Universal reference book for medicines
Product name: TIAPRIDAL В® (TIAPRIDAL В® )

Active substance: tiapride

Type: Antipsychotic drug (antipsychotic)

Manufacturer: SANOFI-AVENTIS FRANCE (France) manufactured by SANOFI WINTHROP INDUSTRIE (France)
Composition, form of production and packaging
Tablets are
white or creamy white in color, round, flat, with edges chamfered on both sides, with a cross-shaped risk on one side and engraved "T100" on the other;odorless or with a faint odor.

1 tab.

thiaprid hydrochloride 111.1 mg,

which corresponds to the content of thiapride 100 mg

[PRING] mannitol - 30 mg, microcrystalline cellulose - 14 mg, povidone - 11 mg, silicon dioxide colloidal water - 10.5 mg, magnesium stearate - 3.4 mg.

10 pieces.
- blisters (2) - packs of cardboard.
The solution for intravenous and / or injection is colorless or almost colorless, transparent.

1 ml of 1 amp.

thiaprid hydrochloride 55.55 mg 111.1 mg,

which corresponds to the content of thiapride 50 mg of 100 mg

[PRING] sodium chloride - 5 mg, water d / and - up to 2 ml.

2 ml ampoules of colorless glass with a break point and two marking rings in the upper part of the ampoule (6) - packings of cellular contour plastic (2) - packs of cardboard.

INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2010.

PHARMACHOLOGIC EFFECT

Antipsychotic drug (antipsychotic).
Has a hypnotic, sedative, analgesic effect. Eliminates dyskinesia of central origin.
The antipsychotic effect is due to the blockade of dopamine D 2 receptors in the mesolimbic and mesocortical systems.

Has a pronounced analgesic effect, both with interoceptive and exteroceptive pain.
Sedative action is due to blockade of adrenoreceptors of the reticular formation of the brainstem; antiemetic effect - blockade of dopamine D 2 receptors in the trigger zone of the vomiting center; hypothermic action - blockade of dopamine receptors of the hypothalamus.
PHARMACOKINETICS

After oral administration of 200 mg of thiapride, the maximum plasma concentration in the plasma is 1.3 Ојg / ml - achieved in 1 hour.
After intramuscular injection of 200 mg of thiapride, the maximum plasma concentration in the plasma is 2.5 Ојg / ml - achieved in 30 minutes.
Bioavailability of tablets is 75%.
When taken directly before meals, bioavailability is increased by 20%, and the maximum concentration in plasma is increased 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 the ratio of concentrations in milk and in blood 1,2.
The binding 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 in the urine, and the kidney clearance reaches 330 ml / min.
Pharmacokinetics in special clinical cases

In patients with impaired renal function, excretion correlates with QC.
If the QC is below 20 ml / min, the daily dose of the drug should be adjusted depending on the severity of renal failure: apply a half dose at a CC of 11-20 ml / min and a quarter dose at a CC of 10 ml / min.
INDICATIONS

Pills

For adults:

- relief of psychomotor agitation and aggressive conditions, especially with chronic alcoholism or in old age;

- intensive chronic pain syndrome.

For adults and children over 6 years of age:

- different types of chorea;

- Gilles de la Tourette's syndrome.

For children over 6 years of age:

- Behavioral disorders with agitation and aggression.

Injection

- relief of psychomotor agitation and aggressive conditions, especially with chronic alcoholism or in old age;

- intensive chronic pain syndrome.

DOSING MODE

Pills

The drug in the form of tablets is prescribed only for adults and children over 6 years of age .

If the patient's condition allows, the treatment should start with a low dose of the drug, then gradually increase it.
It is always necessary to select the minimum effective dose.
Coping of psychomotor agitation and aggressive conditions, especially in chronic alcoholism: the drug is prescribed to adults at a dose of 200-300 mg / day, the course of treatment is 1-2 months.
Older patients - 50 mg 2 times / day; the dose can be gradually increased by 50-100 mg every 2-3 days to a maximum daily dose of 300 mg.
Chorea, Gilles de la Tourette's syndrome: adults are prescribed 300-800 mg / day;
treatment should be started at a dose of 25 mg / day, then slowly increase it until the minimum effective dose is reached. Children over 6 years of age are prescribed 3-6 mg / kg / day.
With intensive chronic pain syndrome, adults are usually prescribed in a dose of 200-400 mg / day.

In behavioral disorders with agitation and aggressiveness in children over 6 years of age, the dose is 100-150 mg / day.

Injection

It is intended for use only in adults .

Enter in / m or / in.
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.
Coping of psychomotor agitation and aggressive conditions, especially in chronic alcoholism: adults usually prescribe drugs at a dose of 200-300 mg / day.
With delirious syndrome or pre-dilarious state - 400-1200 mg / day, the maximum dose - 1800 mg / day. Injections should be carried out every 4-6 hours.
Elderly patients - 200-300 mg / day, that is 2-3 injections with 6-hour intervals;
the maximum single dose is 100 mg.
Intensive chronic pain syndrome: the dose is, as a rule, 200-400 mg (2-4 ampoules) / day.

SIDE EFFECT

From the central nervous system and peripheral nervous system: asthenia, fatigue (9.4%);
drowsiness (6.6%); insomnia (4.4%); agitation, psychomotor agitation (3.7%); apathic states (2.8%); dizziness (2.6%); headache (2%); Parkinsonism - tremor (2.3%), increased blood pressure, bradykinesia (1.2%), hypersalivation (1.2%);rarely - early dyskinesia and dystonia (spasmodic torticollis, oculogic crises, trism), akathisia (0.9%). These symptoms are usually reversible after the drug is discontinued or anticholinergic antiparkinsonian agents are prescribed.
With long-term use - tardive dyskinesia (stereotyped involuntary movements of the tongue, face and limbs) Anticholinergic antiparkinsonian drugs appointed as correctors can worsen the patient's condition.

The development of the ZNS is possible.

On the part of the endocrine system: hyperprolactinaemia and associated disorders (<0.2%) - amenorrhea, galactorrhea, swelling of the breast, chest pain, impotence or ejaculation, weight gain.

From the cardiovascular system: prolongation of the QT interval, atrial fibrillation, postural hypotension.

CONTRAINDICATIONS

- diagnosed or suspected prolactin-dependent tumors, for example, pituitary prolactinoma and breast cancer;

- diagnosed or suspected pheochromocytoma;

hypertensive crisis;

- marked renal and / or liver failure;

- I trimester of pregnancy;

- the period of lactation (breastfeeding);

- Children's age (up to 6 years);

- combination with sultopride;

- combinations with dopamine receptor agonists (amantadine, apomorphine, bromocriptine, cabergoline, entacapone, lizard, pergolide, pyribedil, pramipexole, quinagolide, ropinirole), except for patients suffering from Parkinson's disease;

- combinations with drugs that can cause arrhythmias: class I A antiarrhythmics (quinidine, hydroquinidine, disopyramide) and class III (amiodarone, sotalol, dofetilide, ibutilide), some antipsychotics (thioridazine, chlorpromazine, levomepromazine, trifluoperazine, cyamemazine, amisulpride , sulpiride, pimozide, haloperidol, droperidol), as well as with the following drugs: levodopa, bepridil, cisapride, difemanyl, erythromycin, misolastine, vincamine (w / w), sparfloxacin, moxifloxacin;

- Hypersensitivity to the components of the drug.

Caution should be applied to the drug in chronic renal failure (with the application it is necessary to reduce the dose and strengthen the observation);
epilepsy (due to the possibility of lowering the threshold of convulsive readiness); with cardiovascular diseases in the stage of decompensation; Parkinson's disease; together with drugs containing ethanol; with bradycardia (heart rate <55 bpm); hypokalemia; congenital elongation of the QT interval; together with drugs capable of causing pronounced bradycardia (heart rate <55 bpm), hypokalemia, slowing of cardiac conduction or prolongation of the QT interval; in elderly patients.
PREGNANCY AND LACTATION

The drug is contraindicated in the first trimester of pregnancy and during lactation.

Regarding the effect on the fetal brain of neuroleptics used in pregnancy, there is no data.
It is not recommended to use tiapride in the II and III trimesters of pregnancy. However, if there is a need for the drug, it is recommended to limit the dose and duration of treatment as far as possible.
With prolonged treatment and / or use of the drug in high doses and / or late pregnancy, neurologic functions of the newborn should be monitored.

It is not known whether thiaprid is excreted in breast milk, so if it is necessary to use the drug during lactation, breastfeeding should be discontinued.

SPECIAL INSTRUCTIONS

ZNS is 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, appears to be predisposing.
Tiapride causes a dose-dependent lengthening of the QT interval.
It is known that this effect increases the risk of serious ventricular arrhythmias, it increases in the background of a bradycardia, with hypokalemia, as well as in case of congenital or acquired prolongation of the QT interval (when combined with drugs extending the QTc interval).
Before starting the drug should be corrected hypokalemia.
Clinical picture, electrolyte balance and ECG should be monitored.
With extrapyramidal syndrome caused by neuroleptics, anticholinergic drugs should be prescribed instead of dopamine receptor agonists.

Impact on the ability to drive vehicles and manage mechanisms

During the treatment period, patients should refrain from engaging in potentially hazardous activities requiring increased concentration and speed of psychomotor reactions



OVERDOSE

Symptoms: excessive sedative effect, drowsiness, oppression of consciousness down to coma, arterial hypotension, extrapyramidal symptoms.

Treatment: withdrawal of the drug, gastric lavage (with tablets poisoning), symptomatic and detoxification therapy, monitoring of vital functions of the body, especially cardiac activity (risk of prolongation of the QT interval) until the symptoms of intoxication disappear completely.
In severe extrapyramidal symptoms - anticholinergic drugs.
Since tiaprid is slightly dialyzed, hemodialysis is not recommended to remove the active substance.
The antidote of tiapride is unknown.
DRUG INTERACTION

Combinations are contraindicated

In combination with antiarrhythmic drugs of class I A (quinidine, hydroquinidine, disopyramide) and class III (amiodarone, sotalol, dofetilide, ibutilide), some antipsychotics (thioridazine, chlorpromazine, levomepromazine, trifluoperazine, cyamemazine, sulpiride, amisulpride, pimozide, haloperidol, droperidol) and other drugs such as bepridil, cisapride, difemanyl, erythromycin, misolastine, vincomamine, increases the risk of ventricular arrhythmias, as well as atrial fibrillation.

Ethanol enhances the sedative effect of antipsychotics (neuroleptics).

With the simultaneous use of levodopa and antipsychotic drugs (antipsychotics) antagonism of the action is observed.

In patients with Parkinson's disease, it is recommended to use minimal effective doses of levodopa and thiaprid.
Dopamine receptor 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 NSA).
With the simultaneous use of Tiapridal with sparfloxacin, moxifloxacin, the risk of ventricular arrhythmia and atrial fibrillation increases.
If the combination can not be avoided, it is necessary to determine the value of the QT interval and provide ECG monitoring.
Combinations that require caution

The risk of ventricular arrhythmia and atrial fibrillation increases with simultaneous use of Tiapridal with preparations that cause bradycardia (blockers of slow calcium channels - diltiazem, verapamil, beta adrenoblockers, clonidine, guanfacine, digitalis preparations, cholinesterase inhibitors - dozepil, rivastigmine, galantamine, pyridostigmine , neostigmine), with drugs that can cause hypokalemia (potassium-withdrawing diuretics, laxatives, amphotericin B, GCS, tetracosactide).

Combinations that should be taken into account

With simultaneous use with antihypertensive drugs, an additive effect is observed, the risk of postural hypotension increases.

Strengthening of the oppressive effect on the CNS occurs with the simultaneous use of Tiapridal with drugs depressing the functions of the central nervous system: morphine derivatives (opioid analgesics, antitussives and substitution therapy);
barbiturates; benzodiazepines and other anxiolytics; hypnotics; antidepressants with sedative effect; blockers of histamine H 1 -receptors with sedative effect; antihypertensive agents of central action; baclofen; thalidomide.
TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

The drug should be stored out of reach of children, dry, protected from light at a temperature of no higher than 25 В° C.
Shelf life of tablets is 5 years, solution for injection is 3 years.
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