Risperidone Organica - instructions for use, dose, side effects, contraindications

Composition:in 1 tablet of the drug contains: active substance risperidone - 2 mg;
auxiliary substances: starch corn pregelatinized starch (starch 1500) - 43.3 mg, silicon dioxide colloid (aerosil) 0.5 mg, magnesium stearate monohydrate 0.3 mg, stearic acid 0.6 mg, microcrystalline cellulose 43, 3 mg, opadrai II white (polyvinyl alcohol - 2 mg, talc - 0.74 mg, macrogol (polyethylene glycol) - 1.01 mg, titanium dioxide-1.25 mg) -5 mg.
For a dosage of 4 mg:
1 tablet contains: active substance risperidone 4 mg; auxiliary substances: starch corn pregelatinized starch (starch 1500) - 86.6 mg, silicon dioxide colloid (aerosil) - 1 mg, magnesium stearate monohydrate - 0.6 mg, stearic acid - 1.2 mg, microcrystalline cellulose - 86.6 mg , opadrai II white (polyvinyl alcohol - 4 mg, talc - 1.48 mg, macrogol (polyethylene glycol) - 2.02 mg, titanium dioxide - 2.5 mg) - 10 mg.

Description:The tablets covered with a film cover, white or almost white color, round, biconcave form. On the cross-section, two layers are visible, the inner layer is white or white with a weak, creamy shade of color.

Pharmacotherapeutic group:antipsychotic agent (antipsychotic).

ATX: & nbsp

N.05.A.X Other antipsychotics

N.05.A.X.08 Risperidone

Pharmacodynamics:Risperidone is an antipsychotic agent, it also has a sedative, antiemetic and hypothermic effect. Risperidone Organica is selective antagonist of 5-HT₂-serotonin and D₂dopamine receptors, is also associated with alpha₁-adrenoceptors and with slightly less affinity with H₁-gistamine and 2-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 the productive symptoms of schizophrenia (delirium, hallucinations), aggressiveness, automatism. Causes less inhibition of motor activity and less degree induces catalepsy, than classical antipsychotic drugs (antipsychotics). Balanced central antagonism to serotonin and dopamine can reduce the risk of extrapyramidal symptoms and extend the therapeutic effect of the drug to include negative and affective symptoms of schizophrenia. Risperidone Organic can cause a dose-dependent increase in plasma prolactin concentration.

Pharmacokinetics:When taken orally, Risperidone Organica is completely absorbed (regardless of food intake) and the maximum concentration in the blood plasma is reached after 1-2 hours.
Risperidone Organica is metabolized by the isoenzyme CYP2D6 to form 9-hydroxyrisperidone, which has a similar pharmacological effect. Risperidone Organica and 9-hydroxyrisperidone are an effective antipsychotic fraction. The further metabolism of risperidone is in N-dealkylation. When taken orally, Risperidone Organica is withdrawn with a half-life of about 3 hours. It was established that the half-life of 9-hydroxyrisperidone and the active antipsychotic fraction is 24 hours. In most patients, the equilibrium concentration of Risperidone Organic is observed one day after the start of treatment. The equilibrium state of 9-hydroxyrisperidone in most cases is achieved 3-4 days after the start of treatment. The concentration of Risperidone Organic in plasma is proportional to the dose of the drug (within therapeutic doses). Risperidone Organa is rapidly distributed in the body. The volume of distribution is 1-2 l / kg. In plasma, Risperidone Organica is associated with albumin and acid alpha-1-glycoprotein. The Riceridone Organic fraction, which is bound by the plasma protein, is 88% and 77, respectively, in the case of 9-hydroxyrisperidone.It is excreted by the kidneys - 70% (of which 35-45% in the form of pharmacologically active fraction) and 14% with bile. The rest is made up of inactive metabolites.
Pharmacokinetics in special clinical cases
In elderly patients, as well as in patients with renal insufficiency, the concentration of the drug in the plasma increases, and the half-life (T1 / 2) increases.
Concentrations of Risperidone Organic in plasma in patients with hepatic insufficiency do not change.

Indications:Schizophrenia (acute and chronic) and other psychotic conditions with productive and / or negative symptoms. Abuse of medicines or drug dependence. As an auxiliary therapy: in the treatment of mania in bipolar disorders; behavioral disorders in adolescents with 15 years of age and adults with reduced intellectual level or mental retardation, in cases where destructive behavior (aggressiveness, impulsivity, autoaggression) is leading in the clinical picture of the disease.

Contraindications:Hypersensitivity to the components of the drug; children under the age of 15; lactation period.

Carefully:Diseases of the cardiovascular system (chronic heart failure, myocardial infarction, myocardial conduction abnormalities), dehydration and hypovolemia, cerebrovascular disease, Parkinson's disease, seizures (including history), severe renal or hepatic insufficiency (see. Dosing recommendations ), abuse of drugs or drug dependence (see. for dosage recommendations), conditions that predispose to the development of tachycardia type "pirouette" (bradycardia , Electrolyte imbalance, concomitant drugs interval prolonging Q-T), brain tumor, intestinal obstruction, acute drug overdose cases, Reye's syndrome (antiemetic effect of risperidone Organics may mask symptoms of these conditions).

Pregnancy and lactation:The safety of Risperidone Organic in pregnant women has not been studied. During pregnancy, the drug is used if the expected benefit to the mother exceeds the possible risk to the fetus.
Because Risperidone Organica and 9-hydroxyrisperidone penetrate into breast milk, women who use the drug,do not breast-feed.

Dosing and Administration:Inside.
Schizophrenia
Adults and children over 15 years. Risperidone Organica may be given once or twice a day. The initial dose is -2 mg per day. On the second day, the dose should 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 higher than 10 mg per day showed no higher efficacy compared with smaller doses and may cause extrapyramidal symptoms, because the safety of doses above 16 mg per day has not been studied, doses above this level can not be used. Information on use for the treatment of schizophrenia in children under the age of 15 is not available.
Drug Abuse or Drug Dependence
The recommended daily dose of the drug is 2-4 mg.
Mania in bipolar disorders
The recommended initial dose of the drug is 2 mg per day at a time. If necessary, this dose may be increased by 2 mg per day, not more often than every other day.For most patients, the optimal dose is 2-6 mg per day.
Long-term use of Risperidone Organic in adolescents should be carried out under the constant supervision of a physician.
Use in children under 15 years of age Not recommended.

Side effects:The incidence of adverse reactions was classified as follows: very often (> 10%), often (> 1% and <10%), infrequently (> 0.1% and <1%), rarely (> 0.01% and <0 , 1%), very rarely (<0.01%).
Infections: very often - in elderly patients with dementia - urinary tract infections; often - nasopharyngitis, upper respiratory tract infections, sinusitis, urinary tract infections, in elderly patients with dementia - pneumonia, phlegmon, rhinitis, influenza-like diseases; infrequently - ear infections, viral infections, pharyngitis, tonsillitis, bronchitis, eye infections, localized infections, cystitis, onychomycosis, acrodermatitis, bronchopneumonia, respiratory infections, tracheobronchitis.
From the nervous system: very often - headache, insomnia, parkinsonism, including extrapyramidal symptoms (tremor, rigidity, hypersalivation, bradykinesia, akathisia, acute dystonia); often - dizziness,drowsiness, blurred vision; infrequent - decreased ability to concentrate, increased fatigue; very rarely - mania or hypomania, agitation, anxiety, stroke (in elderly patients with predisposing factors). In patients with schizophrenia infrequent - hypervolemia (either because of polydipsia, or because of the syndrome of inadequate secretion of the antidiuretic hormone), tardive dyskinesia (involuntary rhythmic movements predominantly of the tongue and / or face); rarely - malignant neuroleptic syndrome (hyperthermia, muscle rigidity, instability of autonomic functions (profuse sweating, tachycardia and other heart rhythm disturbances, fluctuations in blood pressure, skin pallor, dyspnea, urination disorder), impaired consciousness and increased activity of creatine phosphokinase), neuroleptic malignant syndrome thermoregulation; there is no data on the incidence of epileptic seizures.
From the digestive system: often - nausea or vomiting, dyspepsia, dryness of the oral mucosa, constipation, abdominal pain; infrequently - increased activity of "hepatic" transaminases, hypo- or hypersalivation, anorexia and / or increased appetite, increase or decrease in body weight.
From the cardiovascular system: often - reflex tachycardia; infrequently, -orthostatic hypotension or increased blood pressure; very rarely - atrial fibrillation.
Respiratory, thoracic disorders and disorders of the mediastinum: often nasal congestion, shortness of breath, epistaxis, sinus congestion, elderly patients with dementia - cough, rhinorrhea; infrequently - wheezing, aspiration pneumonia, dysphonia, productive cough, blockage of the respiratory tract, wet wheezing, respiratory failure, edema of the nose, hyperventilation; very rarely - sleep apnea syndrome.
From the hematopoiesis: often anemia; infrequently - granulocytopenia; very rarely - thrombocytopenia, agranulocytosis.
From the immune system: infrequently - hypersensitivity; very rarely - anaphylactic shock.
Endocrine system: infrequently - galactorrhea, menstrual disorder, amenorrhea, weight gain; rarely - gynecomastia; very rarely - hyperglycemia and exacerbation of pre-existing diabetes, a violation of the secretion of antidiuretic hormone.
From the side of the kidneys and urinary tract: often - urinary incontinence; infrequently - pain when urinating; very rarely - urinary retention.
On the part of the reproductive system and mammary glands: often - absence of ejaculation; infrequent - menstruation, amenorrhea, gynecomastia, vaginal discharge, erectile dysfunction, ejaculatory disturbance, breast enlargement, sexual dysfunction, retrograde ejaculation; very rarely - priapism.
Allergic reactions: often - a rhinitis, an eruption; infrequently - angioedema, photosensitization.
From the skin: infrequently - dry skin, hyperpigmentation, itching, seborrhea.
From the osteomuscular system and connective tissue: often - back pain, arthralgia, pain in the extremities, in elderly patients with dementia - gait disturbances, swelling of the joints; infrequently - muscular pain in the chest, stiffness in the joints, muscle weakness, rhabdomyolysis.
Common violations: often - fatigue, asthenia, fever, pain in the chest, in elderly patients with dementia: peripheral edema, gait disturbance; infrequent - thirst, flu-like condition edema, poor health, swelling of the face, general edema, chills, cold extremities, withdrawal syndrome; very rarely - hypothermia.
Violations of laboratory and instrumental indicators: often an increase in the activity of creatine phosphokinase, an increase in heart rate, in elderly patients with dementia - an increase in body temperature; infrequently, an increase in alanine aminotransferase activity, an ECG disorder, an increase in the number of eosinophils in the blood, an increase in the activity of aspartate aminotransferase, an increase in the number of leukocytes in the blood, an increase in blood glucose levels, a decrease in hemoglobin concentration, a decrease in hematocrit, a decrease in body temperature, a decrease in blood pressure; very rarely - prolongation of the Q-T interval on an electrocardiogram.

Overdose:In case of an overdose, the possibility of an overdose from taking several drugs should be considered.
Symptoms: drowsiness, sedation, depression, tachycardia, lowering of blood pressure, extrapyramidal disorders, in rare cases, prolongation of the Q-T interval.
Treatment: it is necessary to ensure free airway patency for adequate oxygenation and ventilation, gastric lavage (after intubation, if the patient is unconscious) and the appointment of activated carbon in combination with laxatives.Symptomatic therapy aimed at maintaining vital body functions. To timely diagnose possible violations of the rhythm of the heart, it is necessary to start monitoring the electrocardiogram as soon as possible. Careful medical observation and monitoring of the electrocardiogram is carried out until the symptoms of intoxication disappear completely. There is no specific antidote. Reduction of blood pressure and collapse should be eliminated by intravenous fluid infusions and / or sympathomimetic drugs. In case of development of acute extrapyramidal symptoms, m-holinoblokatory (trihexyphenidyl).

Interaction:Given that Risperidone Organica has an effect primarily on the central nervous system, it should be used with caution in combination with other central-action drugs and with alcohol. Risperidone Organica reduces the effectiveness of levodopa and other dopamine receptor agonists. Clozapine reduces the clearance of Risperidon Organica.
When carbamazepine was used, the active antipsychotic fraction of Risperidone Organic in the plasma decreased.Similar effects can be observed with the use of other inducers of microsomal liver enzymes.
Phenothiazine derivatives, tricyclic antidepressants and some beta-blockers can increase the concentrations of Risperidone Organica in plasma, but this does not affect the concentration of the active antipsychotic fraction. Fluoxetine can increase the concentration of Risperidone Organica in plasma, but to a lesser extent - the concentration of the active antipsychotic fraction, so the dose of Risperidone Organic should be adjusted.
When using Risperidone Organic, together with other drugs, highly binding to plasma proteins, clinically expressed displacement of a drug, no protein fraction of the plasma is observed.
Hypotensive drugs increase the severity of lowering blood pressure on the background of Risperidone Organic.

Special instructions:Precautions for use
Transition from therapy with other antipsychotic drugs. When schizophrenia, at the beginning of treatment with Risperidon Organic, it is recommended to gradually cancel the previous therapy, if it is clinically justified.If patients are transferred from the therapy of depot forms of antipsychotics, then it is recommended to start taking Risperidone Organic instead of the next scheduled injection. Periodically, the need to continue therapy with antiparkinsonian drugs should be evaluated.
In connection with the alpha-adrenergic blocking action of Risperidone Organic, orthostatic hypotension may occur, especially during the initial dose selection period. With a decrease in blood pressure should consider reducing the dose. In patients with diseases of the cardiovascular system, as well as during dehydration, hypovolemia or cerebrovascular disorders, the dose should be increased gradually, according to recommendations. The occurrence of extrapyramidal symptoms is a risk factor for the development of tardive dyskinesia. In case of signs and symptoms of tardive dyskinesia, consideration should be given to the abolition of all antipsychotics.
The administration of antipsychotics, including Risperidone Organica, to patients with Parkinson's disease or dementia with Levy bodies should be carried out with caution, sinceIn both groups of patients, sensitivity to antipsychotics has been increased (including blunting of pain sensitivity, confusion, postural instability with frequent falls and extrapyramidal symptoms), and the risk of developing a neuroleptic malignant syndrome characterized by hyperthermia, muscle rigidity, instability of autonomic functions, impaired consciousness and increased activity of creatine phosphokinase (also may be observed myoglobinuria (rhabdomyolysis) and acute kidney Single failure) to cancel all antipsychotic drugs, including risperidone Organics. With the withdrawal of carbamazepine and other inducers of "hepatic" enzymes, the dose of Risperidone Organica should be reduced.
In elderly patients with dementia in the treatment of atypical antipsychotic agents, including Risperidone, there is an increased mortality in comparison with placebo. When Risperidone was used for this population, the incidence of fatalities was 4.0% for patients taking Risperidone, compared with 3.1% for placebo.The average age of the deceased patients is 86 years (range 67-100 years).
In elderly patients with dementia taking oral forms Risperidone, there was an increased mortality in patients taking furosemide and Risperidone (7.3%, mean age 89 years, range 75-97 years) compared with the group taking only risperidone (4.1%, average age 84 years, range 75-96 years) and a group that only took furosemide (3.1%, the average age is 80 years, the range is 67-90 years). There are no pathophysiological mechanisms that explain this observation. Nevertheless, special care should be taken when prescribing the drug in such cases. There was no increase in mortality in patients taking other diuretics simultaneously with risperidone. Regardless of treatment, dehydration is a common risk factor for mortality and should be carefully monitored in elderly patients with dementia.
When treating the drug Risperidone hyperglycemia, diabetes mellitus, or exacerbation of already existing diabetes mellitus. Establishing the relationship between the use of atypical antipsychotics and impaired glucose metabolismis complicated by an increased risk of developing diabetes in patients with schizophrenia and the prevalence of diabetes mellitus in the general population. Given these factors, the relationship between the use of atypical antipsychotics and the development of side effects associated with hyperglycemia is not fully established. In all patients, it is necessary to conduct clinical monitoring for the presence of symptoms of hyperglycemia and diabetes mellitus.
In the treatment with risperidone, there was a significant increase in body weight. It is necessary to monitor the body weight of patients with drug therapy Risperidone. Caution should be exercised when prescribing Risperidone Organica to patients with a history of cardiac arrhythmias, patients with congenital Q-T interval prolongation and when combined with drugs that increase the Q-T interval.
The ability of typical neuroleptics to reduce the threshold of convulsive readiness is known. Caution should be used to administer Risperidone Organica to patients with epilepsy. Therapy with a potent D2 receptor antagonist by Organic riceperidone can lead to the development of tumors of the pituitary gland, hyperprolactinemia and galactorrhea.
The use of antipsychotics can cause dysphagia and a violation of esophageal motility.
Risperidone Organica and other antipsychotics should be used with caution in patients with Alzheimer's dementia who have an increased risk of aspiration pneumonia.
Patients should be advised to refrain from overeating due to the possibility of weight gain.
During treatment it is necessary to refrain from drinking alcohol.
It is recommended that the drug be gradually phased out, because after a sharp cessation of treatment with high doses of neuroleptics, the development of withdrawal syndrome (vomiting, nausea, increased sweating, insomnia) is possible.

Effect on the ability to drive transp. cf. and fur:During treatment, it is necessary to refrain from practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:Tablets of 2 mg or 4 mg.

Packaging:For 2, 3, 5 or 6 contour packs of 10 tablets together with instructions for medical use in a cardboard bundle.
For 20, 30, 50 or 60 tablets in a bank of light-protective glass, along with instructions for medical use in a cardboard pack.

Storage conditions:In the dark place at a temperature of no higher than 25 ° C.
Keep out of the reach of children.

Shelf life:2 years. Do not use at the end of the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:PL-000857

Date of registration:14.10.2011

The owner of the registration certificate:ORGANICS, JSC ORGANICS, JSC Russia

Manufacturer: & nbsp

ORGANICS, JSC Russia

Information update date: & nbsp24.10.2015

Illustrated instructions

Instructions

Risperidone Organica (Risperidone Organika)