Ридонекс

General characteristics. Structure:

Active agent: 1 mg, 2 mg or 4 mg of a risperidon in each tablet film coated.

Excipients:
Tablets of 1 mg:
Kernel: sodium lauryl sulfate, silicon dioxide colloid, gipromelloza, magnesium stearate, starch prezhelatinizirovanny, cellulose microcrystallic, lactoses monohydrate.
Cover: OPADRI II. yellow 85F32072 (ferrous oxide red E172, CI77491, ferrous oxide yellow E172, CI77492, titanium E171, CI77891 dioxide, talc, macrogoal, polyvinyl alcohol).
Tablets of 2 mg:
Kernel: sodium lauryl sulfate, silicon dioxide colloid, gipromelloza, magnesium stearate, starch prezhelatinizirovanny, cellulose microcrystallic, lactoses monohydrate.
Cover: OPADRI II. yellow 85F32069 (ferrous oxide red E172, CI77491, ferrous oxide yellow E172, CI77492, titanium E171, CI77891 dioxide, talc, macrogoal, polyvinyl alcohol).
Tablets of 4 mg:
Kernel: sodium lauryl sulfate, silicon dioxide colloid, gipromelloza, magnesium stearate, starch prezhelatinizirovanny, cellulose microcrystallic, lactoses monohydrate.
Cover: OPADRI II. orange 85F23450 (ferrous oxide red E172, CI77491, ferrous oxide yellow E172, CI77492, titanium E171, CI77891 dioxide, talc, macrogoal, polyvinyl alcohol).

Pharmacological properties:

Antipsychotic means (neuroleptic) derivative of a benzizoksazol; renders also sedative, antiemetic and hypothermal action. The selection monoaminergichesky antagonist, possesses a high tropnost to serotonergic 5-HT2 and dofaminergichesky D2 receptors, contacts also alfa1-adrenoceptors and at a little smaller affinity with H1-gistaminergichesky and alfa2-adrenergic receptors. 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. Suppresses productive symptomatology (nonsense, hallucinations, aggression), automatism. Causes smaller suppression of motor activity and to a lesser extent induces a katalepsy, than classical antipsychotic medicines (neuroleptics).

The balanced central antagonism to serotonin and dopamine can reduce tendency to extrapyramidal side effects and expand therapeutic influence of drug with coverage of negative and affective symptoms of schizophrenia. Can induce the increase in concentration of prolactin depending on a dose in plasma. Pharmacokinetics. Absorption - bystry and full (food does not influence completeness and speed of absorption). Time of achievement of the maximum concentration of medicine in plasma (TCmax) - 1-2 h Css of a risperidon in an organism at most of patients is reached within 1 day, 9-hydroxy-risperidona - 4-5 days. Concentration of a risperidon in plasma are proportional to a drug dose (within therapeutic doses). It is quickly distributed, gets into TsNS, breast milk. Distribution volume - 1.1 l/kg. Communication with proteins of plasma (with an alfa1-glycoprotein and albumine) a risperidona - 90%, 9-hydroxy-risperidona - 77%. CYP2D6 cytochrome to an active metabolite of 9-hydroxy-risperidona is metabolized by enzyme (рисперидон and 9-hydroxies-risperidon make active antipsychotic fraction). Some other way metabolism N-dealkylation is. An elimination half-life (T1/2) of a risperidon - 3 h, T1/2 of 9-hydroxy-risperidona and active antipsychotic fraction - 20-24 h.
It is brought by kidneys (70%, out of them - 35-45%) in the form of pharmacological active fraction) and with bile (14%).
At a single dose high levels of active concentration in plasma and slow removal at elderly patients and at patients with a renal failure are noted.

Indications to use:

Schizophrenia and other psychotic states with dominance of productive symptomatology (nonsense, hallucinations, aggression), negative symptomatology (scarcity of the speech, emotional and social detachment).
Affective frustration at various mental diseases.

Route of administration and doses:

Inside, adults and children are more senior than 15 years - 1 or 2 times a day.
- Schizophrenia
Initial dose - 2 mg/days. For the 2nd day - to 4 mg/days. From this point the dose can or be kept at the previous level, or to correct individually in need of range - 4-6 mg/days.
Doses higher than 10 mg/days did not show higher performance in comparison with smaller doses and can cause emergence of extrapyramidal symptoms.
The maximum dose - 16 mg/days.
- Bipolar disorders at manias an initial dose - 2 mg/days on 1 reception.
Increase in a dose (on 1 mg/days) - not more often than every other day. An optimum dose - 1-6 mg/days.
- Renal failure and liver
- In the presence of a disease of kidneys and a liver, irrespective of the indication, it is necessary to apply a half initial and the subsequent doses.

Features of use:

- Elderly patients with dementia.
At elderly patients, irrespective of therapy, dehydration increases risk of mortality therefore at elderly patients with dementia it is necessary to avoid liquid loss.
- Cerebrovascular side effects
Ридонекс® it is necessary to apply with extra care at treatment of behavioural frustration at patients with dementia because the risk of cerebrovascular side effects can increase (cerebrovascular complications, passing disturbance of cerebral circulation) in this connection it is reasonable to conduct a short-term course of therapy.
- Alpha and adrenoceptor blocking effect
Ридонекс®, because of alpha and adrenoceptor blocking effect - especially at the beginning of therapy, during titration of a dose - can cause orthostatic hypotension therefore there can be a need of a dose decline.
Also it is necessary to apply Ridoneks® with care in the presence of cardiovascular pathology (for example, heart failure, a myocardial infarction, conductivity disturbance, dehydration, a hypovolemia or a cerebrovascular disease. In spite of the fact that at use of a risperidon did not note lengthening of an interval of QT, it is necessary to use drug with care if the patient uses drugs to which lengthening of an interval of QT is peculiar. If the sedation caused by the drug Ridoneks® insufficient instead of increase in a dose of a risperidon, for decrease in risk of emergence of side effects it is reasonable to use other drugs, for example, benzodiazepines.
- Late dyskinesia / extrapyramidal syndrome
The drugs having antagonistic action on dopamine receptors can cause late dyskinesia of which involuntary rhythmical twitchings first of all of language and/or persons are characteristic. Emergence of extrapyramidal signs is risk of formation of late dyskinesia. If there are symptoms of late dyskinesia, it is necessary to make the decision on phase-out of all antipsychotic means.
- Malignant antipsychotic syndrome
On the course of a course of therapy by neuroleptics the malignant antipsychotic syndrome (a hyperthermia, muscle tension, autonomous (vegetative) instability, disturbance of consciousness and increase in level of a kreatinfosfokinaza (KFK), a myoglobinuria (an acute necrosis of skeletal muscles) and an acute renal failure) can develop. At emergence of these signs, it is necessary to interrupt a therapy course with antipsychotic means, including Ridoneks®, and to appoint symptomatic therapy (for example, дантролен infusion solution for in/in introductions).
- Hyperglycemia
Very seldom, at therapy risperidony noted a hyperglycemia, or an aggravation of a current of a diabetes mellitus therefore in the presence of a diabetes mellitus or with risk of development of a hyperglycemia it is necessary to control glucose level in blood.
Classical neuroleptics reduce a threshold of convulsive activity therefore it is necessary to be careful at treatment of patients with epilepsy.
For the prevention of addition in weight, it is possible to advise the patient, to control meal.
The sudden termination of reception of antipsychotic means, especially at preliminary use of high doses of drug, very seldom can make sick, vomiting, perspiration, concern, sleeplessness, resuming of psychotic symptoms or an incoordination (an akathisia, dystonia, dyskinesia) therefore gradual drug withdrawal is offered.
Like other antagonists dopamine D2 receptors, рисперидон can increase prolactin level in a blood plasma too. Patients who in the anamnesis have a malignant tumor of mammary glands or prolactin - a dependent tumor need to consider it at purpose of a risperidon.
There is no sufficient experience in use of a risperidon for patients with schizophrenia more young than 15 years.
Because the tablets Ridoneks® contain lactoses monohydrate, drug cannot be used at seldom met hereditary intolerance of a galactose, a lactose intolerance or a sprue of a glucose/galactose.

Effect of drug on ability of driving of transport and for work with mechanisms with the increased risk of traumatism
It is necessary to abstain during treatment for occupations potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

Risperidon is usually had well. In some cases side effects cannot be distinguished from signs of a basic disease.
On systems of bodies and for emergence frequency (it is very frequent: ≥1/10; often: ≥1/100 - <1/10; not often: ≥1/1000 - <1/100; seldom: ≥1/10 000 - <1/1000; very seldom: <1/10 000) side effects of a risperidon can be the following:
- From a nervous system: very often: headache, extrapyramidal symptoms (tremor, rigidity, hypersalivation, bradykinesia, akathisia, acute dystonia); often: dizziness, drowsiness, sight ambiguity; not often: decline in the ability to concentration of attention, increased fatigue; very seldom: sleeplessness, a mania or a hypomania, uneasiness, agitation, a stroke (at elderly patients with the contributing factors).
At patients with schizophrenia - it is not frequent: a hypervolemia (either because of a polydipsia, or because of a syndrome of inadequate secretion of antidiuretic hormone), late dyskinesia (the involuntary rhythmic movements, preferential language and/or the person); seldom: antipsychotic malignant syndrome (hyperthermia, muscular rigidity, instability of autonomous functions, disturbance of consciousness and increase in level of a kreatinfosfokinaza), thermal control disturbances; there are no data on the frequency of developing of epileptic seizures.
- From the alimentary system: often: nausea or vomiting, dyspepsia, dryness in a mouth, locks, an abdominal pain, it is not frequent: increase in activity of "hepatic" transaminases, hypo - or hypersalivation, anorexia, increase or decrease in body weight.
- From cardiovascular system: often: reflex tachycardia, it is not frequent: orthostatic hypotension or increase in the arterial pressure (AP).
- From bodies of a hemopoiesis: seldom: neutropenia, thrombocytopenia.
- From endocrine system: not often: a galactorrhoea, disturbances of a menstrual cycle, an amenorrhea, increase in body weight, it is rare: gynecomastia; very seldom: hyperglycemia.
- From urinogenital system: often: disturbances of an erection, priapism; not often: disturbances of an ejaculation, disturbance of an orgasm, urine incontience.
- Allergic reactions: often: rhinitis, rash; not often: Quincke's disease, photosensitization.
- From integuments: not often: itch xeroderma, hyperpegmentation, seborrhea.
- Other: often: arthralgia.
Sharp cancellation of antipsychotic means can lead to emergence of signs of cancellation (see the section "Special instructions).

Interaction with other medicines:

Reduces efficiency of a levodopa and other agonists of dopamine.
Fenotiazina, tricyclic antidepressants and beta adrenoblockers increase concentration in plasma (do not influence concentration of active antipsychotic fraction).
Fluoxetine can increase concentration of a risperidon in plasma, but to a lesser extent - concentration of active antipsychotic fraction.
At a concomitant use of carbamazepine, etc. inductors of "hepatic" enzymes decrease in concentration of active antipsychotic fraction in plasma is noted.
Clozapine reduces clearance of a risperidon.
Ethanol, medicines, the oppressing TsNS - the additive oppression of the TsNS function.
Hypotensive medicines increase expressiveness of decrease in the ABP against the background of a risperidon.
Fluoxetine can increase concentration of a risperidon in plasma (to a lesser extent active antipsychotic fraction).
To be careful at simultaneous use of Ridoneks® and furosemide since elderly patients with dementia have a combined use of furosemide and a risperidon increases risk of mortality.
The mechanism of interaction of these two active ingredients is unknown.
At combined use of other diuretics (especially tiazid in small doses) and the risperidon of this phenomenon was not noted.

Contraindications:

Hypersensitivity to any of drug components, the lactation period, children's age up to 15 years (efficiency and safety are not established).

With care.
Brain tumor, intestinal impassability, overdose by medicines, a syndrome to Reja (the antiemetic effect of a risperidon can mask symptoms of these states), diseases of cardiovascular system (chronic heart failure, the postponed myocardial infarction, an atrioventricular block), dehydration, disturbance of cerebral circulation, a hypovolemia, Parkinson's disease, spasms (including in the anamnesis), abuse of medicines or the medicinal dependence, a heavy renal/liver failure, states contributing to development of tachycardia like "pirouette" (bradycardia, disturbance of electrolytic balance, the accompanying reception of the medicines extending Q-T interval), pregnancy.
Ридонекс® it is necessary to apply with care in the presence of diseases of kidneys and a liver.

Pregnancy and period of a lactation.
Pregnancy
Clinical trials on studying of safety of a risperidon at pregnancy at the person were not conducted. In tests for animals, рисперидон did not show direct reproductive toxicity, observed several indirect deviations connected with TsNS and the level of prolactin. In one of researches did not reveal teratogenic effect of a risperidon. Thus, it is possible to Ridoneks® to apply at pregnancy only if the expected advantage of therapy for mother exceeds potential risk for a fruit.
Lactation
It is proved that рисперидон and 9-hydroxies-risperidon are emitted in maternal milk therefore during feeding by a breast it is necessary to avoid drug use.

Overdose:

Symptoms:
Drowsiness, sedation, tachycardia, decrease in the ABP, extrapyramidal frustration, it is rare - lengthening of an interval of Q-T.
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 - in/in to enter infusion solutions and/or adrenostimulyator. In case of development of acute extrapyramidal symptoms - anticholinergic medicines. Constant medical observation and monitoring should be continued before disappearance of symptoms of intoxication.

Storage conditions:

List B.
To store at a temperature not above 25 °C.
To store in the place, unavailable to children!

Issue conditions:

According to the recipe

Packaging:

Tablets film coated on 1 mg, 2 mg and 4 mg.
On 10 tablets film coated in the blister from PVC / ПВДХ-плёнки and aluminum foil. 2 blisters in a cardboard pack with the application instruction.