Active substanceZuclopentixolZuclopentixol
Similar drugsTo uncover
  • Clopixol
    pills inwards 
    H. Lundbeck A / S     Denmark
  • Clopiksol Depot
    solution w / m 
    H. Lundbeck A / S     Denmark
  • Clopixol-Acuffase
    solution w / m 
    H. Lundbeck A / S     Denmark
  • Dosage form: & nbspFilm-coated tablets.
    Composition:

    Active substance - Zuclopentixola dihydrochloride 2.364 mg / 11.82 mg / 29.55 mg, corresponding to 2 mg / 10 mg / 25 mg of zuclopentixol; Excipients - potato starch 22.2 mg / 29.2 mg / 31.6 mg, lactose monohydrate 17.4 mg / 21.6 mg / 22.0 mg, microcrystalline cellulose 9.0 mg / 13.5 mg / 18.0 mg, copovidone 3.0 mg / 4.5 mg / 6.0 mg, glycerol 85% 1.2 mg / 1.8 mg / 2.4 mg, talc 4.2 mg / 6.3 mg / 8.4 mg, hydrogenated castor oil 0.48 mg / 0.72 mg / 0.96 mg, magnesium stearate 0.42 mg / 0.63 mg / 0.84 mg.

    Sheath: Hypromellose 5 1.37 mg / 2.05 mg / 2.74 mg, macrogol 6000 0.274 mg / 0.411 mg / 0.548 mg, titanium dioxide (E171) 0.445 mg / 0.479 mg / 0.091 mg, iron oxide red (E172) 0.011 mg / 0.205 mg / 0.822 mg.

    Description:

    2 mg - round, biconcave tablets, covered with a film membrane of pale pink color. The color on the cross-section is white;

    10 mg - round, biconcave tablets, covered with a film membrane of a pinkish-brown color. The color on the cross-section is white;

    25 mg - round, biconvex tablets, covered with a film membrane of red-brown color. The color on the cross-section is white.

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

    N.05.A.F.05   Zuclopentixol

    Pharmacodynamics:

    Clopixol is an antipsychotic drug (neuroleptic) of the thioxanthene group.

    Antipsychotic action of neuroleptics is associated with blockade of dopamine receptors, and, possibly, blockade of 5-HT (5-hydroxytryptamine) receptors.

    In vitro zuclopentixol has a high affinity for dopamine receptors D1 and D2, as well as alpha 1-adrenergic receptors and serotonin 5-HT receptors2, but does not have an affinity for muscarinic cholinergic receptors. The drug has a weak affinity for H1 histamine receptors, and does not have alpha2-adrenergic blocking activity. In vivo affinity for D2 receptors predominate over affinity to D1 receptors.

    Like most antipsychotics zuclopentixol increases the level of prolactin in the serum.

    Zuclopentixol is intended for the treatment of acute and chronic psychoses and for the treatment of mentally retarded patients with hyperactive and aggressive behavior.

    In addition to significantly weakening or completely eliminating the main symptoms of schizophrenia such as hallucinations, delusions and thinking disorders, zuclopentixol also has a pronounced effect on the accompanying symptoms - hostility, suspicion, agitation and aggression.

    Zuclopentixol has a transient, dose-dependent sedative effect. The rapid development of sedation at the onset of therapy is usually an advantage in the treatment of acute psychosis. Tolerance to the nonspecific sedative effect of the drug develops rapidly. The specific inhibitory effect of Clopixol is particularly beneficial in the treatment of patients with agitation, anxiety, hostility or aggressiveness.

    Pharmacokinetics:

    Bioavailability of zuclopentixol at oral intake is about 44%. The maximum concentration in the serum is reached after about 4 hours.

    Apparent volume of distribution (Vd)β is about 20 l / kg. Binding to blood plasma proteins is about 98-99%.

    Zuclopentixol slightly penetrates the placental barrier and in small amounts is excreted in breast milk. The half-life is approximately 20 hours. Metabolites do not have neuroleptic activity and are excreted, mainly with faeces and, in part, with urine.

    When supporting therapy in patients with schizophrenia with mild or moderate severity of the disease, the level of serum concentration in the serum at 2.8-12 ng / ml (7-30 nmol / L) is recommended (that is, measured immediately before administration).

    Indications:

    Acute and chronic schizophrenia and other psychotic disorders, especially with hallucinations, paranoid delusions and mental disorders, as well as agitation, anxiety, hostility or aggressiveness.

    The manic phase of manic-depressive psychosis.

    Agitation and other behavioral disorders in mentally retarded patients.

    Contraindications:

    Hypersensitivity to zuclopentixol or any of the excipients.

    Known hypersensitivity to tixanthene group drugs. Acute intoxication with ethanol, barbiturates and opiates.

    Collapse, oppression of consciousness of any origin, coma, presumed or established subcortical brain damage.

    Hereditary intolerance to galactose, insufficiency of lactase or impaired absorption of glucose and galactose.

    Carefully:

    Organic diseases of the brain, mental retardation, convulsive disorders, hepatic insufficiency, cardiovascular diseases in history, including prolongation of the QT interval, bradycardia <50 beats per minute, recent acute myocardial infarction,decompensated heart failure, arrhythmia, hypokalemia, hypomagnesemia and genetic predisposition to such conditions, the presence of risk factors for stroke (including acute arteriosclerosis), parkinsonism, opioid and alcohol dependence; pregnancy, the period of breastfeeding; children and adolescents under 18 years of age (due to inadequate clinical data).

    Pregnancy and lactation:

    During pregnancy, Clopixol should be used only if the intended benefit to the mother exceeds the potential risk to the fetus.

    In newborns whose mothers took neuroleptic drugs at the end of pregnancy or during childbirth, there may be signs of intoxication, such as lethargy, tremors and excessive excitability. In addition, such neonates have a low Apgar score.

    During treatment with Clopixol, breast-feeding is allowed, if it is clinically necessary. Nevertheless, it is recommended to observe the condition of the newborn, especially in the first 4 weeks after birth.

    Dosing and Administration:

    Tablets are taken orally: swallowed, washed down with water.

    Doses of the drug should be selected individually, depending on the patient's condition. Typically, small doses (from 2-10 mg and higher, depending on the indication) should be initially used, which then quickly grow to optimal, depending on the clinical effect. A maintenance dose can be prescribed once a day before bedtime.

    Acute attack of schizophrenia, other acute psychotic disorders, severe agitation and mania.

    Usually 10-50 mg / day.

    In severe disorders and conditions of moderate severity, the initial dose of 20 mg / day may, if necessary, increase by 10-20 mg in 2-3 days to 75 mg per day or more. The maximum single dose is 40 mg. The maximum daily dose is 150 mg.

    Chronic psychotic conditions in schizophrenia and other chronic psychoses.

    Supportive dose of 20-40 mg / day.

    Agitation in patients with mental retardation.

    Usually 6-20 mg / day. If necessary, the dose may increase to 25-40 mg / day.

    Elderly patients:

    Elderly patients should be given minimum doses from the possible dose range (2-6 mg and above).

    Decreased liver function:

    Clopixol should be used with caution in patients with hepatic insufficiency. Patients with impaired liver function should be given half of the recommended doses, and if possible, monitor the level of the drug in the blood serum.

    Decreased kidney function:

    Clopixol may be given in usual doses to patients with reduced renal function.

    Side effects:

    Most side effects are dose-dependent. The incidence of side effects and their intensity are most pronounced in the early stages of treatment and decrease with the continuation of therapy.

    Information on the incidence of side effects is presented on the basis of literature data and spontaneous reports. The frequency is indicated as: very often (≥1 / 10), often (from ≥1 / 100 to <1/10), infrequently (from 1/1000 to <1/100), rarely (from ≥1 / 10000 to <1 / 1000), very rarely (<1/10000), or unknown (can not be estimated based on existing data).

    From the nervous system: very often - drowsiness, akathisia, hyperkinesis, hypokinesia; often - a tremor, a dystonia, a muscular hypertonus, a giddiness, a headache, paresthesias, infringements of attention, an amnesia,violation of gait; infrequently - tardive dyskinesia, hyperreflexia, parkinsonism, fainting, speech disorders, dyskinesia, ataxia, hypotension, convulsive disorders, migraine; very rarely - malignant neuroleptic syndrome.

    From the side of mental activity: often - insomnia, depression, anxiety, nervousness, agitation, unusual dreams, decreased libido; infrequently - apathy, increased libido, nightmarish dreams, confusion.

    From the cardiovascular system: often tachycardia, palpitation; infrequently - lowering blood pressure, "hot flashes"; rarely - an extended QT interval on an electrocardiogram; very rarely venous thromboembolism.

    On the part of the organs of vision: often - a violation of accommodation, visual impairment; infrequently - mydriasis (dilated pupil), involuntary movement of eyeballs.

    From the side of the organ of hearing and labyrinth: often - dizziness; infrequently - a hyperacusion, a noise in the ears.

    From the respiratory system: often shortness of breath, nasal congestion.

    From the digestive system: very often - dry mouth; often - increased salivation, constipation, vomiting, dyspepsia, diarrhea; infrequently - pain in the abdomen, nausea, flatulence.

    Metabolic disorders and eating disorders: often - increased appetite, weight gain; infrequent - loss of appetite, weight loss; rarely - hyperglycemia, impaired glucose tolerance, hyperlipidemia.

    On the part of the reproductive system: infrequently - violations of ejaculation, erectile dysfunction, violation of orgasm in women, vulvovaginal dryness; rarely - galactorrhea, gynecomastia, amenorrhea, priapism.

    From the urinary system: often painful urination, urinary retention, polyuria.

    Hepatic and hepatobiliary disorders: infrequently - changes in laboratory parameters of liver function; very rarely - cholestatic hepatitis, jaundice.

    From the endocrine system: rarely - hyperprolactinaemia.

    From the blood and lymphatic system: rarely thrombocytopenia, neutropenia, leukopenia, agranulocytosis.

    From the skin and subcutaneous tissue: often - hyperhidrosis, itching; infrequently - photosensitivity, pigmentation disorder, seborrhea, skin rash, dermatitis, purpura.

    From the musculoskeletal system: often - myalgia; infrequently - muscular rigidity, trismus, torticollis.

    From the immune system: rarely - hypersensitivity, anaphylactic reactions.

    On the part of the body as a whole: often - asthenia, fatigue, malaise, pain; infrequently - thirst, hypothermia, pyrexia.

    Extrapyramidal disorders may occur, especially in the early stages of treatment. In most cases, these side effects are successfully controlled by reducing the dose and / or using antiparkinsonian drugs. However, routine use of anti-Parkinsonics to prevent side effects is not recommended. They do not relieve the manifestations of tardive dyskinesia and can worsen them. It is recommended that the dose be reduced or, if possible, discontinuation of therapy with zuclopentixol. With persistent akathisia, benzodiazepines may be useful or propranolol.

    When receiving zuclopenthixol also been reported the following side effects that occur when taking other antipsychotics: in rare cases, lengthening the interval QT, ventricular arrhythmia - tachycardia and fibrillation, sudden death, cardiac arrest and the development of paroxysmal ventricular tachycardia (torsade des pointes).

    A sharp discontinuation of zuclopentixol administration may be accompanied by the occurrence of 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, sensations of heat and cold, tremor. Symptoms usually begin within 1-4 days after cancellation and decrease within 7-14 days.

    Overdose:

    Symptoms.

    Drowsiness, coma, motor disorders, convulsions, shock, hyperthermia / hypothermia.

    In case of an overdose at the same time as taking medications that affect cardiac activity, ECG changes, QT interval prolongation, polymorphic pirouette ventricular tachycardia, cardiac arrest and ventricular arrhythmias were recorded.

    Treatment.

    Symptomatic and supportive. Measures should be taken to maintain the respiratory and cardiovascular systems. Do not use epinephrine (adrenaline), tk. this can lead to a subsequent lowering of blood pressure. Seizures can be stopped with diazepam, and motor disorders biperidenom.
    Interaction:

    Clopixol can enhance the sedative effect of alcohol, the effects of barbiturates and other CNS depressant substances.

    Clopixol should not be administered together with guanethidine and similarly acting agents, as antipsychotics may increase or decrease the effect of certain antihypertensive agents; The antihypertensive effect of guanethidine and similarly acting drugs is reduced.

    Simultaneous use of neuroleptics and lithium increases the risk of neurotoxicity.

    Tricyclic antidepressants and neuroleptics mutually inhibit each other's metabolism.

    Clopixol may reduce the effectiveness of levodopa and the effect of adrenergic drugs.

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

    Because the zuclopentixol partially metabolized by the isoenzyme CYP2D6, then simultaneous administration with drugs inhibiting this isoenzyme may lead to a decrease in the clearance of zuclopentixol. The increase in the QT interval, characteristic for therapy with antipsychotic agents, can be enhanced by simultaneous administration of drugs prolonging the QT interval: antiarrhythmic drugs IA and III classes (quinidine, amiodarone, sotalol, dofetilide), some antipsychotics (thioridazine), some antibiotic-macrolides (erythromycin) and antibiotics of the quinolone series (gatifloxacin, moxifloxacin), some antihistamines (terfenadine, astemizole), as well as cisapride, lithium and other drugs that increase the QT interval. You should avoid the simultaneous administration of Clopixol and the above drugs.

    Clopiksol should be administered with caution at the same time as drugs that cause electrolyte disorders (thiazide and thiazide-like diuretics) and drugs that can increase the concentration of zuclopentixol in blood plasma, because of the possible increase in the risk of prolonging the QT interval and the occurrence of life-threatening arrhythmias.

    Special instructions:

    For prolonged therapy, especially in large doses (above 25-40 mg / day), careful monitoring should be carried out, periodically assessing the condition of patients in order to decide on the possibility of reducing the maintenance dose.

    When treating any neuroleptic, there is the possibility of developing a malignant neuroleptic syndrome (CNS). The main symptoms of the NSA are hyperthermia,Muscular rigidity and impaired consciousness in combination with dysfunction of the autonomic nervous system (labile arterial pressure, tachycardia, increased sweating). In addition to the immediate discontinuation of antipsychotics, the use of general supportive measures and symptomatic treatment is extremely important.

    With concomitant diabetes, the use of Clopixol may alter the insulin and glucose levels in the blood, which may require correction of the dose of hypoglycemic drugs.

    Like other drugs belonging to the therapeutic class of neuroleptics, Clopixol may cause an extension of the QT interval. Constantly extended intervals of QT may increase the risk of malignant arrhythmias.

    There have been reports of cases of venous thromboembolism in the presence of neuroleptics. Due to the fact that patients treated with neuroleptics are often at risk for developing venous thromboembolism, risk factors for venous thromboembolism need to be determined and precautions taken prior to and during treatment with Clopixol.

    In randomized, placebo-controlled clinical trials, the use of some atypicalantipsychotic drugs in patients with dementia there was a 3-fold increase in the risk of cerebrovascular adverse reactions. The mechanism of such an increase in risk is unknown. It is also possible to exclude risk increases when other antipsychotics are used in other patient groups. Care should be taken in patients with risk of stroke.

    Data from two large observational studies showed that elderly patients with dementia who took antipsychotics had a slight increase in the risk of death, compared with patients who did not take antipsychotics. Sufficient data for an accurate assessment of the magnitude of the risk and the reasons for its increase are not available. Clopixol is not registered for the treatment of behavioral disorders in elderly patients with dementia.

    When alcohol is used against the background of treatment with zuclopentixol, the oppressive effect on the central nervous system may be increased.

    Tablets contain hydrogenated castor oil, which can cause indigestion and diarrhea.

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

    Patients should be warned about the sedative effect of the drug and the possible effect of its admission on the abilitydriving and management of vehicles.

    Form release / dosage:

    Tablets, film-coated 2 mg, 10 mg, 25 mg.

    Packaging:

    For 50 or 100 tablets in a plastic container with protection from opening by children and control of the first autopsy. On the cover by embossing method, a scheme for opening the container is made. Container with instructions for use in a cardboard box.

    Storage conditions:

    At a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    2 years.

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

    Terms of leave from pharmacies:On prescription
    Registration number:П N014166 / 01-2002
    Date of registration:22.10.2008
    The owner of the registration certificate:H. Lundbeck A / SH. Lundbeck A / S Denmark
    Manufacturer: & nbsp
    Representation: & nbspLUNDBEK EXPORT A / C LUNDBEK EXPORT A / C Denmark
    Information update date: & nbsp04.09.2015
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