Active substanceThioridazineThioridazine
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  • Dosage form: & nbspcoated tablets
    Composition:
    Active substance: thioridazine hydrochloride 0.010 g (10 mg) or 0.025 g (25 mg); auxiliary substances: sugar milk (lactose), potato starch, microcrystalline cellulose, polyvinylpyrrolidone (povidone), sodium carboxymethyl starch, aerosil (silicon dioxide colloid), magnesium stearate, hydroxypropylmethylcellulose, tween-80. titanium dioxide, talc.

    Description:
    The tablets covered with a cover white or white with a yellowish shade of color, round, biconcave form.

    Pharmacotherapeutic group:antipsychotic (neuroleptic) remedy
    ATX: & nbsp

    N.05.A.C.02   Thioridazine

    Pharmacodynamics:
    Thioridazine is a piperidine derivative of phenothiazine, has an antipsychotic, tranquilizing, antidepressant, antipruritic and antiemetic effect. The mechanism of antipsychotic action is associated with the blockade of postsynaptic dopaminergic receptors in the mesolimbic structures of the brain.The central antiemetic effect is due to oppression or blockade of dopamine D2-penenTopoB in the chemoreceptor trigger zone IV of the ventricle, peripheral - blockade of the vagus nerve in the gastrointestinal tract. It also has sympatholytic and m-holinoblocking action. In small doses, it has an anxiolytic effect, reduces the feeling of inner tension and anxiety, and exhibits antipsychotic (neuroleptic) properties in higher doses. Antihistamine and anticholinergic action is most pronounced among all drugs from the group of neuroleptics. In average therapeutic doses, as a rule, does not cause extrapyramidal disorders and drowsiness. Causes hyperprolactinemia.

    Pharmacokinetics:
    Absorption is high, the time of the maximum concentration (C max) in the blood plasma is 1-4 hours after ingestion. About 90% of the drug binds to plasma proteins. Metabolised in the liver with the formation of active metabolites (mesoridazine and sulfonidazine). The half-life (T1 / 2) is 6-40 hours. Mesoridazine is pharmacologically more active than the parent substance, has a larger T1 / 2, is less associated with proteins, a free concentration is higher than that of thioridazine. Excretion in unchanged form and in the form of metabolites - kidneys (35%), with bile (about 50%).Excreted in breast milk.

    Indications:Schizophrenia, bipolar disorder; neuroses accompanied by fear, anxiety, psychomotor agitation, mood lowering, sleep disturbance, obsessive states; psychotic disorders, accompanied by hyperreactivity and excitement; severe behavioral disorders associated with psychotic disorders or neurological diseases, accompanied by aggressiveness, inability to prolong the concentration of attention; abstinence syndrome (substance abuse, alcoholism), psychomotor agitation of various genesis; moderate and severe depression in adults; Huntington's disease, tics; Skin diseases that occur with a strong and painful itching; in children's psychiatry apply in behavior disorders with increased psychomotor activity.
    Contraindications:
    Hypersensitivity, severe CNS function depression and comatose states of any etiology, craniocerebral trauma, progressive systemic diseases of the brain and spinal cord; severe cardiovascular insufficiency, severe arterial hypotension, blood diseases (hypo- and aplastic processes).Pregnancy, lactation, children's age (up to 4 years).

    Carefully:
    Alcoholism (predisposition to hepatotoxic reactions), pathological changes in blood (hemopoiesis), breast cancer (as a result of phenothiazine-induced prolactin secretion, the potential risk of disease progression and resistance to endocrine and cytotoxic drugs increases), angle-closure glaucoma, prostatic hyperplasia with clinical manifestations, hepatic and / or renal insufficiency, peptic ulcer of the stomach and duodenum (during the period bostreniya); diseases accompanied by an increased risk of thromboembolic complications; Parkinson's disease (extrapyramidal effects are intensified); epilepsy; mixedem; chronic diseases accompanied by respiratory failure (especially in children); Reye syndrome (increased risk of hepatotoxicity in children and adolescents); cachexia, vomiting (the antiemetic effect of phenothiazines may mask vomiting associated with overdose of other drugs). Elderly age.

    Dosing and Administration:
    Inside. Dosing regimen is individual.
    Adults:
    In acute psychosis, mania, schizophrenia and agitational depression: on an outpatient basis, 150-400 mg per day; in a hospital - 250-800 mg per day. Treatment usually begins with low doses, 25-75 mg per day, gradually increasing to the optimal therapeutic dose, which is usually achieved within 7 days, and the antipsychotic effect is observed after 10-14 days. The course of treatment is several weeks. Supportive daily dose: 75-200 mg once before bedtime. At treatment of persons of advanced age usually apply low doses: 30-100 mg per day. The drug should be withdrawn gradually.
    For mild mental and emotional disorders - 30-75 mg per day, with moderate to severe disorders - 50-200 mg per day. Begin treatment with low doses, gradually increasing them to the optimal therapeutic dose. In psychosomatic disorders: 10-75 mg per day. To suppress severe itching, the dose of the drug is set individually and it should not exceed 200 mg.
    For children:
    From 4 to 7 years - 10-20 mg per day. Multiplicity of reception - 2-3 times a day.
    From 8 to 14 years - 20-30 mg per day. Multiplicity of admission - 3 times a day.
    From 15 to 18 years - 30-50 mg per day. Multiplicity of admission - 3 times a day.

    Side effects:
    From the side of the central nervous system:
    Confusion of consciousness, late dyskinesia, psychomotor agitation, insomnia, extrapyramidal and dystonic disorders, parkinsonism, emotional disturbances, thermoregulation disorders, decreased convulsive threshold, syncope.
    From the gastrointestinal tract:
    Hyposalivation, anorexia, increased appetite, dyspepsia, nausea, vomiting, diarrhea, paralytic ileus, weight gain, hypertrophy of the papillae of the tongue, rarely - cholestatic hepatitis.
    From the cardiovascular system:
    Hypotension, tachycardia.
    On the part of the hematopoiesis system:
    In isolated cases - agranulocytosis, leukopenia, granulocytopenia, eosinophilia, thrombocytopenia, aplastic anemia, pancytopenia.
    Allergic reactions:
    Skin allergic reactions, erythema, rash, exfoliative dermatitis, angioedema, bronchospastic syndrome, nasal congestion, photophobia.
    From the genitourinary system:
    Reduction of libido, ejaculation, paradoxical ishuria, dysuria, priapism.
    From the endocrine system:
    False positive pregnancy tests, dysmenorrhea, hyperprolactinemia, gynecomastia, weight gain.
    From the sense organs:
    Visual impairment, photophobia.
    Other:
    Melanosis of the skin (with prolonged use in high doses).

    Overdose:
    Drowsiness, confusion, urinary retention, disorientation, coma, areflexia, hyperreflexia, dry mouth, nasal congestion, postural hypotension, respiratory center depression, convulsions, hypothermia. Treatment is symptomatic, aimed at reducing absorption and accelerating the excretion of the drug. Gastric lavage with a solution of activated charcoal, laxatives (for example, magnesium sulfate). The introduction of isotonic solutions. Control of the function of the cardiovascular and respiratory systems. If necessary, consistently perform artificial ventilation, monitoring the function of the cardiovascular system, preventing the development of metabolic acidosis. There is no specific antidote.

    Interaction:
    Strengthens the depressing effect on the central nervous system when combined with general anesthetics, opiates, barbiturates, ethanol, atropine. Enhances the hepatotoxic effect of antidiabetic drugs. With amphetamine - it acts antagonistically.With levodopa - reduces antiparkinsonian action. With guanethidine reduces the antihypertensive effect of the latter, but enhances the effect of other antihypertensive drugs, which increases the risk of significant orthostatic hypotension. Reduces the effect of anticoagulants. Tyson's action can weaken anticonvulsant drugs, cimetidine. At the same time, while taking with antiepileptic drugs (including barbiturates) thioridazine reduces their effect (reduces the epileptic threshold). Quinidine - potentiates cardiodepressive action. Ephedrine - contributes to a paradoxical decrease in blood pressure. Sympathomimetics - intensify the arrhythmogenic effect. Probucol, astemizole, cisapride, disopyramide, erythromycin, pimozide, procainamide and quinidine contribute to an additional elongation of the QT interval, which increases the risk of developing ventricular tachycardia. Antithyroid drugs increase the risk of agranulocytosis. Reduces the effect of funds that reduce appetite (with the exception of fenfluramine). Reduces the effectiveness of the emetic action of apomorphine, enhances 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, MAO inhibitors, antihistamines possible elongation and increased sedation and antiholi chergicheskogo effects. With thiazide diuretics - increased hyponatremia. With drugs lithium - reduced absorption in the gastrointestinal tract, increasing the rate of excretion by the kidneys of lithium ions, increased severity of extrapyramidal disorders, early signs of lithium toxicity (nausea and vomiting) can be masked pro- tivorvotnym effect thioridazine. In combination with beta-blockers enhances the hypotensive effect, it increases the risk of irreversible retinopathy, arrhythmias and tardive dyskinesia.

    Special instructions:
    During the period of treatment is necessary to control the morphological composition of the blood, avoid drinking alcohol and classes of potentially hazardous activities that require high concentration and psychomotor speed reactions.
    Influence on ability of management of motor transport and maintenance of machinery in motion
    Tyson reduces coordination and reduces the response, especially at the beginning of treatment, so during drug treatment should refrain from driving vehicles and servicing moving mechanisms.
    Form release / dosage:
    Tablets of 10 mg and 25 mg
    Packaging:
    on 10 pieces in a contour cellular packing from a film of polyvinylchloride and aluminum foil. For 60 tablets in a can of lightproof glass. Each jar or 6 contour squares, together with the instruction for use, is placed in a pack of cardboard.

    Storage conditions:
    List B. In a dry, sheltered from light, out of reach of children, at a temperature of no higher than 25 ° C.

    Shelf life:
    2 years. Do not use after the expiration date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:P N003419 / 01
    Date of registration:24.03.09
    The owner of the registration certificate:VEROPHARM SA VEROPHARM SA Russia
    Manufacturer: & nbsp
    Information update date: & nbsp09.09.2015
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