Expiration date: 11/2025

Structure and Composition:

Film-coated tablets. One tablet contains active substance:

risperidone 1, 2, 3 or 4 mg

Excipients: lactose monohydrate, corn starch, magnesium stearate MCC silica colloidal anhydrous sodium lauryl sulphate

wrapper table. 1 mg: Dye Opadry-Y-1-7000 white (hypromellose, titanium dioxide, macrogol 400)

wrapper table. 2, 3, 4 mg: Opadry green dye (Titanium dioxide Hypromellose Macrogol 400 ariavit indigo carmine aluminum lake ariavit quinoline yellow aluminum lake)

in blister 10 pcs. In the paper cartons 2 blisters.

Description pharmaceutical form:

Tablets 1 mg: oblong, biconvex, film-coated, white or nearly white, engraved with "E 751" - on one side and with Valium - on another, without or almost odorless.

Tablets 2mg: oblong, biconvex, film-coated, light green color, with chasing "E 752" - on one side and with Valium - on another, without or almost odorless.

Tablets 3 mg: oblong, biconvex, light green, film-coated, engraved with "E 753" on one side and with Valium - on another, without or almost odorless.

Tablets 4mg: oblong, biconvex green, film-coated, engraved with "E 754" - on one side and with Valium - on another, without or almost odorless.

Pharmacokinetics:

When administered risperidone completely absorbed (regardless of the meal) and the plasma Cmax observed after 1 -2 hours. Risperidone is metabolized involving cytochrome P450 isoenzyme CYP2D6 to form a 9-hydroxyrisperidone which has a similar pharmacological action. Risperidone and 9-hydroxyrisperidone is an effective antipsychotic fraction. Subsequent metabolism of risperidone is N-dealkylation. When administered risperidone outputted from T1 / 2 of about three hours. It is found that the T1 / 2 and the 9-hydroxyrisperidone active antipsychotic fraction is 24 hours.

In most patients, the equilibrium concentration of risperidone is observed one day after the start of treatment. The equilibrium state of 9-hydroxyrisperidone in most cases is achieved after 3-4 days of treatment.

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

Risperidone is rapidly distributed in the body. The volume of distribution of 1.2 l / kg. The risperidone plasma associated with albumin and acidic glycoprotein & alpha1-. Fraction of risperidone and 9-hydroxyrisperidone associated with plasma proteins of 88 and 77%, respectively.

Excreted by the kidneys - 70% (35-45% of them as a pharmacologically active fraction) and 14% in the bile. In single dose have high levels of the active plasma concentrations and a slower elimination in elderly patients and patients with poor kidney function.

Description of the pharmacological actions:

Risperidone is an antipsychotic, also has a sedative, antiemetic and hypothermic effect. Risperidone is a selective monoaminergic antagonist with a strong affinity for serotonergic 5-NT2- and the D2-dopaminergic receptors, also binds to alpha1-adrenoceptor & and somewhat lower affinity - with H1-histaminergic and alpha2-adrenergic & receptors. It has no affinity for holinoretseptorami.

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

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

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

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

Risperidone can cause dose-dependent increase in plasma prolactin concentrations.

Indications:

• schizophrenia (acute and chronic) and other psychotic states with productive and / or negative symptoms
  
• affective disorders in a variety of mental illnesses
  
• behavioral disturbances in patients with dementia with symptoms manifestation of aggressiveness (anger, physical abuse), Abuse of mental activity (agitation, delirium) or psychotic symptoms
  
• as adjuvant therapy in the treatment of mania in bipolar disorder
  
• as adjunctive therapy of behavior disorders in adolescents from 15 years and adult patients with reduced intellectual level or mental retardation, in cases where destructive behavior (aggressiveness, impulsivity, autoaggression) is leading the clinical picture of the disease.
  

Contraindications:

Hypersensitivity to the drug during lactation.

Carefully:

• diseases of the cardiovascular system (chronic heart failure, myocardial infarction, conduction disorders of the heart muscle)
  
• Dehydration and hypovolemia
  
• cerebrovascular accidents
  
• Parkinson's disease
  
• seizures (including history)
  
• severe renal or hepatic insufficiency (see. dosing recommendations)
  
• drug abuse or drug dependency (see. for dosage recommendations)
  
• conditions that predispose to the development of tachycardia type "pirouette" (bradycardia, electrolyte imbalance, concomitant drugs prolonging the QT interval)
  
• brain tumor, intestinal obstruction, acute cases of drug overdose, Reye's syndrome (an antiemetic effect of risperidone may mask the symptoms of these conditions)
  
• pregnancy, children under 15 years (effectiveness and safety have been established).
  

Application of pregnancy and breastfeeding:

risperidone safety in pregnant women has not been studied. When pregnancy only be used if a positive effect justifies the potential risk.

Since risperidone and 9-hydroxyrisperidone into breast milk, women using the drug should not breast-feed.

Side effect:

CNS: insomnia, agitation, anxiety, headache, sometimes - drowsiness, 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 the syndrome of inappropriate secretion of antidiuretic hormone), tardive dyskinesia (involuntary rhythmic movements mainly language 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 liver transaminases, dry mouth, hypo- or hypersalivation, anorexia and / or increased appetite, increased or decreased body weight.

Since the cardiovascular system: sometimes - orthostatic hypotension, reflex tachycardia, or increased blood pressure.

From the side of hematopoiesis: neutropenia, thrombocytopenia.

From endocrine system: galactorrhea, gynecomastia, irregular menstruation, amenorrhea, weight gain, hyperglycemia and exacerbation of preexisting diabetes mellitus.

With the genitourinary system: priapism, erectile dysfunction, abnormal ejaculation, anorgasmia, urinary incontinence.

Allergic reactions: rhinitis, rash, angioedema, photosensitivity.

For the skin: dry skin, hyperpigmentation, itching, seborrhea.

Other: arthralgia.

Drug Interactions:

Given risperidone has effect primarily on the central nervous system, it should be used with caution in combination with other centrally acting drugs and alcohol.

Risperidone reduces the effectiveness of levodopa or other dopamine agonists.

Clozapine decreases clearance of risperidone.

When using carbamazepine marked reduction in the concentration of the active antipsychotic fraction of risperidone in plasma. Similar effects may be observed with other hepatic enzyme inducers.

Phenothiazines, tricyclic antidepressants and some beta-blockers & may increase the concentration of risperidone in the plasma, but this does not affect the concentration of the active antipsychotic fraction.

Fluoxetine can increase plasma concentrations of risperidone, but to a lesser degree - the concentration of the active fraction antipsychotic, risperidone dose should therefore be corrected.

In the application of risperidone with other drugs that are highly bound to plasma proteins, clinically pronounced displacement of a drug from the plasma protein fraction is observed.

Antihypertensive drugs increase the severity of blood pressure lowering on the background of risperidone.

Dosage and administration:

Schizophrenia. Adults and children over 15 years. Rileptid may be administered 1-2 times per day. 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, either individually adjusted if necessary. Typically, the optimal dose is 4-6 mg / day. In some cases it may be justified by a slower increase in the dose and lower initial and maintenance doses.

Doses above 10 mg / day did not show a higher efficiency compared to lower doses and may cause the appearance of extrapyramidal symptoms. Due to the fact that the safety of doses above 16 mg / day has not been studied, doses above this level can not be applied.

For information on the use for the treatment of schizophrenia in children under 15 years are not available.

Elderly patients. Recommended initial dose of 0.5 mg to receiving two times a day. The dosage can be individually increased by 0.5 mg 2 times per day to 1.2 mg two times a day.

Diseases of the liver and kidneys. Recommended initial dose of 0.5 mg to receiving two times a day. This dose can be gradually increased to 1.2 mg per reception 2 times per day.

Abuse of drugs or drug dependency. The recommended daily dose - 2-4 mg.

Behavioral disorders in patients with dementia. Recommended starting dose of 0.25 mg per reception 2 times a day. If necessary dosage can be individually increased by 0.25 mg 2 times a day, no more than a day. For most patients, the optimal dose is 0.5 mg two times a day. However, some patients are shown receiving 1 mg 2 times a day.

On reaching the optimum dose of the drug can be recommended once daily.

Mania in bipolar rasstroystvah.Rekomendovannaya initial dose - 2 mg per day in one step. If necessary, this dose may be increased to 2 mg per day, no more than a day. For most patients the optimal dose is 2-6 mg / day.

Conduct disorders in patients with mental retardation

Patients body weight of 50 kg or more. The recommended initial dose - 0.5 mg 1 time a day. If necessary, this dose may be increased to 0.5 mg per day, no more than a day. For most patients, the optimal dose is 1 mg per day.

However, preferred for some patients receiving 0.5 mg per day, whereas some require increasing doses up to 1.5 mg per day.

Patients weighing less than 50 kg. The recommended initial dose - 0.25 mg 1 time a day. If necessary, this dose may be increased by 0.25 mg per day, no more than a day. For most patients, the optimal dose is 0.5 mg per day. However, preferred for some patients receiving 0.25 mg per day, whereas some require increasing doses up to 0.75 mg per day.

Long-term use Rileptida adolescents should be carried out under the constant supervision of a physician.

Use in children under 15 years is not recommended.

Overdose:

Symptoms: drowsiness, sedation, depression of consciousness, tachycardia, hypotension, extrapyramidal disorder, in rare cases - lengthening of the QT interval.

Treatment: it is necessary to ensure a free airway to ensure adequate oxygenation and ventilation, gastric lavage (after intubation if the patient is unconscious) and the appointment of activated charcoal in combination with laxatives. Symptomatic therapy directed at maintaining vital functions.

For early diagnosis of possible cardiac arrhythmias need to begin ECG monitoring as soon as possible. Careful medical supervision and ECG monitoring is carried out to complete disappearance of symptoms of intoxication. There is no specific antidote.

Special instructions:

Transition from other antipsychotic therapy. In schizophrenia, the beginning of treatment with risperidone, we recommend gradually cancel the previous therapy, if clinically justified. If patients are transferred from the depot forms of therapy antipsychotics, risperidone it is recommended to start in place of the next scheduled injection. Periodically assess the need for continued therapy potivoparkinsonicheskimi PM. In connection with the & alpha-adrenoceptor blocking action may occur Rileptida orthostatic hypotension, especially during the initial dose adjustment. 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, as recommended (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 should consider abolishing all antipsychotics. In the event of a neuroleptic malignant syndrome, characterized by hyperthermia, muscle rigidity, autonomic instability functions, impairment of consciousness, and increased levels of creatine kinase, it is necessary to cancel all antipsychotic drugs, including risperidone.

In patients with schizophrenia increases the risk of suicide attempts, so the treatment of patients with increased risk of suicide should be under strict supervision.

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

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

During treatment should refrain from activities potentially hazardous activities that require high concentration and psychomotor speed reactions, as well as the intake of alcohol.