Torendo Ku-tab - instructions for use, dose, side effects, contraindications

Mannitol - 27.80 mg; butyl methacrylate, dimethylaminoethyl methacrylate and methyl methacrylate copolymer [1: 2: 1] - 1,50 mg, povidone-K25 - 0.10 mg, microcrystalline cellulose - 4.00 mg, low-substituted giprolase - 3.00 mg, aspartame - 0.40 mg, crospovidone - 4.00 mg, iron dye red oxide (E172) - 0.02 mg, mint flavor 0.10 mg, flavoring menthol - 0.10 mg, calcium silicate - 7.50 mg, magnesium stearate - 1.00 mg.

Tablets for resorption, 1 mg:

Active substance: Risperidone - 1.00 mg.

Excipients:

Mannitol - 55.60 mg; butyl methacrylate, dimethylaminoethyl methacrylate and methyl methacrylate copolymer [1: 2: 1] - 3.00 mg, povidone-K25 - 0.20 mg, microcrystalline cellulose - 8.00 mg, giprolose low-substituted - 6.00 mg, aspartame - 0.80 mg, crospovidone - 8.00 mg, iron dye red oxide (E172) - 0.04 mg, mint flavor - 0.20 mg, menthol flavoring - 0.20 mg, calcium silicate - 15.00 mg, calcium silicate - 15.00 mg, magnesium stearate - 2.00 mg.

Tablets for resorption, 2 mg:

Active substance: Risperidone - 2.00 mg.

Excipients:

mannitol - 111,20 mg; butyl methacrylate, dimethylaminoethyl methacrylate and methyl methacrylate copolymer [1: 2: 1] - 6,00 mg, povidone-K25 - 0,40 mg, microcrystalline cellulose - 16,00 mg, low-substituted giprolose - 12.00 mg, aspartame - 1.60 mg, crospovidone - 16,00 mg, iron dye red oxide (E172) - 0,08 mg, mint flavor - 0,40 mg, menthol flavoring - 0,40 mg, calcium silicate - 30,00 mg, magnesium stearate - 4,00 mg.

Description:

Tablets 0.5 mg, 1 mg and 2 mg:

Round, slightly biconvex tablets of light pink color with visible impregnations.

Pharmacotherapeutic group:antipsychotic agent (antipsychotic).

ATX: & nbsp

N.05.A.X Other antipsychotics

N.05.A.X.08 Risperidone

Pharmacodynamics:

Risperidone is a selective monoaminergic antagonist with a high affinity for serotonin 5-HT₂ and dopamine D2 receptors. Risperidone also binds to alpha₁-adrenoceptors and to a lesser extent with H₁-gistamines and alpha₂- adrenergic receptors. Risperidone does not have an affinity for cholinergic receptors. Although risperidone is a potent antagonist D₂-receptors and therefore eliminates the productive symptoms in schizophrenia, it causes less motor and depressive disorders and less potentiates catalepsy than classical antipsychotics. Balanced antagonism against central serotonin and dopamine receptors contributes to a decrease in the tendency to potentiate extrapyramidal disorders and expands the therapeutic the effect of the drug on the negative and productive symptoms of schizophrenia. Risperidone also has a sedative, antiemetic and hypothermic effect.

Pharmacokinetics:

Risperidone is completely absorbed after ingestion and reaches a maximum concentration in the blood plasma for 1-2 hours. Absorption does not depend on food intake, so risperidone can be taken regardless of food intake.

Risperidone is metabolized with isoenzyme CYP2D6 up to 9-hydroxy-risperidone, which has similar pharmacological activity with riceperidone. Risperidone and 9-hydroxy-risperidone form an active antipsychotic fraction. Another way of metabolizing risperidone is N-dealkylation.

After ingestion in patients with psychoses, the half-life (T_1/2) risperidoneis about 3 hours, T_1/29-hydroxy-risperidone and active antipsychotic fraction - 24h.

In most patients, the equilibrium concentration of risperidone is reached within 1 day; and the equilibrium concentration of 9-hydroxy-risperidone - within 4-5 days.

The concentration of risperidone in the blood plasma depends on the dose, and has a wide therapeutic range.

Risperidone is rapidly distributed in the body. The volume of distribution is from 1 to 2 l / kg. In plasma, 88 % risperidone (77% of this amount 9-hydroxy-risperidone) are associated with proteins (albumins and alpha₁glycoproteins).

A week after the application of risperidone, 70% of the dose is excreted by the kidneys and 14% from bile through the intestine. In the urine risperidone and 9-hydroxy-risperidone constitute 35-45% of the dose. The rest is inactive metabolites.

A study with a single application of risperidone showed that in elderly people and patients with renal insufficiency, a higher concentration of the drug in the blood plasma is achieved and its elimination is slowed. The concentration of risperidone in blood plasma in patients with liver failure remained normal.

Indications:- schizophrenia (acute and chronic) and other psychotic conditions with productive and / or negative symptoms;

- affective disorders in various mental illnesses;

- behavioral disorders in patients with dementia in the manifestation of symptoms of aggression (outbursts of anger, physical abuse), with mental disorders (excitation, delirium) or psychotic symptoms;

- as an auxiliary therapy in the treatment of mania in bipolar disorders;

- as an adjunctive therapy for behavioral disorders in adolescents with 15 years of age and in adult patients with reducedintellectual level or mental retardation, in cases where destructive behavior (aggressiveness, impulsiveness, autoaggression) is leading in the clinical picture of the disease.

Contraindications:Hypersensitivity to the components of the drug; the period of breastfeeding, mania in bipolar affective disorders in children under the age of 18 (efficacy and safety not installed), schizophrenia (acute and chronic) and other psychotic conditions with productive and / or negative symptoms in children under the age of 15; affective disorders in various mental illnesses in children under the age of 15 years.

Carefully:

-pregnancy;

- cardiovascular disease (chronic heart failure, myocardial infarction, conduction of cardiac muscle conduction);

dehydration and hypovolaemia;

- cerebral circulation disorders;

-Parkinson's disease;

- convulsions (including in the anamnesis);

severe kidney and / or liver failure;

- Drug abuse or drug dependence;

-States predisposing to the development of tachycardia such as "pirouette" (bradycardia, electrolyte imbalance, simultaneous use of drugs that extend the interval QT);

- Brain tumor, intestinal obstruction, cases of acute drug overdose, Reye's syndrome (antiemetic effect of risperidone may mask the symptoms of these conditions);

- Old age with dementia;

-application in combination with furosemide;

-thrombophlebitis;

hyperglycemia.

Pregnancy and lactation:

The safety of the use of risperidone in pregnant women has not been proven. The use of the drug Thorendo® Cou-Tab is only possible if the benefit to the mother exceeds the potential risk to the fetus.

Because the risperidone and 9-hydroxy-risperidone penetrate into breast milk, women who use the drug Torendo® Ku-tab should refrain from breastfeeding.

Dosing and Administration:

Tablets for resorption are fragile, they should not be squeezed out through the foil packaging, they can break. Open the package by gently pulling the edge of the blister foil marked with a dot, remove the tablet and immediately put it on the tongue.The tablet begins to dissolve in the mouth within seconds and can be swallowed without water. Do not mix the tablet in your mouth with food, do not bite and do not chew.

Schizophrenia (acute and chronic) and other psychotic conditions with productive and / or negative symptoms

Adults and children over 15 years of age

The drug Torendo® Cou-Tab can be used 1 or 2 times a day. The initial dose is 2 mg per day. On the second day, the dose should be increased to 4 mg per 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 per day. In some cases, a slower dose increase and lower initial and maintenance doses may be justified.

Doses above 10 mg per day did not show a higher efficacy compared with smaller doses and may cause extrapyramidal symptoms. Due to the fact that the safety of doses above 16 mg per day has not been studied, doses above this level should not be used.

Behavioral disorders in patients with dementia in the manifestation of symptoms of aggression (outbursts of anger, physical abuse).Violations of mental activity (agitation, delirium) or psychotic symptoms

The recommended initial dose of 0.25 mg 2 times a day (should use an adequate dosage form). Dosage, if necessary, can individually increase by 0.25 mg 2 times a day, not more often than every other day. For most patients, the optimal dose is 0.5 mg 2 times a day. However, some patients receive 1 mg twice daily.

When the optimal dose is reached, the drug may be recommended once a day.

Mania in bipolar disorders

The recommended initial dose is 2 mg once a day. If necessary, this dose can be increased by 2 mg per day, not more often than every other day. For most patients, the optimal dose is 2-6 mg per day.

Behavioral disorders in adolescents with 15 years of age and adults with reduced intellectual or mental retardation

Patients with a body weight of 50 kg or more - The recommended initial dose is 0.5 mg once a day. If necessary, this dose can be increased by 0.5 mg per day, not more often than every other day. For most patients, the optimal dose is a dose of 1 mg per day.However, for some patients it is preferable to take 0.5 mg per day, while some require an increase in the dose to 1.5 mg per day.

Elderly patients

The initial dose of 0.5 mg 2 times a day. Dosage can individually increase by 0.5 mg 2 times a day to 1-2 mg 2 times a day.

Children

The use of the drug Thorendo® Ku-tab in children younger than 15 years is contraindicated.

Long-term use of the drug Thorendo® Ku-tab in adolescents over the age of 15 requires constant monitoring by a physician.

Impaired renal and / or liver function

Therapy with the drug Thorendo® Ku-tab is recommended to begin with 0.5 mg 2 times a day. The dose can be gradually increased by 0.5 mg of risperidone 2 times a day to 1 - 2 mg per day. In this group of patients, Thorendo® Cu-tab should be used with caution, until more complete information is obtained.

Drug Abuse or Drug Dependence The recommended daily dose of the drug is 2-4 mg.

Patients weighing less than 50 kg - The recommended initial dose of the drug is 0.25 mg once a day. If necessary, this dose may be increased by 0.25 mg per day, not more often than every other day. For most patients, the optimal dose is 0.5 mg per day.However, for some patients it is preferable to take 0.25 mg per day, while others require an increase in the dose to 0.75 mg per day.

Side effects:

Classification of the incidence of adverse events (WHO):

very often> 1/10 (more than 10%);

often from> 1/100 to <1/10 (more than 1%, but less than 10%);

infrequently from> 1/1000 to <1/100 (more than 0.1%, but less than 1%;)

rarely from> 1/10000 to <1/1000 (more than 0.01%, but less than 0.1%)

rarely from <1/10000, including individual messages (less than 0.01%)

On the part of the hematopoiesis system:

infrequently - neutropenia, thrombocytopenia;

very rarely - anemia, eosinophilia, agranulocytosis;

From the endocrine system:

very rarely - weight gain, hyperglycemia and exacerbation of pre-existing diabetes, water intoxication due to polydipsia or inadequate syndrome secretion of antidiuretic hormone (SNSSADG);

From the nervous system:

often - agitation, anxiety, insomnia, headache, agitation;

infrequently - drowsiness, dizziness, increased fatigue, impaired concentration of attention;

rarely - extrapyramidal symptoms *, mania or hypomania, hypervolemia (due to either polydipsia or the syndrome of inappropriate ADH secretion);

very rarely - tardive dyskinesia (involuntary rhythmic movements, predominantly of the tongue and / or face), malignant neuroleptic syndrome **, seizures, epileptic seizures, thermoregulation disorders;

From the sense organs:

infrequently - visual impairment, conjunctivitis, blepharitis, dryness of the cornea, lacrimation, pain in the eyes, pain in the ears, tinnitus;

rarely - glaucoma, blurred vision;

From the cardiovascular system:

often - tachycardia (including reflex tachycardia),

infrequent - a decrease in blood pressure (including orthostatic hypotension), increased blood pressure, stroke (in elderly patients with predisposing factors), AV blockade, sinus bradycardia, thrombosis;

From the respiratory system:

often - rhinitis, cough;

infrequent - nasal congestion, sensation of perspiration in the throat, aspiration pneumonia;

rarely - nocturnal apnea, pneumonia, influenza, sinusitis, otitis media, tonsillitis;

From the digestive system:

infrequent - dryness of the oral mucosa, hyper- or hypo-salivation, constipation, dyspepsia, nausea, vomiting, abdominal pain, anorexia;

rarely - an intestinal obstruction;

From the skin:

rarely - dry skin, hyperpigmentation, rash, itching, seborrhea, angioedema, photosensitization;

From the urinary system:

often - urinary incontinence;

infrequently - cystitis;

On the part of the reproductive system:

infrequently - galactorrhea, amenorrhea, menstrual irregularities;

rarely - gynecomastia, priapism, erectile dysfunction, ejaculation disorders, anorgasmia;

From the musculoskeletal system:

often - pain in the back, pain in the limbs;

infrequently - muscle weakness, myalgia, arthralgia;

rarely - rhabdomyolysis;

Laboratory indicators:

infrequently hyperprolactinemia ***;

very rarely - hyperglycemia; increased activity of "liver" transaminases;

Other:

rarely - peripheral edema.

* Extrapyramidal symptoms: risperidone has a lower ability to cause extrapyramidal disorders than classical antipsychotics. However, in some cases, the following extrapyramidal symptoms may develop: tremor, stiffness, hypersalivation, bradykinesia, akathisia, acute dystonia. These symptoms are usually mild and reversible after lowering the dose and / or administering antiparkinsonian drugs (if necessary).

** Malignant neuroleptic syndrome (CNS): a rare, potentially dangerous condition associated with the use of antidepressants, including risperidone. Symptoms of ZNS: increased body temperature (hyperpyrexia), muscle rigidity, changes in mental status and instability of the autonomic nervous system (arrhythmia, fluctuations in blood pressure, tachycardia, profuse sweating, heart rhythm disturbance, increased activity of creatine phosphokinase (CK)).

During the application of risperidone, some cerebrovascular symptoms have been reported; they developed mainly among elderly patients with existing risk factors.

***Hyperprolactinemia: risperidone depending on the dose may cause an increase in the level of prolactin in the blood with the following possible manifestations: galakkorei, gynecomastia, menstrual cycle disorders and amenorrhea.

Overdose:

Symptoms: drowsiness, sedation, depression, tachycardia, arterial hypotension, extrapyramidal disorders, in rare cases, lengthening the interval Q-T.

Treatment: ensuring free airway patency for adequate oxygenation and ventilation; gastric lavage (after intubation, if the patient is unconscious) and the appointment of activated charcoal in combination with laxatives.

Symptomatic therapy is aimed at maintaining vital body functions.

For timely diagnosis of a possible heart rhythm disturbance, it is necessary to start ECG monitoring as soon as possible. Careful medical supervision and ECG monitoring are performed until the symptoms of intoxication disappear completely.

There is no specific antidote. With a reduction in blood pressure and vascular collapse, intravenous infusion solutions and / or adrenostimulators are recommended. In the case of development of acute extrapyramidal symptoms - anticholinergics.

Interaction:

Risperidone has an effect primarily on the central nervous system, so it should be used with caution in combination with other drugs of central action and with ethanol.

Risperidone reduces the effectiveness of levodopa and other dopamine agonists.

Clozapine reduces the clearance of risperidone.

When carbamazepine was used, it was noted decrease in concentration active antipsychotic fraction of risperidone in plasma. Similar effects can be observed with the use of other inducers of hepatic enzymes.After withdrawal of carbamazepine or other inducers of hepatic enzymes, the dose of risperidone should be Evaluate repeatedly and, if necessary, reduce. Phenothiazines, tricyclic antidepressants, and certain β-blockers may increase the concentration of risperidone in blood plasma, but this does not affect the concentration of the active antipsychotic fraction.Fluoxetine may increase the concentration of risperidone in the blood plasma and, to a lesser extent, the concentration of the active antipsychotic fraction, therefore the dosage of risperidone should be adjusted.

With the simultaneous use of risperidone and other drugs that actively bind to blood plasma proteins, there is no clinically significant displacement of drugs from the connection with plasma proteins.

Hypotensive drugs increase blood pressure lowering in the background of risperidone.

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 simultaneous use of risperidone with furosemide in elderly patients on the Background of cerebrovascular dementia was associated with high mortality.The mechanism of such interaction has no clear explanation. It is necessary to evaluate the ratio of potential benefit and possible risk for these patients with the simultaneous use of respiratory and diuretic drugs, incl. furosemide.

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.

The lowering of AD effect of guanitidine is blocked.

Attention and caution accompanying risperidone with medications that extend the interval QT, such as other APS, antiarrhythmics IA, III classes, moxifloxacin, erythromycin, methadone, mefloquine, erythromycin, tricyclic antidepressants, lithium preparations and cisapride. It is necessary to be careful with the concomitant administration of risperidone with drugs that can cause disturbances in electrolyte metabolism, such as thiazide diuretics (hypokalemia). This combination increases the risk of developing a malignant arrhythmia. Simultaneous use of ethanol and drugs that depress the central nervous system, give additive inhibition of the central nervous system.

Special instructions:

Transition from therapy with other antipsychotic drugs

When schizophrenia, at the beginning of the use of the drug Thorendo® Ku-tab, it is recommended to gradually cancel the previous therapy, if it is clinically justified. If the patient is transferred from the therapy of depot forms of antipsychotics, then the use of the drug Thorendo® KU-tab is recommended to begin instead of the next scheduled injection. Periodically, the need to continue therapy with antiparkinsonian drugs should be evaluated.

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

In connection with α-adrenoblocking action of risperidone may cause orthostatic hypotension, especially during the initial dose selection. With arterial hypotension, the question of dose reduction should be considered. In patients with diseases of the cardiovascular system, as well as in dehydration, hypovolemia or cerebrovascular disorders, the dose should be increased gradually.

The occurrence of extrapyramidal symptoms is a risk factor for the development of tardive dyskinesia. In case of signs and symptoms of tardive dyskinesia, consideration should be given to the abolition of all antipsychotics.

When identifying the NSA, it is necessary to immediately stop using the drug Thorendo® Ku-tab. With the withdrawal of carbamazepine and other inducers of "liver" enzymes, the dose of risperidone should be reduced.

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

In elderly patients with impaired liver and / or kidney function, careful dose selection and special monitoring are necessary.

Caution should be exercised in the treatment of patients with Parkinson's disease, since it is possible that the drug Thorendo® Cou-Tab can aggravate the course of this disease.

It is known that classical antipsychotics reduce the threshold of convulsive readiness. Care should be taken when treating patients with epilepsy.

Food does not affect the absorption of the drug Thorendo® Ku-tab.

Special information on excipients

The drug Torendo® Ku-Tab contains aspartame, which is a source of phenylalanine and may be harmful to people with phenylketonuria.

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

During the period of application of the preparation, the Thorendo® Cu-tab is necessary refrain from driving vehicles and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions, due to the possibility of developing dizziness, impaired concentration, and other side effects.

Form release / dosage:

Tablets for resorption, 0.5 mg, 1 mg and 2 mg.

Packaging:

10 tablets per blister of combined material OPA / Al / PVC film and PE / Al foil (Coldforming OPA/Al/PVC film and PET / Al peel off foil).

By 3 blisters in a pack of cardboard along with instructions for use.

Storage conditions:

At a temperature of no higher than 30 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LS-002602

Date of registration:21.11.2011

The owner of the registration certificate:KRKA, dd, Novo mesto, AOKRKA, dd, Novo mesto, AO

Manufacturer: & nbsp

KRKA, dd, Novo mesto, AO Slovenia

Representation: & nbspKRKA KRKA Slovenia

Information update date: & nbsp21.10.2015

Illustrated instructions

Instructions

Torendo® Ku-Tab (Torendo® Q-Tab)