Active substanceRisperidoneRisperidone
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  • Dosage form: & nbspTfilm-covered abeys.
    Composition:

    Active substance: 1 mg, 2 mg or 4 mg of risperidone in each film-coated tablet.

    Excipients:

    Tablets 1 mg:

    Core: sodium lauryl sulfate, silicon dioxide colloid, hypromellose, magnesium stearate, pregelatinized starch, microcrystalline cellulose, lactose monohydrate.

    Sheath: ODPADRI II. yellow 85F32072 (iron oxide red E172, CI 77491, iron oxide yellow E172, CI 77492, titanium dioxide E171, CI 77891, talc, macrogol, polyvinyl alcohol).

    Tablets 2 mg:

    Core: sodium lauryl sulfate, silicon dioxide colloid, hypromellose, magnesium stearate, pregelatinized starch, microcrystalline cellulose, lactose monohydrate.

    Sheath: ODPADRI II. yellow 85F32069 (iron oxide red E172, O 77491, iron oxide yellow E172, CI 77492, titanium dioxide E171, CI 77891, talc, macrogol, polyvinyl alcohol).

    Tablets 4 mg:

    Core: sodium lauryl sulfate, silicon dioxide colloid, hypromellose, magnesium stearate, pregelatinized starch, microcrystalline cellulose, lactose monohydrate.

    Shell: ODPADRI II. orange 85F23450 (iron oxide red E172, CI 77491, iron oxide yellow E172, CI 77492, titanium dioxide E171, CI 77891, talc, macrogol, polyvinyl alcohol).

    Description:

    Tablets 1 mg

    Yellow, round, biconvex tablets, film-coated with engraving N04 on one side of the tablet.

    Tablets 2 mg

    Brownish-yellow, round, biconvex tablets, covered with a film sheath, with engraving N05 on one side of the tablet.

    Tablets 4 mg

    Light brown, round, biconvex tablets, covered with a film sheath, with engraving N07 on one side of the tablet.

    Pharmacotherapeutic group:antipsychotic agent (antipsychotic)
    ATX: & nbsp

    N.05.A.X   Other antipsychotics

    N.05.A.X.08   Risperidone

    Pharmacodynamics:Antipsychotic agent (antipsychotic), benzisoxazole derivative; also has a sedative, antiemetic and hypothermic effect.
    Selective monoaminergic antagonist, has a high tropism for serotonergic 5-HT2 and dopaminergic D2receptors, also binds to alpha1-adrenoceptors and with slightly less affinity for H1-gistaminergic and alpha2-adrenergic receptors. Has no tropism for cholinergic receptors.
    Antipsychotic effect due to blockade of dopamine H2receptors of the mesolimbic and mesocortical system.
    Sedative action is due to blockade of adrenoreceptors of the reticular formation of the brainstem; antiemetic effect - blockade of dopamine D2-receptors of the trigger zone of the vomiting center; hypothermic action - blockade of dopamine receptors of the hypothalamus.
    Suppresses productive symptoms (delirium, hallucinations, aggressiveness), automatism.
    It causes less inhibition of motor activity and to a lesser degree induces catalepsy than classical antipsychotic drugs (antipsychotics).
    A balanced central antagonism to serotonin and dopamine can reduce the propensity to extrapyramidal side effects and extend the therapeutic effect of the drug to cover the negative and affective symptoms of schizophrenia.
    Can induce a dose-dependent increase in prolactin concentration in plasma.
    Pharmacokinetics:

    Absorption is fast and complete (food does not affect the completeness and absorption rate). Time to reach the maximum concentration of the drug in the plasma (TCmOh) - 1-2 hours. Css risperidone in the body in most patients is achieved within 1 day, 9-hydroxy-risperidone - 4-5 days. The concentrations of risperidone in plasma are proportional to the dose of the drug (within therapeutic doses). Quickly distributed, penetrates into the central nervous system, breast milk. The volume of distribution is 1.1 l / kg. The connection with plasma proteins (with alpha 1-glycoprotein and albumin) risperidone - 90%, 9-hydroxy-risperidone - 77%.

    Metabolized by cytochrome enzyme CYP2D6 to the active metabolite of 9-hydroxy-risperidone (risperidone and 9-hydroxy-risperidone constitute the active antipsychotic fraction). Another way of metabolism is N-dealkylation. The half-life (T1/2) risperidone - 3 h, T1/2 9-hydroxy-risperidone and active antipsychotic fraction - 20-24 h.

    It is excreted by the kidneys (70%, of them - 35-45% in the form of a pharmacologically active fraction) and with bile (14%).

    With a single admission, high levels of active plasma concentrations and slow excretion in elderly patients and in patients with renal insufficiency are noted.

    Indications:

    Schizophrenia and other psychotic conditions with a predominance of productive symptoms (delirium, hallucinations, aggressiveness), negative symptoms (poor speech, emotional and social detachment).

    Affective disorders in various mental illnesses.

    Contraindications:

    Hypersensitivity to any of the components of the drug, lactation period, children under 15 years of age (efficacy and safety not established).

    Carefully:

    Tumor of the brain, intestinal obstruction, drug overdose,Reye syndrome (antiemetic effect of risperidone may mask the symptoms of these conditions), diseases of the cardiovascular system (chronic heart failure, suffered myocardial infarction, atrioventricular blockade), dehydration, cerebral circulation, hypovolemia, Parkinson's disease, convulsions (incl. in the anamnesis), drug abuse or drug dependence, severe renal / hepatic insufficiency, conditions predisposing to the development of tachycardia such as pirouette (brady ardiya, electrolyte imbalance, concomitant drugs, prolonging the interval Q-T), pregnancy.

    Ridonex® should be used with caution in the presence of kidney and liver diseases.

    Pregnancy and lactation:

    Pregnancy

    Clinical studies to study the safety of risperidone during pregnancy in humans have not been conducted. In animal tests risperidone did not show direct reproductive toxicity, several indirect deviations associated with the central nervous system and prolactin level were observed. None of the studies revealed a teratogenic effect of risperidone.Thus, Ridonex® can be used during pregnancy only if the expected benefit of therapy for the mother exceeds the potential risk to the fetus.

    Lactation

    It is proved that risperidone and 9-hydroxy-risperidrenn are excreted in the mother's milk, so during the breast-feeding should avoid the use of the drug.

    Dosing and Administration:

    Inside, adults and children over 15 years of age - 1 or 2 times a day.

    Schizophrenia

    The initial dose is 2 mg / day. On day 2 - up to 4 mg / day. From this moment, the dose can either be kept at the same level, or individually adjusted if necessary in the range of 4-6 mg / day.

    Doses above 10 mg / day did not show a higher efficacy compared with smaller doses and could cause extrapyramidal symptoms. The maximum dose is 16 mg / day.

    Bipolar disorders in mania: the initial dose is 2 mg / day for 1 dose. Increase the dose (by 1 mg / day) - not more often than every other day. The optimal dose is 1-6 mg / day.

    Impaired renal and hepatic function

    In the presence of kidney and liver disease, regardless of the indication, it is necessary to apply half of the initial and subsequent doses.
    Side effects:

    Risperidone is usually well tolerated. In some cases, side effects can not be distinguished from the signs of the underlying disease.

    According to organ systems and frequency of occurrence (very often: ≥1 / 10; often: ≥1 / 100 - <1/10; infrequent: ≥1 / 1000 - <1/100; rarely: ≥1 / 10 000 - <1 / 1000; very rarely: <1/10 000).

    Side effects of risperidone may be as follows:

    From the nervous system: very often: headache, extrapyramidal symptoms (tremor, rigidity, hypersalivation, bradykinesia, akathisia, acute dystonia); often: dizziness, drowsiness, blurred vision; infrequent: decreased ability to concentrate, increased fatigue; very rarely: insomnia, mania or. hypomania, anxiety, agitation, stroke (in elderly patients with predisposing factors).

    In patients with schizophrenia - infrequently: hypervolemia (either due to polydipsia, or due to the syndrome of inadequate secretion of the antidiuretic hormone), tardive dyskinesia (involuntary rhythmic movements, predominantly of the tongue and / or face); rarely: neuroleptic Malignant syndrome (hyperthermia, muscle rigidity, instability of autonomous functions,impaired consciousness and increased levels of creatine phosphokinase), thermoregulation disorders; there is no data on the incidence of epileptic seizures.

    From the digestive system: often: nausea or vomiting, indigestion, dry mouth, constipation, abdominal pain; infrequently: increased activity of "hepatic" transaminases, hypo- or hypersalivation, anorexia, increased or decreased body weight.

    From the side of the cardiovascular system: often: reflex tachycardia; infrequently: orthostatic hypotension or increased blood pressure (BP).

    On the part of the organs of hematopoiesis: rarely: neutropenia, thrombocytopenia.

    From the endocrine system: infrequently: galactorrhea, menstrual irregularities, amenorrhea, weight gain; rarely: gynecomastia; very rarely: hyperglycemia.

    From the genitourinary system: often: erectile dysfunction, priapism; infrequently: violations of ejaculation, violations of orgasm, urinary incontinence.

    Allergic reactions: often: rhinitis, rash; infrequently: angioedema, photosensitization.

    From the skin: infrequent: itching dry skin, hyperpigmentation, seborrhea.

    Other: often: arthralgia.

    Abrupt abolition of antipsychotics may lead to the appearance of withdrawal symptoms (see section "Special instructions").

    Overdose:

    Symptoms:

    Drowsiness, sedation, tachycardia, decreased blood pressure, extrapyramidal disorders; rarely - interval lengthening Q-T.

    Treatment:

    Provide free airway patency to ensure adequate oxygen supply and ventilation, gastric lavage (after intubation, if the patient is unconscious) and the appointment of activated carbon along with a laxative. Immediately begin monitoring the ECG to identify possible arrhythmias. There is no specific antidote. It is necessary to carry out symptomatic therapy aimed at maintaining vital body functions. With a decrease in blood pressure and vascular collapse - IV infusion solutions and / or adrenostimulants. In case of development of acute extrapyramidal symptoms - anticholinergic drugs. Continuous medical surveillance and monitoring should continue until the symptoms of intoxication disappear.

    Interaction:

    Reduces the effectiveness of levodopa and other dopamine agonists.

    Phenothiazines, tricyclic antidepressants and beta-adrenoblockers increase the concentration in the plasma (do not affect the concentration of the active antipsychotic fraction).

    Fluoxetine can increase the concentration of risperidone in plasma, but to a lesser extent - the concentration of the active antipsychotic fraction.

    With the simultaneous administration of carbamazepine and other inducers of "hepatic" enzymes, a decrease in the concentration of the active antipsychotic fraction in plasma is noted.

    Clozapine reduces the clearance of risperidone.

    Ethanol, drugs, depressing the central nervous system - additive inhibition of the central nervous system.

    Hypotensive drugs increase the severity of blood pressure lowering on the background of risperidone.

    Fluoxetine may increase the concentration of risperidone in the plasma (to a lesser extent, the active antipsychotic fraction).

    Caution is advised when using Ridonex® and furosemide concomitantly. In elderly patients with dementia, the combined use of furosemide and risperidone increases the risk of death.

    The mechanism of interaction of these two active substances is unknown.

    With the joint use of other diuretics (especially thiazides in small doses) and risperidone this phenomenon was not noted.

    Special instructions:

    Elderly patients with dementia

    In elderly patients, irrespective of therapy, dehydration increases the risk of death, therefore, in elderly patients with dementia, fluid loss should be avoided.

    Cerebrovascular side effects

    Ridonex® should be used with extreme caution in the treatment of behavioral disorders in patients with dementia, because the risk of cerebrovascular side effects (cerebrovascular complications, transient cerebral circulation impairment) may increase, and therefore it is advisable to conduct a short-term course of therapy.

    Alpha-adrenergic blocking effect

    Ridonex®, due to the alpha-adrenergic blocking effect - especially at the beginning of therapy, during the titration period - can cause orthostatic hypotension, so it may be necessary to reduce the dose.

    Care should also be taken with Ridonex ® in the presence of cardiovascular pathology (eg, heart failure, myocardial infarction, conduction disorders, dehydration, hypovolemia or cerebrovascular disease.) Although risperidone did not show an extension of the interval QT, it is necessary to apply the drug with caution in the event that the patient uses drugs that are characterized by lengthening the interval QT.

    In case the sedative effect caused by Ridonex® is insufficient, instead of increasing the dose of risperidone, it is advisable to use other drugs, for example benzodiazepines, to reduce the risk of side effects.

    Late dyskinesia / extrapyramidal syndrome

    Drugs that have an antagonistic effect on dopamine receptors may cause tardive dyskinesia, which are characterized by involuntary rhythmic jerking, primarily of the tongue and / or face. The appearance of extrapyramidal signs is a risk of the formation of tardive dyskinesia. In the event that signs of tardive dyskinesia appear, a decision must be made to stop the use of all antipsychotics.

    Malignant neuroleptic syndrome

    During the course of therapy with neuroleptics, malignant neuroleptic syndrome (hyperthermia, rigidity of muscles, autonomic (instable) instability, impaired consciousness and increased levels of creatine phosphokinase (CK), myoglobinuria (acute skeletal muscle necrosis), and acute renal failure may develop).When these signs appear, it is necessary to interrupt the course of therapy with antipsychotic drugs, including Ridonex®, and prescribe symptomatic therapy (eg, dantrolene infusion solution for intravenous administration).

    Hyperglycaemia

    Very rarely in the treatment with risperidone, hyperglycemia or exacerbation of the course of diabetes mellitus was noted, therefore, in the presence of diabetes or in the presence of a risk of developing hyperglycemia, it is necessary to monitor the level of glucose in the blood.

    Classical antipsychotics reduce the threshold of convulsive activity, so care must be taken when treating patients with epilepsy.

    To prevent weight gain, you can advise the patient to control food intake.

    The sudden cessation of the use of antipsychotics, especially with the preliminary administration of large doses of the drug, can very rarely cause nausea, vomiting, sweating, anxiety, insomnia, the resumption of psychotic symptoms or impaired coordination of movement (akathisia, dystonia, dyskinesia).

    Like other dopamine antagonists D2-receptors, risperidone can also increase the level of prolactin in the blood plasma. This should be taken into account when appointing risperidone to patients who have a history of malignant breast tumor or prolactin-dependent tumor.

    There is insufficient experience in the use of risperidone in patients with schizophrenia younger than 15 years.

    Due to the fact that Ridonex® tablets contain lactose monohydrate, the drug should not be used with rarely encountered hereditary intolerance to galactose, lactase deficiency, or glucose / galactose malabsorption syndrome.

    Effect on the ability to drive transp. cf. and fur:

    It is necessary to abstain during the treatment from employment by potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

    Form release / dosage:Tablets, film-coated, 1 mg, 2 mg and 4 mg.
    Packaging:

    For 10 tablets coated with a film sheath in a blister of PVC / PVDH film and aluminum foil.

    2 blisters in a cardboard box with instructions for use.

    Storage conditions:

    Store at a temperature not exceeding 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    3 years.

    Do not use the product after the expiry date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-007744/09
    Date of registration:02.10.2009
    Expiration Date:Unlimited
    The owner of the registration certificate:GEDEON RICHTER, OJSC GEDEON RICHTER, OJSC Hungary
    Manufacturer: & nbsp
    Representation: & nbspGEDEON RICHTER OJSC GEDEON RICHTER OJSC Hungary
    Information update date: & nbsp17.12.2016
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