Acute and chronic psychoses in schizophrenia, especially those with symptoms of impaired activity. Chronic alcohol psychosis, psychosomatic disorders. Depressive disorder when other antidepressants are ineffective or their use is impossible. Migraine and dizziness of various etiologies (including Meniere's disease). Supportingly in the treatment of alcohol addiction.
A neuroleptic from the group of benzamide derivatives. It exhibits both antipsychotic and antidepressant effects. Sulpiride has some properties in common with classical neuroleptics - antagonism towards Dopamine receptors in the brain. The differences include: no cataleptic effect in therapeutically effective doses, no effect on the metabolic turnover of noradrenaline and serotonin, insignificant effects on anticholinesterase activity, lack of action on muscarinic receptors and GABA receptor. Sulpiride stimulates the secretion of prolactin, improves blood flow and secretion of mucus in the mucous membrane of the stomach and duodenum, has an anti-emetic effect. Sulpiride is slowly absorbed from the gastrointestinal tract, reaching Cmax after 3-6 h. Presence of food reduces absorption by about 30%. The bioavailability of the drug is low (27-34%) and depends on inter-individual differences. The drug is quickly distributed in the tissues; it penetrates the blood-brain barrier to a small extent. It binds about 40% of plasma proteins. T0,5 in the blood is 8-9 hours; in patients with severe renal impairment it is prolonged up to 20-26 h after intravenous administration. It is excreted in the urine and faeces, mainly unchanged.
Contraindications:
Hypersensitivity to the active substance or to any of the excipients. Phaeochromocytoma (diagnosed or suspected diagnosis). acute porphyria. Tumors associated with excessive prolactin secretion (eg pituitary adenoma, breast cancer). Concomitant use of levodopa. Breast-feeding.
Precautions:
Special care should be taken in patients with Parkinson's disease, due to the risk of extrapyramidal disorders and akathisia. Use with caution in patients with unstable epilepsy and patients with a history of seizures; with risk factors predisposing to ventricular arrhythmias, incltorsade de pointes (with congenital QT prolongation, cardiovascular disease predisposing to QT prolongation, bradycardia, electrolyte disturbances, major hypokalemia - it should be evened out and in patients treated simultaneously with other drugs that may cause bradycardia, hypokalemia, conduction of conduction in the myocardium or prolongation of the interval QT); at risk of stroke; with renal insufficiency (dosage modification is necessary); Elderly. In the phase of aggression or agitation, small doses of the drug may exacerbate symptoms. Caution should be exercised in the event of hypomania. In patients with aggressive or stimulatory behaviors accompanied by impulsivity, sulpiride may be used with a sedative medicine. As with the use of other neuroleptics, a neuroleptic malignant syndrome may occur - in the event of syndrome symptoms or high fever with an unexplained cause, sulpiride should be discontinued. Use with caution in patients with risk factors for developing venous thrombosis or risk of stroke. The drug is not indicated for the treatment of dementia related disorders. The product contains lactose - should not be used in patients with rare hereditary galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose.
Pregnancy and lactation:
Pregnancy is not recommended. In neonates exposed to antipsychotics (including amisulpride), during the third trimester of pregnancy, side effects may occur, including extrapyramidal disorder and / or withdrawal symptoms. We observed agitation, increased tension, decreased tension, tremor, drowsiness, respiratory distress syndrome or feeding disorders. Therefore, newborns should be carefully monitored.Sulpiride is excreted in breast milk, therefore breast-feeding is not recommended.
Side effects:
Common: calming or drowsiness. Rarely: extrapyramidal symptoms, acute dyskinesia, tardive dyskinesia (rhythmic involuntary movements primarily of the tongue and / or facial muscles) observed after long-term treatment - anticholinergic anti-parkinsonian drugs are ineffective in such cases and may even exacerbate symptoms, neuroleptic malignant syndrome, rotational movements eyeball, spastic torticollis, ostracods. Very rare: increased liver enzymes, maculopapular rash. Frequency unknown: hyperprolactinemia, lack of menstruation, gynecomastia, sexual frigidity, impotence, mumps (outside the feeding period), orthostatic hypotension, excessive salivation, neuroleptic malignant syndrome, weight gain; no cases of venous thrombosis, including cases of deep vein thrombosis, have been reported with antipsychotics. Individual cases:torsade de pointes,lengthening of the QT, neonatal withdrawal syndrome.
Dosage:
Orally.Schizophrenia. Adults: the starting dose is 400-800 mg / day in 2 divided doses (morning and early evening), depending on the symptoms. Patients who predominate positive symptoms (thinking disorders, hallucinations, delusions, senseless actions) are recommended for higher doses: initially at least 400 mg 2 times a day, and if necessary - higher. The maximum daily dose is 1200 mg. Only in the case of refractory disorders, the daily dose can be increased up to 1600 mg, administered in divided doses. In patients who predominate negative symptoms (depression, speech depression - retardation, lack of reactivity, listlessness, and depression), lower doses are recommended: initially 400 mg twice daily, and dose reduction to 200 mg twice daily increases the effect of stimulating sulpiride. Patients with mixed symptoms (positive and negative, without dominating one of them) usually react to 400-600 mg given twice a day.Depressive disorders: the initial dose is between 50-150 mg / day. The dose is then increased to 150-300 mg / day.Psychosomatic disorders, neuroses: usually 150-300 mg / day.Migraine and dizziness: usually 50-200 mg / day.Special groups of patients. There is no need to change the dosage in elderly patients. In patients with impaired renal function, depending on the degree of renal function, the dose should be reduced or the interval between doses should be lengthened. Use in children under 14 years is not recommended (no clinical data available).Way of giving. The preparation should be administered in divided doses, at least 1 hour before or 2 h after a meal. Antacids and sucralfate reduce the absorption of sulpiride - the preparation should be used 2 hours before administration of these drugs.
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