TORENDO
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: KRKA d.d. (Slovenia)
Pharmaceutical form, composition and packaging
Pills, Film-coated white or nearly white, Oval, lenticular, with Valium on one side.
| 1 tab. | |
| risperidone | 1 mg |
Excipients: tsellaktoza (spray dried compound, consisting of 75% the alpha lactose monohydrate and 25% cellulose powder), microcrystalline cellulose, Croscarmellose sodium, Colloidal anhydrous silica, sodium lauryl, magnesium stearate.
The composition of the shell: Opadry white 03N28785 (a mixture of hypromellose, titanium dioxide, TALC, propylene glycol).
10 PC. – blisters (2) – packs cardboard.
10 PC. – blisters (3) – packs cardboard.
10 PC. – blisters (6) – packs cardboard.
Pills, Film-coated light orange, Oval, lenticular, with Valium on one side.
| 1 tab. | |
| risperidone | 2 mg |
Excipients: tsellaktoza (spray dried compound, consisting of 75% the alpha lactose monohydrate and 25% cellulose powder), microcrystalline cellulose, Croscarmellose sodium, Colloidal anhydrous silica, sodium lauryl, magnesium stearate.
The composition of the shell: Opadry white 03N28785 (a mixture of hypromellose, titanium dioxide, TALC, propylene glycol), dye iron oxide yellow (E172), iron oxide red dye (E172).
10 PC. – blisters (2) – packs cardboard.
10 PC. – blisters (3) – packs cardboard.
10 PC. – blisters (6) – packs cardboard.
Pills, Film-coated yellow color, Oval, lenticular, with Valium on one side.
| 1 tab. | |
| risperidone | 3 mg |
Excipients: tsellaktoza (spray dried compound, consisting of 75% the alpha lactose monohydrate and 25% cellulose powder), microcrystalline cellulose, Croscarmellose sodium, Colloidal anhydrous silica, sodium lauryl, magnesium stearate.
The composition of the shell: Opadry white 03N28785 (a mixture of hypromellose, titanium dioxide, TALC, propylene glycol), quinoline yellow dye (E104).
10 PC. – blisters (2) – packs cardboard.
10 PC. – blisters (3) – packs cardboard.
10 PC. – blisters (6) – packs cardboard.
Pills, Film-coated light green, Oval, lenticular, with Valium on one side.
| 1 tab. | |
| risperidone | 4 mg |
Excipients: tsellaktoza (spray dried compound, consisting of 75% the alpha lactose monohydrate and 25% cellulose powder), microcrystalline cellulose, Croscarmellose sodium, silicon oxide, colloidal anhydrous, sodium lauryl, magnesium stearate.
The composition of the shell: Opadry white 03N28785 (a mixture of hypromellose, titanium dioxide, TALC, propylene glycol), quinoline yellow dye (E104), dye indigo carmine (E132).
10 PC. – blisters (2) – packs cardboard.
10 PC. – blisters (3) – packs cardboard.
10 PC. – blisters (6) – packs cardboard.
Pharmacological action
Antipsychotic drug (anxiolytic).
Risperidone is a selective antagonist of monoaminergičeskim with pronounced affinity for serotoninergic 5-NT2-receptors and dopamine D2-Receptor, also associated with the α1-adrenoreceptors and, with somewhat less affinity, with histamine H1-рецепторами и a2-adrenoreceptor. It does not have affinity for holinoretseptorami. It has also a sedative, antiemetic and hypothermic effect.
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 effect due to blockade of dopamine D2-receptor trigger zone of the vomiting center.
Gipotermicescoe effect blockade dopaminovykh receptors in the hypothalamus.
Reduces productive symptoms (delirium, hallucinations), automatism. It causes minimal suppression of motor activity and to a lesser extent induces catalepsy, than classical antipsychotics (neuroleptics).
Balanced central antagonism of 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
Absorption
The ingestion completely absorbed risperidone (regardless of the meal) and Cmax in plasma observed through 1-2 no.
Distribution
Concentration risperidona plasma is proportional to the dose of the drug (within the therapeutic dose).
Risperidone is rapidly distributed in the body. Vd is 1-2 l / kg. Plasma risperidone contact albuminom and acidic α-1-glycoproteins. A faction of risperidone and 9-hydroxy-risperidone, associated plasma protein, up 88% and 77%, respectively.
Metabolism
Risperidone is metabolizmu with the participation of izofermenta CYP2D6 with formation of 9-hydroxy-risperidone, which has a similar pharmacological action.
Risperidone and 9-hydroxy-risperidone are effective antipsychotic fraction. Further metabolism of risperidone is N-dealkilirovania. The ingestion of risperidone displays with T1/2 about 3 no. T1/2 9-hydroxy-risperidone and the active antipsychotic fraction is 24 no.
In most patients, Css risperidone observed after 1 day after treatment. Css 9-hydroxy-risperidone in most cases achieved through 3-4 days after initiation of treatment.
Deduction
Excreted in the urine -70% (of them 35-45% in the form of a pharmacologically active fraction) and 14% – the bile.
Pharmacokinetics in special clinical situations
In elderly patients or patients with insufficient kidney function the one-time use of the drug has a high concentration of active substances in the plasma and slow their excretion.
Testimony
- Acute and chronic schizophrenia and other psychotic states 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), for violations of mental activity (excitation, delirium) or psychotic symptoms;
- As an adjuvant therapy in the treatment of mania in bipolar disorder;
as adjuvant therapy in adolescents with conduct disorders 15 years and adult patients with reduced intellectual level or mental retardation, in cases, if the destructive behavior (aggressiveness, impulsiveness, autoagressiâ) is leading the clinical picture of the disease.
Dosage regimen
In schizophrenia
Adults and children over the age of 15 years risperidone may be appointed 1-2 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 >10 mg / day showed a higher efficiency compared with lower doses and may cause extrapyramidal symptoms. Because, that the safety of the drug in doses >16 mg / day has not been studied, doses above this level should not be used.
Information on how to use the drug to treat schizophrenia from children under the age of 15 years no.
Elderly patients It is recommended to use the drug in a dose on 0.5 mg 2 times / day. Dose can be increased individually on 0.5 mg 2 times / day to 1-2 mg 2 times / day.
Patients with diseases of the liver and kidney It is recommended to use the drug in a dose on 0.5 mg 2 times / day. This dose can be gradually increased to 1-2 mg 2 times / day.
When drug abuse or drug dependence
Recommended daily dose 2-4 mg.
When behavioral disorders in patients with dementia
The recommended initial dose of the drug – by 0.25 mg 2 times / day (adequate dosage form). If necessary dose can be individually increase on 0.25 mg 2 times / day, no more than a day. For most patients, the optimal dose is 0.5 mg 2 times / day. Some patients shows the drug on 1 mg 2 times / day. On reaching the optimal dose of the drug may be recommended 1 time / day.
Mania in bipolar disorder
The recommended initial dose of the drug – by 2 mg/day at a time. 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.
Conduct disorders in patients with delayed mental development
Patients, weighing ≥ 50 kg It is recommended to use the drug in a dose on 0.5 mg 1 time / day. If necessary, this dose may be increased by 0.5 mg / day, no more, than a day. For most patients, the optimal dose is 1 mg / day. However, for some patients it is preferable to use 0.5 mg / day, or increase doses up to 1.5 mg / day.
Patients, weighing ≤ 50 kg recommended use of the drug in the initial dose of 0.25 mg 1 time / day. If necessary, this dose may be increased by 0.25 mg / day, no more, than a day. For most patients, the optimal dose is 0.5 mg / day. However, for some patients it is preferable to use 0.25 mg / day, or increase doses up to 0.75 mg / day.
Prolonged use of the drug Torendo® teenagers should be under the constant supervision of a doctor.
Use of the drug in children under the age of 15 years not recommended.
Side effect
From the central and peripheral nervous system: insomnia, ažitaciâ, alarm, headache; sometimes – drowsiness, fatigue, dizziness, impaired concentration, blurred vision; rarely – extrapyramidal symptoms (tremor, rigidity, hyperptyalism, bradikineziâ, akathisia, acute dystonia), mania or gipomaniya, stroke (in elderly patients with predisposing factors), and hypervolemia (due to polydipsia or syndrome of inappropriate secretion of antidiuretic hormone), pozdnyaya dyskinesia (involuntary rhythmic movements mainly language and / or the person), NMS (hyperthermia, muscle rigidity, instability of autonomous functions, impairment of consciousness and increased CPK), violation of thermoregulation and seizures.
From the digestive system: constipation, dyspepsia, nausea or vomiting, abdominal pain, increase in liver transaminases, dry mouth, hyposalivation or gipersalivacia, anorexia and / or increased appetite, increase or reduction of body weight.
Cardio-vascular system: sometimes – orthostatic hypotension, reflex tachycardia, increased blood pressure.
On the part of the endocrine system: galactorrhea, gynecomastia, menstrual disorders, amenorrhea, weight gain, giperglikemiâ, exacerbation of pre-existing diabetes mellitus.
Reproductive system: priapism, erectile dysfunction, abnormal ejaculation, anorgazmija.
From the hematopoietic system: neutropenia, thrombocytopenia.
Dermatological reactions: xerosis, giperpigmentatsiya, itch, seborrhea.
Allergic reactions: rhinitis, rash, angioedema, photosensitivity.
Other: arthralgia, urinary incontinence.
Contraindications
- Lactation;
- Childhood and adolescence up 15 years (efficacy and safety have not been established);
- Hypersensitivity to the drug.
FROM caution use in patients with diseases of the cardiovascular system (congestive heart failure, myocardial infarction, conduction disorder of the heart muscle), Dehydration and hypovolemia, violation of cerebral circulation, Parkinson's disease, convulsions (incl. history), Renal or severe hepatic insufficiency, drug abuse or drug addiction, states, predisposing to the development of the type of tachycardia “pirouette” (bradycardia, electrolyte imbalance, concomitant drugs, prolonging the QT interval), brain tumors, bowel obstruction, cases of acute overdose of drugs, Reye's syndrome (antiemetic effect of risperidone may mask the symptoms of these conditions).
Pregnancy and lactation
Safety of risperidone during pregnancy have not been studied.
Use of the drug during pregnancy is possible only in case, when the intended benefits to the mother outweighs the potential risk to the fetus.
Since risperidone and 9-hydroxy-risperidone are excreted in breast milk, If necessary, use during lactation should decide the issue of termination of breastfeeding.
Cautions
Schizophrenia early treatment risperidonom it is recommended to gradually cancel previous therapy, if clinically warranted. If patients are transferred from the depot-therapy forms of antipsychotics, the application of risperidone to start instead of the next scheduled injection. Periodically should evaluate the need for continuing therapy potivoparkinsoničeskimi drugs.
In connection with the α-adrenoblokirutm effect of risperidone may occur ortostatical gipotenzia, especially during the initial titration. In the event of hypotension should consider lowering the dose. In patients with diseases of cardiovascular system, as well as dehydration, hypovolemia, or cerebrovascular disorders, the dose should be increased gradually, according to the recommendations.
The occurrence of extrapyramidal symptoms is a risk factor for tardive dyskinesia. If you experience signs and symptoms of late psoriasis, should consider the abolition of all antipsychotics.
In vozniknovenii NMS, characterized by hypertension, muscle rigidity, instability of autonomous functions, violation of consciousness and increased levels of CPK must cancel all antipsychotic medicines, including risperidone.
If you cancel the carbamazepine and other inductors of liver enzymes dose risperidone should be reduced.
Patients should refrain from eating too much in connection with the possibility of increasing body mass index.
Use in Pediatrics
Use of the drug in children under the age of 15 years not recommended.
Effects on ability to drive vehicles and management mechanisms
During treatment should refrain from activities potentially hazardous activities, require high concentration and speed of psychomotor reactions, as well as from alcohol (ethanol).
Overdose
Symptoms: drowsiness, sedation, depression of consciousness, tachycardia, hypotension, extrapyramidal disorder, in rare cases, QT prolongation.
Treatment: necessary to ensure a free airway to ensure adequate oxygenation and ventilation, gastric lavage (after intubation, If the patient is unconscious) and assigning the activated carbon in combination with laxatives. Symptomatic therapy, aimed at the maintenance of the vital functions of the body.
For early diagnosis of possible disturbances of cardiac rhythm as quickly as possible to begin ECG monitoring. Careful medical supervision and ECG monitoring is carried out to complete disappearance of symptoms of intoxication. The specific antidote is absent.
Drug Interactions
Because risperidone has an effect primarily on the central nervous system, It should be used with caution in combination with other drugs central action and ethanol.
Risperidone reduces the effectiveness of levodopa and dopamine agonists other.
Clozapine reduces the clearance of risperidone.
When using carbamazepine concentration has decreased active antipsihoticescoy fraction of plasma risperidone. Similar effects may be observed with other hepatic enzyme inducers.
Fenotiazinы, tricyclic antidepressants and some β-adrenoblokatora may strengthen concentration risperidona plasma, however, this does not affect the concentration of the active antipsychotic fraction.
Fluoxetine can increase plasma concentrations of risperidone, but to a lesser extent the concentration of the active antipsychotic fraction, therefore the dose of risperidone should be adjusted.
While the application of risperidone with drugs, highly bound to plasma proteins, symptomatic displacement of a drug from the plasma protein fraction is observed.
Antihypertensive medicines increase the severity of BP reduction on the background of risperidone.
Conditions of supply of pharmacies
The drug is released under the prescription.
Conditions and terms
List B. The drug should be stored out of reach of children at or above 30 ° C. Shelf life – 3 year.
