Soleron 100mg 30 tablets — Made in Ukraine — Free Delivery

Pharmacological properties

Pharmacodynamics. Amisulpride is an antipsychotic agent belonging to the class of substituted benzamides. amisulpride selectively, with high affinity binds to d2 / d3 subtypes of dopaminergic receptors. amisulpride has no affinity for serotonin, histamine, adrenergic and cholinergic receptors.

When used in high doses, it predominantly blocks dopaminergic neurons, which are localized in the mesolimbic structures, and not in the striatal system. This specific affinity explains the prevalence of the antipsychotic action of amisulpride over its extrapyramidal effects.

At low doses, it predominantly blocks presynaptic D2 / D3 receptors, which explains its effect on the negative symptoms of schizophrenia.

It is known that in a study involving patients with acute schizophrenia, amisulpride significantly reduced the severity of secondary negative symptoms of the disease to a much greater extent than haloperidol.

Pharmacokinetics. After taking amisulpride, two absorption peaks are noted: one is reached quickly, 1 hour after the dose, and the other is between the 3rd and 4th hours after administration. The plasma concentration is 39 ± 3 and 54 ± 4 ng / ml, respectively, after taking a dose of 50 mg.

The volume of distribution is 5.8 l / kg of body weight. Since the binding to blood plasma proteins is low (16%), interaction with other preparations is unlikely. The absolute bioavailability is 48%. Amisulpride is poorly metabolized in the body: two inactive metabolites have been identified, accounting for about 4% of the administered dose. Cumulation of amisulpride does not occur, its pharmacokinetics remains unchanged after repeated doses. T1 / 2 of amisulpride is approximately 12 hours after oral administration.

Amisulpride is excreted unchanged in the urine. Renal clearance is about 330 ml / min.

Food rich in carbohydrates (containing up to 68% liquid) significantly reduces the AUC, Tmax and Cmax of amisulpride in the blood. Such changes in these parameters were not observed after ingestion of fatty foods. The effect of these changes with amisulpride treatment is unknown.

Liver failure. Since amisulpride is slightly metabolized, there is no need to reduce the dose for patients with hepatic impairment.

Renal failure In patients with renal insufficiency, T½ does not change, while the systemic clearance decreases by 2.5–3 times. Amisulpride AUC doubles in mild renal failure, and almost 10 times in moderate renal failure. Practical experience is limited and there are no data on doses of 50 mg. Amisulpride is poorly dialyzable.

Elderly patients. The available pharmacokinetic data for patients aged 65 years and older indicate that after a single dose of 50 mg Cmax, T½ and AUC increase by 10-30%. There are no data on repeated doses.

Indications

Schizophrenia.

Application

Used internally.

If the daily dose does not exceed 400 mg, Soleron should be taken 1 time per day. Doses above 400 mg should be divided into 2 doses per day.

In acute psychotic episodes, the recommended initial dose is 400-800 mg, the maximum daily dose is no more than 1200 mg. The safety of doses above 1200 mg / day has not been sufficiently studied. In this regard, the preparation should not be used in such doses. The maintenance dose or dose adjustment must be set individually, in accordance with the patient's response. Supportive treatment is carried out in the minimum effective dose, which is set individually.

For patients with predominantly negative symptoms, it is recommended to prescribe the preparation in a dose of 50 (½ tablet 100 mg) to 300 mg / day. The dose is selected individually. The optimal dose is about 100 mg / day.

Elderly patients. The safety of amisulpride in elderly patients was assessed in a limited number of patients. This preparation should be used with extreme caution in this subgroup of patients, given the risk of hypotension and sedation. In patients with renal insufficiency, a dose reduction of the preparation may also be required (see SPECIAL INSTRUCTIONS).

Impaired renal function. Since the excretion of amisulpride is carried out by the kidneys, in case of impaired renal function for patients with creatinine clearance of 30-60 ml / min, the daily dose should be reduced by half, and for patients with creatinine clearance of 10-30 ml / min - to 1/3.

Due to insufficient data on the use of amisulpride in patients with severe renal failure (creatinine clearance 10 ml / min), it is recommended to carefully monitor the health status of such patients.

Liver dysfunction. Since the preparation is poorly metabolized in the body, it is not required to reduce its dose in case of impaired liver function.

Contraindications

Hypersensitivity to the active substance or any component of the preparation. diagnosed or suspected pheochromocytoma, since severe cases of ag have been described in patients with pheochromocytoma who have used antidopaminergic preparations, including some benzamides. diagnosed or suspected prolactin-dependent tumors such as prolactin-secreting pituitary adenoma and breast cancer. use in combination with levodopa (see interactions). combination with medicines that can lead to torsades de pointes (see interactions). in combination with mechitazine, citalopram, escitalopram, non-antiparkinsonian dopamine agonists (cabergoline, quinagolide).

Side effects

They are classified by frequency according to this scale: very often (≥1 / 10), often (≥1 / 100, 1/10), infrequently (≥1 / 1000, 1/100), rarely (≥1 / 10,000, 1/1000), very rare (1/10 000), the frequency is unknown (cannot be determined from the available data).

In some cases, it can be difficult to distinguish between side reactions and symptoms of the underlying disease.

From the nervous system: very often - extrapyramidal symptoms (including tremor, rigidity, hypertonicity, hypersalivation, akathisia, hypokinesia, dyskinesia). The intensity of these symptoms is usually mild, they are partially reversible without discontinuation of the preparation when anticholinergic antiparkinsonian therapy is prescribed. The incidence of dose-dependent extrapyramidal symptoms is very low in patients taking the preparation at a dose of 50–300 mg / day to eliminate predominantly negative symptoms; often - daytime sleepiness; acute dystonia (spastic torticollis, oculogyric crisis, trismus), which does not require discontinuation of the preparation and disappears with the use of anticholinergic antiparkinsonian preparations; infrequently - tardive dyskinesia, characterized by involuntary movements mainly of the tongue and / or facial muscles, usually develops with prolonged use of the preparation (anticholinergic antiparkinsonian preparations are ineffective in this case, they can cause an increase in symptoms); convulsions; frequency unknown - neuroleptic malignant syndrome, sometimes fatal.

Mental disorders: often - insomnia, anxiety, agitation, frigidity; frequency unknown - confusion.

Endocrine disorders: often - a reversible increase in the level of prolactin in the blood plasma (disappears after discontinuation of the preparation), which can lead to galactorrhea, amenorrhea, gynecomastia, swelling of the mammary glands, erectile dysfunction.

Metabolic disorders: often - an increase in body weight; infrequently - hyperglycemia; frequency unknown - hypertriglyceridemia and hypercholesterolemia.

From the digestive system: often - constipation, nausea, vomiting, dry mouth.

From the side of the cardiovascular system: often - arterial hypotension; infrequently - bradycardia; frequency unknown - lengthening of the Q – T interval on the ECG; fibrillation-flutter-type ventricular arrhythmias and ventricular tachycardia, which can lead to ventricular fibrillation and cardiac arrest; sudden death (see SPECIAL INSTRUCTIONS). Venous thromboembolism (VTE), including pulmonary embolism (sometimes fatal) and deep vein thrombosis, has been observed with antipsychotics.

From the hepatobiliary system: often - an increase in the activity of liver enzymes, mainly transaminases.

From the immune system: infrequently - allergic reactions.

On the part of the skin and subcutaneous tissues: the frequency is unknown - urticaria, angioedema.

From the side of the blood and lymphatic system: the frequency is unknown - leukopenia, neutropenia, agranulocytosis.

Others: neonatal withdrawal syndrome.

Special instructions

Malignant neuroleptic syndrome. As with the use of other antipsychotics, during treatment with Solleron, the development of a malignant neuroleptic syndrome (which can lead to fatal consequences) is possible, characterized by hyperthermia, muscle stiffness, dysfunction of the peripheral nervous system, impaired consciousness, and an increased level of CPK in the blood plasma. with the development of hyperthermia, especially when used in high doses, all antipsychotic preparations, including Solleron, should be canceled.

Elongation of the Q – T interval. Amisulpride can cause a dose-dependent lengthening of the QT interval on the ECG, which increases the risk of dangerous ventricular tachyarrhythmias such as ventricular fibrillation-flutter. The risk of developing dangerous ventricular arrhythmias increases with bradycardia, hypokalemia, in the case of congenital or acquired syndrome of prolonged Q – T interval (combination with preparations that lengthen the Q – T interval).

If the clinical situation allows, then before using the preparation, it is recommended to make sure that there are no factors that can contribute to the development of this rhythm disturbance: bradycardia 55 beats / min, hypokalemia, congenital prolonged Q-T interval, simultaneous use of preparations that can cause severe bradycardia (55 beats ./min), hypokalemia, slowing of intracardiac conduction or lengthening of the Q – T interval (see CONTRAINDICATIONS, INTERACTIONS). Patients who require long-term treatment with antipsychotics are recommended to conduct an ECG study before their appointment.

Cerebral stroke. There is evidence that elderly patients with dementia who have been treated with some atypical antipsychotics have an increased risk of stroke. The mechanism for this increased risk is unknown. It is possible that there is an increased risk associated with other antipsychotics, and for other populations of patients. If patients have a risk factor for cerebral stroke, this preparation should be used with caution.

Elderly patients with dementia. Elderly people with dementia-related psychosis and those taking antipsychotics are at increased risk of death.

The results of studies carried out in patients who used mainly atypical antipsychotics showed that, compared with placebo, the risk of death increased by 1.6-1.7 times. Although the causes of death in clinical trials with atypical antipsychotics varied, the majority of deaths were either cardiovascular (eg, heart failure, sudden death) or infectious (eg, pneumonia) etiology. Available evidence suggests that traditional antipsychotics can increase mortality in the same way as atypical antipsychotics. The role of antipsychotics and the characteristics of the patient's body in increasing mortality remains unclear.

VTE. With the use of antipsychotic preparations, cases of VTE have been reported. Since patients taking antipsychotic preparations often have acquired risk factors for VTE, possible risk factors for VTE should be determined before starting treatment with Soleron or during such therapy, and preventive measures should be taken.

Mammary cancer. Amisulpride can increase prolactin levels. In this regard, it is necessary to prescribe amisulpride to patients with a personal or family history of breast cancer with caution, and careful monitoring is necessary during therapy with this preparation.

Hyperglycemia. Cases of hyperglycemia or impaired glucose tolerance, development or exacerbation of diabetes have been reported in patients treated with certain atypical antipsychotics, including amisulpride (see SIDE EFFECTS). It is necessary to carry out clinical and laboratory monitoring in accordance with the current recommendations in patients receiving treatment with Soleron. Particular attention should be paid to patients with diabetes mellitus or with risk factors for the development of diabetes mellitus. If hyperglycemia associated with the use of the preparation is detected, it is necessary to consider discontinuing the preparation.

Convulsions. Amisulpride can lower the seizure threshold, therefore, medical supervision of patients taking Soleron with a history of seizures is necessary.

Special patient groups. Since the excretion of amisulpride is carried out by the kidneys, in case of impaired renal function, the dose should be reduced or another treatment should be considered (see APPLICATION). There are no data available for patients with severe renal impairment.

In the elderly, Soleron, like other antipsychotics, should be used with extreme caution because of the risk of arterial hypotension or sedation. For such patients, it may be necessary to reduce the dose of the preparation due to impaired renal function.

It is necessary to use Soleron with extreme caution in Parkinson's disease, as it can worsen the course of the disease. Amisulpride should be used only if it is impossible to avoid treatment with antipsychotics.

Withdrawal syndrome. After abrupt withdrawal of high-dose antipsychotics, cases of withdrawal have been reported. The development of involuntary movement disorders (such as ataxia, dystonia, dyskinesia) has been reported. In this regard, the gradual abolition of amisulpride is advisable.

Other. With the use of antipsychotics, including amisulpride, the development of leukopenia, neutropenia, agranulocytosis was reported. An increase in body temperature or the presence of an infection of unknown etiology may indicate leukopenia (see SIDE EFFECTS) and require immediate hematological examination.

It is not recommended to use this preparation in combination with alcohol, dopaminergic antiparkinsonian preparations, antiparasitic preparations that can provoke torsades de pointes; with methadone, levodopa, antipsychotics, or preparations that can provoke torsades de pointes (see INTERACTIONS).

The preparation contains lactose, therefore it is not recommended for use in patients with lactase deficiency, galactosemia, or glucose or galactose malabsorption syndrome.

Use during pregnancy and lactation. Pregnancy. It is known that amisulpride has not shown reproductive toxicity in animal studies. There was a decrease in fertility associated with the pharmacological effects of preparations (effect mediated by prolactin). Its teratogenic effect was not noted either.

Clinical data on the use of amisulpride during pregnancy are limited. Accordingly, the safety of its use during pregnancy has not been established, therefore, the use of the preparation is not recommended, except in cases where the advantage outweighs the risk. If amisulpride is used during pregnancy, neonates may experience side effects of amisulpride. When used in the third trimester of pregnancy in newborns, adverse reactions may occur, such as extrapyramidal symptoms and / or withdrawal symptoms, which may vary in severity and duration. Adverse reactions such as agitation, hypertonicity, hypotension, tremors, drowsiness, respiratory distress, or difficulty feeding have been reported. In this regard, careful monitoring of the condition of newborns is necessary.

Lactation. It is not known whether amisulpride passes into breast milk, so breastfeeding is contraindicated.

Children. The safety and efficacy of using amisulpride for the treatment of children aged 15 years and older have not been established; data on the use of amisulpride in adolescents with schizophrenia are limited. Therefore, the use of amisulpride in children over the age of 15 is not recommended, for children under 15 years of age, it is contraindicated.

The ability to influence the reaction rate when driving or working with other mechanisms. Patients, especially those who drive a car or other mechanisms, should be warned about the risk of drowsiness in connection with the use of this preparation (see SIDE EFFECTS).

Interactions

Contraindicated combinations. preparations that can cause pirouette ventricular tachycardia:

• class Ia antiarrhythmics such as quinidine, disopyramide;
• class III antiarrhythmics such as amiodarone, solatol;
• other preparations such as bepridil, cisapride, sultopride, thioridazine, methadone, i.v. erythromycin, i.v. vincamycin, halofantrine, pentamidine, sparfloxacin.

Levodopa: mutual antagonism between levodopa and antipsychotics. Contraindications regarding the simultaneous use of levodopa with amisulpride is based only on the pharmacological action of both compounds: both act on dopamine receptors; thus, reciprocal antagonism of both compounds could lead to potential ineffectiveness of these preparations.

Combinations not recommended. Amisulpride can increase the effect of alcohol on the central nervous system.

Preparations  that increase the risk of developing pirouette ventricular tachycardia or may prolong the Q – T interval:

• preparations that induce bradycardia, such as β-adrenergic receptor blockers, calcium channel blockers that induce bradycardia, such as diltiazem and verapamil, clonidine, guaifenesin; digitalis preparations;
• preparations that induce hypokalemia: hypokalemic diuretics, stimulating laxatives, intravenous amphotericin B, glucocorticoids, tetracosactide. Hypokalemia must be corrected;
• antipsychotics such as pimozide, haloperidol; imipramine antidepressants; lithium.

Combinations to consider. CNS depressants, including narcotics, analgesics, sedative antihistamine H1 receptor blockers, barbiturates, benzodiazepines and other anxiolytics, clonidine and derivatives.

Antihypertensive preparations and other antihypertensive preparations.

Overdose

To date, there are few data regarding acute overdose of amisulpride. the registered signs and symptoms are mainly the result of an increase in pharmacological activity, which is clinically manifested by dizziness, drowsiness, sedation, arterial hypotension, extrapyramidal symptoms, coma. there have been reports of lethal cases with the use of amisulpride, mainly with simultaneous use with other psychotropic preparations.

The specific antidote for amisulpride is unknown.

In case of acute overdose, it is necessary to determine whether another preparation was used at the same time, and to take appropriate measures: supportive therapy, monitoring of vital body functions, especially monitoring of cardiac activity (danger of prolongation of the Q-T interval) until the patient's condition is completely normalized. When pronounced extrapyramidal symptoms appear, anticholinergics are prescribed. The use of hemodialysis is not effective because amisulpride is poorly dialyzed.

Storage conditions

In its original packaging at a temperature not exceeding 25 ° C.