Fluansoxol (Fluanxol®)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceFlupentixolFlupentixol
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  • Fluansoxol
    solution w / m 
    H. Lundbeck A / S     Denmark
  • Fluansoxol
    pills
    H. Lundbeck A / S     Denmark
    • Dosage form: & nbspcoated tablets
    Composition:
    The active substance flupenthixola dihydrochloride is 0.584 mg / 1.168 mg / 5.84 mg, which corresponds to 0.5 mg / 1 mg / 5 mg flupenthixol.
    Auxiliary substances - lactose monohydrate 27.7 mg / 37.0 mg / 38.0 mg, potato starch 55.4 mg / 73.5 mg / 77.0 mg, gelatin 2.4 mg / 2.76 mg / 3, 32 mg, talc 6.3 mg / 8.4 mg / 9.1 mg, magnesium stearate 0.45 mg / 0.6 mg / 0.65 mg. The envelope is gelatin 0.371 mg / 0.558 mg / 0.558 mg, sucrose 35.9 mg / 50.0 mg / gv 60.9 mg, sucrose powder 20.5 mg / 16.2 mg / 49.2 mg, iron oxide yellow (E172) 0.25 mg / 0.25 mg / 0.3 mg, polishing wax Capol 1295® (mixture of beeswax wax and carnauba wax).

    Description:
    0.5 mg and 1 mg - round, biconvex brownish-yellow tablets covered with sugar coating;
    5 mg - oval, biconvex brownish-yellow tablets, covered with sugar shell.

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

    N.05.A.F.01   Flupentixol

    Pharmacodynamics:
    Antipsychotic action of neuroleptics is associated with blockade of dopamine receptors, and, possibly, blockade of 5-HT (5-hydroxytryptamine) receptors.
    The antipsychotic effect of flupenthixol begins to manifest itself with the administration of a daily dose of 3 mg and its severity increases with increasing dose. Flupentixol has a pronounced anxiolytic effect.The drug possesses disinhibitory (anti-astatic and activating) properties, promotes activation of patients, improves their communication skills and facilitates social adaptation.
    In small and medium doses (up to 25 mg per day) Flupentixol does not have a sedative effect, however, when the drug is prescribed in a dose exceeding 25 mg / day, a sedative effect may develop.
    When taking small doses (up to 3 mg / day) flupenthixol has antidepressant effect.

    Pharmacokinetics:
    Bioavailability of flupentixol for oral administration is about 40%. The maximum concentration in the serum is reached after about 4-5 hours. The apparent volume of distribution (Vd) p is about 14.1 l / kg. Binding to plasma proteins is about 99%.
    Flupentixol slightly penetrates the placental barrier and in small amounts is excreted in breast milk. The half-life is approximately 35 hours. Metabolites do not have neuroleptic activity; are allocated, basically, with a feces and, partially, with urine.
    With maintenance therapy in patients with schizophrenia with mild or moderate severity of the disease, it is recommended to maintain a minimumis measured immediately before administration), the concentration of flupenthixol in the serum in the range of 1-3 ng / ml (2-8 nmol / l).

    Indications:
    In a dose of up to 3 mg / day.
    Depressions of mild and moderate severity, combined with anxiety, asthenia and lack of initiative.
    Chronic neurotic disorders with anxiety, depression and apathy. Psychosomatic disorders with asthenic manifestations.
    At a dose of 3 mg / day or more.
    Schizophrenia and schizophrenia-like psychosis with a predominance of hallucinatory symptoms, delusions and mental disorders, accompanied by apathy, anergy, mood reduction and autism.

    Contraindications:
    Hypersensitivity to flupentixol or any of the excipients (in including known hypersensitivity to phenothiazines), hereditary intolerance to galactose and / or fructose, insufficiency of lactase, insufficiency of sucrose and isomaltase, impaired absorption of glucose and galactose.
    Vascular collapse, oppression of consciousness of any origin (including those caused by taking alcohol, barbiturates or opioids), coma. Children's age (up to 18 years).

    Carefully:
    organic diseases of the brain; mental retardation; convulsive disorders; severe hepatic impairment; hypokalemia, hypomagnesemia and genetic predisposition to such conditions; Cardiovascular disease history (transient risk of lowering blood pressure), including lengthening the interval QT, bradycardia <50 beats per minute, recent acute myocardial infarction, decompensated heart failure, arrhythmia; presence of risk factors for stroke; glaucoma (and predisposition to it); ulcerative stomach trouble and
    duodenum; opioid and alcohol dependence (may exacerbate CNS depression); pheochromocytoma, leukopenia; breathing disorder associated with acute infectious diseases, bronchial asthma or emphysema; Parkinson's disease (exacerbation of extrapyramidal disorders); urinary retention, prostatic hyperplasia with clinical symptoms (urinary retention risk), Reye's syndrome (increased risk of hepatotoxicity); pregnancy, the period of breastfeeding.
    It is not recommended to prescribe to patients in a state of psychomotor agitation a dose of the drug up to 25 mg / day, t. The activating action of Fluanxol can lead to an exacerbation of this symptomatology.

    Pregnancy and lactation:
    During pregnancy, Fluanxol should be used only if the intended benefit to the mother exceeds the potential risk to the fetus.
    In newborns whose mothers have taken antipsychotics in the last trimester 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 Fluansoxol, 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.
    Depression. Neurotic disorders. Psychosomatic disorders: Initially 1 mg daily as a single morning dose or 0.5 mg twice a day. After a week, with insufficient therapeutic effect, the dose can be increased to 2 mg per day. Daily dose of more than 2 mg and up to 3 mg should be; divided into several receptions.
    Elderly patients: the recommended daily dose is 0.5-1.5 mg.
    The response of patients to Fluanxol usually occurs within 2-3 days. If the effect of the maximum dose (3 mg per day) is not observed within a week, then the drug should be discontinued.
    Schizophrenia and schizophreniform psychosis.
    Doses of the drug should be selected individually, depending on the patient's condition. Typically, initially, small doses should be used, which then grow rapidly to optimal, depending on the clinical effect.
    The initial daily dose - 3-15 mg - is divided into 2-3 doses. If necessary, the dose can be increased to 20-30 mg per day. The maximum daily dose is 40 mg. Conventional maintenance therapy is 5-20 mg per day. The maintenance dose can be administered once a day in the morning.
    Elderly patients: lower doses are recommended.
    The duration of therapy depends on the nature of the disease. Therapy of chronic psychoses can last several years.
    Decreased kidney function:
    Fluanexol may be given in usual doses to patients with reduced renal function.
    Decreased liver function:
    Patients with reduced liver function should be given a lower dose, and if possible, monitor the concentration of flupenthixol in serum.

    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 (> 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 - dizziness, headache, tremor, dystonia; from infrequently to rarely - tardive dyskinesia, dyskinesia,
    Parkinsonism, speech disorders, convulsive disorders, late dystonia; very rarely - malignant neuroleptic syndrome.
    From the side of mental activity: often - insomnia, depression, nervousness, agitation, decreased libido; infrequently - confusion.
    From the cardiovascular system: often - tachycardia,
    palpitation; infrequently - orthostatic hypotension,lowering blood pressure, "hot flashes"; rarely - prolongation of QT interval on electrocardiogram; very rarely venous thromboembolism.
    From the blood and lymphatic system: rarely -
    thrombocytopenia, neutropenia, granulocytopenia, agranulocytosis, leukopenia, hemolytic anemia.
    From the side of the eye: often - a violation of accommodation, visual impairment, corneal and / or lens opacity, with possible visual impairment; infrequently - involuntary movement of eyeballs.
    From the side of the digestive system: very often - dry mouth; often - constipation, diarrhea, indigestion, increased salivation, vomiting; infrequently - abdominal pain, nausea, flatulence, cholestatic jaundice (more likely between 2 and 4 weeks of treatment).
    Metabolic disorders and eating disorders: often - increased appetite, weight gain; infrequent - loss of appetite; rarely - hyperglycemia, impaired glucose tolerance, hyperlipidemia.
    From the respiratory system: often - shortness of breath.
    From the endocrine system: rarely - hyperprolactinaemia,
    dysmenorrhea, diabetes mellitus, decreased potency, change in carbohydrate metabolism.
    From the urinary system: often - urinary retention,
    painful urination.
    From the skin and subcutaneous tissue: often - itching, increased sweating; infrequently - dermatitis, skin rash,
    photosensitization.
    From the musculoskeletal system: often - myalgia; infrequently -
    muscular rigidity.
    From the side of the reproductive system: infrequently - erectile dysfunction, ejaculation disorders; rarely - gynecomastia, galactorrhea, amenorrhea.
    Hepatic and hepatobiliary disorders: infrequently - change
    laboratory indicators of liver function; very rarely - jaundice.
    From the immune system: rarely - hypersensitivity,
    anaphylactic reactions.
    On the part of the body as a whole: often - weakness, asthenia.
    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, the 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 flupenthixol therapy. With persistent akathisia, benzodiazepines may be useful or propranolol.
    When taking flupentixol, the following side effects associated with the administration of other neuroleptics were also observed: in rare cases, prolongation of the QT interval, ventricular arrhythmias - fibrillation and tachycardia, sudden death and development of paroxysms of ventricular tachycardia (Torsade des Pointes).
    A sharp discontinuation of flupentixol may be accompanied by the occurrence of "cancellation" reactions. The most common symptoms: nausea, vomiting, anorexia, diarrhea, rhinorrhea, sweating, myalgia, paresthesia, insomnia, nervousness, anxiety and agitation. Patients may also experience dizziness, sensations of heat and cold and tremor. Symptoms usually begin within 1 to 4 days after withdrawal and decrease within 7-14 days.

    Overdose:
    Symptoms.
    Drowsiness, coma, motor disorders, convulsions, shock, hyperthermia / hypothermia.
    When an overdose was concomitant with taking medications that affect cardiac activity, changes were recorded on the ECG,prolongation of QT interval, development of paroxysms of ventricular tachycardia (Torsade des Pointes), cardiac arrest, ventricular arrhythmia.
    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 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:
    Fluanxol can enhance the sedative effect of alcohol, the effects of barbiturates and other CNS depressant substances.
    Fluanxol should not be administered together with guanethidine or similarly acting drugs because of the possible weakening of the antihypertensive effect of these drugs.
    Simultaneous use of neuroleptics and lithium increases the risk of neurotoxicity.
    Tricyclic antidepressants and neuroleptics mutually inhibit each other's metabolism.
    Fluanxol can reduce the effect of levodopa and the effect of adrenergic drugs.Simultaneous use with metoclopramide and piperazine increases the risk of extrapyramidal disorders.
    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. Avoid simultaneous administration of Fluanxol and the above drugs.
    Fluanxol should be administered with caution at the same time with drugs that cause electrolyte disorders (thiazide and thiazide-like diuretics) and drugs that can increase the concentration of flupenthixol in the blood plasma, because of the possible increase in the risk of prolonging the QT interval and the occurrence of life-threatening arrhythmias.

    Special instructions:
    When treating any neuroleptic, there is the possibility of developing a malignant neuroleptic syndrome (CNS). The main symptoms of CNS are hyperthermia, muscle 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, Fluanxol's administration can change the concentration of insulin and glucose in the blood, which may require correction of the doses of hypoglycemic drugs.
    If the patient has previously been treated with neuroleptics or tranquilizers with sedative action, then their administration should be discontinued gradually.
    With long-term therapy, especially the maximum daily doses, careful monitoring is necessary, periodically assessing the condition of patients to decide on the possibility of reducing the maintenance dose.
    Like other drugs belonging to the therapeutic class of neuroleptics, Fluanxol can 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 venous thromboembolism, risk factors for venous thromboembolism need to be determined and precautions taken before and during Fluanxol treatment.
    In randomized, placebo-controlled clinical trials of the use of some atypical antipsychotics in patients with dementia, there was a 3-fold increase in the risk of cerebrovascular vascular 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 with Fluanxol in patients at risk for 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 to 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. Fluanexol is not registered for the treatment of behavioral disorders in elderly patients with dementia.
    When alcohol is used against the background of treatment with flupentixol, the oppressive effect on the central nervous system may be increased.

    Effect on the ability to drive transp. cf. and fur:
    During the period of treatment it is necessary to refrain from driving motor vehicles and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

    Form release / dosage:
    Tablets coated with 0.5 mg, 1 mg, 5 mg.

    Packaging:
    0.5 mg and 1 mg: For 50 or 100 tablets in a plastic container with protection from opening 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.
    5 mg: For 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 N012625 / 01
    Date of registration:05.05.2008
    The owner of the registration certificate:H. Lundbeck A / SH. Lundbeck A / S Denmark
    Manufacturer: & nbsp
    Information update date: & nbsp21.10.2015
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