РИЛЕПТИД®

General characteristics. Structure:

Active ingredient: each tablet contains 1 mg, 2 mg, 3 mg or 4 mg of active agent - a risperidon. Excipients: lactoses monohydrate, starch corn, cellulose microcrystallic, magnesium stearate, silicon dioxide colloid anhydrous, sodium lauryl sulfate. The cover of a tablet of 1 mg contains: Opadry-Y-1-7000 dye white (gipromelloza, titanium dioxide, macrogoal 400). The cover of tablets on 2, 3 and 4 mg contains: Opadry dye green (a gipromelloza, titanium dioxide, a macrogoal 400, ariavit indigo carmine an aluminum varnish, ariavit a quinolinic yellow aluminum varnish.

Description: Tablets of 1 mg: Oblong, biconvex tablets, coated, white or almost white color, with an engraving E 751 on one party and from risky - on another, without or almost inodorous. Tablets of 2 mg: Oblong, biconvex tablets, coated, light green color, with an engraving "Е 752" on one party and from risky - on another, without or almost inodorous. Tablets of 3 mg: Oblong, biconvex light green tablets, coated, with an engraving "Е 753" on one party and from risky - on another, without or almost inodorous. Tablets of 4 mg: Oblong, biconvex green tablets, coated, with an engraving "Е 754" on one party and from risky - on another, without or almost inodorous.

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 B2 receptors, contacts also with an alpha 1 adrenoceptors and at a little smaller affinity H1-gistaminergichesky and alfa2-adrenergic receptors. Antipsychotic action does not possess a tropnost to holinoretseptor B2 receptors of mesolimbic and mesocortical system are caused by blockade dopamine. 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 R-450 IID6 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:

Schizophrenia Adults and children is more senior than 15 years. Rileptid 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. Data on use 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. 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, the weighing 50 kg and more - the recommended initial dose of drug - 0.5 mg in once put. 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 some need increase in a dose up to 0,75 mg a day is more preferable to some patients. Long reception of Rileptid 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.

Features of use:

Transition from therapy by other antipsychotic drugs. At schizophrenia, in an initiation of treatment risperidony, it is recommended to cancel gradually the previous therapy if it is clinically justified. If patients are transferred from therapy of depot by forms of antipsychotic drugs, then reception of a risperidon is recommended to be begun instead of the following planned injection. Periodically it is necessary to estimate need of continuation of therapy by potivoparkinsonichesky medicines. Due to the α-adrenoceptor blocking action of Rileptid there can be orthostatic hypotonia, especially during initial selection of a dose. When developing hypotonia it is necessary to consider a question of a dose decline. At patients with diseases of cardiovascular system, and also at dehydration, a hypovolemia or cerebrovascular disturbances, the dose should be increased gradually, according to recommendations (see the Route of administration and doses). Emergence of extrapyramidal symptoms is risk factor for development of late dyskinesia. In case of signs and symptoms of late dyskinesia, it is necessary to consider a question of cancellation of all antipsychotic drugs. At emergence of the antipsychotic malignant syndrome which is characterized by a hyperthermia, muscular rigidity, instability of autonomous functions, disturbances of consciousness and increase in level of a kreatinfosfokinaza it is necessary to cancel all antipsychotic medicines, including рисперидон. At patients with schizophrenia the risk of attempts of suicide therefore treatment of patients with the increased risk of suicide has to be carried out under strict observation increases. At cancellation of carbamazepine and other inductors of "hepatic" enzymes the dose of a risperidon has to be lowered. Patients should recommend to refrain from an overeating in connection with a possibility of increase in body weight. 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.

Contraindications:

Hypersensitivity to drug components; lactation period.

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 of respiratory tracts 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 below 25 °C. In the place, unavailable to children. Period of storage 3 years. Not to use after the date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets coated 1 mg, 2 mg, 3 mg, 4 mg: on 10 pieces in the blister from the PVC/PVDH/ave a foil. 1, 2 or 6 blisters together with the instruction on a medical use in a cardboard pack.