Thiapridal, tablets 100 mg 20 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 h in women and 3.6 h in men.

It is 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 decrease in excretion correlates with the value of Cl creatinine. Daily dose in creatinine Cl less than 20 ml/min should be decreased twice, in creatinine Cl less than 10 ml/min – 4 times.

Indications

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

Active ingredient

Thiapride

Composition

Active ingredient:

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

Auxiliary substances:

mannitol,

microcrystalline cellulose,

povidone,

colloidal silicon dioxide,

magnesium stearate.

How to take, the dosage

The drug in tablet form is prescribed only to adults and children over 6 years of age.

If the patient’s condition allows, treatment should start with a low dose of the drug, then gradually increasing it. The lowest effective dose should always be chosen.

Correction of psychomotor agitation and aggressive states, especially in chronic alcoholism: the drug is prescribed to adults in a dose of 200-300 mg/, the course of treatment is 1-2 months. In elderly patients, 50 mg 2; the dose may be gradually increased by 50-100 mg every 2-3 days to a maximum daily dose of 300 mg.

Chorea, Gilles de la Tourette syndrome: adults are prescribed 300-800 mg/; treatment should start with a dose of 25 mg/, then slowly increase it until the minimum effective dose is reached. Children over 6 years of age are prescribed 3-6 mg/kg/

In intense chronic pain syndrome, adults are usually prescribed at a dose of 200-400 mg/

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

Interaction

Not recommended combinations

• When used in conjunction with class 1a (quinidine, hydroquinidine, disopyramide) and class III (amiodarone, sotalol, dofetilide, ibutilide) antiarrhythmic drugs, some neuroleptics (thioridazine, chlorpromazine, levomepromazine, trifluoperazine, cyamemazine, sulpiride, amisulpride, pimozide, haloperidol, droperidol) and other drugs such as bepridil, cisapride, difemanil, erythromycin, misolastin, vincamine, increase the risk of ventricular arrhythmias as well as atrial fibrillation.
• Alcohol
  Alcohol increases the sedative effects of neuroleptics.
• Levodopa
  A joint antagonism of levodopa and neuroleptics is observed. In patients with Parkinson’s disease, minimum effective doses of levodopa and thiapride are recommended.
• Dopaminergic agonists may cause or exacerbate psychotic disorders. If neuroleptic treatment is necessary in a patient with Parkinson’s disease receiving a dopaminergic drug, the dose of the latter should be gradually reduced until withdrawal (abrupt withdrawal may lead to the development of a malignant neuroleptic syndrome).
• Sparfloxacin, moxifloxacin:
  The risk of ventricular arrhythmias as well as atrial fibrillation is increased. If the combination cannot be avoided, the QT interval should be checked first and an ECG should be provided.

Combinations requiring caution

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

Combinations to consider

• Antihypertensive drugs (all):
  Additive effect, increased risk of postural hypotension.
• Drugs that depress CNS function:
  Morphine derivatives (analgesics, anti-cough drugs, and substitution agents); barbiturates; benzodiazepines and other anxiolytics; sleeping pills; antidepressants with sedative effects; HI antihistamines with sedative effects; central-action antihypertensive agents; baclofen; thalidomide contribute to increased CNS function depression.

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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.

Tiapride 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 interval C).

Hypokalemia should be corrected prior to initiation of the drug; in addition, clinical, electrolyte balance and ECG should be monitored. 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.

Because 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 pregnancy, neurological function monitoring of the neonate is warranted.

Breastfeeding

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

Similarities

Thiapride