Risperidon

General characteristics. Structure:

Active agent: 1 mg of a risperidon.

Auxiliary granules of a veshchestva:laktoz, the talc purified of magnesium stearate, sodium glikolit starch, a gidroksipropilmetiltsellyuloz, titanium dioxide, polyethyleneglycol 6000, propylene glycol.

The drug used for treatment of depressions, schizophrenia and other mental disorders.

Pharmacological properties:

Pharmacodynamics. Antipsychotic drug, derivative benzizoksazola. Risperidon is the selection monoaminergicheeky antagonist. Possesses high аффинно­стью to serotoninovy 5-HT2-and dopamine D2 receptors. Communicates with α1-adrenoceptors and at a little smaller affinity with α2-адренорецепторами and H1 histamine. Has no affinity to holinoretseptor. Risperidon is powerful D2 antagonist, but causes smaller suppression of a motor aktivyonost, to a lesser extent induces a katalepyosiya, than classical neuroleptics. The balanced antagonism to serotoninovy and dopamine receptors in TsNS reduces probability of development of extrapyramidal side effects, promotes expansion of therapeutic effect of drug, including negative and affective symptoms of schizophrenia.     

Risperidon can induce dozozavisimy increase in concentration of prolactin in a blood plasma.

Pharmacokinetics. Absorption. After intake рисперидон it is completely absorbed from a GIT. Smakh in plasma is reached during 1-2 h. Food does not exert impact on drug absorption therefore Risperidon it is possible to accept irrespective of meal.

Raspedeleniye. Risperidon is quickly distributed in an organism, _Vd makes 1-2 l/kg. Risperidon for 88% contacts proteins of plasma, 9-hydroxy-risperidon - for 77% is preferential with albumine and _{an alfa1-glycoprotein}.

_{Sssrisperidona} in an organism at most of patients it is reached within 1 day.

_{Sss9-gidroksi-risperidona} it is reached within 4-5 days. Concentration of a risperidon in plasma are proportional to a drug dose (within therapeutic doses).

Metabolism. Risperidon is metabolized in a liver with the participation of CYP2D6 isoenzyme with formation of 9-hydroxy-risperidona which possesses pharmacological action similar to a risperidon. Risperidon and 9-hydroxies-risperidon make active antipsychotic fraction. Some other way metabolism of a risperidon N-dealkylation is.

Removal. After intake at patients with psychosis of T1/2 of a risperidon makes of plasma the 3rd p. T1/2 of 9-hydroxy-risperidona and active antipsychotic fraction makes 24 h. In a week of administration of drug of 70% of a dose 14% - with a stake are removed with urine. In urine рисперидон and 9-hydroxies-risperidon make 35-45% of a dose. Other quantity is made by inactive metabolites.

Pharmacokinetics in special clinical cases. At patients of advanced age and at patients with a renal failure after a single dose of drug higher concentration in plasma and the slowed-down removal of a risperidon were inside observed.

At patients with a liver failure of concentration of a risperidon in plasma were left without changes.

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 (hallucinations, nonsense, disorders of thinking, hostility, suspiciousness) and/or negative (the dulled affect, emotional and social detachment, scarcity of the speech) symptomatology;

- affective symptomatology (a depression, sense of guilt, alarm) at patients with schizophrenia

at various mental states;

- behavioural frustration at patients with dementia, at manifestation of symptoms of aggression (fits of anger, physical abuse), disturbances of psikhicheyosky activity (excitement, nonsense) or psychotic symptoms.

As medicine of auxiliary therapy (as the mood stabilizer), behavioural frustration at teenagers since 15 years and adult patients with intellectual level below an average or a delay of intellectual development, in cases if the destructive behavior (aggression, impulsiveness, an autoaggression) is the leader in a clinical picture of a disease.

Route of administration and doses:

In a schizophrenia initiation of treatment Risperidon it is necessary to cancel gradually administration of drugs, preceding Risperidon if it is clinically justified. At the same time if patients are transferred from therapy of depot forms of antipsychotic drugs, then therapy by Risperidon is recommended to be begun instead of the following planned injection. Periodically it is necessary to estimate need for continuation of the current therapy by protivoparkinsonichesky drugs.

To adults and children 15 years are more senior. Risperidon it is possible to appoint 1 or 2 times a day. The initial dose of drug makes 2 mg/days. For the second day it is necessary to increase a dose to 4 mg a day. Then the dose is kept at the previous level or individually selected. Usually optimum dose are 4-6 mg a day. Sometimes perhaps slower increase in a dose and lower the initial and supporting doses. At 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 ekstrayopiramidny symptoms increases. As safety of use of drug in doses more than 16 mg a day is not studied, this dose cannot be exceeded. In need of additional sedation along with Risperidon it is possible to appoint benzodiazepine derivatives.

Patients have a pozhilogovozrasta and at patients with renal and hepatic недостаточно­стью an initial dose and the subsequent, it is necessary to reduce twice.

At diseases of a liver and kidneys it is recommended to begin with 500 mkg 2 times a day. It is possible to increase this dose to 1-2 mg 2 times a day. At behavioural frustration at patients with dementia the initial dose on 250 mkg 2 times a day is recommended. If necessary it is possible to increase a dose on 250 mkg 2 times a day, but not a bowl than every other day. For most of patients an optimum dose are 500 mkg 2 times a day, in certain cases — on 1 mg of 2 times/days.

The initial dose on 500 mkg 2 times a day is recommended to patients of advanced age. If necessary it is possible to increase a dose to 1-2 mg 2 times a day.

Children are younger than 15 years – data on use of a risperidon for treatment of schizophrenia are absent.

Features of use:

Due to the alpha and adrenoceptor blocking action of Risperidon there can be orthostatic hypotension, especially during initial selection of a dose. When developing arterial 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.

There are messages that emergence of extrapyramidal symptoms is risk factor for development of late dyskinesia. Risperidon causes emergence of extrapyramidal symptoms, than classical neuroleptics less often. If there are signs and symptoms of late dyskinesia, it is necessary to consider a question of cancellation of all antipsychotic drugs.

In case of development of the malignant antipsychotic syndrome which is characterized by a hyperthermia, muscular rigidity, instability of vegetative functions, disturbances of consciousness and increase in the KFK level it is necessary to cancel all antipsychotic drugs, including Risperidon.

At cancellation of carbamazepine and other inductors of liver enzymes Risperidon's dose has to be lowered.

Patients during treatment by Risperidon should recommend to refrain from an overeating in connection with a possibility of increase in body weight.

Influence on ability to driving of motor transport and to control of mechanisms: During treatment patients should avoid driving of motor transport and other activity demanding high concentration of attention and speed of reactions.

Pregnancy and lactation. Safety of use of drug of Risperidon at pregnancy at the person is not studied. Risperidon it is possible to appoint at pregnancy only if the expected advantage of therapy for mother exceeds potential risk for a fruit.

Side effects:

Risperidon is usually well had by patients.  

From TsNS: often - sleeplessness, agitation, alarm, a headache; sometimes - drowsiness, fatigue, dizziness, disturbance of concentration of attention, disturbance of clearness of sight; seldom - extrapyramidal symptoms (including a tremor, rigidity, hypersalivation, a bradykinesia, an akathisia, acute dystonia). These symptoms are usually poorly expressed and reversible at a dose decline and/or appointment (in need of) protivoparkinsonichesky drugs.

At patients with schizophrenia late dyskinesia, the malignant neyrolepticheyosky syndrome (MNS), disturbances of a termoregulyayotion and convulsive attacks are possible.

From the alimentary system: sometimes — a lock, dyspepsia, nausea and/or vomiting, abdominal pains, and increase in activity of pechenochyony enzymes.

From urinogenital system: sometimes — a priapism, disturbance of an erection, disturbance of an ejaculation, an anoorgazmiya, an urine incontience.

From cardiovascular system: seldom – orthostatic hypotension and reflektoryony tachycardia, arterial hypertension. Against the background of therapy risperidony development of strokes, generally at elderly patients with the contributing factors is described.

From endocrine system: the galactorrhoea, a gynecomastia, disturbances of a menstrual cycle, an amenorrhea, increase in a masyosa of a body are possible.

From system of a hemopoiesis: perhaps small decrease in quantity of neutrophils and/or thrombocytes.

Allergic reactions: sometimes – rhinitis, skin rash, a Quincke's disease.

Interaction with other medicines:

Risperidon can act as the antagonist of a levodopa and agonists of a dopamine.

At simultaneous use of carbamazepine decrease in concentration of aktivyony antipsychotic fraction of a risperidon in plasma was noted. Similar effects can be observed also at use of other inductors of liver enzymes. At cancellation of carbamazepine and other inductors of liver enzymes Risperidon's dose should be reconsidered and if necessary, to reduce.

Fenotiazina, tricyclic antidepressants and some beta adrenoblockers can increase concentration of a risperidon in a plazyoma, however it does not influence concentration of active antipsychotic fraction.

Fluoxetine can increase concentration of a risperndon in plasma, however, to a lesser extent concentration of active aitipsikhotichesky fraction.

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

Contraindications:

- Hypersensitivity to Risperidon and other components of drug;

- Lactation (breastfeeding).

With care it is necessary to use drug at patients with diseases of cardiovascular system (including at chronic heart failure, the postponed myocardial infarction, conductivity disturbances), at dehydration, a hypovolemia, disturbance of cerebral circulation, Parkinson's disease, spasms (including in the anamnesis), a heavy renal or liver failure, at abuse of medicines or medicinal dependence, at the states contributing to development of tachycardia like "pirouette" (bradycardia, disturbance of electrolytic balance, the accompanying reception of the medicines extending QT interval) at tumors of a brain, intestinal impassability, in cases of acute overdose of drugs, at a syndrome to Reja (since the antiemetic effect of a risperidon can mask symptoms of these states), patients aged up to 15 years (since safety and efficiency of use of drug are not established).

Overdose:

Symptoms: drowsiness, manifestations of sedative action, tachycardia, arterial hypotension, extrapyramidal symptoms; in rare instances - increase in an interval of QT.

Treatment: to provide free passability of respiratory tracts for maintenance of adequate ventilation of the lungs. A gastric lavage (after an intubation, if the unconscious patient) and purpose of absorbent carbon together with laxative. It is necessary to begin immediately monitoring of an ECG for identification of possible disturbances of a cordial rhythm. The specific antidote is unknown. The symptomatic therapy directed to maintenance of vitally vazhyony functions of an organism is carried out. At arterial hypotension and a vascular collapse it is necessary to vvoyodit intravenously infusion solutions and/or to use sympathomimetic drugs. At acute extrapyramidal symptoms anticholinergic prepayorata are appointed. Constant medical observation and monitoring should be continued before disappearance of symptoms of intoxication.

Storage conditions:

In the place protected from moisture and light at a temperature not over +25 ºС. To store in the place, unavailable to children! Period of validity 3 years.

Issue conditions:

According to the recipe

Packaging:

On 20, 40 or 60 tablets in polymeric banks, in a pack together with a leaf insert.