Thiapridal, 50 mg/ml 2 ml 12 pcs

Tiapridal is neuroleptic, anxiolytic, analgesic.

It selectively blocks central dopamine D₂ receptors without affecting D₁ receptors.

Pharmacodynamics

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

Pharmacokinetics

After an intravenous injection of 200 mg C_max (2.5 mcg/mL) is determined after 30 minutes, after 200 mg oral administration (1.3 mcg/mL) after 1 hour. Bioavailability is 75% (taking immediately before meals increases bioavailability by 20%, C_max by 40%). Absorption in the elderly is delayed.

Distribution is quick: in 1 hour it is determined in many tissues and organs, passes through BBB and placental barrier, penetrates into breast milk (concentration in milk is half of that in blood plasma). Practically does not bind with plasma proteins, erythrocytes. T_1/2 is 2.9 hours in women and 3.6 hours in men. It is moderately metabolized: 70% of the dose taken is found unchanged in urine.

The excretion is mainly by the kidneys; Cyl is 330 ml/minute. In patients with impaired renal excretory function the degree of decrease in excretion correlates with the value of Cl creatinine. Daily dose in creatinine Cl less than 20 ml/min should be reduced by half, in creatinine Cl less than 10 ml/min – by 4 times.

Indications

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

Active ingredient

Composition

Active substance:

Tiapride hydrochloride 111.1 mg, corresponding to 100 mg of tiapride base;

Auxiliary substances:

sodium chloride,

water for injection.

How to take, the dosage

For intramuscular or intravenous administration. The drug is only used in adults. The minimum effective dose should always be chosen. If the patient’s condition allows, treatment should be started with a low dose, then gradually increasing it.

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

In the delirium syndrome or pre-delirium state: adults 400-1200 mg/day (up to a maximum of 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.

Interaction

Not recommended combinations

Combinations requiring caution

Combinations to consider

Special Instructions

Malignant neuroleptic 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 blood pressure lability, may precede the onset of hyperthermia and, therefore, represent early, warning signals. Some risk factors, such as dehydration or organic brain damage, although this effect of neuroleptics can be explained by idiosyncrasy, appear to be predisposing. Thiapride causes dose-dependent prolongation of the QT interval.

This effect is known to increase the risk of serious ventricular arrhythmias and is increased with bradycardia, hypokalemia, and congenital or acquired long QT interval (combination with drugs that prolong the QT C interval). Hypokalemia should be corrected before starting the drug administration; in addition, control of the clinical picture, electrolyte balance and ECG should be ensured. In extrapyramidal syndrome caused by neuroleptics, anticholinergic drugs should be administered instead of dopaminergic agonists.

Impact on the ability to drive and operate machinery: during treatment it is necessary to refrain from potentially dangerous activities requiring increased concentration and rapid psychomotor reactions.

Contraindications

Hypersensitivity, pheochromocytoma (including suspected), pregnancy, breastfeeding.

Side effects

In long-term use of Tiapridal in high doses, somnolence, muscle hypotonia, dyskinesia (early – spastic, torticollis, trismus, oculomotor disorders; and late), extrapyramidal symptoms, myorelaxation, decreased BP, amenorrhea, galactorrhea, hyperprolactinemia, gynecomastia, impotence, frigidity, weight gain, malignant neuroleptic syndrome (unexplained hyperthermia – requires drug withdrawal).

Overdose

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

Treatment: drug withdrawal, symptomatic and detoxification therapy, monitoring of vital body functions (especially cardiac activity – risk of QT interval prolongation) until symptoms of intoxication completely disappear. In case of severe extrapyramidal symptoms – anticholinergic treatment. Since thiapride is poorly dialyzed, hemodialysis is not recommended for removal of the substance. The antidote for thiapride is unknown.

Pregnancy use

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

There are no data available regarding the effect of neuroleptics used during pregnancy on the fetal brain (it is preferable not to use thiapride during pregnancy). However, if the drug is still used during pregnancy, it is recommended to limit the dose and duration of treatment if possible.

If prolonged treatment and/or high doses are used and/or in late gestation, monitoring of neurological function of the neonate is warranted.

Breastfeeding

It is not known whether thiapride penetrates into breast milk, so breastfeeding is prohibited.

Similarities