Tiapride (Tiapride)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceTiaprideTiapride
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  • Tiapride
    pills inwards 
    ORGANICS, JSC     Russia
  • Tiapride
    solution w / m in / in 
    ORGANICS, JSC     Russia
  • Tiapridal®
    pills inwards 
    Sanofi-Aventis France     France
  • Tiapridal®
    solution w / m in / in 
    Sanofi-Aventis France     France
    • Dosage form: & nbsppills
    Composition:
    1 tablet contains the active substance - 111.1 mg of thiaprid hydrochloride (in terms of thiapride base - 100.0 mg). auxiliary substances: lactose monohydrate (sugar milk) - 46.4 mg. potato starch - 1 8.0 mg. povidone (low molecular weight polyvinylpyrrolidone) - 1.8 mg. magnesium stearate - 2.7 mg.

    Description:
    White or white tablets with a weak yellowish color
    flat-cylindrical shape with a bevel.

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

    N.05.A.L.03   Tiapride

    Pharmacodynamics:
    Antipsychotic agent (antipsychotic); has a hypnotic, sedative, analgesic effect. Eliminates dyskinesia of central origin. Has a pronounced analgesic effect, both with interoceptive and exteroceptive pain. The antipsychotic effect is due to the blockade of dopamine 02 receptors of the mesolimbic and mesocortical system. Sedative action is due to blockade of adrenoreceptors of the reticular formation of the trunkbrain; antiemetic effect - blockade of dopamine 02-receptors in the trigger zone of the vomiting center; hypothermic action - blockade of dopamine receptors of the hypothalamus.

    Pharmacokinetics:
    After ingestion of 200 mg of thiaprid, the maximum concentration of the drug in the plasma !, 3 μg / ml - is achieved in 1 hour.
    Bioavailability of tablets is 75%. When they are taken immediately before meals, bioavailability increases by 20%, and the maximum concentration in plasma by 40%. Absorption in the elderly is slowing down.
    Distribution in the body occurs quickly (less than 1 hour). Penetrates through the blood-brain barrier and through the placenta, cumulation does not occur. The animals noted the penetration of the drug into milk, with a concentration ratio in milk and in blood of 1: 2.
    The connection with plasma proteins and with erythrocytes is weak. The metabolism of tiaprid is very small: 70% of the dose is found in the urine in an unchanged form. The plasma elimination half-life is 2.9 hours for women and 3.6 hours for men. Excretion occurs mainly with urine, and the renal clearance reaches 330 ml / minute.

    Indications:
    In adults:
    Psychomotor agitation and aggressive conditions, especially with chronic alcoholism or in old age.
    Intense chronic pain syndrome.
    In adults and children over 6 years of age:
    Different types of chorea, Gilles de la Tourette syndrome.
    In children older than 6 years:
    Disorders of behavior with agitation and aggression.

    Contraindications:
    Hypersensitivity to tiapride or other components of the drug.
    Diagnosed or suspected prolactin-dependent tumors, for example: pituitary prolactinoma and breast cancer.
    Diagnosed or suspected pheochromocytoma.
    In combination with sultopride.
    Pregnancy (first trimester).
    Lactation period.
    Children's age (up to 6 years).
    Hypertensive crisis.
    Pronounced renal and / or hepatic insufficiency.
    In combination with dopaminergic agonists (amantadine. apomorphine. bromocriptine, cabergoline, entacapone, lisuride, pergolide, piribedil, pramiieksole, quinagolide, ropinirole), except for patients suffering from Parkinson's disease.
    In combination with drugs that can cause heart rhythm disturbances: antiarrhythmic drugs 1a class (quinidine, hydroquinidine, disopyramide) and class III (amiodarone, sotalol, dofetilide, ibutilide), some neuroleptics (thioridazine, chlorpromazine, levomepromazine, trifluoperazine, cyamemazine, amisulpride, sulpiride, pimozide, haloperidol, droperidol), as well as with the following preparations: levodopa, bepridil, cisapride, difemanyl, erythromycin, mizolastin, intravenous wincamine, sparfloxacin, moxifloxacin. (see the section "Interaction with other medicinal products"),

    Carefully:
    Chronic renal failure. In use, it is necessary to reduce the dose and increase surveillance (see Dosage and Administration);
    Epilepsy, due to the possibility of lowering the convulsive threshold; Cardiovascular diseases in the stage of decompensation;
    Parkinson's disease;
    Joint use of medicines containing alcohol;
    In the elderly, with bradycardia (less often 55 bpm), hypokalemia, congenital lengthening of the QT interval, as well as with the joint use of drugs capable of causing a pronounced bradycardia (less than 55 bpm), hypokalemia. a decrease in cardiac conduction or an extension of the QT interval.

    Pregnancy and lactation:
    The drug is contraindicated in the first trimester of pregnancy and during lactation.
    Regarding the effect of neuroleptics used during pregnancy on the fetal brain, there is no data (preferably not to use tiapride during pregnancy).
    However, if the drug is still used during pregnancy, it is recommended, as far as possible, to limit the dose and duration of treatment.
    With prolonged treatment and / or the use of high doses and / or late pregnancy, control of the neurological functions of the newborn is justified.
    Lactation
    It is not known whether the tiapride in breast milk, so it is recommended to stop breastfeeding while taking the drug.
    Dosing and Administration:
    Only for adults and children over 6 years.
    It is always necessary to select the minimum effective dose. If the patient's condition allows, treatment should be started with a low dose, then gradually increasing it.
    Psychomotor agitation and aggressive conditions, especially with chronic alcoholism or in old age:
    In adults: 200-300 mg / day, treatment course 1 - 2 months.
    In the elderly: 50 mg twice a day. The dose can be gradually increased by 50 100 mg every 2-3 days to a maximum daily dose of 300 m.
    Chorea, Gilles de la Tourette syndrome Adults: 300 to 800 mg / day
    Treatment should begin with a dose of 25 mg per day, then slowly increase it until the minimum effective dose is reached.
    - In patients with impaired renal function: if the creatinine clearance is less than 20 ml / min, the daily dose of the drug should be adjusted depending on the severity of renal failure: a half dose is used with creatinine clearance of 11-20 ml / min and a quarter of the dose with creatinine clearance of 10 ml / min.
    In children older than 6 years: 3-6 mg / kg / day
    Intense chronic pain syndrome.
    Usual dose for adults is 200 - 400 mg / day.
    Behavioral disorders with agitation and aggression in children over the age of 6 le d - dose is 100-150 mg / day.

    Side effects:
    Asthenia, fatigue
    Drowsiness
    Insomnia
    Agitation, psychomotor agitation Apathy states Dizziness Headache
    Parkinson's syndrome: tremor, increased blood pressure, bradykinesia. hypersalivation.
    Much less often:
    Early dyskinesia and dystonia (spastic torticollis, oculogic crises, trism), akathisia.
    These symptoms are usually reversible after the drug is discontinued or anticholinergic antiparkinson agents are prescribed.
    Late dyskinesia (stereotypic involuntary movements of the tongue, face and limbs) that occurs with prolonged use (anticholinergic antiparkinsonics,The appointments as proof-readers can worsen a condition of the patient).
    Hyperprolactinaemia and associated disorders (less than 0.2%): amenorrhea, galactorrhea, swelling of the breast, chest pain, impotence or ejaculatory impairment,
    An increase in body weight,
    The extension of the QT interval,
    Atrial fibrillation,
    Postural hypotension,
    Malignant neuroleptic syndrome.

    Overdose:
    Symptoms: excessive sedation, drowsiness, oppression of consciousness right up to coma,
    arterial hypotension, extrapyramidal symptoms.
    Treatment: cancellation of the drug, gastric lavage (with tablets poisoning),
    symptomatic and detoxification therapy, monitoring of the vital functions of the body (especially for cardiac activity (risk of prolongation of the QT interval) until the symptoms of intoxication disappear completely.When there are severe extrapyramidal symptoms, anticholinergic treatment.
    Because the tiapride weakly subjected to dialysis, to remove the substance is not recommended to use hemodialysis. The antidote of tiapride is unknown.

    Interaction:
    When used in conjunction with antiarrhythmic drugs may increase the risk of developingventricular arrhythmias, as well as atrial fibrillation.
    Alcohol enhances the sedative effect of neuroleptics.
    There is a joint antagonism between the action of levodopa and neuroleptics. In patients with Parkinson's disease, it is recommended that minimal effective doses of levodopa and thiaprid be used.
    Dopaminergic agonists can cause or exacerbate psychotic disorders. If treatment with neuroleptics is necessary for a patient suffering from Parkinson's disease receiving a dopaminergic drug, the dose of the latter should be gradually reduced to cancellation (sudden cancellation may lead to the development of a malignant neuroleptic syndrome).
    Drugs that cause bradycardia and hypokalemia when taken together with tiaprid may increase the risk of ventricular arrhythmias, as well as atrial fibrillation. Joint reception with antihypertensive drugs increases the risk of postural hypertension. Drugs that depress the functions of the central nervous system, when combined with thiapride, contribute to an intensifying oppressive effect.

    Special instructions:
    Malignant neuroleptic syndrome: Malignant neuroleptic syndrome, characterized by pallor, hyperthermia,rigidity of muscles, dysfunction of the peripheral nervous system, impaired consciousness. Symptoms of peripheral nervous system dysfunction, such as increased sweating and lability of blood pressure, may precede the onset of hyperthermia and, therefore, constitute early warning signals. Some risk factors, such as dehydration or organic brain damage, despite the fact that such an effect of neuroleptics may be explained by idiosyncrasy, are probably predisposing.
    OT extension: tiapride causes a dose-dependent lengthening of the Q Q interval. It is known that this effect increases the risk of serious ventricular arrhythmias, it increases in the background of a bradycardia, with hypokalemia, and also in the case of a congenital or acquired long QT interval (combination with QTc-prolonging drugs).
    Hypokalemia should be adjusted before starting the drug, except for goy. should monitor the clinical picture, electrolyte balance and electrocardiogram.
    With extrapyramidal syndrome caused by neuroleptics, anticholinergic drugs should be prescribed instead of dopaminergic agonists.
    During the treatment period, it is necessary to refrain from engaging in potentially dangerous activities that require a high concentration of attention and speed of psychomotor reactions.

    Effect on the ability to drive transp. cf. and fur:During the treatment period, it is necessary to refrain from engaging in potentially dangerous activities that require a high concentration of attention and speed of psychomotor reactions.
    Form release / dosage:
    Tablets of 100 mg. 3 contourcell packs of 10 tablets or 30 tablets in a glass of lightproof glass, together with instructions for use in a cardboard pack.

    Packaging:
    • (10) - packings, cellular, outline (3) - packs, cardboard
    • (30) - polymer cans (1) - packs of cardboard
    • (30) - cans of light-protective glass (1) - packs cardboard
    Storage conditions:
    In the dark place at a temperature of no higher than 30 ° C. Keep out of the reach of children.

    Shelf life:
    5 years.
    Do NOT use after the expiration date indicated on the package
    Terms of leave from pharmacies:On prescription
    Registration number:LSR-004200/08
    Date of registration:30.05.2008
    The owner of the registration certificate:ORGANICS, JSC ORGANICS, JSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp28.08.2015
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