Distribution in the body is rapid (less than 1 h). It penetrates through the blood-brain barrier and the placenta without accumulation. The volume of distribution is clinical equipoise. Animals in drug penetration mentioned milk with a ratio of concentrations in milk and blood of 1.2.
It binds to plasma proteins, weakly binds to red blood cells. Tiapride metabolized slightly (to 15%), largely inactive metabolites. Not found conjugated metabolites. 70% of the injected dose detected in the urine unchanged. Half-life in plasma after intramuscular injection of 2.9 hours in women and in men 3.6 hours. Selection is primarily by the kidneys by glomerular filtration and tubular secretion, renal clearance is 330 ml / minute.
In patients with impaired renal function selection tiapride it depends on creatinine clearance, while reducing the excretion of the drug which slows .
Tiapride slightly removed from the blood by dialysis (11 ± 7 mg) for 4 hours following intramuscular administration in a dose of 100 mg.
Indications for use:
– Relief of psychomotor agitation and clinical equipoise aggressive states, especially in chronic alcoholism, or the elderly.
– Thrust intense pain.
– Hypersensitivity to tiaprid or to other components of the preparation.
– Diagnosed or suspected prolactin-dependent tumors, such as prolactinoma pituitary gland and breast cancer.
– Pheochromocytoma, suspected pheochromocytoma.
– Parkinson’s disease (except in cases of urgent need for tiapride).
– Children and adolescence (for this dosage form).
– Co-administration of levodopa (see “Interaction with other medicinal products.”).
– Simultaneous treatment with cabergoline, quinagolide (see “Interaction with other medicinal products.”).
– In patients with predisposing factors for clinical equipoise the development of arrhythmias (with bradycardia less than 55 beats per minute; with impaired electrolyte balance, particularly with hypokalemia, hypomagnesemia, congenital QT prolongation, with drugs concomitant therapy, capable of causing severe bradycardia (less than 55 beats per minute), violations of electrolyte balance, to slow intracardiac conduction, or prolong the QT interval, as tiaprid may prolong the QT interval and increase the risk of serious ventricular arrhythmias, including the development of ventricular tachycardia type “pirouette” (see. “Interactions with other medicinal products” “Special instructions”).
– in conjunction with dopaminergic antiparkinsonian drugs (amantadine, apomorphine, bromocriptine, entacapone, lisuride, pergolide, piribedil, ropinirole, selegiline) in patients with Parkinson’s disease, if there is an urgent need to apply tiapride (see “Interaction. with other drugs “,” Special instructions “).
– patients severe cardiovascular disease (because of the potential gain of ischemic disorders in blood pressure reduction).
– in the elderly (increased risk of sedation, orthostatic hypotension).
– in elderly patients with dementia (see. “Special Instructions”).
– Patients with the “Special Instructions” risk factors for stroke (see).
– In patients with renal failure clinical equipoise.
– Patients with epilepsy (neuroleptics can reduce the epileptogenic threshold, although this effect in tiapride not studied).
– patients with risk factors for thromboembolism ( “Cautions” see.).
– During pregnancy (see ‘pregnancy and lactation’.).
– When concomitant use of drugs containing ethanol (see. “Interaction with other medicinal products”).