Торендо® Ku-tab

General characteristics. Structure:

Active ingredient: 0,5 mg, 1,0 mg or 2,0 mg of a risperidon.

Excipients: Mannitolum, butylmethacrylate, dimethylaminoethylmethacrylate and a metilmetarilat (1:2:1), K-25 povidone, cellulose microcrystallic, a hypro rod (hydras of an oksa the cellulose low-replaced LH-21), aspartame, кросповидон, dye ferrous oxide red (Е 172 spent on drink), fragrance mint, fragrance menthol, calcium silicate, magnesium stearate.

The antipsychotic means rendering also sedative, antiemetic and hypothermal action.

Pharmacological properties:

Pharmacodynamics. Risperidon is antipsychotic means, renders also sedative, antiemetic and hypothermal action. Risperidon is the selection monoaminergichesky antagonist with the expressed affinity to serotonergic 5-HT2 and dofaminergichesky D2 receptors, contacts also with an alpha 1 adrenoceptors and at a little smaller affinity H1-gistaminergichesky and alfa2-adrenergic receptors. Does not possess a tropnost to holinoretseptor

Antipsychotic action is caused by blockade dopamine D2 receptors of mesolimbic and mesocortical system.

Sedative action is caused by blockade of adrenoceptors of a reticular formation of a trunk of a brain; antiemetic action - blockade dopamine D2 receptors of a trigger zone of the emetic center; hypothermal action - blockade of dopamine receptors of a hypothalamus.
Reduces productive symptomatology (nonsense, hallucinations), automatism. Causes smaller suppression of motor activity and to a lesser extent induces a katalepsy, than classical anti-psychotics (neuroleptics).

The balanced central antagonism to serotonin and dopamine can reduce risk of emergence of extrapyramidal symptomatology.

Risperidon can cause dozozavisimy increase in concentration of prolactin in plasma.

Pharmacokinetics. At intake рисперидон it is completely soaked up (irrespective of meal) and the maximum levels of concentration in a blood plasma are observed in 1-2 hours. Risperidon is exposed to metabolism with participation of P4502D6 of cytochrome with formation of 9-hydroxy-risperidona which possesses similar pharmacological action. Risperidon and 9-hydroxies-risperidon represent effective antipsychotic fraction. Further metabolism of a risperidon consists in N-dealkylation. At intake рисперидон about 3 hours are removed with an elimination half-life. It is established that the elimination half-life of 9-hydroxy-risperidona and active antipsychotic fraction makes 24 hours.

At most of patients equilibrium concentration of a risperidon is observed in one day after an initiation of treatment. The equilibrium condition of 9-hydroxy-risperidona is in most cases reached in 3-4 days after an initiation of treatment.

Concentration of a risperidon in plasma is proportional to a drug dose (within therapeutic doses).

Risperidon is quickly distributed in an organism. The volume of distribution makes 1-2 l/kg. In plasma рисперидон it is connected with albumine and acid alpha 1 - a glycoprotein. The fraction of a risperidon which is connected by protein of plasma makes 88% and 77%, respectively, in case of 9-hydroxy-risperidona.

Also 14% with bile are brought by kidneys of-70% (out of them 35-45% in the form of pharmacological active fraction). At a single dose high levels of active concentration in plasma and slow removal at elderly patients and patients with insufficient function of kidneys are noted.

Indications to use:

• schizophrenia (acute and chronic) and other psychotic states with productive and/or negative symptomatology;
• affective frustration at various mental diseases;
• behavioural frustration at patients with dementia at manifestation of symptoms of aggression (fits of anger, physical abuse), at disturbances of mental activity (excitement, nonsense) or psychotic symptoms;
• as auxiliary therapy at treatment of manias at bipolar disorders;
• as auxiliary therapy of disorders of behavior at teenagers since 15 years and adult patients with the reduced intellectual level or a delay of intellectual development, in cases if the destructive behavior (aggression, impulsiveness, an autoaggression) is the leader in a clinical picture of a disease.

Route of administration and doses:

Торендо® Ku-tab for a rassasyvaniye brittle, they should not be squeezed out through a packaging foil since they can break. Packaging is opened, having carefully pulled for the edge of a foil of the blister noted by a point and take a tablet, then it should be put immediately on language. The tablet begins to resolve in a mouth within seconds and can be swallowed without water. The tablet should not be got to the core or chewed.

Schizophrenia. Adults and children are more senior than 15 years. Risperidon can be appointed one or two times a day. An initial dose - 2 mg a day. For the second day it is necessary to increase a dose to 4 mg a day. From this point the dose can or be kept at the previous level, or to correct individually if necessary. Usually optimum dose are 4-6 mg a day. In some cases slower increase in a dose and lower initial and maintenance doses can be justified.

Doses higher than 10 mg a day did not show higher performance in comparison with smaller doses and can cause emergence of extrapyramidal symptoms. Because safety of doses higher than 16 mg a day was not studied, doses are higher than this level it is impossible to apply.

Data on use of drug for treatment of schizophrenia at children are younger than 15 years are absent.

Elderly patients. The initial dose of 0.5 mg on reception twice a day is recommended. It is possible to increase a dosage individually on 0.5 mg twice a day to 1-2 mg twice a day.

Diseases of a liver and kidneys. The initial dose of 0.5 mg on reception 2 times a day is recommended. It is gradually possible to increase this dose to 1-2 mg by reception twice a day.

Abuse of medicines or medicinal dependence - the recommended daily dose of drug - 2-4 mg.

Behavioural frustration at patients with dementia. The initial dose on 0,25 mg on reception twice a day is recommended (it is necessary to use an adequate dosage form). If necessary it is possible to increase a dosage individually on 0:25 mg 2 times a day, not more often than every other day. For most of patients an optimum dose are 0,5 mg twice a day. However reception on 1 mg 2 times a day is shown to some patients.

On reaching an optimum dose administration of drug can be recommended once a day.

Manias at bipolar disorders. The recommended initial dose of drug - 2 mg a day at one time. If necessary this dose can be raised on 2 mg a day, not more often than every other day. For most of patients an optimum dose are 2-6 mg a day. Disorders of behavior at patients with a delay of intellectual development.

Patients, and more - the recommended initial dose of drug — 0.5 mg in once put the weighing 50 kg. If necessary this dose can be raised on 0,5 mg a day, not more often than every other day. For most of patients an optimum dose is the dose of 1 mg a day. However reception on 0,5 mg a day whereas some need increase in a dose up to 1,5 mg a day is more preferable to some patients.

Patients, the weighing less than 50 kg - the Recommended initial dose of drug - once put 0.25 mg. If necessary this dose can be raised on 0,25 mg a day, not more often than every other day. For most of patients an optimum dose is the dose of 0,5 mg a day. However reception on 0,25 mg a day whereas others need increase in a dose up to 0,75 mg a day is more preferable to some patients.

Long reception of Torendo® of Ku-tab at teenagers has to be carried out under constant control of the doctor.

Use for children is younger than 15 years it is not recommended. Hypersensitivity to drug components; the lactation period, children's age up to 15 years (efficiency and safety are not established).

Features of use:

With care appoint:

• Pregnancy
• Diseases of cardiovascular system (chronic heart failure, the postponed myocardial infarction, disturbances of conductivity of a cardiac muscle)
• dehydration and hypovolemia
• disturbances of cerebral circulation
• Parkinson's disease
• spasms (including in the anamnesis)
• heavy renal or liver failure
• abuse of medicines or medicinal dependence
• the states contributing to development of tachycardia like "pirouette" (bradycardia, disturbance of electrolytic balance, the accompanying reception of the medicines extending QT interval)
• a brain tumor, intestinal impassability, cases of acute overdose of drugs, a syndrome to Reja (the antiemetic effect of a risperidon can mask symptoms of these states)
• Advanced age with dementia
• Use in combination with furosemide
• Thrombophlebitis
• Hyperglycemia

Safety of a risperidon at pregnant women was not studied. At pregnancy it is possible to use only if the positive effect justifies possible risk.

As рисперидон and 9-hydroxies-risperidon get into breast milk, the women using drug should not nurse.

During treatment it is necessary to refrain from occupations potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions and also from alcohol intake.

Side effects:

From a nervous system: sleeplessness, agitation, alarm, a headache, sometimes — drowsiness, increased fatigue, dizziness, disturbance of concentration of attention, a sight ambiguity, it is rare - extrapyramidal symptoms (a tremor, rigidity, hypersalivation, a bradykinesia, an akathisia, acute dystonia), a mania or a hypomania, a stroke (at elderly patients with the contributing factors), and also a hypervolemia (either because of a polydipsia, or because of a syndrome of inadequate secretion of antidiuretic hormone), late dyskinesia (the involuntary rhythmic movements preferential of language and/or persons), an antipsychotic malignant syndrome (a hyperthermia, muscular rigidity, instability of autonomous functions, disturbance of consciousness and increase in level of a kreatinfosfokinaza), disturbances of thermal control and epileptic seizures.

From the alimentary system: locks, dyspepsia, nausea or vomiting, an abdominal pain, increase in activity of "hepatic" transaminases, dryness in a mouth, hypo - or hypersalivation, anorexia and/or strengthening of appetite, increase or decrease in body weight.

  From   cardiovascular  system:   sometimes  orthostatic  hypotension, reflex tachycardia or increase in arterial pressure. From bodies of a hemopoiesis: neutropenia, thrombocytopenia.

From endocrine system: a galactorrhoea, a gynecomastia, disturbance of a menstrual cycle, an amenorrhea, increase in body weight, a hyperglycemia and an aggravation of the diabetes mellitus existing earlier.

From urinogenital system: priapism, disturbances of an erection, disturbance of an ejaculation, anorgazmiya, urine incontience.

Allergic reactions: rhinitis, rash, Quincke's disease, photosensitization.

From integuments: xeroderma, hyperpegmentation, itch, seborrhea. Other: arthralgia.

Interaction with other medicines:

Taking into account that рисперидон has effect first of all on the central nervous system, it should be applied with care in combination with other drugs of the central action and with alcohol.

Risperidon reduces efficiency of a levodopa and other agonists of dopamine. Clozapine reduces clearance of a risperidon.

When using carbamazepine decrease in concentration of active antipsychotic fraction of a risperidon in plasma was noted. Similar effects can be observed when using other inductors of liver enzymes. Fenotiazina, tricyclic antidepressants and some β-adrenoblockers can increase concentration of a risperidon in plasma, however it does not influence concentration of active antipsychotic fraction.

Fluoxetine can increase concentration of a risperidon in plasma, however to a lesser extent - concentration of active antipsychotic fraction therefore doses of a risperidon should be adjusted.

At use of a risperidon together with other drugs highly contacting proteins of plasma, clinically expressed replacement of any drug from protein fraction of plasma is not observed.

Hypotensive medicines increase expressiveness of a lowering of arterial pressure against the background of a risperidon.

Cimetidinum and ranitidine increase concentration of a risperidon in plasma, but the antipsychotic effect at the same time does not increase because coupling of active metabolites is reduced.

Simultaneous use of a risperidon with furosemide at elderly patients against the background of cerebrovascular dementia was associated with high mortality.

The mechanism of such interaction has no accurate explanation. It is necessary to estimate a ratio of potential advantage and possible risk for these patients at simultaneous use of a risperidon and duiretichesky means, including furosemide.

Risperidon can increase the ABP, reducing efficiency of phenoxybenzamine, a labetalol and other alpha blocking sympathomimetics, Reserpinum, Methyldopums and other antihypertensives of the central deytstviye.

The effect of a guanitidin lowering the ABP is blocked.

The accompanying reception of a risperidon with the medicines extending QT interval such as other FPÖ, antiarrhytmic means of IA, III classes, moxifloxacin, erythromycin, methadone, мефлоквин, tricyclic antidepressants, drugs of lithium and цисаприд requires attention and care. It is necessary to be careful at the accompanying reception of a risperidon with medicines which can cause disturbances of electrolytic exchange, such as thiazide diuretics (hypopotassemia). Such combination increases risk of development of malignant arrhythmia.

Simultaneous use of ethanol and means, the oppressing TsNS, give the additive oppression of function of the central nervous system.

Contraindications:

Hypersensitivity to drug components; the period of breastfeeding, a mania at bipolar affective disorders at children aged up to 18 years (efficiency and safety are not established), schizophrenia (acute and chronic) and other psychotic states with productive and/or negative symptomatology at children aged up to 15 years; affective frustration at various mental diseases at children aged up to 15 years.

Overdose:

Symptoms: drowsiness, sedation, consciousness oppression, tachycardia, arterial hypotension, extrapyramidal frustration, in rare instances lengthening of an interval of QT. Treatment: it is necessary to provide free passability respiratory путьй for ensuring adequate oxygenation and ventilation, a gastric lavage (after an intubation if the unconscious patient) and purpose of absorbent carbon in a combination to purgatives. The symptomatic therapy directed to maintenance of the vital functions of an organism.

For timely diagnosing of possible disturbances of a heart rhythm it is necessary to begin monitoring of an ECG as soon as possible. Careful medical observation and an ECG carry out monitoring to total disappearance of symptoms of intoxication. The specific antidote is absent.

Storage conditions:

To store at a temperature no more than 30 °C. To store in    the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets for a rassasyvaniye on 0,5 mg, 1 mg and 2 mg. On 10 tablets in the blister from the combined material OOPS / PVC a film and PE / Is scarlet / Is scarlet a foil (Coldforming OPA/AL/PVC film and PET/AL peel off foil). On 3 blisters in a pack cardboard together with the application instruction.