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 solution contains active substance: fluphenazine decanoate - 25 mg and Excipients: benzyl alcohol 15 mg, sesame oil up to 1 ml.
    Description:
    Transparent oily liquid of light yellow color, can have a faint smell of benzyl alcohol.
    Pharmacotherapeutic group:Antipsychotic agent (antipsychotic)
    ATX: & nbsp

    N.05.A.B.02   Fluphenazine

    Pharmacodynamics:Antipsychotic agent (antipsychotic) long-acting; refers to the group of polyvalent neuroleptics has a pronounced antipsychotic effect, combined with some activating effect, as well as moderate sedation, has antiemetic effect. Antipsychotic action due to blockade of dopamine D2receptors of the mesolimbic and mesocortical system. Sedation (expressed moderately and observed withapplication in high doses) is due to blockade of adrenoreceptors of the reticular formation of the brainstem; antiemetic effect - blockade of dopamine D2receptors of the trigger zone of the vomiting center; hypothermic action - blockade of dopamine receptors of the hypothalamus. The effect of the drug usually manifests itself 24-72 hours after the injection, the antipsychotic effect is most pronounced in terms of 48 to 96 hours after intramuscular injection.
    Pharmacokinetics:

    Fluphenazine in the form of a high-molecular fatty acid ester and an oily solution accumulates in fat stores and is slowly released.

    After intramuscular injection, the maximum plasma concentration is reached after approximately 24 hours. Fluphenazine binds to plasma proteins more than - 90%.

    Fluphenazine passes through the blood-brain barrier, easily penetrates the placental barrier and is not removed from the body by hemodialysis.

    Fluphenazine active and is completely metabolized in the liver with the participation of cytochrome P450 enzyme system (including isozyme CYP2D6) and excreted in urine and bile. The activity of fluphenazine metabolites has not been studied.

    The half-life of fluphenazine from the blood plasma is 7-10 days.

    Indications:

    Long-term maintenance therapy of chronic forms of schizophrenia.

    Prevention of exacerbations of schizophrenia.

    Contraindications:

    Hypersensitivity to fluphenazine or other components of the drug. Severe cardiovascular diseases (decompensated chronic circulatory failure, arterial hypotension).

    Severe oppression of the CNS function and comatose states of any etiology; craniocerebral trauma, progressive systemic diseases of the brain and spinal cord.

    Dysfunction of the liver and blood system.

    Pregnancy, lactation.

    Children under 12 years.

    Carefully:
    • Alcoholism (increased predisposition to hepatotoxic reactions),
    • allergic reactions to phenothiazine derivatives in the anamnesis,
    • pathological changes in blood (violation of hematopoiesis),
    • mammary cancer,
    • angle-closure glaucoma,
    • hyperplasia of the prostate with clinical manifestations,
    • hepatic and / or renal failure,
    • Stomach ulcer and duodenal ulcer (during exacerbation);
    • diseases accompanied by an increased risk of thromboembolic complications;
    • Parkinson's disease;
    • epilepsy, convulsive fits 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
    • elderly age.
    Dosing and Administration:

    The drug Moditen® Depot is not intended for courses of therapy for less than 3 months.

    Initial dose: for most patients, an initial dose of 12.5 to 25 mg (0.5-1 mL) is recommended. Subsequent doses and intervals between administrations are determined depending on the response to treatment.

    The initial dose to patients who have not previously been treated with phenothiazine derivatives should be selected by the administration of fluphenazine of rapid action (fluphenazine hydrochloride). Supportive therapy

    One injection allows you to control the symptoms of schizophrenia for 4 weeks. During maintenance therapy, the effect of a single dose in some patients persists for up to 6 weeks. The dose of Moditen Depot should not exceed 100 mg. If more than 50 mg of the drug is required, each subsequent dose should be increased with caution no more than 12.5 mg.

    Patients with severe agitation

    Treatment should be started with a rapid action fluphenazine, such as fluphenazine hydrochloride for injection. After the acute symptoms subsided, 25 mg (1 ml) of fluphenazine decanoate solution for intramuscular injection can be used.

    Subsequent doses, if necessary, are adjusted.

    Patients with an increased risk of complications

    If there is a certain hypersensitivity to phenothiazine derivatives or disorders predisposing to adverse reactions, treatment should be started with fluphenazine hydrochloride inside or parenterally. After evaluating the pharmacological effect and determining the optimal dose, fluphenazine decanoate may be administered for intramuscular administration at an equivalent dose.

    The subsequent correction of the dose is carried out depending on the response to treatment.

    There is no single scheme for the transition from fluphenazine of rapid action to the administration of a solution of fluphenazine decanoate. However, it is known that a dose of 20 mg per day of fluphenazine hydrochloride is equivalent to one injection of 1 ml (25 mg) of a flufenazine decanoate solution every three weeks. Most elderly patients require smaller doses - from 1/4 to 1/3 of the dose given to young patients, and monitoring the response to treatment. If necessary, the dose can be gradually increased.

    Side effects:

    From the side of the central nervous system:

    extrapyramidal disorders such as extrapyramidal syndrome, dystonia, dyskinesia, akathisia, oculogyric crises, opisthotonos, and hyperreflexia, tardive dyskinesia (syndrome manifested by involuntary choreoathetoid movements of the tongue, the face muscle of the mouth, lips or jaws (e.g., protruding tongue inflating cheeks Extruding lips, chewing movements) muscles of the trunk and extremities).

    Other neurological disorders:

    neuroleptic malignant syndrome (ZNE) from potentially lethal (hyperpyrexia, muscle rigidity, altered mental status, autonomic disorders - frequency oscillation, pulse or blood pressure, tachycardia, increased sweating, irregular heartbeat), ZNE may also be accompanied by the development of leukemia, fever, increased activity of creatine phosphokinase (CK), impaired liver function and acute heart failure; drowsiness, confusion, changes in the encephalogram and protein content in the cerebrospinal fluid, cerebral edema.

    From the side of the autonomic nervous system:

    Orthostatic hypotension, fluctuations in blood pressure, nausea, loss of appetite, drooling, polyuria, sweating, dryness in pryj headache, constipation (usually after a dose reduction or drug withdrawal), hypotension.

    There are also visual disturbances, glaucoma, atony of the bladder, intestinal obstruction, tachycardia, nasal congestion.

    From the side of the cardiovascular system:

    Elongation of the QT interval, ventricular arrhythmias, including ventricular fibrillation, ventricular tachycardia, sudden death, cardiac arrest.

    Metabolic and endocrine disorders:

    changes in body weight, peripheral edema, hyponatremia, syndrome of impaired secretion of antidiuretic hormone, pathological lactation, gynecomastia, menstrual irregularity, false positive pregnancy test, impotence in men, changes in libido in women.

    Allergic reactions:

    itching, erythema, urticaria, seborrhea, photosensitivity, eczema and exfoliative dermatitis, anaphylactic reactions, bronchospasm, angioedema, laryngeal edema.

    On the part of the blood system:

    leukopenia, agranulocytosis, thrombocytopenic and non-thrombocytopenic purpura, eosinophilia and pancytopenia.

    On the part of the liver function:

    cholestatic jaundice, especially in the first months of therapy, changes in laboratory, liver function indicators and clinical signs of hepatitis.

    Other:

    convulsive attacks, with prolonged treatment - fever, vomiting, lupus-like syndrome, ECG changes, as well as skin pigmentation, clouding of the lens and cornea, impaired renal function, pigmentary - retinopathy, development of a closed-angle glaucoma, irreversible dyskinesia, asymptomatic form of pneumonia, venous thromboembolism , including pulmonary embolism and deep vein thrombosis.

    Overdose:
    Expressed extrapyramidal disorders, hypotension, excessive, sedative effect, oppression, consciousness up to the dot com with areflexia. In such cases, it is necessary to cancel the medicine and begin supporting symptomatic treatment.
    With the development of severe hypotension, immediate intravenous administration of vasoconstrictive drugs is necessary. Epinephrine (epinephrine) should not be used, because with simultaneous admission with. derivatives of phenothiazine. there is a perverted reaction (an even greater decrease in blood pressure). With the development of severe extrapyramidal disorders, antiparkinsonian drugs are prescribed for several weeks. Antiparkinsonics should be phased out gradually in order to avoid recurrence of extrapyramidal disorders.
    Hemodialysis, peritoneal dialysis, exchange transfusions and forced diuresis in case of poisoning with Moditen® Depot are ineffective.
    Interaction:

    Against the background of the use of fluphenazine, the effect of alcohol, drugs, depressing central nervous system (hypnotics, sedatives) and strong analgesics is enhanced. Simultaneous use with narcotic analgesics can cause hypotension, oppression of the central nervous system and respiration.

    Tricyclic antidepressants: phenothiazine derivatives disrupt the metabolism of tricyclic antidepressants. Serum concentrations of both tricyclic antidepressants and phenothiazines increase. Sedation and m-cholinoblocking effects may be prolonged or prolonged, as well as the arrhythmogenic effect of tricyclic antidepressants.

    Lithium preparations with simultaneous application with fluphenazine may increase neurotoxicity.

    Angiotensin-converting enzyme (ACE) inhibitors thiazide diuretics: it is possible to intensify the hypotensive effect.

    Other antihypertensives: the antihypertensive effect of guanethidine, clonidine and possibly other anti-adrenergic agents may be reduced. Clonidine can reduce the antipsychotic effect of phenothiazines.

    Beta-blockers: can increase concentrations of beta-adrenoblockers and derivatives of phenathiazine in blood plasma.

    With the simultaneous use of beta-adrenoblockers and phenothiazine derivatives, a reduction in the dose of drugs of both groups is recommended.

    Metrizamide can cause convulsive seizures amid the use of fluphenazine. Recommended to cancel fluphenazine 48 hours before myelography and do not prescribe it at least 24 hours after myelography.

    Epinephrine and other adrenomimetics: derivatives of phenothiazine are their pharmacological antagonists, as a result of which development of severe hypotension is possible.

    Levodopa: phenothiazine derivatives can reduce the antiparkinsonian effect of the drug.

    M-holinoblokatory: when fluphenazine is administered in combination with m-holinoblokatorami it is possible to strengthen the blocking of cholinergic receptors, especially in the elderly. M-cholinoblocking effects are potentiated or prolonged.

    When using the drug Moditen Depot simultaneously with m-holinoblokatorami careful monitoring and selection of doses of drugs is necessary.

    Anticonvulsants: fluphenazine can reduce their anticonvulsant effect.

    Hypoglycemic agents: phenothiazine derivatives cause decompensation of diabetes mellitus.

    Cimetidine can reduce the concentration of phenothiazine derivatives in the blood plasma.

    Antacids / Antidiarrheal agents may interfere with the absorption of fluphenazine.

    Amphetamy / Anorexigenic the agents are pharmacological antagonists of fluphenazine.

    Substrates or inhibitors of the isoenzyme CYP2D6: fluphenazine is metabolized by the CYP2D6 isoenzyme and is also an inhibitor of this isoenzyme. Consequently, plasma concentrations and effects of fluphenazine may increase with the administration of such drugs, resulting in cardiotoxicity, adverse reactions caused by m-holin-blocking action, or orthostatic hypotension.

    Special instructions:

    In connection with the possible cross-sensitivity, caution should be given to the Moditen® Depot preparation in patients with allergic reactions to phenothiazine derivatives in the anamnesis.

    With the development of cholestatic jaundice as an adverse reaction, treatment with Moditen® Depot should be discontinued.

    When performing surgical operations, patients who take high doses of phenothiazine derivatives may experience a sharp decrease in blood pressure.

    It may be necessary to reduce the doses of anesthetics or antipsychotics in some patients when treated with the Moditene® Depot; Potentiation of the effect of m-holinoblockers is possible, since fluphenazine has m-anticholinergic action.

    Caution is advised to prescribe the Moditen® Depot in very hot weather or poisoning with phosphoric insecticides, patients with seizures in the anamnesis (as cases of large epileptic seizures are described in the course of treatment with fluphenazine), as well as patients with mitral valve insufficiency or other cardiovascular disorders, vascular system or with pheochromocytoma.

    It is necessary to prescribe with caution the drug for breast cancer, tk. as a result of derivatives induced phenothiazine prolactin secretion increases the risk of disease progression and resistance to treatment with endocrine and cytotoxic drugs.

    Cases of development, venous thromboembolism were noted with the use of antipsychotic medications. Since patients who take antipsychotic medications often have risk factors for venous thromboembolism, it is necessary to assess these factors before and during treatment and take appropriate preventive measures.

    When prescribing to patients with Parkinson's disease, extrapyramidal effects may increase.

    Emerging as side effects, extrapyramidal symptoms are usually reversible, but can be persistent. The likelihood and severity of such unwanted adverse reactions depends more on individual sensitivity than on other factors, but the magnitude of the dose and age of the patient are important. The patient should be warned in advance about such manifestations and their reversibility.Usually, to eliminate these undesirable phenomena, it is sufficient to prescribe m-holinoblokatorov or antiparkinsonic drugs and / or reduce the dose of the drug.

    Late dyskinesia

    The severity of this syndrome and the resulting worsening of the condition can vary considerably in different patients. Late dyskinesia is manifested either during treatment, with a lower dose, or after discontinuation of therapy. Early detection of tardive dyskinesia is very important. For the detection of this syndrome, the initial stage is recommended / periodic dose reduction, neuroleptic (if possible on the condition of the patient) and patient monitoring during this period. This approach is extremely important; because treatment with antipsychotics can mask the manifestations of tardive dyskinesia.

    Malignant neuroleptic syndrome

    With the development of this adverse reaction should immediately stop taking neuroleptics and other medications that do not affect the maintenance of vital functions, as well as intensive symptomatic treatment, continuous monitoring of vital functions, and therapy of concomitant diseases.

    Disorders of cerebral circulation

    Approximately 3-fold increase in the risk of developing cerebrovascular disorders was observed with the administration of some atypical neuroleptics in patients with dementia in the anamnesis. There was an increase in the mortality of elderly patients with a history of dementia during antipsychotic medications. The degree of risk and the causes of this phenomenon are unknown.

    The cause of this phenomenon is unknown, however, the increased risk of developing cerebral circulation disorders in other populations of patients or with the administration of other neuroleptics can not be ruled out. In this regard, care must be taken when taking Moditen® Depot with patients at risk of developing cerebrovascular accident.

    Hypotension against treatment with fluphenazine is rare. At the same time, in patients with pheochromocytoma, cerebrovascular, renal and severe heart failure (for example, in patients with mitral valve insufficiency), hypotension with Moditen® Depot is more frequent; careful monitoring is necessary for these patients. With the development of severe hypotension, rapid intravenous administration of vasoconstrictive drugs is necessary.Is best suited for that norepinephrine for injections. Epinephrine It should not be used because phenothiazine derivatives distort the reaction to epinephrine, resulting in an even greater reduction in blood pressure.

    With the development of diseases of the mucous membrane of the mouth, gums or throat or. infection of the upper respiratory tract in combination. with a change in the number of leukocytes confirming the inhibition of hematopoiesis, therapy with Moditen® Depot should be canceled, and the necessary medical measures are immediately started.

    Patients with seizures in the anamnesis should be cautious appoint phenothiazine derivatives, including the drug Moditen® Depot.

    It should be taken into account that the antiemetic effect of phenothiazine derivatives (including Moditen® Depot) can mask vomiting associated with overdose of other drugs.

    Abrupt withdrawal of the drug: mainly the reception of phenothiazine derivatives. does not cause psychic dependence, however, cases of gastritis, nausea and vomiting, and dizziness with a sharp abolition of high doses of phenothiazine were noted.These symptoms decreased with subsequent withdrawal after taking antiparkinsonian drugs for several weeks.

    The drug contains sesame oil, which in rare cases can cause severe allergic reactions.

    Gasoline alcohol contained in the product can cause severe toxic and anaphylactoid reactions in children older than 12 years.

    The intake of alcohol during the treatment of drugs is prohibited.

    Do not store medication in the refrigerator, as it will lead to the deposition of triglycerides belonging to the sesame oil. When the sludge drug should be heated to 37 ° C, the precipitate was dissolved without loss of activity of the active substance.

    Effect on the ability to drive transp. cf. and fur:
    The drug has a strong effect on the patient's psychomotor reactions, so during the treatment period it is forbidden to work with mechanisms or drive a car.
    Form release / dosage:
    Solution for intramuscular administration oily 25 mg / ml.
    Packaging:1 ml per ampoule of clear, colorless glass. 5 ampoules per plastic tray. 1 plastic tray together with instructions for use in a cardboard box.
    Storage conditions:

    At a temperature of 15 to 25 ° C in a dark place.

    KEEP OUT OF THE REACH OF CHILDREN.

    Shelf life:

    2 years.

    Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:P N 015939/01
    Date of registration:18.09.2009
    Expiration Date:Unlimited
    Date of cancellation:2017-01-13
    The owner of the registration certificate:Bristol-Myers SquibbBristol-Myers Squibb France
    Manufacturer: & nbsp
    Representation: & nbspBRISTOL-Majers SKVIBB, LLCBRISTOL-Majers SKVIBB, LLCRussia
    Information update date: & nbsp11.06.2018
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