Risperidone-SZ, pills 4mg, 30pcs

Composition

1 film-coated tablet contains: Active ingredient: risperidone – 4 mg

Excipients (core): lactose monohydrate (milk sugar) – 114.0 mg; microcrystalline cellulose-19.7 mg; pre-gelatinized corn starch (Starch 1500) – 3.0 mg; magnesium stearate-1.0 mg; potato starch-11.0 mg; povidone (polyvinylpyrrolidone medium molecular weight) – 7.3 mg.

Shell composition:

Opadray II – 5 mg (polyvinyl alcohol, partially hydrolyzed-2.2000 mg; talc-1.0000 mg; macrogol (polyethylene glycol 3350) – 0.6175 mg; titanium dioxide E 171-0.6545 mg; soy lecithin E 322-0.1750 mg; aluminum varnish based on yellow quinoline-0.1010 mg; aluminum varnish based on Indigo Carmine-0.2520 mg).

Pharmacological action

Antipsychotic agent (neuroleptic)ATX code: [N05AX08]Pharmacodynamics

Risperidone is an antipsychotic drug derived from benzisoxazole, which also has sedative, antiemetic and hypothermic effects.

Risperidone is a selective monoaminergic antagonist and has a high affinity for serotonergic 5-HT2 and dopaminergic B2 receptors. Risperidone also binds to a, -adrenergic receptors and, somewhat weaker, to Nghistaminergic and a2-adrenergic receptors. Risperidone has no tropicity to cholinergic receptors. The antipsychotic effect is due to the blockade of 02-dopaminergic receptors of the mesolimbic and mesocortical systems.

Risperidone reduces the productive symptoms of schizophrenia (delusions, hallucinations), aggressiveness, automatism, and induces catalepsy to a lesser extent than typical antipsychotics. Balanced central antagonism to serotonin and dopamine can reduce the tendency to extrapyramidal side effects and expand the therapeutic effect of the drug to cover the negative and affective symptoms of schizophrenia.

Clinical data of Schizophrenia

The effectiveness of risperidone in the short-term treatment of schizophrenia was demonstrated in four studies lasting from 4 to 8 weeks, which included 2,500 patients who met the DSM-IV criteria for schizophrenia. In a 6-week placebo-controlled study, when titrated to a dose of 10 mg/day twice daily, risperidone was superior to placebo on the Short Psychiatric Evaluation Scale (BPRS).

In a 6-week placebo-controlled study using risperidone in four fixed doses (2,6,10 and 16 mg/day,2 times a day), in group 4, risperidone was more effective than placebo on the positive and negative syndromes assessment scale (PANSS). In an 8-week comparative study of five fixed doses of risperidone (1,4,8,12 and 16 mg/day, twice daily), risperidone in the 4.8 and 16 mg/day groups was more effective than risperidone 1 mg / day on the PANSS scale. In a 4-week comparative placebo-controlled study of two fixed doses of risperidone (4 and 8 mg/day, once daily), risperidone in both groups was more effective than placebo on several points of the PANSS scale.

Manic episodes in bipolar disorder

The efficacy of risperidone as monotherapy for acute manic episodes in type I bipolar disorder was demonstrated in three double-blind, placebo – controlled trials involving approximately 820 patients with

type 1 bipolar disorder, according to the DSM-IV scale. In these three studies, risperidone at doses of 1-6 mg / day (an initial dose of 3 mg in two studies and 2 mg in one study) was statistically superior to placebo in the primary endpoint, i. e., in the change in the sum of points on the Mania Young Score Scale (YMRS) after 3 weeks compared to the baseline. The results for secondary performance endpoints are generally consistent with the results for the primary endpoint. The percentage of patients with > 50% reduction in YMRS scores after 3 weeks compared to baseline was significantly higher for risperidone than in the placebo group.

The effectiveness of risperidone in combination with mood regulators in the treatment of mania was demonstrated in two three-week double-blind studies on approximately 300 patients meeting the DSM-IV criteria for bipolar disorder type 1. In a 3-week study, risperidone in doses from 1 to 6 mg / day, an initial dose

of 2 mg / day, in combination with lithium or valproate was more effective than lithium or valproate only at the end of the study by the primary set criterion, that is, by the change in the sum of YMRS scores compared to the initial one at the third week.

Long-term aggression in dementia

The efficacy of risperidone in the treatment of psychobehavioral symptoms of dementia, including behavioral problems such as aggression, agitation, psychosis, activity, and affective disorders, was demonstrated in three double-blind placebo-controlled trials in 1,150 patients with moderate to severe dementia. One study was conducted at fixed doses of 0.5.1 and 2 mg / day. Two studies examined non-fixed doses, including groups with risperidone doses of 0.5 to 4 mg / day and 0.5 to 2 mg / day, respectively. Risperidone has shown clinically and statistically high efficacy in the treatment of aggression and, to a lesser extent, arousal and psychosis in elderly patients with dementia (according to the behavioral Pathology scale in Alzheimer’s disease (BEHAVE-AD) and the Cohen Mansfield questionnaire for Arousal (CMAI)).

Behavioral disorders

The efficacy of risperidone in the short-term treatment of aggressive behavior was demonstrated in placebo-controlled studies in approximately 240 patients aged 5 to 12 years with disruptive behavior disorders according to the DSM-IV system and below-average intellectual functioning or with mild mental retardation or moderate learning disabilities. In both studies, risperidone at doses ranging from 0.02 to 0.06 mg / kg / day was significantly more effective than placebo at the pre-established primary efficacy endpoint.

Pharmacokinetics

Risperidone is completely absorbed after oral use, reaching maximum plasma concentrations in 1-2 hours. The absolute oral bioavailability of risperidone is 70%.

Food does not affect the absorption of risperidone, so it can be prescribed regardless of food intake.

Risperidone is rapidly distributed in the body. The volume of distribution is 1-2 l/kg. In plasma, risperidone binds to albumin and alpha-acid glycoprotein. Risperidone is 90% bound by plasma proteins, and 9-hydroxyrisperidone is 77% bound. The equilibrium concentration of risperidone in the body in most patients is reached within 1 day. The equilibrium concentration of 9-hydroxyrisperidone is reached after 4-5 days. Plasma concentrations of risperidone are proportional to the dose of the drug (within therapeutic doses).

Risperidone is metabolized by the CYP2D6 isoenzyme to 9-hydroxy-risperidone, which has a pharmacological effect similar to risperidone. Risperidone and 9-hydroxyrisperidone constitute the active antipsychotic fraction. Metabolism depends on the genetic polymorphism of the CYP2D6 isoenzyme.

Another route of risperidone metabolism is N-dealkylation.

After oral use in patients with psychosis, risperidone is eliminated from the body with a half-life (T 1/2) of about 3 hours. T 1/2 of 9-hydroxyrisperidone and the active antipsychotic fraction is 24 hours.

After a week of taking the drug,70% of the dose is excreted in the urine,14% – in the feces. In the urine, risperidone plus 9-hydroxyrisperidone account for 3545% of the dose. The remaining amount is made up of inactive metabolites.

Special patient groups

A single-dose study of the drug revealed a higher plasma concentration and slower elimination in the elderly and in patients with renal insufficiency. Plasma concentrations of risperidone in patients with hepatic insufficiency were normal.

The pharmacokinetics of risperidone and 9-hydroxyrisperidone in paediatric patients are similar to those in adult patients.

There is no effect of gender, nationality, or smoking on the pharmacokinetics of risperidone.

Indications

Treatment of schizophrenia.

Treatment of manic episodes in the structure of moderate and severe bipolar disorder.

Short-term (up to 6 weeks) treatment of persistent aggression in patients with moderate to severe Alzheimer’s dementia – if non-pharmacological correction methods are ineffective and there is a risk of harm to the patient or others. Short-term (up to 6 weeks) symptomatic treatment of persistent aggression in children aged 5-16 years with moderate to severe mental retardation, due to the severity of which pharmacological correction methods are required (as part of complex therapy).

Use during pregnancy and lactation

There are no data on the safety of risperidone use in pregnant women; In animal experiments, risperidone did not have a direct toxic effect on the reproductive system, but caused some indirect effects mediated through prolactin and the central nervous system. In none of the studies did risperidone have a teratogenic effect, If a woman took antipsychotic drugs (including Risperidone-SZ) in the third trimester of pregnancy, there is a risk of extrapyramidal disorders and/or withdrawal syndrome of varying severity in newborns. These symptoms may include restlessness, hypertension, hypotension, tremor, drowsiness, respiratory problems, and feeding disorders.

Risperidone-SZ can be used during pregnancy only in cases where the potential benefit to the woman outweighs the possible risk to the fetus.

Since risperidone and 9-hydroxyrisperidone pass into breast milk, women using Risperidone-SZ should not breastfeed.

Contraindications

individual hypersensitivity chuvstvitelnosti to risperidone or any other ingredient of this medicine;

– lactase deficiency, lactose intolerance, glucose-galactose malabsorption;

– in the treatment of persistent aggression in conduct disorder in children with mental retardation moderate and severe children up to age 5 years (experience of not enough)

– for other indications children up to age 18 years.

WITH CAUTION

Use with caution in the following conditions::

– cardiovascular disease (congestive heart failure, myocardial infarction, conduction disorders cardiac muscle);

– dehydration and hypovolemia;

– cerebrovascular disease;

Parkinson’s disease,

convulsions and epilepsy (such cispa in the anamnesis);

– severe renal or hepatic insufficiency (see section “Method of use and dose”),

the prescription drug abuse or drug dependence (see section “Method of use and dose”);

– status predisposing to the development of tachycardia type “pirouette” (bradycardia, electrolyte imbalance, concomitant medication, lengthening of the QT interval):

– brain tumor, intestinal obstruction, cases of acute drug overdose, Reis syndrome (the antiemetic effect of risperidone may mask the symptoms of these conditions):

– pregnancy and lactation.

Side effects

Side effects of Risperidone-SZ in therapeutic doses are given with frequency distribution and systemic organ classes. The frequency of side effects was classified as follows: very frequent (*1/10 cases), frequent (>1/100 and >< 1/10 cases), infrequent (> 1/1000 and < 1/10 cases), infrequent (>< 1/100 cases), rare (>1/10000 and < 1/100 cases), rare (>< 1/1000 cases) and very rare (

InLekiii:

very often in elderly patients with dementia – urinary tract infection; often, nasopharyngitis, and upper respiratory tract infection, bronchitis, sinusitis, urinary tract infection, rhinitis, flu-like illness: in elderly patients with dementia – pneumonia, cellulitis;

infrequently – ear infection, viral infection, tonsillitis, eye infection, localized infection, cystitis, onychomycosis, acrodermatitis, infections of the respiratory tract.

Hematological disorders and disorders of the lymphatic system

infrequently-thrombocytopenia, anemia, neutropenia, leukopenia, decreased hematocrit;

rarely-granulocytopenia, agranulocytosis

Co stolons of the immune system:

infrequently-hypersensitivity;

very rarely-anaphylactic reactions, anaphylactic shock.

From the endocrine system: often-hyperprolactinemia,

rarely-violation of the secretion of antidiuretic hormone, diabetic coma.

Metabolic and nutritional disorders:

often-increased appetite, in elderly patients with dementia-decreased appetite; infrequently-polydipsia, anorexia, diabetes mellitus: rarely-hypoglycemia, water intoxication; very rarely-diabetic ketoacidosis.

Mental disorders: very often – insomnia;

often-anxiety, sleep disorders, nervousness, lethargy, in elderly patients with dementia-confusion;

infrequently-flattening of affect, mania, decreased libido, depression, nightmares; very rarely-anorgasmia.

Nervous system disorders:

often – parkinsonism (hypersalivation, a syndrome of “gears”, akinesia, bra – dykinesia, hypokinesia, skeletal muscle rigidity, Mesopotamia face), drowsiness, headaches, sedation, dizziness;

often, akathisia (including anxiety), tremor, dystonia (including muscle spasms, involuntary muscle contraction, contracture of the muscles, involuntary movements of the eyeballs, paralysis of the tongue), lethargy, postural dizziness, dyskinesia (including muscle twitching, chorea and choreoathetosis), dysarthria, drooling, impaired attention, gait disturbance, increased sleepiness; in elderly patients with dementia – depression, salivation, cerebrovascular disorders; rarely, lack of response to stimuli, loss of coordination, loss of consciousness, fainting, slurred speech, hypesthesia, paresthesia, psychomotor hyperactivity, tardive dyskinesia, cerebrovascular disorders;

rarely – neuroleptic malignant syndrome, extrapyramidal symptoms (tremor, rigidity, hypersalivation, bradykinesia, akathisia, acute dystonia), rhythmic nodding.

Ophthalmic disorders:

often-decreased visual acuity, in elderly patients with dementia-conjunctivitis; infrequently-conjunctival hyperemia, involuntary rotation of the eyeballs, crusting on the edges of the eyelids, dry eyes, increased lacrimation, photophobia, increased intraocular pressure.

From the side of the ear and labyrinth:

infrequently – tinnitus, ear pain, vertigo, chronic otitis media.

From the cardiovascular system

often – tachycardia, orthostatic hypotension, decreased blood pressure, palpitations, in elderly patients with dementia – transient ischemic attack; rarely – bradycardia, sinus arrhythmia, atrial fibrillation, atrioventricular block, “tides” of blood, conduction disorder of the heart muscle; very rarely – deep vein thrombosis, pulmonary embolism, venous thromboembolism. Respiratory, thoracic disorders and disorders of the mediastinum: often – nasal congestion, dyspnea, epistaxis, nasal sinuses, cough, runny nose, pain in the region of the larynx and pharynx, the congestion in the lungs, in elderly patients with dementia – cough, runny nose;

rarely, wheezing, aspiration pneumonia, dysphonia, airway obstruction, moist rales, respiratory disorder; rare syndrome, sleep apnea, hyperventilation.

From the gastrointestinal tract:

often – nausea, constipation, dyspepsia, vomiting, diarrhea, drooling, dry mouth, stomach discomfort, abdominal pain, in elderly patients with dementia-dysphagia, fecaloma; infrequently-fecal incontinence, flatulence, gastroenteritis, toothache, tongue edema, cheilitis. dysgeusia; very rarely-intestinal obstruction, pancreatitis.

Hepatobiliary disorders: rarely-jaundice.

Skin and subcutaneous tissue disorders:

often-rash, itching, acne, in elderly patients with dementia – erythema;

infrequently-eczema, dry skin, seborrheic dermatitis, hyperkeratosis, skin pigmentation disorder

, skin inflammation, skin damage, angioedema, alopecia;

rarely-dandruff.

Musculoskeletal and connective tissue disorders:

often – musculoskeletal pain, back pain, arthralgia, limb pain, myalgia,

neck pain, in elderly patients with dementia-gait disorders, joint swelling;

infrequently-joint stiffness, muscle weakness;

rarely-rhabdomyolysis.

From the kidneys and urinary tract: often-urinary incontinence, enuresis, pollakiuria; infrequently-urinary retention, dysuria.

From the reproductive system and mammary glands: often-lack of ejaculation, galactorrhea;

infrequently-menstrual disorders, amenorrhea, gynecomastia, vaginal discharge, erectile dysfunction, ejaculation disorder, breast enlargement, sexual dysfunction, breast discharge; very rarely-priapism.

Influence on the course of pregnancy, postpartum and perinatal conditions: very rarely – withdrawal syndrome in newborns.

General violations:

often – fatigue, asthenia, fever, chest pain, weight gain, slowness, in elderly patients with dementia-peripheral edema, gait disorders, mild edema;

infrequently-thirst, fever, malaise, facial edema, chills; rarely-hypothermia, withdrawal syndrome, cold extremities.

Violations of laboratory and instrumental indicators: often – increased heart rate in elderly patients with dementia – increased body temperature;

infrequently – an increase in the number of eosinophils in the blood, increase the activity of creativos farinaz, reducing the number of leukocytes in the blood, increase the activity of liver enzymes, increased activity of gamma-glutamyl transferase, reduced hematocrit, increase in transaminases, increase in the concentration of cholesterol in the blood, increasing the concentration of triglycerides in the blood, granulocytopenia, hyperglycemia, weight loss, prolonged QT interval on the electrocardiogram, changes on the electrocardiogram. Class-effects

Very rare cases of QT prolongation have been reported in post-marketing studies of risperidone. In addition, effects such as ventricular arrhythmia, ventricular fibrillation, ventricular tachycardia, sudden death, cardiac arrest, fluttering and flickering were noted.

Venous thromboembolism

Cases of venous thromboembolism, including cases of pulmonary embolism, as well as deep vein thrombosis, have been reported with the use of neuroleptics (frequency unknown).

Weight gain

In a 6-8-week placebo-controlled study in adult patients with schizophrenia treated with risperidone and placebo, clinically significant weight gain of 7% or more was observed in the risperidone group (18%), which is higher than in the placebo group (9%). In a 3-week placebo-controlled study in adult patients with acute mania, weight gain of 7% or more by the end of the study was adequate in the risperidone group (2.5%) and placebo (2.4%) and was slightly greater in the control group (3.5%).

In children and adolescents with antisocial manifestations and other behavioral disorders in long-term studies, the average body weight increased by 7.3 kg after 12 months of treatment. The expected increase in body weight in healthy children aged 5-12 years is from 3 to 5 kg per year. Girls 12-16 years old gain from 3 to 5 kg per year, and boys about 5 kg per year.

Elderly patients with dementia

Side effects in elderly patients with dementia in clinical trials were: transient ischemic attack, stroke; urinary tract infections, peripheral edema, drowsiness, cough.

Children

Types of adverse reactions in children are similar to those observed in adult patients. The following adverse reactions were reported with a frequency of 5% in children (5 to 17 years) and at least twice the frequency observed in clinical trials in adults:

drowsiness, sedation, fatigue, headache, increased appetite, vomiting, upper respiratory tract infections, nasal congestion, abdominal pain, dizziness, cough, fever, tremor, diarrhea, and enuresis.

The effect on puberty has not been studied with long-term treatment with risperidone.

Interaction

Given that Risperidone-SZ primarily affects the central nervous system, it should be used with caution with alcohol, opiates, antihistamines, and benzodiazepines because of the increased risk of sedation.

Risperidone reduces the effectiveness of levodopa and other dopamine receptor agonists. However, if concomitant use is necessary, especially in end-stage Parkinson’s disease, the minimum effective dose of each treatment should be prescribed.

Caution should be exercised when using Risperidone-SZ in combination with drugs that increase the QT interval, for example, Class 1a antiarrhythmic drugs (for example, quinidine, disopyramide, procainamide), Class III antiarrhythmic drugs (for example, amiodarone, sotalol), tricyclic antidepressants (amitriptyline), tetracyclic antidepressants (maprotilin), certain antihistamines medications, other antipsychotic medications, certain antimalarial medications (quinine and mefloquine), and certain medications that cause electrolyte disturbances (hypokalemia, hypomagnesemia), bradycardia, or inhibit the hepatic metabolism of risperidone.

Clozapine reduces the clearance of risperidone.

When using carbamazepine, a decrease in the concentration of the active antipsychotic fraction of risperidone in plasma was noted. Similar effects can be observed with other inducers of the CYP3A4 isoenzyme and P-glycoprotein. When carbamazepine or other inducers of the SURZA 4/P-glycoprotein isoenzyme are prescribed and discontinued, the dose of Risperidone-SZ should be adjusted.

Fluoxetine and paroxetine, inhibitors of the CYP2D6 isoenzyme, increase the concentration of risperidone in plasma, but to a lesser extent the concentration of the active antipsychotic fraction. When prescribing and after discontinuing fluoxetine or paroxetine, the dose of Risperidone-SZ should be adjusted. Other inhibitors of the CYP2D6 isoenzyme, such as quinidine, can alter the plasma concentration of risperidone in the same way.

Verapamil, an inhibitor of the CYP3A4 isoenzyme and P-glycoprotein, increases the concentration of risperidone in plasma.

Topiramate modestly reduces the bioavailability of risperidone, but not the active antipsychotic fraction. This interaction is not considered clinically significant. Phenothiazine derivatives, tricyclic antidepressants, and some p-blockers may increase plasma concentrations of risperidone, but this does not affect the concentration of the active antipsychotic fraction. Amitriptyline does not affect the pharmacokinetics of risperidone and the active antipsychotic fraction. Cimetidine and ranitidine increase the bioavailability of risperidone, but have minimal effect on the concentration of the active antipsychotic fraction. Erythromycin, an inhibitor of the CYP3A4 isoenzyme, does not affect the pharmacokinetics of risperidone and the active antipsychotic fraction. Cholinesterase inhibitors (galantamine and donepezil) do not have a clinically significant effect on the pharmacokinetics of risperidone and the active antipsychotic fraction.

When using Risperidone-SZ together with other drugs that are highly bound to plasma proteins, there is no clinically pronounced displacement of any drug from the plasma protein fraction.

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

Risperidone has no clinically significant effect on the pharmacokinetics of lithium, valproic acid, digoxin, or topiramate.

Food intake does not affect the absorption of risperidone.

How to take, course of use and dosage

Inside, regardless of food intake

1. Schizophrenia

Adults. Risperidone can be given once or twice a day.

The initial dose of Risperidone-SZ is 2 mg per day. On the second day, the dose should be increased to 4 mg per day. From this point on, the dose can either be kept at the same level, or individually adjusted if necessary. Usually, the optimal dose is from 4 to 6 mg per day. In some cases, a slower increase in the dose and lower initial and maintenance doses may be justified.

Doses higher than 10 mg / day have not been shown to be more effective than lower doses and may cause extrapyramidal symptoms. Due to the fact that the safety of doses above 16 mg per day has not been studied, doses above this level should not be used. Elderly patients. An initial dose of 0.5 mg twice daily is recommended.

The dose can be individually increased by 0.5 mg twice a day to a dose of 1 to 2 mg twice a day.

Children

There is no information on the use of the drug for the treatment of schizophrenia in children under 18 years of age.

2 Manic episodes in the structure of moderate to severe bipolar disorder

Adults. The recommended starting dose of the drug is 2 mg per day in one dose. If necessary, this dose can be increased by at least 1 mg per day after 24 hours. For most patients, the optimal dose is from 1-6 mg per day.

Elderly patients. An initial dose of 0.5 mg twice daily is recommended. If necessary, the dose can be individually increased by 0.5 mg twice a day to a dose of 1 to 2 mg twice a day. Caution should be exercised when prescribing the drug to elderly patients.

Children

There are no data on the use of the drug for the treatment of manic episodes in the structure of moderate and severe bipolar disorder in children under 18 years of age.

3. Persistent aggression in patients with moderate to severe Alzheimer’s dementia

An initial dose of 0.25 mg twice daily is recommended. If necessary, the dose can be individually increased to 0.25 mg 2 times a day, no more than every other day. For most patients, the optimal dose is 0.5 mg twice daily. However, some patients are shown to take 1 mg 2 times a day. Risperidone should not be used for more than 6 weeks in the treatment of persistent aggression in patients with moderate to severe Alzheimer’s dementia.

4. Persistent aggression in behavioral disorders in children aged 5-16 years with moderate and severe mental retardation

Patients with a body weight of 50 kg or more – the recommended initial dose of the drug is 0.5 mg once a day. If necessary, this dose can be increased by 0.5 mg per day, no more than every other day. For most patients, the optimal dose is 1 mg per day. However, for some patients,0.5 mg per day is preferable, while some require an increase in the dose to 1.5 mg per day.

Patients with a body weight of 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, no more than every other day. For most patients, the optimal dose is 0.5 mg per day, but for some patients,0.25 mg per day is preferable, while some require an increase in the dose to 0.75 mg per day.

Long-term use of Risperidone-SZ in adolescents should be carried out under the constant supervision of a doctor.

Risperidone-SZ is not recommended for children under 5 years of age, as there are no data on such disorders in children under 5 years of age.

Renal and hepatic insufficiency

Patients with kidney disease have a reduced ability to remove the active antipsychotic fraction compared to other patients. In patients with liver diseases, there is an increased concentration of the free fraction of risperidone in the blood plasma. The initial and maintenance dose should be reduced by 2 times according to the indications, and the dose increase in patients with liver and kidney diseases should be carried out more slowly.

Risperidone should be administered with caution in this category of patients.

Overdose

Symptoms: drowsiness, sedation, tachycardia, low blood pressure, extrapyramidal symptoms. Prolongation of the QT interval and seizures were observed. Bidirectional ventricular tachycardia was observed with the combined use of an increased dose of risperidone and paroxetine.

In case of overdose, the possibility of overdose from taking several medications should be considered.

Treatment. It is necessary to achieve and maintain free airway patency to ensure adequate oxygen supply and ventilation, perform gastric lavage (after intubation, if the patient is unconscious) and prescribe activated charcoal along with a laxative. ECG monitoring should be started immediately to detect possible arrhythmias.

There is no specific antidote, and appropriate symptomatic therapy should be performed. Low blood pressure and collapse should be treated with intravenous fluid infusions and / or sympathomimetic medications. In case of acute extrapyramidal symptoms, m-holinoblockers (for example, trihexyphenidyl) should be prescribed. Continuous medical supervision and monitoring should be continued until the symptoms of intoxication disappear.

Special instructions

Transition from therapy with other antipsychotic drugs. In patients with schizophrenia, it is recommended to gradually cancel the previous therapy at the beginning of treatment with Risperidone-SZ, if this is clinically justified. At the same time, if patients are transferred from depot therapy with forms of antipsychotic drugs, it is recommended to start therapy with Risperidone-SZ instead of the next scheduled injection. Periodically, the need for continuing current antiparkinsonian therapy should be evaluated.

Use in elderly patients with dementia. Elderly patients with dementia who are treated with atypical antipsychotics have an increased mortality rate compared to placebo in studies of atypical antipsychotics, including risperidone. When using risperidone for this population, the death rate was 4.0% for patients taking risperidone, compared to 3.1% for placebo. The average age of deceased patients is 86 years (range 67-100 years).

For elderly patients with dementia taking oral forms of risperidone, increased mortality was observed in patients taking furosemide and risperidone (7.3%, mean age 89 years, range 75-97 years) compared to the risperidone-only group (3.1%, mean age 84 years, range 70-96 years) and the furosemide-only group (4.1%, mean age 80 years, range 67-90 years). No pathophysiological mechanisms have been established to explain this observation. However, special care should be taken when prescribing the drug in such cases. There was no increase in mortality in patients taking other diuretics concomitantly with risperidone. Regardless of treatment, dehydration is a common risk factor for mortality and should be carefully monitored in elderly patients with dementia.

Cerebrovascular disorders

In patients with dementia treated with atypical antipsychotic agents, there is an approximately 3-fold increase in the risk of cerebrovascular adverse reactions in randomized placebo-controlled clinical trials. A generalized analysis of the results of six placebo-controlled risperidone trials, mainly in elderly patients (older than 65 years) with dementia, showed that cerebrovascular adverse reactions (serious and non-serious, combined) occurred in 3.3% (33/1009) of patients treated with risperidone and in 1.2% (8/712) of patients treated with placebo. The odds ratio is 2.96 (95% confidence interval). The mechanism of this risk has not been studied. An increased risk cannot be excluded from other antipsychotic medications and other patient groups. Risperidone should be used with caution in patients with risk factors for stroke.

The risk of adverse cerebrovascular reactions is significantly higher in patients with mixed or vascular dementia than in patients with Alzheimer’s dementia. Therefore, patients with mixed or vascular dementia should not be prescribed risperidone.

It is necessary to evaluate the risks and therapeutic benefits of risperidone in elderly patients with dementia, taking into account the prognostic risk factors for stroke in a particular patient. The patient and his or her surroundings should be warned about the need for urgent reporting of symptoms and signs of potential cerebrovascular adverse reactions, in particular sudden weakness or numbness of the face, upper and lower extremities, speech or vision disorders. In this case, all therapeutic options are urgently considered, including discontinuation of risperidone.

In the case of sustained aggression in patients with Alzheimer’s dementia, risperidone is intended only for short-term use as a supplement to non-pharmacological measures if they are ineffective or limited in the absence of a potential danger to the patient or his environment. Constant monitoring and evaluation of the patient’s condition is required, as well as justification for the need for further treatment.

Orthostatic hypotension. Due to the a-blocking effect of risperidone, orthostatic hypotension may occur, especially during the initial dose selection period. A clinically significant reduction in blood pressure is observed when risperidone is co-administered with antihypertensive drugs. When lowering blood pressure, you should consider reducing the dose. In patients with diseases of the cardiovascular system, as well as with dehydration, hypovolemia or cerebrovascular disorders, the dose should be increased gradually, according to the recommendations.

Leukopenia, neutropenia, agranulocytosis

Leukopenia, neutropenia, and agranulocytosis have been reported with antipsychotic medications, including Risperidone-SZ. Agranulocytosis was observed very rarely during post-marketing observations. Patients with a clinically significant decrease in the number of white blood cells in the anamnesis or drug-dependent leukopenia/neutropenia are recommended to perform a complete blood test during the first months of therapy, discontinuation of treatment with Risperidone-SZ should be considered at the first clinically significant decrease in the number of white blood cells in the absence of other possible causes. Patients with clinically significant neutropenia should be monitored for fever or infection symptoms and start treatment immediately if such symptoms occur. Patients with severe neutropenia (absolute neutrophil count less than 1 x 109/l) should discontinue Risperidone-SZ until the white blood cell count returns to normal.

Venous thromboembolism

Cases of venous thromboembolism have been reported with the use of antipsychotic drugs. Since patients taking antipsychotic medications are often at risk of developing venous thromboembolism, all possible risk factors should be identified before and during treatment with Risperidone-SZ and preventive measures should be taken.

Tardive dyskinesia and extrapyramidal disorders

Drugs that have the properties of dopamine receptor antagonists can cause tardive dyskinesia, which is characterized by rhythmic involuntary movements, mainly of the tongue and / or facial muscles. There are reports that the occurrence of extrapyramidal symptoms is a risk factor for the development of tardive dyskinesia. Risperidone is less likely to cause extrapyramidal symptoms than classical antipsychotics. If signs and symptoms of tardive dyskinesia occur, discontinuation of all antipsychotic medications should be considered.

Neuroleptic malignant syndrome

In case of neuroleptic malignant syndrome characterized by hyperthermia, muscle rigidity, instability of autonomous functions, impaired consciousness, and increased creatine phosphokinase activity (myoglobinuria (rhabdomyolysis) and acute renal failure may also occur), all antipsychotic medications, including Risperidone-SZ, should be discontinued.

Parkinson’s disease and dementia with Lewy bodies

Antipsychotic medications, including Risperidone-SZ, should be used with caution in patients with Parkinson’s disease or Lewy body dementia, as both groups of patients have an increased risk of developing neuroleptic malignant syndrome and increased sensitivity to antipsychotic medications (including blunted pain sensitivity, confusion, postural instability with frequent falls, and extrapyramidal symptoms).

Hyperglycemia and diabetes mellitus

Hyperglycemia, development of diabetes mellitus, and exacerbation of pre – existing diabetes mellitus were observed during treatment with Risperidone-SZ. Establishing the relationship between the use of atypical antipsychotic drugs and impaired glucose metabolism is complicated by an increased risk of diabetes in patients with schizophrenia and the prevalence of diabetes in the general population. Given these factors, the relationship between the use of atypical antipsychotic drugs and the development of side effects associated with hyperglycemia is not fully established. All patients should be clinically monitored for symptoms of hyperglycemia and diabetes

mellitus (see section “Side effects”),

Hyperprolactinemia

Studies on tissue cultures have shown that cell growth in breast tumors can be stimulated by prolactin. Risperidone should be used with caution in patients with hyperprolactinemia and in patients with potentially prolactin-dependent tumors.

Weight gain

When treated with Risperidone-SZ, a significant increase in body weight was observed. It is necessary to monitor the body weight of patients during therapy with Risperidone-SZ. Prolongation of the QT interval

As with other antipsychotic agents, caution should be exercised when prescribing Risperidone-SZ to patients with a history of cardiac arrhythmias, patients with congenital QT prolongation, and when co-administered with drugs that increase the QT interval.

Priapism

Drugs that have alpha-blocking effects can cause priapism. In post-marketing studies of Risperidone-SZ, priapism has been reported.

Regulation of body temperature

Antipsychotic drugs are attributed to such an undesirable effect as a violation of the body’s ability to regulate body temperature. Caution should be exercised when prescribing Risperidone-SZ to patients with conditions that may contribute to an increase in internal body temperature, such as intense physical activity, dehydration, exposure to high external temperatures, or simultaneous use of drugs with anticholinergic activity.

Antiemetic effect

In preclinical studies, the antiemetic effect of risperidone was revealed. This effect, if it occurs in humans, can mask the objective and subjective symptoms of overdose of certain drugs, as well as diseases such as intestinal obstruction, Reye’s syndrome and brain tumors.

Threshold of convulsive activity

The ability of typical antipsychotics to reduce the threshold of convulsive activity is known. Risperidone-SZ should be used with caution in patients with epilepsy.

Withdrawal syndrome

Upon discontinuation of treatment, a gradual dose reduction is recommended. Withdrawal symptoms: Nausea, vomiting, sweating, and insomnia have been reported very rarely when high-dose antipsychotic medications are abruptly discontinued.

Children and teenagers

The sedative effect of risperidone should be carefully monitored, and the time of taking Risperidone-SZ may change.

Body weight should be monitored. Regular assessment of endocrine function, extrapyramidal symptoms, and movement disorders is required.

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25 °C.

Keep out of reach of children

Shelf

life is 3 years. Do not use after the expiration date indicated on the package.

Active ingredient

Risperidone

Conditions of release from pharmacies

By prescription

Dosage form

Tablets