Index of drugs

Treatment of acute and chronic schizophrenia with positive symptoms (such as delusions, hallucinations, thinking disorders, hostility, distrust) and / or negative symptoms (such as dull feelings, emotional and social withdrawal).

1 tabl contains 50 mg or 200 mg, 1 tablet powl. contains 400 mg amisulpride. The preparations contain lactose.

A neuroleptic from the group of benzamides. Amisulpride binds selectively to the dopaminergic subtype D receptors₂ and D₃to which it has high affinity. It does not show affinity for subtype D receptors₁, D₄ and D₅. It does not show affinity for serotonin, α-adrenergic, histamine H receptors, which is typical of other neuroleptics₁ neither cholinergic. In high doses, it more strongly blocks Dopamine receptors in the structures of the limbic system than in the striatum. The drug used in low doses preferentially blocks presynaptic D-receptors₂ and D₃, which results in the release of dopamine and the phenomenon of "disinhibition". The pharmacological properties mentioned above determine the efficacy of amisulpride in both the treatment of negative and positive symptoms of schizophrenia. After oral administration, amisulpride exhibits 2 absorption peaks: one occurs rapidly - about 1 hour after drug administration, the other - between 3 and 4 hours after drug intake. The drug is slightly bound to plasma proteins (16%). The absolute bioavailability is 48%. Amisulpride is only slightly metabolised, 2 inactive metabolites have been identified, representing approximately 4% of the total dose of the drug. The drug does not accumulate in the body, and its pharmacokinetic parameters remain unchanged after repeated dosing. T_0,5 Amisulpride is about 12 hours. The drug is excreted in the urine in unchanged form. The elimination half-life increases in patients with renal insufficiency, while renal clearance decreases by 2.5-3 times.

Hypersensitivity to amisulpride or any of the excipients. Do not use in patients with prolactin-dependent tumors, e.g. pituitary adenomaprolactinoma and breast cancer. Phaeochromocytoma tumor. Severe renal failure (creatinine clearance <10 ml / min). Simultaneous treatment with levodopa and medicines that may cause severe arrhythmia (QT interval prolongation,torsades de pointes): Class I and III anti-arrhythmic drugs (quinidine, disopyramide, mexiletine, flecainide, propafenone, Amiodarone, sotalolol), bepridil, cisapride, sultopride, thioridazine, methadone, intravenous Erythromycin, intravenous vinkaamine, halofantrine, pentamidine, sparfloxacin, imidazole drugs antifungals. Children <18 years. Breastfeeding period.

As with the use of other neuroleptics, it is possible for a neuroleptic malignant syndrome to occur, manifested by hyperthermia, muscle stiffness, autonomic nervous system dysfunction, variable consciousness, and increased serum creatine kinase activity; if hyperthermia occurs, especially after high daily doses, the drug should be discontinued. Special care should be taken in patients with Parkinson's disease, as amisulpride may increase the symptoms of the disease - the drug can only be used when neuroleptic treatment is necessary. Amisulpride causes a dose-dependent prolongation of the QT interval (which may increase the risk of severe ventricular arrhythmias, such astorsades de pointes; before starting treatment it is advisable to make sure that there are no factors that may be conducive to this type of disorder (bradycardia <55 heart beats per minute, electrolyte imbalance, especially hypokalemia and hypomagnesaemia, congenital QT prolongation, and concomitant treatment with products that may cause bradycardia, hypokalemia, release of conduction in the myocardium or prolongation of the QT interval). Caution should be used in patients with an increased risk of stroke (elderly patients have an increased risk of cerebrovascular events).Cases of venous thromboembolism during treatment with antipsychotics have been reported. Patients treated with these medicines often have acquired risk factors for thromboembolism and should be identified and preventive measures taken prior to treatment. Because of the risk of hyperglycaemia, patients with diabetes or those at increased risk of diabetes should be monitored regularly for the duration of treatment. Amisulpride may lower the seizure threshold; Patients with a history of epilepsy should be closely monitored during treatment. In patients with renal insufficiency (with a creatinine clearance = 10-60 ml / min), the dose should be reduced. It is not recommended in elderly patients (> 65 years) - the risk of hypotension or excessive sedation. Due to the risk of withdrawal symptoms and the recurrence of psychotic symptoms and the occurrence of movement disorders, it is recommended to gradually discontinue the drug. The drug contains lactose; should not be used in patients with rare hereditary galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose.

Do not use during pregnancy unless clearly necessary. If amisulpride is used during pregnancy, side effects may be expected in the newborn, therefore it should be monitored for extrapyramidal disorders and / or withdrawal symptoms (which may change depending on the severity of the course and duration of labor to be delivered) , agitation, increased or decreased tension, tremor, drowsiness, respiratory distress syndrome or feeding disorders. Fertility reduction was observed, which was related to the pharmacological effect of amisulpride on prolactin secretion. You should not breast-feed during treatment.

Very common: extrapyramidal symptoms, eg tremor, stiffness, hypokinesia, increased salivary secretion, akathisia, dyskinesia (these symptoms at the optimal doses are usually light and partly disappear after using the anti-Parkinsonian medicine without interrupting amisulpride). Common: weight loss, hypotension; drowsiness, dizziness, acute dystonia (tics or cramps in the neck, eyes or jaw muscles - they disappear without interrupting treatment with amisulpride after the anticholinergic anti-parkinsonism drug); gastrointestinal disorders such as constipation, nausea, vomiting, dry mouth; increased serum prolactin (which may be the cause of mellitus, amenorrhea or menstrual disorders, gynecomastia, pain or breast enlargement, benign prolactin-secreting pituitary tumor and impotence) - resolving after discontinuation of amisulpride; insomnia, anxiety, agitation, orgasm disorders. Uncommon: increased liver enzymes, in particular aminotransferases; bradycardia; usually after long-term treatment, tardive dyskinesia characterized by involuntary movements of primarily the tongue and / or facial muscles (no anti-parkinsonian medication should be used as it may increase the symptoms of the disease), convulsions; hyperglycemia; allergic reactions. Rare: symptoms after a sudden discontinuation of treatment with high doses of the drug, such as: nausea, vomiting and insomnia, recurrence of psychotic symptoms, movement disorders (akathisia, dystonia, dyskinesia). Very rare: QT prolongation and cases of ventricular arrhythmias (torsade de pointes) and ventricular tachycardia (which may lead to ventricular fibrillation, cardiac arrest and death); malignant neuroleptic syndrome. Not known: neonatal withdrawal syndrome, venous thromboembolism.

Orally.Positive symptoms: 400-800 mg / day; in individual cases the dose can be increased up to 1200 mg / day. Do not use higher doses than 1200 mg / day (no data on safety of use). In patients with both positive and negative symptoms, the dose should be adjusted to achieve optimal control of the positive symptoms. Maintenance treatment should be determined individually, giving the lowest effective dose.Negative symptoms50-50 mg / day. Amisulpride in a dose not exceeding 300 mg / day can be used in one dose. Doses over 300 mg should be given in several doses.It is not recommended for elderly patients (> 65 years). In patients with renal insufficiency where the creatinine clearance is 30-60 ml / min - the dose should be halved; in patients with a creatinine clearance of 10-30 ml / min - the dose should be reduced to 1/3; in patients with severe renal impairment (creatinine clearance <10 ml / min), the preparation should not be used. There is no need to modify the dose in case of liver dysfunction. The tablets can be administered with or without food, with sufficient amount of liquid. The tablets should not be chewed. The tablets can be divided into halves.