Treatment of schizophrenia and other psychiatric disorders, including supportive therapy in patients who have had a response to therapy, in order to prevent relapse; treatment of manic episodes in bipolar disorders (auxiliary therapy in combination with normotimics as initial treatment or monotherapy for a period of up to 12 weeks); short term treatment of severe aggression or severe mental symptoms in patients with dementia if there is a threat of harm to themselves or others; symptomatic treatment of defiant oppositional disorders or other social behavior disorders in children, adolescents, and adults with lower-than-average mental development or mental retardation who have manifestations of destructive behavior (impulsivity, autoagression); symptomatic treatment of autistic disorders in children aged 5 years and older, whose symptoms range from hyperactivity to irritability (including aggression, self-harm, anxiety, and pathological cyclical actions).
active substance: risperidone;
1 tablet contains risperidone 2 mg;
Excipients: lactose monohydrate, sodium lauryl sulfate, microcrystalline cellulose, corn starch, magnesium stearate, colloidal anhydrous silica;
composition of shells- polyvinyl alcohol, macrogol, titanium dioxide (E 171), talc, dye yellow FCF (E 110).
Risperidone is a selective monoaminergic antagonist with unique properties. It shows high affinity for serotonergic 5-HT2 and dopaminergic D2 receptors. Risperidone also binds to α1-adrenergic receptors and, with less affinity, to H1-histaminergic and α2-adrenergic receptors. Risperidone does not show affinity for cholinergic receptors. Although risperidone is a potent D2 antagonist associated with its efficacy in productive symptoms of schizophrenia, it does not significantly inhibit motor activity and is less inducing of catalepsy than conventional neuroleptics. Balanced central antagonism of serotonin and dopamine reduces the susceptibility to extrapyramidal side effects and expands the therapeutic effect of the drug to cover the negative and affective symptoms of schizophrenia.
Indication Rispetril :
- Treatment of schizophrenia and other mental disorders, including maintenance therapy, in patients who respond to therapy to prevent recurrence;
- temporary treatment of manic episodes in bipolar disorder (adjuvant therapy in combination with normothymics as initial treatment or as monotherapy for up to 12 weeks). For patients who do not respond to treatment, other treatment options should be considered, including discontinuation of Rispetril.
Treatment can be continued for up to 12 weeks if risperidone is not used in combination with normothymics. This prolonged treatment is used to consolidate the patient’s response. In combination with normothymics, treatment with Rispetril can be discontinued more quickly, as the therapeutic effect of normothymics in combination with risperidone is manifested in the first few weeks of treatment.
No relapse prevention studies have been performed.
Due to the nature of the disease and the drugs used for treatment, including rispetril, attention should be paid to the occurrence of symptoms of depression after the initial response to treatment.
- short-term treatment (up to 12 weeks) of severe aggression or severe mental symptoms in patients with Alzheimer’s dementia in the presence of a threat of harm to themselves or others and in the absence of response to non-pharmacological treatments;
- symptomatic treatment of provocative oppositional disorders or other disorders of social behavior in children, adolescents and adults with mental development below average or mental retardation, which have manifestations of destructive behavior (impulsivity, autoaggression);
- symptomatic treatment of autistic disorders in children over 5 years of age, in which symptoms range from hyperactivity to irritability (including aggression, self-harm, anxiety and pathological cyclic actions). Treatment should be initiated and performed under the supervision of an experienced physician. The use of medicines should be part of an integrated approach to treatment, including social and psychotherapeutic treatments.
Hypersensitivity to the active ingredient or to any of the excipients.
Dementia and symptoms of Parkinson’s disease (rigidity, bradykinesia and parkinsonic posture disorders).
Dementia and suspected dementia with Lewy bodies (in addition to dementia symptoms, at least two of the following symptoms: parkinsonism, visual hallucinations, gait instability).
Method of application and dosage
The usual dose
Rispetril can be used once or twice a day. Doses greater than 8 mg should be divided into two doses (morning and evening). Eating does not affect the absorption of the drug Rispetril.
Gradual discontinuation of treatment is recommended. After abrupt discontinuation of high doses of antipsychotic drugs, acute withdrawal symptoms, including nausea, vomiting, sweating, and insomnia, have been reported very rarely. Recurrence of psychotic symptoms is also possible, involuntary movements have been reported (eg, akathisia, dystonia, and dyskinesia).
To achieve a dose of 0.25-2.5 mg, it is recommended to use Rispetril, oral solution.
Schizophrenia and other mental disorders
Adults (under 65 years old).
Rispetril can be prescribed once or twice a day.
It is necessary to begin reception with 2 mg of Rispetril a day, on the second day the dose can be increased to 4 mg. Thereafter, the dose may be maintained unchanged or, if necessary, individual dose adjustment may be continued. For most patients, the recommended dose is 4-6 mg per day. Some patients may be shown a gradual increase in dose or a decrease in the initial dose.
The maximum daily dose of the drug is 10 mg.
Doses in excess of 10 mg per day have not been shown to be more effective than lower doses, but they may cause extrapyramidal symptoms. As the safety of doses in excess of 16 mg per day has not been studied, doses in excess of this level should not be used.
If additional sedation is required, benzodiazepines may be used concomitantly.
Elderly patients (over 65 years of age).
The recommended starting dose is 0.5 mg twice a day. If necessary, the dose can be increased to 1-2 mg twice a day by increasing by 0.5 mg twice a day.
Manic episodes in bipolar disorder
Adults and children from 15 years old.
The recommended starting dose of Rispetril is 2 mg once a day, in the evening. The dose can be increased individually by adding 1 mg / day no more often than every 24 hours. The recommended dose range is from 2 to 6 mg per day.
As with other symptomatic treatments, long-term use of Rispetril should be periodically reviewed and adjusted throughout therapy. There are no data on the efficacy of rispetril in the treatment of acute bipolar mania lasting more than 12 weeks. If rispetril is used in combination with normothymics, therapy can be stopped earlier, as the onset of treatment can be expected in the first weeks of therapy. Even after the first response to treatment, the possibility of recurrence of depressive symptoms due to the course of the disease and adverse reactions of drugs used for treatment, including rispetril, should be considered.
Elderly patients (from 65 years).
The recommended starting dose is 0.5 mg twice a day. If necessary, the dose can be increased to 1-2 mg twice a day, increasing by 0.5 mg twice a day. As experience in elderly patients is limited, caution is recommended.
Short-term treatment of severe aggression or severe mental symptoms in patients with Alzheimer’s dementia
The recommended starting dose is 0.25 mg twice a day. If necessary, the dose can be increased by increasing the dose by 0.25 mg twice a day no more often than every other day. For most patients, the optimal dose is 0.5 mg twice daily. However, for some patients, the effective dose can be increased to 1 mg twice a day. After reaching the optimal dose, you can consider taking a daily dose once a day. As with other symptomatic treatments, long-term use of Rispetril should be periodically reviewed and adjusted throughout therapy.
Rispetril should be discontinued no later than three months after the start of therapy, and therapy should only be resumed if behavioral disorders recur.
Symptomatic treatment of social behavior disorders or aggressive behavior
Patients weighing> 50 kg
The recommended starting dose is 0.5 mg once a day. If necessary, the dose should be adjusted by adding 0.5 mg once a day no more often than every other day. The optimal dose for most patients is 1 mg once daily. However, for some patients, no more than 0.5 mg once daily is sufficient to achieve a positive effect, while others may require 1.5 mg once daily.
Patients with body weight <50 kg
The recommended starting dose is 0.25 mg once daily. If necessary, the dose can be adjusted by adding 0.25 mg once a day no more often than every other day. The optimal dose for most patients is 0.5 mg once daily. However, for some patients, no more than 0.25 mg once daily is sufficient to achieve a positive effect, while others may require 0.75 mg once daily.
As with other symptomatic treatments, long-term use of Rispetril should be periodically reviewed and adjusted throughout therapy.
There is no experience with the use of rispetril for the symptomatic treatment of social behavioral disorders or aggressive behavior in children under 5 years of age.
Autism (children over 5 years)
The dose should be selected individually, depending on the patient’s condition and clinical response.
Patients with body weight <50 kg
The recommended starting dose is 0.25 mg once daily. From day 4, the dose can be increased by 0.25 mg. A dose of 0.5 mg should be maintained and a clinical response assessed on day 14. Dose escalation of 0.25 mg with an interval of 2 weeks can be considered only for patients with insufficient clinical response.
Patients weighing ≥ 50 kg
The recommended starting dose is 0.5 mg once a day. From day 4, the dose can be increased by 0.5 mg. A dose of 1 mg should be maintained and a clinical response assessed on day 14. Dose escalation of 0.5 mg with an interval of 2 weeks can be considered only for patients with insufficient clinical response.
Rispetril can be used once or twice a day.
Patients who experience drowsiness after taking the drug, it is better to use a daily dose of Rispetril at bedtime. Approximately two-thirds of children with autism complained of weakness, especially during the initial phase of treatment.
Once an adequate clinical response has been achieved, gradual dose reduction should be considered to achieve optimal clinical efficacy and safety.
There is insufficient information to determine the recommended duration of risperidone treatment for patients with autism. Therefore, an experienced specialist should carefully monitor the patient’s condition.
If severe adverse reactions (eg extrapyramidal disorders, tardive dyskinesia or uncontrolled weight gain) occur, the dose of risperidone should be reduced or treatment discontinued.
There is no experience with the use of rispetril for the symptomatic treatment of autism in children under 5 years of age.
To achieve a dose of 0.25-1 mg, it is recommended to use Rispetril, oral solution.
Patients with liver and kidney disease.
In patients with impaired renal function, the active antipsychotic fraction is excreted more slowly than in patients with healthy kidneys. In patients with hepatic impairment, the concentration of the free fraction of risperidone in the blood plasma increases.
Regardless of the indication, these patients are prescribed half of the initial and maintenance doses, dose titration should be slower.
Rispetril should be used with caution in this category of patients.
Transition from therapy with other antipsychotic drugs.
If clinically justified, it is recommended to gradually discontinue previous therapy with other drugs during treatment with Rispetril. However, if the patient is transferred from antipsychotic therapy in the form of a “depot”, it is recommended to start treatment with Rispetril instead of the next scheduled injection. The need to continue current antiparkinsonian therapy should be evaluated periodically.
Risperidone is used to treat disorders of social behavior or aggressive behavior, as well as autistic disorders in children over 5 years of age; for the treatment of manic episodes in bipolar disorder – in children over 15 years of age.
Use during pregnancy or breastfeeding
Although animal studies did not reveal reproductive disorders, there was an indirect effect on prolactin levels. No teratogenic effects were detected. Controlled studies involving pregnant women have not been performed.
Reversible extrapyramidal symptoms were observed in neonates when antipsychotics (including risperidone) were used by the mother during the last trimester of pregnancy. These symptoms included agitation, abnormally increased or decreased muscle tone, tremor, drowsiness, respiratory distress, or feeding problems. These complications can be of varying severity. In some cases, they disappeared after a certain period of time, in some cases, the condition of the infants in the intensive care unit or long-term hospitalization was required.
Rispetril is not recommended during pregnancy unless clearly necessary. If you need to stop taking Rispetril during pregnancy, you should not do it suddenly.
In animal studies, risperidone and 9-hydroxyrisperidone were excreted in breast milk. It has been observed that risperidone and 9-hydroxyrisperidone may also be excreted in human breast milk in small amounts. In some cases, 4.3% of the dose used by the mother in the form of the active antipsychotic fraction of the active substance was determined in breast milk. If necessary, breast-feeding should be discontinued.
Signs and symptoms of overdose observed are known side effects of the drug, which are manifested in an increased form: drowsiness and sedation, tachycardia and hypotension, as well as extrapyramidal symptoms. QT prolongation and convulsions have been reported with overdose. Flicker-flicker associated with risperidone overdose in combination with paroxetine has been reported.
In case of acute overdose, the possibility of drug interaction of several drugs should be analyzed.
Free airway patency should be ensured and maintained to ensure adequate ventilation and oxygenation. Gastric lavage (after intubation if the patient is unconscious) and administration of activated charcoal with a laxative no later than one hour after administration should be considered. Cardiovascular monitoring is shown, which includes continuous ECG recording to detect possible arrhythmias.
Rispetril has no specific antidote. Therefore, appropriate supportive measures should be taken. Hypotension and vascular collapse should be treated with measures such as intravenous infusions and / or sympathomimetic drugs. In case of acute extrapyramidal symptoms, anticholinergic drugs should be prescribed. Continuous medical monitoring and monitoring should be continued until the patient recovers.
- Infections and invasions: pneumonia, bronchitis, upper respiratory tract infections, sinusitis, urinary tract infections, ear infections, influenza, respiratory infections, cystitis, eye infections, tonsillitis, onychomycosis, inflammation of the subcutaneous tissue, viral infection, localized infection;
- From the blood and lymphatic system: neutropenia, decreased white blood cell count, thrombocytopenia, anemia, decreased hematocrit, increased eosinophils;
- From the immune system: hypersensitivity;
- From the endocrine system: hyperprolactinemia;
- From the metabolism and digestion: weight gain, increased appetite, decreased appetite, diabetes, hyperglycemia, polydipsia, weight loss, anorexia, high cholesterol;
- From the psyche: insomnia, sleep disorders, agitation, depression, anxiety,
mania, confusion, decreased libido, nervousness, night terrors;
- From the nervous system: sedation / drowsiness, parkinsonism, headache, akathisia, dystonia, dizziness, dyskinesia, tremor, tardive dyskinesia, cerebral ischemia, lack of response to stimuli, loss of consciousness, depressed consciousness, convulsions, syncope, psychomotor hyperactivity disorder balance, incoordination, postural dizziness, attention deficit, dysarthria, taste disturbances, hypoesthesia, paresthesia;
- From the eyes: blurred vision, conjunctivitis, photophobia, dry eyes, increased tearing, redness of the eyes;
- From the hearing organs: vertigo, tinnitus, ear pain;
- From the cardiac activity: tachycardia, atrial fibrillation, atrioventricular block, cardiac conduction disorders, prolongation of the QT interval on the electrocardiogram, bradycardia, abnormalities on the electrocardiogram, palpitations;
- From the vascular system: hypertension, hypotension, orthostatic hypotension, hot flashes;
- From the respiratory system: dyspnea, pharyngolaryngeal pain, cough, epistaxis, nasal congestion, aspiration pneumonia, pulmonary congestion, impaired airway patency, wheezing, wheezing, dysphonia, respiratory disorders;
- From the digestive system: abdominal pain, abdominal discomfort, vomiting, nausea, constipation, diarrhea, dyspepsia, dry mouth, toothache, fecal incontinence, feces, gastroenteritis, dysphagia, bloating, pancreatitis, gastrointestinal obstruction, swelling of the tongue, cheilitis;
- From the hepatobiliary system: increased levels of transaminases, increased levels of gamma-glutamyl transferase, increased levels of liver enzymes, jaundice;
- From the skin and subcutaneous tissue: rash, erythema.
Keep out of reach of children at a temperature not exceeding 25 ° C, in the original packaging.