RISPOLYUKS
Active material: Risperidone
When ATH: N05AX08
CCF: Antipsychotic drug (anxiolytic)
ICD-10 codes (testimony): F20, F21, F22, F23, F25, F29, F30, F31
When CSF: 02.01.02.03
Manufacturer: LEK d.d. (Slovenia)
Pharmaceutical form, composition and packaging
Pills, Film-coated white, kapsulovidnye, lenticular, with Valium on one side; of presentations – White pressed weight, coated white.
| 1 tab. | |
| risperidone | 1 mg |
Excipients: lactose monohydrate, microcrystalline cellulose, pre-gelatinized starch, Croscarmellose sodium, sodium lauryl, Colloidal anhydrous silica, magnesium stearate.
The composition of the shell: opadraj white Y-1-7000 (gipromelloza 5 SDR, Titanium dioxide (E171), macrogol).
10 PC. – blisters (2) – packs cardboard.
10 PC. – blisters (5) – packs cardboard.
10 PC. – blisters (6) – packs cardboard.
10 PC. – blisters (10) – packs cardboard.
Pills, Film-coated Pink colour, kapsulovidnye, lenticular, scored on both sides; of presentations – White pressed weight, coated liner pink.
| 1 tab. | |
| risperidone | 2 mg |
Excipients: lactose monohydrate, microcrystalline cellulose, pre-gelatinized starch, Croscarmellose sodium, sodium lauryl, Colloidal anhydrous silica, magnesium stearate.
The composition of the shell: opadraj pink 03B 54942 (gipromelloza 6 SDR, Titanium dioxide (E171), macrogol 400, iron oxide red (E172)).
10 PC. – blisters (2) – packs cardboard.
10 PC. – blisters (5) – packs cardboard.
10 PC. – blisters (6) – packs cardboard.
10 PC. – blisters (10) – packs cardboard.
Pills, Film-coated yellow color, kapsulovidnye, lenticular, with Valium on one side; of presentations – White pressed weight, coated liner yellow.
| 1 tab. | |
| risperidone | 3 mg |
Excipients: lactose monohydrate, microcrystalline cellulose, pre-gelatinized starch, Croscarmellose sodium, sodium lauryl, Colloidal anhydrous silica, magnesium stearate.
The composition of the shell: opadraj yellow 03B 52852 (gipromelloza 5 SDR, Titanium dioxide (E171), macrogol 400, quinoline yellow aluminium lacquer).
10 PC. – blisters (2) – packs cardboard.
10 PC. – blisters (5) – packs cardboard.
10 PC. – blisters (6) – packs cardboard.
Pills, Film-coated dark pink, kapsulovidnye, lenticular, scored on both sides; of presentations – White pressed weight, coated liner dark pink.
| 1 tab. | |
| risperidone | 4 mg |
Excipients: lactose monohydrate, microcrystalline cellulose, pre-gelatinized starch, Croscarmellose sodium, sodium lauryl, Colloidal anhydrous silica, magnesium stearate.
The composition of the shell: Pink opadraj 20A 54901 (giproloza, gipromelloza 6 SDR, Titanium dioxide (E171), gland (III) Red oxide (E172), gland (III) Black oxide (E172)).
10 PC. – blisters (2) – packs cardboard.
10 PC. – blisters (5) – packs cardboard.
10 PC. – blisters (6) – packs cardboard.
Pharmacological action
Antipsychotic drug (anxiolytic), benzisoxazole derivative. It has also a sedative, antiemetic and hypothermic effect.
Selective monoaminergic antagonist, possesses high troponostew to serotonergic 5-NT2-receptors and dopaminergičeskim (D)2-Receptor, also associated with the α1-adrenoreceptors and slightly weaker with histamine h1-рецепторами и a2-adrenoreceptor. Does not have an affinity to holinergicakim receptors.
Risperidone is especially effective in the treatment of schizophrenia with productive symptoms (delirium, hallucinations, aggressiveness), also provides positive action when negative symptomatology.
Balanced Central antagonism to serotonin and dopamine can reduce the propensity to èkstrapiramidnym side-effects and enhance the therapeutic effects of the drug involving negative and affective symptoms of schizophrenia. It causes minimal suppression of motor activity and to a lesser extent induces catalepsy, than classical antipsychotic Neuroleptics.
Pharmacokinetics
Absorption
Risperidone after intake of fully absorbed, reaching Cmax through plasma 1-2 no. Eating does not affect the completeness removals.
Distribution
Css risperidone in the blood of most patients achieved during the first days of treatment, 9-gidroksirisperidona – on 4-5 day. Risperidone plasma concentrations are proportional to the dose of the drug (within the therapeutic dose).
Metabolism
Metabolism is carried out with the help of izofermenta CYP2D6 education 9-gidroksirisperidona, pharmacological activity of which is comparable with the activity of risperidone. Risperidone and 9-gidroksirisperidon represent a so-called nejroleptičeskuû faction. Risperidone is also the reaction of N-dealkylation.
Deduction
T1/2 is about 24 h to 9-gidroksirisperidona and neuroleptic fractions in General. If ingestion 70% the dose of risperidone displayed kidneys (35-45% in the form of a pharmacologically active fraction), 14% – the bile. Plasma clearance ingestion is 1.667 ml / s.
Pharmacokinetics in special clinical situations
In elderly patients, as well as in patients with renal insufficiency increases plasma concentration of the drug in, a T1/2 increases.
Concentrations of risperidone in plasma in patients with hepatic insufficiency do not change.
Testimony
- Schizophrenia (severe exacerbations, maintenance therapy) and other psychotic disorders with a predominance of productive and/or negative symptoms;
-bipolar disorders in maniâh;
- Affective disorders in a variety of mental disorders;
- Behavioral disorders in patients with dementia when symptoms persist aggression, violations of the activities (excitation, delirium) or psychotic symptoms;
-behavioral disorders in patients with low intellectual level or mental retardations (incl. as a means of adjuvant therapy to stabilize moods).
Dosage regimen
The drug is taken orally, regardless of the meal, drinking water.
To adults and children over 15 years initial dose Rispolûksa® at acute illness and chronic course is 2 mg / day (in 1 or 2 admission), on the second day – to 4 mg / day; Next, as necessary, the dose can be increased or decreased by 1-2 mg weekly intervals. Doses above 10 mg / day showed a higher efficiency compared with lower doses and may cause extrapyramidal symptoms. The maximum daily dose – 16 mg.
In the case of the need to achieve a sedative action simultaneously with Rispolûksom® You can assign benzodiazepines.
At Kidney and/or liver failure, and for elderly patients the recommended initial dose Rispolûksa® amounts to 500 g 2 times / day. This dose can be gradually (by 500 g) increased to 1-2 mg per reception 2 times / day.
At the same time as the treatment Rispolûksom® recommended phasing out previously hosted neiroleptika. If you previously used neuroleptic-depot for injecting, the first dose of Rispolûksa® instead of injections should be taken in accordance with the regime for introduction of the neiroleptika Depot.
Side effect
Cardio-vascular system: orthostatic hypotension, reflex tachycardia, arterial hypertension, sinusovaya bradycardia, AV блокада 1 degrees, Atrial fibrillation, syncope, peripheral edema.
From the digestive system: dry mouth, nausea, vomiting, dyskinesia, dyspepsia, anorexia, abdominal pain, constipation, Hypo- or hypersalivation, jaundice, dysphagia, gastritis, pancreatitis, increased ALT, IS.
From the nervous system: insomnia, headache, dizziness, excitation, anxiety, drowsiness, fatiguability, decreased ability to concentrate, convulsions; rarely – extrapyramidal disorder (tremor, rigidity, hyperptyalism, bradikineziâ, akathisia, acute dystonia), cerebrovascular accident (in older patients with predraspolagatmi factors), incoordination, speech disorders, gipočuvstvitel′nost′, sleep disorders. In patients with schizophrenia were reported later diskinesia (involuntary movements of the tongue and facial muscle contraction), neuroleptic malignant syndrome (hyperthermia, extreme muscle rigidity, disturbance of consciousness, autonomic disorders, increased activity of CPK, tachypnea), seizures.
With the genitourinary system: priapism, erectile dysfunction, anorgazmija, urinary incontinence, abnormal ejaculation.
On the part of the endocrine system: galactorrhea, gynecomastia, menstrual irregularities, giperglikemiâ, hyperprolactinemia, violation of the formulation of antidiuretic hormone.
Allergic reactions: skin rash, rhinitis, itching, angioedema, anaphylactic shock.
Laboratory findings: neutropenia, thrombocytopenia, anemia, granulocytopenia, agranulocytosis, eozinofilija, leukopenia.
Other: xerosis, giperpigmentatsiya, photosensitivity, hyperkeratosis, increased perspiration, weight gain, arthralgia, myalgia, visual impairment, mania, nasal congestion, nose bleed, sleep apnea, elderly patients with dementia have increased susceptibility to infection, polydipsia.
Contraindications
-hypersensitivity to risperidonu or other components of the drug, lactation.
FROM caution should be prescribed in the following states:
— severe kidney and/or liver failure;
- cardiovascular diseases (congestive heart failure, myocardial infarction, atrioventrikulyarnaya blockade);
- Gipovolemiя;
- State, predisposing to the development of tachycardia type “pirouette” (bradycardia, electrolyte imbalance, concomitant medications, prolonging the QT interval);
- Parkinson's disease;
is a violation of cerebral circulation;
Reye-syndrome;
- Epilepsy, convulsions in history;
-brain tumor;
acute overdose of drugs, drug dependence;
-Dysphagia;
- Bowel obstruction;
- Children up to age 15 years (limited experience in the application);
- Pregnancy.
Pregnancy and lactation
Application of risperidone when pregnancy is possible only in case, if the expected benefit to the mother outweighs the potential risk to the fetus.
The drug is excreted in breast milk, Therefore, when taking the drug should stop breastfeeding.
Cautions
Because, admission Rispolûksa® can lead to an increase in body mass index, the patient should give advice on diet.
When the occurrence of orthostatic hypotension, especially at the beginning of treatment, should consider lowering the dose.
In patients with diseases of the cardiovascular system, as well as dehydration, hypovolemia or cerebrovascular violations dose should be increased gradually.
If you cancel the carbamazepine and other inductors of liver enzymes dose Rispolûksa® It must be reduced.
When symptoms of late psoriasis or malignant neuroleptic Syndrome should consider abolishing all antipsychotic medicines, including Rispolûks®.
It is recommended the gradual elimination of the drug, tk. After the abrupt cessation of treatment with high doses of Neuroleptics may develop withdrawal symptoms (vomiting, nausea, increased perspiration, insomnia).
Effects on ability to drive vehicles and management mechanisms
During treatment risperidonom should be careful when driving vehicles and other potentially hazardous activities, require increased attention and psychomotor speed reactions.
Overdose
Symptoms: drowsiness, sedation, tachycardia, hypotension, extrapyramidal symptoms, rarely – QT prolongation.
Treatment: in acute overdose should ensure a free airway to ensure adequate oxygenation and ventilation, ECG monitoring, gastric lavage, the appointment of activated charcoal and laxatives, symptomatic therapy, designed to maintain vital functions of the body, When the development extrapiramidale symptoms appointment antiholinergicakih drugs. Continuous medical monitoring should continue until the complete disappearance of the symptoms of intoxication. No specific antidote.
Drug Interactions
Antacids reduce the absorption of oral doses.
Risperidone reduces the effectiveness of levodopa and dopamine agonists other.
Antihypertensive medicines increase the severity of the decline AD against the backdrop of the admission of risperidone.
Fenotiazinovye Neuroleptics, tricyclic antidepressants and some beta-adrenoblokatora together with risperidonom can increase its concentration in the blood plasma, without affecting the concentration of Neuroleptic fractions.
Carbamazepine and other inductors of liver enzymes reduce the concentration of the active fractions of risperidone in plasma.
While receiving fluoxetine concentrations of risperidone in plasma, However, the level of “Neuroleptic fractions” increases slightly.
Antipsychotics increase the effects of alcohol, antihistamines, benzodiazepines, drugs, CNS depressants.
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 a temperature no higher than 25 ° C. Shelf life – 2 year.
