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Active ingredients
Chlorprothixen
Release form
Pills
Composition
1 coated tablet contains: active ingredient: Chlorprothixene hydrochloride 25 mg, excipients: corn starch, lactose monohydrate, copovidone, glycerol 85%, microcrystalline cellulose, sodium croscarmellose, talc, magnesium stearate, film coating composition: Opadry OY-S 9478 brown (E 172, E 171) RM 1030
Pharmacological effect
Chlorprothixene is an antipsychotic of the thioxanthenes group. The antipsychotic action of these drugs is associated with blockade of dopamine receptors, as well as, possibly, blockade of 5-HT receptors (5-hydroxytryptamine, serotonin). In vivo, Chlorprothixene has a high affinity for the dopamine Di and D2 receptors. Chlorprothixene also has a high affinity for 5-HT2 receptors and C-adrenoreceptors, which is similar to high-dose phenothiazines, levomepromazine, chlorpromazine and thioridazine, as well as an atypical antipsychotic, kpozapine. Chlorprothixene has been shown to have an affinity for histamine (H-i) receptors at the level of diphenhydramine. In addition, Chlorprothixene has an affinity for cholinergic muscarinic receptors. The profile of chlorprothixene is very similar to that of clozapine, however, chlorprotixene has about 10 times higher affinity for dopamine receptors. In all studies with behavioral models for antipsychotic activity (blocking dopamine receptors), chlorprotixene showed a pronounced antipsychotic effect. The relationship between the two in vivo models, the affinity for the dopamine D2 receptors in vitro and the average daily oral dose of antipsychotic was demonstrated. In clinical use, Chlorprothixene is a high-dose, wide-spectrum, sedative antipsychotic that is used to treat psychotic disorders other than depression. Chlorprothixene reduces the severity or eliminates anxiety, obsessions, agitation, anxiety, 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%) (given to 11,487 patients) suggests that chlorprothixene can be successfully used for maintenance therapy of patients with psychotic disorders.Low doses of Chlorprothixene have an antidepressant effect, which makes it useful to use this drug for mental disorders characterized by anxiety, depression and anxiety. Also, during chlorprothixene therapy, the severity of associated psychosomatic symptoms decreases. Chlorprothixene is not addictive, addictive or forms tolerance. In addition, Chlorprothixene potentiates the action of analgesics, - has its own analgesic effect, as well as antipruritic and antiemetic
Pharmacokinetics
The oral bioavailability of chlorprotixen is about 12%. Chlorprothixene is rapidly absorbed from the intestine, the maximum concentration in serum is reached after 2 hours. The half-life is about 16 hours. Chlorprothixene penetrates the placental barrier and is excreted in small amounts with breast milk. Metabolites do not have neuroleptic activity, are excreted in feces and urine.
Indications
Truxal is a sedative neuroleptic with a wide range of indications, which include: psychosis, including schizophrenia and manic states, occurring with psychomotor agitation, agitation and anxiety, hangover withdrawal syndrome in alcoholism and drug addiction, hyperactivity, irritability, agitation, confusion in elderly patients, behavioral disorders in children, depression, neurosis, psychosomatic disorders, insomnia, pain (in combination with analgesics).
Contraindications
Inhibition of the central nervous system of any origin (including caused by alcohol, barbiturates or opiates), coma, vascular collapse, diseases of the hematopoietic organs, pheochromocytoma. Increased sensitivity to the components of the drug. Truxal should not, if possible, be prescribed to pregnant women and during breastfeeding .
Precautionary measures
Malignant Neuroleptic Syndrome: When taking antipsychotics, there have been reported cases of malignant neuroleptic syndrome with the following symptoms: hyperthermia, muscle rigidity, dysfunction of the autonomic nervous system, impaired consciousness and elevated serum creatine kinase.The risk may be higher when taking a potent agent. Among the cases with a fatal outcome, the majority of patients with existing organic brain syndrome, mental retardation and opiate or alcohol abusers. Treatment: discontinuation of antipsychotics, symptomatic and general supportive inpatient treatment. Symptoms may persist for a week after discontinuing oral antipsychotics. Due to the dilation of the pupil, patients with small anterior chamber of the eye and angle-closure glaucoma may develop acute glaucoma. Due to the risk of malignant arrhythmias, Truxal should be prescribed with caution in patients with a history of cardiovascular diseases and in patients with cases of an extended QT interval in family history. Before starting treatment, an ECG examination is necessary. With a QT interval of more than 450 msec in men and 470 msec in women, chlorprothixene is contraindicated. During therapy, the need for an ECG is assessed individually by the doctor. When lengthening the interval from. In the course of treatment, it is necessary to prescribe smaller doses of Truxal, and if the QT interval is longer than 500 ms, the therapy should be stopped. During treatment, it is recommended to conduct a periodic assessment of electrolyte balance. The simultaneous use of other antipsychotics should be avoided. Chlorprothixene should be used with caution in patients with organic brain syndrome, convulsive disorders, severe liver or kidney dysfunction, severe pseudo-paralytic myasthenia and benign prostatic hypertrophy. Precautions should be taken in patients with: - pheochromocytoma, - neoplasia due to prolactin, - severe hypotension - Parkinson's disease - diseases of the hematopoietic system, - hyperthyroidism, - urination disorder, urinary retention, pyloric stenosis of intestinal obstruction. Chlorprothixene can change the concentration of insulin: In order to make a decision about the possibility of reducing the maintenance dose during long-term therapy, especially with maximum daily doses, it is necessary to conduct regular monitoring of the patient's condition. It was reported on the development of venous thromboembolism while taking antipsychotics.Due to the fact that patients under treatment with antipsychotic drugs are often at risk of developing venous thromboembolism, before and during treatment with chlorprotixene, it is necessary to determine the risk factors for developing venous thromboembolism and take preventive measures. Use in children and adolescents under 18: Truxal is not recommended for use in children and adolescents. These studies on the efficacy and safety of chlorprotixen in children and adolescents are not enough. Therefore, chlorprotixen should be prescribed to children and adolescents (under 18) only if indicated, and after a thorough assessment of the benefits-risk ratio. Elderly patients: Cerebrovascular adverse reactions: In patients at risk of developing stroke, chlorprotixen should be used with caution. In a randomized, placebo-controlled clinical study on the use of some atypical antipsychotics in patients with dementia, a 3-fold increase in the risk of cerebrovascular adverse reactions was observed. The mechanism for such an increase in risk is unknown. Increased risk cannot be ruled out when other antipsychotics are used in other groups of patients. Elderly patients are particularly susceptible to orthostatic hypotension. Increased mortality in elderly patients with dementia Data from two large observational studies have shown that elderly patients with dementia who took antipsychotics showed a slight increase in the risk of death compared to patients who did not take 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: Tablets contain lactose monohydrate. Patients with hereditary intolerance to galactose, Lapp's lactase deficiency, impaired absorption of glucose and galactose should not take the drug
Use during pregnancy and lactation
During pregnancy, Truxal should be used, the benefit to the mother outweighs the potential risk to the fetus. There is no data on the use of Chlorprothixene in pregnant women.Newborns whose mothers took antipsychotic periods of pregnancy or during childbirth may experience intoxication, such as lethargy, tremor, and excessive excitability. In addition, these newborns have a low Apgar score. Newborns whose mothers took antipsychotics (including chlorprothixen) may show signs of side effects during the third trimester of pregnancy, including extrapyramidal symptoms and / or "withdrawal" syndrome, which after birth can vary in severity and duration. The following side effects were reported: agitation, hypertension, hypotension, tremor, drowsiness, respiratory depression and feeding difficulties. Thus, newborns should be carefully monitored. During breastfeeding, Truxal can only be used if it is clinically recognized. 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 the newborn. The dose absorbed by the child is about 2% of the dose taken by the mother. Animal studies do not indicate an increase in fetal side effects or any other negative effect on the reproductive process.
Dosage and administration
Psychoses, including schizophrenia and manic states. Treatment begins with 50 - 100 mg / day, gradually increasing the dose to achieve the 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 Truxal is usually divided into 2 - 3 doses, given the pronounced sedative effect of Truxal, it is recommended to prescribe a smaller part of the daily dose in the daytime, and a large part in the evening. Hungover withdrawal syndrome in alcoholism and drug addiction. The daily dose divided into 2 - 3 doses is 500 mg. The course of treatment usually lasts 7 days. After disappearance of withdrawal symptoms, the dose is gradually reduced. A maintenance dose of 15 to 45 mg / day helps stabilize the condition, reduces the risk of developing the next binge.In elderly patients with hyperactivity, irritability, agitation, confusion, 15–90 mg / day is prescribed. The daily dose is usually divided into 3 doses. In children, for the correction of behavioral disorders, Truxal is prescribed at the rate of 0.5-2 mg per 1 kg of weight. Depressive states, neurosis, psychosomatic disorders. Truxal can be used for depression, especially when combined with anxiety, tension, as an adjunct to antidepressant therapy or on its own. Truxal can be prescribed for neurosis and psychosomatic disorders, accompanied by anxiety and depressive disorders, up to 90 mg / day. The daily dose, as a rule, is divided into 2-3 doses. Since taking Truxal does not cause addiction or drug dependence, it can be used for a long time. Insomnia. At 15 - 30 mg in the evening for 1 hour before bedtime. Pains Truxal's ability to potentiate the action of analgesics can be used in the treatment of patients with pain. In these cases, Truxal is prescribed together with analgesics in doses of 15 to 300 mg.
Side effects
Drowsiness, tachycardia, dry mouth, excessive sweating, or accommodation difficulties. These side effects, usually occurring at the beginning of therapy, often disappear as it continues. Orthostatic hypotension may occur, especially when Truxal is used in high dosages. Vertigo, dysmenorrhea, skin rash, and constipation are rare. Extrapyramidal symptoms are especially rare. Isolated cases of decrease in seizure threshold, transient benign leukopenia and hemolytic anemia are described. With prolonged use, especially in high doses, cholestatic jaundice, galactorrhea, gynecomastia, weakening of potency and libido, increased appetite, weight gain can be observed.
Overdose
Symptoms Drowsiness, hypo-or hyperthermia, extrapyramidal symptoms, convulsions, shock, coma. Treatment. Symptomatic and supportive. Gastric lavage should be performed as soon as possible, the use of a sorbent is recommended. Measures should be taken to support the activity of the respiratory and cardiovascular systems. Do not use adrenaline, becausethis can lead to a subsequent lowering of blood pressure. Spasms can be stopped by diazepam, and extrapyramidal symptoms biperidenom.
Interaction with other drugs
The inhibitory effect of Chlorprothixene on the central nervous system can be enhanced while taking it with ethanol and ethanol-containing drugs, anesthetics, opioid analgesics, sedatives, hypnotics, antipsychotics. The anticholinergic effect of Chlorprothixene is enhanced with simultaneous use of anticholinergic, antihistamine and anti-Parkinsonian drugs. The drug enhances the action of antihypertensive drugs. The simultaneous use of Chlorprothixene and adrenaline can lead to arterial hypotension and tachycardia. The use of Chlorprothixene reduces the threshold of seizure activity, which requires an additional dose adjustment of antiepileptic drugs in patients with epilepsy. The ability of Chlorprothixene to block dopamine receptors reduces the effectiveness of levodopa. Extrapyramidal disorders may occur with simultaneous use of phenothiazines, metoclopramide, haloperidol, reserpine.
special instructions
Truxal should be used with caution in patients suffering from epilepsy, parkinsonism, in severe cerebral atherosclerosis, with a tendency to collapse, in severe cardiovascular and respiratory failure, in marked impaired liver and kidney function, diabetes, prostate hypertrophy. The use of Truxal can lead to a false positive result when conducting an immunobiological test of urine for pregnancy, a false increase in the level of bilirubin in the blood, a change in the QT interval on an electrocardiogram. During treatment, Truxalom is recommended to refrain from the use of alcoholic beverages, to avoid increased insolation. Acceptance of Truxal has a negative impact on activities that require a high rate of mental and physical reactions (for example, driving, servicing cars, working at height, etc.).