Tiapridal solution 50mg/ml 2ml ampoules, 12pcs

Composition

Active ingredient:

111.1 mg of tiapride hydrochloride, which corresponds to 100 mg of tiapride base;

Auxiliary substances:

sodium chloride,

water for injection.

Pharmacological action

Tiapridal – antipsychotic, anxiolytic, analgesic.

Selectively blocks central dopamine_D2receptors without affecting_D1receptors.

Pharmacodynamics

It has antipsychotic and anxiolytic effects, including in the treatment of alcohol, opium and nicotine withdrawal. Eliminates dyskinesia, promotes clarity of thinking in elderly patients, has analgesic properties.

Pharmacokinetics

After an intravenous injection of 200 mg, the_cmax (2.5 mcg/ml) is determined in 30 minutes, after taking 200 mg orally (1.3 mcg / ml) — after 1 hour. Bioavailability-75% (taking immediately before meals increases bioavailability by 20%, _cmax-by 40%). Absorption in the elderly is slow.

Distribution is fast: after 1 hour it is detected in many tissues and organs, passes the BBB and placental barrier, penetrates into breast milk (the concentration in milk is half that in blood plasma). Practically does not bind to plasma proteins, red blood cells. T_1/2 — 2.9 hours in women and 3.6 hours in men. Moderately metabolized: 70% of the dose taken is found unchanged in the urine.

Excretion occurs mainly by the kidneys; Cl is 330 ml/min. In patients with impaired renal excretory function, the degree of decreased excretion is correlated with the value of Cl creatinine. The daily dose with creatinine clearance less than 20 ml / min should be reduced by 2 times, less than 10 ml / min-by 4 times.

Indications

Behavioral disorders (agitation, aggressiveness), especially in patients with alcoholism; pain (intense, non-stopping); dyskinesia (spontaneous, late, Huntington’s chorea).

Use during pregnancy and lactation

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

There are no data available on the effect of antipsychotics used during pregnancy on the fetal brain (preferably, do not use tiapride during pregnancy). However, if the drug is still used during pregnancy, it is recommended to limit the dose and duration of treatment as much as possible.

With prolonged treatment and/or the use of high doses and/or in late pregnancy, monitoring of neurological functions of the newborn is justified.

Breast-feeding

It is not known whether tiaprid passes into breast milk, so breastfeeding is prohibited.

Contraindications

Hypersensitivity, pheochromocytoma (including suspected), pregnancy, breast-feeding.

Side effects

Long — term use of Tiapridal in high doses may sometimes cause drowsiness, muscle hypotension, dyskinesia (early — spastic, torticollis, trismus, oculomotor disorders; and late), extrapyramidal symptoms, muscle relaxation, lowering blood pressure, amenorrhea, galactorrhea, hyperprolactinemia, gynecomastia, impotence, frigidity, weight gain, neuroleptic malignant syndrome (unexplained hyperthermia-requires discontinuation of the drug).

Interaction

Not recommended combinations

• When used together with class 1 antiarrhythmic drugs (quinidine, hydroquinidine, disopyramide) and class III (amiodarone, sotalol, dofetilide, ibutilide), antiarrhythmic drugs, certain antipsychotics (thioridazine, chlorpromazine, levomepromazine, trifluoperazine, cyamemazine, sulpiride, amisulpride, pimozide, haloperidol, droperidol) and other medications, such as bepridil, cisaprid, difemanil, erythromycin, mizolastine, and vincamine, increase the risk of ventricular arrhythmias, as well as atrial fibrillation.
• Alcohol increases the sedative effect of neuroleptics.
• Levodopan is a common antagonism of levodopa and neuroleptics. In patients with Parkinson’s disease, it is recommended to use the minimum effective doses of levodopa and tiapride.
• Dopaminergic agonists can cause or increase psychotic disorders. If antipsychotic treatment is necessary for a patient suffering from Parkinson’s disease who is receiving a dopaminergic drug, the dose of the latter should be gradually reduced until withdrawal (abrupt withdrawal may lead to the development of neuroleptic malignant syndrome).
• Sparfloxacin, moxifloxacin: The risk of ventricular arrhythmias, as well as atrial fibrillation, increases. If the combination cannot be avoided, first check the QT interval and provide ECG monitoring.

Combinations that require caution

• Drugs that cause bradycardia (slow calcium channel blockers: diltiazem, verapamil; beta-blockers; clonidine, guanfacine; digitalis preparations, cholinesterase inhibitors: donezepil, rivastigmine, galantamine, pyridostigmine, neostigmine).
• Drugs that can cause hypokalemia: potassium-releasing diuretics, laxatives, amphotericin B, glucocorticoids, tetracosactide. The risk of ventricular arrhythmias, as well as atrial fibrillation, increases.

Combinations to take into account

• Antihypertensive medications (all): Additive effect, increased risk of postural hypotension.
• Drugs that inhibit the function of the central nervous system: Morphine derivatives (analgesics, antitussives, and substitutional therapies); barbiturates; benzodiazepines and other anxiolytics; hypnotics; antidepressants with sedative effects; antihistamines with sedative effects; antihypertensive agents of central action; baclofen; thalidomide contribute to increased suppression of CNS function.

How to take, course of use and dosage

For intramuscular or intravenous use. The drug is used only for adults. It is always necessary to select the minimum effective dose. If the patient’s condition allows, treatment should begin with a low dose, then gradually increase it.

Relief of psychomotor agitation and aggressive states, especially in patients with chronic alcoholism or in the elderly:  the usual dose is 200-300 mg / day.

For delirious syndrome or delirious condition:  adults – 400-1200 mg / day (maximum up to 1800 mg / day). Injections should be given every 4-6 hours; in the elderly-200-300 mg / day, that is,2-3 injections at 6-hour intervals. Do not exceed a single dose of 100 mg.

Intense chronic pain syndrome:  adults – 200-400 mg / day, that is,2-4 ampoules per day.

Overdose

Symptoms:  excessive sedation, drowsiness, depression of consciousness up to coma, hypotension, extrapyramidal symptoms.

Treatment:  withdrawal of the drug, symptomatic and detoxification therapy, monitoring of vital body functions (especially cardiac activity – the risk of prolongation of the QT interval) until the symptoms of intoxication completely disappear. If severe extrapyramidal symptoms occur, anticholinergic treatment is recommended. Since tiapride is poorly dialyzed, it is not recommended to use hemodialysis to remove the substance. The antidote of tiapride is unknown.

Special instructions

Neuroleptic malignant syndrome is characterized by pallor, hyperthermia, muscle rigidity, peripheral nervous system dysfunction, and impaired consciousness. Signs of peripheral nervous system dysfunction, such as increased sweating and lability of blood pressure, can precede the onset of hyperthermia and, therefore, represent early warning signals. Some risk factors, such as dehydration or organic brain damage, despite the fact that such an effect of neuroleptics can be explained by idiosyncrasy, seem to be predisposing. Tiapride causes a dose-dependent prolongation of the QT interval.

It is known that this effect increases the risk of serious ventricular arrhythmias, it increases against the background of bradycardia, hypokalemia, as well as in the case of congenital or acquired long QT interval (combination with drugs that prolong the QT interval with). Hypokalemia should be corrected before starting the drug, in addition, it is necessary to monitor the clinical picture, electrolyte balance and ECG. In neuroleptic-induced extrapyramidal syndrome, anticholinergic drugs should be used instead of dopaminergic agonists.

Influence on the ability to drive motor vehicles and manage mechanisms:  during the treatment period, it is necessary to refrain from engaging in potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Form of production

Solution for intravenous and intramuscular use

Storage conditions

Store in a dry place protected from light at a temperature not exceeding 25°C.

Shelf life

3 years

Active ingredient

Tiaprid

Conditions of release from pharmacies

By prescription

Dosage form

solution for injection and infusion

Purpose

Children over 6 years of age, Adults by doctor’s prescription, Children by doctor’s prescription