Chlorprotixen Zentiva (Chlorprothixen-Zentiva)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceChlorprotixenChlorprotixen
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    • Dosage form: & nbspfilm coated tablets
    Composition:

    Each tablet, film-coated, 15 mg contains: active substance chlorprotixene hydrochloride - 15 mg; Excipients core: corn starch - 10 mg, lactose monohydrate - 92 mg, sucrose - 10 mg, calcium stearate - 1.5 mg, talc - 1.5 mg; film sheath: hypromellose 2910/5 - 2,011 mg, macrogol 6000 - 0.069 mg, macrogol 300 - 0.49 mg, talc - 1.43 mg, aluminum lacquer based on the sunset sunset yellow (E 110) - 1 mg.

    Each tablet, film-coated, 50 mg contains: active substance - chlorprotixene hydrochloride - 50 mg; auxiliary substances core: corn starch 37.5 mg, lactose monohydrate - 135 mg, sucrose - 20 mg, calcium stearate - 3.75 mg, talc - 3.75 mg; film membrane: hypromellose 2910/5 - 3,6594 mg, macrogol 6000 - 0,1333 mg, macrogol 300 - 0,9166 mg, talc - 2,4194 mg, titanium dioxide - 0,3423 mg, iron dye oxide yellow - 0 , 0290 mg.

    Description:

    Tablets 15 mg: round biconvex tablets, covered with a film shell of orange color. View at a break: the core is from white to almost white.

    Tablets 50 mg: round biconvex tablets, covered with a film membrane from light brown to light yellow color. View at a break: the core is from white to almost white.

    Pharmacotherapeutic group:antipsychotic agent (antipsychotic)
    ATX: & nbsp

    N.05.A.F.03   Chlorprotixen

    Pharmacodynamics:

    Chlorprotixen is a neuroleptic, a derivative of thioxanthene. Has antipsychotic, pronounced sedative and moderate antidepressant effect. The antipsychotic effect of chlorprotixen is associated with its blocking effect on dopamine receptors. With the blockade of these receptors, the antiemetic and analgesic properties of the drug are also associated. Chlorprotixen is able to block 5-HT2-receptors, a1-adrenoceptors, as well as Hi-gastamine receptors, what determines its adrenoblocking antihypertensive and antihistamine actions.

    Pharmacokinetics:

    The bioavailability of chlorprotixen at oral intake is about 12%. After ingestion quickly and well absorbed. In the walls of the intestine and liver is subjected to pre-systemic metabolism. Has the effect of "first pass" through the liver.Penetrates through the placental barrier and into breast milk.

    Excreted by the kidneys and intestines, mainly in the form of metabolites: when receiving a daily dose of 300 mg - about 29% as chlorprothixene, 41% - chlorprothixene sulfoxide. The half-life is 8-12 hours.

    Indications:

    - psychoses, including schizophrenia and manic conditions, which occur with psychomotor agitation, agitation and anxiety;

    - abstinence syndrome in alcoholism and drug addiction

    - hyperactivity, irritability, agitation, confusion in elderly

    patients;

    - impaired behavior in children;

    - Depressive states, neuroses, psychosomatic disorders;

    - Insomnia;

    - pain (in combination with analgesics).

    Contraindications:

    Hypersensitivity to the drug (including phenothiazines). Depression of the central nervous system (CNS) of any origin (including those induced by alcohol, barbiturates, or opiates), coma, cardiovascular collapse, pathological changes in blood, bone marrow depression, pheochromocytoma, hereditary diseases such as fructose or lactose intolerance,deficiency of lactase or glucose-galactose malabsorption, deficiency of sugar / isomaltase (due to the presence of lactose and sucrose), children under 6 years.

    Carefully:

    with a tendency to collapse, with severe cardiovascular and respiratory insufficiency (due to acute infectious diseases, asthma or emphysema of the lungs), the risk of transient increase in blood pressure (AD), severe atherosclerosis of the cerebral vessels, glaucoma (including predisposition to it), ulcerative stomach and duodenal ulcers, renal and / or hepatic insufficiency, urinary retention and the risk of urinary retention in clinical manifestations of prostatic hyperplasia, Reye's syndrome (increased risk pathotoxic effects), Parkinson's disease (possibly intensifying extrapyramidal disorders), epilepsy (there may be more seizures as a result of lowering the convulsive threshold), diabetes mellitus. Alcohol abuse can exacerbate CNS depression.

    Pregnancy and lactation:

    Chlorprotixen should not be given to pregnant women and during breastfeeding.

    Dosing and Administration:

    Chlorprotixen Zentiva can be used for a long time because it does not cause the development of addiction or drug dependence.

    Psychoses, including schizophrenia and manic conditions:

    Treatment begins with 50-100 mg / day, gradually increasing the dose to achieve the optimal effect, usually up to 300 mg / day. The maintenance dose is usually 100-200 mg / day. The maximum daily intake for adults is 600 mg.

    The daily dose of Chlorprothixen Zentiva is usually divided into 2-3 administrations, given the expressed sedative effect of Chlorprothixen Zentiva, it is recommended to prescribe a smaller part of the daily dose in the daytime, and most in the evening.

    Abstinence syndrome with alcoholism and drug addiction

    The daily dose divided into 2-3 doses is 500 mg. The course of treatment usually lasts 7 days. After the disappearance of manifestations of withdrawal, the dose gradually decreases. The maintenance dose of 15-45 mg / day allows to stabilize the condition, reduces the risk of developing another binge.

    In elderly patients

    In the presence of hyperactivity, irritability, agitation, confusion, 15-90 mg / day is prescribed. The daily dose, as a rule, is divided into 3 doses.

    Children

    To correct for the violation of behavior, Chlorprothixen Zentiva is prescribed at a rate of 0.5-2 mg per kg of body weight.

    Depressive states, neuroses, psychosomatic disorders

    Chlorprotixen Zentiva can be used for depression, especially when combined with anxiety, stress, as an adjunct to therapy with antidepressants or alone.

    Chlorprotixen Zentiva can be prescribed for neuroses 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.

    Insomnia

    For 15-30 mg in the evening for 1 h before bedtime.

    Pain

    The ability of Chlorprothixen Zentiva to potentiate the action of analgesics can be used in the treatment of patients with pain. In these cases, Chlorprothixen Zentiva is prescribed together with analgesics in doses of 15 to 300 mg.

    Side effects:

    The frequency of adverse reactions listed below was determined according to the following (World Health Organization classification): very often more than 1/10, often from more than 1/100 to less than 1/10, infrequently from more than 1/1000 to less than 1/100 , rarely - from more than 1/10000 to less than 1/1000, very rarely - from less than 1/10000, including individual messages.

    From the side of the nervous system: drowsiness, fatigue, dizziness, psychomotor retardation, easy extrapyramidal hypokinetic-hypertensive syndrome, akathisia (within the first 6 hours after administration), dystonic reactions persisting tardive dyskinesia (these side effects usually occur at the beginning of therapy and often disappear as it continues); rarely - malignant neuroleptic syndrome, late dystonia.

    From the cardiovascular system: orthostatic hypotension (especially with the use of Chlorprotixen Zentiva in high doses), transient tachycardia and changes in the Q-T interval on an electrocardiogram.

    From the side of the digestive system: transient dryness of the oral mucosa; rarely - constipation, cholestatic jaundice with prolonged use, especially in high doses (more likely between 2-4 weeks of treatment).

    On the part of the endocrine system: rarely - dysmenorrhea, with prolonged use in high doses - galactorrhea, gynecomastia, diabetes mellitus, decreased potency and / or libido, increased appetite, change in carbohydrate metabolism, weight gain, increased sweating, temporary at the beginning of therapy.

    From the sense organs: clouding of the cornea and / or lens with possible visual impairment, paresis of accommodation at the beginning of treatment and disappearing as the therapy continues.

    On the part of the organs of hematopoiesis: rarely - agranulocytosis (more likely between 4-10 weeks of treatment), single cases of transient benign leukopenia and hemolytic anemia.

    Other: urinary retention, skin rash, dermatitis, photosensitivity, withdrawal syndrome, blood flushes to the face.

    Overdose:

    Symptoms: Drowsiness, hypo- or hyperthermia, extrapyramidal symptoms, convulsions, shock, coma.

    Treatment: Symptomatic and supportive. As soon as gastric lavage is to be performed, the use of activated charcoal is recommended. Measures should be taken to maintain the respiratory and cardiovascular system,cardiovascular systems. Do not use epinephrine, t. this can lead to a subsequent lowering of blood pressure. Seizures can be suppressed with diazepam, and extrapyramidal disorders with biperidenum.

    Interaction:

    The inhibitory effect of chlorprotixen on the central nervous system may be enhanced bysimultaneous admission with ethanol and ethanol containing drugs, anesthetics, opioid analgesics, sedatives, hypnotics, antipsychotics.

    The anticholinergic effect of chlorprotixen is enhanced by the simultaneous use of M-cholinoblockers, antihistamines and anti-Parkinsonian agents. The use of chlorprotixen leads to a decrease in the threshold of convulsive activity, which requires an additional correction of the dose of antiepileptic drugs in patients with epilepsy.

    The ability of chlorprotixen to block dopamine receptors decreases the effectiveness of levodopa.

    Compatible with timoleptics (including amitriptyline, nortriptyline, imipramine, dolepin).

    Perhaps the emergence of extrapyramidal disorders with the simultaneous use of phenothiazines, metoclopramide, haloperidol, reserpine.

    There may be a perversion of the peripheral vasoconstrictive effect caused by dopamine in high doses, epinephrine and ephedrine (the presence of alpha-adrenergic blocking action in chlorprotixen). The prescription of thioxanthenes may reduce the vasoconstrictor effect of phenylephrine.

    The drug enhances the effect of antihypertensive drugs.The simultaneous use of chlorprotixen and epinephrine can lead to arterial hypotension and tachycardia.

    Reduces the hypotensive effect of guanetidine due to its displacement from adrenergic neurons and inhibition of its capture by these neurons.

    Quinidine causes a risk of side effects from the heart. It may mask the symptoms of ototoxicity (tinnitus, dizziness) of ototoxic drugs (especially antibiotics).

    Due to hyperprolactinemia, a correction of the dosing regimen of bromocriptine may be required.

    Special instructions:

    The use of Chlorprothixen Zentiva may lead to a false positive result when an immunobiological test of urine for pregnancy, false gilerbilirubinemia, a change in the QT interval on an electrocardiogram.

    Dystonic reactions are most common in children and young patients; usually appear early in the course of treatment and may subside within 24-48 hours after cessation of treatment.

    Parkinsonian extrapyramidal effects can occur in the first few days of treatment, but usually their frequency increases with increasing dose; may be more frequent in elderly patients and older children

    Late dyskinesia at the beginning of treatment is dose-dependent, but its frequency may increase with prolonged treatment and with the achievement of the total dose; can persist after the termination of the use of thioxanthenes.

    During the treatment it is necessary to perform a blood test and determine the leukocyte formula, monitor the liver function, ophthalmological examination, as well as careful observation to identify early signs of tardive dyskinesia and dystonia.

    The likelihood of hypotensive and extrapyramidal reactions in adolescents is higher than in adults.

    Malignant neuroleptic syndrome may occur at any time during treatment with antipsychotic drugs, but more often it develops shortly after initiation of therapy or after the transfer of the patient from another neuroleptic, during combined treatment with other psychoactive drugs or after increasing the dose.

    Although not all listed side effects are specifically associated with each thioxanthene, it is likely that they may occur when using any drug from this group.

    During treatment should refrain from taking ethanol,exposure to extremely high temperatures (the risk of heat stroke), insolation.

    To avoid the development of the "withdrawal" syndrome, discontinuation of treatment should be gradual.

    Effect on the ability to drive transp. cf. and fur:

    During the administration of Chlorprothixen Zentiva, caution should be exercised when driving vehicles and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

    Form release / dosage:Film coated tablets 15 mg, 50 mg.
    Packaging:For 10 tablets in a blister of PVC / A1. For 3 or 5 blisters together with instructions for use in a cardboard bundle.
    Storage conditions:

    At a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    3 years.

    Do not use after the expiry date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:П N012015 / 01
    Date of registration:21.06.2010
    The owner of the registration certificate:Zentiva c.s.Zentiva c.s. Czech Republic
    Manufacturer: & nbsp
    ZENTIVA, k.s. Czech Republic
    Representation: & nbspZENTIVA PHARMA, LLCZENTIVA PHARMA, LLC
    Information update date: & nbsp19.10.2015
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