Sizodon-San instructions for use, dose, side effects, contraindications

Composition:Each tablet, coated with a shell, contains:
Active substances: Risperidone - 1 mg, 2 mg, 3 mg, 4 mg
Auxiliary substances: lactose, starch, microcrystalline cellulose, sodium benzoate, purified talc, magnesium stearate, silicon dioxide colloid, sodium starch glycolate, shell composition: eudragit E-100, titanium dioxide, dye sanlet yellow, polyethylene glycol 6000, sodium lauryl sulfate, isopropyl alcohol , acetone, purified water.

Description:Round, biconvex tablets, covered with an orange shell, having a risk on one side.

Pharmacotherapeutic group:Antipsychotic agent (antipsychotic).

ATX: & nbsp

N.05.A.X Other antipsychotics

N.05.A.X.08 Risperidone

Pharmacodynamics:Sizodon-san is an antipsychotic agent, it also has a sedative, antiemetic and hypothermic effect. Sizodon-san is a selective monoaminergic antagonist with pronounced affinity to serotoninergic 5-HT2 and D2-dopaminergic receptors, also binds to the alpha 1-adrenoceptors and at slightly lower affinity of H1-histaminergic and alpha2 adrenergic receptors. Has no tropism for cholinergic receptors.
The antipsychotic effect is due to the blockade of dopamine 02 receptors of the mesolimbic and mesocortical system.
Sedative action is due to blockade of adrenoreceptors of the reticular formation of the brainstem; antiemetic effect - blockade of dopamine 02-receptors in the trigger zone of the vomiting center; hypothermic action - blockade of dopamine receptors of the hypothalamus.
Reduces productive symptoms (delirium, hallucinations), automatism. It causes less inhibition of motor activity and to a lesser degree induces catalepsy than classical antipsychotics (antipsychotics).
A balanced central antagonism to serotonin and dopamine may reduce the risk of extrapyramidal symptoms.
Sizodon-san can cause a dose-dependent increase in prolactin concentration in the plasma.

Pharmacokinetics:When taken orally, Sizodon-san is completely absorbed (regardless of food intake) and maximum levels of plasma concentration are observed after 1-2 hours. Sizodon-san undergoes a metabolism involving P-450 IID6 cytochrome with the formation of 9-hydroxy-risperidone, which has a similar pharmacological effect. Risperidone and 9-hydroxy-risperidone are an effective antipsychotic fraction. The further metabolism of Sizodon-san is in N-dealkylation. When ingestion Sizodon-san is withdrawn with a half-life of about 3 hours. It was found that the half-life of 9-hydroxy-risperidone and the active antipsychotic fraction is 24 hours.
In most patients, the equilibrium concentration of Sisodon-san is observed one day after the start of treatment. The equilibrium state of 9-hydroxy-risperidone in most cases is achieved 3-4 days after the start of treatment.
The concentration of Sisodon-san in plasma is proportional to the dose of the drug (within therapeutic doses).
Sizodon-san is quickly distributed in the body. The distribution volume is 1 -2 l / kg. In plasma, Sisodon-san is associated with albumin and acid alpha-1-glycoprotein. The fraction of risperidone that is bound by the plasma protein is 88% and 77%, respectively, in the case of 9-hydroxy-risperidone.
It is excreted by the kidneys -70% (of which 35-45% in the form of pharmacologically active fraction) and 14% with bile. With a single admission, high levels of active plasma concentrations and slow excretion in elderly patients and patients with insufficient renal function are noted.

Indications:- schizophrenia (acute and chronic) and other psychotic conditions with productive and / or negative symptoms;
- affective disorders in various mental illnesses;
- Behavioral disorders in patients with dementia in the manifestation of symptoms of aggression (outbursts of anger, physical violence), with mental disorders (agitation,delirium) or psychotic symptoms;
- as an auxiliary therapy in the treatment of mania in bipolar disorders;
- as an auxiliary therapy of behavioral disorders in adolescents with 15 years of age and adults with reduced intellectual level or mental retardation, in cases where destructive behavior (aggressiveness, impulsivity, autoaggression) is leading in the clinical picture of the disease.

Contraindications:Hypersensitivity to the components of the drug; lactation period.

Carefully:- Diseases of the cardiovascular system (chronic heart failure, suffered myocardial infarction, conduction disorders of the heart muscle)
- dehydration and hypovolemia
- disorders of cerebral circulation
- Parkinson's disease
- convulsions (including in the anamnesis)
- severe renal or hepatic insufficiency (see recommendations for dosing)
- Drug abuse or drug dependence (see recommendations for dosing)
- conditions predisposing to the development of tachycardia such as "pirouette" (bradycardia, electrolyte imbalance, concomitant medication prolonging the QT interval)
- Brain tumor, intestinal obstruction, cases of acute drug overdose, Reye's syndrome (antiemetic effect of risperidone may mask the symptoms of these conditions)
- Pregnancy, children under 15 years of age (efficacy and safety not established).

Pregnancy and lactation:Safety of Sizodon-san in pregnant women has not been studied. When pregnancy can be used only if the positive effect justifies the possible risk.
Because the risperidone and 9-hydroxy-risperidone penetrate into breast milk, women who use the drug should not be breast-fed.

Dosing and Administration:Schizophrenia.
Adults and children over 15 years. Sizodon-san can be given once or twice a day. The initial dose is 2 mg per day. On the second day, the dose should be increased to 4 mg per day. From this moment the dose can either be kept at the same level, or individually adjusted if necessary. Usually the optimal dose is 4-6 mg per day. In some cases, a slower dose increase and lower initial and maintenance doses may be justified.
Doses above 10 mg per day did not show a higher efficacy compared with smaller doses and may cause extrapyramidal symptoms.Due to the fact that safety of doses above 16 mg per day has not been studied, doses above this level can not be used.
Information on use for the treatment of schizophrenia in children under the age of 15 is not available.
Elderly patients. Recommended initial dose of 0.5 mg per reception twice a day. Dosage can individually increase by 0.5 mg twice a day to 1-2 mg twice a day.
Diseases of the liver and kidneys. Recommended initial dose of 0.5 mg per reception 2 times a day. This dose can be gradually increased to 1-2 mg per reception twice a day.
Drug Abuse or Drug Dependence - The recommended daily dose of the drug is 2-4 mg.
Behavioral disorders in patients with dementia.
An initial dose of 0.25 mg per reception is recommended twice a day (an adequate dosage form should be used). Dosage, if necessary, can individually increase by 0.25 mg 2 times a day, not more often than every other day. For most patients, the optimal dose is 0.5 mg twice daily. However, some patients receive 1 mg 2 times a day.
Once the optimal dose is reached, the drug may be recommended once a day.
Mania in bipolar disorders
The recommended initial dose of the drug is 2 mg per day at a time. If necessary, this dose may be increased by 2 mg per day, not more often than every other day. For most patients, the optimal dose is 2-6 mg per day.
Behavioral disorders in patients with mental retardation
Patients weighing 50 kg or more - the recommended initial dose of the drug is 0.5 mg once daily. If necessary, this dose can be increased by 0.5 mg per day, not more often than every other day. For most patients, the optimal dose is a dose of 1 mg per day. However, for some patients it is preferable to take 0.5 mg per day, while some require an increase in the dose to 1.5 mg per day.
Patients weighing less than 50 kg - The recommended initial dose of the drug is 0.25 mg once a day. If necessary, this dose can be increased by 0.25 mg per day, not more often than every other day. For most patients, the optimal dose is 0.5 mg per day.
However, for some patients it is preferable to take 0.25 mg per day, while some require an increase in the dose to 0.75 mg per day.
Long-term use of Sizodon-san in adolescents should be carried out under the constant supervision of a doctor.
Use in children younger than 15 years is not recommended.

Side effects:From the nervous system: insomnia, agitation, anxiety, headache, sometimes drowsiness, increased fatigue, dizziness, impaired concentration, blurred vision, rarely - extrapyramidal symptoms (tremor, rigidity, hypersalivation, bradykinesia, akathisia, acute dystonia), mania or hypomania, stroke in elderly patients with predisposing factors), as well as hypervolemia (either due to polydipsia, or because of the syndrome of inadequate secretion of the antidiuretic hormone), tardive dyskinesia (involuntary rhythmic movements predominantly Single and / or persons), neuroleptic malignant syndrome (hyperthermia, muscle rigidity, autonomic instability functions, impaired consciousness and increased CPK), thermoregulation disorders and seizures.
From the digestive system: constipation, dyspepsia, nausea or vomiting, abdominal pain, increased activity of "liver" transaminases, dry mouth, hypo- or hypersalivation, anorexia and / or increased appetite, weight gain or loss.
From the cardiovascular system: sometimes orthostatic hypotension, reflex tachycardia, or increased blood pressure.
From the hematopoiesis: neutropenia, thrombocytopenia.
From the endocrine system: galactorrhea, gynecomastia, menstrual irregularity, amenorrhea, weight gain, hyperglycemia and exacerbation of pre-existing diabetes.
From the genitourinary system: priapism, erectile dysfunction, ejaculation disorders, anorgasmia, urinary incontinence.
Allergic reactions: rhinitis, rash, angioedema, photosensitivity.
From the skin: dry skin, hyperpigmentation, itching, seborrhea.
Other: arthralgia.

Overdose:Symptoms: drowsiness, sedation, depression, tachycardia, arterial hypotension, extrapyramidal disorders, in rare cases, prolongation of the QT interval. Treatment: it is necessary to ensure free airway patency to ensure adequate oxygenation and ventilation, gastric lavage (after intubation, if the patient is unconscious) and the appointment of activated carbon in combination with laxatives.Symptomatic therapy aimed at maintaining vital body functions.
For timely diagnosis of possible cardiac arrhythmias, ECG monitoring should be started as soon as possible. Careful medical observation and ECG monitoring is performed until the symptoms of intoxication disappear completely. There is no specific antidote.

Interaction:Given that Sizodon-san has an effect primarily on the central nervous system, it should be used with caution in combination with other central-action drugs and with alcohol.
Sizodon-san reduces the effectiveness of l-dopa and other dopamine agonists.
Clozapine reduces the clearance of Sizodon-san.
When carbamazepine was used, there was a decrease in the concentration of the active antipsychotic fraction of Sizodon-san in plasma. Similar effects can be observed with the use of other inducers of hepatic enzymes.
Phenothiazines, tricyclic antidepressants and some β-adrenoblockers can increase plasma concentrations of Sisodon-san, but this does not affect the concentration of the active antipsychotic fraction.
Fluoxetine can increase the concentration of Sisodon-san in plasma, but to a lesser extent the concentration of the active antipsychotic fraction, so the dose of Sizodon-san should be adjusted.
With the use of Sizodon-san along with other drugs, highly binding to plasma proteins, there is no clinically pronounced displacement of any drug from the plasma protein fraction.
Hypotensive drugs increase the severity of lowering blood pressure on the background of Sizodon-san.

Special instructions:Transition from therapy with other antipsychotic drugs When schizophrenia, at the beginning of treatment by Sizodon-san, it is recommended to gradually cancel the previous therapy, if it is clinically justified. If patients are transferred from depot therapy to forms of antipsychotics, it is recommended that Sisodon-san should be started instead of the next scheduled injection. Periodically, the need to continue therapy with antiparkinsonian drugs should be evaluated.
In connection with the α-adrenoblocking action of Sizodon-san, orthostatic hypotension can occur, especially during the initial dose selection.If hypotension occurs, consider lowering the dose. In patients with diseases of the cardiovascular system, as well as in dehydration, hypovolemia or cerebrovascular disorders, the dose should be increased gradually, according to the recommendations (see Dosage and Administration).
The occurrence of extrapyramidal symptoms is a risk factor for the development of tardive dyskinesia. In case of signs and symptoms of tardive dyskinesia, consideration should be given to the abolition of all antipsychotics. When neuroleptic malignant syndrome characterized by hyperthermia, muscle rigidity, instability of autonomic functions, impaired consciousness and increased level of creatine phosphokinase, it is necessary to cancel all antipsychotic medications, including Sizodon-san.
With the withdrawal of carbamazepine and other inducers of "liver" enzymes, the dose of Sizodon-san should be reduced.
Patients should be advised to refrain from overeating due to the possibility of weight gain.

Effect on the ability to drive transp. cf. and fur:During treatment, it is necessary to refrain from engaging in potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions, as well as on the intake of alcohol.

Form release / dosage:Tablets, coated with a coat of 1 mg, 2 mg, 3 mg, 4 mg.

Packaging:For 10 tablets in an aluminum strip. For 1, 2 or 3 strips in a cardboard box with instructions for use.

Storage conditions:List B. In a dry, protected from light and out of reach of children, at a temperature of not more than + 25 ° C.

Shelf life:3 years. Do not use the product after the date shown on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-005404/08

Date of registration:14.07.2008

Expiration Date:Unlimited

The owner of the registration certificate:San Pharmaceutical Industries Co., Ltd.San Pharmaceutical Industries Co., Ltd. India

Manufacturer: & nbsp

Sun Pharmaceutical Industries, Ltd. India

Representation: & nbspSAN PHARMACEUTICAL INDUSTRIES LTD. SAN PHARMACEUTICAL INDUSTRIES LTD. India

Information update date: & nbsp2016-12-27

Illustrated instructions

Instructions

Sizodon-san (Sizodon-Sun)