SOLIAN

Active material: Amysulpryd
When ATH: N05AL05
CCF: Antipsychotic drug (anxiolytic)
ICD-10 codes (testimony): F20, F21, F22, F23, F25, F29
When CSF: 02.01.02.01
Manufacturer: SANOFI WINTHROP INDUSTRY (France)

Pharmaceutical form, composition and packaging

Pills white or nearly white, round, flat, with the dividing mark on one side and engraving “AMI 100” – another.

Excipients: lactose monohydrate, sodium carboxymethyl starch (sodium glikolat amylopectin) (Type A), microcrystalline cellulose, gipromelloza, magnesium stearate.

30 PC. – blisters (1) – cardboard boxes.

Pills white or nearly white, round, flat, with the dividing mark on one side and engraving “AMI 200” – another.

Excipients: lactose monohydrate, sodium carboxymethyl starch (sodium glikolat amylopectin) (Type A), microcrystalline cellulose, gipromelloza, magnesium stearate.

30 PC. – blisters (1) – cardboard boxes.

Pills, coated white, oblong-oval, lenticular, Engraved “AMI 400” and the dividing line between “AMI” and “400” on one side; of presentations – homogeneous mass of white, or almost white.

Excipients: sodium glikolat amylopectin (Type A), lactose monohydrate, microcrystalline cellulose, gipromelloza, magnesium stearate, polioksil 40 stearate, Titanium dioxide (E171).

30 PC. – blisters (1) – cardboard boxes.

Pharmacological action

Antipsychotic drug (anxiolytic).

Amisulpride has selective affinity to dopaminergicheskim receptors subtipov (D)₂/D₃ and has no affinity to subtipam (D)₁, D₄ and D₅.

Unlike classical and atypical neuroleptics, amisulpride has no affinity for serotoninergic receptors, gistaminovym N₁-Receptor, α-adrenoreceptoram and holinoreceptoram.

When used in high doses does postsinapticalkie D₂-receptors, localised in limbic structures, Unlike similar receptors in the striatum. Not causing catalepsy and does not lead to the development of hypersensitivity dopaminovykh (D)₂-receptors after treatment.

In low doses it preferentially blocks presinapticalkie D₂/D₃-receptors, stimulating the release of dopamine.

Atypical pharmacological profile makes antipsychotic amisulprida effect at high doses, coming as a result of the embargo postsynaptic receptor dopaminovykh, and its effectiveness in low doses on negative symptoms as a result of the blockade of presinapticakih dopaminovykh receptors.

To a lesser extent amisulpride vyzyvaet extrapyramidal side effects, that could be due to its superior limbic activity.

In patients with schizophrenia with acute bouts of Solian^® acts as a secondary negative symptoms, and affective symptoms (incl. depressive mood and retardation).

Pharmacokinetics

Absorption

After taking the drug inside are marked with two peak absorption amisulprida: one achieved through 1 no, and the second – between 3 and 4 h after administration. After taking Soliana^® dose 50 amisulprida mg concentration in plasma was respectively 39 ± 3 and 54 ± 4 ng/ml. The absolute bioavailability 48%.

Taking the drug in conjunction with food, rich in carbohydrates (contains 68% liquids), reliably reduces the AUC, doctizhenija time and amount (C)_max. Changes in pharmacokinetics when taken with fatty foods at the same time is not observed. The clinical significance of these data is unknown.

Distribution

V_d is equal to 5.8 l / kg. Since linking blood plasma low (16%), interaction with other drugs is unlikely. Cumulation is not marked, and pharmacokinetic parameters are not changed when taken repeated doses.

Metabolism and excretion

Amisulpride biotransformiroetsa in small degree, about 4%. Identified 2 inactive metabolite. T_1/2 amilsulprida is approximately 12 no. Excreted in the urine as unchanged. Renal clearance is approximately 330 ml / min.

Pharmacokinetics in special clinical situations

Rich in carbohydrates food reliably reduces the AUC, T_max and C_max amisulprida, While rich fat food changes above farmakokineticeskih indicators does not cause. However, the significance of these observations in everyday clinical practice is unknown.

Because the drug is poorly metabolizmu, There is no need to decrease the dose for patients with impaired liver function.

In the application in patients with kidney failure T_1/2 It does not change, but systemic clearance is reduced by a factor of 2.5 to 3. AUC amisulprida in a small renal failure is doubled, and moderate in almost 10 time. Practical experience, However, limited, and no results on the application doses, exceeding 50 mg. Amisulpride weakly undergoes dialysis.

Data for farmakokinetike amisulprida in elderly patients (senior 65 years) limited. After receiving a single dose of the drug 50 mg C_max, T_1/2 and AUC above on 10-30%, than in younger patients. Data for farmakokinetike when kursovom older patients missing.

Testimony

-acute and chronic schizophrenia, accompanied by pronounced productive (incl. delirium, hallucinations, thought disorder) and / or negative (incl. affective uploshchennosti, the absence of emotion and caring communication) disorders, incl. in patients with predominantly negative symptoms.

Dosage regimen

At acute psychotic episodes the recommended dose is from 400 to 800 mg / day.

In some cases, the dose may be increased to 1200 mg / day. Dose increase taking into account individual portable products.

The maximum daily dose should not exceed 1200 mg.

At mixed negative and productive symptoms doses should be selected so, to provide optimal control over productive symptoms: on average 400 mg 800 mg / day. Maintenance treatment should be set individually at the level of the minimum effective dose.

At the predominance of negative symptoms recommended daily dose ranges from 50 to 300 mg. The selection of doses should be individualized.

At doses, exceeding 400 mg / day, Solian^® should be appointed in 2 admission.

Elderly patients Solian^® assign with caution due to possible development of arterial hypotension or excessive sedation.

At renal failure the dose for patients with KK from 30 to 60 ml / min should be reduced to 1/2, at KK from 10 to 30 ml / min – to 1/3.

Side effect

CNS: often – insomnia, alarm, ažitaciâ; sometimes – extrapyramidal symptoms (incl. tremor, hypertension, hyperptyalism, akathisia, gipokineziya), the intensity which when supporting doses usually moderate, symptoms of a partially reversible without canceling Soliana^® using the anticholinergic protivoparkinsonicheskih funds (frequency of dozozavisimyh extrapiramidale symptoms remains very low in patients with predominantly negative symptoms doses of 50-300 mg/day); rarely – daytime sleepiness; rarely – acute dystonia (incl. spasmodic torticollis, oculogyric crises, Trizm), which is reversible and is adjusted using the anticholinergic protivoparkinsonicheskih funds; prolonged use – pozdnyaya dyskinesia, characterized by rhythmic, involuntary movements mainly language and/or persons (anti-parkinsonian N04 remedies are ineffective and can cause a worsening of symptoms); in a few cases – neuroleptic malignant syndrome, seizures.

From the digestive system: rarely – constipation, nausea, vomiting, dry mouth; in some cases – increase in liver enzymes (mostly transaminase).

On the part of the endocrine system: often – increase the level of prolactin in blood plasma (reversible after the drug), that could cause galaktoreju, Amenorrhoea, gynecomastia, breast tenderness, impotence, frigidity, as well as the increase in body mass index.

Cardio-vascular system: rarely – hypotension, bradycardia, QT prolongation; very rarely-atrial fibrillation.

Other: in some cases – allergic reactions.

Contraindications

— concomitant prolaktinzawisimae tumors (incl. prolactinoma pituitary, breast cancer);

- Pheochromocytoma;

- Severe renal insufficiency (CC<10 ml / min);

-combined use with sultopridom;

-combined use with dopaminovykh receptors agonists (incl. amantadin, apomorfin, bromocriptine, cabergoline, entacapone, lizurid, pergolid, piriʙedil, pramipexol, hinagolid, ropynyrol, selegiline), with the exception of patients with Parkinson's disease;

- Children up to age 14 years;

- Lactation (breast-feeding);

-hypersensitivity to amisulpridu and other components of the drug.

FROM caution the drug should be used during pregnancy, epilepsy, parkinsonizme, renal failure, as well as in elderly patients.

Pregnancy and lactation

Safety of amisulprida in pregnancy has not been established. Hence, the drugs in pregnancy is not recommended, except, where the presumed benefit to the mother justifies the potential risk to the fetus.

Application of the amisulprida contraindicated in lactation.

Cautions

May develop malignant neuroleptic syndrome, characterized by hyperthermia, muscle stiffness, dysfunction of the peripheral nervous system, elevated CPK. With the development of hyperthermia, especially against the backdrop of high doses, all antipsychotic drugs (including Solian^®) should be abolished.

As amisulprida excretion is performed by the kidneys, If serious violations of the kidney dose should be adjusted and schema therapy. Experience of the use of the drug in patients with severely impaired (CC<10 ml / min) kidney function is not.

Because the drug is poorly metabolised, in human liver lower dose is not required.

With regard to the possible lowering convulsant threshold when applying amisulprida patients with epilepsy in history require constant monitoring during therapy Solianom^®.

In patients older amisulpride should be used with special caution because of the potential risk of arterial hypotension or excessive sedation.

In Parkinson's disease, in the appointment antidopaminergicheskih drugs and amisulprida should be used with caution because of possible deterioration of. Amisulpride should only be used, If neuroleptic therapy cannot be avoided.

Amisulpride causes dose-dependent elongation QT interval, thereby increasing the risk of serious ventricular arrhythmias (type “pirouette”). Pending the appointment of a drug, and, possibly, Depending on the clinical condition of the patient to control factors, conducive to the development of arrhythmias: bradycardia (Heart Rate<55 u. / min), kaliopenia, innate elongation QT interval.

Patients, requiring long-term treatment neiroleptikami, in the initial assessment of the status of the ECG should be undertaken.

In connection with the contents of the tablets lactose, the drug is contraindicated in congenital galactosemia, syndrome violations removals glucose or Galactose or lactase deficiency.

Effects on ability to drive vehicles and management mechanisms

Amisulpride affects reaction speed, bringing the ability to engage in potentially dangerous activities may be weakened.

Overdose

Experience, associated with an overdose of amisulprida, limited.

Symptoms: strengthening the known pharmacological effects of the drug (incl. drowsiness, sedation, hypotension, extrapyramidal symptoms, coma).

Treatment: in acute overdose should explore possible combination with other drugs and to take the necessary measures: careful monitoring of the vital functions of the organism; video monitoring of the ECG (risk of fracture QT interval); in case of severe extrapyramidal symptoms, should appoint antiholinergicakie means. Hemodialysis nyeeffyektivyen. A specific antidote for amisulprida does not exist.

Drug Interactions

Combinations, that are contraindicated

With dopaminovykh receptor agonists (incl. amantadin, apomorfin, bromocriptine, cabergoline, entacapone, lizurid, pergolid, piriʙedil, pramipexol, hinagolid, ropynyrol, selegiline), with the exception of patients with Parkinson's disease.

Agonists dopaminovykh receptors and antipsychotics have shown mutual antagonism. In jekstrapiramidnom syndrome, caused by Neuroleptics, instead of dopaminovykh receptors agonists should apply anticholinergic drugs.

While applying Soliana^® with a sultopridom increased risk of ventricular arrhythmias, especially atrial fibrillation.

Combinations, that are not recommended

With drugs, that can cause arrhythmia type “pirouette”: antiarrhythmics class IA (incl. quinidine, gidroxinidin, disopyramide) and class III (incl. Amiodarone, sotalol, dofetilid, iʙutilid), Some antipsychotics (incl. tioridazin, chlorpromazine, levomepromazin, trifluoperazine, ciamemazin, sulьpirid, tiapride, pimozid, haloperidol, droperidol) and other drugs (incl. bepridil, cisapride, difemanil, in/in erythromycin, mizolastin, in/in vincamine, galofantrin, sparfloxacine, gatifloxacin, moxifloxacin, pentamidine, in/in Spiramycin). Increased risk of ventricular arrhythmias, in particular, the development of arrhythmias type “pirouette”. If the combination of drugs is not avoidable, prior to his appointment to hold control of the QT interval and start ECG monitoring.

Ethanol increases the sedative action of Neuroleptics. You should avoid alcohol consumption and use of drugs, containing alcohol.

Account should be taken of the mutual antagonism action of levodopa and Neuroleptics in the appointment of these drugs. In patients with Parkinson's disease are recommended to use the minimum effective dose of both drugs.

Combinations, require special care

With drugs, causing bradycardia (incl. Beta-adrenoblokatora/sotalola/calcium channel blockers, causing bradycardia – diltiazem and verapamil), clonidine, guanfacinom, drugs naperstanki, cholinesterase inhibitors (incl. donepezil, rivastigmine, tacrine, ambenonij, galantamin, pyridostigmine, neostigmine).

With drugs, which can cause hypokalemia (incl. kaliivforodaschie diuretics, laxatives, in/in the amphotericin b, GCS, tetrakozaktidy).

When the above mentioned combinations of drugs, the risk of ventricular arrhythmias, especially the development of arrhythmias type “pirouette”.

Combinations, that should be taken into account

With antigipertenzivei means and beta-blockers in heart failure (incl. Bisoprolol, karvedilol, metoprolol) has a vasodilator action, increasing the risk of orthostatic hypotension (additive effect).

Derivatives of morphine (incl. analgesics, cold preparations), ʙarʙituratami, benzodiazepines and other anxiolitikami, sleeping pills, sedatives antidepressants (incl. Amitriptyline, Doxepin, mianserin, mirtazapine, trimipramin), sedative antihistamines, antigipertenzivei means central action, neiroleptikami and other drugs (incl. ʙaklofen, Thalidomide, pizotifen) leads to the strengthening of the oppressive action on the central nervous system (reduced concentration and risk for drivers and machine operators transport).

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

The drug should be stored out of reach of children, dry place at a temperature below 25° c. Shelf life – 3 year.