Neyrispin-Zdorovye, tab. 1,0mg No. 10х2

General characteristics. Structure:

International and chemical names: risperidon, 3-[2-[4 (6-fluoro-1,2-benzisoksazol-3-silt) piperidine-1-silt] ethyl] - 2-methyl-6,7,8,9-tetrahydro-4H-»¿Ó¿ñ« [1,2] - a pyrimidine - 4 - it;
main physical and chemical properties: tablets, coated;
tablets on 0,5 mg – pink color with a nacreous shade;
on 1 mg – white color with a nacreous shade;
on 2 mg – yellowish-orange color with a nacreous shade;
on 4 mg – light green color with a nacreous shade;
structure: one tablet contains рисперидон (in terms of 100% substance) - 0,5mg; 1 mg; 2 mg; 4 mg;
excipients: lactoses monohydrate, cellulose microcrystallic, sodium of a kroskarmeloz, potato starch, polyvinylpirrolidone low-molecular, polyethyleneglycol 4000, sodium lauryl sulfate, magnesium stearate, aerosil, titanium dioxide, кандурин, a gipromeloza, dye for tablets: 0,5 mg – "Sepispers dry red And";
2 mg - "Evrosert Sunset yellow"; 4 mg - "Sepispers dry yellow R" and "Sepispers dry blue І".

Pharmacological properties:

Pharmacodynamics. Antipsychotic means. Derivative benzizoksazola, the selection monoaminergichesky antagonist. Has high affinity to serotoninovy 5-HT2 and dopamine D2 receptors, contacts also a1-adrenoceptors and, at a little smaller affinity, H1-histamine and a2-adrenoceptors. Has no affinity to holinoretseptor.
Being powerful D2 antagonist (that, is considered, is the cornerstone of the mechanism of improvement of productive symptomatology of schizophrenia), рисперидон causes less expressed suppression of motor activity and in much smaller degree induces a katalepsy, than classical neuroleptics. The balanced central antagonism of a risperidon to serotonin and dopamine reduces expressiveness of extrapyramidal side effects and expands therapeutic impact of drug on negative and affective symptoms of schizophrenia.

Pharmacokinetics. Irrespective of meal рисперидон it is completely soaked up. The maximum concentration in plasma is reached in 1 – 2 hour. Contacts proteins of plasma (albumine and an alfa1-acid glycoprotein) for 88%. It is quickly distributed, gets into TsNS fabrics, the volume of distribution makes 1 – 2 l/kg. It is metabolized in a liver with the participation of P450 IID6 isoenzyme partially with education equal on activity of the 9-gidroksirisperidon contacting proteins of plasma for 77%, partially – on the way of N-dealkylation. Equilibrium concentration of a risperidon is reached within 1 day, a 9-gidroksirisperidon – in 4 – 5 days. An elimination half-life of a risperidon – the 3rd hour, a 9-gidroksirisperidon – 24 hours. In 1 week of reception of 70% it is removed with urine,
14% – through digestive tract; 35 – 45% are excreted in the form of active agents.
At patients of advanced age and/or with a renal failure after a single dose of drug the increased concentration in plasma and the slowed-down removal of a risperidon are observed.

Indications to use:

Schizophrenia (including for the first time the arisen acute psychosis, a bad attack of schizophrenia, chronic schizophrenia); psychotic states with expressed productive (nonsense, hallucinations, disorders of thinking, hostility, suspiciousness) and/or with 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 at chronic schizophrenia; behavioural frustration at patients with dementia at manifestation of symptoms of aggression (fits of anger, physical abuse) and disturbances of mental activity (excitement, nonsense), and also at patients with a delay of intellectual development or with domination in a clinical picture of destructive tendencies; manias at bipolar disorders (as means of auxiliary therapy, as the mood stabilizer).

Route of administration and doses:

Appoint inside irrespective of meal, one or two times a day. The dosage for adults and children is more senior than 15 years:
At schizophrenia: in the first day – 2 mg, for the second day – 4 mg. Further it is possible or to keep a dose at the level of 4 mg a day, or, if necessary, individually to skoregirovat. Usually optimum dose are 4 – 6 mg a day. At use of drug in a dose more than 10 mg a day increase in efficiency is not observed, however the risk of development of extrapyramidal symptoms increases.
Elderly patients or patients with a liver or renal failure treatment should begin with a dose 0,5 mg 2 times a day with gradual increase to 1 – 2 mg 2 times a day.
Behavioural frustration at patients with dementia: an initial dose – on 0,25 mg it is possible to raise 2 times a day, if necessary a dose on 0,25 mg two times a day, but not more often than every other day. An optimum dose for most of patients – on 0,5 mg 2 times a day. Reception on 1 mg 2 times a day is shown to some patients.
Bipolar disorders at manias: an initial dose – 2 mg a day in 1 reception, if necessary a dose raise on 2 mg a day, but not more often than every other day. An optimum dose – 2 – 6 mg a day.
Behavioural frustration at patients with a delay of intellectual development or with domination in a clinical picture of destructive tendencies: patients with body weight have 50 kg and more initial dose – 0,5 mg a day in 1 reception, if necessary the dose is raised on 0,5 mg a day, but not more often than every other day. An optimum dose – 1 mg a day. Patients with body weight have less than 50 kg an initial dose – 0,25 mg a day in 1 reception, if necessary the dose is raised on 0,25 mg a day, but not more often than every other day. An optimum dose – 0,5 mg a day.
After achievement of an effective dose administration of drug can be recommended once a day.
The highest daily dose of drug – 16 mg a day.

Features of use:

At the beginning of therapy of Neyrispinom-Zdorovye it is recommended to cancel gradually the previous antipsychotic therapy if it is clinically justified. At the same time, if patients are transferred from therapy by the prolonged forms of neuroleptics, administration of drug is recommended to be begun instead of the previous drug. In an initiation of treatment, especially at selection of a dose, there can be orthostatic hypotonia therefore Neyrispin-Zdorovye with extra care and gradual increase in a dose it is necessary to apply to treatment of patients with diseases of cardiovascular system, at dehydration, a hypovolemia and cerebrovascular disturbances. When developing hypotension the dose should be reduced. Also with extra care it is necessary to use drug for treatment of patients with Parkinson's disease and epilepsy because of a possibility of deterioration in a basic disease. At emergence of symptoms of late dyskinesia, a malignant antipsychotic syndrome it is necessary to stop reception of all antipsychotic drugs, including Neyrispin-Zdorovye. Patients have to be warned about a possibility of increase in body weight.
At treatment risperidony it is necessary to refuse all types of activity demanding bystry reaction and also alcohol intake.
Use of a risperidon during pregnancy is possible only when the expected effect of therapy exceeds potential risk for a fruit. Safety and efficiency of use of a risperidon for treatment of children is studied insufficiently though now such clinical trials are conducted.

Side effects:

From the central nervous system and sense bodys: often – sleeplessness, agitation, alarm, a headache; sometimes – drowsiness, fatigue, dizziness, disturbance of concentration of attention, disturbance of clearness of sight; seldom – extrapyramidal frustration (a tremor, rigidity, a gipresalivation, a bradykinesia, an akathisia, acute dystonia), convulsive attacks, late dyskinesia, an antipsychotic malignant syndrome, thermal control disturbance are possible.
From the alimentary system: abdominal pains, dyspepsia, lock, nausea, vomiting, increase in level of liver enzymes.
From cardiovascular system and blood: seldom – orthostatic hypotension, reflex tachycardia, hypertensia, small decrease in neutrophils and/or thrombocytes, a hypervolemia, a stroke (at elderly patients with the contributing factors).
From endocrine system: a galactorrhoea, a gynecomastia, disturbances of a menstrual cycle, an amenorrhea, increase in body weight, it is rare – a hyperglycemia, an exacerbation of diabetes.
From a reproductive system: seldom – a priapism, disturbances of an erection, an ejaculation, an orgasm.
Allergic reactions: seldom – rhinitis, a Quincke's disease, skin rash.
Others: sometimes – an urine incontience.

Interaction with other medicines:

Neyrispin-Zdorovye it is necessary to apply with care along with other drugs of the central action. At combined use of a risperidon with drugs antagonists of dopamine receptors, late dyskinesia can be observed (in the form of involuntary rhythmic movements, preferential language and/or the person) that demands cancellation of all antipsychotic drugs. Risperidon can act as the antagonist of a levodopa.
Fenotiazina, tricyclic antidepressants, b-adrenoblockers, fluoxetine can increase concentration of a risperidon in blood, without influencing concentration active anti-
psychotic fraction. At combined use with carbamazepine and other inductors of liver enzymes decrease in concentration of an active antipsa is noted
hotichesky fraction of a risperidon in blood. At the termination of reception of such drugs Neyrispin's dose should be reconsidered.
In need of additional sedation along with Neyrispinom-Zdorovye it is possible to appoint benzodiazepine derivatives.

Contraindications:

Individual hypersensitivity, the lactation period, pregnancy, children's age (up to 15 years).

Overdose:

Symptoms: drowsiness, manifestation of excessive sedative action, tachycardia, arterial hypotension, extrapyramidal symptoms, in isolated cases – increase at an ECG of an interval of QT. Treatment: to provide free passability of respiratory tracts for maintenance of adequate supply with oxygen and ventilation. A gastric lavage, purpose of absorbent carbon together with laxative. Monitoring of an ECG for identification of disturbances of a cordial rhythm. The symptomatic therapy directed to maintenance of zhiznennovazhny functions of an organism. In the presence of arterial hypotension and a vascular collapse – infusional therapy and/or sympathomimetic drugs. At development of extrapyramidal frustration – purpose of anticholinergic drugs. There is no specific antidote.
Constant medical observation and monitoring should be continued before disappearance of symptoms of intoxication.

Storage conditions:

To store in the dry, protected from light place at a temperature from 15 °C to 30 °C. To store in the place, unavailable to children.
Period of validity - 2 years.

Issue conditions:

According to the recipe

Packaging:

Tablets on 0,5 mg, 1 mg, 2 mg, 4 mg No. 10х2 in blister strip packagings.
Tablets on 1 mg, 2 mg, 4 mg No. 100 in a container plastic in a box; No. 100 in a container plastic.