Expiration date: 04/2025

Structure and Composition:

Tablets, film-coated. One tablet contains active substance:

risperidone 1, 2 or 4 mg

Other ingredients: sodium lauryl sulfate, colloidal silicon dioxide, magnesium stearate, hypromellose pregelatinized starch, lactose monohydrate MCC

film (1 mg tablet) shell: Opadry II yellow 85F32072 (iron oxide red - E172, the CI 77491, iron oxide yellow - E172, the CI 77492, titanium dioxide - E171, the CI 77891, talc, macrogol, polyvinyl alcohol)

film (2 mg tablet) shell: Opadry II yellow 85F32069 (iron oxide red - E172, the CI 77491, iron oxide yellow - E172, the CI 77492, titanium dioxide - E171, the CI 77891, talc, macrogol, polyvinyl alcohol)

sheath film (4 mg tablets): Opadry II Orange 85F23450 (iron oxide red - E172, the CI 77491, iron oxide yellow - E172, the CI 77492, titanium dioxide - E171, the CI 77891, talc, macrogol, polyvinyl alcohol)

in blisters made of PVC / PVDC / aluminum foil of 10 pieces. In the paper cartons 2 blisters.

Description pharmaceutical form:

Tablets 1 mg: Round biconvex shape, film-coated yellow, engraved with «N04» on one side.

Tablets 2 mg: Round biconvex shape, film-coated brownish-yellow, engraved with «N05» on one side.

Tablets 4 mg: Round biconvex shape, film-coated light-brown color, with an engraving «N07» on one side.

Pharmacokinetics:

Absorption - rapid and complete (the food does not affect the completeness and rate of absorption). Tmax plasma PM -. 1.2 h Css risperidone in the body of most patients achieved within 1 day, 9-hydroxy-risperidone - 4-5 days. Risperidone plasma concentrations are proportional to the dose of the drug (in the range of therapeutic doses). Distributed quickly penetrates the CNS, breast milk. Vd - 1,1 l / kg. Communication with plasma proteins (from & alpha-1-glycoprotein and albumin) risperidone - 90%, a 9-hydroxy-risperidone - 77%. Metabolized by P450 isoenzyme CYP2D6 to an active metabolite 9-hydroxy-risperidone (risperidone and 9-hydroxy-risperidone constitute antipsychotic active fraction). Another way of metabolism is N-dealkylation. T1 / 2 of risperidone - 3 hours, T1 / 2 of 9-hydroxy-risperidone, and the active fractions antipsychotic - 20-24 h.

Excreted by the kidneys 70% (of them - 35-45% as a pharmacologically active fraction) and the bile - 14%.

In single dose have high levels of the active plasma concentrations and a slower elimination in elderly patients and patients with renal insufficiency.

Description of the pharmacological actions:

Antipsychotics (antipsychotic), benzisoxazole derivative also has sedative, antiemetic and hypothermic effect. Selective monoaminergic antagonist that has a high affinity for serotonergic 5-HT2 and dopaminergic the D2-receptor also binds to alpha1-adrenoceptor & and somewhat lower affinity to 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. Suppresses productive symptoms (delusions, hallucinations, aggressiveness), automatism. It causes minimal suppression of motor activity and to a lesser extent induces catalepsy than classic antipsychotic drugs (neuroleptics). Balanced central antagonism of serotonin and dopamine may reduce the propensity for extrapyramidal side effects and enhance the therapeutic effects of the drug, covering the negative and affective symptoms of schizophrenia. Can induce dose-dependent increase in plasma prolactin concentrations.

Indications:

schizophrenia and other psychotic states with a predominance of positive symptoms (delusions, gallyutsinadii, aggressiveness), negative symptoms (poverty of speech, emotional and social detachment)

affective disorders in a variety of mental illnesses.

Contraindications:

• hypersensitivity to any component of the drug
  
• lactation
  
• Children up to age 15 years (effectiveness and safety have been established).
  

Precautions: brain tumor, intestinal obstruction, an overdose of drugs, Reye's syndrome (an antiemetic effect of risperidone may mask the symptoms of these conditions), diseases of the cardiovascular system (chronic heart failure, myocardial infarction, AV block), dehydration, cerebral circulation, hypovolemia , Parkinson's disease, seizures (including history), drug abuse or drug dependence, severe renal / hepatic insufficiency, a condition predisposing to the development of tachycardia type "pirouette" (bradycardia, electrolyte imbalance, concomitant drugs, prolonging the interval QT), pregnancy.

Ridonex should be used with caution if you have kidney and liver diseases.

Application of pregnancy and breastfeeding:

Clinical studies on the safety of risperidone during pregnancy have not been conducted in humans. In animal studies, risperidone did not show direct toxicity observed reproductive indirect multiple abnormalities associated with CNS and prolactin levels. In none of the studies revealed a teratogenic effect of risperidone. Therefore Ridonex may be used during pregnancy only if the expected benefit of therapy to the mother outweighs the potential risk to the fetus.

It is proved that risperidone and 9-hydroxy-risperidrn stand in mother's milk, so during breast-feeding should avoid use of the drug.

Side effect:

Risperidone is generally well tolerated. In some cases, side effects can not be distinguished from the sign of underlying disease.

Side effects described respiridona lower frequency systems and organs. Criteria frequency of side effects: very common (& ge1 / 10) are often (& ge1 / 100, <1/10), uncommon (& ge1 / 1000, <1/100), rarely (& ge1 / 10,000, <1/1000), very rare (<1 / 10000).

From the nervous system: very often - headache, extrapyramidal symptoms (tremor, rigidity, hypersalivation, bradykinesia, akathisia, acute dystonia) often - dizziness, drowsiness, blurred vision infrequently - decreased ability to concentrate, fatigue, very rarely - insomnia, mania or hypomania, anxiety, agitation, stroke (in elderly patients with predisposing factors).

In patients with schizophrenia: rare - hypervolemia (or iz-za polydipsia or iz-za syndrome of inappropriate secretion of ADH), tardive dyskinesia (involuntary rhythmic movements mainly language and / or persons) rarely - neuroleptic malignant syndrome (hyperthermia, muscle rigidity, instability autonomic function, impaired consciousness and increased CPK), thermoregulation disorders are no data on the frequency of epileptic seizures.

From the digestive system: often - nausea or vomiting, dyspepsia, dry mouth, constipation, abdominal pain, rarely - increase of activity of hepatic transaminases, hypo-or hypersalivation, anorexia, increased or decreased body weight.

From the CCC: often - reflex tachycardia rarely - orthostatic hypotension, or increased blood pressure.

From the side of hematopoiesis: rarely - neutropenia, thrombocytopenia.

From endocrine system: rarely - galactorrhea, menstrual disorders, amenorrhea, weight gain is rare - a gynecomastia rarely - hyperglycemia.

With the genitourinary system: often - erectile dysfunction, priapism infrequently - abnormal ejaculation, orgasm disorders, urinary incontinence.

Allergic reactions: often - rhinitis, rash, rarely - angioedema, photosensitivity.

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

Other: often - arthralgia.

Abrupt withdrawal of antipsychotic drugs may lead to signs of withdrawal (see. "Precautions").

Drug Interactions:

It reduces the effectiveness of levodopa and other dopamine agonists.

Phenothiazines, tricyclic antidepressants and blockers & beta-increase the concentration in the plasma (not affect the concentration of the active antipsychotic fraction).

Fluoxetine can increase the concentration of risperidone in the plasma, but to a lesser degree - the concentration of the active antipsychotic fraction.

At simultaneous reception of carbamazepine and other hepatic enzyme inducers marked reduction in the concentration of the active antipsychotic fraction in plasma.

Clozapine decreases clearance of risperidone.

Ethanol, drugs that suppress the central nervous system - an additive CNS depression function.

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

Fluoxetine can increase the concentration of risperidone in the blood plasma, to a lesser extent - active antipsychotic fraction.

Care must be taken while using the drug Ridonex and furosemide, because in elderly patients with dementia, the combined use of furosemide and risperidone increases the risk of mortality. The mechanism of the interaction of these two active substances is unknown. In a joint application of other diuretics, especially thiazides in low doses, risperidone and this phenomenon is not observed.

Dosage and administration:

Inside.

Adults and children over 15 years - 1 or 2 times a day.

Schizophrenia. Initial dose - 2 mg / day. On Day 2 - to 4 mg / day. Since then, the dose can either maintain the same level, either individually adjusted, if necessary, in the range of 4-6 mg / day.

Doses above 10 mg / day did not show higher efficiency compared with lower doses and may cause the appearance of extrapyramidal symptoms.

The maximum dose - 16 mg / day.

Bipolar disorder with mania. Initial dose - 2 mg / day for 1 admission. Increasing the dose to 1 mg / day - not more than one day. The optimal dose - 1-6 mg / day.

Impaired function of the kidneys and liver. In the presence of liver and kidney disease, regardless of reading, it is necessary to use half of the initial and subsequent doses.

Overdose:

Symptoms: drowsiness, sedation, tachycardia, decreased blood pressure, extrapyramidal disorder is rare - elongation of the QT interval.

Treatment. Ensuring free airway for an adequate supply of oxygen and ventilation, gastric lavage (after intubation if the patient is unconscious) and the appointment of activated charcoal together with a laxative.

Immediately begin ECG monitoring to detect possible arrhythmias. No specific antidote. It is necessary to carry out symptomatic therapy aimed at maintaining vital functions. By reducing blood pressure and vascular collapse in / introduce infusion solutions and / or adrenostimulyatorov, and in the case of acute extrapyramidal symptoms - anticholinergic drugs. Constant medical supervision and ECG monitoring should be continued until the disappearance of symptoms of intoxication.

Precautionary measures:

Elderly patients with dementia

In elderly patients, regardless of treatment, dewatering increases the risk of mortality, so in elderly patients with dementia to avoid fluid loss.

Cerebrovascular adverse effects

Ridonex should be used with extreme caution in the treatment of behavioral disorders in patients with dementia due to the fact that may increase the risk of cerebrovascular adverse events (cerebrovascular complications, transient ischemic attack), so it is advisable to carry out a short-term therapy.

& Alpha-adrenoceptor blocking effect

Ridonex of & alpha-adrenoceptor blocking effect, especially at the beginning of therapy during titration may produce orthostatic hypotension, so it may be necessary to reduce the dose.

You should also apply Ridonex with caution in the presence of cardiovascular events such as heart failure, myocardial infarction, conduction abnormalities, dehydration, hypovolemia, or cerebrovascular disease. Despite the fact that the application of risperidone is not marked lengthening the interval QT, should be prescribed with caution in the event that the patient takes the drugs, which tend to prolongation of the interval QT. If sedation caused by the drug Ridonex insufficient, instead of increasing the dose of risperidone for reducing the risk of side effects, it is advisable to use other drugs, such as benzodiazepines.

Tardive dyskinesia / extrapyramidal syndrome

Preparations having an antagonistic effect on the dopamine receptors may cause tardive dyskinesia, characterized by involuntary rhythmic jerking, especially language and / or facial. The emergence of extrapyramidal symptoms is a risk of formation of tardive dyskinesia. If signs of tardive dyskinesia appear, you need to decide to terminate the application of all antipsychotics.

Neuroleptic malignant syndrome

During the course of therapy with neuroleptics may develop neuroleptic malignant syndrome: hyperthermia, muscle rigidity, autonomic (vegetative) instability, impaired consciousness and increased creatine phosphokinase, myoglobinuria (rhabdomyolysis) and acute renal failure. When you see these signs need to interrupt therapy antipsychotics, including Ridonex and Symptomatic treatment (eg dantrolene infusion solution for the on / in the introduction).

hyperglycemia

Very rarely observed in the treatment of risperidone hyperglycemia or exacerbation of diabetes mellitus, however the presence of diabetes or risk if necessary hyperglycemia to control blood glucose levels.

Classical neuroleptics lower the threshold for seizure activity, therefore, caution should be exercised when treating patients with epilepsy. To prevent weight gain, you can advise the patient to control food intake.

Sudden discontinuation of antipsychotic drugs, especially in the preliminary use of large doses of the drug, very rarely can cause nausea, vomiting, sweating, restlessness, insomnia, psychotic symptoms or resumption incoordination movements (akathisia, dystonia, dyskinesia), it is therefore proposed a gradual withdrawal of the drug.

Like other antagonists of dopamine D2-receptor, risperidone can also increase the level of prolactin in blood plasma. This should be considered in the appointment of risperidone in patients who have a history of breast cancer is a tumor or prolaktinzavisimaya.

There is little experience in the use of risperidone in patients with schizophrenia is younger than 15 years.

Due to the fact that Ridonex tablets contain lactose monohydrate, the drug should not be used at the rarely seen hereditary galactose intolerance, lactase deficiency or malabsorption syndrome glucose / galactose.

Effects on ability to drive or to perform work requiring higher rate of physical and mental reactions. It should refrain during treatment from activities potentially hazardous activities that require high concentration and psychomotor speed reactions.