Speridan 4

General characteristics. Structure:

Active agent: рисперидон 1/2/4 mg

Pharmacological properties:

Pharmacodynamics. 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 HP (neuroleptics). The balanced central antagonism to serotonin and dopamine can reduce tendency to extrapyramidal pobychny actions 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). 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). Other way of metabolism is N-dealkylation. T1/2 of a risperidon is 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, etc. 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. Behavioural frustration at patients with dementia at manifestation of symptoms of aggression (fits of anger, physical abuse), at activity disturbances (excitement, nonsense) or psychotic symptoms. As HP of auxiliary therapy (as the mood stabilizer) - behavioural frustration at children, teenagers 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:

Inside, adults and children are more senior than 15 years - 1 or 2 times a day. An 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. To elderly patients and at diseases of a liver and kidneys: an initial dose - 0.5 mg 2 times a day. It is possible to increase a dose individually to 1-2 mg 2 times a day. Behavioural frustration at patients with dementia: an initial dose - 0.25 mg 2 times a day. Increase in a dose - on 0:25 mg 2 times a day, not more often than every other day. An optimum dose - 0.5 mg 2 times a day (to some patients reception on 1 mg 2 times a day is shown). On reaching an optimum dose reception is possible once a day. Bipolar disorders at manias: an initial dose - 2 mg/days on 1 reception. Increase in a dose (on 2 mg/days) - not more often than every other day. An optimum dose - 2-6 mg/days. Behavioural frustration at patients with a delay of intellectual development or with domination in a clinical picture of destructive tendencies. Patients with the body weight of 50 kg and more: an initial dose - 0.5 mg once a day. Increase in a dose - on 0.5 mg/days, not more often than every other day. An optimum dose - 1 mg/days. Patients with body weight less than 50 kg: an initial dose - 0.25 mg once a day. Increase in a dose - on 0:25 mg/days, not more often than every other day. An optimum dose - 0.5 mg/days. It is recommended to reduce twice both an initial dose, and the subsequent increases in a dose at aged patients and at patients with a renal or liver failure.

Features of use:

With care. The brain tumor, intestinal impassability, overdose of HP, a syndrome to Reja (the antiemetic effect of a risperidon can mask symptoms of these states), diseases of CCC (HSN, the postponed myocardial infarction, AV blockade), dehydration, disturbance of cerebral circulation, a hypovolemia, Parkinson's disease, spasms (including in the anamnesis), abuse the HP or 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 HP extending Q-T interval), pregnancy, children's age (up to 15 years) - efficiency and safety are not established.

Side effects:

From a nervous system: sleeplessness, agitation, uneasiness, a headache, sometimes - drowsiness, increased fatigue, dizziness, decline in the ability to concentration of attention, a sight ambiguity, it is rare - extrapyramidal symptoms (a tremor, rigidity, hypersalivation, a bradykinesia, an akathisia, acute dystonia), a mania or a hypomania, a stroke (at elderly patients with the contributing factors). At patients with schizophrenia - a hypervolemia (either because of a polydipsia, or because of a syndrome of inadequate secretion of ADG), late dyskinesia (the involuntary rhythmic movements, preferential language and/or the person), a neyroleytichesky malignant syndrome (a hyperthermia, muscular rigidity, instability of autonomous functions, disturbance of consciousness and increase in the KFK level), thermal control disturbances, epileptic seizures.

From the alimentary system: locks, dyspepsia, nausea or vomiting, an abdominal pain, increase in activity of "hepatic" transaminases, dryness in a mouth, hypo - or hypersalivation, anorexia, increase or decrease in body weight.

From CCC: sometimes - orthostatic hypotension, reflex tachycardia or increase in the ABP.

From bodies of a hemopoiesis: neutropenia, thrombocytopenia.

From endocrine system: galactorrhoea, gynecomastia, disturbances of a menstrual cycle, amenorrhea, increase in body weight, hyperglycemia.

From urinogenital system: priapism, disturbances of an erection, disturbance of an ejaculation, disturbance of an orgasm, urine incontience.

Allergic reactions: rhinitis, rash, Quincke's disease, photosensitization.

From integuments: xeroderma, hyperpegmentation, itch, seborrhea. Other: arthralgia.

Interaction with other medicines:

Reduces efficiency of a levodopa, etc. dopamine agonists. Fenotiazina, tricyclic antidepressants and beta adrenoblockers increase concentration in plasma (do not influence concentration of active antipsikhotichysky 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, HP, the oppressing TsNS, - the additive oppression of the TsNS function. Hypotensive HP 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). Special instructions: 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 HP, then reception is recommended to be begun instead of the following planned injection. Periodically it is necessary to estimate need for continuation of the current therapy in protivoparkinsonichesky HP. The risk of development of a mania or hypomania can be significantly reduced when using low dosages or their gradual building. When developing orthostatic hypotension, especially in an initial stage of selection of a dose, it is necessary to consider a question of a dose decline. At patients with diseases of CCC, and also at dehydration, a hypovolemia or cerebrovascular disturbances the dose should be increased gradually. If there are signs and symptoms of late dyskinesia, it is necessary to consider a question of cancellation of all antipsychotic HP; an antipsychotic malignant syndrome - it is necessary to cancel all antipsychotic HP, including рисперидон. At carbamazepine cancellation, etc. inductors of "hepatic" 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. During treatment it is necessary to be careful during the driving of motor transport and occupation other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Contraindications:

Hypersensitivity, lactation period

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 HP. Constant medical observation and monitoring should be continued before disappearance of symptoms of intoxication.

Storage conditions:

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

Issue conditions:

According to the recipe

Packaging:

tablets coated 1, 2, 4 mg (blisters)