Expiration date: 06/2025
Release form and composition:
Tablets, film-coated white color, round, lenticular, scored on one side on the break white.
1 tablet contains:
risperidone 1 mg
Excipients: lactose anhydrous, corn starch, magnesium stearate, silica colloidal anhydrous, cellulose microcrystalline.
Shell composition: dye Opadry II white 33G28707 (hypromellose (hydroxypropyl methylcellulose), lactose monohydrate, macrogol 3000, titanium dioxide, glyceryltrinitrate), Carnauba wax.
10 PCs. - blisters (2) - packs of cardboard.
10 PCs. - blisters (6) - packs cardboard.
Tablets, film-coated orange, round, lenticular, scored on one side on the break white.
1 tablet contains:
risperidone 2 mg
Excipients: lactose anhydrous, corn starch, magnesium stearate, silica colloidal anhydrous, cellulose microcrystalline.
Shell composition: dye Opadry orange OY-8729 (hypromellose (hydroxypropylmethylcellulose), macrogol 400, titanium dioxide, sunset yellow FCF (E110), quinoline yellow (E104)), macrogol 6000, Carnauba wax.
10 PCs. - blisters (2) - packs of cardboard.
10 PCs. - blisters (6) - packs cardboard.
Tablets, film-coated green, round, biconvex, with valium (in four parts) on one side on the break white.
1 tabletcontains:
risperidone 4 mg
Excipients: lactose anhydrous, corn starch, magnesium stearate, silica colloidal anhydrous, cellulose microcrystalline.
Shell composition: dye Opadry AMB green 80W21165 (iron oxide black (E172), Indigo Carmine (?132), soy lecithin, polyvinyl alcohol, quinoline yellow (E104), talc, titanium dioxide, xanthan gum), Carnauba wax.
10 PCs. - blisters (2) - packs of cardboard.
10 PCs. - blisters (6) - packs cardboard.
Pharmacological action:
Antipsychotic drug (neuroleptic) derivative benzisoxazole. Also has sedative, antiemetic and hypothermic effect.
Risperidone is a selective monoaminergic antagonist with a strong affinity for serotonin 5-HT2 and dopaminovykh D2-receptors. Also risperidone is associated with apha1-adrenergic receptors and, with a slightly lower affinity with the histamine H1-receptors and apha2-adrenergic receptors. Has no affinity for cholinergic receptors.
Antipsychotic effect due to blockade of dopamine D2-receptors and the mesolimbic mesocortical system.
Sedative effect due to blockade of adrenergic receptors reticular formation of the brain stem, antiemetic action - blockade of dopamine D2-receptor trigger zone of the vomiting center hypothermic action - blockade of dopamine receptors in the hypothalamus.
Reduces the productive symptoms (delusions, hallucinations, aggressiveness), automatism. Causes minimal suppression of motor activity and to a lesser extent induces catalepsy than classic antipsychotics (neuroleptics).
Balanced Central antagonism to serotonin and dopamine can reduce the risk of extrapyramidal symptoms.
Risperidone may cause a dose-dependent increase in the concentration of prolactin in plasma.
Pharmacokinetics:
The ingestion of risperidone completely absorbed (regardless of the meal) and the maximum concentration in plasma observed through 1-2 h.
Risperidone metabolized with the participation of P-450 IID6 of cytochrome C with formation of 9-hydroxyrisperidone, which has a similar pharmacological action. Risperidone and 9-hydroxyrisperidone are an effective antipsychotic fraction.
The ingestion of risperidone displayed with a halflife of about 3 hours. It is established that the half-life of 9-hydroxyrisperidone and the active antipsychotic fraction is 24 hours.
In most patients, the equilibrium concentration of risperidone observed one day after starting treatment. Equilibrium 9-gidroksirisperidona in most cases achieved through 3-4 days after start of treatment. The concentration of risperidone in plasma increases with dose (within the therapeutic doses).
Risperidone is rapidly distributed in the body. The volume of distribution is 1 to 2 l/kg In plasma, risperidone is bound to albumin and A1-glycoprotein. The binding of risperidone to plasma proteins is 88 %, 9-gidroksirisperidona-77 %.
Excreted by the kidneys - 70 % (of which 35 - 45% in the form of a pharmacologically active fraction) and 14 % - with bile. The rest are inactive metabolites.
The elderly patients after a single reception of the drug inside the observed increased concentrations of the active fraction in plasma to 30 %, and in patients with renal insufficiency - up to 60 % and reduced clearance of antipsychotic fraction.
The presence of liver failure does not affect the contents of the concentration of risperidone in plasma, but in these patients the average number of free fraction in plasma was 35% higher.
Indications:
- schizophrenia (acute and chronic) and other psychotic state with a predominance of positive symptoms (delusions, hallucinations, aggressiveness) and negative symptoms (poverty of speech, emotional and social detachment)
- affective disorders in various mental diseases
- behavioral disorders in patients with dementia when symptoms of aggression (angry outbursts, physical violence), disorders of activity (excitation, delirium) or psychotic symptoms
- as adjuvant therapy in the treatment of mania in bipolar disorders
- as adjunctive therapy of behavioral disorders in adolescents 15 years and adult patients with reduced intellectual level or mental retardation, in cases of, if destructive behavior (aggressiveness, impulsivity, autoaggression) is leading the clinical picture of the disease.
Dosing regimen:
Rispaxol can be taken during a meal or in between meals. The tablets should be taken with a little water.
When schizophrenia adults and children over 15 years the drug is prescribed 1 or 2 times/day. Initial dose of 2 mg/day. On the second day, the dose should be increased to 4 mg/day. From this point the dose can either maintain at the same level, either individually adjusted if necessary. Usually the optimal dose is 4-6 mg/day. In some cases, can be justified by a slower increase of the dose and lower initial and maintenance doses.
Doses above 10 mg/day did not show higher efficiency compared with lower doses and can cause extrapyramidal symptoms. Due to the fact that the safety of doses exceeding 16 mg/day have not been studied, doses above this level can not be applied.
Information on the use for the treatment of schizophrenia in children younger than 15 years do not exist.
Elderly patients recommended initial dose is on 500 mcg 2 times/day. The dose can be individually increased by 500 mg 2 times/day up to 1-2 mg 2 times/day.
In diseases of the liver and kidney recommended initial dose is on 500 mcg 2 times/day. This dose can be gradually increased to 1-2 mg per reception 2 times/day.
When prescription drug abuse or drug dependence recommended daily dose is 2-4 mg.
When behavioral disorders in patients with dementia the recommended initial dose is on 250 mcg 2 times/day (should use appropriate dosage form). Dosage if necessary, can be individually increased by 250 mcg 2 times/day, not more than a day. For most patients the optimal dose is 500 mcg 2 times/day. However, some patients are shown receiving 1 mg 2 times/day.
Upon reaching the optimal dose can be recommended the drug 1 times/day.
With mania in bipolar disorder recommended initial dose - 2 mg per day. If necessary, the dose may be increased to 2 mg per day, not more than a day. For most patients the optimal dose is 2-6 mg/day.
When behavioral disorders in patients with mental retardation patients weighing 50 kg or more, appoint 500 mg 1 times/day. If necessary, this dose can be increased 500 mg/day, not more than a day. For most patients the optimal dose is the dose of 1 mg/day. However, some patients prefer to receive 500 mcg/day, whereas some require increasing doses up to 1.5 mg/day. Patients with body weight less than 50 kg administered 250 mg/day. If necessary, the dose may be increased to 250 mg/day, not more than a day. For most patients the optimal dose is the dose 500 mg/day. However, for some patients receiving preferable 250 mcg/day, whereas some require increasing doses up to 750 mg/day.
Long-term use of Risperidone in adolescents should be under constant supervision of a doctor. The use in children under 15 years of age is not recommended.
Side effects:
Like other medicines, rispaxol can have a side effect, which, however, appears not at all. Rispaxol has good tolerability. These possible side effects.
CNS: insomnia, agitation, anxiety, headache sometimes drowsiness, fatigue, dizziness, impaired concentration, impaired clarity of vision, rarely - extrapyramidal symptoms (tremor, rigidity, hypersalivation, bradykinesia, akathisia, acute dystonia). Patients with schizophrenia possible hypervolemia (either due to polydipsia, either due to syndrome of inappropriate secretion of antidiuretic hormone), tardive dyskinesia (involuntary rhythmic movements mainly language and/or individuals) CSN (hyperthermia, muscle rigidity, instability of autonomic functions, violation of consciousness and improving the level of CPK), disorders of thermoregulation and seizures.
From the digestive system: constipation, dyspepsia, nausea, vomiting, abdominal pain, increased liver enzymes, dry mouth, Hypo - or hypersalivation, anorexia, increased appetite, increase or decrease in body mass.
Of the cardiovascular system: orthostatic hypotension, reflex tachycardia, increased blood pressure. The therapy Rispaxol describes the development of stroke, mostly in elderly patients with predisposing factors.
With the hematopoietic system: neutropenia, thrombocytopenia.
From the endocrine system: possible galactorrhea, gynecomastia, menstrual disorders, amenorrhea in rare cases, hyperglycemia or deteriorating course of diabetes mellitus.
From the urogenital system: priapism, erectile dysfunction, violation of ejaculation, anorgasmia, urinary incontinence.
Dermatological reactions: dry skin, hyperpigmentation, itching, seborrhea, photosensitivity.
Allergic reactions: rhinitis, rash, angioedema.
Other: arthralgia.
Contraindications:
- lactation (breast-feeding)
- hypersensitivity to the drug.
With caution should designate product if:
- diseases of the cardiovascular system (chronic heart failure, myocardial infarction, violations conductivity cardiac muscles)
- dehydration and hypovolemia
- violations of cerebral circulation
- Parkinson's disease
- convulsions (including history)
- renal failure, severe
- severe hepatic insufficiency
- prescription drug abuse or drug dependence
- conditions predisposing to the development of tachycardia type pirouette (aetiology, violation of elektrolitnogo balance, concomitant intake of medicines, extension QT interval)
- brain tumors, intestinal obstruction, acute cases of drug overdose, Reye's syndrome (an antiemetic effect of risperidone may mask the symptoms of these conditions)
- pregnancy (efficacy and safety not established)
- children up to 15 years (efficacy and safety not established).
Pregnancy and lactation:
Safety of application of risperidone in pregnant women has not been studied. During pregnancy, the drug can be used only if a positive effect justifies the potential risk. Since risperidone and 9-hydroxyrisperidone are excreted in breast milk, women who use the drug should not breast-feed.
Special instructions:
In schizophrenia, early treatment with risperidone, it is recommended to gradually undo the previous therapy, if clinically justified. If patients are transferred from therapy depot forms of antipsychotic drugs, the appointment of risperidone is recommended to start instead of the next scheduled injection. Periodically assess the need for continued therapy antiparkinsonian drugs.
In connection with the alpha-adrenoblokiruyuschee effect of risperidone may develop orthostatic hypotension, especially during initial dose selection. In the event of hypotension should consider lowering the dose.
In patients with diseases of the cardiovascular system, as well as in dewatering, hypovolemia or cerebrovascular disorders, the dose should be increased gradually, according to the 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 should consider abolishing all antipsychotics.
With the emergence of the neuroleptic malignant syndrome characterized by hyperthermia, muscle rigidity, instability of autonomic functions, disorders of consciousness and increased levels of CPK must cancel all antipsychotic medicines, including risperidone.
The abolition of carbamazepine and other inductors of liver enzymes dose of risperidone should be reduced.
Patients should be advised to refrain from overeating in connection with the possibility of increasing body mass.
Rispaxol tablets contain lactose. This drug should not be taken by patients with intolerance to sugars (congenital galactose intolerance, lactase deficiency or malabsorption syndrome glucose/galactose).
Effects on ability to drive vehicles and management mechanisms
Rispaxol can affect active, which requires quick reactions. Therefore, you should not drive a car or service mechanisms not yet identified the individual tolerance of the drug.
Overdose:
Symptoms: drowsiness, sedative effect, depression of consciousness, tachycardia, hypotension, extrapyramidal disorder, in rare cases, a prolonged QT interval.
Treatment: must provide free airway to ensure adequate oxygenation and ventilation, gastric lavage (after intubation, if patient is unconscious) and the appointment of activated charcoal in combination with laxatives. Symptomatic therapy aimed at maintaining vital body functions. For timely diagnosis of possible heart rhythm disturbances you must immediately begin ECG monitoring. Thorough medical supervision and ECG monitoring is carried out until complete disappearance of symptoms of intoxication. There is no specific antidote.
Drug interactions:
Given the fact that Rispaxol has an effect primarily on the Central nervous system, it should be used with caution in combination with other centrally acting drugs and ethanol.
Rispaxol reduces the effectiveness of levodopa and other dopamine agonists.
Clozapine reduces the clearance of risperidone.
While the use of rispaxol and carbamazepine, a decrease of the concentration of the active antipsychotic fraction of risperidone in plasma. Similar effects may occur when using other inductors of liver enzymes.
While the use of rispaxol phenothiazines, tricyclic antidepressants and some beta-blockers may increase the concentration of risperidone in plasma, however this does not affect the concentration of active antipsychotic fraction.
While the use of rispaxol fluoxetine may increase the concentration of risperidone in plasma, however, to a lesser extent the concentration of active antipsychotic fraction.
When applying rispaxol together with other drugs, in a high degree of binding to plasma proteins, clinically significant displacement of any product from the protein fractions of plasma is not observed.
Antihypertensive drugs increase the severity of blood pressure reduction in patients receiving rispaxol.
Terms and conditions of storage:
The drug should be stored in a dark, inaccessible to children place at temperature not exceeding 25°C. shelf Life - 2 years.
