At different mental illness always carried out drug treatment. A number of drugs are well suited even for alcoholism and other mental disorders.

Chlorprothixene - description and properties

Chlorprothixene-Zentiva is a medicine in the form of tablets; its action is related to neuroleptics and antipsychotic drugs. It is implemented by strict recipe, which remains in the pharmacy after purchase. The dosage of the medicine is 0.05, 0.015 mg, the price for 30 tablets of 0.05 mg is 230 rubles. Chlorprothixene is produced in the Czech Republic by Sotex.

The main active ingredient in the composition is chlorprothixene hydrochloride.

How additional substances The composition contains sucrose, lactose, corn starch, calcium stearate, talc. The tablets are round in appearance, white at the break, and covered with a yellow or brownish film coating on top. The active substance is a derivative of thioxanthene and is classified as an antipsychotic. Its effects are:

• sedative;
• antiemetic;
• antidepressant;
• antipsychotic.

The drug also has hypnotic effect and works as an alpha-blocker. The antipsychotic effect is associated with blocking specific dopamine receptors in the brain. The antiemetic effect is due to a decrease in the activity of the trigger region in the medulla oblongata. The calming effect appears after inhibition of the reticular system in the brain stem. As a side effect, the drug suppresses the production of most brain hormones, only the amount of prolactin increases.

When taken orally, only 10-12% is absorbed active component, absorption occurs from small intestine. In blood maximum concentration detected 2 hours after administration. After 16 hours, 50% of the drug is excreted in feces and urine. It tends to accumulate in breast milk and also penetrates the placenta.

Indications and contraindications

The indications for use of the drug Chlorprothixene-Zentiva are varied and relate to various areas of medicine. Most often it is recommended for patients with the following indications:

The drug is often used in elderly people against the background of dyscirculatory encephalopathy associated with atherosclerosis cerebral vessels or other diseases. In old age, Chlorprothixene may be indicated for dementia.

The drug is often recommended after traumatic brain injuries in combination with other drugs.

The medicine is prescribed for alcohol abuse - delirium delirium; its use is also justified for insomnia, different types sleep disorders. Children are prescribed tablets to take for behavioral disorders, neurotic and psychosomatic disorders. There are other indications for taking pills:

The drug is also given as sedative before surgery, as a premedication. Contraindications include any acute conditions associated with depression of consciousness - coma, collapse, including due to drug overdose. Tablets are not prescribed for pheochromocytoma, blood diseases, or intolerance to components. During pregnancy and lactation it is given only for health reasons!

Side effects

Side effects can be quite serious, so the drug is administered in a course of therapy only as prescribed by a doctor. Taking may cause some disorders of the nervous system:

Treatment often leads to unpleasant phenomena in the gastrointestinal tract. These include stomach pain and cholestatic jaundice. A number of patients develop arrhythmia (tachycardia) and blood pressure drops. On the part of the eyes, clouding of the cornea and visual disturbances may appear. Abnormalities in the blood composition are possible in the form of leukopenia or leukocytosis, anemia.

Hormone-producing organs are able to respond to therapy with decreased potency, gynecomastia in men, amenorrhea, and galactorrhea.

Some patients develop a rash on the body, others allergic reactions. Sweating may also increase, appetite and body weight may increase. Dry mouth, constipation, and impaired urine output often appear.

Instructions for use

The drug can be taken over a long course; it does not cause addiction or dependence. In people with pain, it combines well with analgesics, enhancing their effect. In this case, the dosage is 15-300 mg/day depending on the severity pain syndrome. The daily dose is divided into 2-3 doses, and it is recommended to drink it in the evening most due to its hypnotic effect.

For insomnia, drink 15-30 mg of Chlorprothixene once an hour before bedtime, this helps normalize falling asleep and the quality of night's rest.

An antipsychotic from the group of thioxanthene derivatives, it mainly has a strong sedative and anxiolytic, as well as a weak anti-autistic effect. The drug is also an antihistamine and antiemetic (acts by inhibiting chemoreceptors in spinal cord). Its antipsychotic effects include blocking postsynaptic dopamine receptors in the brain, as well as blocking α-adrenergic receptors and inhibiting the release of most hypothalamic and pituitary hormones. Increases prolactin concentrations by blocking prolactostatin, a prolactin release inhibitory factor (PIF) from the pituitary gland. May cause minor extrapyramidal symptoms during prolonged use. The drug reduces body temperature. Rapidly absorbed from gastrointestinal tract, begins to act within 30 minutes after administration. Penetrates the blood-brain barrier. Binds to plasma proteins (more than 99%). Intensively metabolized in the liver, excreted in the form of metabolites in urine and feces. t1/2 is 8–12 hours. Penetrates the placental barrier and, in small quantities, into breast milk.

Chlorprothixene: instructions for use

Endogenous and organic psychoses with a pathological state motor activity and aggressiveness. Anxiety and insomnia in neurosis and psychosomatic disorders. Alcoholic psychoses. Premedication before surgery to reduce neurovegetative reactions and prevent postoperative vomiting.

Chlorprothixene: contraindications

Increased sensitivity to any of the components of the drug or to thioxanthenes, central nervous system depression (also as a result of alcohol poisoning or medicines), vascular collapse, impaired hematopoiesis, impaired morphology. Do not use in children under 6 years of age. Exercise extreme caution in patients suffering from alcoholism or abusing drugs that have an inhibitory effect on the central nervous system. nervous system(intensification of action), patients with delayed mental development, patients with epilepsy (increased incidence of seizures), patients with a tendency to faint, with Parkinson's disease (exacerbation of extrapyramidal symptoms), patients exposed to extreme temperatures, with serious impairment of liver, cardiovascular and respiratory system(for example, with pneumonia, asthma, emphysema), elderly patients, patients with closed-angle glaucoma, myasthenia gravis, diabetes mellitus, prostatic hyperplasia ( increased risk urinary retention), as well as during electroconvulsive therapy. When using the drug in children, there is an increased risk of hepatotoxicity with symptoms of Reye's syndrome. Chlorprothixene may cause false positive results V immunological test for pregnancy, in a urine test for the presence of bilirubin, and may also cause changes in the QT interval in the ECG. Cases of venous thromboembolism have occasionally occurred during treatment with antipsychotic drugs. Acquired risk factors for venous thromboembolism often occurred in patients receiving antipsychotic drugs. For this reason, before starting treatment and during the use of chlorprothixene, all possible factors risk of disease and take preventive measures. Studies have found an increased risk fatal outcome in elderly patients with dementia taking antipsychotic drugs compared with patients not using these drugs. Chlorprothixene is not recommended for the treatment of behavioral disorders associated with senile dementia.

Chlorprothixene: interactions with other drugs

During the concomitant use of hypnotics, antidepressants and anticonvulsants, analgesics, muscle relaxants, antipsychotics and antihistamines the older generation, as well as alcohol consumption during treatment, may exacerbate the mutually inhibitory effects on the central nervous system. The weak anticholinergic effect of chlorprothixene may be enhanced by concurrent use of anticholinergic, antihistamine and antiparkinsonian drugs. The drug may block the α-adrenergic action of epinephrine, which can cause hypotension and tachycardia. May reduce the effect of levodopa by blocking dopamine receptors. Because the drug lowers the seizure threshold, dosage adjustments of antiepileptic drugs may be necessary. With simultaneous use of phenothiazines, metoclopramide, or reserpine, there may be a risk of exacerbation of extrapyramidal symptoms. Chlorprothixene may increase serum prolactin levels; If bromocriptine is used concurrently, the dosage of this drug may need to be adjusted. Thioxanthenes may mask the ototoxic effects of other drugs.

Chlorprothixene: side effects

Risk of occurrence side effects increases with long-term use high doses. When using high doses at the beginning of treatment, the following most often occur: fatigue, orthostatic hypotension, drowsiness, apathy; these symptoms usually disappear later. Often occur: drowsiness, headache, dizziness, tachycardia (especially with a sudden increase in dose), orthostatic hypotension, constipation, fatigue, weight gain. Not very common: dystonia, akathisia, extrapyramidal symptoms, dry mouth. Sometimes the following may occur: hypersensitivity, apathy, increased anxiety, epileptiform seizures, impaired accommodation, nasal congestion, nausea, dermatitis, photosensitivity, itching, erythema, eczema, impaired thermoregulation. Very rare: hematopoietic disorder, hyperglycemia, neuroleptic malignant syndrome, tardive dyskinesia, retinitis pigmentosa, corneal deposits, cardiac arrest, bradycardia, asthma, laryngeal edema, cholestatic jaundice, lupus syndrome, excessive secretion uric acid in urine, disorder menstrual cycle, gynecomastia, galactorrhea, increased prolactin levels in the blood. After use antipsychotic drugs Cases of venous thromboembolism (including cases of pulmonary embolism and deep vein thrombosis) have occurred. Doses of 2.5–4 g for adults and 4 mg/kg body weight for children can be fatal. Symptoms of overdose: drowsiness, lethargy, respiratory depression, hypotension (may occur after a few hours and last for 2-3 days), tachycardia, elevated temperature, muscle rigidity or uncontrolled movements, miosis, and during regression of these symptoms, seizures, hyperactivity and hematuria may occur. Symptomatic and supportive therapy: gastric lavage with saline solution, use activated carbon, assisted ventilation and body temperature regulation. For hypotension, norepinephrine and metaraminol are administered parenterally. Do not use adrenaline due to the risk of paradoxical hypotension.

Pregnancy and lactation

Category C. The drug should be used during pregnancy only after careful consideration of the balance between the expected therapeutic benefits of treatment for the mother and the possible risk to the fetus. Use of the drug in the third trimester of pregnancy may cause extrapyramidal and/or withdrawal syndrome in newborns varying degrees severity and duration. Cases of hypertension, hypotension, tremor, drowsiness, respiratory distress syndrome or disorders associated with lactation. A small amount of the drug passes into breast milk. Do not use during lactation.

Chlorprothixene: dosage

Orally. Individually, depending on the indications and tolerance to the drug. Adults: neurosis: 15 mg 1–3 ×/day, psychotic disorders: 50–100 mg 2–4 ×/day; The daily dose should be divided so that most of the drug is taken in the evening before bed. Children: 1–2 mg/kg body weight/day.

Notes

The drug chlorprothixene causes drowsiness and may adversely affect activities that require increased attention, clear coordination and quick decision-making (including management vehicles, mechanical equipment maintenance, work on high altitude), especially at the beginning of treatment.

Drugs on the market containing chlorprothixene

Tablets Chlorprothixene 15 mg

Tablets Chlorprothixene 50 mg

Tablets Chlorprothixene Zentiva 15 mg

The sleeping pill Chlorprothixene is a fairly powerful antipsychotic. He has a very wide range impact. The product is characterized by a sedative effect, thanks to which you can calmly fall asleep.

Description

The sleeping pill Chlorprothixene is a medication characterized by neuroleptic, anticonvulsant, tranquilizing, and antipsychotic effects. It has the property of strengthening the effect of analgesic medications.

The drug begins to act 20 minutes after taking it. Active substances absorbed very quickly. Promptly absorbed in the intestines. The maximum concentration in the blood is observed after 2-3 hours. Half-life from the body is observed after 16 hours.

The antipsychotic drug eliminates irritability and nervousness, so you can sleep peacefully. The product should be taken half an hour before bedtime.

During treatment, patients should not potentially engage in dangerous species activities that require increased attention. It is also not recommended to drive vehicles during treatment.

Indications

Chlorprothixene is a sedative neuroleptic that has a wide spectrum of effects. The medication is indicated for:

• insomnia;
• behavioral disorders in patients of a younger age category;
• psychoses, which include schizophrenia;
• depressive states;
• sclerosis;
• brain injuries;
• somatic diseases;
• convulsive cough;
• spasms of the gastrointestinal tract;
• risk of miscarriage;
• postoperative conditions;
• preparation for anesthesia;
• pain.

Actively used in case of hangover due to alcoholism. Effectively combats irritability, agitation and confusion in older people.

Important! Only a doctor should prescribe the drug after examining the patient.

Contraindications

Despite the fact that the drug has high efficiency, it also has a number of contraindications. These include:

• comatose states;
• disease of the hematopoietic organs;
• depression of the central nervous system;
• vascular collapse;
• pheochromocytoma;
• hypersensitivity to individual substances in the composition.

The medication should be prescribed with extreme caution for epilepsy, parkinsonism, severe atherosclerosis cerebral vessels. It is also necessary to be careful when choosing this remedy for patients with a tendency to collapse, with impaired liver and liver function, diabetes mellitus, and prostate hypertrophy.

Side effects

Usually the drug is tolerated extremely well by patients. But when taking the drug, individual reactions of the body may occur. These include:

• the appearance of fatigue;
• psychomotor retardation;
• excessive worry;
• dizziness;
• tachycardia;
• amenorrhea;
• dry mouth;
• constipation;
• increased appetite;
• disturbance of carbohydrate metabolism;
• dysuria;
• photodermatitis;
• increased sweating.

The list of third-party reactions is quite long, so it is necessary to take the drug with extreme caution and only under the supervision of your doctor.

pros

Patients who took this drug, noted the following advantages of the drug:

• the manifestation of third-party reactions is not so common;
• especially effective in manic states.

Minuses

Patients using this drug managed to note and negative sides this remedy. These include:

• is highly addictive;
• questionable effectiveness in severe stages of mental disorders;
• possible manifestation of third-party reactions;
• individual hypersensitivity to individual components.

For children

The drug is in demand in pediatrics. Approved for use for behavior correction. Prescribed 0.5-2 mg per kg of body weight. Required dosage prescribed only by a doctor after examining the patient and according to the symptoms that appear.

But it should be noted that in children taking the medication there may be a risk of progression of hepatotoxicity with signs of Reye's syndrome.

During pregnancy and lactation

If possible, you should not use the drug if you are pregnant or breastfeeding. The drug should be prescribed only in severe situations and only by a doctor.

Elderly

The medication is prescribed to older people in case of irritability, confusion, and hyperactivity. The usual dosage is 15-90 mg per day. Daily dosage usually divided into 3 doses. During the treatment period elderly patient must be under the supervision of your attending physician.

Interaction with alcohol

It is not recommended to drink alcohol together with this medication. It has a depressing effect on the central nervous system, and alcohol only enhances the effect. When drinking alcohol together with medication, you may experience tachycardia, arterial hypotension, nausea and vomiting. The consequences of drinking alcohol during treatment are extremely dangerous. You shouldn't put yourself at risk.

Reviews

Yanina Zemlyakova, 28 years old

“I have been taking this remedy for over a year. I want to say right away that the medication is terribly addictive. Once I miss a pill, I can't sleep at all. But when I take this product, I sleep like a baby. The downside is the presence of third-party effects. Lately I have become a little lethargic and feel drowsy all the time.”

Grigory Metelkin, 34 years old

“This is a pretty good antipsychotic. It helps me a lot in eliminating all sleep disturbances. After taking it I fall asleep well and there are no night awakenings. The feeling of anxiety is gone. I was pleased with this drug. But I don’t recommend self-medicating or running to the pharmacy if you have insomnia. Firstly, the product is available with a doctor's prescription. Secondly, it has contraindications and side effects.”

Dmitry Donskoy, 48 years old

“I work as a security guard and very often I have to stay awake. Because of this, I had problems sleeping. My health deteriorated significantly and I began to feel unwell. I went to see a doctor who recommended this remedy to me. I was pleased. Personally, I did not have any third-party reactions. I tolerated taking this medication extremely well. I can’t say anything about others, since each organism is individual, but this remedy is the most effective among all that I have tried.”

Analogs

Analogues according to active substance speakers:

• Truxal;
• Chlorprothixene 15 Lechiva;
• Chlorprothixene 50 Treatment.

Analogues according to pharmacological group speakers:

• Azaleptin;
• Aminazine;
• Galoper;
• Hedonin;
• Droperidol;
• Kutipin;
• Rilept;
• Zeldox;
• Clozapine;
• Clopixol;
• Xeplion;
• Lakvel;
• Rezalen.

Only the attending physician can replace the drug. Each of the medications has its own number of contraindications and side effects. For this reason, self-medication can harm your health and aggravate the current situation. The doctor will be able to select another drug and prescribe the right dosage and frequency of administration.

Prices

The price of the drug varies and depends on the form of its release. The cost is:

• tablets 15 mg, 30 pcs. – from 135 rubles;
• tablets 50 mg, 30 pcs. – from 220 rubles;
• injection solution - from 140 rubles.

Availability in pharmacies

The medicine is sold in pharmacies only with a prescription from a doctor.

Chlorprothixene is an effective hypnotic, but has a number of side effects. This drug should be taken with caution. But nevertheless, the medicine is approved for use by children and the elderly. It is equally important to follow the prescribed dosage and frequency of taking this drug.

Catad_pgroup Antipsychotics (neuroleptics)

Chlorprothixene - official instructions by application

Registration number:

LP-004840 - 110518

Trade name of the drug

Chlorprothixene

International nonproprietary or generic name

Chlorprothixene

Dosage form:

Film-coated tablets.

Compound

One film-coated tablet, 15 mg, contains:

Active substance:

Chlorprothixene hydrochloride - 15,000 mg

Excipients:

Corn starch - 10,000 mg
Lactose monohydrate - 92,000 mg
Sucrose - 10,000 mg
Calcium stearate -1,500 mg
Talc - 1,500 mg

Film casing:

Opadry 32F250007 red - 5,000 mg

One film-coated tablet, 50 mg, contains:

Active substance:

Chlorprothixene hydrochloride - 50,000 mg

Excipients:

Corn starch - 37,500 mg
Lactose monohydrate - 135,000 mg
Sucrose - 20,000 mg
Calcium stearate - 3,750 mg
Talc - 3,750 mg

Film casing:

Opadry 32F220033 yellow - 7,500 mg

Description

15 mg tablets:

Biconvex, orange film-coated tablets.

50 mg tablets:

Biconvex film-coated tablets from light brown to light yellow.

Pharmacotherapeutic group

Antipsychotic (neuroleptic).

ATX code: N05AF03.

Pharmacological properties

Chlorprothixene is an antipsychotic drug derived from thioxanthene. It has antipsychotic, pronounced sedative and moderate antidepressant effects.

Pharmacodynamics

The antipsychotic effect of neuroleptics is associated with blockade of dopamine receptors, and also, possibly, blockade of 5-HT (5-hydroxytryptamine) receptors. In vivo, chlorprothixene has a high affinity for dopamine receptors type D1 and D2. Chlorprothixene also has high affinity for 5-HT2 receptors, α1-adrenergic receptors, histamine (H1) and cholinergic muscarinic receptors. The receptor binding profile of chlorprothixene is very similar to that of clozapine, but it has approximately 10 times higher affinity for dopamine receptors.

Chlorprothixene reduces the severity or eliminates anxiety, obsessions, psychomotor agitation, restlessness, insomnia, as well as hallucinations, delusions and other psychotic symptoms. Very low frequency the development of extrapyramidal effects (about 1%) and tardive dyskinesia (about 0.05%) indicate that chlorprothixene can be successfully used for maintenance treatment of patients with psychotic disorders.

Low doses of chlorprothixene have an antidepressant effect, which makes useful application drug for mental disorders characterized by anxiety, depression and restlessness. Also, during therapy with chlorprothixene, the severity of associated psychosomatic symptoms. Chlorprothixene does not cause addiction, dependence or tolerance. In addition, chlorprothixene potentiates the effect of analgesics, has its own analgesic effect, as well as antipruritic and antiemetic effects.

Pharmacokinetics

Suction

When administered orally, maximum plasma concentrations are achieved in approximately 2 hours (range 0.5-6 hours). The average oral bioavailability of chlorprothixene is approximately 12% (range 5-32%).

Distribution

The apparent volume of distribution (Vd)p is approximately 15.5 l/kg. Binding to plasma proteins is more than 99%. Chlorprothixene penetrates the placental barrier.

Biotransformation

The metabolism of chlorprothixene occurs primarily through sulfoxidation and N-demethylation of the side chain. Ring hydroxylation and N-oxidation are less pronounced. Chlorprothixene is determined in bile, which indicates the presence of enterohepatic circulation of the drug. Metabolites of chlorprothixene lack neuroleptic activity.

Removal

The half-life is approximately 16 hours (range 4-33 hours). The average systemic clearance (Cls) corresponds to approximately 1.2 l/min. Chlorprothixene is excreted in feces and urine.

In women who are breastfeeding, chlorprothixene is excreted in milk in small quantities. The ratio of drug concentration in mother's milk and in blood plasma 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 acutely intoxicated at the time of the study.

Indications for use

• Schizophrenia and other psychoses occurring with psychomotor agitation, agitation and anxiety.
• Withdrawal syndrome for alcoholism and drug addiction.
• Depressive states, neuroses, psychosomatic disorders with anxiety, tension, restlessness, insomnia, sleep disorders.
• Epilepsy and oligophrenia, combined with mental disorders: agitation, agitation, mood lability and behavioral disturbances.
• Pain (in combination with analgesics).
• Geriatrics: hyperactivity, agitation, irritability, confusion, anxiety, behavioral and sleep disorders.

Contraindications

• Hypersensitivity to chlorprothixene or any of the excipients.
• Hypersensitivity to drugs of the thioxanthene group.
• Vascular collapse, depression of consciousness of any origin (including those caused by the intake of alcohol, barbiturates or opiates), coma.
• Known uncorrectable hypokalemia or hypomagnesemia.
• Patient history of clinically significant cardiovascular diseases(eg, bradycardia (heart rate less than 50 beats per minute), recently suffered a heart attack myocardium, decompensated heart failure, cardiac hypertrophy, arrhythmias, for which class IA and III antiarrhythmics are prescribed), ventricular arrhythmias or polymorphic ventricular tachycardia pirouette type (lorsade de Pointes).
• Congenital long QT syndrome or acquired long QT interval (QTC over 450 ms in men and 470 ms in women).
• Simultaneous use with drugs that significantly prolong the QT interval.
• Lactose or fructose intolerance, lactase deficiency, glucose-galactose malabsorption, sucrase/isomaltase deficiency (due to the presence of lactose and sucrose in the composition).

Carefully

Organic diseases of the brain; mental retardation; a family history of relatives suffering from cardiovascular diseases, as well as cases of prolongation of the QT interval; seizure disorders; severe liver and renal failure; rare pathological condition in the form of a shallow anterior chamber of the eye and its narrow angle (the development of attacks of acute glaucoma associated with pupil dilation is possible); myasthenia gravis; benign prostatic hypertrophy; pheochromocytoma; prolactin-dependent neoplasms; heavy arterial hypotension or orthostatic disorders; Parkinson's disease; diseases of the hematopoietic system; hyperthyroidism; painful urination, urinary retention; pyloric stenosis; intestinal obstruction; presence of risk factors for stroke; diabetes; abuse of opiates and alcohol; pregnancy, period breastfeeding; children's and adolescence under 18 years of age (due to lack of strictly controlled studies).

Use during pregnancy and breastfeeding

Pregnancy

Clinical experience in pregnant women is limited. Chlorprothixene should not be prescribed during pregnancy unless the expected benefit to the patient exceeds possible risk for the fetus. Newborns exposed antipsychotics(including chlorprothixene) during the third trimester of pregnancy are at risk of developing adverse reactions, including extrapyramidal symptoms and/or withdrawal symptoms, which may vary in severity and duration after delivery. Cases of agitation, increased and decreased tone, tremors, drowsiness, respiratory distress, and eating disorders have been recorded. Therefore, newborns should be closely monitored.

Breast-feeding

Taking into account the fact that chlorprothixene is present in human milk in small concentrations, it is unlikely to have any effect negative impact per child if the drug is prescribed to the mother in therapeutic doses. The dose administered orally to the child is approximately 2% of the daily maternal dose, adjusted for body weight. During treatment with Chlorprothixene, breastfeeding is allowed if deemed clinically necessary. However, it is recommended to monitor the condition of the newborn, especially in the first 4 weeks after birth.

Fertility

Adverse events such as hyperprolactinemia, galactorrhea, amenorrhea, ejaculation disorders, and erectile disfunction(see section " Side effect"). These adverse reactions may have bad influence on sexual function and fertility of women and/or men.

If clinically significant hyperprolactinemia, galactorrhea, amenorrhea or manifestations of sexual dysfunction occur, dosage reduction (if possible) or discontinuation of the drug should be considered. These side effects are reversible after discontinuation of the drug.

Potential Impact medicine fertility has not been studied in animals.

Directions for use and doses

The tablets are swallowed whole with water.

The dosage is selected individually depending on the patient's condition. As a rule, at the beginning of treatment they are prescribed small doses, which increase to the optimal effective level as quickly as possible depending on the therapeutic response.

Schizophrenia and other psychoses. Manic states

Treatment begins with 50-100 mg/day, gradually increasing the dose to

achieving optimal effect, usually up to 300 mg/day. In some cases, the dose may be increased to 1200 mg/day. The maintenance dose is usually 100-200 mg/day.

The daily dose of chlorprothixene is usually divided into 2-3 doses, taking into account sedative effect chlorprothixene, it is recommended to prescribe a smaller part of the daily dose in daytime, and most of it in the evening.

Withdrawal syndrome in alcoholism and drug addiction

Daily dose, divided into 2-3 doses, is 500 mg over a period of up to 7 days. After symptoms of withdrawal disappear, the dose is gradually reduced. A maintenance dose of 30-75 mg/day allows you to stabilize the condition, reduces the risk of developing another binge, a further dose reduction may be required.

Depressive states, neuroses, psychosomatic disorders

Chlorprothixene can be used for depression, especially when combined with anxiety, tension, as an addition to antidepressant therapy or independently. Chlorprothixene can be prescribed for neuroses and psychosomatic disorders accompanied by anxiety and depressive disorders at a dose of up to 75 mg/day. The daily dose is usually divided into 2-3 doses. Since taking chlorprothixene does not cause addiction or drug dependence, it can be used for a long time. Maximum dose is 150 mg/day.

Epilepsy and mental retardation combined with mental disorders

The daily dose is 50 mg and is usually divided into 2-3 doses. The daily dose can be increased to 75-100 mg/day. For epilepsy, adequate anticonvulsant dosage should be maintained.

Elderly patients

In elderly patients, the dosage is selected individually; the dose range is 15-75 mg/day.

Insomnia

15-30 mg 1 hour before bedtime once.

Pain

The ability of chlorprothixene to potentiate the action of analgesics can be used in the treatment of patients with pain. In these cases, chlorprothixene is prescribed in doses of 75 to 300 mg per day; it can be used in conjunction with analgesics.

Children and teenagers (up to 18 years old)

Renal dysfunction

In patients with impaired renal function, the dosage should be selected with caution, and serum levels of the drug should be monitored whenever possible.

Liver dysfunction

In patients with impaired liver function, the dosage should be selected with caution, and serum levels of the drug should be monitored whenever possible.

Side effect

The most common adverse reactions, 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.

Information on the incidence of side effects is presented based on literature data and spontaneous reports.

Frequency adverse reactions, given below was determined according to the classification of the World Health Organization: very often (≥ 1/10), often (from ≥1/100 to<1/10), нечасто (от ≥1/1000 до <1/100), редко (от ≥1/10000 до <1/1000), очень редко (<1/10000), либо неизвестно (не может быть оценена на основании существующих данных).

Blood and lymphatic system disorders:

rarely - thrombocytopenia, neutropenia, leukopenia, agranulocytosis.

Immune system disorders:

rarely - hypersensitivity, anaphylactic reactions.

Endocrine system disorders:

rarely - hyperprolactinemia.

Metabolic and nutritional disorders:

often - increased appetite, weight gain; infrequently - loss of appetite, weight loss; rarely - hyperglycemia, impaired glucose tolerance.

Mental disorders:

often - insomnia, nervousness, agitation, decreased libido.

Nervous system disorders:

very often - drowsiness, dizziness; often - dystonia, headache; uncommon - tardive dyskinesia, parkinsonism, seizures, akathisia; very rarely neuroleptic malignant syndrome.

Visual disorders:

often - disturbance of accommodation, visual impairment; infrequently - involuntary movements of the eyeballs.

Cardiac disorders:

often - tachycardia, palpitations; rarely - prolongation of the QT interval on the electrocardiogram.

Vascular disorders:

infrequently - arterial hypotension, flushing of the face with a feeling of heat; very rarely - venous thromboembolism.

Disorders of the respiratory system, chest and mediastinal organs:

rarely - shortness of breath.

Gastrointestinal disorders:

very often - dry mouth, increased salivation; often - constipation, dyspepsia, nausea; infrequently - vomiting, diarrhea.

Disorders of the liver and biliary tract:

infrequently - changes in laboratory parameters of liver function; very rarely - jaundice.

Disorders of the skin and subcutaneous tissues:

often - increased sweating; uncommon - skin rash, itching, photosensitivity, dermatitis.

Musculoskeletal and connective tissue disorders:

often - myalgia; infrequently - muscle rigidity.

Renal and urinary tract disorders:

infrequently - urinary retention, painful urination.

Pregnancy, postpartum and perinatal conditions:

unknown - neonatal withdrawal syndrome.

Disorders of the genital organs and breast:

uncommon - ejaculation disorders, erectile dysfunction; rarely - gynecomastia, galactorrhea, amenorrhea.

General disorders and disorders at the injection site:

often - asthenia, fatigue.

Extrapyramidal disturbances may occur, especially in the early stages of treatment. In most cases, these side effects are successfully controlled by dose reduction and/or use of antiparkinsonian drugs. However, routine use of antiparkinsonian drugs to prevent side effects is not recommended. They do not improve the symptoms of tardive dyskinesia and may worsen them. It is recommended to reduce the dose or, if possible, discontinue treatment with chlorprothixene.

For persistent akathisia, benzodiazepines or propranolol may be helpful.

When taking chlorprothixene, as with other antipsychotics, the following rare side effects have also been reported: prolongation of the QT interval, ventricular arrhythmias - ventricular fibrillation, ventricular tachycardia, sudden death and polymorphic ventricular tachycardia of the "pirouette" type (Torsade de Pointes).

During the use of antipsychotic drugs, cases of priapism have been recorded - prolonged erection, usually painful, which can lead to erectile dysfunction. The frequency of this phenomenon is unknown (see section "Special instructions").

Abrupt cessation of chlorprothixene may be accompanied by withdrawal reactions. The most common symptoms are nausea, vomiting, anorexia, diarrhea, rhinorrhea, sweating, myalgia, paresthesia, insomnia, nervousness, anxiety and agitation. Patients may also experience dizziness, extra sensations of hot and cold, and tremors. Symptoms typically begin within 1-4 days of discontinuation and decrease within 7-14 days.

Overdose

Symptoms

Drowsiness, coma, convulsions, shock, extrapyramidal symptoms, hyperthermia/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, polymorphic ventricular tachycardia of the “pirouette” type (Torsade de Pointes), cases of cardiac arrest and ventricular arrhythmia have been reported.

Treatment

Symptomatic and supportive. Gastric lavage should be carried out as quickly as possible, and the use of activated carbon is recommended. Measures should be taken to maintain the functioning of the respiratory and cardiovascular systems. Epinephrine should not be used as this may lead to a subsequent decrease in blood pressure. Seizures can be treated with diazepam, and extrapyramidal disorders with biperiden.

A dose of 2.5 g - 4 g can be fatal, in children about 4 mg/kg. Adults survived after taking 10 g, and a three-year-old child after taking 1000 mg.

Interaction with other drugs

Chlorprothixene may enhance the sedative effect of alcohol, the effect of barbiturates and other CNS depressants.

Chlorprothixene should not be prescribed together with guanethidine and similarly active drugs, since antipsychotics can enhance or weaken the effect of antihypertensive drugs; the antihypertensive effect of guanethidine and similarly active drugs is reduced.

Concomitant use of antipsychotics and lithium drugs 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.

The simultaneous use of Chlorprothixene and drugs with established anticholinergic effects enhances their anticholinergic effects.

Concomitant use with metoclopramide and piperazine increases the risk of developing extrapyramidal disorders.

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

The increase in the QT interval on the electrocardiogram, characteristic of therapy with antipsychotic drugs, can be enhanced by concomitant use of drugs that significantly prolong the QT interval:

antiarrhythmic drugs of classes IA and III (quinidine, amiodarone, sotalol, dofetilide), some antipsychotics (thioridazine), some macrolide antibiotics (erythromycin) and quinolone antibiotics (gatifloxacin, moxifloxacin), some antihistamines (terfenadine, astemizole), as well as cisapride, lithium and other drugs; significantly increasing the QT interval. The simultaneous use of Chlorprothixene and the above drugs should be avoided. Chlorprothixene should be used with caution concurrently with drugs that cause electrolyte disturbances (thiazide and thiazide-like diuretics) and drugs that can increase plasma concentrations of chlorprothixene due to a possible increased risk of QT prolongation and life-threatening arrhythmias.

Neuroleptics are metabolized by hepatic isoenzymes of the cytochrome P450 system. Drugs that inhibit the 2D6 isoenzyme (eg, paroxetine, fluoxetine, chloramphenicol, disulfiram, isoniazid, monoamine oxidase inhibitors, oral contraceptives, and, to a lesser extent, buspirone, sertraline and citalopram) may increase plasma levels of chlorprothixene.

special instructions

When using any antipsychotic, there is a risk of developing neuroleptic malignant syndrome (hyperthermia, muscle rigidity, fluctuation of consciousness, instability of the autonomic nervous system). Patients with existing psychoorganic syndrome, mental retardation, as well as those who abuse opiates and alcohol make up a significant proportion of deaths. Treatment: discontinuation of the antipsychotic. Symptomatic therapy and general supportive treatment measures. Dantrolene and bromocriptine may be effective. After taking antipsychotics by mouth, symptoms may persist for more than one week.

In patients with such rare conditions as a small anterior chamber of the eye and a narrow angle, acute attacks of glaucoma associated with pupil dilation are possible.

Due to the risk of developing malignant arrhythmias, chlorprothixene should be used with caution in patients with a history of cardiovascular disease and in patients with a family history of long QT interval.

ECG monitoring is necessary before starting treatment.

Chlorprothixene is contraindicated if the QTC interval at baseline is more than 450 ms in men and 470 ms in women (see section "Contraindications").

During therapy, the need for ECG monitoring should be assessed by the physician, taking into account the individual characteristics of the patient. During treatment, reduce the dosage if the QT interval is prolonged or discontinue therapy if the QTC is > 500 ms.

The simultaneous use of other antipsychotic drugs should be avoided (see section "Interaction with other drugs").

Like other antipsychotics, chlorprothixene should be used with caution in patients with psychoorganic syndrome, seizures, liver, kidney and cardiovascular diseases in the later stages, as well as patients with myasthenia gravis and benign prostatic hyperplasia.

Caution must be exercised when using the drug in patients with

• pheochromocytoma,
• prolactin-dependent tumors,
• severe arterial hypotension or orthostatic regulation
• Parkinson's disease,
• diseases of the hematopoietic system,
• hyperthyroidism,
• urinary disorders, urinary retention,
• pyloric stenosis (pyloric stenosis), intestinal obstruction.

Like other psychotropic drugs, chlorprothixene may change the concentration of insulin and glucose in the blood, so patients with diabetes may require dosage adjustments of antidiabetic drugs.

Patients undergoing long-term treatment, especially with high doses, are subject to careful monitoring over time with periodic assessment of the need to reduce the maintenance dose. Cases of venous thromboembolism (VTE) have been reported while taking antipsychotic drugs. Due to the fact that patients treated with antipsychotic drugs are often at risk for developing VTE, risk factors for VTE should be identified before and during treatment with chlorprothixene and precautions taken.

It has been reported that antipsychotics with α-adrenergic blocking effects may cause priapism; it is possible that chlorprothixene also has this property. If severe priapism occurs, medical intervention may be required. Patients should be warned about the need to urgently seek medical help if objective and subjective signs of priapism appear.

Use of the drug in children and adolescents under 18 years of age

A sufficient number of studies have not been conducted to study the effectiveness and safety of the use of chlorprothixene for the treatment of children and adolescents.

Elderly patients

Cerebrovascular adverse reactions

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. Chlorprothixene should be used with caution in patients at risk of stroke. Elderly individuals are particularly at risk of developing orthostatic hypotension.

Increased mortality in older patients with dementia

Data from two large observational studies showed that older patients with dementia taking antipsychotic drugs had a nonsignificant increased risk of death compared with patients not taking antipsychotic drugs. There is no sufficient data to accurately assess the magnitude of the risk and the reasons for its increase. Chlorprothixene is not registered for the treatment of behavioral disorders in elderly patients with dementia.

Excipients

Impact on the ability to drive vehicles and operate machinery

Chlorprothixene is a drug that has a sedative effect. Patients receiving psychotropic drugs may experience some impairment of general attention and concentration, so they should be warned about the need to be careful when driving vehicles and operating machinery.

Release form

Film-coated tablets, 15 mg, 50 mg.

10 tablets in a blister pack made of polyvinyl chloride film and printed varnished aluminum foil.

1, 3 or 5 blister packs along with instructions for use are placed in a cardboard pack.

30 or 60 tablets in a polymer jar with first opening control and a polymer lid.

1 polymer jar together with instructions for use are placed in a cardboard pack.

Best before date:

Do not use the drug after the expiration date.

Storage conditions:

At a temperature not higher than 25 °C. Keep out of the reach of children.

Vacation conditions

On prescription.

Registration Certificate Holder

Limited Liability Company "Pharmacy in Plus" (000 "AVP"), Russia, 117186, Moscow, Nagornaya street, building 20, building 1.

Manufacturer/organization accepting claims

JSC "Pharmproekt", Russia, 192236, St. Petersburg, st. Sofiyskaya, 14.

A drug Chlorprothixene- neuroleptic, antipsychotic, thymoleptic, antiemetic, anticonvulsant drug.
It has antiserotonin, cholinergic and adrenolytic activity. Blocks dopamine receptors in polyneuronal synapses of the brain (relieves the productive symptoms of psychosis - delusions and hallucinations), as well as in the nigrostriatal zone and tubuloinfundibular region (which causes extrapyramidal disorders). Binds histamine, serotonin, alpha-adrenergic and cholinergic receptors in the central nervous system, inhibits the trigger zone of the vomiting center.
When taken orally, it is quickly absorbed. The action occurs within 20 minutes. Subjected to first-pass metabolism (in the intestinal walls and liver); due to the “first pass” effect, plasma concentrations are always lower than with intramuscular administration. Penetrates through the placental barrier and into breast milk. It is excreted by the kidneys and intestines, primarily in the form of metabolites (at a daily dose of 300 mg - about 29% as chlorprothixene, 41% as chlorprothixene sulfoxide). T1/2 is 8-12 hours.

Indications for use

Indications for use of the drug Chlorprothixene are: psychoses, including schizophrenia and manic states, occurring with psychomotor agitation, agitation and anxiety; depressive states during menopause; paroxysms of excitement associated with fear and tension; dyscirculatory encephalopathy, traumatic brain injury, withdrawal syndrome in alcoholism and drug addiction; hyperactivity, irritability, agitation, confusion in elderly patients; sleep disturbance in anxiety states, premedication, anxiety (including in patients with burns), pruritic dermatosis, bronchospasm, vomiting, pain syndrome (in combination with analgesics). In child psychiatry: psychosomatic and neurotic disorders, behavioral disorders in children.

Mode of application

For oral administration for adults daily dose Chlorprothixene varies from 10 mg to 600 mg, for children - from 5 mg to 200 mg.
The frequency of administration and duration of treatment are determined by the indications.

Side effects

From the nervous system and sensory organs: increased fatigue, dizziness, psychomotor retardation, mild extrapyramidal hypokinetic-hypertensive syndrome, akathisia (within the first 6 hours after administration), dystonic reactions, persistent tardive dyskinesia, opacification of the cornea and/or lens with possible impairment vision, accommodation paresis; rarely - neuroleptic malignant syndrome, tardive dystonia.
From the cardiovascular system and blood (hematopoiesis, hemostasis): orthostatic hypotension, tachycardia, change in the QT interval on the ECG; rarely - agranulocytosis (more likely between 4-10 weeks of treatment), leukopenia, hemolytic anemia.
From the gastrointestinal tract: dryness of the oral mucosa, constipation, cholestatic jaundice (more likely between 2-4 weeks of treatment).
From the genitourinary system: urinary retention, dysmenorrhea, decreased potency and/or libido.
Allergic reactions: skin rash, dermatitis, photosensitivity.
Other: withdrawal syndrome, flushing, galactorrhea, gynecomastia, increased appetite, changes in carbohydrate metabolism, weight gain, increased sweating.

Contraindications

Contraindications to the use of the drug Chlorprothixene are: hypersensitivity; poisoning with central nervous system depressants (including alcohol), coma, vascular collapse, pheochromocytoma, diseases of the hematopoietic organs, pregnancy, breastfeeding, children (up to 6 years).
With caution: diseases of the cardiovascular system (risk of transient increase in blood pressure), severe cerebral atherosclerosis, glaucoma (including predisposition to it), tendency to collapse, peptic ulcer of the stomach and duodenum; respiratory distress associated with acute infectious diseases, asthma or emphysema, urinary retention, Parkinson's disease (increased extrapyramidal effects), prostatic hyperplasia with clinical manifestations (risk of urinary retention), Reye's syndrome (increased risk of hepatotoxicity), epilepsy (in as a result of a decrease in the seizure threshold, an increase in seizures is possible), diabetes mellitus, severe impairment of liver and/or kidney function.

Pregnancy

Chlorprothixene Contraindicated for use during pregnancy and lactation.

Interaction with other drugs

Depressive effect Chlorprothixene on the central nervous system may be enhanced by simultaneous use with general anesthetics, narcotic analgesics, sedatives, hypnotics, other neuroleptics, as well as with ethanol and ethanol-containing drugs. The anticholinergic effect is enhanced by the simultaneous use of anticholinergic, antihistamine and antiparkinsonian drugs. Chlorprothixene enhances the effect of antihypertensive drugs and reduces the effectiveness of levodopa. The simultaneous use of chlorprothixene and epinephrine can lead to arterial hypotension and tachycardia.

Overdose

Symptoms of drug overdose Chlorprothixene: convulsions, respiratory failure, severe drowsiness, coma, tachycardia, hyperthermia, decreased blood pressure.
Treatment: gastric lavage, administration of activated charcoal and saline laxatives, symptomatic and supportive therapy. Dialysis is ineffective.

Storage conditions

In a place protected from light, at a temperature not exceeding 25°C.

Release form

Chlorprothixene - film-coated tablets.
Packaging: 30 tablets.

Compound

1 film-coated tablet Chlorprothixene contains the active substance: chlorprothixene hydrochloride 15 and 50 mg.
Excipients: corn starch, lactose monohydrate, sucrose, calcium stearate, talc.
Shell composition: hypromellose 2910/5, macrogol 6000, macrogol 300, talc, aluminum varnish based on sunset yellow dye.

Main settings

Name:	CHLOROPROTIXENE
ATX code:	N05AF03 -