RILEPTID
Active material: Risperidone
When ATH: N05AX08
CCF: Antipsychotic drug (anxiolytic)
ICD-10 codes (testimony): F20, F21, F22, F23, F25, F29, F30, F31, F79
When CSF: 02.01.02.03
Manufacturer: EGIS PHARMACEUTICALS Plc (Hungary)
Pharmaceutical form, composition and packaging
Pills, coated light green, oblong, lenticular, Engraved “E752” on one side and with Valium – another, with little or no odor.
| 1 tab. | |
| risperidone | 2 mg |
Excipients: lactose monohydrate, corn starch, microcrystalline cellulose, magnesium stearate, Colloidal anhydrous silica, sodium lauryl.
The composition of the shell: Opadry green dye (gipromelloza, Titanium dioxide, macrogol 400, ariavit indigo carmine aluminum lake, ariavit quinoline yellow aluminum lake).
10 PC. – blisters (2) – packs cardboard.
Pills, coated green color, oblong, lenticular, Engraved “E754” on one side and with Valium – another, with little or no odor.
| 1 tab. | |
| risperidone | 4 mg |
Excipients: lactose monohydrate, corn starch, microcrystalline cellulose, magnesium stearate, Colloidal anhydrous silica, sodium lauryl.
The composition of the shell: Opadry green dye (gipromelloza, Titanium dioxide, macrogol 400, ariavit indigo carmine aluminum lake, ariavit quinoline yellow aluminum lake).
10 PC. – blisters (2) – packs cardboard.
Pharmacological action
Antipsychotic drug, benzisoxazole derivative. It has also a sedative, antiemetic and hypothermic effect.
Risperidone – selective monoaminergic antagonist, It has high affinity for serotonin 5-HT2-receptors and dopamine D2-Receptor. Cвязывается с a1-adrenergic receptors and slightly weaker – with histamine H1-рецепторами и a2-adrenoreceptor. It does not have affinity for holinoretseptorami.
Antipsychotic effect due to blockade of dopamine D2-receptors and the mesolimbic system Mesocortical. Sedative effect due to blockade of adrenergic receptors of the 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 of the hypothalamus.
Rileptid® reducing productive symptoms of schizophrenia (delirium, hallucinations), automatism, at least causes the suppression of motor activity and to a lesser extent induces catalepsy, than classical neuroleptics. Balanced central serotonin antagonism and dopamine can reduce susceptibility to extrapyramidal side effects.
Risperidone may cause a dose-dependent increase in the concentration of prolactin in plasma.
Pharmacokinetics
Absorption
After oral risperidone completely absorbed from the gastrointestinal tract, regardless of the meal. Cmax plasma achieved through 1-2 no.
Distribution
Risperidone is rapidly distributed in the body. Vd is 1-2 l / kg. Risperidone 88% c bound to plasma proteins, 9-hydroxy-risperidone – on 77% (mainly to albumin and alpha acid1-glycoprotein).
Css Risperidone in the body is achieved in most patients for 1 day.
Css 9-hydroxy-risperidone is reached within 3-4 days. Risperidone plasma concentrations are proportional to the dose of the drug (within the therapeutic dose).
Metabolism
Risperidone is metabolized in the liver with the participation of CYP2D6 isoenzyme to form a 9-hydroxy-risperidone, which has a similar pharmacological action of risperidone. Risperidone and 9-hydroxy-risperidone constitute active antipsychotic fraction. Another way of metabolism of risperidone is N-dealkylation.
Deduction
Once inside the T1/2 Risperidone plasma is 3 no. T1/2 9-hydroxy-risperidone and the active antipsychotic fraction up 24 no.
70% dose (of them 35-45% in the form of 9-hydroxy-risperidone) excreted in the urine, 14% – with feces.
Pharmacokinetics in special clinical situations
Elderly patients and patients with renal failure after a single oral dose showed higher plasma concentrations, and slow elimination of risperidone.
Testimony
- Acute and chronic schizophrenia and other psychotic disorders with productive and / or negative symptoms;
- Affective disorders in a variety of mental disorders;
- Behavioral disorders in patients with dementia when symptoms persist aggression (outburst, physical abuse), mental activity (excitation, delirium) or psychotic symptoms;
- As an adjunct therapy means the treatment of mania in bipolar disorder;
- As a means of adjuvant therapy of behavioral disorders in adolescents with 15 years and adult patients with reduced intellectual level or mental retardation in cases, if the destructive behavior (aggressiveness, impulsiveness, autoagressiâ) It is leading the clinical picture of the disease.
Dosage regimen
At Schizophrenia adults and children over 15 years Rileptid® appointed 1 or 2 times / day. The initial dose - 2 mg / day. On the second day, the dose should be increased to 4 mg / day. From this point the dose can either maintain the same level of, either individually adjusted, if necessary,. Typically, the optimal dose is 4-6 mg / day. In some cases it can be justified by a slow increase in the dose and lower initial and maintenance doses.
Doses above 10 mg / day showed a higher efficiency compared with lower doses and may cause extrapyramidal symptoms. Because, that the safety of doses above 16 mg / day has not been studied, doses above this level can not be used.
For information on the use of Rileptida® for the treatment of schizophrenia children under 15 years no.
Elderly patients the drug is prescribed in an initial dose of 500 g 2 times / day. The dose can be individually increased by 500 g 2 times / day to 1-2 mg 2 times / day.
At human liver and kidneys the initial dose is at 500 g 2 times / day. This dose can be gradually increased to 1-2 mg 2 times / day.
At drug abuse or drug addiction The recommended daily dose is 2-4 mg.
When treating behavioral disturbances in patients with dementia The recommended starting dose is on 250 g 2 times / day. Dose if necessary individually to increase 250 g 2 times / day no more, than a day. For most patients, the optimal dose is 500 g 2 times / day. However, some patients show reception 1 mg 2 times / day.
Upon reaching the optimal dose can be recommended taking the drug 1 time / day.
At bipolar disorder when mania The recommended starting dose is 2 mg / day 1 reception. If necessary, this dose may be increased by 2 mg / day, no more, than a day. For most patients, the optimal dose is 2-6 mg / day.
At behavioral disorders in patients with mental retardation to patients body weight 50 kg or more The recommended starting dose is 500 g 1 time / day. If necessary, this dose may be increased by 500 mg / day no more, than a day. For most patients, the optimal dose is 1 mg / day. For some patients, preferable reception 500 mg / day, While some want to increase the dose to 1.5 mg / day.
To patients weighing less than 50 kg The recommended starting dose is 250 g 1 time / day. If necessary, this dose may be increased by 250 mg / day no more, than a day. For most patients the optimal dose is 500 mg / day. For some patients, preferable reception 250 mg / day, While some want to increase the dose to 750 mg / day.
Long-term use of the drug in Adolescents It should be carried out under the supervision of a physician.
Side effect
CNS: insomnia, ažitaciâ, alarm, headache; sometimes – drowsiness, fatiguability, dizziness, impaired concentration, blurred vision; rarely – extrapyramidal symptoms (tremor, rigidity, hyperptyalism, bradikineziâ, akathisia, acute dystonia). Mania or hypomania possible, stroke (in elderly patients with predisposing factors), gipervolemia (either due to polydipsia, either because the syndrome of inappropriate secretion of ADH), pozdnyaya dyskinesia (involuntary rhythmic movements mainly language and / or the person), neuroleptic malignant syndrome (hyperthermia, muscle rigidity, instability of autonomous functions, impairment of consciousness and increased CPK), violation of thermoregulation and seizures.
From the digestive system: constipation, dispepciya, nausea, vomiting, stomach ache, increase in liver enzymes, dry mouth, Hypo- or hypersalivation, anorexia, increased appetite, increase or reduction of body weight.
Cardio-vascular system: orthostatic hypotension and reflex tachycardia, increased blood pressure.
From the hematopoietic system: neutropenia, thrombocytopenia.
On the part of the endocrine system: possible galactorea, gynecomastia, menstrual irregularities, amenorrhea, the development of hyperglycemia or worsening of diabetes.
On the part of the reproductive system: priapism, erectile dysfunction, abnormal ejaculation, anorgazmija.
Allergic reactions: rhinitis, skin rash, angioedema.
Dermatological reactions: xerosis, giperpigmentatsiya, itch, seborrhea, photosensitivity.
Other: arthralgia, urinary incontinence.
Contraindications
- Lactation (breast-feeding);
- Hypersensitivity to the drug.
FROM caution should use the drug in patients with diseases of the cardiovascular system (incl. in chronic heart failure, myocardial infarction, conduction disorders), with dehydration, gipovolemii, violation of cerebral circulation, Parkinson's disease, convulsions (incl. history), severe renal or hepatic insufficiency, the abuse of drugs or drug dependence, under conditions, predisposing to the development of the type of tachycardia “pirouette” (bradycardia, electrolyte imbalance, concomitant drugs, prolonging the QT interval), when brain tumors, bowel obstruction, in cases of acute drug overdose, when Reye's syndrome (tk. antiemetic effect of risperidone may mask the symptoms of these conditions), Pregnancy, patients aged 15 years (tk. safety and efficacy of the drug is not installed).
Pregnancy and lactation
The safety of risperidone during pregnancy has not been studied. Application Rileptida® Pregnancy may only, if the expected benefit outweighs the potential risk.
Since risperidone and 9-hydroxy-risperidone are excreted in breast milk, If necessary, use during lactation should stop breastfeeding.
Cautions
In schizophrenia the beginning of treatment Rileptidom® It recommended phased previous therapy, if clinically warranted. Moreover, if patients are transferred from the depot forms of therapy antipsychotics, it is recommended to start therapy Rileptidom instead of the next scheduled injection. Periodically evaluate the need to continue current therapy antiparkinsonian drugs.
Due to the alpha-adrenoceptor blocking action Rileptida® orthostatic hypotension may occur, especially during the initial titration. In the event of hypotension should consider lowering the dose. In patients with diseases of the cardiovascular system, as well as dehydration, hypovolemia, or cerebrovascular disorders, the dose should be increased gradually.
It should be taken into account, that the occurrence of extrapyramidal symptoms is a risk factor for tardive dyskinesia. If you experience signs and symptoms of tardive dyskinesia, should consider the abolition of all antipsychotics.
In the case of neuroleptic malignant syndrome, characterized by hyperthermia, muscle rigidity, instability of autonomic functions, impairment of consciousness and increased CPK, you must cancel all antipsychotics, including Rileptid®.
Patients with schizophrenia increases the risk of suicide attempts, Therefore, treatment of these patients should be under strict medical supervision.
In case of cancellation of carbamazepine and other hepatic enzyme inducers a dose Rileptida® It must be reduced.
Patients during treatment Rileptidom® should be advised to refrain from eating because of the possibility of weight gain.
During treatment Rileptidom® should refrain from drinking alcohol.
Use in Pediatrics
Data on the safety and efficacy of Rileptida® in children under 15 years no, therefore, use of the drug in this category of patients is not recommended.
Effects on ability to drive vehicles and management mechanisms
During treatment, patients should refrain from activities potentially hazardous activities, require high concentration and speed of psychomotor reactions.
Overdose
Symptoms: drowsiness, symptoms of sedation, depression of consciousness, tachycardia, hypotension, extrapyramidal symptoms, rarely – QT prolongation.
Treatment: should ensure a free airway to ensure adequate oxygenation and ventilation. Displaying gastric lavage (after intubation, if the patient is unconscious) and assigning activated carbon combined with a laxative. Should immediately begin ECG monitoring to detect possible cardiac arrhythmias. The specific antidote is absent. Symptomatic therapy. The constant medical supervision and monitoring should continue until symptoms of intoxication.
Drug Interactions
Considering, that Rileptid® an impact primarily on the CNS, it should be used with caution in combination with other centrally acting drugs and alcohol.
Rileptid® reduces the effectiveness of levodopa and other dopamine agonists.
Clozapine reduces the clearance of risperidone.
In an application Rileptida® and carbamazepine, a decrease of concentration of the active antipsychotic fraction of risperidone in plasma. Similar effects may be observed with other hepatic enzyme inducers.
In an application with Rileptidom® fenotiazinы, tricyclic antidepressants and some beta-blockers may increase the plasma concentrations of risperidone, however, this does not affect the concentration of the active antipsychotic fraction.
In an application with Rileptidom® Fluoxetine can increase plasma concentrations of risperidone, to a lesser extent the concentration of the active antipsychotic fraction.
In applying Rileptida® together with other drugs, highly bound to plasma proteins, symptomatic displacement of a drug from the plasma protein fraction is observed.
Antihypertensive drugs increase the severity of BP reduction in patients receiving Rileptida®.
Conditions of supply of pharmacies
The drug is released under the prescription.
Conditions and terms
The drug should be stored out of reach of children at or above 25 ° C. Shelf life – 3 year.
