Active substanceTrifluoperazineTrifluoperazine
Similar drugsTo uncover
  • Triftazine
    pills inwards 
  • Triftazine
    solution w / m 
  • Triftazine
    pills inwards 
    DALHIMFARM, OJSC     Russia
  • Triftazine
    solution w / m 
    DALHIMFARM, OJSC     Russia
  • Triftazin-Darnitsa
    solution w / m 
  • Dosage form: & nbspsolution for intramuscular injection
    Composition:

    Active substance:

    Trifluoperazina dihydrochloride (trifazalin hydrochloride) in terms of 100 % substance 2.0 mg

    Excipients:

    Sodium citrate pentasecvvydrate (sodium citrate for injection) in terms of sodium citrate - 1.0 mg,

    Water for injection - up to 1 ml.

    Description:transparent colorless or slightly colored liquid
    Pharmacotherapeutic group:antipsychotic agent (antipsychotic)
    ATX: & nbsp

    N.05.A.B.06   Trifluoperazine

    Pharmacodynamics:

    Antipsychotic agent (neuroleptic), piperazine derivative of phenothiazine.

    Possesses thetothe same sedative, antiemetic, anti-catabolic, cataleptic, hypotensive, hypothermic and m-holinoblocking weak.

    Antipsychotic action due to blockade D2-dopamine receptors of the mesolimbic and mesocortical system,has a blocking effect on alpha-adrenergic receptors and inhibits the release of hormones of the hypothalamus and pituitary gland (with blockade of dopamine receptors prolactin secretion by the pituitary gland increases). Blockade of alpha-adrenergic receptors of blood vessels determines its hypotensive effect.

    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 gastrointestinal tract.

    Hypothermic action - blockade of dopamine receptors of the hypothalamus.

    Structurally similar to chlorpromazine, has a higher activity, better tolerated. Sedative action and influence on the autonomic nervous system is less pronounced than in other phenothiazine derivatives, extrapyramidal and antiemetic effects are stronger.

    Pharmacokinetics:

    Absorption is high. The connection with plasma proteins is 95%. The time required to reach the maximum concentration with intramuscular injection is 1-2 hours.Penetrates through the blood-brain barrier, the placenta and into breast milk. Intensively metabolized in the liver, metabolites are pharmacologically inactive. The half-life is 15-30 hours.

    It is excreted mainly by the kidneys (in the form of metabolites) and with bile. During hemodialysis dialysis is poorly (high bond with plasma proteins).

    Indications:

    Psychoses, schizophrenia, hallucinatory and affective-delusional state, psychomotor agitation, vomiting (central genesis).

    Contraindications:

    Hypersensitivity to the components of the drug (including other phenothiazine derivatives), severe cardiovascular diseases (decompensated chronic heart failure, arterial hypotension), severe inhibition of the central nervous system (including drugs) and coma condition of any etiology, craniocerebral trauma, progressive diseases of the brain and spinal cord, oppression of bone marrow hematopoiesis, severe hepatic insufficiency, children's age (up to 6 years).

    Carefully:Alcoholism, (increased predisposition to hepatotoxic reactions), angina pectoris,Valvular heart lesions that limit the amount of minute blood volume (possibly the development of severe arterial hypotension), pathological changes in blood (hemopoiesis), breast cancer (as a result of induced phenotypesthiazines of prolactin secretion increase the potential risk of disease progression and resistance to endocrine and cytostatic drugs), closed-angle glaucoma, prostatic hyperplasia with clinical manifestations, hepatic and / or renal insufficiency, peptic ulcer of stomach and duodenal ulcer during exacerbation; diseases accompanied by an increased risk of thromboembolic complications; Parkinson's disease (extrapyramidal effects are intensified); epilepsy; myxedema; chronic diseases accompanied by respiratory failure (especially in children); Reye syndrome (increased risk of manifestations of hepatotoxicity in children and adolescents); cachexia, vomiting (antiemetic effect of phenothiazines may mask vomiting associated with overdose of other medicines), elderly age.When taking the drug should avoid exposure to high temperatures (possibly a violation of thermoregulation).

    Malignant neuroleptic syndrome can occur at any time during treatment with neuroleptics and lead to death.

    Pregnancy and lactation:It is not recommended to administer the drug during pregnancy and during breastfeeding.
    Dosing and Administration:

    Intramuscularly.

    1 to 2 mg if necessary every 4 to 6 hours, the maximum dose is 10 mg / day.

    Elderly, as well as emaciated and debilitated patients, the initial dose is reduced by 2 times.

    Children older than 6 years - 1 mg 1 - 2 times a day.

    Side effects:From the nervous system: drowsiness, dizziness, insomnia (at the beginning of treatment), with prolonged use in high doses (0.5-1.5 g / day) - akathisia, dystonic extrapyramidal reactions (spasms of the muscles of the face, neck and back, tick-like movements or twitches, the movement of the trunk, the inability to move the eyes, weakness in the arms and legs), parkinsonism (difficulty in speaking and swallowing, loss of balance control, masklike face, shuffling gait, stiffness of hands and feet,trembling of hands and fingers), tardive dyskinesia (smacking lips and lips, inflating cheeks, fast or wormlike movements of the tongue, uncontrolled chewing movements, uncontrolled movements of hands and feet), malignant neuroleptics(convulsions, difficulty or rapid breathing, palpitations or irregular heartbeats, pulse, hyperthermia, unstable blood pressure, increased sweating, loss of control of urination, severe muscle stiffness, unusually pale skin, excessive fatigue and weakness), psychic indifference, late reaction on external irritations and other changes in the psyche, convulsions.

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

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

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

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

    From the hematopoiesis: oppression of bone marrow hematopoiesis (thrombocytopenia, leukopenia, agranulocytosis (for 4-10 weeks of treatment), pancytopenia, eosinophilia), hemolytic anemia.

    Laboratory indicators: false positive tests for pregnancy and phenylketonuria.

    From the cardiovascular system: tachycardia, lowering of blood pressure (including orthostatic hypotension) especially in elderly patients and people with alcoholism (at the beginning of treatment), heart rhythm disturbances, lengthening of the interval Q-T, decline or inversion of the T wave, an increase in angina attacks (against the background of increased physical activity).

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

    Other: staining stains from blue-violet to brown, photosensitivity, discoloration of sclera and cornea,decrease in the tolerance of high temperatures (up to the development of heat stroke - hot dry skin, loss of sweating ability, confusion), myasthenia gravis.

    Local reactions: may occur infiltrates, when liquid forms on the skin - contact dermatitis.
    When taking neuroleptics phenotiazinovogo number of cases of sudden death (including possibly caused by cardiac causes)
    Overdose:

    Symptoms: areflexia or hyperreflexia, blurred vision, cardiotoxic (arrhythmia, heart failure, lowering of arterial pressure, shock, tachycardia, change in the complex QRS, ventricular fibrillation, cardiac arrest), neurotoxic effects, including agitation, confusion, convulsions, disorientation, drowsiness, stupor or coma; mydriasis, dry mouth, hyperpyrexia or hypothermia, muscle stiffness, vomiting, pulmonary edema, or respiratory depression.

    Treatment: symptomatic: with arrhythmia - intravenously injected phenytoin 9-11 mg / kg, heart failure - cardiac glycosides, with a marked decrease in blood pressure - intravenous fluid or vasopressor drugs such as noreleinine, phenylephrine, (avoid the appointment of alpha and beta-adrenomimetics, such as epinephrine, since it is possible a paradoxical reduction in blood pressure, due to blockade of alpha-adrenoreceptors, trifluoperazine), with convulsions - diazepam (avoid the appointment of barbiturates, due to the subsequent depression of the central nervous system and respiratory depression), Parkinsonism diphenyltropine, diphenhydramine. Control function of the cardiovascular system for at least 5 days, the functions of the central nervous system, respiration; body temperature measurement, psychiatrist consultation. Dialysis is ineffective.

    Interaction:

    Weaken the effects of levodopa and phenamine derivatives, the latter reduce the antipsychotic activity of trifluoperazine. Strengthens the action of ethanol and other drugs, drugs that depress the central nervous system (funds for general anesthesia, narcotic analgesics, opioids, barbiturates), as well as atropine.

    At simultaneous reception with antiepileptic medicines (including barbiturates) trifluoperazine reduces their effect (reduces the epileptic threshold).

    Reduces the effect of anorectic drugs (with the exception of fenfluramine).

    Reduces the effectiveness of the emetic action of apomorphine, strengthens its inhibitory effect on the central nervous system.

    Increases the concentration in the plasma of prolactin and prevents the action of bromocriptine.

    When coupled with a tricyclic antidepressant, maprotiline, inhibitors of monoamine oxidase may elongation and increased sedation and anticholinergic effects, thiazide diuretics - strengthening hyponatraemia with lithium drugs - increase lithium rate of excretion by the kidneys, increasing the severity of extrapyramidal disorders, early signs of lithium toxicity (nausea and vomiting ) may be masked by the antiemetic effect of trifluoperazine.

    In combination with beta-blockers enhances the hypotensive effect, it increases the risk of irreversible retinopathy, arrhythmias and tardive dyskinesia. Reduces the effect of indirect anticoagulants.

    The use of alpha and beta adrenostimulators (epinephrine) and sympathomimetics (ephedrine) can lead to a paradoxical decrease in blood pressure.

    Amitriptyline, amantadine, H1-histamine receptor blockers and other drugs with m-cholinoblocking effect increase m-cholinoblocking activity. Aluminum and magnesium-containing antacid drugs or anti-diarrhea adsorbents reduce absorption.

    Antithyroid drugs increase the risk of agranulocytosis. Probucol, astemizole, cisapride, disopyramide, erythromycin, pimozide, procainamide, hidnidin promote additional lengthening of the interval Q-T, which increases the risk of developing ventricular tachycardia.

    With the simultaneous use of phenothiazides with propranolol, an increase in the concentration of both drugs is noted.

    Special instructions:

    For the correction of extrapyramidal disorders, antiparkinsonian drugs are used - trihexyphenidyl and others; dyskinesias are cut by subcutaneous injection of 2 ml of a 20% solution of caffeine and 1 ml of a 0.1% solution of atropine).

    In elderly patients, the development of irreversible dyskinesia. When there are signs of late dyskinesia, a malignant neuroleptic syndrome treatment should be canceled.

    Against the background of therapy with phenothiazine derivatives, it is possible to obtain false positive tests for phenylketonuria.

    The use of phenothiazine derivatives should be discontinued no less than 48 hours before the proposed myelography (resumption is possible in 24 hours).

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

    During the treatment it is not recommended to drive vehicles,activities requiring rapidity of psychomotor reactions and precise movements.

    Form release / dosage:

    Solution for intramuscular injection 2 mg / ml.

    Packaging:

    1 ml per ampoule of neutral glass.

    For 10 ampoules together with instructions for use and a knife for opening ampoules or a scarifier ampoule in a box of cardboard.

    5 ampoules per circuit cell box made of polyvinyl chloride film and foil of aluminum printed lacquered or foil-free.

    2 contour squares with an ampoule opener or a scarifier ampoule and instructions for use are placed in a pack of cardboard.

    When using ampoules with notches, rings and break points, the scarifierA bullet or knife for opening ampoules is allowed not to be invested.
    Storage conditions:

    In the dark place at a temperature of 15 to 25 ° C.

    Keep out of the reach of children.

    Shelf life:3 years.
    Do not use after the expiration date stated on the package

    Terms of leave from pharmacies:On prescription
    Registration number:P N001406 / 01-2002
    Date of registration:21.04.2008
    The owner of the registration certificate:DALHIMFARM, OJSC DALHIMFARM, OJSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp18.10.2015
    Illustrated instructions
      Instructions
      Up