Rezalen

General characteristics. Structure:

Active agent: рисперидон 1 mg

Excipients: lactoses мононогидрат - 36,5 mg, starch prezhelatinizirovanny

- 9,0 mg, cellulose microcrystallic - 50,0 mg, sodium lauryl sulfate - 1,5 mg, silicon dioxide colloid - 1,0 mg, magnesium stearate - 1,0 mg, опадрай white 20H 58983 - 2,500 mg (a gipromelloza - 1,540 mg, titanium dioxide - 0,370 mg, is sawn through glycol - 0,308 mg, a hypro rod of-0,154 mg, talc - 0,128 mg).

Tablets film coated 2 mg:

Each tablet film coated contains

Active agent: рисперидон 2 mg

Excipients: lactoses мононогидрат - 73,0 mg, starch prezhelatinizirovanny - 18,0 mg, cellulose microcrystallic - 100,0 mg, sodium lauryl sulfate - 3,0 mg, silicon dioxide colloid - 2,0 mg, magnesium stearate - 2,0 mg, опадрай orange II 31G 53291 - 5,000 mg (a gipromelloza - 1,700 mg, lactoses monohydrate - 1,200 mg, titanium dioxide - 1,176 mg, a macrogoal - 4000 - 0,450 mg, a macrogoal - 400 - 0,250 mg, dye a sunset of yellow-0,024 mg).

Tablets film coated Zmg: 
Each tablet film coated contains
 Active agent: рисперидон 3 mg
Excipients: lactoses мононогидрат - 109,5 mg, starch prezhelatinizirovanny - 27,0 mg, cellulose microcrystallic - 150,0 mg, sodium lauryl sulfate - 4,5 mg, silicon dioxide colloid - 3,0 mg, magnesium stearate - 3,0 mg, опадрай yellow II 31G 52408 - 7,500 mg (a gipromelloza - 2,550 mg, lactoses monohydrate - 1,800 mg, titanium dioxide - 1,620 mg, a macrogoal - 4000 - 0,675 mg, a macrogoal - 400 - 0,300 mg, dye of quinolinic yellow-0,180 mg, talc - 0,375 mg).

Tablets film coated 4 mg:

Each tablet film coated contains

Active agent:
рисперидон 4 mg

Excipients: lactoses мононогидрат - 146,0 mg, starch prezhelatinizirovanny - 36,0 mg, cellulose microcrystallic - 200,0 mg, sodium lauryl sulfate - 6,0 mg, silicon dioxide colloid - 4,0 mg, magnesium stearate - 4,0 mg, опадрай green II 31G 51195 - 10,00 mg (a gipromelloza - 3,400 mg, lactoses monohydrate - 2,400 mg, titanium dioxide - 2,058 mg, a macrogoal - 4000 - 0,900 mg, a macrogoal - 400 - 0,400 mg, dye quinolinic yellow - 0,282 mg, talc - 0,500 mg, indigo carmine - 0,060 mg).

Description

Rezalen of a tablet film coated 1 mg

Tablets of a kapsulovidny form, film coated white color, from a dividing tablet, risky from two parties, and an engraving of "RSN" and "1" on one of the parties of a tablet on both sides from dividing risks. A type of tablets on a break: the homogeneous pressed mass from white till almost white color.
Rezalen of a tablet film coated 2 mg

Tablets of a kapsulovidny form, film coated light orange color, from a dividing tablet, risky from two parties, and an engraving of "RSN" and "2" on one of the parties of a tablet on both sides from dividing risks. A type of tablets on a break: the homogeneous pressed mass from white till almost white color.
Rezalen of a tablet film coated 3 mg

Tablets of a kapsulovidny form, film coated yellow color, from a dividing tablet, risky from two parties, and an engraving of "RSN" and "3" on one of the parties of a tablet on both sides from dividing risks. A type of tablets on a break: the homogeneous pressed mass from white till almost white color.
Rezalen of a tablet film coated 4 mg

Tablets of a kapsulovidny form, film coated light green color, from a dividing tablet, risky from two parties, and an engraving of "RSN" and "4" on one of the parties of a tablet on both sides from dividing risks. A type of tablets on a break: the homogeneous pressed mass from white till almost white color.

Pharmacological properties:

Pharmacodynamics. Antipsychotic means (neuroleptic) derivative of a benzizoksazol. Has high affinity to serotoninovy 5-HT2-and to dopamine 02 receptors. Contacts cti-adrenoceptors and, at a little smaller affinity, histamine N] - and ag-adrenoceptors. Has no affinity to holinoretseptor. Though рисперидон is powerful Eg-antagonistom (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 digestive tract, the maximum concentration in plasma is reached within 1-2 h. Food does not exert impact on absorption of a risperidon.

Equilibrium concentration of a risperidon in an organism at most of patients is reached within 1 day. Ravnovesky concentration 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, the volume of distribution makes 1-2 l/kg. In plasma рисперидон also the alpha contacts albumine! glycoprotein. Linkng of a risperidon with proteins of plasma makes 88%, a 9-gidroksirisperidon - 77%. Risperidon is metabolized in a liver with the participation of an isoenzyme of CYP2D6 of system of P450 cytochrome 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 the elimination half-life of a risperidon makes 3 h. The elimination half-life of a 9-gidroksirisperidon and active antipsychotic fraction makes 24 h.

In 1 week of reception of 70% 14% - through digestive tract are removed by kidneys. In urine the summary contents of a risperidon and 9-gidroksirisperidon makes 35-45%". Other quantity is the share of inactive metabolites.

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), at disturbances of mental activity (excitement, nonsense) or at 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 0,5-2 mg a day, for the second day - 4 mg a day. 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 a day. Appointing drug Rezalen whose possibility of the smallest dosing in this dosage form makes 0,5 mg, it is necessary to consider that 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 0,5 mg two times a day is recommended. If necessary it is possible to increase a dose to 1-2 mg two times a day.

Maximum dose: at use of a risperidon in a dose more than 10 mg a day 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 a day is not studied therefore further exceeding of a dose is inadmissible.

At purpose of drug patients of advanced age should consider that they can be more sensitive to effect of drug owing to the slowed-down metabolism.

Features of use:

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 a malignant antipsychotic syndrome it is necessary to cancel all antipsychotic means, including рисперидон.

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.

At use of a risperidon for elderly patients with dementia (average age of 85 years, range of 73-97 years) it must be kept in mind risk of the increased mortality owing to increase in disturbances of cerebral circulation.

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.

Side effects:

Frequency of this or that side effect is defined by means of the following table:

         Frequency                            Emergence of side effects
          often:                                 at 1-10 patients from 100
          sometimes:                               less, than at 1 patient from 100
          seldom:                                 less, than at 1 patient from 1 000
          very seldom:                       less, than at 1 patient from 10 000
          in some cases:           less than 0,01%

From a nervous system: 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, a malignant antipsychotic syndrome, 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: priarpizm, disturbances of an erection, disturbance of an ejaculation, disturbance of an orgasm.

From cardiovascular system: seldom - орто static 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. Other: urine incontience. Pregnancy and lactation
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.

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 (3-adreno locators 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;
- lactation period;
- children's age up to 18 years;
- a lactose intolerance (is a part of drug).

Overdose:

Symptoms: drowsiness, sedation, tachycardia, a lowering of arterial pressure (ABP), extrapyramidal frustration, it is rare - lengthening of an interval of QT on an ECG.

Treatment: to provide free passability of respiratory tracts for ensuring adequate supply with oxygen and ventilation, a gastric lavage (after an intubation if the unconscious patient) and purpose of absorbent carbon together with laxative. To immediately begin monitoring of an ECG for detection of possible arrhythmias. There is no specific antidote. It is necessary to carry out the symptomatic therapy directed to maintenance of the vital functions of an organism. At decrease in the ABP and a vascular collapse - intravenously to enter infusion solutions and/or adrenostimulyator. In case of development of acute extrapyramidal symptoms - purpose of anticholinergic medicines. Constant medical observation and monitoring should be continued before disappearance of symptoms of intoxication.

Storage conditions:

In the dry place at a temperature not above 25 °C. To store in the place, unavailable to children. Period of validity 2 years. Not to use after expiry date.

Issue conditions:

According to the recipe

Packaging:

Tablets film coated 1 mg, 2 mg, 3 mg, 4 mg. 10 tablets in the blister from the aluminum foil covered with a film from PVH/PVDH. 2, 3 or 6 blisters with the application instruction in a cardboard pack.