Rispaksol - instructions for use, dose, side effects, contraindications

2 mg tablets: lactose anhydrous - 145.0 mg; corn starch - 10.0 mg, magnesium stearate - 2.0 mg, silicon dioxide colloid, anhydrous 1.0 mg; microcrystalline cellulose - 40.0 mg;

tablets 4 mg: lactose, anhydrous - 290.0 mg; corn starch - 20.0 mg, magnesium stearate - 4.0 mg, silicon dioxide colloid, anhydrous - 2.0 mg; cellulose microcrystalline - 80.0 mg.

Tablet casing:

2 mg tablets: dye Opadray orange OhY-8729 (hydroxypropylmethylcellulose (hypromellose), macrogol 400, titanium dioxide, yellow "sunset sunset" FCF (E 110), yellow quinoline (E 104)) 3.7 mg, macrogol 6000 - 0.3 mg, carnauba wax - q.s.;

tablets 4 mg: coloring Opadrai AMB green 80W21165 (E 172), indigocarmine (E 132), soy lecithin, polyvinyl alcohol, yellow quinoline (E 104), talc, titanium dioxide, xanthan gum) 8.0 mg, carnauba wax - q.s.

Description:

Tablets 2 mg: round, biconvex tablets with a risk on one side, coated with an orange coating. On the site of the fault white.

Tablets 4 mg: round, biconvex tablets with a risk (four parts) on one side, covered with a shell of green. On the site of the fault white.

Pharmacotherapeutic group:antipsychotic agent (antipsychotic)

ATX: & nbsp

N.05.A.X Other antipsychotics

N.05.A.X.08 Risperidone

Pharmacodynamics:

Antipsychotic agent (antipsychotic), benzisoxazole derivative; also has a sedative, antiemetic and hypothermic effect.

Risperidone is a selective monoaminergic antagonist with a pronounced affinity for serotonergic 5-HT₂ and dopaminergic D₂receptors, also binds to alpha₁-adrenoceptors and, with slightly less affinity, with H₁-gistaminergic and alpha₂-adrenergic receptors. Has no tropism for cholinergic receptors

The antipsychotic effect is due to the blockade of dopamine D₂receptors of the mesolimbic and mesocortical system.

Sedative action is due to blockade of adrenoreceptors of the reticular formation of the brainstem; antiemetic effect - blockade of dopamine D₂receptors of the trigger zone of the vomiting center; hypothermic action - blockade of dopamine receptors of the hypothalamus.

Reduces productive symptoms (delirium, hallucinations, aggressiveness), automatism. It causes less inhibition of motor activity and to a lesser degree induces catalepsy than classical antipsychotics (antipsychotics).

A balanced central antagonism to serotonin and dopamine may reduce the risk of extrapyramidal symptoms.

Risperidone can cause a dose-dependent increase in prolactin concentration in the plasma.

Pharmacokinetics:

Suction

Risperidone after oral administration is completely absorbed, reaching the maximum concentrations in the plasma after 1-2 hours. Absolute the bioavailability of risperidone after ingestion is 70%, relative bioavailability - 94% when compared with risperidone in the form of a solution. Food does not affect the absorption of the drug, so risperidone can be administered regardless of food intake. The equilibrium concentration of risperidone in the body in most patients is reached within 1 day. The equilibrium concentration of 9-hydroxyrispsridone is reached within 4-5 days.

Distribution

Risperidone is rapidly distributed in the body. The volume of distribution is 1-2 l / kg. In the plasma risperidone binds to albumin and alpha₁acid glycoprotein. Risperidone 90% bound to plasma proteins, 9-hydroxyrisperidone - by 77%.

Metabolism and excretion

Risperidone is metabolized isoenzyme CYP 2D6 to 9-hydroxyrisperidone, which has a similar risperidone pharmacological action.

Risperidone and 9-hydroxyrisperidone constitute an active antipsychotic fraction.

Isozyme CYP 2D6 is subject to genetic polymorphism. In patients with intensive isoenzyme metabolism CYP 2D6 risperidone quickly turns into 9-hydroxyrisperidone, while in patients with weak metabolism this transformation occurs much more slowly. Although patients with intensive metabolism have a lower concentration of risperidone and a higher concentration of 9-hydroxyrisperidone than patients with poor metabolism, the total pharmacokinetics of risperidone and 9-hydroxyrisperidone after taking one or more doses is similar in patients with intensive and weak metabolism CYP 2D6.

Another way of metabolizing risperidone is N-dealkylation.

Research in vitro on microsomes of the human liver showed that risperidone in clinically relevant concentrations, in in general, does not inhibit metabolism medicines, subject to biotransformation by isoenzymes of the P450 system, including CYP1A2, CYP2C8/9/10, CYP 2D6, CYP2E1, CYP3A4 and CYP 3A5. A week after the start of the drug, 70% of the dose is excreted in the urine, 14% - with feces. In the urine risperidone together with 9-hydroxyrisperidone constitute 35-45% of the dose. The remaining quantity are inactive metabolites. After oral administration in patients with psychosis risperidone is excreted from the body with a half-wave period (T_1/2) for about 3 hours. T_1/29-hydroxyrisperidone and active antipsychotic fraction is 24 hours.

Linearity

The concentration of risperidone in plasma is directly proportional to the dose taken in the therapeutic dose range.

Elderly patients and patients with hepatic and /or renal insufficiency

After a single dose of risperidone in elderly patients, the concentration of active antipsychotic fraction in plasma was on average 43% higher, the half-life lasted 38% longer, and the clearance decreased by 30%. In patients with renal insufficiency, there was an increase in plasma concentration and a decrease in clearance of the active antipsychotic fraction by an average of 60%. In patients with hepatic insufficiency the concentration of risperidone in plasma did not change, but the average concentration of the free fraction of risperidone increased by 35%.

Children

The pharmacokinetics of risperidone, 9-hydroxyrisperidone and the active antipsychotic fraction in children are comparable to that of adult patients.

Influence of sex, race and smoking

Population pharmacokinetic analysis did not reveal an obviousinfluences sex, race or smoking on the pharmacokinetics of risperidone and the active pharmacokinetic fraction.

Indications:

- LThe diagnosis of schizophrenia in adults and children aged 13 to 17 years;

- treatment of manic episodes associated with bipolar disorder of moderate to severe in adults.

Contraindications:

- Hypersensitivity to the components of the drug;

- phenylketonuria;

- Children up to the age of 13 (the inability to provide for this drug a minimum effective dose of less than 1 mg).

Carefully:

- Diseases of the cardiovascular system system (chronic cardiac deficiency, myocardial infarction, conduction disorders heart muscle);

- dehydration and hypovolemia;

- disorders of cerebral circulation;

- Parkinson's disease;

- convulsions (including in the anamnesis);

- severe renal or hepatic insufficiency (see recommendations for dosing);

- abuse of medicinal drugs or drug dependence (see recommendations for dosing);

- conditions predisposing to the development of tachycardia such as "pirouette" (bradycardia, electrolyte imbalance, concomitant medication prolonging the interval QT);

- brain tumor, intestinal obstruction, cases of acute drug overdose, Rice syndrome (antiemetic effect of risperidone may mask the symptoms of these conditions);

- risk factors for thromboembolism of venous vessels;

- disease of diffuse Levi bodies;

- elderly patients with cerebrovascular dementia;

- hyperglycemia;

- simultaneous application with furosemide.

Pregnancy and lactation:

Pregnancy

There were no full studies of risperidone in pregnant women. According to observations in the postmarketing period, during the use of risperidone during the last trimester of pregnancy, the newborn has reversible extrapyramidal symptoms, so newborns should be carefully monitored.

In animal studies risperidone did not have a teratogenic effect, but other types of toxic effects on the reproductive system were observed. The potential risk to people is unknown. The drug can be used during pregnancy only if the expected benefit of using a pregnant woman exceeds the potential risk to the fetus.If it is necessary to stop taking the drug during pregnancy, the drug should be withdrawn gradually.

Lactation

In animal studies risperidone and 9-hydroxyrisperidone penetrated into breast milk. People also found the penetration of risperidone and 9-hydroxyrisperidone into breast milk. Data on side effects in infants who are breastfed are absent. Therefore, the question of breastfeeding should be addressed in the light of the possible risk to the child.

Dosing and Administration:

Schizophrenia

Adults

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

Doses above 10 mg per day did not show higher efficacy, but compared with smaller doses, and may cause extrapyramidal symptoms.Due to the fact that safety of doses above 16 mg per day has not been studied, doses above this level should not be used.

Children from 13 to 17 years old

The minimum effective dose is 1-2 mg. If it is necessary to use smaller doses, as well as with a gradual increase in the dose risperidone should be used in the appropriate dosage form and dosage.

With good portability the recommended dose is 3 mg per day. Despite the effectiveness in treating schizophrenia in adolescents at doses of 1-6 mg per day, no additional efficacy was observed at doses above 3 mg per day, higher doses caused more side effects.

The use of doses above 6 mg per day has not been studied.

Patients who have sustained drowsiness, it is recommended to take half the daily dose 2 times a day.

Mania in bipolar disorders

Adults

An initial dose of 2 mg per day is recommended at a time. If necessary, this dose can be increased by 1 mg per day, not more than a day. For most patients, the optimal dose is 1-6 mg per day. The use of doses above 6 mg per day in patients with manic episodes has not been studied. As for any other symptomatic therapy, the desirability of continuing treatment with risperidone should be regularly evaluated and confirmed.

Diseases of the liver and kidneys

In patients with kidney disease, the ability to excrete the active antipsychotic fraction is reduced, compared with other patients. In patients with liver disease, there is an increase in the concentration of free fraction of risperidone in blood plasma.

Recommended initial and the maintenance dose in accordance with the indications should be reduced by a factor of 2, increasing the dose in patients with liver and / or kidney disease should be slower. Risperidone should be administered with caution in this category of patients.

Mode of application

Inside. Eating does not affect the absorption of the drug.

If it is necessary to use doses less than 1 mg, it is recommended to apply the drug in the appropriate dosage form and dose.

Termination of the drug is recommended to be carried out gradually.

After a sharp cessation of high doses of antipsychotics, acute symptoms of "withdrawal" were very rarely observed, including nausea, vomiting, increased sweating and insomnia.

Transition from therapy with other antipsychotic drugs

At the beginning of risperidone treatment, it is recommended to gradually abolish previous therapy, if it is clinically justified. In this case, if patients are transferred from the treatment of depot forms of antipsychotics, then risperidone therapy should be started instead of the next planned dose. Periodically, the need to continue the current therapy antiparkinsonian drugs.

Side effects:

The most frequently observed side effects were Parkinsonism, headache and insomnia.

The following side effects are classified according to organ systems and frequency of occurrence: very often (≥1 / 10), often ((≥1 / 100 and <1/10), infrequently (≥1 / 1000 and <1/100), rarely (≥1 / 10000 and <1/1000), very rarely (<1/10000) and unknown (can not be estimated from the available data).

In each private group, side effects are presented in order of decreasing importance.

Violations laboratory and instrumental indicators:

often - an increase in the level of prolactin¹, weight gain;

infrequently - lengthening of the interval QT on an electrocardiogram (ECG),abnormal ECG, an increase in the level of transaminases, a decrease in the number of leukocytes in the blood, an increase in body temperature, an increase in the number of eosinophils in the blood, a decrease in the level of hemoglobin, an increase in the level of creatine phosphokinase;

rarely - lowering of body temperature.

From the cardiovascular system:

often - tachycardia;

infrequently - atrioventricular block, bundle bundle block, fibrillation atrial, sinus bradycardia, palpitation.

Hematologic disorders and disorders of the lymphatic system:

infrequently - anemia, thrombocytopenia;

rarely - granulocytopenia;

unknown - agranulocytosis.

From the nervous system:

Often - parkinsonism², head pain;

often - akathisia², dizziness², tremor², dystonia², drowsiness, sedation, lethargy, dyskinesia²;

infrequently - absence of reaction to stimuli, loss of consciousness, syncope, depressed state, stroke, transient ischemic attack, dysarthria, attention violation, hypersomnia, postural dizziness, imbalance, tardive dyskinesia, speech impairment, coordination disorder, kinesthesia;

rarely - malignant neuroleptic syndrome (ZNC), diabetic coma, cerebrovascular disorders, cerebral ischemia, impaired movement.

Ophthalmic disorders:

often - fuzzy vision;

infrequently - conjunctivitis, ocular hyperemia, visual impairment, discharge from the eyes, edema around the eyes, dry eyes, increased lacrimation, photophobia;

rarely - reduced visual acuity, involuntary eyeball rotation, glaucoma, moving iris syndrome (for cataract surgery).

From the ear and the labyrinth:

infrequently - pain in the ear, tinnitus.

Respiratory, thoracic disorders and disorders of the mediastinum:

often - shortness of breath, nosebleeds, cough, nasal congestion, pain in the area larynx and pharynx;

infrequently - wheezing, aspiration pneumonia, congestion in the lungs, respiratory failure, wet wheezing, blockage of the respiratory tract, dysphonia;

rarely - sleep apnea syndrome, hyperventilation.

From the gastrointestinal tract:

often - vomiting, diarrhea, constipation, nausea, pain in the abdomen, dry mouth, discomfort in the stomach;

infrequently - dysphagia, gastritis, incontinence kala, hypersalivation, fecaloma;

rarely - intestinal obstruction, pancreatitis, edema of the lips, cheilitis.

From the side of the kidneys and urinary tract:

often - enuresis;

infrequently - delay of urination, dysuria, urinary incontinence, pollakiuria.

From the skin and subcutaneous tissues:

often rash, erythema;

infrequently - Quincke's edema, skin lesions, violation of the skin, itching, acne, skin color disorder, alopecia, seborrheic dermatitis, dry skin, hyperkeratosis;

rarely - dandruff.

From the side of the musculoskeletal system and connective tissue:

often - arthralgia, back pain, pain in the limbs;

infrequently - muscle weakness, myalgia, neck pain, swelling of the joints, pose disorders, joint stiffness, muscle pain in the chest;

rarely - rhabdomyolysis.

From the endocrine system:

rarely - disturbance of the production of antidiuretic hormone.

Disorders of metabolism and nutrition:

often - increased appetite, decreased appetite;

infrequently - diabetes³, anorexia, bylipopsy, hyperglycemia:

rarely - hypoglycemia;

rarely - diabetic ketoacidosis;

unknown - water intoxication.

Infections:

often - pneumonia, influenza, bronchitis, upper respiratory tract infections, urinary tract infections;

infrequently - sinusitis, viral infections, ear infection, tonsillitis, inflammation of subcutaneous fat, average otitis media, eye infections, localized infections, acarobacteria, respiratory tract infections, cystitis, onychomycosis;

rarely - chronic otitis media.

Vesselssimple violations:

Infrequently - hypotension, orthostatic hypotension, hot flashes.

Are common violations and phenomena caused by the administration of the drug:

often - Pyrexia, fatigue, peripheral edema, asthenia, pain in the chest;

infrequently - edema of the face, gait disturbance, poor health, sluggishness, flu-like condition, thirst, discomfort in the chest, chills;

rarely - general edema, hypothermia, withdrawal syndrome, cold extremities.

From the immune system:

infrequently hypersensitivity;

rarely - medicinal hypersensitivity;

unknown anaphylactic reaction.

Hepatobiliary disorders:

rarely - jaundice.

From the side of the reproductive system and mammary glands:

infrequently - amenorrhea, sexual dysfunction, erectile dysfunction, ejaculation disorder, galactorrhea, gynecomastia, menstruation, vaginal discharge;

unknown - Priapism.

Mental disorders:

Often - Insomnia;

often - anxiety, excitement, sleep disorders;

infrequently - confusion, mania, decreased libido, lethargy, nervousness;

rarely anorgasmia, flattening of affect.

¹ - giperprolaktinemiya in some cases can lead to gynecomastia, menstrual disorders, amenorrhea and galactorrhea.

²- Extrapyramidal disorders may manifest as: Parkinsonism (hypersalivation, musculoskeletal stiffness, drooling, rigidity of the "cogwheel" type, bradykinesia, hypokinesia, masculine face, muscle tension, akinesia, muscle stiffness, rigidity of the occipital muscles, parkinsonic gait, breach of the glabellar reflex), akathisia (akathisia, anxiety, hyperkinesia and restless leg syndrome), tremor, dyskinesia (dyskinesia, muscle twitching, choreoathetosis, athetosis and myoclonus), dystonia.

Dystonia includes dystonia, muscle spasms, hypertension, torticollis, involuntary muscle contractions, muscle contracture, blepharospasm, eyeball movements, paralysis of the tongue, facial spasm, laryngospasm, myotonia, opisthotonus, oropharyngeal spasm, pleurovastonus, spasm of the tongue and trismus.Tremor includes tremor and Parkinson's tremor tremor. There is a wider range of symptoms that do not always have extrapyramidal origin.

³ - diabetes mellitus was observed in 0.18% of patients taking risperidone compared with 0.11% of patients in the placebo group. The overall incidence of diabetes by the results of all clinical trials was 0.43% of all patients taking risperidone.

Class Effects

As with other antipsychotics, in Very few cases were observed after the postmarketing period increasing the tooth QT. Other class effects from the cardiovascular system, observed with the use of antipsychotics, which increase the prong QT, include: ventricular arrhythmia, ventricular fibrillation, ventricular tachycardia, sudden death, cardiac arrest and bidirectional ventricular tachycardia.

Venous thromboembolism

With the use of antipsychotics, there have been cases of venous thromboembolism, including pulmonary embolism and cases of deep vein thrombosis (the frequency is unknown).

Weight gain

In patients with schizophrenia, an increase in body weight of at least 7% at 6-8 weeks was observed in 18% of patients taking risperidone, and in 9% of patients taking placebo. In patients with manic episodes, the number of cases of weight gain of 7% or more after 3 weeks of treatment was comparable in the group taking risperidone (2.5%) and in the placebo group (2.4%).

In children with behavioral disorders during long-term clinical trials, the body weight increased by an average of 7.3 kg after 12 months of therapy. The expected increase in body weight in children 5-12 years old with normal development is 3-5 kg per year. From the age of 12-16, the increase in body weight should be 3-5 kg per year for girls and about 5 kg per year for boys.

Additional information about specific populations of patients

Side effects, which in elderly patients with dementia and in children were observed with a greater frequency than in adult patients, are described below:

Elderly patients with dementia

Transient ischemic attack and stroke were observed at a frequency of 1.4% and 1.5%, respectively. With a frequency ≥ 5% and with a frequency at least 2 times higher than in others patient populations: infections urinary tract, peripheral edema, lethargy and cough.

Children

In children (5-17 years) with a frequency ≥ 5% and with a frequency at least 2 times higher than in others Patient populations: drowsiness / sedation, fatigue, headache, increased appetite, vomiting, upper respiratory tract infections, nasal congestion, abdominal pain, dizziness, cough, pyrexia, tremor, diarrhea, enuresis.

Overdose:

Symptoms

In general, the observed symptoms of overdose represent the already known pharmacological effects of risperidone in a strengthened form: drowsiness, sedation, tachycardia, arterial hypotension, extrapyramidal symptoms.

The lengthening of the interval QT and convulsions. Bi-directional ventricular tachycardia was noted at simultaneous use of an increased dose of risperidone and paroxetine.

In case of acute overdose should to consider the possibility of an overdose of taking several drugs.

Treatment

It is necessary to achieve and maintain free airway to ensure adequate oxygen supply and ventilation. Gastric lavage (after intubation, if the patient is unconscious) and taking activated charcoal together with a laxative should be done only if the drug was taken no more than an hour ago.Immediately begin monitoring the ECG to identify possible arrhythmias. Specific antidote does not exist, appropriate symptomatic therapy should be conducted. Arterial hypotension and vascular collapse should be eliminated by intravenous fluid infusions and / or sympathomimetic drugs. When developing severe extrapyramidal symptoms, anticholinergic preparations. Continuous medical surveillance and monitoring should continue until the symptoms of intoxication disappear.

Interaction:

As in the case of other antipsychotic drugs, caution should be exercised with the simultaneous use of risperidone with drugs that increase the interval QT (for example, with antiarrhythmic drugs Ibut of class (quinidine, disopyramide, procainamide and others), class III (amiodarone, sotalol and others), tricyclic antidepressants (amitriptyline and others), tetracyclic antidepressants (maprotiline , etc.), some antihistamine drugs, other antipsychotic drugs, some antimalarial drugs (quinine, mefloquine and others), drugs that cause electrolyte imbalance (hypokalemia, hypomagnesemia), bradycardia, or inhibit the hepatic metabolism of risperidone. This list is not exhaustive.

The effect of risperidone on other drugs

Risperidone should be used with caution in combination with other drugs of central action, especially with alcohol, opiates, antihistamines and benzodiazepines because of the increased risk of sedation.

Risperidone may reduce effectiveness of levodopa and other agonists of dopamine. If necessary, this combination, especially at the terminal stage of the disease Parkinson's, should be prescribed the lowest effective dose of each drug.

With the simultaneous use of risperidone with antihypertensive drugs, clinically significant hypotension was observed.

Risperidone does not have a clinically significant effect on the pharmacokinetics of lithium, valproate, digoxin, or topiramate.

The effect of other drugs on risperidone

Carbamazepine causes a decrease in the concentration of active antipsychotic fraction of risperidone in plasma.

Similar effects can be observed with simultaneous use of other inducers hepatic enzymes and P-glycoprotein (for example, rifampicin, phenytoin, phenobarbital). With the appointment and after the withdrawal of carbamazepine or other inducers of hepatic enzymes and P-glycoprotein, the dose of risperidone should be adjusted.

Fluoxetine and paroxetine. which are inhibitors of the isoenzyme CYP2D6, increase the concentration of risperidone in plasma and to a lesser extent - the concentration of active antipsychotic fraction.

It is assumed that other inhibitors isoenzyme CYP2D6 (eg,quinidine) affect the concentration of risperidone in the same way. When the appointment and after the abolition of fluoxetine or paroxetine, the dosage of risperidone should be adjusted.

Verapamil, which is an inhibitor of isoenzyme CYP 3A4 and P-glycoprotein, increases the concentration of risperidone in plasma.

Galantamine and donepezil have no clinically significant effect on the pharmacokinetics of risperidone and its active antipsychotic fractions.

Phenothiazines, tricyclic antidepressants and some β-blockers may increase concentration of risperidone in plasma, however 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 a minimal effect on the concentration of active antipsychotic fraction.

Erythromycin, isoenzyme inhibitor CYP3A4, does not affect the pharmacokinetics of risperidone and active antipsychotic fraction.

Simultaneous application with paliperidone may increase the concentration of antipsychotic fraction.

Special instructions:

Application v elderly patients with dementia

Increased mortality in elderly patients with dementia

In elderly patients with dementia in the treatment of atypical antipsychotic agents, incl. risperidone, there is an increased mortality compared with placebo. The rate of deaths was 4.0% of patients taking risperidone, but compared with 3.1% for placebo. The average age of the deceased patients was 86 years (67-100 years). At present, the cause of the increase in this risk is unknown,in which an increase in mortality may be applicable to antipsychotics, rather than to the characteristics of this group of patients.

Co-administration with furosemide

In elderly patients with dementia, there was an increased mortality with simultaneous furosemide and risperidone taken orally (7.3%, mean age 89 years, range 75-97 years) compared with the group taking only risperidone (3.1%, average age 84 years, range 70-96 years) and a group that only took furosemide (4.1%, average age 80 years, range 67-90 years). Simultaneous use of risperidone with other diuretics (mainly with thiazide diuretics in small doses) was not accompanied by an increase in mortality. Regardless of treatment, dehydration is a common risk factor for mortality and should be carefully monitored in elderly people with dementia.

In elderly patients with dementia, there was an increase in the side effects from the cerebrovascular system (acute and transient cerebral circulatory disorders), including deaths in patients (mean age 85 years, range 73-97 years) with risperidone compared with placebo .

Cardiovascular effects

In patients with dementia who took certain atypical antipsychotics, an increased risk of cerebrovascular side effects was approximately 3-fold. Serious and frivolous cerebrovascular side effects occurred in 3.3% of patients taking risperidone, and y 1,2% patients taking placebo. The risk ratio was 2.96 at a confidence interval of 95%. Increased risk is not excluded for other antipsychotics, as well as for other patient populations. Risperidone should be used with caution in patients with a risk factor for stroke.

The risk of cerebrovascular side effects is much higher in patients with mixed or vascular dementia, compared with patients with Alzheimer's dementia. Therefore, patients with dementia of any type other than Alzheimer's should not take risperidone.

Physicians should evaluate the risk / benefit ratio of risperidone in elderly patients with dementia, taking into account the precursors of stroke risk in each patient individually. Patients and persons caring for them,should be warned that it is necessary to immediately report the signs and symptoms of cardiovascular events, such as sudden weakness or immobility / numbness in the face, legs, hands, as well as speech difficulties and vision problems. All possible treatment options should be considered, including discontinuation of risperidone.

Risperidone can only be used for short-term treatment of persistent aggression in patients with dementia due to moderate and severe Alzheimer's disease, in addition to non-pharmacological methods correction, in case of their ineffectiveness or limited effectiveness, and when the network is at risk of harming the patient to himself or others. Always necessary appraise The condition of patients and the need to continue therapy with risperidone.

Orthostatic hypotension

Risperidone has alpha-blocking activity, and therefore can cause orthostatic hypotension in some patients, especially during the initial dose selection. Clinically significant hypotension was observed with simultaneous use with antihypertensive drugs.

Risperidone should be used with caution in patients with known cardiovascular diseases (eg, heart failure, myocardial infarction, violation conduction of the heart muscle, dehydration, hypovolemia or cerebrovascular disease).

Corresponding dose adjustment is necessary. In the case of hypotension, it is necessary to evaluate the possibility of reducing the dose.

Late dyskinesia and extrapyramidal disorders

Drugs that have the properties of dopamine receptor antagonists can cause late dyskinesia, which is characterized by rhythmic involuntary movements, predominantly of the tongue and / or mimic muscles. The occurrence of extrapyramidal symptoms is a risk factor for the development of tardive dyskinesia. If patients have objective or subjective symptoms indicating tardive dyskinesia, one should consider the desirability of abolishing all antipsychotics, including risperidone.

Malignant antipsychotic syndrome (CNS)

Antipsychotic drugs, including risperidone. can cause CNS, which is characterized by hyperthermia, rigidity of muscles, instability of autonomic nervous system function, depression of consciousness, increased concentration of creatinine phosphokinase in serum. In patients with ZNS, myoglobinuria (rhabdomyolysis) and acute renal failure may also occur. If a patient experiences objective or subjective symptoms of ZPS, all antipsychotics should be immediately discontinued, including risperidone.

Parkinson's disease and dementia with Levi bodies

Purpose antipsychotic drugs, including risperidone. patients with Parkinson's disease or dementia with Levy bodies should be treated with caution, since both groups of patients have increased risk of developing CNS and increased sensitivity to antipsychotics (including blunting of pain sensitivity, confusion, postural instability with frequent falls and extrapyramidal symptoms) . When taking risperidone, there may be a worsening of the course of Parkinson's disease.

Hyperglycemia and diabetes mellitus

In the treatment with risperidone, hyperglycemia, diabetes mellitus and exacerbation of already existing diabetes were observed.It is likely that the previous increase in body weight is also predisposing to this factor. It is very rare to observe ketoacidosis and rarely - diabetic coma. All patients need to be clinically monitored for symptoms of hyperglycemia (polydipsia, polyuria, polyphagia and weakness). Patients with diabetes should be regularly monitored for glucose.

Weight gain

In the treatment with risperidone, a significant increase in body weight was observed. It is necessary to monitor the body weight of patients.

Hyperprolactinemia

Caution should be exercised when prescribing risperidone to patients with hyperprolactinemia and patients with possible prolactin-dependent tumors.

Interval lengthening QT

As with other antipsychotics, caution should be exercised in prescribing risperidone to patients with known cardiovascular diseases, lengthening of the interval QT in a family history, bradycardia, electrolyte balance disorders (hypokalemia, hypomagnesemia), since this may increase the risk of arrhythmogenic effect; and with the simultaneous use of drugs that extend the interval QT.

Convulsions

Risperidone should be used with caution in patients with a history of seizures or other medical conditions in which the convulsive threshold may be reduced.

Priapism

In connection with the alpha-adrenergic blocking action of risperidone, priapism may occur when it is used.

Regulation of body temperature

Antipsychotic drugs can cause a violation of the body's ability to regulate the temperature. Caution should be exercised when using risperidone in patients with conditions that may to promote an increase in the internal temperature of the body, which includes intensive physical activity, dehydration of the body, exposure to high external temperatures or simultaneous use of drugs with anticholinergic activity.

Venous thromboembolism

Because patients who take antipsychotics often have a risk of developing venous thromboembolism, all possible risk factors should be identified both before and during risperidone treatment, and preventive measures should be taken.

Children and teens

Before prescribing risperidone to children or adolescents with mental retardation, it is necessary to carefully evaluate their condition for the presence of physical or social causes of aggressive behavior such as pain or inadequate requirements of the social environment.

The sedative effect of risperidone should be carefully monitored in this population because of the possible effect on learning ability. The change in the time of risperidone intake can improve the control of the effect of sedation on the attention of adolescents and children. The use of risperidone was associated with an average increase in body weight and body mass index. Changes in growth were within the expected age norms. The effect of long-term use of risperidone on sexual development and growth has not been fully studied.

Due to the possible impact of prolonged hyperprolactemia on growth and sexual development in children and adolescents, regular clinical evaluation hormonal status, including measurement of height, weight, observation of sexual development, menstrual cycle and other possible prolactin-dependent effects.

During treatment with risperidone, regular monitoring of the presence of extrapyramidal symptoms and other movement disorders should be performed.

Excipients

The preparation RISPAXOL® contains lactose. It should not be taken patients with intolerance to sugars, namely rare congenital intolerance to galactose, a deficiency of lactase, or a glucose / galactose malabsorption syndrome.

Effect on the ability to drive transp. cf. and fur:RISPAXOL® can affect active activities, which require rapid reaction. Therefore, do not drive or service machinery until an individual drug tolerance is identified.

Form release / dosage:

Tablets, film-coated, 2 mg and 4 mg.

Packaging:

For 10 tablets in a blister of polyvinylchloride film and aluminum foil.

For 2 or 6 blisters, 10 tablets together with the instructions for use are placed in a cardboard box.

Storage conditions:

Store in a dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

4 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-004316/08

Date of registration:03.06.2008 / 14.10.2014

Expiration Date:Unlimited

The owner of the registration certificate:GRINDEX, JSC GRINDEX, JSC Latvia

Manufacturer: & nbsp

Grindeks, JSC Latvia

Representation: & nbspGrindeks Rus, Open CompanyGrindeks Rus, Open CompanyRussia

Information update date: & nbsp22.12.2016

Illustrated instructions

Instructions

Rispaxol® (Rispaksole®)