Triftazin-Darnitsa (Triphtazin-Darnitsa)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceTrifluoperazineTrifluoperazine
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    • Dosage form: & nbspsolution for intramuscular injection
    Composition:

    1 ml of the solution contains:

    active substance: trifluazine (trifluoperazine dihydrochloride) in terms of 100% dry matter 2.00 mg;

    Excipients: sodium citrate dihydrate 1 mg, water for injection up to 1 ml.

    Description:clear colorless or slightly yellowish liquid
    Pharmacotherapeutic group:antipsychotic agent (antipsychotic)
    ATX: & nbsp

    N.05.A.B.06   Trifluoperazine

    Pharmacodynamics:

    Antipsychotic agent (neuroleptic), piperazine derivative of phenothiazine. It also has sedative, antiemetic, anti-icic, cataleptic, hypotensive, hypothermic and mild anticholinergic action. 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) D2dopamine receptors, as well as blockade of endings n.vagus in the gastrointestinal tract.

    Hypothermic action - blockade of dopamine receptors of the hypothalamus.

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

    Pharmacokinetics:

    Absorption is high. Bioavailability after oral administration - 35% (has the effect of "first passage" through the liver). The connection with plasma proteins is 95%. TCmax- 2-4 hours, with intramuscular injection - 1-2 hours.Penetrates through the blood-brain barrier, the placenta and into breast milk.

    Intensively metabolized in the liver, metabolites are pharmacologically inactive. T1 / 2 - 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:Psychotic disorders, incl. schizophrenia. Psychomotor agitation. Neuroses with a predominance of anxiety and fear. Symptomatic treatment of nausea and vomiting.
    Contraindications:

    Hypersensitivity (including to other phenothiazines), severe cardiovascular diseases (decompensated chronic heart failure, arterial hypotension), severe depression of the central nervous system (including against the background of the drug) and coma 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 3 years), pregnancy, lactation.

    Carefully:Alcoholism (increased predisposition to hepatotoxic reactions), angina pectoris,Valvular heart disease, limiting the amount of minute blood flow (possible development of severe arterial hypotension), pathological changes in blood (hemopoiesis), breast cancer (as a result of prolactin-induced phenothiazines, the potential risk of disease progression and resistance to endocrine and cytotoxic drugs increase) , zakratougolnaya glaucoma, hyperplasia, prostate with clinical manifestations, hepatic and / or renal failure, gastric ulcer and duodenum 12 (in 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's syndrome (nRisk of manifestation is increased hepatotoxicity in children and adolescents); cachexia, vomiting (antiemetic effect of phenothiazines may mask vomiting associated with overdose of other medicines), elderly age.Patients exposed to high temperatures.

    Dosing and Administration:

    Adults: intramuscularly 1-2 mg, if necessary every 4-6 hours. With more frequent injections, cumulation phenomena are possible. The maximum daily dose is 10 mg / day.

    With depressive-hallucinatory and depressive-delirious states, Trifthazin-Darnitsa is used together with antidepressants.

    As an anti-emetic agent Triftazin-Darnitsa. is prescribed in doses of 1-4 mg per day.

    Children over 6 years (with manic-depressive psychosis) - 1 mg 1-2 times a day.

    Elderly, as well as debilitated and debilitated patients, the initial dose is reduced by a factor of 2.

    Treatment Triftazinom-Darnitsa should be strictly individualized depending on the course of the disease. Treatment terms can be 3-9 months, and in some cases and more.

    Side effects:

    From the central and peripheral nervous system: headache, drowsiness, dizziness, insomnia, akathisia, dystonic extrapyramidal reactions, pseudoparkinsonism, late disamnesia, neuroleptic malignant syndrome, phenomena of mental indifference,delayed response to external stimuli, akinetic-rigid phenomena, hyperkinesia, tremor, autonomic disorders, tardive dyskinesia, dystonia, thermoregulation disorders.

    On the part of the organs of the sense system: paresis of accommodation, retinopathy, clouding of the lens and cornea.

    From the gastrointestinal tract: dry mouth, anorexia, bulimia, nausea, vomiting, diarrhea, constipation, gastralgia.

    From the liver and bile ducts: cholestatic icterus, hepatotoxicity.

    From the endocrine system and metabolic disorders: hypo- or hyperglycemia, glucosuria, menstrual cycle disorders (dysmenorrhea, amenorrhea), gynecomastia, weight gain, galactorrhea, chest pain, lactation, and libido disorders.

    From the cardiovascular system: tachycardia, lowering blood pressure (orthostatic hypotension), heart rhythm disturbances, changes on the electrocardiogram (lengthening of the interval QT, smoothing of the T wave), cardiac arrest.

    From the side of the Kuovi system: thrombocytopenia, agranulocytosis, anemia (hemolytic, aplastic), pancytopenia, leukopenia, thrombocytopenic purpura, eosinfilia.

    From the genitourinary system: decreased potency, ejaculatory disorders, priapism, urinary retention, oliguria, urinary tract disorders.

    Dermatological disorders: photoderma, reddening of the skin, depigmentation of the skin.

    Allergic Reagents: skin rashes, hives, angioedema, anaphylactic shock.

    Overdose:Symptoms: malignant neuroleptic syndrome, collapse, hypothermia, coma, toxic hepatitis.
    Treatment: symptomatic: when a collapse is introduced nikethamide, caffeine, phenylephrine. Neurological complications usually decrease with decreasing dose, as well as the appointment of cyclodol; with the development of neuroleptic depression, antidepressants and psychostimulants are used. Dialysis is ineffective.
    Interaction:

    Means that inhibit central nervous function systems (means for anesthesia, opioid analgesics, barbiturates, anxiolytics, ethanol, ethanol containing drugs) - the effect of the drug is increased, depression of the central nervous system is intensified and respiration is inhibited.

    Inductors CYP1A2 (carbamazepine, phenobarbital, rifampicin, aminoglutethimide) - reduce the concentration and effect of Triftazin-Darnitsa.

    Inhibitors CYP1A2 (amiodarone, ciprofloxacin, fluvoxamine, ketoconazole, norfloxacin, ofloxacin, rofecoxib) - increase the concentration and effect of Triftazin-Darnitsa.

    Alpha-adrenoblockers - gipotenzivnye effects of the drug.

    Levodopa and phenamines - reduce the effectt of the preparation.

    Anti-epileptic drugs - with simultaneous use decreases the effect of antiepileptic drugs.

    Antithyroid drugs - the risk of developing agranulocytosis increases.
    Astemizole, disopyramide, erythromycin, procainamide - The risk of developing tachycardia increases.

    Tricyclic antidepressants, maprotiline, monoamine oxidase inhibitors - lengthening and strengthening of sedative and anticholinergic effects of Triftazin-Darnitsa are possible.

    Lithium preparations - it is possible to intensify extrapyramidal disorders, early onset of signs of lithium intoxication.

    Adrenomimetica sympathomimetics - simultaneous application can lead to a paradoxical decrease in blood pressure.

    Mutually enhanced effects with simultaneous intake of ethanol.

    Anticonvulsants - it is possible to reduce the convulsive threshold.

    Drugs that cause extrapyramidal reactions (metoclopramide) - it is possible to increase the frequency and severity of extrapyramidal disorders.

    Antihypertensive drugs - possibly the development of orthostatic arterial hypotension.

    Prochlorperazine - a prolonged loss of consciousness is possible.

    The drug can weaken the vasoconstrictive effect of ephedrine and epinephrine, enhance the anticholinergic effects of other drugs, inhibit the effect of amphetamines, levodopa, clonidine, guanetidine.

    Bromocriptine - phenothiazines inhibit the ability of bromocriptine to reduce the concentration of prolactin in the serum of the blood.

    Propranolol, sulfadoxine - increase the concentration of Triftazin-Darnitsa in blood plasma.

    Polypeptide antibiotics - simultaneous application can cause paralysis of the respiratory muscles.

    Trazodone - an additive hypotensive effect is observed.

    Valproic acid - with simultaneous application, an increase in the concentration of valproic acid in the blood plasma is observed.

    Special instructions:

    Neuroleptic malignant syndrome can occur at any time in the process treatment with neuroleptics and lead to lethal outcome.

    The introduction of epinephrine for the relief of trifluoperazine-induced hypotension is impractical,since the alpha-adrenergic effect of epinephrine can be blocked, and stimulation of beta-adrenoreceptors can further reduce blood pressure and the development of tachycardia.

    In elderly patients, the development of irreversible dyskinesia. When signs of late dyskinesia, neuroleptic malignant syndrome, treatment should be discontinued.

    Avoid exposure to high temperatures (thermoregulation may be impaired).

    Against the background of therapy with phenothiazines, it is possible to receive false positive tests for phenylketonuria.

    The appointment of phenothiazines 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 period, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions, avoiding the use of ethanol.

    Form release / dosage:Solution for intramuscular injection introduction.
    Packaging:1 ml per ampoule of transparent glass.
    It is allowed to paste on the ampoule paper label with self-adhesive coating.
    5 ampoules with an autopsy knife ampoules or scarifier ampoule into the contour mesh packing (cassette).
    Two contoured cell packs with instruction on medical application in a pack.
    For 10 ampoules with instructions for medical use and knife for opening ampoules or by ampoule scapegrator box with corrugated liner. Boxes are pasted with a label-parcel post.
    When packaging ampoules with a color ring or break point, knives for opening ampoules or ampoule scalers are not included.

    Storage conditions:

    Keep out of reach of children, at a temperature of 5 ° C to 25 ° C.

    Shelf life:

    4 years.

    Do not use after the expiration date stated on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:П N010601
    Date of registration:08.08.2011
    The owner of the registration certificate:DARNITSA PHARMACEUTICAL FIRM, CJSCDARNITSA PHARMACEUTICAL FIRM, CJSC Ukraine
    Manufacturer: & nbsp
    Information update date: & nbsp18.10.2015
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