Риспаксол®

General characteristics. Structure:

Active ingredient: 1 mg, 2 mg or 4 mg of a risperidon.

Excipients: lactose anhydrous, starch corn, magnesium stearate, silicon dioxide colloid anhydrous, cellulose microcrystallic.

Covers: dye of Opadray orange OY-8729 (gipromelloz (gidroksipropilmetiltsellyuloz) macrogoal 400, titanium dioxide, yellow "sunset" of FCF (E110), yellow quinolinic (E104), macrogoal 6000, karnaubsky wax

Means with antipsychotic, sedative action (neuroleptic).

Pharmacological properties:

Pharmacodynamics. Antipsychotic drug (neuroleptic), derivative benzizoksazola. Renders also sedative, antiemetic and hypothermal action.

Risperidon is the selection monoaminergichesky antagonist with the expressed affinity to serotoninovy 5-HT2 and dopamine D2-retseptoram. Also рисперидон communicates with α1-адренорецепторами and, at a little smaller affinity, with histamine H1 receptors and α2-адренорецепторами. Does not possess a tropnost to holinoretseptor.
 
Antipsychotic action is caused by blockade dopamine D2 receptors of mesolimbic and mesocortical system.

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, aggression), 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 a 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 h.

Risperidon is exposed to metabolism with participation of R-450 IID6 of cytochrome with formation of a 9-gidroksirisperidon who possesses similar pharmacological action. Risperidon and 9-gidroksirisperidon represent effective antipsychotic fraction.

At intake рисперидон about 3 hours are removed with an elimination half-life. It is established that the elimination half-life of a 9-gidroksirisperidon 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 a 9-gidroksirisperidon 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 contacts albumine and and - a 1-glycoprotein. Linkng of a risperidon with proteins of plasma makes 88%, 9-gidroksirisperidona-77%.

It is brought by kidneys - 70% (out of them 35 - 45% in the form of pharmacological active fraction) and 14% - with bile. Other quantity is the share of inactive metabolites.

At patients of advanced age after a single dose of drug the increased concentration of active fraction in plasma to 30%, and at patients with a renal failure - to 60%, and also reduced clearance of antipsychotic fraction were inside observed.

Existence of a liver failure does not influence the maintenance of concentration of a risperidon in plasma, but at such patients the average number of free fraction in plasma was 35% higher.

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:

Rispaksol it is possible to accept during meal or in breaks between meals. Tablets should be washed down with a small amount of water.

At schizophrenia to adults and children 15 years drug are more senior appoint 1 or 2 times/days. An initial dose - 2 mg/days. For the second day it is necessary to increase a dose to 4 mg/days. 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/days. In some cases slower increase in a dose and lower the initial and supporting doses can be justified.

Doses higher than 10 mg/days did not show higher performance in comparison with smaller doses and can cause emergence of extrapyramidal symptoms. Because safety of doses more than 16 mg/days 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.

The initial dose on 500 mkg of 2 times/days is recommended to elderly patients. The dose can be increased individually on 500 mkg of 2 times/days to 1-2 mg of 2 times/days.

At diseases of a liver and kidneys the initial dose on 500 mkg of 2 times/days is recommended. It is gradually possible to increase this dose to 1-2 mg by reception of 2 times/days.

At abuse of medicines or medicinal dependence the recommended daily dose of drug makes 2-4 mg.

At behavioural frustration at patients with dementia the initial dose on 250 mkg of 2 times/days is recommended (it is necessary to use an adequate dosage form). If necessary it is possible to increase a dosage individually on 250 mkg 2, not more often than every other day. For most of patients an optimum dose are 500 mkg of 2 times/days. However reception on 1 mg of 2 times/days is shown to some patients.

On reaching an optimum dose administration of drug of 1 times/days can be recommended.

At a mania 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/days.

At disorders of behavior at patients with a delay of intellectual development to patients with the body weight of 50 kg and more appoint 500 mkg of 1 times/days. If necessary this dose can be raised on 500 mkg/days, not more often than every other day. For most of patients an optimum dose is the dose of 1 mg/days. However reception on 500 mkg/days whereas some need increase in a dose up to 1.5 mg/days is more preferable to some patients. To patients with body weight less than 50 kg are appointed on 250 mkg/days. If necessary this dose can be raised on 250 mkg/days, not more often than every other day. For most of patients an optimum dose is the dose of 500 mkg/days. However reception on 250 mkg/days whereas some need increase in a dose up to 750 mkg/days is more preferable to some patients.

Long reception of Risperidon 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:

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 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 protivoparkinsonichesky drugs.

Due to the alpha and adrenoceptor blocking action of a risperidon orthostatic hypotension, especially during initial selection of a dose can develop. When developing hypotension 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.

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 the KFK level it is necessary to cancel all antipsychotic medicines, including рисперидон.

At cancellation of carbamazepine and other inductors of liver 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.

Rispaksol's tablets contain lactose. This drug should not be accepted to patients with intolerance of sugars (inborn intolerance of a galactose, deficit of lactase or a sprue of a glucose/galactose).

Rispaksol can influence vigorous activity for which speed of reactions is necessary. Therefore it is not necessary to drive the car or to service mechanisms, individual portability of drug is not revealed yet.

Safety of use of a risperidon for pregnant women was not studied. At pregnancy drug can be used only if the positive effect justifies possible risk. As рисперидон and 9-gidroksirisperidon are allocated with breast milk, the women using drug should not nurse.

Side effects:

From a nervous system and sense bodys: a sleep disorder, including sleeplessness or drowsiness, hypererethism, fatigue, disturbance of attention, concern, alarm, a headache, dizziness, extrapyramidal frustration (rigidity, a hypokinesia, hypersalivation, an akathisia, acute dystonia), late dyskinesia, an antipsychotic malignant syndrome, thermal control disturbance, convulsive attacks, a stroke (at predisposed patients of advanced age), a sight illegibility.

From cardiovascular system and blood (a hemopoiesis, a hemostasis): orthostatic hypotension, reflex tachycardia, arterial hypertension, neytro-and thrombopenia, Werlhof's disease.

From bodies of a GIT: nausea, vomiting, dispeptic phenomena, abdominal pain, lock, increase in level of hepatic transaminases.

From urinogenital system: dysmenorrhea, amenorrhea, impotence, disturbance of an erection and ejaculation, anorgazmiya, decrease libido, priapism, polyuria, urine incontience, hypostases.

Allergic reactions: skin rash, Quincke's disease.

Others: rhinitis, a galactorrhoea, a gynecomastia, increase in body weight, a hypervolemia (owing to a polydipsia or a syndrome of inadequate secretion of ADG), a hyperglycemia (at patients with a diabetes mellitus).

Interaction with other medicines:

Taking into account that Rispaksol makes impact first of all on TsNS, it should be applied with care in combination with other drugs of the central action and ethanol.

Rispaksol reduces efficiency of a levodopa and other agonists of a dopamine.

Clozapine reduces clearance of a risperidon.

At simultaneous use of a rispaksol and 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.

At simultaneous use with rispaksoly fenotiazina, tricyclic antidepressants and some beta adrenoblockers can increase concentration of a risperidon in plasma, however it does not influence concentration of active antipsychotic fraction.

At simultaneous use with rispaksoly fluoxetine can increase concentration of a risperidon in plasma, however, to a lesser extent concentration of active antipsychotic fraction.

At use of a rispaksol together with other drugs highly contacting proteins of plasma, clinically expressed replacement of any drug from protein fraction of plasma is not observed.

Anti-hypertensive drugs increase expressiveness of decrease in the ABP against the background of reception of a rispaksol.

Contraindications:

- Period of a lactation (breastfeeding).
- Hypersensitivity to drug components.

With care it is necessary to appoint drug at:

- Diseases of cardiovascular system (chronic heart failure, the postponed myocardial infarction, disturbances of conductivity of a cardiac muscle).
- Dehydration and hypovolemia.
- Disturbances of cerebral circulation.
- Parkinson's diseases.
- Spasms (including in the anamnesis).
- Renal failure of heavy degree.
- Heavy liver failure.
- Abuse of medicines or medicinal dependence.
- The states contributing to development of tachycardia like "pirouette" (bradycardia, disturbance of electrolytic balance, the accompanying reception of the medicines extending QT interval).
- Tumors of a brain, intestinal impassability, cases of acute medicinal overdose, a syndrome to Reja (the antiemetic effect of a risperidon can mask symptoms of these states).
- Pregnancies (efficiency and safety are not established).
- Children's age up to 15 years (efficiency and safety are not established).

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:

Drug should be stored in protected from light, the place, unavailable to children, at a temperature not above 25 °C.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in the blister from PVC and aluminum. 2 or 6 blisters in cardboard packaging together with an inmtruktion.