Active substanceRisperidoneRisperidone
Similar drugsTo uncover
  • Leptinorm
    pills inwards 
  • Rezalen
    pills inwards 
  • Rezalen
    pills inwards 
  • Rideonex®
    pills inwards 
    GEDEON RICHTER, OJSC     Hungary
  • Rilept
    pillspowder inwards 
  • Rileptid®
    pills inwards 
  • Ridonal®
    pills inwards 
    Alkaloid, JSC     Macedonia
  • Rispaxol®
    pills inwards 
    GRINDEX, JSC     Latvia
  • Risperidone
    pills inwards 
    RAFARMA, CJSC     Russia
  • Risperidone
    pills inwards 
    VERTEKS, AO     Russia
  • Risperidone
    pills inwards 
    NORTH STAR, CJSC     Russia
  • Risperidone
    pills inwards 
    ATOLL, LLC     Russia
  • Risperidone
    pills inwards 
  • Risperidone
    pills inwards 
    MAKIZ-PHARMA, LLC     Russia
  • Risperidone
    pills inwards 
  • Risperidone
    solution inwards 
    ATOLL, LLC     Russia
  • Risperidone Zentiva
    pills inwards 
    Zentiva c.s.     Czech Republic
  • Risperidone Organica
    pills inwards 
    ORGANICS, JSC     Russia
  • Risperidone-TL
    pills inwards 
  • Rispolept®
    solution inwards 
  • Rispolept®
    pills inwards 
  • Rispolept® Quiquette
    pills inwards 
  • Rispeplet Konsta®
    powder w / m 
  • Rispolux®
    pills inwards 
    Sandoz d.     Slovenia
  • Risset®
    pills inwards 
  • Risset® Qwitab
    pills inwards 
  • Sizodon-san
    pills inwards 
  • Speridan®
    pills inwards 
  • Torendo®
    pills inwards 
  • Torendo® Ku-Tab
    pills inwards 
  • Dosage form: & nbsptablets, dispersible in the oral cavity
    Composition:1 tablet contains: active substance risperidone 2.0 mg; Excipients: mannitol (Pearlitol 50C) 174.850 mg mannitol (Pearlitol 200 SD) 16,15 mg, sodium carboxymethylstarch (type A) 6.0 mg mint flavor (HF84 NAT, WONF-SD 491) 1.0 mg.

    Description:Round Valium tablets of white color with a smooth surface and a porous or rough edges.
    Pharmacotherapeutic group:antipsychotic agent (antipsychotic)
    ATX: & nbsp

    N.05.A.X   Other antipsychotics

    N.05.A.X.08   Risperidone

    Pharmacodynamics:An antipsychotic agent (neuroleptic) (APS), a benzisoxazole derivative; also has a sedative, antiemetic and hypothermic effect. Selective monoaminergic antagonist, has a high affinity for 5-HT2-serotonergic receptors and D2-dopaminergic receptors, binds also to alpha1-adrenergic receptors and, somewhat weaker, to H1-histaminergic and alpha2-adrenergic receptors. Has no tropism for cholinergic receptors.
    The antipsychotic effect is due to the blockade of D2-dopaminergic receptors of the mesolimbic and mesocortical system. Sedative action is due to blockade of adrenoreceptors of the reticular formation of the brainstem; antiemetic action - blockade of D2-dopamine receptors in the trigger zone of the vomiting center; hypothermic action - blockade of dopamine receptors of the hypothalamus.
    Suppresses productive symptoms (delirium, hallucinations, aggressiveness), automatism. It causes less inhibition of motor activity and to a lesser degree induces catalepsy than classical antipsychotics.A balanced central antagonism to serotonin and dopamine can reduce the propensity to extrapyramidal side effects and extend the therapeutic effect of the drug to cover the negative and affective symptoms of schizophrenia.
    Pharmacokinetics:

    Absorption is fast and complete (food does not affect the completeness and absorption rate). The absolute bioavailability of risperidone is 70%, the relative bioavailability of risperidone tablets is 94% compared to the solution. The maximum concentration in the blood plasma is detected after 1-2 hours. The concentration of risperidone in the plasma depends on the dose. Quickly and well distributed in the body. The volume of distribution is 1-2 l / kg. Metabolized in the liver with the participation of isoenzyme CYP2D6. The main pathway of biotransformation is hydroxylation to form the main active metabolite of 9-hydroxy-risperidone, which has similar pharmacological properties with risperidone. Another way of biotransformation, which has a minimum value, is N-dealkylation. Risperidone and 9-hydroxy-risperidone form the active antipsychotic fraction (AAPP). In plasma, 88% of risperidone and 77% of 9-hydroxy-risperidone bind to proteins (albumin and alpha1-glycoprotein).Although hydroxylation of risperidone is susceptible to genotypic polymorphism, the differences in pharmacokinetics and the effect of active metabolites in different phenotypes are minimal. The half-life (T1/2) risperidone with active metabolism for about 3 hours, at a slow one for 20 hours, T1/2 9-hydroxy-risperidone with an active metabolism of 21 h, at a slow one - 30 h. T1/2 AAPF in both phenotypes is 24 hours. The equilibrium concentration of risperidone in the body in most patients is established within 1 day, and 9-hydroxy-risperidone for 4-5 days. After one week of use, 70% of the risperidone taken is excreted by the kidneys, 14% - with feces, 35-45% of the fraction excreted in the urine, consists of unchanged risperidone and 9-hydroxy-risperidone. The pharmacokinetics of risperidone in adults and children does not differ. With a single admission in the plasma of elderly patients there is a decrease in clearance of AAPF by 30% and an increase in T1/2on 38%. In patients with renal insufficiency, the clearance of the AAPF decreases by 60%. In patients with hepatic insufficiency, the concentration of risperidone in plasma did not differ from other patients, despite the fact that the mean free fraction of risperidone was increased by approximately 35%.

    Indications:

    - Schizophrenia.

    - Treatment of manic episodes of moderate to severe severity due to bipolar disorder.

    Contraindications:

    Hypersensitivity to risperidone and other components of the drug; period of pregnancy and breastfeeding; children's age till 18 years.

    Carefully:

    Chronic heart failure; ischemic heart disease, myocardial infarction; atrioventricular block; dehydration; impaired cerebral circulation; dementia associated with Lewy bodies or Parkinson's disease; convulsions (including in the anamnesis); severe hepatic impairment; drug abuse or drug dependence; conditions predisposing to the development of tachycardia such as "pirouette" (bradycardia, electrolyte imbalance, concomitant medication prolonging the interval QT); risk factors for thromboembolism of venous vessels; brain tumor, including prolactinoma of the pituitary gland; intestinal obstruction; acute overdose of medicines; Reye syndrome (antiemetic effect of risperidone can mask the symptoms of these conditions); elderly patients.

    Pregnancy and lactation:

    The safety of the use of risperidone in pregnancy is not well understood. According to post-marketing research, the use of risperidone during the third trimester of pregnancy can cause the development of reversible extrapyramidal symptoms in newborns. The use of the drug Risset® Qtitab during pregnancy is not recommended. Because the risperidone and 9-hydroxy-risperidone penetrate into breast milk, if necessary, the use of the drug Risset® Qitab during lactation should stop breastfeeding.

    Dosing and Administration:

    Inside. Tablets of the Risset® Kvitab preparation for resorption are very fragile, they should not be divided and chewed. Remove tablets from the blister with dry hands, pulling up the edge of the foil, and immediately place them on the tongue. If the tablets are taken with food, then there should be no food in the mouth when the patient puts the tablet on the tongue. Tablets begin to disintegrate in the mouth after a few seconds, and after that they can be swallowed immediately, without washing down with water. If necessary, you can drink the tablet with water or another liquid.

    Schizophrenia

    It is recommended to take 1 -2 times / day. The initial dose of 2 mg / day.On the 2nd day the dose can be increased to 4 mg / day. From this moment the dose can either be kept at the same level, or individually adjusted if necessary. Usually the optimal dose is 4-6 mg / day. In a number of cases, for example, in patients with a new episode of the disease, a slower dose increase and lower initial and maintenance doses may be justified. With the use of the Risset® Kvitab preparation in doses of more than 10 mg / day, there was no increase in the therapeutic effect compared with smaller doses, and the likelihood of developing extrapyramidal symptoms increased. The maximum daily dose is 16 mg / day.

    For elderly patients a dose of 2-4 mg / day is recommended.

    Treatment of manic episodes of moderate to severe severity due to bipolar disorder

    It is recommended to take 1 time / day. The initial dose of 2 mg / day. If necessary, increase the dose by 1 mg / day should not be earlier than 24 hours. The recommended range of doses from 2 to 6 mg / day. It is necessary to regularly evaluate the feasibility of further use of the Risset® Kvitab preparation in patients with this pathology.

    For elderly patients a dose of 2-4 mg / day is recommended.

    When liver and kidney disease a dose of 2-4 mg / day is recommended.

    Side effects:

    The incidence of side effects is classified according to the recommendations of the World Health Organization: very often - not less than 10%; often - not less than 1%, but less than 10%; infrequently - not less than 0,1%, but less than 1%; rarely - not less than 0.01%, but less than 0.1%; very rarely - less than 0.01%, including single messages; frequency is unknown - insufficient data for estimating the frequency of the phenomenon in the population.

    Infections: often - pneumonia, influenza, tracheobronchitis, upper respiratory tract infections, urinary tract infections; infrequently - sinusitis, ear infections, viral infections, tonsillitis, inflammation of the subcutaneous tissue, otitis media, eye infection, onychomycosis, acarodermatitis, cystitis; rarely - chronic otitis media.

    From the side of metabolism and nutrition: often - increase / decrease in appetite; infrequently - anorexia, polydipsia; very rarely diabetic ketoacidosis; frequency unknown - water intoxication.

    On the part of the blood and lymphatic system: infrequently - anemia, thrombocytopenia; rarely - granulocytopenia; very rarely - neutropenia, thrombocytopenia; frequency unknown - agrunulocytosis.

    From the immune system: infrequently - a hypersensitivity reaction; frequency unknown - anaphylactic reaction.

    From the nervous system: very often - insomnia, parkinsonism (including extrapyramidal disorders, musculoskeletal rigidity, cogwheel syndrome, akinesia, bradykinesia, hypokinesia, muscle rigidity); anxiety, nervousness, confusion, lethargy, akathisia, tremor, sedation, dystonia (including muscle spasms, involuntary muscle contractions, muscle contractions, eyeball movements, tongue paralysis), lethargy, postural bleeding, dyskinesia (including muscle twitching, chorea and choreoathetosis), syncope, transient ischemic attack, depressed state, drooling, stroke, attention impairment; infrequent excitation, flattening of affect, sleep disturbance, weakening of libido, anorgasmia, lack of response to stimuli, impaired coordination, loss of consciousness, speech disorder, hypoesthesia, impaired movement, tardive dyskinesia, malignant neuroleptic syndrome, diabetic coma; very rarely - mania.

    From the gastrointestinal tract: often - nausea, vomiting, diarrhea, constipation, abdominal pain, indigestion, dry mouth, discomfort in the stomach; infrequently - dysphagia, gastritis, fecal matter; rarely - intestinal obstruction, jaundice, pancreatitis, cheilitis, aptialism.

    From the cardiovascular system (SSS): often - tachycardia; rarely - orthostatic hypotension, atrioventricular block, palpitations, sinus bradycardia, blockade branch gastrointestinal atrial bundle branch block, "tides"; rarely - stroke and transient ischemic attack (mainly in elderly patients with dementia associated with psychosis); unknown - venous thromboembolism.

    From the side of the organ of vision: often - blurring of vision; infrequently - conjunctivitis, hyperemia of the eye, dry eyes, increased tear, orbital edema, photophobia; rarely - glaucoma, decreased visual acuity, rotational nystagmus.

    From the side of the organ of hearing and labyrinth: infrequently - pain, "ringing" in the ears.

    On the part of the respiratory system: often - shortness of breath, nosebleed, cough, nasal congestion, sore throat; infrequently - rhinitis, respiratory failure, dysphonia, "wheezing" breathing, aspiration pneumonia, productive cough, blockage of the respiratory tract, wet wheezes, swelling of the nose; very rarely - hyperventilation, sleep apnea syndrome.

    From the endocrine system: rarely - inadequate secretion of antidiuretic hormone.

    From the side of the reproductive system: infrequently - amenorrhea, violation of sexual function, erectile dysfunction, ejaculation, galactorrhea, gynecomastia, menstrual cycle disorder; frequency is unknown - priapism.

    From the side of the kidneys and urinary tract: often - enuresis; infrequently - dysuria, urinary incontinence, pollakiuria.

    From the skin and subcutaneous tissues: often - skin rash, erythema; infrequently - a violation of skin pigmentation, itching, acne, skin damage, erythematous rashes, alopecia, seborrheic dermatitis, dry skin, hyperkeratosis; rarely - dandruff.

    From the side of the musculoskeletal and connective tissue: often - arthralgia, back pain, pain in the limbs; infrequently - muscle weakness, myalgia, neck pain, swelling of the joints, joint stiffness, chest pain; rarely rhabdomyolysis.

    Laboratory and instrumental data: often - an increase in the concentration of prolactin in the blood plasma, an increase in body weight; infrequent - lengthening of the interval QT on an electrocardiogram (ECG), hyperglycemia; increased activity of "hepatic" transaminases, neutropenia, eosinophilia, decreased hemoglobin; increased body temperature; rarely - a decrease in body temperature.

    Common violations: often - fatigue, asthenia, peripheral edema, gait disturbance; infrequently - thirst, flu-like condition, poor health, sluggishness, chills, cold extremities, edema of the face, general swelling.

    Overdose:

    Symptoms: increased pharmacological effects - drowsiness, sedation, tachycardia, pronounced lowering of blood pressure (BP), extrapyramidal symptoms. It has been reported that risperidone is taken in a dose of 360 mg. The data obtained suggest a rather wide range of safety of risperidone. In rare cases, an overdose marked lengthening interval QT, tachycardia such as "pirouette", seizures. In the case of acute overdose with combined therapy, the possibility of involving other drugs should be analyzed.

    Treatment: it is necessary to ensure free airway patency to maintain adequate gas exchange in the body; gastric lavage (after intubation if the patient is unconscious) and the use of activated charcoal together with a laxative. Immediately begin monitoring the parameters of the electrocardiogram to detect possible arrhythmia.There is no specific antidote. Symptomatic therapy aimed at maintaining the function of the central nervous system (CNS) and CCC, detoxification therapy should be performed. If there is a pronounced decrease in blood pressure or a vascular collapse, intravenous infusion solutions and / or use sympathomimetic drugs should be administered. In case of development of acute extrapyramidal symptoms, anticholinergic drugs should be used. Continuous medical supervision of vital functions should be continued until the symptoms of intoxication disappear.

    Interaction:

    Given that APS, including risperidone, have an impact primarily on the central nervous system, they should be used with caution in combination with other drugs of central action. APS strengthen the action of ethanol, opiates, antihistamines and benzodiazepines. For the treatment with risperidone, benzodiazepines can be added if an additional sedative effect is required.

    When therapy with a combination of risperidone with other APS, lithium, antidepressants, antiparkinsonics, drugs with a central anticholinergic effect increases the risk of developing tardive dyskinesia.

    Risperidone has no effect on the clinical effect and pharmacokinetics of lithium, valproate, digoxin and topiramate, therefore, with such combinations, dose adjustment is not required.

    Risperidone reduces the effectiveness of levodopa and other dopamine agonists. A similar effect is possible with risperidone at the same time as other drugs that induce the metabolism of microsomal enzymes of cytochrome P450, such as barbiturates, rifampicin, phenytoin and St. John's wort. In this case, the dose of risperidone should be reviewed or reduced.

    Do not use risperidone simultaneously with carbamazepine to patients with mania in bipolar disorder. When carbamazepine was used, there was a decrease in plasma concentration of AAPF in risperidone.

    Clozapine reduces the clearance of risperidone.

    Phenothiazines, tricyclic antidepressants, and some beta-blockers may increase the concentration of risperidone in plasma, but this does not affect the concentration of AAPP.

    Quinidine, fluoxetine, paroxetine, terbinafine and other isoenzyme inhibitors CYP2D6 may increase the concentration of risperidone in plasma, but to a lesser extent the concentration of AAPF.

    Carbamazepine, rifampicin, St. John's wort, phenytoin, phenobarbital are isoenzyme inducers CYP3A4 and reduce the concentration of ACE inhibitor risperidone in plasma. With the withdrawal of carbamazepine and other isoenzyme inducers CYP3A4 The dose of risperidone should be reduced.

    Verapamil, being an inhibitor CYP3A4, increases the concentration of risperidone in plasma. Cimetidine and ranitidine increase the concentration of risperidone in plasma, but the antipsychotic effect does not increase, because the adhesion of active metabolites is reduced.

    The alpha-1-adrenoceptor effect of risperidone can increase blood pressure, reducing the effectiveness of phenoxybenzamine, labetalol and other alpha-blocking sympathomimetics, reserpine, methyldopa and other antihypertensive agents of central action. In contrast, the antihypertensive effect of guanitidine is blocked.

    The attention and caution of simultaneous reception of risperidone with drugs that extend the interval QT, such as other antipsychotics, antiarrhythmics IA and III classes, moxifloxacin, methadone, mefloquine, erythromycin, tricyclic antidepressants, lithium and cisapride.

    It is necessary to be careful when taking risperidone simultaneously with drugs that can cause disturbances in electrolyte metabolism, such as thiazide diuretics (hypokalemia). This combination increases the risk of developing a malignant arrhythmia.

    When risperidone is used together with other drugs that are highly binding to plasma proteins, no clinically pronounced displacement of any active substance from the plasma protein fraction is observed.

    Special instructions:

    When schizophrenia, at the beginning of treatment with risperidone, it is recommended to gradually cancel the previous therapy, if it is clinically justified. If patients are transferred from depot therapy to APS, it is advisable to start the treatment instead of the next scheduled injection. Periodically, the need to continue current therapy with antiparkinsonian drugs should be evaluated.

    Simultaneous use of risperidone with furosemide in elderly patients with dementia was associated with high mortality. The mechanism of such interaction has no clear explanation.Nevertheless, care should be taken in such cases.

    There are no data on the efficacy and safety of risperidone in children under 18 years of age.

    Risperidone should be used with caution in elderly patients who have a history of cerebrovascular disorders. there is a risk of developing a stroke or transient ischemic attack.

    APS, including risperidone, promote the development of thromboembolic complications in patients with a predisposition to the formation of thrombi. Before starting risperidone therapy, all possible risk factors for venous thromboembolism should be identified and appropriate measures taken to prevent the development of thromboembolic complications.

    The risk of developing mania or hypomania can be significantly reduced by applying low dosages or gradually increasing them.

    When orthostatic hypotension occurs, especially in the initial period of dose selection, consideration should be given to reducing the dose. In patients with SSS, as well as with dehydration, hypovolemia or cerebrovascular disorders, the dose should be increased gradually.

    APS, including risperidone, should be used with caution in patients with congenital lengthening of the interval QT, coronary heart disease, conduction disturbance, arrhythmia or simultaneous use of medications that cause lengthening of the interval QT, as well as hypokalemia.

    If there are signs and symptoms of tardive dyskinesia / extrapyramidal symptoms, consideration should be given to the abolition of all APS.

    With the development of malignant neuroleptic syndrome (NSA), it is necessary to cancel all APS, including risperidone, and conduct symptomatic treatment. After the normalization of the condition, the doctor decides whether to resume therapy with risperidone. To prevent the development of NSA during the treatment of APS, it is necessary to regularly adjust the dose taken.

    It is necessary to carefully evaluate the ratio of potential benefit and possible risk in the use of risperidone in patients with dementia associated with corpuscles

    Levy or Parkinson's disease, since such patients may have an increased risk of developing CNS and increased sensitivity to APS.

    In patients with diabetes mellitus or the risk of developing diabetes, it is necessary to monitor the concentration of glucose in the blood.

    Patients should be advised to refrain from overeating due to the possibility of weight gain.

    In rare cases, with an increase in the dose of APS, including risperidone, symptoms of nausea, vomiting, increased sweating, and drowsiness may appear. It is necessary either to stop taking the drug before the symptoms disappear, or to reduce its dose.

    Effect on the ability to drive transp. cf. and fur:

    During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

    Form release / dosage:

    Tablets, dispersible in the oral cavity 2 mg.

    Packaging:

    For 14 tablets in a blister of OPA / Al / PVC and aluminum foil. For 2 or 4 blisters together with instructions for use in a cardboard box.

    Storage conditions:

    Store at a temperature not exceeding 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    2 years.

    Do not use after the expiry date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-001629
    Date of registration:06.04.2012
    The owner of the registration certificate:Teva Pharmaceutical Enterprises Co., Ltd.Teva Pharmaceutical Enterprises Co., Ltd. Israel
    Manufacturer: & nbsp
    Representation: & nbspTeva Teva Israel
    Information update date: & nbsp17.10.2015
    Illustrated instructions
      Instructions
      Up