Chlorprotixen, 50 mg 30 pcs
€26.13 €22.64
Chlorprotixene is a neuroleptic derivative of thioxanthene. It has antipsychotic, marked sedative and moderate antidepressant effect.
Antipsychotic effect of neuroleptics is associated with blockade of dopamine receptors, and possibly also blockade of 5-NT
(5-hydroxytryptamine) receptors. In vivo, chlorprotixene has a high affinity for dopamine receptors type D1 and D2. Chlorprotixene also has high affinity for 5-HT2 receptors, a1-adrenoceptors, histamine (H1) and cholinergic muscarinic receptors. The receptor binding profile of chlorprotixen is very similar to that of clozapine, but it has approximately 10 times higher affinity for dopamine receptors.
Chlorprotixen 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 chlorprotixen can be successfully used for maintenance therapy of patients with psychotic disorders.
Low doses of chlorprotixen have an antidepressant effect, which makes the drug useful in mental disorders characterized by anxiety, depression and anxiety. Chlorprotixene therapy also reduces the severity of associated psychosomatic symptoms. Chlorprotixene is not addictive, addictive, or tolerant. In addition, chlorprotixene potentiates the effect of analgesics, has its own analgesic effect as well as antipruritic and antiemetic…
Pharmacokinetics
Absorption
When taken orally the maximum concentration in plasma is reached after about 2 hours (range 0.5-6 hours). The average bioavailability of Chlorprotixen when ingested is approximately 12% (range 5-32%).
Distribution
The apparent volume of distribution (Vd)β is approximately 15.5 L/kg. Binding to plasma proteins is over 99%.
Chlorprotixene penetrates the placental barrier.
Biotransformation
Metabolism of chlorprotixene is primarily by sulfoxidation and N-demethylation of the side chain. The hydroxylation of the ring and N-oxidation are expressed to a lesser extent. Chlorprotixene is determined in bile, indicating the presence of intestinal-hepatic circulation of the drug. Chlorprotixene metabolites lack neuroleptic activity.
Excretion
The elimination half-life is approximately 16 hours (range 4 – 33 hours). Mean systemic clearance (Cls) corresponds to approximately 1.2 L/min. Chlorprotixene is excreted with feces and urine.
In women who are breastfeeding, chlorprotixene is excreted in small amounts with milk. The maternal milk to plasma drug concentration ratio ranges from 1.2 to 2.6.
No differences in plasma concentrations or excretion rates were found between the control group and the alcohol dependent patient group, regardless of whether the latter were sober or acutely intoxicated during the study.
Indications
Anxiety, Neurosis, Depression, Manic Depressive Psychosis, Hangover, Schizophrenia, Delirium, Insomnia, Irritability, Mental disorders – Schizophrenia and other psychoses with psychomotor agitation, agitation and anxiety.
– withdrawal syndrome in alcoholism and drug addictions.
– Depressions, neurosis, psychosomatic disorders with anxiety, tension, restlessness, insomnia and sleep disorders.
– Epilepsy and oligophrenia combined with mental disorders: agitation, agitation, mood lability and behavior disorders.
– Pain (in combination with analgesics).
– Geriatrics: hyperactivity, agitation, irritability, confusion, anxiety, behavior and sleep disorders.
Active ingredient
Chlorprotixen
Composition
One film-coated tablet, 50 mg contains:
Active ingredient:
Chlorprotixene 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 jacket:
Opadray 32F220033 Yellow – 7.500 mg
Interaction
Chlorprotixene may increase the sedative effect of alcohol, barbiturates and other CNS depressants.
Chlorprotixene should not be prescribed together with guanethidine and similarly acting agents, as neuroleptics may enhance or weaken the effect of antihypertensive drugs; the antihypertensive effect of guanethidine and similarly acting drugs is reduced.
Concomitant use of neuroleptics and lithium drugs increases the risk of neurotoxicity.
Tricyclic antidepressants and neuroleptics mutually inhibit each other’s metabolism.
Chlorprotixen may decrease the efficacy of levodopa and the effects of adrenergic drugs.
Concomitant use of Chlorprotixen 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 chlorprotixen may suppress or eliminate the alcohol/disulfiram reaction.
The QT interval prolongation on the electrocardiogram characteristic of antipsychotic therapy may be enhanced by concomitant administration of drugs that significantly prolong the QT interval: Class IA and III antiarrhythmic drugs (quinidine, amiodarone, sotalol, dofetilide), some antipsychotics (thioridazine), some macrolide antibiotics (erythromycin) and quinolone-type antibiotics (gatifloxacin, moxifloxacin), some antihistamines (terfenadine, astemizole), as well as cisapride, lithium and other drugs that significantly increase the QT interval. Concomitant administration of Chlorprotixen and the above drugs should be avoided. It is necessary to use with caution concomitantly with drugs that cause electrolyte disorders (thiazide and thiazide-like diuretics), and drugs that can increase the concentration of chlorprotixen in plasma, because of the possible risk of QT interval prolongation and life-threatening arrhythmias.
Neuroleptics are metabolized by liver cytochrome P450 isoenzymes. Drugs that inhibit the 2D6 isoenzyme (e.g., paroxetine, fluoxetine, chloramphenicol, disulfiram, isoniazid, monoamine oxidase inhibitors, oral contraceptives, and, to a lesser extent, buspirone, sertraline and citalopram) can increase plasma levels of chlorpromethixene.
Contraindications
– Hypersensitivity to chlorprotixene or any of the excipients.
– Hypersensitivity to drugs of thioxanthene group.
– Vascular collapse, depression of consciousness of any origin (including that caused by alcohol, barbiturates or opiates), coma.
– Known unregulated hypokalemia or hypomagnesemia.
– Presence of clinically significant cardiovascular diseases (e.g., bradycardia (heart rate less than 50 beats per minute), recent myocardial infarction, decompensated heart failure, cardiac hypertrophy, arrhythmias in which Class IA and III antiarrhythmics are prescribed), ventricular arrhythmias or polymorphic ventricular tachycardia by the type “pirouette” (Torsade de Pointes) in the patient history.
– Congenital syndrome of prolonged QT interval or acquired prolonged QT interval (QTc over 450 msec in men and 470 msec in women).
– Simultaneous 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).
With caution
Organic brain disease; mental retardation; family history of relatives with cardiovascular disease and cases of QT interval prolongation; seizure disorders; severe hepatic and renal insufficiency; rare pathological condition in the form of a shallow anterior chamber of the eye and its narrow angle (possible development of acute glaucoma attacks associated with pupil dilation); severe pseudoparalytic myasthenia gravis; benign prostatic hypertrophy pheochromocytoma; prolactin-dependent neoplasms; severe arterial hypotension or orthostatic disorders; Parkinson’s disease; diseases of the hematopoietic system; hyperthyroidism; painful urination, urinary retention; pilostenosis; intestinal obstruction; presence of risk factors for stroke; diabetes; opiate and alcohol abuse; pregnancy, breast-feeding period; childhood and adolescence under 18 years (due to insufficient strictly controlled studies).
Side effects
Drowsiness, tachycardia, dry mouth, increased sweating, and difficulty with accommodation. These side effects, usually occurring at the beginning of therapy, often disappear as the therapy continues. Orthostatic hypotension may be observed, especially when using Chlorprotixen in high doses.
Dizziness, dysmenorrhea, skin rashes, constipation are rare. Extrapyramidal symptoms are particularly rare. There have been single cases of decreased seizure threshold, transient benign leukopenia and hemolytic anemia.
With long-term use, especially in high doses the following may be observed: cholestatic jaundice, galactorrhea, gynecomastia, decreased potency and/or libido, increased appetite, increased body weight.
Pregnancy use
Pregnancy
Clinical experience with pregnant women is limited. Chlorprotixen should not be administered during pregnancy unless the expected benefit to the patient exceeds the possible risk to the fetus.
Newborns exposed to antipsychotics (including chlorprotixen) during the third trimester of pregnancy are at risk for adverse reactions, including extrapyramidal symptoms and/or the appearance of withdrawal syndrome, which may vary in severity and duration after delivery. Instances of agitation, increased and decreased tone, tremor, somnolence, respiratory distress, and eating disorders have been reported. Therefore, newborns should be closely monitored.
Breastfeeding
Given that Chlorprotixene is present in minor concentrations in the mother’s milk, it is unlikely to have adverse effects on the child if the drug is prescribed to the mother in therapeutic doses. The oral dose delivered to the child is approximately 2% of the maternal daily dose adjusted for body weight. Breastfeeding is allowed during treatment with Chlorprotixen if deemed clinically necessary. Nevertheless, it is recommended to monitor the newborn, especially during the first 4 weeks after birth.
Fertility
Adverse events such as hyperprolactinemia, galactorrhea, amenorrhea, ejaculation disorders, and erectile dysfunction have been reported in humans (see side effects section). These adverse reactions may have a negative effect on sexual function and fertility of women and/or men.
In case of clinically significant hyperprolactinemia, galactorrhea, amenorrhea or manifestations of sexual dysfunction, the issue of dosage reduction (if possible) or cancellation of the drug should be considered. These side effects are reversible after discontinuation of the drug.
The potential effect of the drug on fertility in animals has not been studied.
Similarities
Truxal, Chlorprotixen
Weight | 0.018 kg |
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Manufacturer | Pharmproject, Russia |
Medication form | pills |
Brand | Pharmproject |
Other forms…
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