SIZODON Facility

Active material: Risperidone
When ATH: N05AX08
CCF: Antipsychotic drug (anxiolytic)
ICD-10 codes (testimony): F20, F21, F22, F23, F25, F29, F30, F31, F79
When CSF: 02.01.02.03
Manufacturer: Sun Pharmaceutical Industries Ltd. (India)

Pharmaceutical form, composition and packaging

Pills, coated orange, round, lenticular, with Valium on one side.

Excipients: lactose, starch, microcrystalline cellulose, Sodium benzoate, Talcum cleared, magnesium stearate, colloidal silicon dioxide, sodium starch glycolate.

The composition of the shell: эudrazhit E-100, Titanium dioxide, dye Sunset Yellow, polyethylene glycol 6000, sodium lauryl, isopropanol, acetone, Purified water.

10 PC. – aluminum strips (1) – packs cardboard.
10 PC. – aluminum strips (2) – packs cardboard.
10 PC. – aluminum strips (3) – packs cardboard.

Pharmacological action

Antipsychotics (anxiolytic). It has also a sedative, antiemetic and hypothermic effect. Sizodon Fund – selective monoaminergic antagonist with pronounced affinity to serotonin 5-HT₂– и допаминовым D₂-Receptor, also associated with the α₁-adrenoceptors and at slightly lower affinity – with histamine H₁– и a₂-adrenoreceptor. It does not have affinity for holinoretseptorami.

Antipsychotic effect due to blockade of dopamine D₂-receptors and the mesolimbic system Mesocortical.

Sedative effect due to blockade of adrenergic receptors of the reticular formation of the brain stem; antiemetic effect – blockade of dopamine D₂-receptor trigger zone of the vomiting center; hypothermic effect – blockade of dopamine receptors of the hypothalamus.

Reduces productive symptoms (delirium, hallucinations), automatism. It causes minimal suppression of motor activity and to a lesser extent induces catalepsy, than classical antipsychotics (neuroleptics).

Balanced central serotonin antagonism and dopamine can reduce the risk of extrapyramidal symptoms.

San Sizodon can cause dose-dependent increase in plasma prolactin.

Pharmacokinetics

Absorption

Once inside Sizodon San completely absorbed from the gastrointestinal tract (regardless of the meal), C_max risperidone in the blood plasma observed by 1-2 no.

The concentration of risperidone in the blood plasma is proportional to the dose of the drug (in the therapeutic dose range).

Distribution

In most patients, C_ss risperidone observed after 1 day after treatment. The equilibrium state of 9-hydroxy-risperidone is reached in most cases 3-4 days after initiation of treatment.

Risperidone is rapidly distributed in the body. V_d is 1-2 l / kg. Plasma protein binding (albumin and acid α₁-glycoprotein) of risperidone and 9-hydroxy-risperidone 88% and 77% respectively.

Metabolism

Risperidone is metabolized with the participation of isoenzyme CYP2D6 to form a 9-hydroxy-risperidone, which has a similar pharmacological action. Risperidone and 9-hydroxy-risperidone are effective antipsychotic fraction. Subsequent metabolism of the drug is in the N-dealkylation.

Deduction

When receiving the drug inside T_1/2 risperidone is about 3 no. Established, that T_1/2 9-hydroxy-risperidone and the active antipsychotic fraction is 24 no.

Report the news - 70% (of them 35-45% in the form of a pharmacologically active fraction) and 14% the bile.

Pharmacokinetics in special clinical situations

In single dose have high concentrations of the active substance and its active metabolite in the blood plasma and slow excretion in elderly patients and in patients with renal insufficiency.

Testimony

- Schizophrenia (acute and chronic) and other psychotic states with productive and / or negative symptoms;

- Affective disorders in a variety of mental disorders;

- Behavioral disorders in patients with dementia when symptoms persist aggression (outburst, physical abuse), for violations of mental activity (excitation, delirium) or psychotic symptoms;

- As an adjuvant therapy in the treatment of mania in bipolar disorder;

- As adjunctive therapy of conduct disorder in adolescents aged 15 and older and adult patients with reduced intellectual level or mental retardation, in cases, if the destructive behavior (aggressiveness, impulsiveness, autoagressiâ) It is leading the clinical picture of the disease.

Dosage regimen

Schizophrenia

Adults and children over 15 years San Sizodon can assign 1 or 2 once a day.

The initial dose – 2 mg / day. On the second day, the dose should be increased to 4 mg / day. From this point the dose can either maintain the same level of, either individually adjusted, if necessary,. Typically, the optimal dose is 4-6 mg / day. In some cases it can be justified by a slow increase in the dose and lower initial and maintenance doses.

The drug in doses more 10 mg / day did not show higher efficiency compared with lower doses and may cause extrapyramidal symptoms. Because, that the safety of the drug in doses more 16 mg / day has not been studied, can not exceed the specified dose.

Data on the use of the drug for the treatment of schizophrenia children under 15 years no.

To elderly patients The recommended starting dose is on 500 g 2 times / day. If necessary, the dose can be increased by 500 g 2 times / day to 1-2 mg 2 times / day.

At liver and kidney diseases The recommended starting dose – by 500 g 2 times / day. This dose can be gradually increased to 1-2 mg per reception 2 times / day.

In patients, Drug abuse, or drug dependence The recommended dose is 2-4 mg / day.

Behavioral disorders in patients with dementia

The recommended starting dose – by 250 g 2 times / day (should use adequate dosage form). The dose can be increased if necessary by 250 g 2 times / day, no more than a day. For most patients the optimal dose is 500 g 2 times / day. However, some patients show reception 1 mg 2 times / day.

Upon reaching the optimal dose can be recommended taking the drug 1 time / day.

Mania in bipolar disorder

The recommended starting dose is 2 mg 1 time / day. If necessary, the dose can be increased by 2 mg / day, no more than a day. For most patients the optimal dose is 2-6 mg / day.

Conduct disorders in patients with mental retardation

To patients with a body weight 50 kg or more The recommended starting dose - 500 g 1 time / day. If necessary, this dose may be increased by 500 mg / day, no more than a day. For most patients the optimal dose is 1 mg / day. However, for some patients, preferred reception 500 mg / day, in other cases requiring higher dosages to 1.5 mg / day.

To Patients weighing less than 50 kg The recommended starting dose - 250 g 1 time / day. If necessary, this dose may be increased by 250 mg / day, no more than a day. For most patients the optimal dose is 500 mg / day. However, for some patients, preferred reception 250 mg / day, in other cases requiring higher dosages to 750 mg / day.

Long-term treatment Adolescents San Sizodon drug should be under constant medical supervision. Use of the drug in children under 15 years not recommended.

Side effect

From the central and peripheral nervous system: insomnia, ažitaciâ, alarm, headache; sometimes - drowsiness, fatigue, dizziness, impaired concentration, blurred vision; rarely – extrapyramidal symptoms (tremor, rigidity, hyperptyalism, bradikineziâ, akathisia, acute dystonia), mania or gipomaniya, stroke (in elderly patients with predisposing factors), and hypervolemia (either due to polydipsia, either because the syndrome of inappropriate secretion of ADH), pozdnyaya dyskinesia (involuntary rhythmic movements mainly language and / or the person), NMS (hyperthermia, muscle rigidity, instability of autonomous functions, impairment of consciousness and increased CPK), violation of thermoregulation, seizures.

From the digestive system: constipation, dyspepsia, nausea or vomiting, abdominal pain, increase in liver transaminases, dry mouth, Hypo- or hypersalivation, anorexia and / or increased appetite, increase or reduction of body weight.

Cardio-vascular system: sometimes orthostatic hypotension, reflex tachycardia, or increased blood pressure.

From the side of hematopoiesis: neutropenia, thrombocytopenia.

On the part of the endocrine system: galactorrhea, gynecomastia, menstrual disorders, amenorrhea, weight gain, Hyperglycemia and exacerbation of preexisting diabetes mellitus.

On the part of the reproductive system: priapism, erectile dysfunction, abnormal ejaculation, anorgazmija.

From the urinary system: urinary incontinence.

Allergic reactions: rhinitis, rash, angioedema, photosensitivity.

Dermatological reactions: xerosis, giperpigmentatsiya, itch, seborrhea.

Other: arthralgia.

Contraindications

- Lactation (breast-feeding).

- Hypersensitivity to the drug.

FROM caution use in patients with diseases of the cardiovascular system (congestive heart failure, myocardial infarction, conduction disorder of the heart muscle); Dehydration and hypovolemia; violation of cerebral circulation; Parkinson's disease; with cramps (incl. history); severe renal insufficiency, severe hepatic insufficiency; drug abuse or drug addiction; under conditions, predisposing to the development of ventricular tachycardia type “pirouette” (bradycardia, electrolyte imbalance, concomitant drugs, prolonging the QT interval); when a brain tumor, bowel obstruction, cases of acute overdose of drugs, when Reye's syndrome (antiemetic effect of risperidone may mask the symptoms of these conditions); Pregnancy, children under the age of 15 years (efficacy and safety have not been established).

Pregnancy and lactation

Clinical data on the safety of the drug Sizodon San in pregnancy. Use of the drug during pregnancy is possible only in case, when the intended benefits to the mother outweighs the potential risk to the fetus.

Since risperidone and 9-hydroxy-risperidone are excreted in breast milk, If necessary, use during lactation should decide the issue of termination of breastfeeding.

Cautions

Transition from other antipsychotic therapy. In schizophrenia, at the beginning of treatment Sizodon San, It recommended phased previous therapy, if clinically warranted. If a patient is transferred from the depot forms of therapy antipsychotics, the reception Sizodon-Sana is recommended to start in place of the next scheduled injection. Periodically assess the need for continued therapy antiparkinsonian drugs.

In connection with alfa-adrenoceptor blocking action Sizodon-Sana orthostatic hypotension may occur, especially during the initial titration. In the event of hypotension should consider lowering the dose. In patients with diseases of the cardiovascular system, as well as dehydration, hypovolemia, or cerebrovascular disorders, the dose should be increased gradually, according to the recommendations.

The occurrence of extrapyramidal symptoms is a risk factor for tardive dyskinesia. In the case of signs and symptoms of tardive dyskinesia, should consider the abolition of all antipsychotics. In vozniknovenii NMS, characterized by hyperthermia, muscle rigidity, instability of autonomous functions, impairment of consciousness and increased CPK, you must cancel all antipsychotic drugs, including San Sizodon.

In case of cancellation of carbamazepine and other hepatic enzyme inducers dose Sizodon San should be reduced.

Patients should be advised to refrain from eating because of the possibility of weight gain.

During treatment, patients should avoid alcohol.

Effects on ability to drive vehicles and management mechanisms

During treatment, patients should avoid driving vehicles and other activities, require high concentration and speed of psychomotor reactions.

Overdose

Symptoms: drowsiness, sedation, depression of consciousness, tachycardia, hypotension, extrapyramidal disorder, in rare cases, QT prolongation.

Treatment: necessary to ensure a free airway to ensure adequate oxygenation and ventilation, gastric lavage (after intubation, if the patient is unconscious) and assigning the activated carbon in combination with laxatives. Displaying symptomatic therapy, designed to maintain vital body functions.

For early diagnosis of possible disturbances of cardiac rhythm as quickly as possible to begin ECG monitoring. Careful medical supervision and ECG monitoring is carried out to complete disappearance of symptoms of intoxication. The specific antidote is absent.

Drug Interactions

Considering, San Sizodon that has an effect primarily on the central nervous system, it should be used with caution in combination with other drugs and central action ethanol.

Sizodon San reduces the effectiveness of levodopa and other dopamine agonists.

Clozapine reduces the clearance of risperidone.

With simultaneous use of carbamazepine and Sizodon-Sana, a decrease of concentration of the active antipsychotic fraction of risperidone in plasma. Similar effects can be observed in the application of other hepatic enzyme inducers.

Fenotiazinы, Tricyclic antidepressants and some beta blockers can increase the concentration of risperidone in the blood plasma, however, this does not affect the concentration of the active antipsychotic fraction of the drug.

Fluoxetine can increase the concentration of risperidone in the blood plasma, but to a lesser extent the concentration of the active antipsychotic fraction, so if this combination requires dose adjustment Sizodon-shan.

When using Sizodon-Sana in combination with other drugs, characterized by a high degree of binding to plasma proteins, symptomatic displacement of a drug from the plasma protein fraction is observed.

Antihypertensive medicines increase the severity of BP reduction during treatment Sizodon-shan.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

List B. The drug should be stored out of reach of children, dry, dark place at a temperature no higher than 25 ° C. Shelf life – 3 year.