Thiapride, tablets 100 mg 20 pcs

Pharmacotherapeutic group

Antipsychotic medicine (neuroleptic)

ATX code

N05AL03

Pharmacodynamics: Antipsychotic drug (neuroleptic); has sedative sedative analgesic effect. It eliminates dyskinesia of central origin. It has a pronounced analgesic effect both for interoceptive and exteroceptive pain. Antipsychotic effect is caused by blockade of dopamine 02-receptors of mesolimbic and mesocortical system. Sedative action is caused by blockade of adrenoreceptors of reticular formation of brain stem; antiemetic action – by blockade of dopamine 02-receptors of trigger zone of vomiting center; hypothermic action – by blockade of dopamine receptors of hypothalamus.
Pharmacokinetics: After oral administration of 200 mg tiapride, the maximum concentration of the drug in plasma !3 mcg/ml is reached in 1 hour.

The bioavailability of the tablets is 75%. When taken immediately before meals the bioavailability is increased by 20% and the maximum concentration in plasma by 40%. Absorption in the elderly slows down.

Distribution in the body is fast (less than 1 hour). It penetrates through the blood-brain barrier and there is no cumulation through the placenta. The drug penetration into milk was noted in animals with the ratio of concentrations in milk to blood 1:2.

Binding with plasma proteins and erythrocytes is weak. Thiapride metabolism is very low: 70% of the dose is found unchanged in urine. The plasma elimination half-life is 29 hours in women and 36 hours in men. Excretion occurs mainly with urine and renal clearance reaches 330 ml/minute.

Indications

In adults: Psychomotor agitation and aggressive states especially in chronic alcoholism or in old age.

Intense chronic pain syndrome.

In adults and children over 6 years of age: Various types of chorea Gilles de la Tourette syndrome.

In children over 6 years: Behavioral disorders with agitation and aggression.

Active ingredient

Thiapride

Composition

1 tablet contains:

Active ingredient – 111.1 mg thiapride hydrochloride (in terms of thiapride base – 100.0 mg).

Excipients: lactose monohydrate (milk sugar) – 46.4 mg potato starch – 8.0 mg. povidone (polyvinylpyrrolidone low molecular weight medical) – 1.8 mg. magnesium stearate – 2.7 mg.

How to take, the dosage

Only for adults and children over 6 years.

It is always necessary to choose the minimum effective dose. If the patient’s condition allows it, the treatment should begin with a low dose and then gradually increase it.

Psychomotor agitation and aggressive states especially in chronic alcoholism or elderly:

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 up to the maximum daily dose of 300 mg.

Chorea syndrome of Gilles de la Tourette In adults: 300 – 800 mg/day.

The treatment should be begun with the dose – 25 mg per day and then slowly increased until the minimum effective dose is achieved.

– In patients with impaired renal function: if creatinine clearance is less than 20 ml/min the daily dose of the preparation should be adjusted according to the severity of renal failure: half dose is used in creatinine clearance 11-20 ml/min and a quarter dose in creatinine clearance 10 ml/min.

In children over 6 years of age: 3-6 mg/kg/day

Intense chronic pain syndrome.

The usual dose for adults is 200 – 400 mg/day.

Behavioral disorders with agitation and aggression in children over 6 le g – the dose is 100 – 150 mg/day.

Interaction

When used in conjunction with antiarrhythmic drugs, the risk of ventricular arrhythmias and atrial fibrillation may increase.

Alcohol increases the sedative effect of neuroleptics.

Joint antagonism of levodopa and neuroleptics is observed. In patients suffering from Parkinson’s disease it is recommended to use minimal effective doses of levodopa and tiapride.
Dopaminergic agonists may cause or aggravate psychotic disorders. If neuroleptic treatment is necessary for a patient with Parkinson’s disease receiving dopaminergic drugs the dose of the latter should be gradually reduced until withdrawal (abrupt withdrawal may lead to development of malignant neuroleptic syndrome).

Drugs that cause bradycardia and hypokalemia combined with thiapride may increase the risk of ventricular arrhythmias and atrial fibrillation. Co-administration with antihypertensive agents increases the risk of postural hypertension. Drugs depressing central nervous system functions when combined with tiapride increase the depressant effect.

Special Instructions

Malignant neuroleptic syndrome: Malignant neuroleptic syndrome is characterized by pallor hyperthermia muscle rigidity peripheral nervous system dysfunction 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.

Lengthening of the OT interval: Thiapride causes a dose-dependent lengthening of the Q G interval. This effect is known to increase the risk of serious ventricular arrhythmias and is increased against the background of bradycardia with hypokalemia and in case of congenital or acquired long QT interval (combination with drugs prolonging QTc interval).

Hypokalemia should be corrected before the start of the drug except goju. Clinical monitoring of electrolyte balance and electrocardiogram should be ensured.
In extrapyramidal syndrome caused by neuroleptics anticholinergic drugs should be administered instead of dopaminergic agonists.

During the treatment it is necessary to refrain from potentially dangerous activities that require high concentration and rapid psychomotor reactions.
Impact on the ability to operate vehicles and vehicles: During the treatment it is necessary to refrain from potentially dangerous activities that require high concentration and rapid psychomotor reactions.

Contraindications

• High sensitivity to thiapride or other drug components.
• Diagnosed or suspected prolactin-dependent tumors such as pituitary prolactinoma and breast cancer.
• Diagnosed or suspected pheochromocytoma.
• In combination with sultopride.
• Pregnancy (first trimester).
• Lactation period.
• Child age (under 6 years).
• Hypertensive crisis.
• Developed renal and/or hepatic insufficiency.
• In combination with dopaminergic agonists (amantadine. apomorphine. bromocriptine cabergoline entacapone lisuride pergolide piribedil pramiexol quinagolide ropinirole) except in patients with Parkinson’s disease.
• In combination with drugs that may cause cardiac arrhythmias: Class 1a antiarrhythmic drugs (quinidine hydroquinidine disopyrampd) and Class III drugs (amiodarone sotalol dofetilide ibutilide) some neuroleptics (thioridazine chlorpromazine levomepromazine trifluoperazine cyamemazine amisulpride sulpiride pimozide haloperidol droperidol) and with the following drugs: levodopa bepridil cisapride diphemanil erythromycin misolastin intravenous vincamine sparfloxacin moxifloxacin. (See “Interaction with other medicinal products”)

Cautions:

• Cronic renal insufficiency. When used, the dose should be reduced and monitoring should be increased (see. Dosage and administration);
• Epilepsy due to the possibility of lowering the seizure threshold; Cardiovascular disease in decompensation;
• Parkinson’s disease;
• Combined use of drugs containing alcohol;
• In the elderly with bradycardia (less than 55 beats.
• Hypokalemia congenital prolongation of QT interval as well as co-administration of drugs capable of causing significant bradycardia (less than 55 bpm) hypokalemia, decreased cardiac conduction or prolongation of QT interval.
  

Side effects

• Asthenia fatigue
• Sleepiness
• Drowsiness
• Antisy
• Parkinson’s syndrome: tremor increased blood pressure bradykinesia. Hypersalivation.
• Significantly less common: Early dyskinesia and dystonia (spastic torticollis oculogyric tricism) akathisia.

These symptoms are usually reversible after withdrawal of the drug or administration of anticholinergic anti-Parkinsonian agents.

Late dyskinesia (stereotypic involuntary facial and limb tongue movements) occurring with prolonged use (anticholinergic antiparkinsonian agents prescribed as correctors may worsen the patient’s condition).

Hyperprolactinemia and associated disorders (less than 02%): amenorrhea galactorrhea swollen breasts breast pain impotence or ejaculation disorders

Increased body weight

QT interval prolongation

Atrial fibrillation

Postural hypotension

Malignant neuroleptic syndrome.

Overdose

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

Treatment: withdrawal of the drug gastric lavage (if poisoned with pills)
symptomatic and detoxification therapy monitoring of vital body functions (especially cardiac activity (risk of QT interval prolongation) until symptoms of intoxication completely disappear. If severe extrapyramidal symptoms appear – anticholinergic treatment.

Since thiapride is poorly dialyzed to remove the substance, hemodialysis is not recommended. The antidote for thiapride is unknown.

Pregnancy use

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

No data is 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, monitoring the neurological functions of the newborn is warranted.

Breastfeeding

It is unknown whether thiapride penetrates into breast milk so breastfeeding should be stopped while taking the drug.

Similarities

Tiaprid, Tiapridal