Teraligen

Indications for use

It has antiemetic, sedative and antitussive effects. The reaction to external stimuli decreases, as does psychomotor agitation, affective tension, the feeling of fear is suppressed, and a weakening of aggressiveness is noted. Teraligen is used as a sleeping pill, but in a general sense it is not. Neuroleptics simply induce drowsiness and speed up the onset of sleep. And this must be taken into account in certain specialties.

Teraligen may induce drowsiness and accelerate the onset of sleep

That is, the pharmacological use of Teraligen is quite wide. The medicine is available in the form of dark pink, film-coated tablets. It contains 5 mg of alimemazine tartrate.

Teraligen is effective for neurotic disorders due to trauma, intoxication, vascular disorders in combination with autonomic disorders, anxiety and mild depressive disorders.

This medicine is used to treat the following diseases:

somatized mental disorders;
states of excitement and anxiety against the background of somatic pathologies;
sleep disorders of various origins;

The drug is used to treat mental disorders and depression

psychopathy with asthenic and psychoasthenic disorders;
anxiety-depressive conditions within the framework of borderline endogenous and vascular diseases;
senestopathic depression;
allergic reactions (symptomatic treatment);
neuroses and neurosis-like conditions of endogenous and organic origin with a predominance of senestopathic, hypochondriacal, phobic and psychovegetative disorders.

Teraligen valenta 5 mg 100 pcs. film-coated tablets

pharmachologic effect

Antipsychotic (neuroleptic).

Composition and release form Teraligen valenta 5 mg 100 pcs. film-coated tablets

Tablets - 1 tablet:

active ingredient: alimemazine tartrate - 5.0 mg or 10.0 mg;
excipients: lactose monohydrate, microcrystalline cellulose, pregelatinized starch, colloidal silicon dioxide (aerosil), croscarmellose sodium, magnesium stearate;
shell composition: Opadry II 85F34655: partially hydrolyzed polyvinyl alcohol, macrogol-3350, talc, titanium dioxide E 171, carmine red dye E 120, aluminum varnish based on sunset yellow dye E 110, aluminum varnish based on indigo carmine E 132.

Film-coated tablets, 5 mg and 10 mg.

25 tablets in a blister pack or in a blister pack with perforation made of polyvinyl chloride film and printed varnished aluminum foil.

1, 2 or 4 contour packages along with instructions for use are placed in a pack.

Description of the dosage form

Dark pink film-coated tablets with an embossed symbol on one side and a stripe on the other.

Directions for use and doses

Inside. Without chewing. The effect of the drug is dose-dependent; doses are selected depending on the goals of therapy.

For adults

To achieve a vegetative stabilizing effect, 15-60 mg/day.

To achieve an anxiolytic effect, 20-80 mg/day.

To achieve a sedative and/or hypnotic effect, 5-10 mg once (20-30 minutes before bedtime).

For the symptomatic treatment of allergic reactions, 10-40 mg/day.

The course of treatment should begin with 2.5-5 mg in the evening with a gradual increase in the daily dose until the desired effect. The daily dose can be divided into 3-4 doses. The duration of the course of treatment can be from 2 to 6 or more months and is determined by the doctor.

The highest dose for adults is 500 mg/day, for elderly people (over 60 years old) - 200 mg/day.

Children from 7 years of age are prescribed according to the following scheme (depending on age and body weight).

To achieve an anxiolytic effect, 20-40 mg/day.

The course of treatment should begin with 2.5-5 mg with a gradual increase in the daily dose until the desired effect. The daily dose can be divided into 3-4 doses.

To achieve a sedative and/or hypnotic effect, 2.5-5 mg once (20-30 minutes before bedtime).

To achieve a sedative effect in behavioral disorders in psychotic conditions, it is possible to increase the daily dose to 60 mg/day.

For the symptomatic treatment of allergic reactions, 5-20 mg/day.

The duration of the course of treatment can be from 2 to 6 or more months and is determined by the doctor.

Children from 3 years old

For the symptomatic treatment of allergic reactions, 2.5-5 mg 3-4 times a day. The duration of the course of treatment can be from 2 to 6 or more months and is determined by the doctor.

For the purpose of sedation before surgery, children from 3 to 7 years old are prescribed at the rate of 2 mg/kg 1-2 hours before surgery. The maximum daily dose is 2 mg/kg.

Pharmacodynamics

It is a phenothiazine derivative.

Alimemazine acts as a mild sedative and anti-anxiety agent, has a positive effect on senesthopathy, obsession and phobia.

It is used for psychosomatic manifestations that develop as a result of neurovegetative disorders, vascular, traumatic and infectious disorders of the central nervous system. The sedative effect helps normalize sleep in patients in this category.

Has antiemetic and antitussive activity.

The sedative and anxiolytic effect is due to the blockade of adrenergic receptors in the reticular formation of the brain stem. The antiemetic and vegetative-stabilizing effect is due to the blockade of dopamine D2 receptors in the trigger zone of the vomiting center.

Due to its antihistamine activity, alimemazine is used for allergic diseases, especially the respiratory tract, and for itchy skin.

Alimemazine is more active in antihistamine and sedative action than diprazine. The antipruritic effect is due to the effect on type 1 histamine receptors.

Pharmacokinetics

Quickly and completely absorbed by any route of administration. The effect of alimemazine begins 15-20 minutes after administration and lasts 6-8 hours. The binding to plasma proteins is 20-30%. Metabolized in the liver. Excreted by the kidneys - 70-80% in the form of a metabolite (sulfoxide).

Indications for use Teraligen valenta 5 mg 100 pcs. film-coated tablets

In adults and children from 7 years of age

As a sedative (calming), anxiolytic (anti-anxiety) and sleep aid:

dementia (including dementia due to epilepsy), occurring with manifestations of psychomotor agitation, anxiety affect (as part of combination therapy);
organic anxiety disorder (as monotherapy or as part of combination therapy);
schizophrenia (with a predominance of neurosis-like disorders, as part of combination therapy);
mood disorders (affective disorders) - as part of combination therapy;
generalized anxiety disorder (as part of combination therapy);
obsessive-compulsive disorder (as part of combination therapy);
reaction to severe stress and adaptation disorders (acute reaction to stress, post-traumatic stress disorder, unspecified reaction to severe stress, other reactions to severe stress) - as part of combination therapy;
dissociative (conversion) disorders (as part of combination therapy);
somatoform disorders (somatization disorder, undifferentiated somatoform disorder, hypochondriacal disorder, somatoform dysfunction of the autonomic nervous system, persistent somatoform pain disorder, unspecified somatoform disorder, other somatoform disorders) - as part of combination therapy for severe anxiety or when standard therapy is ineffective;
unspecified disorder of the autonomic nervous system, other disorders of the autonomic nervous system (as part of combination therapy);
anorexia nervosa (as part of combination therapy);
emotionally unstable personality disorder (impulsive and borderline types) - as part of combination therapy;
hysterical personality disorder, anxious (avoidant, avoidant) personality disorder (as part of combination therapy);
persistent personality change after experiencing a disaster (as part of combination therapy);
hyperkinetic behavior disorder (as part of combination therapy);
behavioral disorder limited to the family (as part of combination therapy when standard therapy is ineffective);
unsocialized behavior disorder (as monotherapy or as part of combination therapy);
anxiety, agitation and other symptoms and signs related to the emotional state (as part of combination therapy);
other neurotic disorders (neurasthenia, unspecified neurotic disorder) - as part of combination therapy;
insomnia of non-organic etiology (as part of combination therapy when standard therapy is ineffective);
emotional disorders whose onset is specific to childhood (phobic anxiety disorder of childhood, social anxiety disorder of childhood, sibling rivalry disorder, unspecified emotional disorder of childhood, other emotional disorders of childhood) - as part of combination therapy.

As an antiallergic agent:

itching regardless of location and etiology (anal itching, vulvar itching, unspecified anogenital itching, itching due to photocontact dermatitis and solar urticaria, dermatitis, eczema, urticaria, bites or stings from non-venomous insects or other non-venomous arthropods, chicken pox, measles, Diseases Hodgkin's disease, diabetes mellitus, herpes zoster) as monotherapy or as part of combination therapy;
asthma, hay fever, whooping cough (as part of complex therapy as an antiallergic agent to relieve cough, shortness of breath and asthma attacks);
unspecified allergy (as monotherapy or as part of combination therapy).

In children from 3 years old

As an antiallergic agent:

itching regardless of location and etiology (itching due to photocontact dermatitis and solar urticaria, dermatitis, eczema, urticaria, bites or stings from non-venomous insects or other non-venomous arthropods, chickenpox, measles, Hodgkin's disease, diabetes mellitus, shingles, itching of the anus, itching vulva, unspecified anogenital itching) as monotherapy or as part of combination therapy.

As a sedative (calming agent):

during medicinal preparation for surgery (for the purpose of sedation before surgery).

Contraindications

Hypersensitivity to the components of the drug;
lactose intolerance, lactase deficiency, glucose-galactose malabsorption;
angle-closure glaucoma;
prostatic hyperplasia;
severe liver and/or kidney failure;
parkinsonism;
myasthenia gravis;
Reye's syndrome;
simultaneous use of monoamine oxidase inhibitors (MAO);
pregnancy;
lactation period;
children up to 3 years of age when used as an antiallergic agent and for sedation before surgery, up to 7 years for other indications.

Carefully

The drug should be used with caution in case of alcoholism if there is a history of complications when using phenothiazine drugs; with obstruction of the bladder neck; predisposition to urinary retention; for epilepsy; open-angle glaucoma; jaundice; suppression of bone marrow function; arterial hypotension.

Application of Teraligen valenta 5 mg 100 pcs. film-coated tablets during pregnancy and breastfeeding

Contraindicated for use during pregnancy and lactation (breastfeeding). If pregnancy occurs during treatment, the drug should be discontinued.

If it is necessary to use the drug during lactation, breastfeeding should be stopped.

special instructions

Alimemazine may mask the ototoxic effect (tinnitus, dizziness) of co-administered drugs.

Alimemazine increases the body's need for riboflavin.

To prevent distortion of the results of skin prick tests for allergens, the drug should be discontinued 72 hours before allergy testing.

During treatment, false positive results for pregnancy are possible.

During treatment you should not drink alcohol.

Impact on the ability to drive vehicles and operate machinery

During treatment with the drug, you should not engage in activities that require increased concentration of attention and speed of psychomotor reactions (driving a car and other vehicles, working with moving mechanisms, working as a dispatcher and operator).

Overdose

Symptoms: increased manifestations of the described side effects, with the exception of allergic reactions.

Treatment: drug withdrawal, symptomatic therapy.

Side effects Teraligen valenta 5 mg 100 pcs. film-coated tablets

Side effects are extremely rare and mild.

From the nervous system: drowsiness, lethargy, fatigue (occurs mainly in the first days of use and rarely requires discontinuation of the drug), paradoxical reaction (anxiety, agitation, nightmares, irritability); confusion, extrapyramidal disorders (hypokinesia, akathisia, tremor).

From the senses: blurred visual perception (accommodation paresis), noise or ringing in the ears.

From the cardiovascular system: dizziness, decreased blood pressure (BP), tachycardia.

From the digestive system: dryness of the oral mucosa, atony of the gastrointestinal tract, constipation, loss of appetite.

From the respiratory system: dry nose, throat, increased viscosity of bronchial secretions.

From the urinary system: bladder atony, urinary retention.

Other: allergic reactions, inhibition of bone marrow hematopoiesis, increased sweating, muscle relaxation, photosensitivity.

Drug interactions

Alimemazine enhances the effects of narcotic analgesics, hypnotics, anxiolytic (tranquilizers) and antipsychotic (neuroleptic) drugs (drugs), as well as drugs for general anesthesia, m-anticholinergic drugs and antihypertensive drugs (dose adjustment required).

Tricyclic antidepressants and anticholinergic drugs enhance the m-anticholinergic activity of alimemazine.

With the simultaneous use of alimemazine with ethanol, increased depression of the central nervous system is possible.

Alimemazine weakens the effect of phenamine derivatives, m-cholinomimetics, ephedrine, guanethidine, levodopa, dopamine.

When alimemazine is used together with antiepileptic drugs and barbiturates, the threshold for convulsive activity is reduced (dose adjustment required).

When alimemazine is used together with beta-blockers, a pronounced decrease in blood pressure and arrhythmias are possible.

Alimemazine weakens the effect of bromocriptine.

With simultaneous use in nursing mothers, an increase in the concentration of prolactin in the blood serum is possible.

With the simultaneous use of alimemazine and MAO inhibitors (simultaneous use is not recommended) and alimemazine and phenothiazine derivatives, the risk of arterial hypotension and extrapyramidal disorders increases.

With the simultaneous use of alimemazine with drugs that inhibit bone marrow hematopoiesis, the risk of myelosuppression increases.

The combined use of phenothiazine derivatives (which includes alimemazine) with hepatotoxic drugs may enhance the manifestations of hepatotoxicity of the latter.

Instructions for use of the drug Teraligen

Teraligen is taken orally, distributing the daily dose 3-4 times. It should be remembered that the effect of the drug begins 15-20 minutes after administration and lasts about 6-8 hours. Only a doctor can make a diagnosis and prescribe a dosage of medication! Do not self-medicate, it is dangerous.

Recommended dosage for adults:

For difficulty falling asleep: 5-10 mg 1 time per day, 30 minutes before bedtime;
For anxiety: 20 mg 3-4 times a day;
For psychotic conditions: 50-100 mg 4 times a day.

Recommended dosage for children over 7 years of age:

For difficulty falling asleep: 2.5-5 mg 1 time per day, 30 minutes before bedtime;
For allergies: 2.5-5 mg 3-4 times a day;
For anxiety: 5-10 mg 3-4 times a day;
For psychotic conditions: 15 mg 4 times a day.

Psychotropic drugs with multireceptor activity, in particular traditional minor neuroleptics, have firmly won their place not only in psychiatry, but also in many other areas of medicine. However, today there is a tendency to give preference to modern atypical psychotropic drugs due to their greater selectivity of action and better tolerability. But, as practice shows, not all “new” drugs can demonstrate high efficiency, and in turn, not all “old” drugs are characterized by a high severity of adverse effects and can successfully compete with modern drugs in terms of effectiveness. Teraligen (alimemazine) occupies a special place in the group of traditional minor antipsychotics. Alimemazine is one of the phenothiazine derivatives - 10-(3-dimethylamino-2-methylpropyl)-phenothiazine hydrotartrate - and is close in chemical structure to diprazine and levomepromazine. This drug was synthesized in France in the laboratory in 1958 and quickly found its use as a strong “neurostatic, antihistamine and vegetotropic drug” [17]. It is distributed under the trade names: Panectyl - in Canada, Repeltin - in Germany, Temaril - in the USA, Theralen - in France and Italy, Vallergan - in England, etc.

Currently, in Russia, alimemazine exists under the commercial name “Teraligen” and is produced.

The pharmacological properties of alimemazine were first studied by S. Courvoisier [17], I. Rosenblum [24] and A. Fernandez-Zoila [18]. In comparative studies, these authors found that alimemazine has a less pronounced adrenolytic effect than chlorpromazine and is inferior to it in the severity of its antiemetic and general depressive effects, but is superior to it in its effect on the general tone of the autonomic nervous system and in its antispasmodic effect on smooth muscles , as well as antihistamine and antiserotonin effects. Subsequently, many researchers turned to the study of alimemazine, finding new facets of the use of the drug. It was found that alimemazine combines neuroleptic and anxiolytic properties and has significantly less parkinsonian and hypotensive effects than other phenothiazine derivatives. According to the results of early [16, 21, 22, 23] and more modern studies [5, 6, 8] of the mechanism of action of alimemazine, it was found that it has antihistamine, antispasmodic, serotonin-blocking, moderate α-adrenergic blocking, as well as antiemetic, hypnotic, sedative and antitussive actions. The antipsychotic effect is due to the blockade of dopamine D2 receptors of the mesolimbic and mesocortical systems and is implemented in a dose of 200 mg/day, according to the instructions. The vegetative stabilizing effect is associated with the blockade of noradrenergic receptors. Sedative and hypotensive effects are caused by blockade of adrenergic receptors of the reticular formation of the brain stem; sleeping pills and antihistamines - with blockade of histamine receptors; anxiolytic effect - with blockade of serotonin and adrenergic receptors; the antispasmodic effect is associated with blocking cholinergic and noradrenergic receptors; antiemetic effect - with blockade of D2 receptors of the trigger zone of the vomiting center; hypothermic effect - with blockade of dopamine receptors of the hypothalamus. The effect of the drug begins 15–20 minutes after taking it, and the duration of action is 6–8 hours.

Due to its properties, alimemazine quickly found application in a variety of areas of clinical medicine. As a drug that has an antiallergic effect and affects the general tone of the autonomic nervous system [1, 3, 12], the drug began to be used in the practice of treating skin diseases (pruritic and allergic dermatoses) [13, 20] and internal diseases (for dyspneic disorders), otorhinolaryngology (Meniere's disease and Meniere-like attacks), various allergic diseases [5, 21]. In addition, alimemazine is used during the preparation of patients for such painful and complex procedures and studies as esophagoscopy, gastroscopy, etc. In gastroenterology, it is also used to relieve pain in peptic ulcers and chronic colitis [5, 8]. In gynecological practice, the drug is used for premenstrual syndrome, dysmenorrhea, chronic inflammatory processes in the pelvis, lumbodynia, etc. [23].

Being an antipsychotic, Teraligen (alimemazine) has found its widest use in psychiatry and neurology. According to A. Fernandez-Zoila [18], who studied the drug in outpatient practice, Teraligen has pronounced tranquilizing and hypnotic effects. In the treatment of psychotic disorders, it can soften the manifestations of states of psychomotor agitation, hallucinations and normalize sleep. According to various authors [4, 11, 14, 15, 16], Teraligen occupies one of the most important places among anxiolytics, and combination treatment in combination with antidepressants, depending on the characteristics of the structure of the psychopathological syndrome, significantly increases its therapeutic effect in the treatment of affective and neurotic disorders.

Today, in practical psychiatry, Teraligen is equally widely used in hospitals and in outpatient care, both as the main therapeutic drug and in combination with other psychotropic drugs, incl. and neuroleptics. Most often, Teraligen is prescribed for the treatment of borderline and neurotic disorders, in particular hypochondriacal and somatoform conditions with gastrointestinal dysfunction. Clinical example: patient T., 53 years old. Diagnosis: post-traumatic stress disorder, somatoform disorder (ICD-10 code F43.1, F45.32). Nurse, married, has an adult son. Throughout her life she was extremely responsible, efficient, and anxious. After the death of her mother 3 years ago, she grieved the loss, regretted that she might not have done what she could, and felt a sense of guilt. Night sleep was permanently disturbed. Later, about two years ago, she began to notice dyspeptic disorders, mainly in the form of diarrhea after any stressful situations for herself. Subsequently, I almost constantly felt discomfort in the intestinal area, rumbling in the stomach, frequent bowel movements, was fixated on my sensations, and could not fully work. I consulted a gastroenterologist and took treatment that did not bring much effect or the effect was short-lived. I felt disappointed, confused, and suspected an incurable disease. She visited a psychiatrist with complaints of anxiety and insomnia. According to the Hamilton HARS scale, the level of anxiety disorders corresponded to 28 points (high level of anxiety). A β-blocker, an antidepressant from the group of serotonin reuptake inhibitors and Teraligen were prescribed with a gradual increase in the daily dose to 20 mg per day. For the first 3–4 days, the patient experienced severe drowsiness and lethargy. Then she became somewhat more active. During the first five days, the patient's fixation on unpleasant bodily sensations decreased, the feeling of rumbling and bloating decreased, the urge to defecate began to decrease, and falling asleep improved. When assessed on the Hamilton HARS scale, a decrease in the level of anxiety was revealed to 19 points (average level, closer to high). Subsequently, after about 10–14 days, discomfort in the intestinal area decreased significantly and stool returned to normal.

In the treatment of this patient, Teraligen was used as an anti-anxiety, antidepressant, vegetostabilizing, antispasmodic and hypnotic agent. All this was achieved due to the multireceptor effect of the drug associated with the blockade of noradrenergic, histamine, serotonin receptors, as well as cholinergic and adrenergic receptors.

Teraligen is effective in the treatment of panic disorders, incl. with respiratory dysfunction. Clinical example: patient A. 28 years old. Diagnosis: panic disorder in a hysterical personality, adaptation disorder in the form of a mixed anxious and depressive reaction (F41.1, F60.4, F43.22). Middle manager, divorced, has an 8-year-old son. She complained of periodic panic attacks with palpitations, a feeling of suffocation, and fear of death. Such attacks usually occur in transport, closed, crowded spaces. The patient is forced to leave the place where the attack occurs and tries to avoid crowds of people. The attacks last from 40 minutes to an hour, then gradually pass after a change of environment. Subsequently, the patient experiences weakness, lethargy, and tearfulness. Previously, such episodes were noted several times in adolescence, but then spontaneously - without special treatment - stopped. The current deterioration of her condition arose against the background of the divorce process, which the patient perceives extremely painfully, considering herself to be the disadvantaged, offended party. Outside of attacks, the patient experiences a depressed mood with anxiety about the future, often cries, cannot fully engage with her child, lies a lot, demands the attention of relatives and friends, and experiences a constant feeling of lack of air. Night sleep is not disturbed. At the appointment she is capricious, demonstrative, demanding of the doctor, and talks about the real risk of “dying of fear.” During the conversation he sobs noisily, but afterwards he calms down and agrees with the proposed treatment. When assessing the state on the Hamilton HARS scale, a high level of anxiety was revealed, corresponding to 38 points. Prescribed: β-blockers, an antidepressant from the group of serotonin reuptake inhibitors, Teraligen with a gradual increase in dose to 30 mg per day. During the first week of treatment, general anxiety decreased somewhat, but drowsiness was noted during the day. Starting from the 8th–9th day of admission, the patient became more active, began to go outside, and her mood improved. When assessing the condition on the HARS scale, 19 points were noted (the average level is closer to high). After 14 days from the start of treatment, the patient was able to travel several stops on the subway. While on the road, I experienced tension associated with the expectation of a possible attack, but there was no pronounced panic with palpitations and a feeling of lack of air. Subsequently, during the month of taking the prescribed therapy, she regularly used transport and visited shops. She noted minor discomfort, which she dealt with. I was critical of my feelings. On the HARS scale, the level of anxiety disorders corresponded to 13 points (average level). In the treatment of this patient, Teraligen was also used as an anti-anxiety, antidepressant, vegetative stabilizing and antispasmodic agent. Accordingly, clinical effects were achieved through effects on noradrenergic, serotonin, cholinergic and adrenergic receptors.

Teraligen is effective in the treatment of somatoform autonomic dysfunction of the cardiovascular system. Clinical example: patient I., 63 years old, pensioner. Diagnosis: adaptation disorder in the form of a mixed anxiety and depressive reaction, somatoform disorder (F43.22, F45.30). The patient complained of increased nervousness and anxiety, usually associated with solving real pressing problems. Lately he has noticed a decrease in emotional stability even to minor problems. I began to notice similar phenomena after menopause. About 10 years ago, he was diagnosed with hypertension, is being seen by a therapist, and is receiving appropriate treatment. But in emotionally significant situations, he notes an increase in blood pressure, palpitations, increased heart rate, tremor of the fingers, and sometimes a feeling of coldness in the extremities. Periodically experiences difficulty falling asleep, usually associated with emotional stress. On the Hamilton scale, the level of anxiety corresponded to 23 points (medium level of anxiety, closer to high). Prescribed: an antidepressant from the group of serotonin and norepinephrine reuptake inhibitors, Teraligen at a dose of up to 15 mg daily. During the first 3 days of treatment, during the treatment, she noted some lethargy and a feeling of dullness in the morning. Then gradually over the next 4 days these phenomena were reduced. She became more active and noted greater resistance to emotional stress. Episodes of high blood pressure have become much less frequent. In special situations, the patient independently resorts to a one-time additional dose of Teraligen in the amount of 2.5 mg, notifying the doctor. The level of anxiety on the Hamilton scale corresponds to 10 points (medium level, closer to low). As in the two previous cases, Teraligen was prescribed to this patient for vegetostabilizing hypotensive purposes as an anti-anxiety drug and as a means of improving night sleep. The clinical effect was achieved due to the effect of the drug on noradrenergic, histamine, serotonin and adrenergic receptors.

Teraligen is effective in the treatment of asthenic disorders associated with tension and insomnia. Clinical example: patient P., 42 years old. Diagnosis: neurasthenia (F.48.0). I went to see a psychiatrist for the first time. All his life he was an active, active person. Successfully moved up the career ladder. Currently he is the head of a large enterprise, with more than 100 people subordinate to him. Married, has children. After an unfavorable period associated with work, against the background of increased physical and mental stress, in the last 2–3 months I began to notice rapid fatigue, a difficult feeling of internal tension to overcome, irritability directed mainly at loved ones, difficulty falling asleep and a lack of feeling of rest in the morning. On the Hamilton scale, the level of anxiety corresponded to 12 points (average level, closer to low). Was prescribed: nootropic therapy, Teraligen up to 7.5 mg per day. During the first 2–3 days, I began to notice an improvement in falling asleep, and after 5–7 days of use, irritability significantly decreased, self-control improved, and the feeling of internal tension disappeared. At this point, there was a reduction on the Hamilton scale and the level of anxiety corresponded to 6 (medium level, closer to low). In the treatment of this patient, Teraligen primarily served as a sedative and anxiolytic agent for the purpose of correcting behavior and increasing stress resistance, and also as a hypnotic. A quick effect was achieved thanks to Teraligen's effect on histamine, serotonin and adrenergic receptors in the form of their blockade.

As already mentioned, Teraligen is used in the complex treatment of endogenous mental disorders, usually in combination with other antipsychotics and antidepressants to reduce the level of agitation, anxiety and tension, which are often observed as part of affective-delusional attacks and major depressive episodes, as well as other affective disorders, continuous schizophrenia and personality disorders. In both cases, Teraligen does not act as the main therapeutic drug, but is often indispensable due to its effectiveness and lack of side effects. Clinical example: patient M., 26 years old. Diagnosis: schizotypal disorder (F21). Programmer, single, lives with parents. Over the course of 10 years, periodic depression has been observed, characterized by low mood with a feeling of inner emptiness, a dull perception of the surrounding life, lack of awareness of one’s feelings and thoughts, and other depersonalization and derealization disorders, which are present to one degree or another outside depressive episodes. Several times he suffered short-term subpsychotic episodes against the background of stressful situations and exogenous hazards. The personality of a patient of the schizoid type with the phenomena of psychophysical juvenileism, with isolation and elements of eccentricity, with unusual hobbies. As preventive and maintenance therapy, the patient takes an atypical antipsychotic with an antidepressant from the serotonin reuptake inhibitor group. During the period of remission, the patient successfully works and studies. With increased workload, the patient experienced asthenic phenomena in the form of increased nervousness, feelings of internal tension, periodic agitation, and difficulty falling asleep. The level of anxiety assessed on the Hamilton HARS scale corresponded to 17 points (average level, closer to high). At that time, a nootropic drug and Teraligen at a dose of 5 mg in the evening were added to the main maintenance regimen. The dose was selected empirically, based on the patient's subjective feelings. While taking Teraligen, already in the first 2-3 days the patient’s sleep improved at night, the feeling of internal tension in the evening significantly decreased, and his mood evened out. After re-evaluation a week later, the level of anxiety underwent a reduction and corresponded to 4 points, i.e. was absent. In this case, Teraligen was used as an adjunctive sedative-hypnotic, and the corresponding effects were associated with effects on histamine and adrenergic receptors. The rapid effect obtained as a result of the use of such small doses was made possible due to the mutually potentiating effect when using various psychotropic drugs.

In all the described cases, the effective dosage was selected individually by titration, and, as can be seen, in a number of cases the drug was effective even in small doses (2.5–5.0 mg/day). None of the described patients had adverse extrapyramidal effects. As is known from general information about the drug, Teraligen is taken orally. The daily dose can be divided into 3-4 doses. Adult patients take 2.5–5.0–10.0 mg per day (hypnotic effect) and more - up to 60–80 mg per day (anxiolytic effect). In a psychotic state, dosages of up to 0.2–0.4 g per day can be used. According to the instructions, drowsiness is observed in the first 3 days of use (regardless of the patient’s age). But it should be noted that the identification of different types of dosing is very arbitrary, because dosage selection is carried out individually. The drug is prescribed to children from 7 years of age [19]. Due to the very wide range of receptor effects and clinical use of Teraligen, the issue of interaction with other drugs becomes relevant [5, 8, 9].

Analysis of the characteristics of the drug’s action allows us to conclude that Teraligen:

enhances the effect of narcotic analgesics, ethanol, hypnotics, anxiolytic (tranquilizers) and antipsychotic drugs (neuroleptics), as well as drugs for general anesthesia, m-anticholinergic blockers, β-blockers and antihypertensive drugs (dose adjustment required);
weakens the effect of amphetamine derivatives, m-anticholinergic stimulants, ephedrine, guanethidine, levodopa, dopamine, as well as bromocriptine and increases the concentration of prolactin in the blood serum;
the use of Teraligen with antiepileptic drugs and barbiturates reduces the threshold of convulsive activity (dose adjustment required);
tricyclic antidepressants and anticholinergic drugs enhance the m-anticholinergic activity of Teraligen;
monoamine oxidase inhibitors (simultaneous administration with Teraligen is not recommended) and phenothiazine derivatives increase the risk of arterial hypotension and extrapyramidal disorders;
when Teraligen is co-administered with drugs that inhibit bone marrow hematopoiesis, the risk of myelosuppression increases;
hepatotoxic drugs increase the manifestations of hepatotoxicity of the drug Teraligen.

An objective assessment of the effectiveness of the drug is impossible without comparison with other drugs with similar indications for use. Compared to benzodiazepines, Teraligen has an undeniable advantage in the absence of the formation of drug dependence and, therefore, wider possibilities for long-term use [2]. Compared to diphenylmethane derivatives and fabomotizole, Teraligen demonstrates more pronounced anxiolytic activity and the rate of onset of the positive effect [7, 10]. When compared with drugs from the group of minor neuroleptics (periciazine, thioridazine, sulpiride), Teraligen is not inferior to them in terms of the level of sedation and significantly benefits in terms of the virtual absence of side extrapyramidal disorders, in contrast to the above-mentioned drugs, which have quite pronounced side effects [9]; in addition, thioridazine has severe cardiotoxicity, and sulpiride can cause hyperprolactinemia. These undesirable effects are not characteristic of Teraligen. Summarizing all of the above, Teraligen can be characterized as a drug with a wide range of clinical applications not only in psychiatry, but also in neurology and other areas of medicine for the treatment of somatoform, psychosomatic and somatic diseases, incl. and as part of complex therapy. Due to the wide range of dosages, good tolerability and the possibility of long-term use, Teraligen is not only an effective drug, but also extremely convenient to use for both the doctor and the patient.

Contraindications

Teraligen is prohibited for use in the following cases:

parkinsonism;
myasthenia gravis;
Reye's syndrome;
hypersensitivity;
simultaneous use of MAO inhibitors;
pregnancy;
breastfeeding period;
angle-closure glaucoma;
prostatic hyperplasia;
severe liver and kidney diseases;
children's age up to 7 years.

Teraligen is prohibited during pregnancy

Also, the drug is prescribed with caution when:

suppression of bone marrow function;
epilepsy;
arterial hypotension;
chronic alcoholism;
jaundice;
predisposition to urinary retention;
open-angle glaucoma;
obstruction of the bladder neck.

Clinical and pharmacological group

Antipsychotic drug (neuroleptic)

Contraindications

- angle-closure glaucoma;
- prostatic hyperplasia;
- severe liver diseases;
- severe kidney disease;
- parkinsonism;
- myasthenia;
- Reye's syndrome;
- simultaneous use of MAO inhibitors;
- pregnancy;
- period of breastfeeding;
- children under 7 years of age;
- hypersensitivity to the components of the drug.

The drug should be used with caution in chronic alcoholism if there is a history of complications when using phenothiazine drugs, obstruction of the bladder neck, predisposition to urinary retention, epilepsy, open-angle glaucoma, jaundice, suppression of bone marrow function, arterial hypotension.

Dosage

The drug should be taken orally, dividing the daily dose into 3-4 doses.

The onset of action of the drug is after 15-20 minutes, the duration of action is 6-8 hours.

For adults, to achieve a hypnotic effect, 5-10 mg/day; to achieve an anxiolytic effect, 60-80 mg/day. For psychotic conditions - 200-400 mg/day.

Children over 7 years of age (depending on age and body weight) to achieve a hypnotic effect, 2.5-5 mg/day; as a symptomatic treatment of allergic reactions, 5-20 mg/day; to achieve an anxiolytic effect, 20-40 mg/day; in psychotic conditions, it is possible to increase the daily dose of the drug to 60 mg/day.

Side effects

From the central nervous system and peripheral nervous system: drowsiness, lethargy, fatigue (occurs mainly in the first days of taking the drug and rarely requires discontinuation of the drug), paradoxical reaction (restlessness, agitation, nightmares, irritability); rarely - confusion, extrapyramidal disorders (hypokinesia, akathisia, tremor); increased frequency of night apnea, increased seizure activity (in children).

From the senses: blurred visual perception (accommodation paresis), noise or ringing in the ears.
From the cardiovascular system: dizziness, decreased blood pressure, tachycardia.
From the digestive system: dry mouth, gastrointestinal atony, constipation, loss of appetite.
From the respiratory system: dry nose, throat, increased viscosity of bronchial secretions.
From the urinary system: bladder atony, urinary retention.

Other: allergic reactions, inhibition of bone marrow hematopoiesis, increased sweating, muscle relaxation, photosensitivity.

The drug is usually well tolerated by patients. Side effects are rare and mild.

Overdose

Symptoms: depression of consciousness, increased adverse reactions.

Treatment: symptomatic.

Drug interactions

Alimemazine enhances the effect of opioid analgesics, hypnotics, anxiolytic (tranquilizers) and antipsychotic (neuroleptics) drugs, as well as drugs for general anesthesia, m-anticholinergic drugs and antihypertensive drugs. The dose of alimemazine should be adjusted when used concomitantly with the above-mentioned drugs.
With the simultaneous use of alimemazine with amphetamine derivatives, m-cholinomimetics, ephedrine, guanethidine, levodopa, dopamine, the effect of the latter is weakened.
When alimemazine is used concomitantly with ethanol and drugs that depress the central nervous system, central nervous system depression is observed.
With the simultaneous use of alimemazine with antiepileptic drugs and barbiturates, the threshold for convulsive readiness is reduced (dose adjustment of the drug is required).
With the simultaneous use of alimemazine with beta-blockers, the concentration of the latter in the plasma increases (a pronounced decrease in blood pressure and arrhythmias is possible).
With the simultaneous use of alimemazine with bromocriptine, the effect of the latter weakens and the concentration of prolactin in the blood serum increases.
With the simultaneous use of alimemazine with tricyclic antidepressants and anticholinergic drugs, the m-anticholinergic activity of alimemazine is enhanced.
With simultaneous use of alimemazine with MAO inhibitors and phenothiazine derivatives, the risk of arterial hypertension and extrapyramidal disorders increases (simultaneous use is not recommended).
With the simultaneous use of alimemazine with drugs that inhibit bone marrow hematopoiesis, the risk of myelosuppression increases.
With the simultaneous use of alimemazine with hepatotoxic drugs, the manifestations of hepatotoxicity of the drug increase.

special instructions

During long-term treatment, a general blood test should be systematically performed and liver function assessed.
Alimemazine may mask the ototoxic effect (tinnitus, dizziness) of co-administered drugs.
To prevent distortion of the results of skin prick tests for allergens, the drug should be discontinued 72 hours before allergy testing.
During treatment, false positive pregnancy test results are possible.
During treatment you should not drink alcohol.
Impact on the ability to drive vehicles and operate machinery
During treatment with the drug, you should not engage in activities that require increased concentration.

Pregnancy and lactation

The use of the drug during pregnancy and breastfeeding is contraindicated.

Use in childhood

Contraindicated in children under 7 years of age.

For impaired renal function

The use of the drug is contraindicated in severe kidney disease.

For liver dysfunction

The use of the drug is contraindicated in severe liver diseases. During long-term treatment, liver function should be systematically assessed.

Conditions for dispensing from pharmacies

The drug is available with a prescription.

Storage conditions and periods

The drug should be stored out of the reach of children, in a dry place, protected from light, at a temperature not exceeding 25°C. Shelf life: 3 years.

Release form, composition and packaging

Dark pink film-coated tablets with an embossed symbol on one side and a stripe on the other.

1 tab.

alimemazine tartrate

5 mg

Excipients: lactose, colloidal silicon dioxide, refined sugar (sucrose), wheat starch, tapioca starch (tapioca), talc, magnesium stearate.

Shell composition: hypromellose, macrogol 6000, titanium dioxide, Osprey R110 pink dye, talc.

10 pieces. — cellular contour packages (1) — cardboard packs.
10 pieces. — contour cell packaging (2) — cardboard packs.
10 pieces. — contour cell packaging (5) — cardboard packs.
25 pcs. — cellular contour packages (1) — cardboard packs.
25 pcs. — contour cell packaging (2) — cardboard packs.
25 pcs. — contour cell packaging (5) — cardboard packs.

Side effects

Judging by the clinical data, patients taking Teraligen tablets tolerate the drug well. Therefore, the occurrence of side effects is rare. But if they do exist, then the list of side effects is as follows:

From the genitourinary system: urinary retention, bladder atony.
From the respiratory system: increased viscosity of bronchial secretions, dryness of the mucous membrane of the nose and pharynx.
Allergic reactions: urticaria, photosensitivity, allergic dermatitis, Quincke's edema.
Laboratory indicators: false positive pregnancy test result.
From the senses: decreased visual acuity, ringing and tinnitus. From the blood vessels and heart: arterial hypotension, cardiac arrhythmia, dizziness.
From the digestive tract: dry mouth, intestinal atony, anorexia, constipation.
From the nervous system: asthenia, drowsiness, fatigue, paradoxical reactions (including anxiety, nightmares, irritability and agitation), confusion. In addition, it is possible to develop increased frequency of sleep apnea, increased seizure activity, as well as extrapyramidal disorders (including akathisia, hypokinesia and tremor).
Others: increased sweating, decreased bone marrow function, muscle relaxation.

In addition, alimemazine can distort the results of skin prick tests for various allergens. Therefore, if you are having an allergy test, you should stop taking the drug no later than 72 hours in advance.

Teraligen® Valenta

In adults and children from 7 years of age

As a sedative (calming), anxiolytic (anti-anxiety) and sleep aid

— dementia

(including dementia due to epilepsy), occurring with manifestations of psychomotor agitation, anxiety affect (as part of combination therapy);

— organic anxiety disorder

(as monotherapy or as part of combination therapy);

— schizophrenia

(with a predominance of neurosis-like disorders, as part of combination therapy);

— mood disorders

(affective disorders) - as part of combination therapy;

— generalized anxiety disorder

(as part of combination therapy);

— obsessive-compulsive disorder

(as part of combination therapy);

— reaction to severe stress and adaptation disorders

(acute stress reaction, post-traumatic stress disorder, unspecified reaction to severe stress, other reactions to severe stress) - as part of combination therapy;

— dissociative (conversion) disorders

(as part of combination therapy
);
- somatoform disorders

(somatization disorder, undifferentiated somatoform disorder, hypochondriacal disorder, somatoform dysfunction of the autonomic nervous system, persistent somatoform pain disorder, unspecified somatoform disorder, other somatoform disorders) - as part of combination therapy for severe anxiety or when standard therapy is ineffective;

— unspecified autonomic nervous system disorder, other autonomic nervous system disorders

(as part of combination therapy);

— anorexia nervosa

(as part of combination therapy);

— emotionally unstable personality disorder (impulsive and borderline types)

- as part of combination therapy;

— histrionic personality disorder, anxious (avoidant) personality disorder

(as part of combination therapy);

— persistent personality changes after experiencing a disaster

(as part of combination therapy);

— hyperkinetic behavior disorder

(as part of combination therapy);

— family-confined conduct disorder

(as part of combination therapy when standard therapy is ineffective);

— unsocialized behavior disorder

(as monotherapy or as part of combination therapy);

— restlessness, agitation and other symptoms and signs related to emotional state

(as part of combination therapy);

- other neurotic disorders
(neurasthenia, unspecified neurotic disorder)
- as part of combination therapy;

— insomnia of non-organic etiology

(as part of combination therapy when standard therapy is ineffective);

— emotional disorders whose onset is specific to childhood

(phobic anxiety disorder in childhood, social anxiety disorder in childhood, sibling rivalry disorder, unspecified emotional disorder in childhood, other emotional disorders in childhood) - as part of combination therapy.

As an antiallergic agent

— itching regardless of location and etiology

(pruritus of the anus, pruritus of the vulva, unspecified anogenital pruritus, pruritus due to photocontact dermatitis and solar urticaria, dermatitis, eczema, urticaria, bites or stings from non-venomous insects or other non-venomous arthropods, chickenpox, measles, Hodgkin's disease, diabetes mellitus, shingles lichen) in the form of monotherapy or as part of combination therapy;

— asthma, hay fever, whooping cough

(as part of complex therapy as an antiallergic agent to relieve cough, shortness of breath and asthma attacks);

— unspecified allergy

(as monotherapy or as part of combination therapy).

In children from 3 years old

As an antiallergic agent

— itching regardless of location and etiology

(itching from photocontact dermatitis and solar urticaria, dermatitis, eczema, urticaria, bites or stings from non-venomous insects or other non-venomous arthropods, chickenpox, measles, Hodgkin's disease, diabetes mellitus, herpes zoster, anal itching, vulvar itching, unspecified anogenital itching) as monotherapy or as part of combination therapy.

As a sedative (calming) agent

— during medicinal preparation for surgery

(for the purpose of sedation before surgery).

Analogs of the drug Teraligen

Teraligen has no analogues for the active substance - alimemazine tartrate. Substitutes that have a similar pharmacological effect belong to the group of neuroleptics.

Remember that the attending physician must prescribe medications, as well as substitutes!

Remember that the attending physician prescribes medications or their analogues

Klopiksol

Clopixol tablets contain zuclopenthixol hydrochloride. Although this is in some sense a substitute for Teraligen, and they are similar in pharmacological action, Klopixol has a stronger antipsychotic effect. Thanks to this, Clopixol is more often used to treat serious mental health disorders: schizophrenia, hallucinations, paranoia, manic states, dementia.

Clopixol is contraindicated in comatose states, acute poisoning by barbiturates, alcohol, opiates, pregnancy and breastfeeding. Clopixol, unlike Teraligen, is better tolerated by patients. Side effects are similar to Teraligen, but occur even less frequently and are not as pronounced.

Conapax

It is also an antipsychotic drug based on thioridazine hydrochloride. Sonapax has a more pronounced antihistamine and anticholinergic effect compared to other neuroleptics. Indicated for use in those cases described in the instructions for Teraligen. But it can be used to treat children from 4 years of age. Conapax is contraindicated in comatose states, acute depression, porphyria, pheoxomocytoma, hematopoietic disorders, in the first trimester and in the last week of pregnancy, during lactation tions. Sonapax is well tolerated, it can be taken by children, and its price is lower than Teraligen.

Chloprothixene Zentiva

The main active ingredient of Sanofi Chloprothixene tablets is chlorprothixene. Medicines are indicated for the treatment of: psychoses, schizophrenia, depressive states, mental disorders during menopause and for diseases of the brain (traumatic brain injuries, enc ephalopathy), alcoholic delirium, sleep disorders caused by psychosomatic and neurotic disorders, insomnia due to burns, skin diseases, accompanied by itching. Contraindications for use: hypersensitivity, coma, poisoning with drugs that depress nervous activity. When taking tablets, in addition to the side effects characteristic of Teraligen, disorders of the mammary glands and reproductive organs are possible: galactorrhea, amenorrhea, gynecomastia, c decreased libido.

Pipolfen

This is a Hungarian analogue of Teraligen based on promethazine hydrochloride. It is often used as a sedative for postoperative pain (in combination with analgesics), allergic diseases and other cases. Pipolfen has a fairly large list of contraindications and age restrictions, so before treatment, be sure to consult a specialist and read the instructions.

Teraligen and alcohol

The combination of drugs and alcohol does not go away without leaving a trace; it can often lead to very serious consequences. You should be especially careful when taking psychotropic medications like Teraligen.

Teraligen should not be taken with alcohol!

The instructions attached to the medication clearly indicate that it is strictly forbidden to take it with alcohol, since it can only increase the severity and intensity of the underlying pathology.

The annotation for the drug indicates the side effects that occur when combining Teraligen + Alcohol:

irritability and anxiety, nightmares and emotional overexcitement;
drowsiness and excessive fatigue, lethargy;
confusion;
visual impairment, manifested by blurred perceived image;
disorders such as tremor, an internal need to constantly move, or, conversely, a condition associated with insufficient movement activity;
frequent cases of respiratory arrest during night sleep;
extraneous sounds in the ears, frequent dizziness and fainting, decreased blood pressure;
dryness of the mucous membranes in the mouth, nasal cavity, pharynx, lack of appetite, various allergic manifestations;
tachycardia disorders, hyperhidrosis, disorders in bone marrow hematopoiesis;
urinary retention;
lack of normal tone in the muscular system of the gastrointestinal tract, bladder, as well as muscle relaxation, etc.

Remember that antipsychotic drugs have a strong effect on the central nervous system. Only a doctor can prescribe antipsychotics. In addition, a prescription is required to purchase such medications.

Stopping taking antipsychotics (advice from an old psychiatrist)

When are antipsychotics prescribed?

Discontinuation of treatment with antipsychotics is possible and advisable in a number of clinical cases. Patients requiring long-term treatment may need to switch from one antipsychotic to another antipsychotic if their response to treatment has been inadequate or side effects have occurred. Some psychiatrists believe that some antipsychotics are more effective for psychosis than others - Clozapine is considered the most effective antipsychotic, followed by the moderately effective group consisting of Amisulpride, Olanzapine, Risperidone and Paliperidone, and then the remaining new and old antipsychotics such as Haloperidol and Chlorpromazine. on the contrary, other psychiatrists believe that haloperidol is one of the best antipsychotics. A number of psychiatrists believe that antipsychotics can be used for severe major depression, when rapid relief of agitation, insomnia and prevention of the risk of suicide is needed while awaiting the action of antidepressants.

Side effects of antipsychotics

Long-term use of antipsychotic medications can have serious consequences, including tardive dyskinesia, weight gain, metabolic syndrome, diabetes, and cardiovascular complications.

Stopping taking antipsychotics

When discontinuing an antipsychotic, individual circumstances must be carefully considered, including disease severity and medical history, risk of relapse and its consequences, response to treatment and prognostic factors, and the patient's social situation. Antipsychotic medications should be discontinued very slowly under close medical supervision. Abrupt cessation of treatment may result in psychosis, which may be more severe than before antipsychotic treatment was started. This is not uncommon when clozapine is discontinued due to complications such as agranulocytosis or myocarditis. Depending on the pharmacological action of the antipsychotic, several withdrawal syndromes may occur.

When assessing the benefits and harms of taking an antipsychotic, careful consideration should be given to the severity of the disease, complications of treatment (eg, obesity), previous pattern of relapse, risk to self and others, and the psychosocial consequences of relapse. Repeated episodes of psychosis worsen long-term prognosis. Because the risk of relapse after a second episode is high, most doctors recommend long-term treatment.

When can antipsychotics be safely discontinued?

Antipsychotics can be discontinued calmly if antipsychotics (eg, low-dose quetiapine) have been used for anxiety or sleep disturbances and ongoing treatment is not required or desired; antipsychotics have been used to treat disruptive behavior in dementia but are no longer needed due to proper behavioral correction or positive influence of the patient’s environment. In addition, antipsychotics should be discontinued if antipsychotic drugs have been tested for indications not covered by the instructions and turned out to be ineffective.

Withdrawal of antipsychotics after severe depression

Patients who have experienced psychotic depression and have responded to a combination of antidepressants and antipsychotics with or without electroconvulsive therapy can often continue treatment with antidepressants alone. There are no clear recommendations regarding when antipsychotics should be discontinued in such patients. However, after the patient has recovered for some time, it is often possible to gradually reduce the dose while continuing to monitor the patient's mental state (especially if serious risk factors such as suicidality were present initially).

Discontinuation of antipsychotics under medical supervision

Under the supervision of a psychiatrist, antipsychotics are discontinued in the following cases: after the first episode of psychosis, there was a high-quality remission for a year (up to 40% of patients who experienced one episode of psychosis may remain healthy after stopping antipsychotic drugs, or at least need only low doses ), in bipolar mood disorder when antipsychotic drugs are no longer needed, especially if lithium monotherapy is appropriate. If there have been two episodes of psychosis, then taking an antipsychotic medication for at least two years is required. Antipsychotics may also be discontinued under medical supervision if there has been complete recovery from drug-induced psychosis and clinical assessment indicates that antipsychotic treatment is no longer necessary (eg, drug use has ceased). Many psychiatrists believe that if there have been several episodes of psychosis or recovery has been incomplete, then ongoing treatment with antipsychotics is recommended, since the likelihood of exacerbation or relapse of psychosis is high when the drug is stopped.

Discontinuation of long-acting antipsychotics

Some antipsychotics (especially depot injections) have a long half-life and are unlikely to be associated with significant withdrawal symptoms.

Change of antipsychotic

There are a number of clinical situations in which switching from one antipsychotic to another is considered. Before switching, an examination by a psychiatrist is recommended, especially in complex clinical situations or when urgent switching is necessary. A change in antipsychotic drug is recommended when there is an inadequate clinical response to acute symptoms despite dose optimization and adequate duration of treatment. A change in antipsychotic drug is possible if there is poor control of chronic symptoms of psychosis and functional impairments persist during maintenance therapy, if there has been a relapse despite adequate preventive or supportive treatment of a psychotic illness. Persistence of certain symptoms of psychotic illness (eg, negative symptoms and cognitive dysfunction) despite adequate doses of one antipsychotic that may respond better to an alternative antipsychotic is also an indication for a change in medication. Unacceptable side effects at low therapeutic doses before clinical response occurs in susceptible individuals (eg, extrapyramidal effects in Asian patients) also warrant consideration of switching to antipsychotics with a lower risk of side effects. The need to change an antipsychotic due to a physical complication (eg, ziprasidone is contraindicated in cardiovascular disease, antipsychotics that cause severe hyperprolactinemia are contraindicated in breast cancer) are known reasons for changing antipsychotics. Poor adherence to treatment is an indication for switching from an oral antipsychotic to a long-acting injectable depot form.

Switching from one antipsychotic to another is not necessarily a panacea. During the switch, an exacerbation of the disease may occur and new side effects may appear. When switching is made due to an inadequate response, it is important to ensure that the dose of the first antipsychotic has been optimized, the patient has been treated for an adequate period of time, and that the patient is compliant and tolerant of treatment.

These factors must be taken into account when changing antipsychotic drugs.

The choice of a new drug will be determined in part by the reasons for switching, but also must take into account the likely effectiveness, side effects, dosing regimen, and patient or caregiver preferences.

Withdrawal syndrome

Depending on the pharmacology of the antipsychotic, switching from one antipsychotic to another may lead to withdrawal syndromes, especially the withdrawal of anticholinergic drugs such as Quetiapine, Clozapine, Chlopromazine and Olanzapine. Switching from one antipsychotic to another (for example, when looking for a drug with a lower risk of weight gain) may result in loss of effectiveness and withdrawal symptoms.

Clozapine withdrawal

When a patient is switched from clozapine to another antipsychotic, recurrent psychosis and other serious withdrawal effects may occur, regardless of which drug the clozapine is changed to. Discontinuation of clozapine should be done under the supervision of a psychiatrist. The dose should be gradually reduced and not stopped suddenly. However, sometimes this may be unavoidable if, for example, we observe agranulocytosis.

How to stop a neuroleptic

Unlike switching antidepressants, a drug-free period between stopping the first antipsychotic and starting a second is not recommended due to the risk of relapse. When switching from an oral antipsychotic to a depot, depot to depot, or depot to oral, special instructions must be followed.

Direct switching

Although it is possible to stop taking the first drug and immediately start taking the second the next day, this can lead to withdrawal symptoms and possible drug interactions. When the first antipsychotic is Aripiprazole or brexpiprazole, it is possible to switch to them immediately, since both of these drugs have a very long half-life and do not have anticholinergic effects.

Cross titration

Available data in the literature indicate little difference in the risk of relapse between immediate and gradual discontinuation or switching of antipsychotics. Most psychiatrists use a cross-titration strategy. (reducing the dose of the first antipsychotic when introducing the second). A slower approach to titration is to continue taking the first antipsychotic for a certain period at its usual dose, while gradually increasing the therapeutic dose of the second antipsychotic. The first antipsychotic can then be gradually reduced and discontinued. This approach minimizes the risk of relapse, but may cause additional side effects.

When it is necessary to switch from one antipsychotic to another during the treatment of psychosis, clinicians need to have some understanding of the pharmacokinetics and dynamics of antipsychotic drugs in order to plan and carefully monitor the switch. This usually involves taking both drugs at the same time. Stopping and switching antipsychotic medications can lead to serious consequences, especially relapse of psychosis, which can carry serious risks and worsen long-term prognosis. Withdrawal syndromes associated with cholinergic and dopaminergic effects may occur depending on the characteristics of the antipsychotic drugs taken.