Amisulpride - instructions for use, dose, side effects, contraindications

Clinical and pharmacological group: & nbsp

Neuroleptics

Included in the formulation

Limipranil

pills inwards

AKTAVIS GROUP, AO Iceland

Limipranil

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AKTAVIS GROUP, AO Iceland

Solian®

solution inwards

Sanofi-Aventis France France

Solian®

pills inwards

Sanofi-Aventis France France

АТХ:

N.05.A.L.05 Amisulpride

Pharmacodynamics:

Competitive blockade of postsynaptic dopamine (D2 / D3) receptors in the limbic structures of the brain.

Pharmacological effects

Antipsychotic. Antidepressant (at a dose of 400-800 mg / day).

Pharmacokinetics:

F - 48%. The connection with plasma proteins is 16%. Biotransformation in the liver. T1 / 2 - 12 hours Cl - 330 ml / min. Elimination of the kidneys unchanged.

Indications for use and dosing

Schizophrenia (at 50-1200 mg / day), accompanied by a pronounced productive (delusions, hallucinations, thought disorders) and / or negative (affective flattening, lack of emotion and avoiding intercourse) disorders, including patients with a predominance of negative symptoms - for 50-300 mg / day (300 mg / day). In acute psychotic episodes - 400-1200 mg / day (400-800 mg / day)

Indications:

Acute and chronic schizophrenia, accompanied by a pronounced productive (delusions, hallucinations, thought disorders) and / or negative (affective flattening, lack of emotion and avoiding intercourse) disorders in patients with predominantly negative symptoms.

ICD-10

V.F20-F29.F20 Schizophrenia

V.F20-F29.F21 Chrysotile disorder

V.F20-F29.F22 Chronic delusional disorders

V.F20-F29.F23 Acute and transient psychotic disorders

V.F20-F29.F25 Schizoaffective disorder

V.F20-F29.F29 Inorganic psychosis, unspecified

Contraindications:

Hypersensitivity. Concomitant prolactin-dependent tumor (prolactinoma of the pituitary gland and breast cancer). Pheochromocytoma. Severe chronic renal failure (CC <10 mL / min).

Concomitant administration of sultopride, dopamine agonists (amantadine, apomorphine, bromocriptine, cabergoline, entacapone, lizard, pergolide, piribedil, pramipexole, quinagolide, ropinirol, selegiline), except for patients with Parkinson's disease.

Children's age (up to 14 years). Breastfeeding.

Carefully:

With caution should be used for epilepsy, parkinsonism, renal failure. In elderly patients, because of the possible development of arterial hypotension or excessive sedation, use with caution.

In Parkinson's disease, when prescribing antidopaminergic drugs and amisulpride, caution is necessary because of possible deterioration of the condition. Amisulpride It should be used only if neuroleptic therapy can not be avoided.

Pregnancy and lactation:

Pregnancy

FDA recommendation category C.

Lactation

There is no information on the penetration into breast milk. Do not apply!

Dosing and Administration:

Inside:

Depending on the indications and the course of the disease, the daily dose varies from 50 mg to 1200 mg. Amisulpride in a dose of more than 400 mg / day taken in 2 divided doses.

Supportive treatment is set individually at the level of minimum effective doses.

In case of renal insufficiency, the dose for patients with QC from 30 to 60 ml / min should be reduced to 1/2, with KK from 10 to 30 ml / min - up to 1/3.

Use in children

Acute psychotic episode. 15-18 years: 2 times a day; the maximum daily dose is 1.2 g.

Schizophrenia, negative symptoms. 15-18 years: 50-300 mg / day; in a dose of 300 mg - once a day.

Doses in excess of 400 mg / day should be given in 2 divided doses.

Renal failure: with QC 30-60 ml / min dose is reduced by half, with KK 10-30 ml / min - one-third.

Side effects:

Insomnia, anxiety, agitation, extrapyramidal symptoms (tremor, increased blood pressure, hypersalivation, akathisia, hypokinesia), hyperprolactinaemia (galactorrhea, amenorrhea, gynecomastia, breast engorgement, impotence, frigidity). Drowsiness. Constipation, nausea, vomiting, dry mouth, increased activity of liver enzymes (mainly transaminases), acute dystonia (including spasmodic torticollis,oculogic crises, trismus), tardive dyskinesia (involuntary movements of the tongue and facial muscles), convulsions, malignant neuroleptic syndrome, lowering of arterial pressure, bradycardia, lengthening of the interval Q-TA2, atrial fibrillation, allergic reactions.

Overdose:

Drowsiness, sedation, coma, lowering of arterial pressure, extrapyramidal symptoms.

Treatment is symptomatic; monitoring of vital body functions (including cardiac activity due to the risk of prolonging the Q-T interval). When developing extrapyramidal symptoms - anticholinergic drugs. There is no specific antidote. Hemodialysis is ineffective.

Interaction:

β-Adrenoblockers, diltiazem, verapamil, clonidine, guanfacine, foxglove preparations - bradycardia, increased risk of pirouette ventricular arrhythmia.

Antihypertensive drugs - increased their hypotensive effect and increased risk of orthostatic hypotension.

Diuretics, laxatives, amphotericin, glucocorticoids, tetracosactide, neuroleptics (pimozide, haloperidol), antidepressants (imipramine), lithium preparations - hypokalemia, increased risk of pirouette ventricular arrhythmia.

Levodopa is a mutual antagonism between the action of levodopa and amisulpride.

Antiarrhythmic agents of Ia class (quinidine, disopyramide), Class III (amiodarone, sotalol), bepridil, cisapride, sultopride, thioridazine, erythromycin (for intravenous administration), wincamine (for intravenous administration), halofantrine, pentamidine, sparfloxacin - increased risk of pirouette ventricular arrhythmia.

The drugs that oppress the central nervous system (opioid analgesics, hypnotics, tranquilizers, clonidine, antitussives of central action, alcohol), - intensification of their oppressive action.

Special instructions:

Before using the drug, you need to correct hypokalemia.

With the development of hyperthermia the drug must be canceled.

It is possible to reduce the convulsive threshold, so patients with epilepsy in a history require constant observation during treatment. Taking the drug causes a dose-dependent increase in the duration of the Q-T interval, which increases the risk of developing serious ventricular arrhythmias (especially in the presence of bradycardia, hypokalemia, existing congenital or acquired Q-T interval prolongation).Prior to the appointment of amisulpride and during treatment, it is recommended to monitor factors that may contribute to the development of this rhythm disturbance (bradycardia less than 55 per minute, hypokalemia, congenital prolongation of the QT interval, simultaneous use of drugs that cause pronounced bradycardia, hypokalemia, conduction retardation or QT interval prolongation) .

During the treatment period, it is necessary to refrain from engaging in potentially dangerous activities that require a high concentration of attention and speed of psychomotor reactions.

Amisulpride is effective in schizophrenia, causes fewer extrapyramidal adverse reactions than typical neuroleptics. Efficacy with negative symptoms is not proven. The drug is less expensive than new atypical antipsychotics, but direct comparative studies have not been conducted.

Motor disorders during treatment with amisulpride are much less pronounced than with typical antipsychotics. The need for antiparkinsonian drugs is also significantly reduced compared to that of typical neuroleptics

In the treatment of schizophrenia, amisulpiride, risperidone, olanzapine and quetiapine the same performance, but require long-term studies evaluating the various outcomes and quality of life, to judge the comparative effectiveness of atypical antipsychotics. Amisulpride (50 mg / day) with comparable sertraline (50-100 mg / day) of treatment efficacy dysthymia.

It is not represented in the United States Pharmacopeia.

Instructions

Amisulpride (Amisulpridum)