Leptinorm

General characteristics. Structure:

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

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:

Schizophrenia (acute and chronic) and other psychotic states with dominance productive (nonsense, hallucinations, aggression), negative (the dulled affect, emotional and social detachment, scarcity of the speech) or affective (an alarming depression) symptoms; behavioural frustration against the background of dementia (at emergence of symptoms of aggression, disturbances of activity or psychotic symptoms) or delays of intellectual development or reduced I.Q. (at domination of destructive behavior); a mania at bipolar disorders (auxiliary therapy).

Route of administration and doses:

Inside, in 1–2 receptions. Initial and optimum doses: at schizophrenia and bipolar disorder — 2 mg/days and 2–6 mg/days respectively, at disorders of behavior on 0,25 mg and 0,5 mg 2 times a day, at elderly patients and against the background of diseases of a liver and kidneys on 0,5 mg and 1–2 mg 2 times a day respectively.

Features of use:

Use during pregnancy. 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 development of late dyskinesia it is necessary to consider the possibility of cancellation of a risperidon, and at manifestation of an antipsychotic malignant syndrome (a hyperthermia, muscle tension, consciousness disturbance, increase in level of a kreatinfosfokinaza) to stop treatment. It is not necessary to apply in operating time to drivers of vehicles and people whose work is connected with the increased concentration of attention and demands speed of motor reactions.

During therapy it is necessary to avoid alcohol intake. Upon transition to treatment risperidony it is necessary to cancel other antipsychotic means whenever possible previously. With care to combine with other means influencing TsNS. During treatment it is recommended to abstain from an overeating in connection with a possibility of increase in body weight.

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:

Reduces effect of a levodopa and other agonists of dopamine. Fenotiazina, tricyclic antidepressants, fluoxetine and beta adrenoblockers can increase concentration of a risperidon in plasma.

At simultaneous use with carbamazepine, other inductors of liver enzymes (including. The hp, metabolized with participation of enzymes of P450 cytochrome) decreases concentration of active antipsychotic fraction (рисперидон and an active metabolite) in a blood plasma (correction of its dose in case of cancellation of these HP is required).

At prolonged use of carbamazepine removal of a risperidon amplifies, at long reception of clozapine — decreases.

Benzodiazepines, alcohol and means, the TsNS overwhelming functions, strengthen sedative action, antagonists of dopamine receptors increase risk of development of late dyskinesia.

At a concomitant use of anti-hypertensive means strengthening of hypotensive effect of a risperidon is possible.

Contraindications:

Hypersensitivity.

Overdose:

Symptoms: strengthening of sedative action, drowsiness, tachycardia, arterial hypotension, extrapyramidal frustration, lengthening of an interval of QT.

Treatment: gastric lavage, reception of absorbent carbon, purgatives, maintenance of passability of respiratory tracts, monitoring of an ECG, symptomatic and maintenance therapy, constant medical observation. At emergence of extrapyramidal symptoms — introduction of anticholinergics.

Storage conditions:

List B. To store at a temperature not above 25 °C. A period of validity - 24 months.

Issue conditions:

According to the recipe

Packaging:

- tablets, film coated 2 mg; blister 10 pack cardboard 2;
- tablets, film coated 2 mg; blister 10 pack cardboard 3;
- tablets, film coated 4 mg; blister 10 pack cardboard 3;
- tablets, film coated 4 mg; blister 10 pack cardboard 2.