Chlorprothixen, pills 50mg, 30pcs

Composition

One film-coated tablet of 50 mg contains: Active ingredient: Chlorprothixene hydrochloride-50,000 mgsupport substances: Corn starch-37,500 mg Lactose monohydrate-135,000 mg Sucrose-20,000 mg Calcium stearate – 3,750 mg Zinc-3,750 Mgfilm shell: Opadray 32F220033 Yellow-7,500 mg

Pharmacological action

Chlorprothixen is a neuroleptic drug derived from thioxanthene. It has antipsychotic, pronounced sedative and moderate antidepressant effects. The antipsychotic effect of neuroleptics is associated with the blockade of dopamine receptors, as well as, possibly, the blockade of 5-HT(5-hydroxytryptamine) receptors. In vivo, Chlorprothixen has a high affinity for dopamine receptors such as D1 and D2. Chlorprothixen also has a high affinity for 5-HT2-receptors, �1-adrenergic receptors, histamine (H1) and cholinergic muscarinic receptors. The receptor binding profile of Chlorprothixen is very similar to that of clozapine, but it has approximately 10 times higher affinity for dopamine receptors. Chlorprothixen reduces or eliminates anxiety, obsessions, psychomotor 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%) indicate that Chlorprothixen can be successfully used for maintenance therapy of patients with psychotic disorders. Low doses of Chlorprothixen have an antidepressant effect, which makes it useful to use the drug for mental disorders characterized by anxiety, depression and anxiety. Chlorprothixen therapy also reduces the severity of associated psychosomatic symptoms. Chlorprothixen is not addictive, addictive, or tolerant. In addition, Chlorprothixen potentiates the action of analgesics, has its own analgesic effect, as well as antipruritic and antiemetic effects… Pharmacokinetics of absorption When taken orally, the maximum concentration in blood plasma is reached after about 2 hours (range 0.5-6 hours). The average oral bioavailability of Chlorprothixen is about 12% (range 5-32%). Distributionexisting Allocation Volume (Vd)β is about 15.5 l / kg. Binding to plasma proteins is more than 99%. Chlorprothixen penetrates the placental barrier. Biotransformationmetabolism of chlorprothixene is mainly carried out by sulfooxidation and N-demethylation of the side chain. Ring hydroxylation and N-oxidation are less pronounced. Chlorprothixen is detected in the bile, which indicates the presence of intestinal-hepatic circulation of the drug. Chlorprothixen metabolites lack neuroleptic activity. Elimination The elimination half-life is about 16 hours (range 4-33 hours). The average systemic clearance (Cls) corresponds to approximately 1.2 l/min. Chlorprothixen is excreted in the faeces and urine. In women who are breast-feeding, Chlorprothixen is excreted in small amounts in milk. The ratio of the drug concentration in breast milk and in blood plasma varies from 1.2 to 2.6. There were no differences in plasma concentrations or excretion rates between the control group and the group of patients suffering from alcoholism, regardless of whether the latter were sober or in a state of acute intoxication during the study.

Indications

* Schizophrenia and other psychoses that occur with psychomotor agitation, agitation and anxiety. * Withdrawal syndrome in 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 disorders. * Pain (in combination with analgesics). Geriatrics: hyperactivity, agitation, irritability, confusion, anxiety, behavioral and sleep disorders.

Use during pregnancy and lactation

Pregnancyclinical experience of use in pregnant women is limited. Chlorprothixen should not be used during pregnancy unless the expected benefit to the patient exceeds the possible risk to the fetus. Newborns exposed to antipsychotic drugs (including Chlorprothixen) during the third trimester of pregnancy, women are at risk of developing adverse reactions, including extrapyramidal symptoms and / or withdrawal symptoms, which may vary in severity and duration after delivery. There were cases of agitation, increased and decreased tone, tremor, drowsiness, respiratory distress, and eating disorders. Therefore, newborns should be carefully monitored. Breast-feeding given that Chlorprothixen is present in low concentrations in breast milk, it is unlikely to have a negative effect on the child if the drug is prescribed to the mother in therapeutic doses. The dose taken orally in the child’s body is approximately 2% of the daily maternal dose, adjusted for body weight. Breast-feeding is permitted during treatment with Chlorprothixen if clinically necessary. Nevertheless, it is recommended to monitor the condition of the newborn, especially in the first 4 weeks after birth. Human fertility adverse events such as hyperprolactinemia, galactorrhea, amenorrhea, ejaculatory disorders, and erectile dysfunction have been reported (see section “Side effects”). These adverse reactions can have a negative impact on the sexual function and fertility of women and / or men. If clinically significant hyperprolactinemia, galactorrhea, amenorrhea, or sexual dysfunction occurs, consideration should be given to reducing the dosage (if possible) or discontinuing the drug. These side effects are reversible after discontinuation of the drug. The potential effect of the drug on fertility in animals has not been studied.

Contraindications

* Hypersensitivity to Chlorprothixen or any of the excipients. * Hypersensitivity to drugs of the thioxanthene group. * Vascular collapse, depression of consciousness of any origin (including those caused by alcohol, barbiturates or opiates), coma. * Known uncorrectable hypokalemia or hypomagnesemia. • The presence of a history of clinically significant cardiovascular diseases (for example, bradycardia (heart rate less than 50 beats per minute), recent myocardial infarction, decompensated heart failure, cardiac hypertrophy, arrhythmias for which Class IA and III antiarrhythmics are prescribed), ventricular arrhythmias or Torsade de Pointes polymorphic ventricular tachycardia. * Congenital long QT syndrome or acquired long QT interval (QTc over 450 msec in men and 470 msec in women). * Concomitant use with drugs that significantly prolong the QT interval• * lactose or fructose intolerance, lactase deficiency, glucose-galactose malabsorption, sucrose/isomaltase deficiency (due to the presence of lactose and sucrose in the composition). With caution Organic brain diseases; mental retardation; the presence in the family history of relatives suffering from cardiovascular diseases, as well as cases of prolongation of the QT interval; convulsive disorders; severe liver and kidney failure; a rare pathological condition in the form of a small anterior chamber of the eye and its narrow angle (it is possible to develop attacks of acute glaucoma associated with pupil dilation); severe pseudoparalytic myasthenia gravis; benign prostatic hypertrophy; pheochromocytoma; prolactin-dependent neoplasms; severe hypotension or orthostatic disorders; Parkinson’s disease; diseases of the hematopoietic system; hyperthyroidism; painful urination, urinary retention; pylorostenosis; intestinal obstruction; the presence of risk factors for stroke; diabetes mellitus; opiate and alcohol abuse; pregnancy, breastfeeding; children and adolescents under 18 years of age (due to insufficient strictly controlled studies).

Side effects

Drowsiness, tachycardia, dry mouth, excessive sweating, difficulty accommodating. These side effects, which usually occur at the beginning of therapy, often disappear as it continues. Orthostatic hypotension may occur, especially when Chlorprothixen is used in high dosages. Dizziness, dysmenorrhea, skin rashes, constipation are rare. Extrapyramidal symptoms are particularly rare. Isolated cases of reduced seizure threshold, transient benign leukopenia and hemolytic anemia are described. With prolonged use, especially in high doses, may occur: cholestatic jaundice, galactorrhea, gynecomastia, decreased potency and / or libido, increased appetite, weight gain.

Interaction

Chlorprothixen can enhance the sedative effect of alcohol, barbiturates and other substances that depress the central nervous system. Chlorprothixen should not be administered together with guanethidine and similar active agents, since neuroleptics can enhance or weaken the effect of antihypertensive agents; the antihypertensive effect of guanethidine and similarly active drugs is reduced. Concomitant use of antipsychotics and lithium preparations increases the risk of neurotoxicity. Tricyclic antidepressants and antipsychotics mutually inhibit each other’s metabolism. Chlorprothixen may reduce the effectiveness of levodopa and the effect of adrenergic drugs.Concomitant use of Chlorprothixen and drugs with established anticholinergic effects increases their anticholinergic effects. Concomitant use with metoclopramide and piperazine increases the risk of extrapyramidal disorders. The antihistamine effect of Chlorprothixen may inhibit or eliminate the alcohol/disulfiram reaction. The increase in the QT interval on an electrocardiogram, which is characteristic of antipsychotic therapy, can be enhanced with simultaneous use of drugs that significantly prolong the QT interval: class IA and III antiarrhythmic drugs (quinidine, amiodarone, sotalol, dofetilide), some antipsychotic drugs (thioridazine), some macrolide antibiotics (erythromycin) and quinolone antibiotics (gatifloxacin, moxifloxacin), some antihistamines (terfenadine, astemizole), as well as cisapride, lithium, and other drugs that significantly increase the QT interval. Concomitant use of Chlorprothixen and the above medications should be avoided. Chlorprothixen should be used with caution simultaneously with drugs that cause electrolyte disturbances (thiazide and thiazide-like diuretics), and drugs that can increase the concentration of Chlorprothixen in blood plasma, because of the possible increase in the risk of prolongation of the QT interval and the occurrence of life-threatening arrhythmias. Neuroleptics are metabolized by hepatic isoenzymes of the cytochrome P450 system. Drugs that inhibit the 2D6 isoenzyme (for example, paroxetine, fluoxetine, chloramphenicol, disulfiram, isoniazid, monoamine oxidase inhibitors, oral contraceptives, and, to a lesser extent, buspirone, sertraline, and citalopram) may increase the plasma content of Chlorprothixen.

Active ingredient

Chlorprothixen

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

Children as prescribed by a doctor, Adults as prescribed by a doctor

Indications

Manic-Depressive Psychosis, Depression, Mental Disorders, Neurosis, Insomnia, Schizophrenia, Hangover