Active substanceFluphenazineFluphenazine
Similar drugsTo uncover
  • Moditen® depot
    solution w / m 
  • Moditen® depot
    solution w / m 
  • Fluphenazine
    solution w / m 
    R-PHARM, CJSC     Russia
  • Dosage form: & nbspsolution for intramuscular administration [oily]
    Composition:

    1 ml of the solution contains:

    Active substance:

    Fluphenazine decanoate 25.00 mg.

    Excipients:

    Gasoline alcohol 12.00 mg,

    Sesame oil q.s. up to 1.00 ml.

    Description:
    Transparent oily solution of a yellowish color with a faint smell of petrol alcohol.
    Pharmacotherapeutic group:Antipsychotic agent (antipsychotic)
    ATX: & nbsp

    N.05.A.B.02   Fluphenazine

    Pharmacodynamics:

    Fluphenazine is a phenothiazine antipsychotic (neuroleptic), belonging to the group of classical neuroleptics. Has a pronounced antipsychotic effect, in addition, has antiemetic effect. The main mechanism of action is related to the fact that fluphenazine blocks dopamine D2 and D1 receptors of the brain, and to a greater extent than the neuroleptics of the phenothiazine group. Like other neuroleptics, but to a lesser extent, fluphenazine also blocks serotonin 5HT2 and 5HT1 receptors, adrenergic alpha-1 receptors, histamine H1 and cholinergic muscarinic receptors.Thus, its anticholinergic and sedative effects are less pronounced compared with other classical antipsychotics. Blockade of dopamine receptors occurs in all three dopamine systems - nitrostriatnoy, mesolimbic, and tuberoinfundibular, so in addition to the development of clinical effects are also possible various undesirable phenomena such as extrapyramidal reactions, and increased secretion of prolactin.

    In the form of an oily solution has a long-term effect (release of the drug is gradual) - the effect lasts up to 1-2 weeks. and more (depending on the dose).

    Pharmacokinetics:

    Suction and distribution

    Fluphenazine Decanoate - fluphenazine ester and decanoic acid slowly hydrolyzes to release fluphenazine, which enters the systemic circulation. The drug appears in the period from 24 to 72 hours.

    Metabolism and excretion

    Fluphenazine decanoate is metabolized in the liver, excreted by the kidneys and through the intestine.

    The half-life (T1 / 2) is from 7 to 10 days and increases to 14.3 days with repeated injections. The standard injection of Moditen Depot in patients with psychosis lasts from 15 to 35 days. The equilibrium state is reached in 4-6 weeks. Fluphenazine penetrates the placental barrier.

    Indications:
    Prolonged maintenance therapy and prevention of recurrences of schizophrenia and other psychoses.
    Contraindications:
    Hypersensitivity to one of the components of the drug, as well as to other phenothiazines; obvious or suspected subcortical brain lesions, severe disorders of consciousness, severe cerebral atherosclerosis, pheochromocytoma, hepatic insufficiency, marked renal and / or heart failure, in decompensation stage; acute intoxication with drugs depressing the central nervous system (alcohol, antidepressants, antipsychotics, sedatives, anxiolytics, hypnotics and narcotic drugs); pregnancy, the period of breastfeeding, children under 12 years.
    Carefully:
    Alcoholism (increased predisposition to hepatotoxic reactions), violation of hematopoiesis, breast cancer (as a result of prolactin-induced phenothiazines, the risk of disease progression and resistance to endocrine and cytostatic drugs increases), closed-angle glaucoma, prostatic hyperplasia with clinical manifestations,moderate or mild renal and / or hepatic insufficiency, peptic ulcer of stomach and duodenum (during exacerbation); diseases accompanied by an increased risk of thromboembolic complications; Parkinson's disease (extrapyramidal effects are intensified); epilepsy, epileptic seizures in the anamnesis; myxedema; chronic diseases accompanied by respiratory failure (especially in children); Reye syndrome (increased risk of hepatotoxicity in children and adolescents); cachexia, vomiting (antiemetic effect of phenothiazines may mask vomiting associated with overdose of other drugs), elderly age.
    Dosing and Administration:

    The drug Moditen Depot is injected deep into the muscle.

    The needle and syringe must be dry.

    Not intended for courses of therapy for less than 3 months.

    The most optimal doses and frequency of application of the drug are set individually.

    The initial dose of the drug Moditen Depot: 12.5-25 mg.

    If necessary, and taking into account the tolerance, the dose is repeated or increased every 1-3 weeks.

    Supportive dose: up to 50 mg every 1-4 weeks. At a dose exceeding 50 mg, it should be increased with caution of 12.5 mg.

    The maximum single dose for adults is 100 mg.

    Elderly patients

    Elderly patients usually have a dose of 3,125-6,25 mg.

    Children 12 years and over

    The initial dose of Moditen Depot is from 6.25 mg to 18.75 mg per week. Subsequent doses and frequency of application are set individually. Usually, the interval between use of the drug is from 7 to 21 days. When the need for higher doses, the dose of the drug is increased gradually, at 6.25 mg.

    Single dose should not exceed 25 mg.

    In patients with mild or moderate renal impairment (creatinine clearance more than 30 mL / min), smaller doses of the drug (3.125 mg-6.25 mg) are used.

    Side effects:

    Classification of the incidence of adverse events (WHO):

    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 from <1/10000, including individual messages.

    In each group, unwanted effects are presented in order of decreasing severity.

    From the side of the cardiovascular system:

    -not often: tachycardia, mild arterial hypertension, unstable blood pressure;

    - often: prolongation of the interval QT and tooth;

    -very rare: arrhythmia, ventricular tachycardia, fibrillation;

    On the part of the hematopoiesis system:

    -frequency is not known: leukopenia, agranulocytosis, thrombocytopenia, eosinophilia, pancytopenia;

    From the nervous system:

    -frequently: extrapyramidal disorders (pseudoparkinsonism, dystonia, akathisia, oculogic crisis, opisthotonus, hyperreflexia), tardive dyskinesia (involuntary movements of the tongue, facial muscles, mouth, lips, trunk and extremities);

    -only: headache;

    -rarely: malignant neuroleptic syndrome (hyperthermia,

    rigidity of muscles, akinesia, lowering of blood pressure, stupor, coma, drowsiness, lethargy);

    -frequency is unknown: anxiety, excitement or vivid dreams, depressive states, increased suicidal tendencies;

    From the sense organs:

    -Often: blurred vision, glaucoma, increased intraocular pressure;

    -frequently: turbidity of the lens and cornea;

    From the respiratory system:

    - often: nasal congestion;

    -very rare: bronchial asthma;

    From the digestive system:

    -No often: nausea, loss of appetite, salivation, dryness of the oral mucosa, constipation, paralytic ileus;

    -only: cholestatic jaundice;

    From the side of the urinary system:

    -non-often: polyuria, bladder paralysis;

    - often: nocturnal enuresis, urinary incontinence;

    From the skin:

    -Often: increased sweating;

    -rarely: skin pigmentation, photosensitivity, allergic

    dermatitis, urticaria, seborrhea, erythema, eczema, exfoliative dermatitis;

    Metabolic and nutritional disorders:

    -only: increased appetite, weight gain;

    From the side of the reproductive system:

    -non-often: gynecomastia, pathological lactation, violations of libido and impotence, irregularities in the regularity of the menstrual cycle, false positive pregnancy test;

    - rarely: priapism, ejaculation disorder;

    Allergic reactions:

    -very rare: edema of the larynx, angioedema;

    Other:

    There are several reports of sudden, unpredictable and unexplained death among hospitalized patients taking phenothiazines.

    With the development of severe adverse effects, treatment should be discontinued.

    Overdose:

    Symptoms: severe extrapyramidal disorders, sedation, convulsions, impaired consciousness, up to coma accompanied by areflexia, marked decrease in blood pressure, miosis, hypothermia, urinary retention, ECG changes, cardiac rhythm disturbances.

    Treatment is symptomatic. There is no specific antidote.The patient should be under constant observation. In the case of arrhythmias: sodium bicarbonate, magnesium sulfate. Extrapyramidal symptoms can be treated with antiparkinsonian drugs. At the expressed arterial hypotension - noradrenaline; adrenaline may lead to an additional decrease in blood pressure.

    Hemodialysis and forced diuresis are ineffective.

    Interaction:

    With the simultaneous use with flufenazine alcohol, antihistamines, antidepressants, other antipsychotics, sedatives, hypnotics or narcotics, the oppressive effect on the central nervous system increases.

    Barbiturates, non-drug-induced sleeping pills, carbamazepine, griseofulvin, phenylbutazone and rifampicin increase the metabolism of phenothiazines, which leads to an increase in the depressive effect and respiratory depression. Paracetamol, chloramphenicol, disulfiram, MAO inhibitors, tricyclic antidepressants, antidepressants from the group of selective serotonin reuptake inhibitors and oral contraceptives inhibit the metabolism of phenothiazines, which increases the risk of malignant neuroleptic syndrome.

    Phenothiazines affect the metabolism of carbohydrates, which can lead to increased levels of glucose in the blood. Patients with diabetes may need to change the doses of hypoglycemic drugs.

    Fluphenazine blocks the effects of epinephrine and other sympathomimetics, and also reduces the hypotensive effect of alpha-blockers. Due to blockade of dopamine receptors fluphenazine reduces the severity of the antiparkinsonian effect of levodopa.

    Fluphenazine can reduce the threshold of convulsive alertness; so it may be necessary to increase the dose of antiepileptic drugs taken concomitantly.

    Fluphenazine can potentiate the effect of anticoagulants; therefore it is recommended to periodically monitor prothrombin time. Fluphenazine rarely causes severe arterial hypotension. If arterial hypotension does occur, intravenous norepinephrine should be administered immediately. Adrenaline can not be used, because with simultaneous use with phenothiazines, it causes an even greater reduction in blood pressure instead of its increase. This should always be taken into account, especially during surgical operations and anesthesia.

    Avoid simultaneous use of antiarrhythmic drugs, or they should be used under strict medical supervision.

    Special instructions:

    The solution for injection can not be mixed with other solutions.

    The drug Moditen Depot is not effective in treating behavioral disorders in patients with mental retardation.

    With great care, the drug should be used in patients with epilepsy, because it can reduce the threshold of convulsive readiness and potentiate the development of seizures, and cause generalized epileptic seizures.

    The drug Moditen Depot should be administered with caution to patients with cardiovascular diseases (heart failure, coronary heart disease, arrhythmias), since it can cause a decrease in blood pressure.

    The drug Moditen Depot is used with caution in patients with mild to moderate renal impairment.

    Elderly patients and patients with intellectual disabilities should receive minimal effective doses of Moditen Depot, in such patients, undesirable effects may occur more often.

    The drug Moditen Depot is used with caution in patients exposed to high temperatures or in contact with organophosphorous insecticides.

    Do not use the Moditen Depot preparation for patients undergoing scheduled surgery using high doses of anesthetics or substances depressing the central nervous system. there is a risk of developing hypotensive reactions. The drug Moditen Depot should not be used in patients with blood dyscrasias or liver function disorders, or in patients taking medications that can cause similar changes, due to the possibility of developing cholestatic jaundice. Jaundice usually occurs in the first 2-4 weeks of therapy and does not always depend on the dose of the drug or the duration of treatment.

    Caution is required when using Moditen Depot in patients with breast or breast tumors in history (studies have not confirmed any relationship between increased secretion of prolactin and breast tumors with phenothiazines).

    Against the background of using Moditen Depot, asymptomatic pneumonia is possible.

    In patients who receive long-term therapy with antipsychotics, including Moditen Depot, a severe extrapyramidal disorder may develop-tardive dyskinesia. To minimize the risk of its development, it is recommended to use the lowest effective doses. When

    the appearance of signs of tardive dyskinesia treatment should be discontinued.

    When developing extrapyramidal disorders requires the use of antiparkinsonian drugs.

    If, with the simultaneous use of Moditen Depot with an antiparkinsonian drug, therapy with antipsychotics abruptly ceases, the use of an antiparkinsonian drug should be continued for a few more weeks.

    Special information about certain components of the drug The drug Moditen Depot contains gasoline alcohol, which can cause toxic and anaphylactoid reactions in children under 3 years of age.

    Sesame oil can cause allergic reactions.

    Effect on the ability to drive transp. cf. and fur:
    The drug Moditen Depot has a pronounced effect on psychomotor reactions, and therefore, during the period of treatment should abandon the management of vehicles or work with complex technical devices,requiring increased concentration of attention and speed of psychomotor reactions.
    Form release / dosage:
    Solution for intramuscular administration [oily], 25 mg / ml.
    Packaging:

    Ampoules of dark glass 1 ml each. The ampoule has a dot that indicates the ampoule fracture line and a color coding ring. 5 ampoules are placed in a PVC / aluminum foil blister.

    1 blister together with instructions for use are placed in a pack of cardboard.

    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 the drug after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:П N012269 / 01
    Date of registration:23.02.2011 / 27.02.2015
    Expiration Date:Unlimited
    The owner of the registration certificate:KRKA, dd, Novo mesto, AOKRKA, dd, Novo mesto, AO
    Manufacturer: & nbsp
    Representation: & nbspKRKA KRKA Slovenia
    Information update date: & nbsp11.06.2018
    Illustrated instructions
      Instructions
      Up