Risperidon Organika

General characteristics. Structure:

Active ingredient: 2 mg or 4 mg of a risperidon.

Excipients: starch corn prezhelatinizirovanny (starch 1500); silicon dioxide colloid (aerosil); stearate magnesium monohydrate; stearic acid; MKTs; Opadry II white (polyvinyl alcohol, talc, macrogoal (polyethyleneglycol), titanium dioxide.

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

Pharmacological properties:

Pharmacodynamics. Antipsychotic means (neuroleptic) derivative of a benzizoksazol. Has high affinity to serotoninovy 5-HT2-and dopamine D2 receptors. Communicates with α1-адренорецепторами and, at a little smaller affinity, with histamine H1 receptors and α2-адренорецепторами. Has no affinity to holinoretseptor. Though рисперидон is powerful D2 antagonist (that as it is considered, is the main mechanism of improvement of productive symptomatology of schizophrenia), it causes less expressed suppression of motor activity and to a lesser extent induces a katalepsy, than classical neuroleptics. Thanks to the balanced antagonism to serotoninovy and dopamine receptors in TsNS, the probability of development of extrapyramidal side effects decreases.

Risperidon can induce dozozavisimy increase in concentration of prolactin in a blood plasma.

Pharmacokinetics. After intake рисперидон it is completely absorbed from a GIT, Cmax in plasma is reached within 1-2 h. Food does not exert impact on absorption of a risperidon.

Css of a risperidon in an organism at most of patients is reached within 1 day. Css of a 9-gidroksirisperidon is reached within 4-5 days. Concentration of a risperidon in plasma are proportional to a dose (in the range of therapeutic doses).

Risperidon is quickly distributed in an organism, Vd makes 1-2 l/kg. In plasma рисперидон contacts albumine and alfa1 a glycoprotein. Linkng of a risperidon with proteins of plasma makes 88%, a 9-gidroksirisperidon - for 77%.

Risperidon is metabolized in a liver with the participation of CYP2D6 isoenzyme with formation of a 9-gidroksirisperidon who possesses pharmacological action similar to a risperidon. Antipsychotic action is caused by pharmacological activity of a risperidon and 9-gidroksirisperidon. Some other way metabolism of a risperidon N-dealkylation is.

After intake at patients with psychosis of T1/2 of a risperidon makes of plasma the 3rd p. T1/2 of a 9-gidroksirisperidon and active antipsychotic fraction makes 24 h.

In 1 week of reception of 70% 14% - with a stake are removed with urine. In urine the summary contents of a risperidon and 9-gidroksirisperidon makes 35-45%. Other quantity is the share of inactive metabolites.

At patients of advanced age and at patients with a renal failure after a single dose the increased concentration in plasma and the slowed-down removal of a risperidon were inside observed.

Indications to use:

Treatment of schizophrenia (including for the first time the arisen acute psychosis, a bad attack of schizophrenia, chronic schizophrenia); psychotic states with expressed productive (hallucinations, nonsense, disorders of thinking, hostility, suspiciousness) and/or negative (the dulled affect, emotional and social detachment, scarcity of the speech) symptomatology; for reduction of affective symptomatology (a depression, sense of guilt, alarm) at patients with schizophrenia; prevention of a recurrence (acute psychotic states) at the chronic course of schizophrenia; treatment of behavioural frustration at patients with dementia at manifestation of symptoms of aggression (fits of anger, physical abuse), disturbances of mental activity (excitement, nonsense) or psychotic symptoms; treatment of manias at bipolar disorders (as the mood stabilizer as means of auxiliary therapy).

Route of administration and doses:

Individual. At intake the initial dose for adults makes 0.25-2 mg/days, for the 2nd day - 4 mg/days. Further the dose can or be kept at the previous level, or, if necessary, to correct. Usually optimum therapeutic dose, depending on indications, is in range of 0.5-6 mg/days. In some cases slower increase in a dose and lower the initial and supporting doses can be justified.

At schizophrenia for patients of advanced age, and also at associated diseases of a liver and kidneys the initial dose on 500 mkg of 2 times/days is recommended. If necessary it is possible to increase a dose to 1-2 mg of 2 times/days.

Maximum dose: at use of a risperidon in a dose more than 10 mg/days are not observed increases in efficiency in comparison with smaller doses, but the risk of development of extrapyramidal symptoms increases. Safety of use of a risperidon in doses more than 16 mg/days is not studied therefore further exceeding of a dose is not allowed.

Features of use:

With care to apply at patients with diseases of cardiovascular system (including at heart failure, a myocardial infarction, disturbances of conductivity of a cardiac muscle), and also at dehydration, a hypovolemia or cerebrovascular disturbances. At this category of patients the dose should be increased gradually.

The risk of development of orthostatic hypotension is especially increased in an initial stage of selection of a dose. When developing hypotension it is necessary to consider a question of a dose decline.

At use of the drugs having properties of antagonists of dopamine receptors developing of the late dyskinesia which is characterized by the involuntary rhythmic movements was noted (preferential language and/or the person). There are messages that emergence of extrapyramidal symptoms is risk factor for development of late dyskinesia. Risperidon causes emergence of extrapyramidal symptoms to a lesser extent, than classical neuroleptics. At emergence of symptoms of late dyskinesia it is necessary to consider a question of cancellation of all antipsychotic means.

In case of development of ZNS it is necessary to cancel all antipsychotic means, including рисперидон.

With care it is necessary to apply рисперидон at patients with Parkinson's disease as deterioration in this disease is theoretically possible.

It is known that classical neuroleptics reduce a threshold of convulsive readiness. Considering it, рисперидон it is recommended to apply with care at patients with epilepsy.

Risperidon it is necessary to apply with care in combination with other drugs of the central action.

At cancellation of carbamazepine and other inductors of liver enzymes the dose of a risperidon should be reconsidered and, if necessary, to reduce.

During treatment patients should recommend to abstain from an overeating in connection with a possibility of increase in body weight.

Data on safety of use of a risperidon for children aged up to 15 years are absent.

Influence on ability to driving of motor transport and to control of mechanisms. During treatment, before clarification of individual sensitivity to a risperidon, patients should avoid driving of motor transport and other activity demanding high concentration of attention and speed of psychomotor reactions.

Use at pregnancy is possible if the expected advantage of therapy for mother surpasses potential risk for a fruit. In need of use in the period of a lactation breastfeeding should be stopped.

At schizophrenia at associated diseases of a liver the initial dose on 500 mkg of 2 times/days is recommended. If necessary it is possible to increase a dose to 1-2 mg of 2 times/days.

Use at renal failures. At schizophrenia at associated diseases of kidneys the initial dose on 500 mkg of 2 times/days is recommended. If necessary it is possible to increase a dose to 1-2 mg of 2 times/days.

Use for children. Data on safety of use of a risperidon for children aged up to 15 years are absent.

Use for elderly patients. At schizophrenia for patients of advanced age the initial dose on 500 mkg of 2 times/days is recommended. If necessary it is possible to increase a dose to 1-2 mg of 2 times/days.

Side effects:

From TsNS: often - sleeplessness, agitation, alarm, a headache; are possible - drowsiness, fatigue, dizziness, disturbance of ability to concentration of attention, disturbance of clearness of sight; seldom - extrapyramidal symptoms, (including a tremor, rigidity, hypersalivation, a bradykinesia, an akathisia, acute dystonia). At patients with schizophrenia late dyskinesia, ZNS, disturbances of thermal control and convulsive attacks are possible.

From the alimentary system: lock, dispeptic phenomena, nausea, vomiting, abdominal pains, increase in activity of liver enzymes.

From a reproductive system: priapism, disturbances of an erection, disturbance of an ejaculation, disturbance of an orgasm.

From cardiovascular system: seldom - orthostatic hypotension and reflex tachycardia, arterial hypertension.

From endocrine system: galactorrhoea, gynecomastia, disturbances of a menstrual cycle, amenorrhea, increase in body weight.

From system of a hemopoiesis: small decrease in quantity of neutrophils and/or thrombocytes.

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

Others: urine incontience.

Interaction with other medicines:

At simultaneous use of inductors of microsomal enzymes of a liver reduction of concentration of a risperidon in a blood plasma is possible.

At simultaneous use with derivatives of a fenotiazin, tricyclic antidepressants and beta adrenoblockers increase in concentration of a risperidon in a blood plasma is possible.

At simultaneous use with carbamazepine concentration of a risperidon in a blood plasma considerably decreases.

At simultaneous use рисперидон reduces effects of a levodopa and other agonists of dopamine receptors.

At simultaneous use with fluoxetine increase in concentration of a risperidon in a blood plasma is possible.

Contraindications:

Hypersensitivity to a risperidon.

Storage conditions:

To store in the place protected from light, at a temperature not over 25 ºС. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

10 pieces - planimetric strip packagings (2) of a film of the polyvinyl chloride and printing aluminum foil varnished - a pack cardboard.
10 pieces - planimetric strip packagings (3) of a film of the polyvinyl chloride and printing aluminum foil varnished - a pack cardboard.
10 pieces - planimetric strip packagings (5) of a film of the polyvinyl chloride and printing aluminum foil varnished - a pack cardboard.
10 pieces - planimetric strip packagings (6) of a film of the polyvinyl chloride and printing aluminum foil varnished - a pack cardboard.
20 pieces - banks (1) of light-protective glass - a pack cardboard.
30 pieces - banks (1) of light-protective glass - a pack cardboard.
50 pieces - banks (1) of light-protective glass - a pack cardboard.
60 pieces - banks (1) of light-protective glass - a pack cardboard.