular system.
- "Serdolect" is a generic version of "Aprizola". Similar in composition and therapeutic effects.
- "Respiridone" is a psychotropic drug that has a hypothermic, antiemetic, and sedative effect. It overcomes mental disorders well, accompanied by delusions, hallucinations, neurological problems, the effects of stress, and depression. Prescribed for cyanide dementia of the Alzheimer's type, senile dementia, and uncontrolled aggression in adolescents.
- Clozapine is an antipsychotic that eliminates anxiety and destructive behavior. It affects the symptoms of negativism, schizophrenia, manic-depressive psychosis, psychomotor agitation of the emotional-behavioral type, bipolar disorder.
Prices of drugs in pharmacies in Moscow, St. Petersburg, regions
New generation neuroleptics without side effects for subsequent human brain activity are sold in pharmacy chains of the Russian Federation. The price of the drug depends on the region, transportation costs, and supplier.
Name of the locality | "Abilify" | "Quetiapine" | "Flu-anksol" | "Triftazine" | "Olan-zapin" | "Risperidon" |
Moscow | 7382 | 213 | 386 | 77 | 160 | 129 |
Saint Petersburg | 4200 | 294 | 357 | 34 | 226 | 70 |
Amur region | 12000 | 650 | 415 | 98 | 158 | 136 |
Arhangelsk region | 5300 | 994 | 384 | 76 | 218 | 167 |
Belgorod region | 11800 | 657 | 379 | 33 | 422 | 120 |
Bryansk region | 6300 | 218 | 432 | 35 | 338 | 117 |
Lipetsk region | 11800 | 212 | 370 | 29 | 422 | 130 |
Voronezh region | 6297 | 188 | 411 | 26 | 160 | 106 |
Ivanovo region | 12900 | 216 | 397 | 35 | 335 | 113 |
Rostov region | 5400 | 217 | 381 | 24 | 204 | 165 |
Kaliningrad region | 6298 | 218 | 990 | 29 | 216 | 136 |
Vologda Region | 6298 | 219 | 384 | 32 | 218 | 126 |
Irkutsk region | 6298 | 216 | 590 | 24 | 190 | 140 |
A new generation of antipsychotics helps cope with mental and neurological disorders. Modern antipsychotics do not have side effects on a person’s mental and physiological activity. Selected individually in each specific case, psychiatric defects are promptly relieved without interfering with further social adaptation of the individual.
Article design: Vladimir the Great