Risset
Risset: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Risset
ATX code: N05AX08
Active ingredient: risperidone (Risperidone)
Manufacturer: Pliva Hrvatska, d.o.o. (Pliva Hrvatska, doo) (Croatia)
Description and photo updated: 2018-29-11
Prices in pharmacies: from 158 rubles.
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Risset is an antipsychotic drug (neuroleptic).
Release form and composition
Dosage form - film-coated tablets: round, biconvex, scored on one side, white (dosage 1 mg), from light orange to orange (dosage 2 mg), from yellow to yellow with a greenish tinge (dosage 3 mg) or green (dosage 4 mg) color (10 pcs. in blisters, in a cardboard box 2 or 6 blisters and instructions for use of Risset).
Composition of 1 tablet:
- active substance: risperidone - 1, 2, 3 or 4 mg;
- auxiliary components: corn starch, magnesium stearate, lactose monohydrate, talc, sodium carboxymethyl starch, microcrystalline cellulose;
- film shell: 1 mg tablets - opadry II 31F58914 white (sodium citrate dihydrate, macrogol-4000, lactose monohydrate, hypromellose, titanium dioxide); 2 mg tablets - opadray II 31F58914 white, sunset yellow dye (E110); 3 mg tablets - opadray II 31F58914 white, quinoline yellow dye (E104); 4 mg tablets - opadray II 31F58914 white, indigo carmine (E132), quinoline yellow dye (E104).
Pharmacological properties
Pharmacodynamics
Risset's active ingredient is risperidone, a benzisoxazole derivative, a neuroleptic with sedative, hypothermic and antiemetic effects.
Risperidone is a selective monoaminergic antagonist with a high tropism for dopaminergic D 2 and serotonergic 5-HT 2 receptors. It also binds to alpha 1 -adrenergic receptors, with a slightly lower affinity - to alpha 2 -adrenergic and H 1 -histaminergic receptors. Has no tropism for cholinergic receptors.
The antipsychotic effect of risperidone is explained by its ability to block the dopamine D 2 receptors of the mesolimbic and mesocortical systems. Sedation is explained by blockade of adrenergic receptors of the reticular formation of the brain stem, hypothermic action - by blockade of dopamine receptors of the hypothalamus, antiemetic activity - by blockade of dopamine D 2 -receptors of the trigger zone of the vomiting center.
Risset suppresses productive symptoms (hallucinations, delusions, aggressiveness) and automatism. Compared to classical antipsychotics, risperidone inhibits motor activity to a lesser extent, induces catalepsy to a lesser extent.
Due to the balanced central antagonism of risperidone to dopamine and serotonin, the tendency to extrapyramidal side reactions decreases, the therapeutic effect of Rissett is expanded, which also covers the affective and negative symptoms of schizophrenia.
Risperidone can cause a dose-dependent increase in plasma prolactin concentration.
Pharmacokinetics
The drug is quickly and completely absorbed. Food does not affect the volume and rate of absorption. Absolute bioavailability is 74%, relative (tablets versus solution) - 94%. Risperidone reaches its maximum plasma concentration within 1 hour, its active metabolite 9-hydroxyrisperidone - within 3 hours (with a high activity of the CYP2D6 isoenzyme) or 17 hours (with a low activity of the CYP2D6 isoenzyme).
The average time to reach equilibrium concentration of risperidone is 1 day, 9-hydroxyrisperidone is 4–5 days.
The volume of distribution is 1–2 l / kg. The substance is rapidly distributed throughout the body, penetrates into the central nervous system and into breast milk. Plasma concentrations of risperidone and its active metabolite are proportional to the dose taken by Risset (from 1 to 16 mg per day).
Risperidone binds to plasma proteins (albumin and alpha1-acid glycoprotein) by 90%, 9-hydroxyrisperidone - by 77%.
The neuroleptic is metabolized with the participation of the isoenzyme CYP2D6 to form the main metabolite of 9-hydroxyrisperidone. Another metabolic pathway is N-dealkylation.
Risperidone and 9-hydroxyrisperidone constitute the active antipsychotic fraction.
The half-life (T 1/2) of risperidone is 3 or 20 hours (with high and low activity of the CYP2D6 isoenzyme, respectively), 9-hydroxyrisperidone - 21 or 30 hours (with high and low activity of the CYP2D6 isoenzyme, respectively), active antipsychotic fraction - 20 hours …
Excreted: 14% - with bile, 70% - by the kidneys (35-45% in the form of a pharmacologically active antipsychotic fraction).
In patients with chronic renal failure, creatinine clearance (CC) decreases by 60%. In patients with hepatic insufficiency, the plasma concentration of risperidone increases by 35%.
In old age, clearance decreases and T 1/2 of the drug increases.
Indications for use
Risset is used for the relief of acute attacks and long-term maintenance therapy of the following diseases / disorders:
- acute and chronic schizophrenia, other psychotic disorders, accompanied by productive and negative symptoms;
- affective disorders in schizophrenia;
- behavioral disorders developing against the background of dementia with psychotic symptoms, impaired activity (delirium, agitation), symptoms of aggressiveness (outbursts of anger, physical violence);
- behavioral disorders in adults and adolescents from 15 years of age with mental retardation or a reduced intellectual level in cases when the leading symptom of the clinical picture of the disease is destructive behavior (impulsivity, aggressiveness, autoaggression).
As an adjuvant, Risset is prescribed for manias caused by bipolar affective disorders in order to stabilize mood.
Contraindications
Absolute:
- lack of lactase, lactose intolerance, glucose-galactose malabsorption;
- age up to 15 years;
- mania with bipolar affective disorders in children and adolescents under 18;
- lactation period;
- hypersensitivity to any component of the drug.
Relative (Risset tablets are used with caution): Parkinson's disease, seizures (including a history), drug abuse or drug dependence, brain tumor (including pituitary prolactinoma), cerebrovascular accident, diffuse Lewy body disease, Reye's syndrome, acute drug overdose, intestinal obstruction, severe renal / hepatic failure, hypovolemia and dehydration, the presence of risk factors for the development of venous thromboembolism, diseases of the cardiovascular system (cardiac muscle conduction disorders, myocardial infarction, chronic heart failure), predisposing to the development of pirouette-type tachycardia (electrolyte imbalance, bradycardia, concomitant use of drugs that prolong the QT interval),advanced age of patients with dementia, pregnancy.
Risset, instructions for use: method and dosage
Risset tablets should be taken orally 1-2 times a day.
Schizophrenia
On the first day, Risset is prescribed in a daily dose of 2 mg, on the second day - 4 mg. Further, the dose is either kept or adjusted individually. The optimal daily dose is 4–6 mg.
In some cases, for example, in a first-onset episode of schizophrenia, a slower dose escalation and lower initial and maintenance doses may be appropriate.
The maximum allowable daily dose is 16 mg. However, it should be borne in mind that when Risset is taken in doses of 10 mg per day, an increase in the therapeutic effect is usually not observed, while there is a likelihood of developing extrapyramidal symptoms.
Elderly people and patients with kidney or liver diseases are recommended to start treatment with a dose of 0.5 mg 2 times a day. In case of insufficient effect, but provided that Risset is well tolerated, it can be increased to 1-2 mg 2 times a day.
Behavioral disorders in patients with mental retardation
Treatment begins with a dose of 0.5 mg once a day. If necessary, it is increased no more often than every other day, by 0.5 mg. The maximum daily dose is 1.5 mg.
The maintenance dose of Risset is usually 1 mg once a day.
Behavioral Disorders in Patients with Dementia
In most cases, the optimal dose is 0.5 mg 2 times a day. If necessary, it is increased no more often than every other day, by 0.5 mg.
Some patients at the beginning of therapy require the appointment of Risset at a dose of 1 mg 2 times a day.
After improving the condition, the frequency of admission can be reduced to 1 time per day.
Manias in bipolar disorder
For adults, the initial dose of Risset is 2 mg once a day. In the future, if necessary, the doctor selects the dose individually, increasing it no more often than every other day, by 1 mg. The optimal daily dose in most cases is 2–6 mg.
The attending physician should periodically assess the effectiveness of symptomatic therapy and, if necessary, adjust the dosage regimen.
Elderly people and patients with kidney or liver diseases are recommended to start treatment with a dose of 0.5 mg 2 times a day. In case of insufficient effect, but subject to good tolerance of Risset, it is increased to 1-2 mg 2 times a day.
Side effects
- from the central and peripheral nervous system: increased fatigue, insomnia, drowsiness, headache, dizziness, blurred vision, decreased ability to concentrate, anxiety, agitation, extrapyramidal symptoms (acute dystonia, hypersalivation, rigidity, bradykinesia, tremor), akathisia, mania and hypomania. In patients with schizophrenia, the following are possible: thermoregulation disorders, tardive dyskinesia (involuntary rhythmic movements, mainly of the tongue and / or face), epileptic seizures, hypervolemia (due to polydipsia or syndrome of inappropriate antidiuretic hormone secretion), neuroleptic malignant syndrome (impaired consciousness, muscle rigor, instability of autonomous functions, increased activity of creatine phosphokinase);
- on the part of the endocrine system: hyperglycemia, exacerbation of pre-existing diabetes mellitus, increase or decrease in body weight, amenorrhea, menstrual irregularities, gynecomastia, galactorrhea;
- on the part of the cardiovascular system: increased blood pressure, reflex tachycardia, orthostatic hypotension, ventricular fibrillation, pirouette-type ventricular arrhythmia, lengthening of the QT interval, thromboembolism of the venous vessels (including thromboembolism of the pulmonary vessels and deep veins); in elderly patients with dementia - transient ischemic attacks, stroke;
- from the urinary system: urinary tract infection, urinary incontinence;
- from the hematopoietic system: neutropenia, thrombocytopenia;
- from the digestive system: increased appetite, hypo- or hypersalivation, dryness of the oral mucosa, abdominal pain, dyspepsia, constipation, nausea, vomiting, anorexia, increased activity of hepatic transaminases;
- from the reproductive system: anorgasmia, ejaculation disorder, erectile dysfunction, priapism;
- on the part of the skin: itching, hyperpigmentation, dry skin, seborrhea;
- allergic reactions: skin rashes, rhinitis, photosensitivity, angioedema;
- others: arthralgia.
Overdose
There are reports of patients taking the drug in doses up to 360 mg. The data obtained suggest a wide range of Risset safety.
In case of an overdose, an increase in pharmacological effects is noted, which is manifested by drowsiness, sedation, a decrease in blood pressure, tachycardia, and extrapyramidal symptoms. In rare cases, the QT interval is prolonged.
In acute overdose in patients receiving combination therapy, the effect of other drugs should be considered.
Treatment includes gastric lavage (if the patient is unconscious, after intubation), the appointment of activated charcoal and laxatives, ensuring a clear airway (for ventilation and adequate oxygen supply). Electrocardiogram monitoring is required to detect possible arrhythmias.
There is no specific antidote for risperidone. Treatment is symptomatic. With low blood pressure and collapse, intravenous infusion of fluids and / or adrenergic agonists is performed. In acute extrapyramidal disorders, m-anticholinergics are prescribed. The patient requires careful medical supervision until the symptoms of intoxication completely disappear.
special instructions
Prior to the appointment of Risset, patients with schizophrenia should, if possible, gradually discontinue previous therapy. When transferring a patient from depot antipsychotics, the first risperidone intake must replace the next scheduled injection. The physician should periodically evaluate the appropriateness of continuing the current therapy with antiparkinsonian drugs.
Risset increases the risk of thromboembolic complications in patients with a predisposition to blood clots. Before starting treatment, you should find out the presence of all associated risk factors and take appropriate precautions to prevent thromboembolism.
In case of cerebrovascular disorders, dehydration, hypovolemia, cardiovascular diseases, the increase in the dose of the drug should be gradual.
If orthostatic hypotension develops, especially during the dose selection period, it is required to consider reducing the Risset dose.
The risk of developing mania and hypomania during risperidone therapy is reduced if treatment is started at a low dose and increased gradually.
Risset increases appetite. Overeating should be avoided to avoid weight gain.
If symptoms of neuroleptic malignant syndrome or tardive dyskinesia develop, Risset should be canceled and symptomatic therapy should be carried out. Only then can the question of resuming treatment be considered. In order to avoid the development of these complications during the period of therapy, the patient's condition should be monitored and the dose should be regularly adjusted.
Patients with Parkinson's disease and diffuse body disease can be prescribed Risset only after a careful assessment of the balance of benefits and risks, since in these diseases, the sensitivity to antipsychotics is increased and the risk of developing neuroleptic malignant syndrome is increased.
Risset should be used with caution in elderly patients with dementia. According to a meta-analysis of the results of 17 controlled clinical trials, elderly patients (mean age 86 years) with dementia who received atypical antipsychotics (including risperidone) had a higher mortality rate compared to older people who received placebo. The mortality rate was 4% and 3.1%, respectively.
Increased mortality was noted in elderly patients with dementia who received risperidone and furosemide at the same time, compared with groups receiving these drugs separately. The pathophysiological mechanisms that could explain this observation have not been established. In elderly persons receiving other diuretics with risperidone, an increase in mortality was not found. Regardless of the type of therapy, dehydration is a common risk factor for mortality, so it should be carefully monitored during the period of Risset's use.
Placebo-controlled studies have shown an increase in the incidence (compared with placebo) of cerebrovascular accidents (transient ischemic attacks, stroke), including fatal ones, in elderly people with dementia who received risperidone or other atypical antipsychotics.
In patients taking carbamazepine or other inducers of liver microsomal enzymes, if they are canceled, the Risset dose should be reduced.
Influence on the ability to drive vehicles and complex mechanisms
During the entire period of taking Risset, care should be taken when performing potentially hazardous activities that require quick reactions and increased attention.
Application during pregnancy and lactation
The safety of using the drug in pregnant women has not been studied. Risset can only be prescribed when the benefits are clearly higher than the potential risks.
Risperidone and its active metabolite pass into breast milk. If therapy is required during lactation, feeding should be discontinued.
Pediatric use
For children, Risset can only be prescribed by a doctor with experience in child psychiatry.
With impaired renal function
Severe renal failure is a relative contraindication to the appointment of Risset. The drug should be used with caution, dose adjustment is required.
For violations of liver function
Severe hepatic impairment is a relative contraindication to the appointment of Risset. The drug should be used with caution, dose adjustment is required.
Use in the elderly
Risset should be used with caution in elderly patients, especially with dementia. Correction of the dosage regimen may be required.
Drug interactions
Benzodiazepines can be added to Risset for additional sedation.
With caution, you should simultaneously take centrally acting drugs.
Ranitidine and cimetidine increase the plasma concentration of risperidone without increasing the antipsychotic effect.
Tricyclic antidepressants, phenothiazine derivatives and some beta-blockers can increase the plasma concentration of risperidone, but do not affect the concentration of the active antipsychotic phase.
Paroxetine, fluoxetine, quinidine, terbinafine and other inhibitors of the CYP2D6 isoenzyme can increase the plasma level of risperidone, to a lesser extent - the concentration of the active antipsychotic phase.
Clozapine decreases the clearance of risperidone.
Risset should not be used in combination with carbamazepine in patients with mania associated with bipolar affective disorder, since the plasma concentration of the active antipsychotic phase of risperidone decreases.
With the simultaneous use of other antipsychotics, antidepressants, drugs with a central anticholinergic effect, antiparkinsonian drugs, lithium, the likelihood of tardive dyskinesia increases.
In patients with cerebrovascular dementia, the use of a combination of risperidone + furosemide is associated with increased mortality, although the mechanism of this interaction has not been precisely established. In this regard, the possibility of using Risset and diuretics should be evaluated especially carefully, taking into account the expected benefits and possible risks.
With caution, it is necessary to simultaneously use drugs that prolong the QT interval, including other antipsychotics, tricyclic antidepressants, cisapride, lithium, class IA and III antiarrhythmics, methadone, erythromycin, moxifloxacin, mefloquine.
Precautions should be taken with the combined use of drugs that can cause electrolyte disturbances, for example, thiazide diuretics (can provoke hypokalemia). Taking such combinations increases the risk of developing malignant arrhythmias.
The effect of risperidone on other concomitantly used drugs:
- enhances the effects of benzodiazepines, blockers of H1-histamine receptors, narcotic analgesics, ethanol;
- blocks the hypotensive effect of guanethidine;
- reduces the effect of labetalol, phenoxybenzamine and other alpha-blockers, methyldopa, reserpine and other antihypertensive drugs of central action;
- reduces the action of levodopa and other dopamine receptor agonists, as well as, presumably, other inducers of liver microsomal enzymes, such as phenytoin, rifampicin, St. John's wort, barbiturates.
Risset does not affect the clinical effects and pharmacokinetic parameters of topiramate, digoxin, valproic acid and lithium preparations.
Analogs
Risset's analogs are Abilify, Azaleptin, Azaleprol, Aminazine, Amdoal, Ariprizol, Betamax, Haloperidol, Viktoel, Hedonin, Droperidol, Zalasta, Zeldoks, Zyprexa, Zilaxera, Invega, Clozapine, Klopiksalen, Oralisol, Serdinepinectyl, Etperazin and others.
Terms and conditions of storage
Store at a temperature not exceeding 25 ° C, out of the reach of children, in a dry place.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Risset
Reviews about Risset are positive: the drug effectively eliminates many symptoms of schizophrenia and other psychotic disorders, significantly improves the patient's quality of life. Since the drug is highly effective, it is recommended to use it only as directed by a doctor and under his strict control.
Price for Risset in pharmacies
Approximate prices for Risset: 20 tablets of 2 mg - 178-192 rubles, 20 tablets of 4 mg - 218-356 rubles.
Risset: prices in online pharmacies
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Drug name Price Pharmacy |
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Risset 2 mg film-coated tablets 20 pcs. 158 RUB Buy |
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Risset tablets p.p. 2mg 20 pcs. 183 r Buy |
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Risset 4 mg film-coated tablets 20 pcs. 342 r Buy |
Anna Aksenova Medical journalist About the author
Education: 2004-2007 "First Kiev Medical College" specialty "Laboratory Diagnostics".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
