Composition, form of production and packaging
The tablets covered with a film cover of yellow color, round, biconcave, with engraving "N04" on one side.
1 tab.
risperidone 1 mg
[PRING] sodium lauryl sulfate, silicon dioxide colloid, hypromellose, magnesium stearate, pregelatinized starch, microcrystalline cellulose, lactose monohydrate.
The composition of the film shell: opadrai II yellow 85F32072 (iron oxide red (E172, CI 77491), iron oxide yellow (E172, CI 77492), titanium dioxide (E171, CI 77891), talc, macrogol, polyvinyl alcohol).
10 pieces. - blisters (2) - packs of cardboard.
10 pieces. - packings cellular planimetric (2) - packs cardboard.
The tablets covered with a film coat of brownish-yellow color, round, biconcave, with engraving "N05" on one side.
1 tab.
risperidone 2 mg
[PRING] sodium lauryl sulfate, silicon dioxide colloid, hypromellose, magnesium stearate, pregelatinized starch, microcrystalline cellulose, lactose monohydrate.
The composition of the film shell: opadrai II yellow 85F32069 (iron oxide red (E172, CI 77491), iron oxide yellow (E172, CI 77492), titanium dioxide (E171, CI 77891), talc, macrogol, polyvinyl alcohol).
10 pieces. - blisters (2) - packs of cardboard.
10 pieces. - packings cellular planimetric (2) - packs cardboard.
The tablets covered with a film cover of light brown color, round, biconcave, with engraving "N07" on one side.
1 tab.
risperidone 4 mg
[PRING] sodium lauryl sulfate, silicon dioxide colloid, hypromellose, magnesium stearate, pregelatinized starch, microcrystalline cellulose, lactose monohydrate.
The composition of the film shell: opadrai II yellow 85F23450 (iron oxide red (E172, CI 77491), iron oxide yellow (E172, CI 77492), titanium dioxide (E171, CI 77891), talc, macrogol, polyvinyl alcohol).
10 pieces. - blisters (2) - packs of cardboard.
10 pieces. - packings cellular planimetric (2) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2013.
PHARMACHOLOGIC EFFECT
Antipsychotic drug (neuroleptic), benzisoxazole derivative; also has a sedative, antiemetic and hypothermic effect. Selective monoaminergic antagonist, has a high tropism for serotonin 5-HT 2 -receptors and dopamine D 2 -receptors, binds also to? 1- adrenoreceptors and with slightly less affinity with histamine H 1 -receptors and? 2- adrenoreceptors. Has no tropism for cholinergic receptors. The antipsychotic effect is due to the blockade of dopamine D 2 receptors in the mesolimbic and mesocortical systems. Sedative action is due to blockade of adrenoreceptors of the reticular formation of the brainstem; antiemetic effect - blockade of dopamine D 2receptors in 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 expand the therapeutic effect of the drug to include negative and affective symptoms of schizophrenia. Can induce a dose-dependent increase in prolactin concentration in plasma.
PHARMACOKINETICS
Suction
Absorption is fast and complete (food does not affect the completeness and absorption rate). T max in blood plasma - 1-2 h.
Distribution
C ss 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. V d - 1.1 l / kg. The binding to plasma proteins (with alpha1-glycoprotein and albumin) of risperidone - 90%, 9-hydroxy-risperidone - 77%.
Metabolism
Metabolized by the isoenzyme 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.
Excretion
T 1/2 risperidone - 3 h, T 1/2 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%).
Pharmacokinetics in special clinical cases
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.
DOSING MODE
The drug is prescribed to adults and children over 15 years 1 or 2 times / day.
In 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 greater than 10 mg / day did not show a higher efficacy compared with smaller doses and may cause extrapyramidal symptoms. The maximum dose is 16 mg / day.
In bipolar disorders with manias, the initial dose is 2 mg / day for 1 dose. Increase in the dose (by 1 mg / day) - not more often than every other day. The optimal dose is 1-6 mg / day.
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 EFFECT
Risperidone is usually well tolerated. In some cases, side effects can not be distinguished from the signs of the underlying disease.
The frequency of adverse reactions is presented in accordance with the following gradation: very often (? 1/10); often (? 1/100, <1/10); infrequently (> 1/1000, <1/100); rarely (? 1/10 000, <1/1000); very rarely (<1/10 000).
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 because of polydipsia, or because of the syndrome of inadequate secretion of the antidiuretic hormone), tardive dyskinesia (involuntary rhythmic movements, predominantly of the tongue and / or face); rarely - ZNS (hyperthermia, muscle rigidity, instability of autonomic functions, impaired consciousness and increased level of CPK), thermoregulation disorders; there is no data on the incidence of epileptic seizures.
On the part of the digestive system: often - nausea or vomiting, dyspepsia, dry mouth, constipation, abdominal pain; infrequently - increased activity of hepatic transaminases, hypo- or hypersalivation, anorexia, increased or decreased body weight.
From the cardiovascular system: often - reflex tachycardia; infrequently - orthostatic hypotension or increased blood pressure.
From the hemopoiesis: rarely - neutropenia, thrombocytopenia.
On the part of 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: rarely - itching, dry skin, hyperpigmentation, seborrhea.
Other: often - arthralgia.
Abrupt abolition of antipsychotics may lead to the appearance of signs of withdrawal.
CONTRAINDICATIONS
- lactation period;
- Children under 15 years of age (effectiveness and safety not established);
- Hypersensitivity to any of the components of the drug.
With caution , the drug should be prescribed for a brain tumor, intestinal obstruction, kidney and liver diseases, drug overdose, Reye's syndrome (the antiemetic effect of risperidone may mask the symptoms of these conditions), cardiovascular diseases (chronic heart failure, myocardial infarction, AV- blockade), dehydration, cerebral circulation, hypovolemia, Parkinson's disease, seizures (including in anamnesis), drug abuse or leukemia arterial dependence, severe renal / hepatic insufficiency, conditions predisposing to the development of tachycardia such as pirouette (bradycardia, electrolyte imbalance, concomitant medication prolonging the QT interval), pregnancy.
PREGNANCY AND LACTATION
Clinical studies to study the safety of risperidone during pregnancy in humans have not been conducted. In animal trials, risperidone did not show direct reproductive toxicity, several indirect abnormalities associated with the central nervous system and prolactin level were observed. None of the studies revealed a teratogenic effect of risperidone. Thus, Ridonex В® can be used in pregnancy only if the expected benefit of therapy for the mother exceeds the potential risk to the fetus.
It has been shown that risperidone and 9-hydroxy-risperidone are excreted in breast milk, so the use of the drug should be avoided during breastfeeding.
APPLICATION FOR FUNCTIONS OF THE LIVER
In the presence of kidney disease, regardless of the indication, it is necessary to apply half of the initial and subsequent doses.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
In the presence of liver disease, regardless of the indication, it is necessary to apply half of the initial and subsequent doses.
APPLICATION FOR CHILDREN
The drug is prescribed for children older than 15 years .
SPECIAL INSTRUCTIONS
In elderly patients, irrespective of therapy, dehydration increases the risk of death, therefore, in elderly patients with dementia, fluid loss should be avoided.
Ridonex В® 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 blood flow) may increase, so it is advisable to conduct a short-term course of therapy.
Ridonex В® , due to the alpha-adrenergic blocking effect, especially at the beginning of therapy, during the titration period, may cause orthostatic hypotension, so a dose reduction may be necessary.
Caution should also be exercised in the presence of cardiovascular pathology (eg, heart failure, myocardial infarction, conduction disorders, dehydration, hypovolemia or cerebrovascular disease.) Although risperidone has not been shown to prolong the QT interval, it is necessary to use the drug with caution, if the patient uses drugs that are characteristic of prolonging the QT interval.If the sedative effect caused by the Ridonex В® preparation is insufficient, then increasing the dose of risperidone, to reduce the risk of side effects, it is advisable to use other drugs, for example, benzodiazepines.
Drugs that have an antagonistic effect on dopamine receptors may cause tardive dyskinesia, which are characterized by involuntary rhythmic twitching, primarily of the tongue and / or face. The appearance of extrapyramidal symptoms 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.
In therapy with neuroleptics, NSA can develop (hyperthermia, rigidity of muscles, autonomic / autonomic / instability, impaired consciousness and increased CK, myoglobinuria / acute skeletal muscle necrosis / and acute renal failure). When these signs appear, it is necessary to interrupt the course of therapy with antipsychotic drugs, including Ridonex В® , and prescribe symptomatic therapy (eg, dantrolene infusion solution for IV administration).
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), so a gradual withdrawal is suggested.
Like other antagonists of dopamine D 2 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.
Due to the fact that Ridonex В® tablets contain lactose monohydrate, the drug should not be used with rarely encountered hereditary intolerance to galactose, lactase deficiency, or glucose / galactose malabsorption syndrome.
Use in Pediatrics
There is insufficient experience in the use of risperidone in patients with schizophrenia younger than 15 years .
Impact on the ability to drive vehicles and manage mechanisms
During the period of treatment, patients should refrain from engaging in potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.
OVERDOSE
Symptoms: drowsiness, sedation, tachycardia, lowering of blood pressure, extrapyramidal disorders, rarely - prolongation of the QT interval.
Treatment: Provide free airway 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.
DRUG 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 that depress the central nervous system, cause additive suppression of the central nervous system.
Hypotensive drugs increase the severity of blood pressure lowering on the background of risperidone.
Fluoxetine can increase the concentration of risperidone in plasma (to a lesser extent, the active antipsychotic fraction).
Caution should be exercised when using Ridonex В® and furosemide simultaneously. 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.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
List B. The drug should be stored out of reach of children at a temperature of no higher than 25 В° C. Shelf life - 3 years.
