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Composition:


active ingredient: amisulpride;


1 tablet contains amisulpride 100 mg or 200 mg;


excipients: lactose, monohydrate; microcrystalline cellulose; methylcellulose; sodium starch glycolate (type a); magnesium stearate.


Dosage form. Pills.


Basic physical and chemical properties:


- 100 mg tablets: white or almost white round flat tablets with a diameter of approximately


8.0 mm, with a distribution risk on one side and A100 embossed on the other side;


- 200 mg tablets: white or almost white round flat tablets with a diameter of approximately 11.0 mm, with a dividing line on the other side and an embossed A200 on the other side .


Pharmacotherapeutic group.


Antipsychotic drugs. ATX code N05A L05.


Pharmacological properties.


Pharmacodynamics.


Its pharmacodynamic properties are characterized by selective and predominant affinity for the D2 and D3 receptors of the limbic system, while they do not have affinity for the D1 subtypes D4 and D5. Amisulpride has no affinity for serotonin receptors and other neuroreceptors, such as histamine H1 receptors, cholinergic and adrenergic receptors. In addition, amisulpride does not bind to Sigma sites. In high-dose animal studies, amisulpride mainly blocks dopaminergic neurons of the mesolimbic system compared to those of the Striate system. In low doses, amisulpride blocks mainly presynaptic dopaminergic receptors D2 and D3, which explains its effect on negative symptoms. This pharmacological profile explains the clinical efficacy of Solex® against both negative and positive symptoms of schizophrenia.


Pharmacokinetics.


In the human body, amisulpride shows two Maxima of absorption: the first occurs quickly, 1 hour after the dose is applied, and the second – after 3-4 hours.


The corresponding plasma concentrations after taking a dose of 50 mg are 39 ± 3 and 54 ± 4 ng/mL.


The volume of distribution is 5.8 l/kg, binding to plasma proteins is low (16 %), interaction with other drugs associated with proteins is unlikely. Absolute bioavailability is 48%.


Amisulpride is poorly metabolized: two inactive metabolites were identified, which account for about 4% of the total amount of the drug used.


Amisulpride does not accumulate in the body, and its pharmacokinetics remain unchanged after repeated doses.


The elimination half-life after oral administration is approximately 12 hours.


Amisulpride is excreted unchanged in the urine.


Renal clearance is approximately 20 L/h or 330 mL / min.


Carbohydrate-rich food (containing 68% liquid) significantly reduces the AUC, Tmax, Cmax of amisulpride, and after eating fatty foods, no changes are noted. The effect of these changes during treatment with amisulpride is unknown.


Liver failure.


Since amisulpride is poorly metabolized, there is no need to reduce the dose for patients with hepatic insufficiency.


Kidney failure.


In patients with renal insufficiency, the elimination half–life does not change, while systemic clearance decreases by 2.5-3 times.


The AUC of amisulpride in mild renal failure is doubled, and in moderate renal failure – almost 10 times.


Practical experience, however, is limited, and there are no data on doses exceeding 50 mg.


Amisulpride is very poorly dialyzed.


Elderly patients.


Available pharmacokinetic data for patients over 65 years of age indicate that Cmax, T1/2, and AUC increase by 10-30% after a single 50 mg dose. There are no data on repeated doses.


Clinical characteristics.


Indications.


Treatment of schizophrenia.


Contraindications.


- Hypersensitivity to the active substance or to another component of the drug.


- Serious episodes of hypertension have been reported in patients with pheochromocytoma who have taken anti-dopaminergic drugs, including certain benzamides. It is advisable to refrain from prescribing this medicine to patients with diagnosed or suspected pheochromocytoma who have taken anti-dopaminergic drugs, including certain benzamides.


- Prolactin-dependent tumors, such as prolactin-secreting pituitary adenoma and breast cancer, have been identified or suspected.


- In combination with mechitazine, citalopram, escitalopram, domperidone, hydroxyzine, non-protiparkinsonian dopaminergic drugs (cabergoline, quinagolide). Use in combination with levodopa (see the section "interactions with other drugs and other types of interactions").


- Children under 15 years of age (due to lack of clinical data).


- Combination with drugs that may cause torsades de pointes (see the section "interactions with other drugs and other types of interactions").

Interactions with other drugs and other types of interactions.


Sedatives. It should be borne in mind that many drugs or substances can cause additive depressing effects on the central nervous system (CNS) and contribute to reduced attention. These drugs include morphine derivatives (analgesics, antitussives, and drug addiction replacement agents), neuroleptics, barbiturates, benzodiazepines, non-benzodiazepine anxiolytics (such as meprobamate), sleeping pills, sedative antidepressants (amitriptyline, Doxepin, mianserin, mirtazapine, trimipramine), sedative H1-antihistamines, central-acting antihypertensive agents, baclofen and thalidomide.


Drugs that can cause torsades de pointes. This serious arrhythmia can be caused by the use of a variety of medications, such as antiarrhythmic and other medications. Predisposing factors include hypokalemia (see "drugs that reduce potassium"), bradycardia (see "drugs that slow the heart rate"), or pre-existing congenital or acquired prolongation of the QT interval. 


This is especially true for class IA and Class III antiarrhythmic drugs, as well as some antipsychotics. This effect is also caused by other compounds that do not belong to these classes.


For dolasetron, erythromycin, spiramycin, and vincamine, this interaction applies only to intravenous dosage forms.


In general, the use of a drug that causes torsades de pointes, together with another drug that has the same effect, is contraindicated.


However, some of these drugs are exceptions, as their use cannot be avoided, and therefore they are simply not recommended for use in combination with drugs that can cause torsades de pointes. This applies to methadone, antiparasitic agents (halofantrine, lumefantrine, pentamidine) and antipsychotics.


However, these exceptions do not include citalopram, escitalopram, domperidone and hydroxyzine, and therefore their use together with all drugs that can induce torsades de pointes is contraindicated.


Combinations are contraindicated (see the section "contraindications").


Dopamine agonists, with the exception of antiparkinsonian agonists (cabergoline, quinagolide, Rotigotine). Mutual antagonism of the effects of dopamine agonists and neuroleptics.


Citalopram, escitalopram, domperidone, hydroxyzine. Increased risk of ventricular arrhythmias, especially torsades de pointes.


Mechitazine. Increased risk of ventricular arrhythmias, especially torsades de pointes.


Non-recommended combinations (see the section "application features").


Antiparasitic agents that can cause torsades de pointes (chloroquine, halofantrine, lumefantrine, pentamidine). Increased risk of ventricular arrhythmias, particularly torsades de pointes. If possible, discontinue treatment with one of the two medications. If this combination cannot be avoided, pre-treatment QT monitoring and ECG monitoring are recommended.


Dopaminergic antiparkinsonian agents (amantadine, apomofin, bromocriptine, Entacapone, lysuride, pergolide, piribedil, pramipexole, rasagiline, ropinirole, Rotigotine, selegiline, tolcapone). Mutual antagonism of the effects of dopamine agonists and neuroleptics. Dopamine agonists can cause or worsen psychotic disorders. When the use of a neuroleptic drug is necessary for a patient suffering from Parkinson's disease and taking dopamine agonists, it is necessary to gradually reduce the dose of dopamine agonists, and then cancel the use of the drug (abrupt withdrawal of dopaminergic drugs threatens the development of neuroleptic malignant syndrome).


Other drugs that may induce torsades de pointes: class IA antiarrhythmic drugs (quinidine, hydroquinidine, disopyramide) and Class III antiarrhythmic drugs (amiodarone, dronedarone, sotalol, dofetilide, ibutilide), as well as other drugs such as Arsen compounds, bepridil, cisapride, difemanil, dolasetron intravenously, domperidone, erythromycin intravenously, levofloxacin, mechitazine, mizolastine, prucaloprid, VINCAMINE intravenously, moxifloxacin, sparfloxacin, spiramycin intravenously, thioridazine, vandetanib, toremifen. Increased risk of ventricular arrhythmias, particularly torsades de pointes.


Other antipsychotics that may induce torsades de pointes (chlorpromazine, ciamemazine, droperidol, flupentixol, flufenazine, haloperidol, levomepromazine, pimoside, pipamperone, pipotiazine, sertindol, sulpiride, sultoprid, thiaprid, zuclopentixol). Increased risk of ventricular arrhythmias, particularly torsades de pointes.


Alcohol consumption. Alcohol increases the sedative effect of antipsychotics. Amisulpride may increase the effect of alcohol on the central nervous system. Reduced attention can make driving and working with mechanisms dangerous. It is necessary to avoid the use of alcoholic beverages and the use of medicines containing alcohol.


Levodopa. Mutual antagonism of the effects of levodopa and neuroleptics. Patients with Parkinson's disease should use the minimum effective doses of each of these medications.


Methadone. Increased risk of ventricular arrhythmias, particularly torsades de pointes.


Sodium oxybutyrate. Increased CNS depression. Reduced attention can lead to danger when driving vehicles and working with other mechanisms.


Combinations that require taking precautions.


Anagrelide. Increased risk of ventricular arrhythmia, especially torsades de pointes. During the simultaneous use of this drug, clinical and electrocardiographic monitoring is required.


Azithromycin, clarithromycin, ciprofloxacin, levofloxacin, norfloxacin, roxithromycin. Increased risk of ventricular arrhythmias, especially torsades de pointes. With the simultaneous use of these drugs, clinical and ECG monitoring is necessary.


Beta-blockers in patients with heart failure (bisoprolol, carvedilol, metoprolol, Nebivolol). Increased risk of ventricular arrhythmias, especially torsades de pointes. In addition, there is a vasodilating effect and the risk of hypotension, especially orthostatic (additive effect). Clinical and ECG monitoring is required.


Drugs that slow the heart rate (especially class IA antiarrhythmic drugs, beta blockers, some class III antiarrhythmic drugs, some calcium channel blockers, digitalis preparations, pilocarpine, anticholinesterase drugs). Increased risk of ventricular arrhythmias, especially torsades de pointes. Clinical and ECG monitoring is required.


Drugs that reduce potassium concentrations (diuretics that remove potassium, alone or in combination, stimulating laxatives, glucocorticoids, tetracosactides and intravenous amphotericin B). Increased risk of ventricular arrhythmias, particularly torsades de pointes. Any hypokalemia should be corrected before starting treatment with amisulpride, and the clinical picture, electrolyte balance, and ECG should be monitored.


Lithium. Risk of neuropsychiatric signs indicating neuroleptic malignant syndrome or lithium poisoning. Regular clinical monitoring and monitoring of laboratory tests are indicated, especially at the beginning of simultaneous use of these drugs.


Ondansetron. Increased risk of ventricular arrhythmia, especially torsades de pointes. During the simultaneous use of this drug, clinical and electrocardiographic monitoring is required.


Roxithromycin. Increased risk of ventricular arrhythmias, especially torsades de pointes. With the simultaneous use of these drugs, clinical and ECG monitoring is necessary.


Combinations to take into account.


Other sedatives. Increase depression of the central nervous system. Impaired ability to concentrate can make driving vehicles and working with mechanisms dangerous.


Antihypertensive agents. Increased risk of hypotension, particularly postural hypotension.


Nitrate derivatives and related substances. Increased risk of hypotension, especially postural hypotension.


Orlistat. Risk of reducing the therapeutic effect with simultaneous use of Orlistat.

Application features.


Special warnings.


Neuroleptic malignant syndrome.


As with the use of other neuroleptics, it is possible to develop a malignant neuroleptic syndrome, which can lead to death, characterized by hyperthermia, muscle rigidity, dysfunction of the peripheral nervous system, impaired consciousness, and increased CPK levels. If hyperthermia develops, especially when using high doses, all antipsychotic drugs should be discontinued.


Prolongation of the QT interval.


Solex® may cause dose-dependent prolongation of the QT interval on the electrocardiogram, which increases the risk of serious ventricular arrhythmias, such as torsades de pointes.


The risk of serious ventricular arrhythmias increases with bradycardia, hypokalemia, in the case of congenital or acquired prolonged QT interval (combination with drugs that prolong the QT interval) (see the section "adverse reactions").


If the clinical situation allows, before using the drug, it is recommended to make sure that there are no factors that can contribute to the development of this rhythm disorder, such as, for example:


- bradycardia less than 55 beats / min;


- electrolyte imbalance, in particular hypokalemia;


- congenital extended QT interval;


- the use of drugs that can cause severe bradycardia ( 55 beats/min), hypokalemia, decreased cardiac conduction or prolongation of the QT interval (see the section "contraindications").


Patients who need long-term treatment with antipsychotics should have an ECG before starting treatment.


Brain stroke.


Randomized placebo-controlled clinical trials involving elderly patients with dementia who were treated with certain atypical antipsychotics showed an increased risk of developing cerebral stroke compared to placebo.


The mechanism underlying this increased risk is unknown. The presence of an increased risk associated with other antipsychotic drugs and the presence of a risk to other patient populations cannot be excluded. Patients with a risk factor for brain stroke should use this medicine with caution.


Elderly patients with dementia.


The risk of death increases in elderly patients suffering from dementia-related psychosis and taking antipsychotic medications.


An analysis of 17 placebo-controlled clinical trials (average duration – 10 weeks) conducted among patients taking mainly atypical antipsychotics showed that the risk of death increased 1.6–1.7 times compared to placebo in patients treated with these drugs.


After treatment lasting an average of 10 weeks, the risk of death was 4.5% in the treated patients, compared to 2.6% in the placebo group.


Although the causes of death during clinical trials conducted with atypical antipsychotics were different, most deaths were either from cardiovascular (e.g., heart failure, sudden death) or infectious (e.g., pneumonia) causes.


Epidemiological studies show that traditional antipsychotics can increase mortality, as with atypical antipsychotics.


The corresponding role of antipsychotics and individual characteristics of the patient in increasing mortality during epidemiological studies remained unknown. Solex® is not licensed to treat dementia-related behavioral disorders.


Venous thromboembolism.


Cases of venous thromboembolism (VTE), sometimes fatal, have been reported with the use of antipsychotics. Since patients treated with antipsychotics often have acquired risk factors for VTE, before starting treatment with Solex® or against the background of such treatment, possible risk factors for VTE should be identified and preventive measures taken (see the section "adverse reactions").


Hyperglycemia / metabolic syndrome.


Cases of hyperglycemia have been reported in patients treated with certain antipsychotic medications, including amisulpride (see Section "adverse reactions").


It is necessary to conduct clinical and laboratory monitoring in accordance with current recommendations in patients receiving treatment with Solex®. Special attention should be paid to patients with diabetes mellitus or with factors in the development of diabetes.


Convulsions.


Amisulpride may lower the seizure threshold. Therefore, patients with a history of seizures should be carefully monitored during amisulpride therapy.


Special groups of patients.


Since amisulpride is eliminated by the kidneys, for patients with renal insufficiency, its dose should be reduced or other treatment should be considered (see the section "dosage and administration"). There are no data on patients with severe renal insufficiency (see the section "dosage and administration").


Like other antipsychotic medications, amisulpride should be used with extreme caution in elderly patients due to the possible risk of sedation and hypotension. It may also be necessary to reduce the dosage due to renal failure.


As with other anti-dopaminergic agents, caution should be exercised when prescribing amisulpride to patients with Parkinson's disease, as it can cause the disease to worsen. Amisulpride should only be used if it is impossible to avoid treatment with neuroleptics.


Withdrawal symptoms.


Withdrawal symptoms described after abrupt discontinuation of high-dose antipsychotic medications, including nausea, vomiting, and insomnia, were very rarely described after sudden discontinuation of high-dose antipsychotic medications. Relapses of psychotic symptoms may also occur. Involuntary movement disorders (such as akathisia, dystonia, and dyskinesia) have been reported with amisulpride. In this regard, it is advisable to gradually cancel amisulpride.


It is not recommended to use this medicine in combination with alcohol, dopaminergic antiparkinsonian agents, antiparasitic agents that can provoke torsades de pointes; with methadone, levodopa, other antipsychotics or drugs that can provoke torsades de pointes (see the section "interactions with other drugs and other types of interactions").


Hyperprolactinemia. Amisulpride may increase prolactin levels (see Section "adverse reactions"). Patients with hyperprolactinemia and/or a potentially prolactin-dependent tumor should be closely monitored during treatment with amisulpride (see Section "contraindications").


Warnings related to excipients.


This medicine contains lactose. Patients with rare hereditary problems such as galactose intolerance (galactosemia), lactase deficiency, or glucose or galactose absorption disorders should not take this medicine.


Breast cancer.


Solex® may increase prolactin levels. In this regard, amisulpride should be prescribed to patients with a personal or family history of breast cancer, and careful monitoring is necessary during therapy with this drug.


Benign pituitary tumor.


Amisulpride may increase prolactin levels. Cases of benign pituitary tumors, such as prolactinoma, have been observed during amisulpride therapy (see Section "adverse reactions"). In the case of very high prolactin levels or clinical signs of a pituitary tumor (such as visual field defect and headache), pituitary imaging should be performed. If the diagnosis of a pituitary tumor is confirmed, treatment with amisulpride should be discontinued (see the section "contraindications").

Dosage and administration.


If the daily dose does not exceed 400 mg, the drug should be taken 1 time a day.


A dose of more than 400 mg should be divided into 2 doses per day.


Acute psychotic episodes.


You can start treatment with intramuscular administration, which will last for several days, at a maximum dose of 400 mg/day, followed by switching to oral administration.


Doses from 400 mg/day to 800 mg/day are recommended to be administered orally. The maximum oral dose should not exceed 1200 mg/day. The safety of doses greater than 1200 mg/day has not been widely studied. In this regard, such doses should not be used.


The maintenance dose or dose adjustment should be set individually, according to the patient's response.


In all cases, maintenance therapy should be prescribed individually, at the level of the minimum effective dose.


Mostly negative episodes.


Recommended doses range from 50 mg/day to 300 mg/day. Doses should be selected individually. The optimal dose is about 100 mg/day.


Elderly patients.


Amisulpride should be used with extreme caution in patients in this population due to the risk of hypotension and sedation (see Section "contraindications"). In patients with renal insufficiency, it may also be necessary to reduce the dose of the drug.


Kidney failure.


Since amisulpride is excreted by the kidneys, in renal failure with a creatinine clearance of 30-60 mL/min, The Daily Dose should be reduced by half, and in renal failure with a creatinine clearance of 10-30 mL/min – up to a third. Due to insufficient data on patients with severe renal insufficiency (creatinine clearance 10 mL/min), strict monitoring of such patients is recommended (see Section "contraindications").


Impaired liver function.


Since the drug is poorly metabolized, no dose reduction is required.


Children.


The efficacy and safety of amisulpride when used between puberty and 18 years of age have not been established; data on the use of amisulpride in children with schizophrenia are limited. For this reason, the use of amisulpride in the period from puberty to 18 years is not recommended. Amisulpride is contraindicated in children under 15 years of age due to the lack of clinical data.


Overdose.


Currently, there are few data on acute overdose of amisulpride. Reported symptoms are mainly the result of increased pharmacological activity, which is clinically manifested in dizziness, sedation, coma, hypotension, and extrapyramidal symptoms.


There have been reports of fatal outcomes when used concomitantly with other psychotropic drugs.


The specific antidote to amisulpride is unknown. In case of acute overdose, it is necessary to determine whether another drug was used simultaneously, and take appropriate measures:


- careful monitoring of vital functions;


- monitoring of cardiac activity (risk of prolongation of the QT interval) until the patient fully recovers;


- in case of severe extrapyramidal symptoms, anticholinergic agents should be prescribed;


– since amisulpride is poorly dialyzed, the possibilities of hemodialysis to remove this drug compound are limited.


Adverse reactions.


Adverse events are classified by frequency according to the following scale: very common (≥1/10), common (≥1/100,


From the nervous system.


Very common: possible extrapyramidal symptoms (tremor, rigidity, hypertension, increased salivation, akathisia, hypokinesia, dyskinesia). In most cases, they are moderate at maintenance doses and partially reversible without discontinuation of amisulpride when prescribing anticholinergic antiparkinsonian agents.


The dose-dependent frequency of extrapyramidal symptoms is very low in patients treated for predominantly negative symptoms at doses of 50-300 mg/day.


Often drowsiness, possible acute dystonia (spastic torticollis, oculogoric crisis, trismus). It is reversible without discontinuation of amisulpride when prescribing an anticholinergic antiparkinsonian agent.


Infrequently: tardive dyskinesia has been reported, characterized by involuntary movements of the tongue and / or facial muscles, usually after prolonged use of the drug.


Anticholinergic antiparkinsonian agents are ineffective or may cause increased symptoms.


Convulsions.


Rare: neuroleptic malignant syndrome, which is a potentially fatal complication.


Unknown: restless legs syndrome.


Mental disorders


Often: insomnia, anxiety, agitation, frigidity.


Infrequently: confusion.


From the digestive system.


Common: constipation, nausea, vomiting, dry mouth.


From the endocrine system.


Often: increased plasma prolactin levels, which is reversible after discontinuation of the drug. This can cause the following clinical symptoms: galactorrhea, amenorrhea, gynecomastia, chest pain, erectile dysfunction.


Rare: a benign pituitary tumor, such as prolactinoma (see the sections "contraindications" and "application features").


From the side of metabolism and nutrition.


Common: hyperglycemia (see Section "application features"), hypertriglyceridemia and hypercholesterolemia. 


Rare: hyponatremia, syndrome of inadequate secretion of antidiuretic hormone (SIADH)


Laboratory tests.


Common: weight gain.


Infrequently elevated levels of liver enzymes, mainly transaminases, have been reported.


From the immune system.


Infrequently allergic reactions.


From the cardiovascular system.


Common: bradycardia.


Rare:


- prolongation of the QT interval;


- ventricular arrhythmias such as torsades de pointes and ventricular tachycardia, which can lead to ventricular fibrillation and cardiac arrest;


- sudden death (see the section"application features").


Vascular disorders.


Often hypotension.


Infrequently: increased blood pressure.


Rare: cases of venous thromboembolism, including pulmonary embolism, sometimes fatal, and deep vein thrombosis have been reported with the use of antipsychotics (see the section "special instructions for use").

From the blood and lymphatic system.


Infrequently: Leukopenia, neutropenia.


Rare: agranulocytosis (see the section "application features").


From the skin and subcutaneous tissue.


Rare: angioedema, urticaria.


Unknown: light sensitivity reaction.


Pathological conditions during pregnancy, in the postpartum and perinatal periods.


Frequency unknown: withdrawal syndrome in newborns (see Section "use during pregnancy or lactation").


From the musculoskeletal system and connective tissue.


Infrequently: osteopenia, osteoporosis.


From the kidneys and urinary tract.


Infrequently: urinary retention.


From the liver and biliary tract.


Infrequently hepatocellular damage.


Respiratory, torocal, and mediastinal disorders.


Infrequently nasal congestion, aspiration of pneumonia (mainly in combination with other antipsychotics and CNS depressants).


From the side of the visual organs.


Often blurred vision.


Reporting adverse reactions.


Reporting adverse reactions after drug registration is an important measure. This makes it possible to continuously monitor the benefit/risk ratio when using this drug. Medical professionals should report any adverse reactions using the adverse reaction notification system in Ukraine.

Tags: Amisulpride