Tiaprid

General characteristics. Structure:

Active ingredient: 100 mg of a tiaprid in the form of a hydrochloride.

Excipients: sugar milk (lactose); potato starch; PVP low-molecular medical (povidone); magnesium stearate.

The drug possessing antipsychotic, antipsychotic, analgeziruyushchy, somnolent, sedative and anxiolytic action.

Pharmacological properties:

Pharmacodynamics. Antipsychotic means (neuroleptic) from group of the replaced benzamides. Antipsychotic action is caused by blockade dopamine D2 receptors of mesolimbic or mesocortical system. Has analgeziruyushchy effect at interoceptive and exteroceptive pain. Possesses the sedative action caused by blockade of adrenoceptors of a reticular formation of a trunk of a brain; the antiemetic action connected with blockade dopamine D2 receptors of a trigger zone of the emetic center; the hypothermal action caused by blockade of dopamine receptors of a hypothalamus.

Pharmacokinetics. After intake it is quickly absorbed from a GIT. Cmax in a blood plasma is reached in 1 h. Linkng with proteins of plasma low. Gets through GEB. T1/2 makes 3-4 h. It is removed by kidneys preferential in not changed look.

At a renal failure removal of a tiaprid from an organism is slowed down.

Indications to use:

Agitation, aggression, especially at an alcoholism, at elderly people; the steady against therapy, expressed pain syndrome; a chorea, tics at Turett's disease, the heavy behavior disorders which are followed by aggression and agitation.

Route of administration and doses:

Inside, only for adults and children 6 years are more senior. It is necessary to select a minimal effective dose always. If the condition of the patient allows, treatment should be begun with a low dose, gradually raising it.

Psychomotor excitement and aggressive states, especially at an alcoholism or at advanced age: adult — 200–300 mg/days, a course of treatment of 1-2 months; at advanced age — 50 mg 2 times a day. The dose can be increased gradually by 50–100 mg each 2–3 days to the maximum daily dose of 300 mg.

Chorea, Giles de la Tourett's syndrome: adult — 300–800 mg/days. Treatment it is necessary to begin 25 mg/days with a dose, then to slowly raise it to achievement of a minimal effective dose. At patients with a renal failure at creatinine Cl <20 ml/min., the daily dose of drug is established depending on weight of a renal failure. Apply 1/2 doses at Cl of creatinine 11–20 ml/min. and 1/4 doses at Cl of creatinine of 10 ml/min. To children 6 years — 3–6 mg/kg/days are more senior.

Intensive chronic pain syndrome: the usual dose for adults makes 200–400 mg/days.

Disorders of behavior with agitation and aggression at children are aged more senior than 6 years: the dose makes 100–150 mg/days.

Features of use:

With extra care apply at patients with epilepsy because of possible reduction of the threshold of convulsive readiness.

With care to apply at a serious cardiovascular illness, parkinsonism, a renal failure, and also at patients of advanced age.

Parenteral administration is carried out under control of the doctor.

During treatment tiapridy it is not necessary to apply a levodopa, agonists of dopamine receptors (амантадин, Apomorphinum, Bromocriptinum, каберголин, энтакапон, лизурид, перголид, piribedit, прамипексол, хинаголид), сультоприд; the medicines capable to cause arrhythmias like "pirouette" (antiarrhytmic means of I A and III classes, Chlorpromazinum, levomepromazinum, thioridazine, трифлуоперазин, сультоприд, Droperidolum, a haloperidol, Pimozidum, bepridit, цизаприд, difemanit, erythromycin for in/in introductions, Vincaminum for in/in introductions, and also галофантрин, морфлоксацин, pentamidine, спарфлоксацин).

Not to allow alcohol intake.

Influence on ability to driving of motor transport and to control of mechanisms. With care apply at patients whose activity demands concentration of attention and high speed of psychomotor reactions.

At pregnancy тиаприд apply only according to absolute indications in minimal effective doses. Newborns whose mothers at pregnancy received тиаприд are recommended to carry out monitoring of the TsNS and GIT functions.

It is unknown whether it is allocated тиаприд with breast milk. In need of use in the period of a lactation breastfeeding should be stopped.

Side effects:

From TsNS: drowsiness, sleep disorders, agitation, indifference, dizziness, headaches, parkinsonism syndrome; seldom - a spastic wryneck, okulogirny crises, an akathisia, late dyskinesia; in some cases - ZNS.

From endocrine system: seldom - the symptoms caused by a giperprolaktinemiya (an amenorrhea, a galactorrhoea, increase in mammary glands, mammary gland pains, impotence, disturbances of achievement of an orgasm.

From cardiovascular system: increase in an interval of QT, orthostatic hypotension; in some cases - arrhythmias like "pirouette".

Interaction with other medicines:

At simultaneous use of means, the oppressing TsNS (including opioid analgetics, antihistamines, barbiturates, benzodiazepines), strengthening of the oppressing influence on TsNS is possible.

At simultaneous use of anti-hypertensive means strengthening of hypotensive effect is possible.

Contraindications:

Existence or suspicion of prolaktinzavisimy tumors, pheochromocytoma; hypersensitivity to a tiaprid.

Overdose:

Symptoms: an acute or malignant antipsychotic syndrome (extrapyramidal frustration, a hyperthermia), disturbances of consciousness up to a coma.

Treatment: drug withdrawal and purpose of cholinolytic means, symptomatic therapy, plasma exchange.

Storage conditions:

To store in dry, protected from light and the place, unavailable to children, at a temperature not above 30 °C.

Issue conditions:

According to the recipe

Packaging:

30 pieces - banks of dark glass (1) - a pack cardboard.
30 pieces - banks polymeric (1) - packs cardboard.
10 pieces - planimetric strip packagings (3) - packs cardboard.