Active substanceTrifluoperazineTrifluoperazine
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    DALHIMFARM, OJSC     Russia
  • Triftazine
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    DALHIMFARM, OJSC     Russia
  • Triftazin-Darnitsa
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  • Dosage form: & nbspcoated tablets
    Composition:

    In 1 tablet, coated with a coating, contains:

    Active substance: trifluoperazine hydrochloride in terms of trifluoperazine - 5 mg;

    Excipients: sucrose, starch potato, silicon dioxide colloid (aerosil), magnesium stearate, calcium karibbon (precipitated), gelatin, andnidikarmin, beeswax, paraffin liquid (Vaseline oil), talc, glycerol (glycerol).

    Description:

    Round tablets of biconvex form, covered with a shell, blue or blue with a green tint of color. Marble is allowed on the surface of the tablets. Two layers are visible on the cross-section.

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

    N.05.A.B.06   Trifluoperazine

    Pharmacodynamics:

    Antipsychotic agent (neuroleptic), piperazine derivative of phenothiazine.has also sedative, antiemetic, anti-catabolic, cataleptic, hypotensive, hypothermic and weak m-cholinoblocking action. Antipsychotic action due to blockade D2dopamine receptors of the mesolimbic and mesocortical system. Has a blocking effect on alpha-adrenoreceptors and inhibits the release of hormones of the hypothalamus and the pituitary, with the blockade of dopamine receptors leading to an increase in pituitary prolactin release.

    Sedative action is due to blockade of adrenoreceptors of the reticular formation of the brain stem. Antiemetic action - blockade of peripheral and central (chemoreceptor trigger zone of the vomiting center of the cerebellum) D2-dopamine receptors, as well as blockade of the endings of the vagus nerve in the gastro-intestinal tract. Hypothermic action - blockade of dopamine receptors of the hypothalamus.

    Trifluoperazine is structurally similar to chlorpromazine, has a higher activity, better It is tolerated, its use does not develop tolerance for antipsychotic action longer.Sedative action and influence on the autonomic nervous system is less pronounced than in other phenothiazines, extrapyramidal and antiemetic is stronger.

    Pharmacokinetics:

    The degree of absorption of trifluoperazine is high, bioavailability is 35% (it has the effect of "first passage" through the liver). The connection with plasma proteins reaches 95 - 99 %. The maximum concentration in the blood is reached after 2-4 hours after ingestion. Passes through the blood-brain barrier, through the placenta and into breast milk. Intensively metabolized in the liver with the formation of pharmacologically inactive metabolites. The half-life is 15-30 hours Excreted mainly by the kidneys (in the form of metabolites) and with bile.

    When dialysis is performed - weakly dialyzed due to a high degree of binding to whitekami.

    Indications:Psychoses, schizophrenia, hallucinatory and affective-delusional state, psychomotor agitation of various etiologies. Vomiting of the central genesis.
    Contraindications:

    Increased individual sensitivity to the components of the drug; severe cardiovascular diseases (decompensated heart failure, severe arterial hypotension); expressed inhibition of central nervous function systems and coma of any etiology; brain injuries, progressive diseases of the brain and spinal cord. Pregnancyь, lactation period, children's movementgt;

    Carefully:

    Alcoholism (increased predisposition to hepatotoxic reactions), angina pectoris, valvular heart disease, limiting the amount of minute circulation of blood (possibly the development of severe arterial hypertension); pathological changes in blood (hemopoiesis), breast cancer (as a result of phenothiazine-induced prolactin secretion, the potential risk of disease progression and treatment resistance increases endocrine and cytostatic drugs), angle-closure glaucoma, prostatic hyperplasia with clinical manifestations, hepatic and / or renal insufficiency, peptic ulcer of the stomach and duodenum in the period of exacerbation; diseases accompanied by an increased risk of thromboembolic complications; Parkinson's disease (extrapyramidal effects are intensified); epilepsy; myxedema; chronic diseases, accompanied by a violation of breathing (especially in children); Reye syndrome (increased risk of geponotoxicity in children and adolescents); cachexia, vomiting (antiemetic effect of phenothiazines may mask vomiting associated with overdose of other drugs); elderly age; exposure to high temperatures.

    Pregnancy and lactation:The drug is contraindicated during pregnancy and lactation. If it is necessary to use lactation, breastfeeding should be discontinued.
    Dosing and Administration:

    Is taken orally after a meal. Doses are selected individually according to the severity of the condition. When the maximum therapeutic effect is achieved, the dose is gradually reduced to a maintenance dose.

    For mental disorders, usually prescribed 5 mg twice a day, then within 2-3 weeks the dose is gradually increased to 15-20 mg per day divided by 2-3 doses. It takes 2-3 weeks to obtain the desired therapeutic effect and improve the patient's condition. The maximum daily dose is 40 mg.

    At the first stage of dose selection in elderly, emaciated, weakened patients and children, it is advisable to use dosage forms with a lower dosage of trifluoperazine.Elderly, as well as debilitated and debilitated patients, a smaller initial dose is required, which is gradually increased if necessary, taking into account the tolerance.

    As an antiemetic, the drug is prescribed to adults at 5 mg / day.
    Side effects:

    From the central nervous system: drowsiness, dizziness, insomnia (at the beginning of treatment), dry mouth, with prolonged use of high doses - akathisia, dystonic extrapyramidal disorders (spasms of the muscles of the face, neck and back, tick-like movements or twitches, bending movements of the trunk, inability to move eyes, weakness in hands and feet), parkinsonism (difficulty in speaking and swallowing, loss of balance control, masklike face shuffling Pgait, stiffness of hands and feet, trembling of hands and fingers), tardive dyskinesia (smacking lips, puffing cheeks, fast or vermiform dlanguage movements, uncontrolled chewing movements, uncontrolled movements of hands and feet). Dyskinesias are subcutaneously injected with 2 ml of 20% caffeine sodium solution and 1 ml 0.1% atropine solution),Neuroleptic malignant syndrome (convulsions, shortness or rapid breathing, palpitations or irregular heartbeats, hyperthermia, unstable arteriesexcessive pressure, sweating, utcontrol of urination, pronounced muscle regurgitation, unusually pale skin, unusual fatigue and weakness), phenomena of mental indeterminacy, belated reaction to external irritations and other changes in the psyche, in single cases - convulsions (as correctors use antiparkinsonian means - tropacin, cyclodol and other); paradoxical reactions - hallucinations, psychomotor agitation.

    From the sense organs: blurred vision, paresis of accommodation (at the beginning of treatment), with prolonged use - retinopathy, clouding of the lens and cornea.

    From the digestive system: loss of appetite, anorexia, constipation (at the beginning of treatment), bulimia, nausea, vomiting, diarrhea, gastralgia, rarely - cholestatic jaundice, hepatitis, intestinal paresis.

    From the genitourinary system: retention of urine, decreased potency and libido, frigidity (at the beginning of treatment), ejaculation disorders, priapism, oliguria.

    From the endocrine system: hypo- or hyperglycemia, glucosuria, amenorrhea, hyperprolactinemia, dysmenorrhea, galactorrhea, swelling or pain in the mammary glands, gynecomastia, weight gain.

    Co cardiovascular system: tachycardia, frequent seizures stenocardia (against the background of increased physical activity), at the beginning of treatment - lowering blood pressure (including orthostatic hypotension) especially in elderly patients and people with alcoholism; heart rhythm disturbances, changes in the electrocardiogram (lengthening of the interval QT, decrease or inversion of the T wave).

    Allergic reactions: cutaneous rash, hives, angioedema edema, exfoliative dermatitis.

    Laboratory indicators: leukopenia, thrombocytopenia, anemia, agranulocytosis (on days 4-10), pancytopenia, eosinophilia (less often than other phenothiazines), hemolytic anemia, false positive tests for phenylketonuria, false positive pregnancy tests.

    Other: photosensitization, skin and conjunctival staining, discoloration of sclera and cornea, decreased tolerance of high temperatures (up to the developmentheat stroke - hot dry skin, loss of sweating ability, muscle weakness, confusion), myasthenia gravis.

    When taking neuroleptics phenotiazinovogo number of cases of sudden death (including possibly caused by cardiac causes).

    Overdose:

    Symptoms: malignant neuroleptic syndrome (convulsions, respiratory depression, arrhythmias, hyperthermia, unstable blood pressure, sweating, loss of control of urination, pronounced muscle regurgitation, unusually pale skin, confusion, etc.), collapse, hypothermia, coma, toxic hepatitis.

    Treatment: simtomatic. Neurological complications usually decrease with a decrease in dose, as well as the appointment of cyclodol, with the development of neuroleptic depression, antidepressants and psychostimulants are used. Dyskinesias are stopped by caffeine (2 ml of 20% solution subcutaneously) and atropine (1 ml of 0.1% solution). When arrhythmia is administered intravenously phenytoin (9-11 mg / kg), heart failure - cardiac glycosides, with a marked decrease in blood pressure - intravenously injected liquids or vasopressor agents (norepinephrine, phenylephrine), the use of alpha and beta-adrenomimetics should be avoided, such as epinephrine, since it is possible a paradoxical reduction in blood pressure due to blockade of alpha-adrenergic receptors with trifluoperazine. With cramps apply diazepam, the appointment of barbiturates should be avoided due to the possible inhibition of the central nervous system and respiration. Dialysis is ineffective.

    Control of the function of the cardiovascular system, respiration, measurement of body temperature and observation of a psychiatrist is carried out for at least 5 days.

    Interaction:

    With simultaneous applications with drugs that depress the central nervous system (drugs for anesthesia, opioid analgesics, barbiturates, anxiolytics, ethanol and ethanol containing drugs, etc.), it is possible to increase the depression of the central nervous system and respiratory depression. When used simultaneously with tricyclic antidepressants, maprotiline, monoamine oxidase inhibitors, lengthening and strengthening of sedative and anticholinergic effects are possible, increased risk of malignant neuroleptic syndrome; with anticonvulsants (including barbiturates) - it is possiblelowering convulsive threshold; with drugs for the treatment of hyperthyroidism - increases the risk of agranulocytosis; with drugs that cause extrapyramidal reactions - it is possible to increase the frequency and severity of extrapyramidal disorders; with antihypertensive drugs - orthostatic hypotension is possible. When combined with beta-adrenoblockers, the hypotensive effect increases, the risk of developing irreversible retinopathy, arrhythmia and tardive dyskinesia increases; when combined with diuretics - increased hyponatremia; when combined with prochlorperazine - a prolonged loss of consciousness is possible. Trifluoperazine enhances the effect of atropine, reduces the effect of indirect anticoagulants.

    With simultaneous use with lithium drugs, absorption in the gastrointestinal tract decreases, the rate of lithium excretion by the kidneys increases, and the severity of extrapyramidal disorders increases, and early signs of lithium intoxication (nausea and vomiting) may be masked by the antiemetic effect of trifluoperazine.

    Simultaneous administration of alpha and beta-adrenostimulants (epinephrine) and sympathomimetics (ephedrine) can lead to a paradoxical decrease in blood pressure. Trifluoperazine weaken the effects of levodopa and phenamine, the latter reduce the antipsychotic activity of trifluoperazine. Aluminum and magnesium-containing antacids or antidiarrheal adsorbents reduce the absorption of trifluoperazine, amitriptyline, amantadine, antihistamines and other drugs with anticholinergic effect increase its anticholinergic activity. Trifluoperazine reduces the effect of funds that reduce appetite (with the exception of fenfluramine); reduces the effectiveness of the emetic action of apomorphine, enhancing its inhibitory effect on the central nervous system; increases the concentration in the plasma of prolactan and prevents the action of bromocriptine. Probucol, astemizole, cisaride, disopyramide, erythromycin, pimozide, procainamide, quinidine promote additional lengthening of the interval QT, which increases the risk of developing ventricular tachycardia.

    When concomitant administration with propranolol fenotiazidov marked increase in the concentration of both drugs.

    Special instructions:

    ATabout During treatment it is necessary to carry out regular monitoring of the function of the cardiovascular system, liver, kidneys and hematopoiesis system. During the treatment period, alcohol is not allowed. Avoid exposure to high temperatures (possibly a violation of heat regulation).

    In the conduct of myelography, the drug should be discontinued no less than 48 hours before the procedure and do not resume treatment within the next 24 hours. Do not use the drug to prevent vomiting before myelography.

    The antiemetic effect of the drug may mask the signs and symptoms of toxicity caused by overdose of other drugs, and also make it difficult to diagnose diseases such as intestinal obstruction, brain tumor, Reye's syndrome. If the symptoms of extrapyramidal disorders develop, depending on the degree of their severity, lower the dose of the drug or cancel therapy, and then consider resuming treatment, perhaps in smaller doses.

    When signs of late dyskinesia, neuroleptic malignant syndrome, treatment should be discontinued.
    Effect on the ability to drive transp. cf. and fur:

    During the period of treatment with the drug, the patient should refrain from driving and performing work requiring increased attention, rapidity of mental and motor reactions.

    Form release / dosage:

    Coated tablets, 5 mg.

    Packaging:

    For 10 or 50 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil for packaging.

    1 circuit cell pack of 50 tablets or 5 contiguous cell packs for -40-tablets, along with instructions for medical use, are placed in a pack of cardboard.

    It is allowed, for hospitals, to pack 100 or 300 contour packs of 50 tablets each, or 450 contour packs of 10 tablets each, without attachment to the pack, together with the corresponding number of instructions for medical use.

    Storage conditions:

    List B. In a dry, the dark place at a temperature of 15 ° C to 25 ° C. Keep out of the reach of children.

    Shelf life:

    2 years. Do not use the product after the expiration date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:П N015130 / 01
    Date of registration:14.08.2008
    The owner of the registration certificate:HEALTH PHARMACEUTICAL COMPANY, LTD. HEALTH PHARMACEUTICAL COMPANY, LTD. Ukraine
    Manufacturer: & nbsp
    Information update date: & nbsp18.10.2015
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