Expiration date: 03/2025
Release form and composition:
Tablets, film-coated light orange color, oval, biconcave.
One tablet contains Risperidone 2 mg
Excipients: Cellactose (a spray-dried compound consisting of 75% alpha-lactose monohydrate and 25% cellulose powder), microcrystalline cellulose, sodium croscarmellose, anhydrous colloidal silica, sodium lauryl sulphate, magnesium stearate.
Cover structure: Opadry white 03N28785 (mixture of hypromellose, titanium dioxide, talc, propylene glycol), dye iron oxide yellow (E172), iron oxide red dye (E172).
Tablets, film-coated in a light green color, oval, biconcave.
One tablet contains Risperidone 4 mg
Excipients: Cellactose (a spray-dried compound consisting of 75% alpha-lactose monohydrate and 25% cellulose powder), microcrystalline cellulose, sodium croscarmellose, anhydrous colloidal silica, sodium lauryl sulphate, magnesium stearate.
Cover structure: Opadry white 03N28785 (mixture of hypromellose, titanium dioxide, talc, propylene glycol), quinoline yellow dye (E104), indigo carmine dye (E132).
Pharmachologic effect:
The antipsychotic (neuroleptic).
Risperidone is a selective monoaminergic antagonist with a pronounced affinity for the serotonin 5-HT2 receptor and the dopamine D2-receptor also binds with apha1-adrenoceptors and at slightly lower affinity histamine with H1-receptors and apha2-adrenoceptors. It has no affinity for holinoretseptorami. Also it has sedative, antiemetic and hypothermic effect.
Antipsychotic effect due to blockade of dopamine D2-receptors and mesolimbic system Mesocortical.
Sedative effect due to blockade of adrenergic receptors of the reticular formation of the brain.
Antiemetic effect due to blockade of dopamine D2-receptor trigger zone of the vomiting center.
Hypothermic effect due to 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.
Pharmacokinetics:
Suction
When administered risperidone completely absorbed (regardless of the meal) and Cmax in plasma observed after 1-2 hours.
Distribution
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. Vd is 2.1 L / kg. The risperidone binds to plasma albumin and apha-1 acid glycoprotein. Fractions of risperidone and 9-hydroxy-risperidone associated plasma proteins constitute 88% and 77%, respectively.
Metabolism
Risperidone is metabolized with isozyme 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 risperidone is N-dealkylation. When administered risperidone outputted from T1 / 2 of about three hours. The T1 / 2 of 9-hydroxy-risperidone, and the active antipsychotic fraction is 24 hours.
Most patients Css risperidone observed 1 day after the start of treatment. Css 9-hydroxy-risperidone is reached in most cases within 3-4 days after the start of treatment.
breeding
Excreted in the urine and 70% (35-45% of them as a pharmacologically active fraction) and 14% - in the bile.
Pharmacokinetics in special clinical situations
Elderly patients or patients with poor renal function after a single application of the drug have high levels of the active substance concentration in the plasma and slow their excretion.
Indications:
- Acute and chronic schizophrenia and other psychotic states with productive and / or negative symptoms
- Affective disorders in a variety of mental illnesses
- Behavioral disorders in patients with dementia with aggressive manifestation of symptoms (angry outbursts, physical violence), disorders of mental activity (agitation, delirium) or psychotic symptoms
- As an 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.
Dosage and administration:
In schizophrenia
Adults and children over the age of 15 years Risperidone can be administered 1-2 times / 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 gt10 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 the drug in doses gt16 mg / day has not been studied, doses above this level should not be used.
For information on the use of the drug for the treatment of schizophrenia in children under the age of 15 years are not available.
Elderly Patients are advised to use the drug in an initial dose of 0.5 mg 2 times / day. The dose can be individually increased by 2 times 0.5 mg / day to 2.1 mg 2 times / day.
Patients with liver and kidney diseases is recommended to use the drug in an initial dose of 0.5 mg 2 times / day. This dose can be gradually increased to 1.2 mg 2 times / day.
If drug abuse or drug addiction
The recommended daily dose is 2-4 mg.
When behavioral disorders in patients with dementia
The recommended initial dose - 0.25 mg 2 times / days (in appropriate dosage form). If necessary, the dose may be individually increased by 0.25 mg 2 times / day, no more than a day. For most patients, the optimal dose is 0.5 mg 2 times / day. Some patients shows an application of the drug to 1 mg 2 times / day. Upon reaching the optimal dose may be recommended to use the drug 1 time / day.
Mania in bipolar disorder
The recommended initial dose - 2 mg / day at a time. If necessary, this dose may be increased to 2 mg / day, no more than a day. For most patients the optimal dose is 2-6 mg / day.
In disorders of behavior in patients with mental retardation
Patients with body weight ge50 kg is recommended to use the drug in an initial dose of 0.5 mg 1 time / day. If necessary, the dose may be increased to 0.5 mg / day, no more frequently than every other day. For most patients, the optimal dose is 1 mg / day. However, for some patients the use of preferably 0.5 mg / day, or increase the dose to 1.5 mg / day.
Patients with body weight e50 kg is recommended to use the drug in the initial dose of 0.25 mg 1 time / day. If necessary, the dose may be increased to 0.25 mg / day, no more frequently than every other day. For most patients the optimal dose is 0.5 mg / day. However, for some patients the use of preferably 0.25 mg / day, or increasing the dose to 0.75 mg / day.
Prolonged use of the drug Torendo® adolescents should be under constant medical supervision.
Use of the drug in children under the age of 15 years is not recommended.
Side effects:
From the central and peripheral nervous system: 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 (due to polydipsia or the syndrome of inappropriate secretion of antidiuretic hormone), tardive dyskinesia (involuntary rhythmic movements mainly language and / or persons), CSN (hyperthermia, muscle rigidity, autonomic instability, altered consciousness and increased CPK), thermoregulation disorders and seizures.
From the digestive system: constipation, dyspepsia, nausea or vomiting, abdominal pain, increased liver transaminases, dry mouth, sialoschesis or hypersalivation, anorexia and / or increased appetite, increased or decreased body weight.
Since the cardiovascular system: sometimes - orthostatic hypotension, reflex tachycardia, increased blood pressure.
From endocrine system: galactorrhea, gynecomastia, irregular menstruation, amenorrhea, weight gain, hyperglycemia, exacerbation of preexisting diabetes mellitus.
Reproductive system: priapism, erectile dysfunction, ejaculation disorder, anorgasmia.
From hemopoiesis system: neutropenia, thrombocytopenia.
Dermatological reactions: dry skin, hyperpigmentation, itching, seborrhea.
Allergic reactions: rhinitis, rash, angioedema, photosensitivity.
Other: arthralgia, enuresis.
Contraindications:
- Lactation
- Child and adolescence to 15 years (effectiveness and safety have been established)
- Hypersensitivity to the drug.
With care use in patients with diseases of the cardiovascular system (chronic heart failure, myocardial infarction, conduction disorders of the heart muscle), dehydration and hypovolemia, stroke, Parkinson's disease, seizures (including history), renal or hepatic failure, severe, drug abuse or drug dependence, conditions predisposing to the development of tachycardia type pirouette (bradycardia, electrolyte imbalance, concomitant drugs, prolonging the interval QT), a brain tumor, intestinal obstruction, cases of acute drug overdose, Reye's syndrome (antiemetic effect of risperidone may mask the symptoms of these conditions).
Pregnancy and lactation:
The safety of risperidone during pregnancy has not been studied.
Use of the drug during pregnancy is possible only 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.
Special instructions:
In schizophrenia the beginning of treatment with risperidone is recommended to gradually undo the previous therapy, if clinically justified. If patients are transferred from the depot forms of therapy antipsychotics, risperidone is recommended to start in place of the next scheduled injection. Periodically assess the need for continued therapy potivoparkinsonicheskimi drugs.
In connection with apha-adrenoceptor blocking effect of risperidone, orthostatic hypotension can occur, 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.
The occurrence of extrapyramidal symptoms is a risk factor for the development of tardive dyskinesia. If you have signs and symptoms of tardive dyskinesia should consider abolishing all antipsychotics.
When an NMS is characterized by hypertension, muscle rigidity, autonomic instability functions, impairment of consciousness, and increased levels of creatine kinase is necessary to cancel all antipsychotic drugs, including risperidone.
In case of cancellation of carbamazepine and other hepatic enzyme inducers risperidone dose should be reduced.
Patients should refrain from eating because of the possibility of weight gain.
Use in Pediatrics
Use of the drug in children under the age of 15 years is not recommended.
Effects on ability to drive vehicles and management mechanisms
During treatment should refrain from activities potentially hazardous activities that require high concentration and psychomotor speed reactions, as well as the intake of alcohol (ethanol).
Overdose:
Symptoms: drowsiness, sedation, depression of consciousness, tachycardia, hypotension, extrapyramidal disorder, in rare cases, prolongation of the interval QT.
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.
Drug Interactions:
Since risperidone has an effect primarily on the central nervous system, it should be used with caution in combination with other centrally acting drugs and ethanol.
Risperidone reduces the effectiveness of levodopa and 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 plasma concentrations of risperidone, but this does not affect the concentration of the active antipsychotic fraction.
Fluoxetine can increase the concentration of risperidone in the plasma, but to a lesser extent the concentration of the active fraction antipsychotic, risperidone dose should therefore be corrected.
With simultaneous use of risperidone with drugs that are highly bound to plasma proteins, clinically pronounced displacement of a drug from the plasma protein fraction is observed.
Antihypertensive medicines increase the severity of blood pressure lowering on the background of risperidone.
Conditions and terms:
List B. The drug should be stored out of reach of children at or above 30 ° C. Shelf life - 3 years.
