Торендо®

General characteristics. Structure:

Active ingredient: 1,0 mg, 2,0 mg, 3,0 mg or 4,0 mg of a risperidon.

Excipient: tsellaktoza, cellulose microcrystallic, croscarmellose sodium, silicon dioxide colloid, anhydrous, sodium lauryl sulfate, magnesium stearate. Cover: опадрай 03H28785 white - mix (a gipromelloza, titanium dioxide, talc, propylene glycol), ferrous oxide yellow (Е 172), ferrous oxide red (Е 172), quinolinic yellow (Е 104), indigo carmine (Е 132).

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

Pharmacological properties:

Pharmacodynamics. Risperidon is the selection monoaminergichesky antagonist, has high affinity to serotoninovy 5-HT2 and dopamine D2 receptors. Risperidon also contacts alfa1-adrenoceptors and to a lesser extent H1 - histamine and alfa2-adrenoceptors. Risperidon has no affinity to holinoretseptor. Though рисперидон is a powerful antagonist of D2 receptors and therefore eliminates productive symptomatology at schizophrenia, it causes less than motive and depressive disturbances and to a lesser extent exponentiates a katalepsy, than classical neuroleptics. The balanced antagonism concerning the central serotoninovy and dopamine receptors reduces probability of development of extrapyramidal disturbances and increases the therapeutic width of drug concerning influence on negative and productive symptomatology of schizophrenia. Besides, рисперидон has sedative, antiemetic and hypothermal effect.

Pharmacokinetics. Risperidon is completely soaked up after intake and reaches makismalny concentration in a blood plasma during 1-2 h. Absorption does not depend on meal therefore рисперидон it is possible to accept regardless of meal. The maximum concentration of the main metabolite of 9-hydroxy-risperidona is reached to 3 h after administration of drug at patients with intensive metabolism and to 17 h at patients with low intensity of metabolism. Equilibrium concentration of a risperidon at patients with intensive metabolism is reached by the end of the first days of reception of a risperidon and approximately by 5 days at patients with low intensity of metabolism.

Risperidon, as well as the majority of neuroleptics, antidepressants, antiarrhytmic means, is metabolized in a liver with participation of an isoenzyme of CYP2D6. The main metabolite – 9-hydroxy-risperidon which has similar pharmacological activity with risperidony. Risperidon and 9-hydroxies-risperidon form active antipsychotic fraction. About 6-8% of Europeans concern to persons with low activity of CYP2D6. Another, significantly less significant, by metabolism of a risperidon N-dealkylation is.

After intake at patients with psychoses the elimination half-life (T1/2) of a risperidon makes about 3 h, T1/2 of 9-hydroxy-risperidona and active antipsychotic fraction – 24 h.

Concentration of a risperidon in a blood plasma depends on a dose and has broad therapeutic range.

Risperidon is quickly distributed in an organism. The volume of distribution makes from 1 to 2 l/kg. In plasma of 88% of a risperidon (77% of this quantity are presented to 9-hydroxy-risperidonom) are connected with proteins (albumine and alfa1-glycoproteins).

In a week after use of a risperidon of 70% of a dose also 14% - with bile, through intestines are removed by kidneys. In urine рисперидон and 9-hydroxies-risperidon make 35-45% about the accepted dose. Other part – inactive metabolites.

The research with single use of a risperidon showed that at elderly people and patients with a renal failure higher concentration of drug in a blood plasma is reached and its removal is slowed down. Patients with the expressed renal failure have a total clearance of a risperidon and its metabolites decreases by 60% in comparison with healthy volunteers. Concentration of a risperidon in a blood plasma at patients with a liver failure does not differ from that at volunteers.

Indications to use:

• schizophrenia (acute and chronic) and other psychotic states with productive and/or negative symptomatology;
• 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:

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 the initial and supporting 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.

Behavioural frustration at patients with dementia. At inefficiency of medicinal doses of a risperidon to 1 mg (other dosage forms of a risperidon), reception on 1 mg 2 times in days of the drug Torendo® is shown to some patients.

On reaching an optimum dose administration of drug in a dose of 1 mg of 1 times a day can be recommended.

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. For most of patients an optimum dose is the dose of 1 mg a day.

Elderly patients. For performing initial therapy use of low doses of a risperidon to 1 mg (other dosage forms of a risperidon) is recommended. Further it is possible to increase a dosage individually to 1-2 mg 2 times in days of the drug Torendo®.

Children. Use of the drug Torendo® for children is younger than 15 years contraindicated.

Prolonged use of the drug Torendo® at teenagers is more senior than 15 years demands constant control of the doctor.

Renal failure and/or liver. For performing initial therapy use of low doses of a risperidon to 1 mg (other dosage forms of a risperidon) is recommended. Further it is possible to increase a dosage individually to 1 mg 2 times in days of the drug Torendo®.

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

Features of use:

With care appoint to the following group of patients:

• 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 and/or liver failure;
• abuse of medicines or medicinal dependence;
• the states contributing to development of tachycardia like "pirouette" (bradycardia, disturbance of electrolytic balance, simultaneous use of the medicines extending QT interval);
• advanced age with dementia;
• use in combination with furosemide;
• thrombophlebitis;
• hyperglycemia;
• a brain tumor, intestinal impassability, cases of acute overdose of HP, a syndrome to Reja (the proitivorvotny effect of a risperidon can mask symptoms of these states).

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 use of the drug Torendo® it is necessary to refrain from control of vehicles and occupation potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions in connection with a possibility of development of dizziness, disturbance of concentration of attention, etc. side effects.

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 kooyuny covers: 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 r-adreno locators 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.

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), a galactosemia, deficit of lactase, a syndrome of glyukozo-galaktozny malabsorption, children's age 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:

At a temperature not above 30 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets, film coated, 1, 2, 3 or 4 mg. On 10 tablets in the blister. On 2, 3 or 6 blisters in a cardboard pack together with the application instruction.