Antidepressant round tablets in a brown shell. Truxal instructions for use, contraindications, side effects, reviews

Truxal is a neuroleptic drug with antipsychotic, pronounced sedative and moderate antidepressant effects.

Release form and composition

Truxal is available in film-coated tablets:

25 mg each – biconvex, round; shell – dark brown;
50 mg each – biconvex, oval; the shell is dark brown.

The drug is packaged in plastic containers with a screw cap and tamper evident (50 or 100 tablets) and cardboard packs (1 container per pack).

1 tablet contains:

active ingredient: chlorprothixene hydrochloride – 25 or 50 mg;
excipients: copovidone, corn starch, lactose monohydrate, glycerol 85%, croscarmellose sodium, microcrystalline cellulose, magnesium stearate, talc;
shell composition: Opadry OY-S-9478 brown (macrogol 400, hypromellose, titanium dioxide, black iron oxide, red iron oxide).

Indications for use

withdrawal syndrome in drug addiction and alcoholism;
schizophrenia and other psychoses accompanied by anxiety, agitation and psychomotor agitation;
psychosomatic disorders, depressive states, neuroses with tension, anxiety, restlessness, sleep disorders;
mental retardation and epilepsy, accompanied by agitation, agitation, behavioral disorders and mood lability;
irritability, hyperactivity, agitation, anxiety, sleep and behavior disorders, confusion;
sleep and behavior disorders in childhood;
pain syndrome;
spastic conditions in the gastrointestinal tract;
whooping cough;
allergic reactions;
dermatoses that are accompanied by persistent itching;
premedication.

Contraindications

myelodepression;
vascular collapse;
clinically significant cardiovascular diseases (decompensated heart failure, cardiac hypertrophy, recent myocardial infarction, bradycardia, arrhythmias, the treatment of which uses class IA and III antiarrhythmics, ventricular arrhythmias, polymorphic torsade de pointes ventricular tachycardia), including a history;
congenital or acquired long QT interval syndrome (more than 470 ms in women and 450 ms in men);
simultaneous use of drugs that prolong the QT interval;
cerebral atherosclerosis;
depression of consciousness of any etiology (including due to the use of opiates, alcohol or barbiturates), coma;
elderly age;
hereditary galactose intolerance, impaired absorption of galactose and glucose, Lapp lactase deficiency;
pathological changes in the blood picture;
uncorrectable hypomagnesemia or hypokalemia;
hypersensitivity to any components of the drug.

Truxal is taken with caution in the following cases:

mental retardation;
organic brain diseases;
presence in the family history of cases of QT interval prolongation;
severe renal and liver failure;
urinary retention;
stomach and duodenal ulcers;
seizure disorders;
glaucoma, as well as predisposition to it;
benign prostatic hypertrophy;
Reye's syndrome;
myasthenia gravis;
intraocular hypertension;
factors indicating the risk of stroke;
alcohol and opiate abuse;
period of pregnancy and lactation.

Directions for use and dosage

The tablets must be taken orally and washed down with water. The doctor selects the dose of the drug depending on the patient’s condition. Typically, a small dose is used at the initial stage of treatment, which is subsequently increased to the optimal therapeutic dose.

For manic states, schizophrenia and other psychoses, the initial dose of Truxal is from 50 to 100 mg per day. Gradually, the daily dose increases to 300 mg (in some cases - up to 1200 mg). For maintenance therapy, 100–200 mg of the drug per day is prescribed.

The daily dose is usually divided into 2-3 doses. Chlorprothixene has a pronounced sedative effect, so a smaller part of the daily dose should be taken during the day, and the larger part in the evening.

For abstinence from drug addiction and alcoholism, the daily dose is 500 mg (divided into 2-3 doses). Usually the duration of treatment is 7 days. After withdrawal symptoms disappear, the dose is gradually reduced. For maintenance therapy, 25–75 mg of the drug is prescribed.

Truxal can be used in the treatment of depression, especially those accompanied by tension and anxiety (in monotherapy, or as an addition to treatment with antidepressants). The drug at a dose of 75 mg per day can be prescribed for neuroses and psychosomatic disorders, which are accompanied by depressive disorders and anxiety. The maximum daily dose in such cases is 150 mg. The recommended dose is usually divided into 2-3 doses. Chlorprothixene does not cause drug dependence or addiction, so its long-term use is possible.

In the treatment of oligophrenia and epilepsy, which are combined with mental disorders, the recommended dose is 50 mg per day (in some cases it can increase to 75–100 mg). The daily dose is divided into 2-3 doses.

Chlorprothixene potentiates the action of analgesics, so Truxal can be used to treat patients with pain. In this case, the recommended dose is 75–300 mg (combined use with analgesics is allowed).

When treating elderly patients, the daily dose is 25–75 mg.

To correct behavioral disorders in children, Truxal is taken at a rate of 0.5–2 mg per 1 kg of body weight.

For patients with reduced renal and/or liver function, a lower dosage is recommended. During treatment, it is advisable to monitor the level of the drug in the blood serum.

Side effects

nervous system: very often – dizziness, drowsiness; often - headaches, dystonia; uncommon – akathisia, parkinsonism, tardive dyskinesia, seizures; very rarely - development of neuroleptic malignant syndrome;
cardiovascular system: often – palpitations, tachycardia; infrequently - hot flashes, hypotension; rarely - prolongation of the QT interval; very rarely - venous thromboembolism;
digestive system: very often – increased salivation, dry mouth; often – nausea, dyspepsia, constipation; infrequently – diarrhea, vomiting;
respiratory system: rarely - shortness of breath;
mental activity: often – decreased libido, nervousness, insomnia, agitation;
urinary system: infrequently – painful urination, urinary retention;
endocrine system: rarely – hyperprolactinemia;
reproductive system: uncommon – erectile dysfunction, ejaculation disorders; rarely - amenorrhea, galactorrhea, gynecomastia;
immune system: rarely – anaphylactic reactions, hypersensitivity;
musculoskeletal system: often – myalgia; infrequently – muscle rigidity;
metabolic disorders and eating disorders: often - weight gain, increased appetite; uncommon – weight loss, loss of appetite; rarely - impaired glucose tolerance, hyperglycemia;
hematopoietic organs: rarely - thrombocytopenia, leukopenia, agranulocytosis, neutropenia;
organs of vision: often - visual impairment, disturbance of accommodation; infrequently – movement of the eyeballs;
hepatobiliary and liver disorders: infrequently - changes in laboratory parameters of liver function; very rarely - development of jaundice;
skin: often – hyperhidrosis; uncommon – photosensitivity, itching, skin rash, dermatitis;
general: often – asthenia, fatigue.

Taking chlorprothixene (as well as using other antipsychotics) can also cause the following rare side effects:

prolongation of the QT interval;
ventricular tachycardia;
torsade de pointes (Torsade de Pointes);
ventricular arrhythmias;
ventricular fibrillation;
sudden death.

special instructions

The use of Truxal can lead to the development of NMS (neuroleptic malignant syndrome). In this case, the drug should be stopped immediately, symptomatic treatment and general supportive measures should be provided.

With long-term treatment with the drug, tardive dyskinesia may develop. In such cases, it is not recommended to use antiparkinsonian drugs to eliminate symptoms (the symptoms may worsen) - it is necessary to reduce the dose or, if possible, stop treatment with chlorprothixene.

When prescribing Truxal to patients with diabetes mellitus, insulin dosage adjustment may be required.

Taking chlorprothixene may cause false-positive results in immunological pregnancy tests using urine, as well as urine tests for bilirubin.

The drug can cause malignant arrhythmias, so it should be used with caution in the treatment of patients with a history of cardiovascular disease, as well as patients with a family history of long QT interval. An ECG is recommended before starting therapy. When the QT interval is over 450 ms (in men) and over 470 ms (in women), Truxal should not be prescribed.

During treatment, the doctor assesses the patient's condition and, if necessary, may prescribe an ECG examination. If a prolonged QT interval is detected, the dose of the drug should be reduced; if the QT interval is prolonged beyond 500 ms, the drug should be discontinued.

Taking antipsychotics can lead to the development of venous thromboembolism, therefore, before and during treatment with the drug, it is necessary to determine the risk factors for the development of this disease and take precautions.

Truxal is not intended for the treatment of behavioral disorders in elderly patients with dementia.

If you abruptly stop taking chlorprothixene, withdrawal reactions may occur (diarrhea, vomiting, nausea, anorexia, rhinorrhea, myalgia, paresthesia, sweating, insomnia, anxiety, nervousness, agitation, dizziness, tremor, additional sensations of cold and heat). As a rule, the described symptoms appear within 1–4 days after completion of treatment and decrease within 1–2 weeks.

During long-term therapy (especially when using large doses), patients' condition must be carefully monitored to decide whether to reduce the maintenance dosage.

During pregnancy, Truxal is prescribed only in cases where the possible risk to the child is less than the expected benefit to the mother.

Newborns whose mothers took antipsychotics during late pregnancy or childbirth may experience symptoms of intoxication (excessive excitability, tremors, lethargy) and a low Apgar score.

If clinically necessary, treatment with Truxal during lactation is allowed. In such cases, it is necessary to carefully monitor the condition of the newborn (especially in the first 4 weeks after birth).

When using, you should avoid operating moving machinery and vehicles.

Drug interactions

Due to a possible increase in the QT interval, simultaneous use of Truxal with drugs that significantly prolong the QT interval should be avoided:

some antipsychotics (thioridazine);
antiarrhythmic drugs of classes IA and III (amiodarone, dofetilide quinidine, sotalol);
some antihistamines (astemizole, terfenadine);
some quinolone antibiotics (moxifloxacin, gatifloxacin) and macrolide antibiotics (erythromycin);
cisapride;
lithium, etc.

Concomitant use of Truxal and drugs that cause electrolyte disturbances (thiazide-like and thiazide diuretics) increases the risk of prolongation of the QT interval and the development of life-threatening arrhythmias. A similar effect can be observed when interacting with agents that increase the concentration of chlorprothixene in the blood plasma.

The drug reduces the effect of the following medications:

antihypertensive drugs (guanethidine and similar agents);
levodopa;
adrenergic drugs.

Truxal increases the sedative effect of alcohol, and also enhances the effect of anticholinergics, barbiturates, and other CNS depressants.

Concomitant use of lithium and antipsychotics increases the risk of neurotoxicity.

Due to its antihistamine effect, chlorprothixene can eliminate or suppress the disulfiram-alcohol reaction.

The combined use of epinephrine and Truxal may cause blockade of the alpha-adrenergic effects of epinephrine and cause severe hypotension and tachycardia.

When the drug interacts with quinidine, an increased inhibitory effect on the heart may be observed.

Antipsychotics and tricyclic antidepressants can mutually inhibit each other's metabolism.

When Truxal is used simultaneously with piperazine and metoclopramide, the risk of developing extrapyramidal disorders increases.

Analogs

An analogue of Truxal is Chlorprothixene Zentiva.

Terms and conditions of storage

Store at a temperature of no more than 25 °C out of the reach of children.

Shelf life – 5 years.

Conditions for dispensing from pharmacies

Dispensed by prescription.

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Compound

Active substance: chlorprothixene hydrochloride 25 mg/50 mg. Excipients: corn starch, lactose monohydrate, copovidone, glycerol 85%, microcrystalline cellulose, croscarmellose sodium, talc, magnesium stearate.
Shell: Opadry OY-S-9478 brown (hypromellose, macrogol 400, black iron oxide (E 172), red iron oxide (E 172), titanium dioxide (E 171)).

Description

Film-coated tablets, 25 mg: round, biconvex, film-coated tablets, dark brown in color.
Film-coated tablets, 50 mg: oval, biconvex film-coated tablets, dark brown in color.

pharmachologic effect

Chlorprothixene is an antipsychotic agent of the thioxanthene group.
The antipsychotic effect of these drugs is associated with blockade of dopamine receptors, and also, possibly, blockade of 5-HT receptors (5-hydroxytryptamine, serotonin). In vivo, chlorprothixene has a high affinity for dopamine receptors Di and D2. Chlorprothixene also has a high affinity for 5-HT2 receptors and ci-adrenergic receptors, which is similar to high-dose phenothiazines, levomepromazine, chlorpromazine and thioridazine, as well as the atypical antipsychotic cpozapine. Chlorprothixene has been demonstrated to have an affinity for histamine (H-i) receptors similar to that of diphenhydramine. In addition, chlorprothixene has an affinity for cholinergic muscarinic receptors. The binding profile of chlorprothixene is very similar to that of clozapine, but chlorprothixene has approximately 10 times higher affinity for dopamine receptors.
In all studies with behavioral models for antipsychotic activity (blocking dopamine receptors), chlorprothixene demonstrated significant antipsychotic effects. A relationship between the two in vivo models, in vitro dopamine D2 receptor affinity, and the average daily oral antipsychotic dose has been demonstrated.
In clinical use, chlorprothixene is a high-dose, broad-spectrum sedative antipsychotic used to treat psychotic disorders other than depression.
Chlorprothixene reduces the severity or eliminates anxiety, obsessions, psychomotor agitation, restlessness, insomnia, as well as hallucinations, delusions and other psychotic symptoms.
The very low incidence of extrapyramidal effects (about 1%) and tardive dyskinesia (about 0.05%) (in 11,487 patients) suggests that chlorprothixene may be useful for the maintenance treatment of patients with psychotic disorders. Low doses of chlorprothixene have an antidepressant effect, which makes the drug useful for mental disorders characterized by anxiety, depression and restlessness. Also, during therapy with chlorprothixene, the severity of associated psychosomatic symptoms decreases.
Chlorprothixene does not cause addiction, dependence or tolerance. In addition, chlorprothixene potentiates the effect of analgesics - it has its own analgesic effect, as well as antipruritic and antiemetic properties.

Pharmacokinetics

Suction
Maximum plasma concentrations are achieved approximately 2 hours (0.5 to 6 hours) after oral administration. The average oral bioavailability of chlorprothixene is about 12% (range 5 to 32%).
Distribution
The apparent volume of distribution (Vd)(3) is about 15.5 l/kg. Plasma protein binding is more than 99%.
Chlorprothixene penetrates the placental barrier.
Metabolism
Chlorprothixene is predominantly metabolized by sulfoxidation and side chain N-demethylation. Ring hydroxylation and N-oxidation occur to a lesser extent. Chlorprothixene was detected in bile, indicating enterohepatic recirculation. Metabolites do not have antipsychotic activity.
Removal
The half-life (T14P) is approximately 15 hours. Average system clearance is approximately 1.2 l/min. O
Chlorprothixene is excreted by the kidneys and intestines
Excreted in small quantities into breast milk. The milk/blood plasma ratio in breastfeeding women varies from 1.2 to 2.6.
There were no differences in plasma concentrations or elimination rates between the control group and the alcoholic group, regardless of whether the latter were sober or under the influence of alcohol at the time of the study.
Elderly patients (over 65 years old)
Application experience is insufficient.
Liver dysfunction Experience is insufficient.
Renal dysfunction There is insufficient experience with this drug.

Indications for use

Psychotic disorders excluding depression.

Contraindications

Hypersensitivity to the active substance, other thioxanthenes or any of the excipients.
CNS depression regardless of cause (for example, intoxication with alcohol, barbiturates or opiates), vascular collapse, coma.
Chlorprothixene may cause QT prolongation. Prolonged QT interval prolongation may increase the risk of malignant arrhythmia. Therefore, chlorprothixene is contraindicated in patients with a history of clinically significant cardiovascular disease (for example, severe bradycardia (<50 ударов в минуту)), недавно перенесенным инфарктом миокарда, нелеченной сердечной недостаточностью, гипертрофией сердца, аритмиями, при которых назначают антиаритмические средства IA и III классов), а также пациентам с желудочковой аритмией или пируэтной желудочковой тахикардией (torsade de pointes).
Chlorprothixene is contraindicated in patients:
- with uncorrected hypokalemia,
- with uncorrected hypomagnesemia,
- with long QT interval syndrome,
- while taking medications that prolong the QT interval.

Pregnancy and lactation

During pregnancy, Truxal should be used; the benefit to the mother outweighs the potential risk to the fetus.
There are no data on the use of chlorprothixene in pregnant women.
Newborns whose mothers took antipsychotics during pregnancy or during childbirth may experience
intoxications such as lethargy, tremors and excessive excitability. In addition, these newborns have a low Apgar score.
Infants whose mothers took antipsychotics (including chlorprothixene) during the third trimester of pregnancy may show signs of side effects, including extrapyramidal symptoms and/or withdrawal symptoms, which may vary in severity and duration after birth. The following side effects have been reported: agitation, hypertension, hypotension, tremor, somnolence, respiratory depression and feeding difficulties. Thus, newborns should be closely monitored.
During breastfeeding treatment, Truxal can be used only if it is considered clinically necessary. In this case, it is recommended to monitor the condition of the newborn, especially in the first 4 weeks after birth.
Chlorprothixene is excreted in breast milk in such small concentrations that it cannot have a therapeutic effect on newborns.
The dose absorbed by the child is about 2% of the dose taken by the mother.
Animal studies do not indicate an increase in side effects in the fetus or any other negative effects on the reproductive process.

Directions for use and doses

Adults
Psychosis: 50-100 mg/day in divided doses. The dose may be increased to 600 mg/day.
Maintenance dose: 100-200 mg/day in divided doses.
Children and teenagers
Chlorprothixene is not recommended for use in children and adolescents under 18 years of age due to a lack of controlled studies.

Side effect

The most common side effects, which may occur in more than 10% of patients, are dry mouth, increased salivation, drowsiness and dizziness.
Most side effects depend on the dose of the drug used. The incidence of side effects and their severity are most pronounced at the beginning of treatment and decrease as therapy continues.
Especially at the beginning of treatment, movement disorders may be observed. In most cases, such side effects are eliminated by dose reduction and/or use of antiparkinsonian drugs. Prophylactic use of antiparkinsonian drugs is not recommended. Antiparkinsonian drugs do not help with tardive dyskinesia; on the contrary, they can intensify symptoms. It is recommended to reduce the dose or, if possible, discontinue treatment. For persistent akathisia, benzodiazepines or propranolol may help.
Information on the incidence of side effects is presented based on literature data and spontaneous reports.
The frequency is indicated as: very often (>1/10), often (>1/100 to<1/10), нечасто (от >1/1000 to<1/100), редко (>1/10000 to<1/1000), очень редко (<1/10000), либ®^ неизвестно (не может быть оценена на основг
From the heart: often - tachycardia, palpitations)
From the blood and lymphatic system: rarely - thrombocytopenia, neutropenia, leukopenia, agranulocytosis.
From the nervous system: very often - drowsiness, dizziness; often - dystonia, headache; uncommon - tardive dyskinesia, parkinsonism, seizures, akathisia; very rarely - neuroleptic malignant syndrome.
From the side of the organ of vision: often - disturbance of accommodation, visual impairment; infrequently - gaze convulsion.
From the respiratory system: rarely - shortness of breath.
From the gastrointestinal tract: very often - dry mouth, increased salivation; often - constipation, dyspepsia, nausea; infrequently - vomiting, diarrhea.
From the kidneys and urinary tract: infrequently - difficulty urinating, urinary retention.
From the skin and subcutaneous tissues: often - hyperhidrosis; uncommon - skin rash, itching, photosensitivity, dermatitis.
Disorders of the musculoskeletal system and connective tissue: often - myalgia; infrequently - muscle rigidity.
From the endocrine system: rarely - hyperprolactinemia.
Metabolism and nutrition: often - increased appetite, weight gain; infrequently - loss of appetite, weight loss; rarely - hyperglycemia, impaired glucose tolerance.
From the side of blood vessels: infrequently - hypotension, hot flashes; very rarely - venous thromboembolism.
General disorders and disorders at the injection site: often - asthenia, fatigue.
From the immune system: rarely - hypersensitivity, anaphylactic reactions.
From the liver and biliary tract: infrequently - changes in laboratory parameters of liver function; very rarely - jaundice.
From the genital organs and mammary gland: infrequently - ejaculation disorders, erectile dysfunction; rarely - gynecomastia, galactorrhea, amenorrhea.
Mental disorders: often - insomnia, nervousness
Effect on the course of pregnancy, postpartum period:

withdrawal syndrome in newborns. t (f g
When taking chlorprothixene, as with other antipsychotic drugs, the following rare side effects were observed: prolongation of the interval of ventricular arrhythmias - ventricular fibrillation, ventricular tachycardia, torsades de pointes and sudden death.
Abrupt discontinuation of chlorprothixene may lead to the development of withdrawal syndrome. The most common symptoms are nausea, vomiting, anorexia, diarrhea, rhinorrhea, sweating, myalgia, paresthesia, insomnia, nervousness, anxiety and agitation. Patients may also experience dizziness, disturbances in body temperature control, and tremors. Symptoms usually begin within 1-4 days after discontinuation and decrease within 1-2 weeks.

Overdose

Symptoms
Drowsiness, coma, convulsions, shock, extrapyramidal symptoms, hyperthermia or hypothermia. In severe cases, kidney failure is possible.
In case of overdose and simultaneous use with drugs that affect cardiac activity, the development of ECG changes, prolongation of the QT interval, in rare cases of cardiac arrest and ventricular arrhythmias have been reported.
Treatment
Symptomatic and supportive. Flush the stomach as quickly as possible; it is recommended to use activated charcoal. Measures must be taken to maintain the activity of the respiratory and cardiovascular systems. Adrenaline should not be used because this may lead to a subsequent decrease in blood pressure. Seizures can be treated with diazepam, and extrapyramidal disorders with biperiden.
Doses of 2.5-4 g can be fatal, in children - about 4 mg/kg. Adults survived after taking 10 g, and a three-year-old child survived after taking 1000 mg. .

Interaction with other drugs

Truxal can enhance the sedative effect of alcohol, the effects of barbiturates and other central nervous system depressants.
Antipsychotic drugs may enhance or decrease the effect of antihypertensive drugs. The antihypertensive effect of guanethidine and similarly active drugs is reduced.
Concomitant use of antipsychotics and lithium increases the risk of neurotoxicity. Tricyclic antidepressants and antipsychotics mutually inhibit each other's metabolism.
Chlorprothixene may reduce the effectiveness of levodopa and the effect of adrenergic drugs and enhance the effect of anticholinergic drugs. Concomitant use with metocpopramide and piperazine increases the risk of developing extrapyramidal disorders.
The antihistamine effect of chlorprothixene may inhibit the alcohol/disulfiram reaction.
Concomitant use with the following drugs for the treatment of QT interval is contraindicated: -
- antiarrhythmic drugs IA and UL
- some antipsychotic drugs (eg thioridazine),
- some macrolide antibiotics (for example, erythromia
- some quinolone antibiotics
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- some antihistamines (for example, terfenadine, astemizole).
This list is incomplete; simultaneous use of other drugs that can cause a significant prolongation of the OT interval (such as cisapride, lithium) is also contraindicated.
Concomitant use of drugs that cause electrolyte disturbances, such as thiazide diuretics, and that may increase plasma concentrations of chlorprothixene should be avoided due to a possible increased risk of QT prolongation and malignant arrhythmia.
Antipsychotics are metabolized by the liver cytochrome P450 system.
Medicines that inhibit cytochrome CYP 2D6 (for example, paroxetine, fluoxetine, chloramphenicol, disulfiram, isoniazid, MAO inhibitors, oral contraceptives, and to a lesser extent buspirone, sertraline or citalopram) may increase plasma concentrations of chlorprothixene.
The simultaneous use of chlorprothixene and drugs that have anticholinergic effects enhances this anticholinergic effect.

Precautionary measures

Neuroleptic malignant syndrome
When taking antipsychotics, cases of neuroleptic malignant syndrome with the following symptoms have been reported: hyperthermia, muscle rigidity, dysfunction of the autonomic nervous system, impaired consciousness and increased serum creatine kinase. The risk may be higher if you take a strong drug.
Among the fatal cases, the majority are patients with existing organic brain syndrome, mental retardation, and abusing opiates or alcohol.
Treatment: discontinuation of antipsychotic drugs, symptomatic and general supportive inpatient treatment. Symptoms may persist for up to a week after stopping oral antipsychotics.
Due to pupil dilation, patients with a shallow anterior chamber and angle-closure glaucoma may develop acute glaucoma.
Due to the risk of malignant arrhythmias, Truxal should be administered with caution to patients with a history of cardiovascular disease and to patients with a family history of long QT interval.
Before starting treatment, it is necessary to conduct an ECG study. When the QT interval is over 450 ms in men and 470 ms in women, chlorprothixene is contraindicated. During therapy, the need for an ECG is assessed individually by the doctor. If the QT interval prolongs during treatment, smaller doses of Truxal should be prescribed; if the QT interval prolongs beyond 500 ms, therapy should be discontinued.
During treatment, periodic assessment of electrolyte balance is recommended.
Concomitant use of other antipsychotics should be avoided.
Chlorprothixene should be used with caution in patients with organic brain syndrome, seizure disorders, severe hepatic or renal impairment, myasthenia gravis and benign prostatic hypertrophy.
Precautions should be taken in patients with:
- pheochromocytoma,
- neoplasia caused by prolactin,
- severe hypotension
- Parkinson's disease
- diseases of the hematopoietic system,
-hyperthyroidism,
- urination disorders, urinary retention, pyloric stenosis, intestinal obstruction.
Chlorprothixene may alter insulin concentrations
To decide on the possibility of reducing the maintenance dose during long-term therapy, especially with maximum daily doses, it is necessary to regularly monitor the patients' condition.
The development of venous thromboembolism has been reported while taking antipsychotic drugs. Due to the fact that patients treated with antipsychotic drugs are often at risk for developing venous thromboembolism, before and during treatment with chlorprothixene, it is necessary to determine risk factors for the development of venous thromboembolism and take preventive measures.
Use in children and adolescents under 18 years of age
Truxal is not recommended for use in children and adolescents. There is insufficient research data on the effectiveness and safety of chlorprothixene in children and adolescents. Therefore, chlorprothixene should be prescribed to children and adolescents (up to 18 years of age) only if there is an indication for use and after a careful assessment of the benefit-risk ratio.
Elderly patients:
Cerebrovascular adverse reactions
Chlorprothixene should be used with caution in patients at risk of stroke.
In randomized, placebo-controlled clinical trials of certain atypical antipsychotics in patients with dementia, a 3-fold increase in the risk of cerebrovascular adverse reactions was observed. The mechanism for this increased risk is unknown. An increased risk cannot be ruled out when using other antipsychotics in other groups of patients.
Elderly patients are particularly susceptible to orthostatic hypotension.
Increased mortality in older patients with dementia Data from two large observational studies showed that older patients with dementia taking antipsychotics had a small increased risk of death compared with patients not taking antipsychotics. There is no sufficient data to accurately assess the magnitude of the risk and the reasons for its increase.
Truxal is not registered for the treatment of behavioral disorders in elderly patients with dementia.
Excipients
The tablets contain lactose monohydrate. Patients with hereditary galactose intolerance, Lapp lactase deficiency, impaired absorption of glucose and galactose should not take the drug

Compound

Active ingredient: chlorprothixene;

1 tablet contains 25 mg or 50 mg of chlorprothixene hydrochloride

Excipients: corn starch lactose monohydrate, copolyvidone; glycerin (85%); microcrystalline cellulose sodium croscarmellose; talc magnesium stearate coating OPADRY OY-S-9478 brown.

Dosage form

Film-coated tablets.

Basic physicochemical properties: 25 mg tablets - round, biconvex film-coated tablets, dark brown; 50 mg tablets - oval, biconvex film-coated tablets, dark brown.

Pharmacological group

Psycholeptic drug. Thioxanthene derivatives.

Pharmacological properties

Pharmacological.

Chlorprothixene is an antipsychotic from the thioxanthene group.

The antipsychotic effect of antipsychotics is associated with blockade of dopamine receptors, but also with the probable involvement in this process of blockade of 5-HT (5-hydroxytryptamine) receptors.

Chlorprothixene has a high affinity for 5-HT 2 receptors and α 1 -adrenoceptors and in this respect is similar to high-dose phenothiazines, levomepromazine, chlorpromazine, thioridazine and the atypical antipsychotic clozapine. It has high histamine (H 1) affinity, which is equal to the affinity of diphenhydramine. Chlorprothixene demonstrates high affinity for cholinergic muscarinic receptors. The receptor binding profile is quite similar to that of clozapine, although chlorprothixene has almost 10 times greater affinity for dopamine receptors.

Chlorprothixene is a sedative neuroleptic with a wide range of indications.

Chlorprothixene reduces or eliminates anxiety, obsessions, psychomotor agitation, restlessness, nervousness and insomnia, as well as hallucinations, mania and other psychotic symptoms. In low doses it has an antidepressant effect, which makes it acceptable for the treatment of mental disorders accompanied by restlessness-anxiety-depression syndrome; psychosomatic disorders.

Chlorprothixene does not cause addiction, dependence or development of tolerance. Thus, chlorprothixene is effective in the treatment of both psychotic conditions and a wide range of other mental disorders. In addition, chlorprothixene enhances the effect of analgesics, has its own analgesic effect, antipruritic and antiemetic properties.

Pharmacokinetics.

When taking chlorprothixene, maximum plasma levels are observed at approximately 2:00 (range 0.5-6 hours). The average bioavailability after administration is 12% (range 5-32%). Plasma protein binding >99%. Chlorprothixene passes through the placental barrier.

The metabolism of chlorprothixene occurs mainly through sulfonic acidification and N-demethylation.

The half-life (T 1/2 β) is approximately 16 hours (range 4 to 33 hours). Systemic clearance (Cl s) - approximately 1.2 l/min. Excretion occurs in feces and urine.

Chlorprothixene passes into the milk of breastfeeding women in small quantities. The milk/blood plasma concentration ratio is 1.2-2.6.

There is no information on pharmacokinetic parameters in patients with reduced liver and kidney function and in elderly patients.

There were no differences between the concentrations of chlorprothixene in the blood plasma or the rate of elimination in patients in the control group and patients with alcoholism, regardless of the presence or absence of alcohol intoxication in the latter group.

Indications

Schizophrenia and other psychoses with psychomotor restlessness, anxiety and agitation.

Treatment of abstinence in alcoholics and drug addicts.

Depressive syndromes, neuroses, psychosomatic disorders accompanied by anxiety, tension, restlessness, insomnia, sleep disturbance.

Epilepsy and oligophrenia associated with mental disorders such as erethism, agitation, mood lability and behavioral disorders.

Chronic pain (addition to analgesics).

Geriatrics: hyperactivity, agitation, irritability, confusion, anxiety, behavioral and sleep disorders.

Contraindications

Hypersensitivity to the components of the drug or thioxanthene group agents.

Circulatory collapse, depression of the central nervous system of any origin (for example, alcohol, barbiturate or opioid intoxication), coma.

Chlorprothixene may cause QT prolongation. Persistent QT prolongation may increase the risk of malignant arrhythmias. Therefore, chlorprothixene is contraindicated in patients with a history of clinically significant cardiovascular disorders (eg, bradycardia<50 уд / мин, недавний острый инфаркт миокарда, декомпенсированная сердечная недостаточность, сердечная гипертрофия, аритмии, если предназначены антиаритмические средства классов IA и III) и пациентам с анамнезом желудочковых аритмий или Torsade de Pointes.

Chlorprothixene is contraindicated in patients with uncorrected hypokalemia and hypomagnesemia.

Chlorprothixene is contraindicated in patients with inherited long QT syndrome or known acquired long QT interval (QTc greater than 450 ms in men and 470 ms in women).

Concomitant use with drugs that significantly prolong the QT interval.

Interaction with other drugs and other types of interactions

Combinations that require caution when used.

Chlorprothixene may enhance the sedative effects of alcohol, barbiturates and central nervous system inhibitors.

Antipsychotics may increase or decrease the effect of antihypertensive drugs; the hypotensive effect of guanethidine and similar acting agents is weakened.

Concomitant use of antipsychotics and lithium increases the risk of neurotoxicity.

Tricyclic antidepressants and antipsychotics mutually suppress each other's metabolism.

Chlorprothixene may reduce the effectiveness of levodopa and adrenergic agents, and combination with metoclopramide and piperazine increases the risk of developing extrapyramidal symptoms.

The antihistamine effect of chlorprothixene may reduce or eliminate the alcohol/disulfiram reaction.

QT prolongation associated with antipsychotics may be exacerbated during coadministration with other drugs that can significantly prolong the QT interval. The combination of such drugs is contraindicated. Relevant classes include:

class IA and III antiarrhythmic drugs (for example, quinidine, amiodarone, sotalol, dofetilide)
some antipsychotics (eg, thioridazine)
some macrolides (eg, erythromycin)
some antihistamines (eg, terfenadine, astemizole)
some quinolones (eg, gatifloxacin, moxifloxacin).

The list above is incomplete; combination with other individual drugs that can significantly prolong the QT interval (for example, cisapride, lithium) should be avoided.

Drugs that alter electrolyte balance, such as thiazide diuretics (hypokalemia), and drugs that increase chlorprothixene concentrations should also be used with caution as they may increase the risk of QT prolongation and malignant arrhythmias.

Neuroleptic drugs are metabolized by the cytochrome P 450 system of the liver. Drugs that are inhibitors of the cytochrome CYP 2D6 system (for example, paroxetine, fluoxetine, chloramphenicol, disulfiram, isoniazid, MAO inhibitors, oral contraceptives, and to a lesser extent buspirone, sertraline or citalopram) may increase plasma levels of chlorprothixene.

The simultaneous use of chlorprothixene and drugs with anticholinergic activity enhances the anticholinergic effects.

Features of application

The likelihood of developing neuroleptic malignant syndrome (hyperthermia, muscle rigidity, impaired consciousness, dysfunction of the autonomic nervous system) exists with the use of any antipsychotic. The risk is potentially higher when using multiple products. Among the patients in whom deaths were observed, patients with existing organic syndrome, mental retardation, and abuse of opiates and alcohol predominated.

Treatment: discontinuation of antipsychotics, symptomatic and general supportive measures. Dantrolene and bromocriptine can be used.

Attacks of acute glaucoma due to pupil dilation can occur in patients with the rare condition of shallow anterior chamber depth and narrow chamber angle.

Chlorprothixene should be used with caution in patients with a history of cardiac disease or hereditary long QT syndrome due to the risk of malignant arrhythmias.

ECG monitoring is mandatory before starting treatment with chlorprothixene. Chlorprothixene is contraindicated if the QTc interval at the time of such examination is >450 ms in men or >470 ms in women. During treatment, the need for ECG monitoring is determined individually for the patient, the dose is reduced if QT increases, and therapy is stopped if QT c > 500 ms.

Concomitant use with other antipsychotics should be avoided.

Like other antipsychotics, chlorprothixene should be used with caution in patients with organic brain syndrome, seizures, or progressive diseases of the kidneys, liver, or cardiovascular system; in addition, in patients with severe myasthenia gravis, prostate hypertrophy.

Use with caution in patients with the following pathology:

pheochromocytoma;
prolactin deposits neoplasms
severe hypotension or orthostatic disturbances;
Parkinson's disease;
diseases of the hematopoietic system;
hyperthyroidism
urinary disorders, urinary retention, pyloric stenosis, intestinal obstruction.

Like other psychotropic drugs, chlorprothixene can change the body's sensitivity to insulin and glucose, which requires adjustment of antidiabetic therapy in patients with diabetes.

Patients undergoing long-term treatment, especially in high doses, should be subject to careful monitoring and periodic examination with a view to reducing the dosage.

Cases of venous thromboembolism (VTE) have been reported with the use of antipsychotics. Because acquired risk factors for VTE are often present in patients treated with antipsychotics, all possible risk factors for VTE should be identified and addressed before and during treatment with chlorprothixene.

An approximately threefold increase in the risk of cerebrovascular events was observed in randomized, placebo-controlled trials in dementia populations with some atypical antipsychotics. The mechanism for this increased risk is unknown. An increased risk cannot be excluded for other antipsychotics and other patient populations. Chlorprothixene should be used with caution in patients with risk factors for stroke.

Elderly patients are especially sensitive to postural hypotension.

Clinical studies have shown that older patients with dementia who are treated with antipsychotics have a slightly increased risk of death compared with those who are not treated with antipsychotics. There is insufficient data to assess the magnitude of the risk; the reason for the increased risk is unknown.

Chlorprothixene is not intended for the treatment of behavioral disorders associated with dementia.

Priapism has been reported with antipsychotics with α-adrenergic blocking effects, and it is possible that chlorprothixene may also share this ability. Severe priapism may require medical intervention. Patients should be informed of the need for emergency medical attention if signs and symptoms of priapism develop.

Excipients.

Use during pregnancy or breastfeeding.

Clinical experience with pregnant women is limited. Chlorprothixene should not be prescribed during pregnancy unless the expected benefit to the patient outweighs the possible risk to the fetus.

Infants whose mothers took antipsychotics (including Chlorprothixene) during the last trimester of pregnancy may be at risk of adverse effects, including extrapyramidal or withdrawal symptoms, which may vary in severity and duration after delivery. Cases of excitability, hypertension, hypotension, tremor, somnolence, respiratory distress, or difficulty feeding have been reported. So, newborns need careful care.

Data from preclinical studies are insufficient to assess reproductive toxicity.

Chlorprothixene is found in breast milk in low concentrations and is unlikely to affect the infant at therapeutic doses. The dose received by the infant through milk is approximately 2% of the maternal daily dose based on body weight. Breastfeeding may continue during treatment with chlorprothixene if clinically important, but monitoring the infant is recommended, especially in the first four weeks after birth.

Fertility.

Cases of hyperprolactinemia, galactorrhea, amenorrhea, lack of ejaculation and erectile dysfunction have been reported. These conditions can have a negative impact on female and/or male sexual function and fertility.

If clinically significant hyperprolactinemia, galactorrhea, amenorrhea, or sexual dysfunction occurs, dose reduction (if possible) or discontinuation should be considered. The effects after stopping the drug are reversible.

The potential effects on fertility have not been studied in animals.

The ability to influence the reaction rate when driving vehicles or other mechanisms.

Chlorprothixene is a sedative. Patients prescribed psychotropic medications may experience some reduction in overall alertness and concentration and should be warned that their treatment may affect their ability to drive or operate machines.

Directions for use and doses

Adults.

Doses should be set individually, according to the patient’s condition. In general, small doses should be prescribed initially and increased to the optimal effective level as quickly as possible based on therapeutic response.

Schizophrenia and other psychotic states, mania.

The initial dose is 50-100 mg/day with a gradual increase until the optimal effect is achieved. The usual optimal dose of 300 mg per day in some cases can reach 1200 mg / day as needed.

The maintenance dose is usually 100-200 mg/day.

Due to the sedative effect, the dose should be divided into several doses: with smaller doses in the afternoon and larger doses in the evening.

Treatment of abstinence in patients with alcoholism and drug addiction.

500 mg per day in divided doses for 7 days. After overcoming the abstinence period, the dose should be slowly reduced.

A maintenance dose of 25 + 25 + 50 mg (1 + 1 + 2 25 mg tablets) can stabilize the condition and reduce the risk of relapse. Over time, further dose reduction is possible.

Depressive syndromes, neuroses, psychosomatic disorders.

The minimum dose is 25 mg/day. The dose should be gradually increased to 75-100 mg/day, in severe cases - to 150 mg/day. Divide the daily dose into three doses, so apply 1/3 of the evening dose in the morning.

Sleep disturbance.

25 mg at 1:00 before bedtime.

Epilepsy and oligophrenia with mental disorders.

Apply to 100-125 mg/day. Patients with epilepsy need to maintain an adequate dose of anticonvulsants.

Chronic pain.

Can be used in combination with analgesics. Gradually increase the dose from 75-100 mg to 200-300 mg/day.

Geriatrics.

Individual dose selection in the range of 25-75 mg/day.

Impaired kidney and liver function.

Careful dosing and, if possible, determination of serum levels is advisable.

The tablets are swallowed with water.

Overdose

Symptoms: drowsiness, coma, shock, extrapyramidal symptoms, hyper- or hypothermia. In severe cases, kidney damage.

In case of simultaneous overdose with drugs that can affect cardiac activity, there have been cases of ECG changes, QT prolongation, Torsade de Pointes, cardiac arrest and ventricular arrhythmias.

Treatment: symptomatic and supportive therapy. After oral administration, gastric lavage should be performed as soon as possible; activated carbon can be prescribed. Measures should be taken to support the respiratory and cardiovascular systems. Epinephrine should not be used as a decrease in blood pressure may occur. Seizures can be treated with diazepam, and extrapyramidal symptoms with biperiden.

For adults, doses of 2.5-4 g can be lethal, for children - about 4 mg/kg body weight. Adults survived after 10 g, and a three-year-old child survived after taking 1000 mg.

Adverse reactions

Side effects are in most cases dose-dependent. Their frequency and severity are pronounced at the beginning of therapy and decrease with further treatment.

The development of extrapyramidal symptoms is possible, especially in the initial phase of therapy. In most cases, they are corrected by reducing dosages and/or antiparkinsonian drugs. Regular prophylactic use of the latter is not recommended. Dose reduction or, if possible, discontinuation of chlorprothixene therapy is recommended. In case of persistent akathisia, the use of a benzodiazepine or propranolol is recommended.

The frequency of adverse reactions shown in the table below is defined as:

very often (≥1/10), often (≥1/100 to<1/10), нечасто (≥1 / 1000 до <1/100), редкие (≥1 / 10000 до <1/1000) или очень редкие (<1/10000).

From the side of the heart	often	Tachycardia, increased heart rate.
From the side of the heart	rare	Prolongation of the QT interval on the ECG.
From the blood and lymphatic system	rare	Thrombocytopenia, neutropenia, leukopenia, agranulocytosis.
From the nervous system	Often	Drowsiness, dizziness.
	often	Dystonia, headaches.
	infrequently	Tardive dyskinesia, parkinsonism, seizures, akathisia.
	very rare	Neuroleptic malignant syndrome.
visual disturbances	often	Violation of accommodation, vision.
visual disturbances	infrequently	Eye movements.
From the respiratory system, chest and mediastinum	rare	Dyspnea.
From the gastrointestinal tract	Often	Dry mouth, hypersecretion of saliva.
	often	Constipation, dyspepsia, nausea.
	infrequently	Vomiting, diarrhea.
From the kidneys and urinary tract	infrequently	Urinary disorders, urinary retention.
Pregnancy, childbirth, perinatal period	Unknown	Withdrawal syndrome in newborns.
From the skin and subcutaneous tissue	often	Hyperhidrosis.
From the skin and subcutaneous tissue	infrequently	Rash, itching, photosensitivity, dermatitis.
Musculoskeletal disorders	often	Myalgia.
Musculoskeletal disorders	infrequently	Muscle rigidity.
From the endocrine system	rare	Hyperprolactinemia.
Metabolic disorders	often	Increased appetite, weight gain.
	infrequently	Decreased appetite, weight loss.
	rare	Hyperglycemia, impaired glucose tolerance.
From the side of blood vessels	infrequently	Arterial hypotension, hot flashes.
From the side of blood vessels	very rare	Venous thromboembolism.
General and administration site disorders	often	Asthenia, fatigue.
From the immune system	rarely	Hypersensitivity, anaphylactic reactions.
From the liver and biliary tract	infrequently	Abnormal liver tests.
From the liver and biliary tract	very rare	Jaundice.
From the reproductive system and mammary glands	infrequently	Lack of ejaculation, erectile dysfunction.
From the reproductive system and mammary glands	rare	Gynecomastia, galactorrhea, amenorrhea.
mental disorders	often	Insomnia, anxiety, nervousness, decreased libido.

There have been reports of rare cases of QT prolongation, ventricular arrhythmias - ventricular fibrillation, ventricular tachycardia, torsade de pointes and sudden death when using drugs belonging to the therapeutic class of antipsychotics, including chlorprothixene.

Sudden discontinuation of chlorprothixene may cause withdrawal symptoms, the most common of which are nausea, vomiting, anorexia, diarrhea, rhinorrhea, sweating, myalgia, paresthesia, insomnia, restlessness, anxiety and agitation. Patients may also experience dizziness, alternating sensations of heat or cold, and tremors. Symptoms usually begin within 1-4 days of stopping and decrease within 7-14 days.

50 mg tablets - 50 tablets per container; 1 container in a cardboard box.

active substance: chlorprothixene;

1 tablet contains 25 mg or 50 mg of chlorprothixene hydrochloride

Excipients: corn starch, lactose monohydrate, copolyvidone; glycerin (85%); microcrystalline cellulose sodium croscarmellose; talc magnesium stearate coating OPADRY OY-S-9478 brown.

Dosage form

Film-coated tablets.

Basic physical and chemical properties: 25 mg tablets - round, biconvex film-coated tablets, dark brown; 50 mg tablets - oval, biconvex film-coated tablets, dark brown.

Pharmacological group

Psycholeptic drug. Thioxanthene derivatives.

ATX code N05A F03.

Pharmacological properties

Pharmacodynamics.

Chlorprothixene is an antipsychotic from the thioxanthene group.

Chlorprothixene is a sedative neuroleptic with a wide range of indications.

In addition, chlorprothixene enhances the effect of analgesics, has its own analgesic effect, antipruritic and antiemetic properties.

Pharmacokinetics.

When taking chlorprothixene, maximum plasma levels are observed at approximately 2:00 (range 0.5-6 hours). Bioavailability after administration is 12% (range 5-32%). Plasma protein binding >99%. Chlorprothixene passes through the placental barrier.

The metabolism of chlorprothixene occurs mainly through sulfonic acidification and N-demethylation.

The half-life (T 1/2 β) is approximately 16 hours (range 4 to 33 hours). Systemic clearance (Cl s) - approximately 1.2 l/min. Excretion occurs in feces and urine.

Chlorprothixene passes into the milk of breastfeeding women in small quantities. The milk/blood plasma concentration ratio is 1.2-2.6.

There is no information on pharmacokinetics in patients with reduced liver and kidney function and in elderly patients.

Indications

Schizophrenia and other psychoses with psychomotor restlessness, anxiety and agitation.

Treatment of abstinence in alcoholics and drug addicts.

Depressive syndromes, neuroses, psychosomatic disorders accompanied by anxiety, tension, restlessness, insomnia, sleep disturbance.

Epilepsy and oligophrenia associated with mental disorders such as erethism, agitation, mood lability and behavioral disorders.

Chronic pain (addition to analgesics).

Geriatrics: hyperactivity, agitation, irritability, confusion, anxiety, behavioral and sleep disorders.

Contraindications

Hypersensitivity to the components of the drug or thioxanthene group agents.

Circulatory collapse, depression of the central nervous system of any origin (for example, alcohol, barbiturate or opioid intoxication), coma.

Chlorprothixene is contraindicated in patients with uncorrected hypokalemia and hypomagnesemia.

Chlorprothixene is contraindicated in patients with inherited long QT syndrome or known acquired long QT interval (QTc greater than 450 ms in men and 470 ms in women).

Concomitant use with drugs that significantly prolong the QT interval.

Interaction with other drugs and other types of interactions

Combinations that require caution when used.

Chlorprothixene may enhance the sedative effects of alcohol, barbiturates and central nervous system inhibitors.

Antipsychotics may increase or decrease the effect of antihypertensive drugs; the hypotensive effect of guanethidine and similar acting agents is weakened.

Concomitant use of antipsychotics and lithium increases the risk of neurotoxicity.

Tricyclic antidepressants and antipsychotics mutually suppress each other's metabolism.

Chlorprothixene may reduce the effectiveness of levodopa and adrenergic agents, and combination with metoclopramide and piperazine increases the risk of developing extrapyramidal symptoms.

The antihistamine effect of chlorprothixene may reduce or eliminate the alcohol/disulfiram reaction.

QT prolongation associated with antipsychotics may be exacerbated during coadministration with other drugs that can significantly prolong the QT interval.

The combination of such drugs is contraindicated. Relevant classes include:

class IA and III antiarrhythmic drugs (for example, quinidine, amiodarone, sotalol, dofetilide)
some antipsychotics (eg, thioridazine)
some macrolides (eg, erythromycin)
some antihistamines (eg, terfenadine, astemizole)
some quinolones (eg, gatifloxacin, moxifloxacin).

The list above is incomplete; combination with other individual drugs that can significantly prolong the QT interval (for example, cisapride, lithium) should be avoided.

The simultaneous use of chlorprothixene and drugs with anticholinergic activity enhances the anticholinergic effects.

Features of application

Treatment: discontinuation of antipsychotics, symptomatic and general supportive measures. Dantrolene and bromocriptine can be used.

Attacks of acute glaucoma due to pupil dilation can occur in patients with the rare condition of shallow anterior chamber depth and narrow chamber angle.

Chlorprothixene should be used with caution in patients with a history of cardiac disease or hereditary long QT syndrome due to the risk of malignant arrhythmias.

ECG monitoring is mandatory before starting treatment with chlorprothixene. Chlorprothixene is contraindicated if the QTc interval at such examination is >450 ms in men or >470 ms in women. During treatment, the need for ECG monitoring is determined individually for the patient, the dose is reduced if QT increases, and therapy is stopped if QT c > 500 ms.

Concomitant use with other antipsychotics should be avoided.

Use with caution in patients with the following pathology:

pheochromocytoma;
prolactin deposits neoplasms
severe hypotension or orthostatic disturbances;
Parkinson's disease
diseases of the hematopoietic system;
hyperthyroidism
urinary disorders, urinary retention, pyloric stenosis, intestinal obstruction.

Like other psychotropic drugs, chlorprothixene can change the body's sensitivity to insulin and glucose, which requires adjustment of antidiabetic therapy in patients with diabetes.

Patients undergoing long-term treatment, especially in high doses, should be subject to careful monitoring and periodic examination with a view to reducing the dosage.

Elderly patients are especially sensitive to postural hypotension.

Clinical studies have shown that older patients with dementia who are treated with antipsychotics have a slightly increased risk of death compared with those who are not treated with antipsychotics.

There is insufficient data to assess the magnitude of the risk; the reason for the increased risk is unknown.

Chlorprothixene is not intended for the treatment of behavioral disorders associated with dementia.

Priapism has been reported with antipsychotics with α-adrenergic blocking effects, and it is possible that chlorprothixene may share this ability. Severe priapism may require medical intervention. Patients should be informed of the need for emergency medical attention if signs and symptoms of priapism develop.

Excipients.

Use during pregnancy or breastfeeding.

Clinical experience with pregnant women is limited. Chlorprothixene should not be prescribed during pregnancy unless the expected benefit to the patient outweighs the possible risk to the fetus.

Data from preclinical studies are insufficient to assess reproductive toxicity.

Chlorprothixene appears in breast milk in low concentrations; its effect on the infant when using therapeutic doses is unlikely. The dose received by the infant through milk is approximately 2% of the maternal daily dose based on body weight. Breastfeeding may continue during treatment with chlorprothixene if clinically important, but monitoring the infant is recommended, especially in the first four weeks after birth.

Fertility.

If clinically significant hyperprolactinemia, galactorrhea, amenorrhea, or sexual dysfunction occurs, dose reduction (if possible) or discontinuation should be considered.

The effects after stopping the drug are reversible.

The potential effects on fertility have not been studied in animals.

The ability to influence the reaction rate when driving vehicles or other mechanisms.

Chlorprothixene is a sedative. Patients prescribed psychotropic medications may experience some decrease in overall alertness and concentration and should be warned that their treatment may affect their ability to drive or operate machinery.

Directions for use and doses

Adults .

Schizophrenia and other psychotic states, mania.

The initial dose is 50-100 mg/day with a gradual increase until the optimal effect is achieved. The usual optimal dose of 300 mg per day in some cases can reach 1200 mg / day as needed.

The maintenance dose is usually 100-200 mg/day.

Due to the sedative effect, the dose should be divided into several doses: with smaller doses during the day and larger doses in the evening.

Treatment of abstinence in patients with alcoholism and drug addiction.

500 mg per day in divided doses for 7 days. After overcoming the abstinence period, the dose should be slowly reduced.

A maintenance dose of 25 + 25 + 50 mg (1 + 1 + 2 25 mg tablets) can stabilize the condition and reduce the risk of relapse. Over time, further dose reduction is possible.

Depressive syndromes, neuroses, psychosomatic disorders.

Sleep disturbance.

25 mg at 1:00 before bedtime.

Epilepsy and oligophrenia with mental disorders.

Apply to 100-125 mg/day. Patients with epilepsy need to maintain an adequate dose of anticonvulsants.

Chronic pain.

Can be used in combination with analgesics. Gradually increase the dose from 75-100 mg to 200-300 mg/day.

Geriatrics.

Individual dose selection in the range of 25-75 mg/day.

Impaired kidney and liver function.

Careful dosing and, if possible, determination of serum levels is advisable.

The tablets are swallowed with water.

Overdose

Symptoms: drowsiness, coma, shock, extrapyramidal symptoms, hyper- or hypothermia. In severe cases, kidney damage.

In case of simultaneous overdose with drugs that can affect cardiac activity, there have been cases of ECG changes, QT prolongation, Torsade de Pointes, cardiac arrest and ventricular arrhythmias.

Treatment: symptomatic and supportive therapy. After oral administration, gastric lavage should be performed as soon as possible; activated carbon can be prescribed. Measures should be taken to support the respiratory and cardiovascular systems. Epinephrine should not be used as a decrease in blood pressure may occur. Seizures can be treated with diazepam, and extrapyramidal symptoms with biperiden.

For adults, doses of 2.5-4 g can be lethal, for children - approximately 4 mg/kg body weight. Adults survived after 10 g, and a three-year-old child survived after taking 1000 mg.

Adverse reactions

Side effects are in most cases dose-dependent. Their frequency and severity are pronounced at the beginning of therapy and decrease with further treatment.

The development of extrapyramidal symptoms is possible, especially in the initial phase of therapy. In most cases, they are corrected by dose reduction and/or antiparkinsonian drugs. Regular prophylactic use of the latter is not recommended. Dose reduction or, if possible, discontinuation of chlorprothixene therapy is recommended. In case of persistent akathisia, the use of a benzodiazepine or propranolol is recommended.

The frequency of adverse reactions shown in the table below is defined as:

very often (≥1/10), often (≥1/100 to<1/10), нечасто (≥1 / 1000 до <1/100), редкие (≥1 / 10000 до <1/1000) или очень редкие (<1/10000).

From the side of the heart		Tachycardia, increased heart rate.
From the side of the heart		Prolongation of the QT interval on the ECG.
From the blood and lymphatic system		Thrombocytopenia, neutropenia, leukopenia, agranulocytosis.
From the nervous system	Often	Drowsiness, dizziness.
		Dystonia, headaches.
		Tardive dyskinesia, parkinsonism, seizures, akathisia.
	very rare	Neuroleptic malignant syndrome.
visual disturbances		Violation of accommodation, vision.
visual disturbances		Eye movements.
From the respiratory system, chest and mediastinum
From the gastrointestinal tract	Often	Dry mouth, hypersecretion of saliva.
		Constipation, dyspepsia, nausea.
		Vomiting, diarrhea.
From the kidneys and urinary tract		Urinary disorders, urinary retention.
Pregnancy, childbirth, perinatal period	Unknown	Withdrawal syndrome in newborns.
From the skin and subcutaneous tissue		Hyperhidrosis.
From the skin and subcutaneous tissue		Rash, itching, photosensitivity, dermatitis.
Musculoskeletal disorders
Musculoskeletal disorders		Muscle rigidity.
From the endocrine system		Hyperprolactinemia.

Depending on the form of release, Truskal may contain varying amounts of both active and auxiliary compounds.

5 mg. chlorprothixene hydrochloride, and lactose monohydrate, croscarmellose sodium, magnesium stearate, talc, copovidone, corn starch, microcrystalline cellulose, and 85% contained in one tablet (diameter 6 mm), coated with a dark brown film shell, which includes a dye TM 1030, E171, 172 (Opadry OY-S-9478).

15 mg. chlorprothixene hydrochloride , and croscarmellose sodium, corn starch, talc, 85% glycerol, lactose monohydrate, magnesium stearate, copovidone And microcrystalline cellulose is contained in one tablet (diameter 7 mm), coated with a brown film shell, which contains Opadry OY-S-9478 dye.

25 mg. chlorprothixene hydrochloride , and Magnesium stearate, lactolose monohydrate, copovidone, 85% glycerol, croscarmellose sodium, microcrystalline cellulose and talc may be contained in one round and biconvex tablet, the film shell of which includes red and black iron oxide, titanium dioxide, macrogol and Opadry OY-S-9478 dye.

Release form

Truxal Available in tablet form. Tablets vary in size, as well as in the dosage of the active compound contained in one or another dosage form of the drug.

One cardboard package can contain blisters with 50 or 100 pieces of Truxal tablets containing 5, 15 or 25 mg in their chemical composition. chlorprothixene hydrochloride .

pharmachologic effect

This drug belongs to the group neuroleptic and antipsychotic medicines. Truxal affects the human body neuroleptic and at the same time antipsychotic pharmacological effects .

Pharmacodynamics and pharmacokinetics

Thanks to Truxal considered derivative thioxanthene , experts consider this drug to be effective antipsychotic drugs .Antipsychotic effects the drug has an effect because the active compounds contained in the drug affect dopamine receptors .

Truxal blocks these receptors (α1 - adrenergic receptors, 5-HT2 - receptors and H1 - histamine receptors), thereby showing their analgesic , and antiemetic properties. Since the drug is rapidly absorbed, the maximum concentration of medicinal compounds in the blood is achieved within two hours.

The medicine is excreted from the body through urine and feces. Truxal penetrates through placental barrier , i.e. the medicine is excreted through breast milk.

Indications for use

Truxal is taken for:

manic states;
hyperactivity;
withdrawal syndrome;
in old age ;
violation of child behavior;
psychosomatic disorders.

In addition, the drug is used in combination with analgesics for complex therapeutic treatment of pain.

Contraindications

Truxal is contraindicated for:

any forms depressed states of the central nervous system , for example, alcohol, toxic or drug intoxication;
comatose states ;
malfunctions hematopoietic systems ;
vascular collapse ;
pheochromocytoma ;
hypersensitivity .

In addition, the drug is prohibited from being taken during, and it is prohibited from being prescribed to women during .

Side effects

Truxal has the following side effects:

dry mouth;
disorientation.

The above side effects of the drug usually occur at the very beginning of the therapeutic course of treatment and disappear gradually over time. When taking the drug in increased dosages, there may be , hypotension , and also appear rashes on the skin.

Instructions for use of Truxal (Method and dosage)

In accordance with the instructions for Truxal treatment manic states, schizophrenia and others psychoses should start with a dosage not exceeding 100 mg. drug per day. The dose should be increased gradually, usually to a maximum of 300 mg. in a day.

Dosage 500 mg. Truxala three times a day for a week will help relieve withdrawal symptoms due to alcoholism or drug addiction.

Able confusion elderly patients are prescribed up to 90 mg. drug per day. At insomnia You can take up to 30 mg. Truxala approximately one hour before bedtime. Depressive states and others psychosomatic disorders Treat with daily dosages not exceeding 90 mg of the drug. For pain, up to 300 mg is prescribed. Truxala.

Overdose

If the dosage of Truxal is exceeded, the following symptoms may appear:

convulsions;
extrapyramidal syndromes;
hyperthermia;
shock;

In case of an overdose of Truxal, first of all, patients wash out the stomach and then providing support cardiovascular and respiratory systems We carry out symptomatic treatment.

Interaction

Since the depressant effect on CNS It is not recommended for a person to take Truxal together with ethanol-containing and sedative drugs , and analgesics, anesthetics, hypnotics and antipsychotic drugs.

Do not use drugs containing chlorprothixene simultaneously with antiparkinsonian, anticholinergic and antihistamine drugs. It is forbidden to use together with Truxal to avoid and hypotension .

Terms of sale

Prescription release.

Storage conditions

Truxal should be stored at 25°C out of the reach of children.

Best before date

Truxal tablets containing 5 mg. active medicinal components – 3 years;
tablets containing 15.25 and 50 mg. substances – 5 years.

special instructions

Truxal should be administered with caution to patients with epilepsy, at at diseases of the cardiovascular system , at , hypertrophy and dysfunction of the liver , and kidney .

When performing a pregnancy test, the drug may give a false positive result. In addition, the drug affects the indicators QT interval when conducting electrocardiogram research. It is prohibited to drink alcoholic beverages while taking the drug.

While using this medicine, you should avoid driving vehicles and performing work related to the maintenance of potentially dangerous mechanisms.

Truxal's analogs

Level 4 ATX code matches:

Analogs of Truxal include: