Disorders of behavior in elderly patients with dementia. Disturbances during alcohol withdrawal: acute delirium syndrome, withdrawal syndrome. Severe form of Huntington's chorea.
Composition:
1 tabl contains 100 mg of thiapride (as hydrochloride).
Action:
Atypical neuroleptic drug, independent of adenylyl cyclase activity. It works by selectively blocking the dopaminergic subtype D receptors2 and D3. Has low affinity to the subtype D receptors1. It has an anxiolytic effect (the mechanism of this action has not yet been established, however it differs from the mechanism of antidopaminergic activity). Has a positive effect on vigilance in elderly patients. The oral bioavailability of thiapride is 75% (increased by 20% if the drug is administered before a meal), Cmax It is achieved in about 1 hour. It is not bound to plasma proteins. It is metabolized to a small extent and excreted mainly in unchanged form (70%) with urine. T0,5 in the elimination phase, it is 2.9 hours in women and 3.6 hours in men.
Contraindications:
Hypersensitivity to thiapride or to any of the excipients. Prolactin-dependent neoplasms (eg pituitary adenoma prolactinoma and breast cancer). Phaeochromocytoma tumor. Concomitant use with levodopa or other dopaminergic drugs.
Precautions:
Special care should be taken in patients with risk factors for QT prolongation (such as bradycardia <55 beats / min, electrolyte disturbances, especially hypokalemia, congenital QT prolongation, family history of QT prolongation, concomitant use of medications that may cause significant bradycardia, electrolyte abnormalities, conduction abnormalities in the heart or prolongation of the QT interval); with risk factors for stroke; with Parkinson's disease; with history of epilepsy (the possibility of lowering the convulsive threshold); with renal insufficiency (dosage modification is necessary); in old age (risk of sedation); in children (limited data on the effect of the drug in this age group). Before initiating therapy with thiapride and during treatment, all possible risk factors for venous thromboembolism should be identified and appropriate preventive measures should be taken. If symptoms of malignant neuroleptic syndrome or hyperthermia of unknown cause occur, thiapride should be discontinued.
Pregnancy and lactation:
Use with extreme caution in pregnancy. Animal studies do not indicate direct or indirect harmful effects with respect to pregnancy, embryonal / fetal development, parturition or postnatal development, however, clinical data on pregnant women are limited. In women who used high doses of neuroleptics during pregnancy, extrapyramidal symptoms may occur after delivery. If tiapride is given at the end of pregnancy, especially at high doses, atropine-like symptoms may occur, especially when combined with antiparkinsonian medications (tachycardia, over-stimulation, abdominal distension, delayed meconium excretion) and sedation. Extrapyramidal disturbances and / or withdrawal symptoms were observed in newborns whose mothers used antipsychotics in the third trimester of pregnancy: agitation, increased or decreased tension, tremor, drowsiness, respiratory distress syndrome or feeding disorders - newborns should be carefully monitored. Breastfeeding during treatment with thiapride is not recommended. The use of thiapride may cause hyperprolactinemia, with accompanying lack of menstruation, lack of ovulation and fertility disorder, resulting from the interaction with dopaminergic receptors.
Side effects:
Common: dizziness, headache, tremor, increased tension, hypokinesia, drooling, lethargy, drowsiness, insomnia, agitation, lethargy, asthenia, tiredness.Uncommon: anxiety, dystonia (cramps, torticollis, bouts of forced looking up, lockjaw), increase in plasma prolactin (which disappears after discontinuing thiapride, this may be the cause of mellitus, amenorrhea, gynecomastia, breast enlargement and pain, orgasm and impotence disorders), weight gain. Rare: severe dyskinesia. Frequency unknown: tardive dyskinesia, neuroleptic malignant syndrome (which may result in death), QT interval prolongation,torsade de pointesventricular tachycardia (which may lead to ventricular fibrillation or cardiac arrest and sudden death), venous thromboembolism (including pulmonary embolism and deep vein thrombosis), hypotension (usually orthostatic). In elderly patients with dementia who received antipsychotics, there was an approximately 3-fold increase in the risk of stroke and a slightly increased risk of death compared to the untreated group.
Dosage:
Orally. The lowest effective dose should be used. Treatment should be started with a low dose, which should be increased gradually, depending on the patient's clinical condition.Disorders of behavior in elderly patients with dementia200-400 mg / day. Treatment should be started at 50 mg twice daily. Then the dose should be increased by 50-100 mg, at intervals of 2-3 days. The average dose in elderly patients is 300 mg / day. The maximum recommended dose is 400 mg / day.Behavioral disorders during alcohol withdrawal: 300-400 mg / day for 1-2 monthsHuntington's chorea300-1200 mg / day. Initial dose: up to 1200 mg / day, given in at least 3 divided doses. The dose should then be gradually reduced to the maintenance dose, depending on the patient's response.Children aged> 6 years: the usual dose is 100-150 mg / day; up to 300 mg / day.Special groups of patients. Patients with impaired renal function - creatinine clearance (CCr) 30-60 ml / min: administered 75% of the usual dose; CCr 10-30 ml / min: give 50% of the usual dose; CCr <10 ml / min: administer 25% of the usual dose. There is no need to reduce the dose in patients with hepatic impairment. The drug can be taken with or without food.