Composition, form of production and packaging
The tablets covered with a film shell of white or almost white color, oblong, biconcave, with engraving "E751" on one side and with a risk - on the other, without or almost without a smell; with the help of the risks of tablets can be divided into two equal doses.
1 tab.
risperidone 1 mg
[PRING] lactose monohydrate - 76 mg, corn starch - 27 mg, cellulose microcrystalline - 14 mg, magnesium stearate - 1.9 mg, silicon dioxide colloid anhydrous - 0.7 mg, sodium lauryl sulfate - 0.4 mg.
The composition of the shell: opadray-Yl-7000 white - 5 mg (hypromellose - 3.125 mg, titanium dioxide - 1.5625 mg, macrogol 400 - 0.3125 mg).
10 pieces. - blisters (1) - packs of cardboard.
10 pieces. - blisters (2) - packs of cardboard.
10 pieces. - blisters (6) - packs of cardboard.
The tablets covered with a film cover of yellow color, oblong, biconcave, with engraving "E752" on one side and with risk - on the other, without or almost without a smell; with the help of the risks of tablets can be divided into two equal doses.
1 tab.
risperidone 2 mg
[PRING] lactose monohydrate - 76 mg, corn starch - 27 mg, cellulose microcrystalline - 14 mg, magnesium stearate - 1.9 mg, silicon dioxide colloid anhydrous - 0.7 mg, sodium lauryl sulfate - 0.4 mg.
The composition of the shell: opadray 03B220015 yellow - 5 mg (hypromellose - 3.125 mg, titanium dioxide - 1.54785 mg, macrogol 400 - 0.3125 mg, dye quinoline yellow aluminum lacquer (E104) - 0.01465 mg).
10 pieces. - blisters (1) - packs of cardboard.
10 pieces. - blisters (2) - packs of cardboard.
10 pieces. - blisters (6) - packs of cardboard.
The tablets covered with a film cover of light green color, oblong, biconcave, with engraving "Р•753" on one side and with risk - on another, without or almost without a smell; with the help of the risks of tablets can be divided into two equal doses.
1 tab.
risperidone 3 mg
[PRING] lactose monohydrate - 76 mg, corn starch - 27 mg, cellulose microcrystalline - 14 mg, magnesium stearate - 1.9 mg, silicon dioxide colloid anhydrous - 0.7 mg, sodium lauryl sulfate - 0.4 mg.
The composition of the shell: opadray 03B21372 green - 5 mg (hypromellose - 3.125 mg, titanium dioxide - 1.5332 mg, macrogol 400 - 0.3125 mg, dye quinoline yellow aluminum lacquer (E104) 0.0138 mg, indigo carmine aluminum lacquer (E132) 0.0155 mg).
10 pieces. - blisters (1) - packs of cardboard.
10 pieces. - blisters (2) - packs of cardboard.
10 pieces. - blisters (6) - packs of cardboard.
The tablets covered with a film membrane of green color, oblong, biconcave, with engraving "E754" on one side and with risk - on another, without or almost without a smell; with the help of the risks of tablets can be divided into two equal doses.
1 tab.
risperidone 4 mg
[PRING] lactose monohydrate - 76 mg, corn starch - 27 mg, cellulose microcrystalline - 14 mg, magnesium stearate - 1.9 mg, silicon dioxide colloid anhydrous - 0.7 mg, sodium lauryl sulfate - 0.4 mg.
The composition of the shell: opadray 03B21368 green - 5 mg (hypromellose - 3.125 mg, titanium dioxide - 1.416 mg, macrogol 400 - 0.3125 mg, dye quinoline yellow aluminum lacquer (E104) - 0.0691 mg, indigo carmine aluminum lacquer (E132) - 0.0774 mg).
10 pieces. - blisters (1) - packs of cardboard.
10 pieces. - blisters (2) - packs of cardboard.
10 pieces. - blisters (6) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2016.
PHARMACHOLOGIC EFFECT
Antipsychotic drug (antipsychotic).
Mechanism of action
Risperidone is a selective monoaminergic antagonist with a high affinity for serotonin 5-HT 2 -receptors and dopamine D 2 -receptors. Associated with? 1-adrenoreceptors and somewhat weaker - with histamine H 1 -receptors and? 2- adrenoreceptors. Has no tropism for cholinergic receptors.
Risperidone reduces productive symptomatology of schizophrenia, to a lesser extent causes suppression of motor activity and to a lesser degree induces catalepsy than classical antipsychotics. A balanced central antagonism to serotonin and dopamine can reduce the propensity to extrapyramidal side effects and broaden the therapeutic effect of the drug to include negative and affective symptoms of schizophrenia.
Pharmacodynamic effects
Despite the fact that risperidone is a strong D 2 antagonist, which is associated with its influence on positive symptoms of schizophrenia, it, in comparison with classical antipsychotics, to a lesser degree causes inhibition of motor activity and a tendency to catalepsy. Balanced antagonism to central serotonin and dopamine receptors can reduce the tendency to extrapyramidal side effects and include negative and affective symptoms of schizophrenia in the spectrum of therapeutic activity.
PHARMACOKINETICS
Suction
After ingestion, risperidone is completely absorbed from the digestive tract. C max in plasma is achieved after 1-2 hours. Absolute bioavailability of risperidone after oral administration is 70%. The relative bioavailability after oral administration of risperidone in the form of tablets is 94%. Food does not affect the absorption of the drug, so risperidone can be administered regardless of food intake.
Distribution
Risperidone is rapidly distributed in the body. V d is 1-2 l / kg. Risperidone is 90% bound by plasma proteins (mainly with albumin and acid alpha 1- glycoprotein), 9-hydroxyrisperidone - by 77%.
C ss risperidone in the body in most patients is achieved within 1 day. C ss 9-hydroxyrisperidone - for 4-5 days.
The concentration of risperidone in plasma is directly proportional to the dose of the drug (within therapeutic doses).
Metabolism
Risperidone is metabolized by the isoenzyme CYP2D6 to 9-hydroxyrisperidone, which has a pharmacological action similar to risperidone. Risperidone and 9-hydroxyrisperidone constitute the active antipsychotic fraction. The CYP2D6 isozyme is susceptible to genetic polymorphism. In patients with intensive metabolism by the CYP2D6 isoenzyme, risperidone is rapidly converted to 9-hydroxyrisperidone, while in patients with weak metabolism this transformation occurs much more slowly. Although patients with intensive metabolism have a lower concentration of risperidone and a higher concentration of 9-hydroxyrisperidone than patients with poor metabolism, the total pharmacokinetics of risperidone and 9-hydroxyrisperidone (active antipsychotic fraction) after taking one or more doses is similar in patients with intense and weak metabolism of CYP2D6.
Another way of metabolizing risperidone is N-dealkylation. In vitro studies on human liver microsomes showed that risperidone at clinically significant concentrations does not, in general, inhibit the metabolism of drugs that undergo biotransformation with P450 isoenzymes, including CYP1A2, CYP2A6, CYP2C8 / 9/10, CYP2D6, CYP2E1, CYP3A4 and CYP3A5.
Excretion
After ingestion in patients with psychosis, risperidone is excreted from the body with T 1/2 for about 3 hours. T 1/2 of 9-hydroxyrisperidone and the active antipsychotic fraction is 24 hours.
A week after the start of the drug, 70% of the dose is excreted in the urine, 14% - with feces. In urine risperidone together with 9-hydroxyrisperidone constitute 35-45% of the dose. The rest is made up of inactive metabolites.
Pharmacokinetics in specific patient groups
After a single dose of risperidone in elderly patients, the concentration of the active antipsychotic fraction in plasma was 43% higher on average, T 1/2 lasted 38% longer, and the clearance decreased by 30%.
In patients with renal insufficiency, an increase in plasma concentration and a decrease in the clearance of the active antipsychotic fraction was observed on average by 60%.
In patients with hepatic insufficiency, the concentrations of risperidone in the plasma did not change, but the average concentration of the free fraction of risperidone increased by 35%.
The pharmacokinetics of risperidone, 9-hydroxyrisperidone and active antipsychotic fraction in children is comparable to that of adult patients.
Population pharmacokinetic analysis did not reveal the obvious effect of sex, race or smoking on the pharmacokinetics of risperidone and the active pharmacokinetic fraction.
INDICATIONS
- treatment of schizophrenia in adults and children from 13 years;
- treatment of manic episodes associated with bipolar disorder, moderate and severe in adults and children 10 years of age;
- Short-term (up to 6 weeks) symptomatic treatment of persistent aggression in the structure of behavioral disorder in children from 5 years of age with mental retardation diagnosed according to DSM-IV, in which, due to the severity of aggression or other destructive behavior, medication is required. Pharmacotherapy should be part of a wider treatment program, incl. psychological and educational activities. Risperidone should be prescribed by a specialist in the field of pediatric neurology and child psychiatry or a physician familiar with the treatment of behavioral disorders in children and adolescents.
DOSING MODE
The drug is taken orally. Eating does not affect the absorption of the drug.
At the beginning of treatment with Rileptid В® it is recommended to gradually abolish previous therapy, if it is clinically justified. In this case, if patients are transferred from the therapy of depot forms of antipsychotics, then therapy with Rileptid В® is recommended to begin instead of the next scheduled injection. Periodically, the need to continue the current therapy with antiparkinsonian drugs should be evaluated.
Stopping the drug is recommended to be carried out gradually. Acute withdrawal symptoms, including nausea, vomiting, sweating and insomnia, were very rare after a sharp discontinuation of antipsychotics in high doses.
Schizophrenia
Adults Rilefted В® are prescribed 1 or 2 times / day. The initial dose is 2 mg / day. On the second day, the dose can be increased to 4 mg / day. From this moment the dose can either be kept at the same level, or individually adjusted if necessary. Usually the optimal dose is 4-6 mg / day. In some cases, a slower dose increase and lower initial and maintenance doses may be justified.
Doses above 10 mg / day did not show higher efficacy compared with smaller doses and may cause extrapyramidal symptoms. Due to the fact that the safety of doses above 16 mg / day has not been studied, doses above this level should not be used.
For elderly patients, the drug is prescribed in an initial dose of 0.5 mg 2 times / day. The dose can be individually increased by 0.5 mg 2 times / day to 1-2 mg 2 times / day.
At violations of the liver and kidneys, the initial dose is 0.5 mg 2 times / day. The dose can be gradually increased to 1-2 mg 2 times / day.
In children aged 13 to 17 years , the initial dose of 0.5 mg is recommended 1 time / day in the morning or evening. If necessary, the dose can be increased at least after 24 hours at 0.5-1 mg / day to a recommended dose of 3 mg / day with good tolerability. Despite the efficacy shown in the treatment of schizophrenia in adolescents with a drug in doses of 1-6 mg / day, no additional efficacy was observed when the drug was used at doses above 3 mg / day, and higher doses caused more side effects. The use of the drug in doses above 6 mg / day has not been studied.
Patients who have sustained drowsiness, it is recommended to take half the daily dose 2 times / day.
Manic episodes associated with bipolar disorder
Adults prescribe the drug in an initial dose of 2 mg / day at a time. If necessary, this dose can be increased at least 24 hours per 1 mg / day. For most patients, the optimal dose is 1-6 mg / day. The use of the drug in doses above 6 mg / day in patients with manic episodes has not been studied.
As with any other symptomatic therapy, the rationale for continued treatment with RileptidВ® should be regularly assessed and validated.
For elderly patients, the drug is prescribed in an initial dose of 0.5 mg per reception 2 times / day. The dose can be individually increased by 0.5 mg 2 times / day to 1-2 mg 2 times / day. Care should be taken in connection with the limited experience of the drug in elderly patients.
For children aged 10 years, the drug is prescribed in an initial dose of 0.5 mg 1 time / day in the morning or evening. If necessary, the dose can be increased at least after 24 hours at 0.5-1 mg / day to a recommended dose of 1-2.5 mg / day with good tolerability. Despite the efficacy shown in the treatment of manic episodes associated with bipolar disorder in children with a drug in doses of 0.5-6 mg / day, no additional efficacy was observed with the drug at doses above 2.5 mg / day, and higher doses caused more side effects . The use of the drug in doses above 6 mg / day has not been studied. Patients who have sustained drowsiness, it is recommended to take half the daily dose 2 times / day.
Continuous aggression in the structure of behavioral disorders in children aged 5 to 18 years
For patients with a body weight of 50 kg or more, the drug is prescribed in an initial dose of 0.5 mg 1 time / day. If necessary, the dose may be increased by 0.5 mg / day, not more often than every other day. For most patients, the optimal dose is 1 mg / day. However, for some patients it is preferable to take the drug at 0.5 mg / day, while some require an increase in the dose to 1.5 mg / day.
Patients with a body weight of less than 50 kg of the drug prescribed in the initial dose of 0.25 mg 1 time / day. If necessary, the dose can be increased by 0.25 mg / day, not more often than every other day. For most patients, the optimal dose is 0.5 mg / day. However, for some patients it is preferable to take the drug at 0.25 mg / day, while some require an increase in the dose to 0.75 mg / day.
As with any other symptomatic therapy, the rationale for continued treatment with RileptidВ® should be regularly assessed and validated.
The use of the drug in children under 5 years of age is not recommended because of the lack of data.
Special patient groups
In patients with kidney disease, the ability to excrete the active antipsychotic fraction is reduced compared to other patients.
In patients with liver disease, there is an increased concentration of free fraction of risperidone in the blood plasma.
The initial and maintenance dose in accordance with the indications should be reduced 2 times, increasing the dose in patients with liver and kidney disease should be slower.
Rileptide В® should be administered with caution in this category of patients.
SIDE EFFECT
The most frequently observed side effects (incidence of ≥10%) were: parkinsonism, sedation / drowsiness, headache and insomnia.
Dose-dependent adverse reactions were parkinsonism and akathisia.
The side effects of Rileptide В® in therapeutic doses are given with frequency distribution and organ systems.
The frequency of side effects was classified as follows: very often (? 1/10 cases), often (? 1/100 and <1/10 cases), infrequently (? 1/1000 and <1/100 cases), rarely (? 1 / 10 000 and <1/1000 cases), very rarely (<1/10 000 cases) and the frequency is unknown (it is impossible to estimate the frequency from the available data).
In each frequency group, side effects are presented in order of decreasing importance.
Infectious diseases: often - pneumonia, bronchitis, upper respiratory tract infections, sinusitis, urinary tract infections, ear infections, influenza; infrequently - respiratory infections, cystitis, eye infections, tonsillitis, onychomycosis, inflammation of subcutaneous fat, localized infections, viral infections, otitis media, acrodermatitis; rarely - infection.
On the part of the hematopoiesis system: infrequently - neutropenia, decrease in the number of leukocytes, anemia, thrombocytopenia, lowering of hematocrit, increase in the number of eosinophils; rarely - agranulocytosis.
From the immune system: infrequently - hypersensitivity; rarely an anaphylactic reaction.
From the side of metabolism and nutrition: often - weight gain, hyperprolactinemia 1 ; infrequently - diabetes mellitus 2 , hyperglycemia, polydipsia, weight loss, anorexia, increased cholesterol concentration in the blood; rarely - ADH deficiency, the presence of glucose in the urine, water intoxication 3 , hypoglycemia, hyperinsulinemia 3 , increased triglyceride levels in the blood plasma; very rarely diabetic ketoacidosis.
Mental disorders: very often - insomnia 4 ; often - sleep disorders, agitation, depression, anxiety; infrequently - mania, confusion, decreased libido, nervousness, nightmares; rarely - flattening of affect, anorgasmia.
From the nervous system: very often - sedation, drowsiness, Parkinsonism 4 , headache; often - akathisia 4 , dystonia 4 , dizziness, dyskinesia 4 , tremor; infrequently - tardive dyskinesia, cerebral ischemia, lack of response to irritants, loss of consciousness, deterioration of consciousness, convulsions 4 , fainting, increased psychomotor activity, imbalance, coordination disorder, orthostatic dizziness, attention disturbance, dysarthria, taste disorders, hypesthesia, paresthesia; rarely - malignant neuroleptic syndrome, acute disturbance of cerebral circulation, diabetic coma, trembling of the head.
From the side of the organ of vision: often - indistinctness of visual perception; infrequent - photophobia, dry eyes, increased lacrimation, conjunctivitis; rarely - glaucoma, violation of eye movements, involuntary rotation of eyeballs, crust formation at the edge of the eyelids, intraoperative syndrome of trembling iris 3 .
From the organ of hearing and balance: infrequently - vertigo, earache, tinnitus.
From the cardiovascular system: often - tachycardia, hypertension; infrequent atrial fibrillation, AV blockade, conduction abnormality, QT interval prolongation on the ECG, sinus bradycardia, ECG changes, palpitation, hypotension, orthostatic hypotension, hot flashes; rarely - sinus arrhythmia, pulmonary embolism, thrombosis of veins.
From the respiratory system: often - shortness of breath, pain in the larynx and pharynx; cough, nosebleeds, nasal congestion; infrequently - aspiration pneumonia, congestion in the lungs, stasis in the airways, wheezing, wheezing, dysphonia, respiratory system diseases; rarely - sleep apnea syndrome, hyperventilation.
On the part of the digestive system: often - increased appetite, decreased appetite, abdominal pain, abdominal discomfort, vomiting, nausea, constipation, diarrhea, indigestion, dry mouth, toothache; infrequently - faecal incontinence, fekaloma, gastroenteritis, dysphagia, flatulence, increased transaminases, GGT activity increase, increase in liver enzymes; rarely - pancreatitis, intestinal obstruction, swelling of the tongue, cheilitis, jaundice.
From the urinary system: often - urinary incontinence; rare - pollakiuria, urinary retention, dysuria.
Reproductive system and breast: infrequently - erectile dysfunction, abnormal ejaculation, amenorrhea, menstrual violation 4 , gynecomastia, galactorrhea, sexual dysfunction, breast tenderness, discomfort in the breast, vaginal discharge; rarely - priapism 3, Absence of menstruation, hyperemia mammary breast enlargement, secretion from mammary glands.
Skin and subcutaneous tissue disorders: often - a rash, erythema; infrequently - angioedema, pruritus, alopecia, hyperkeratosis, eczema, dry skin, impaired color, acne, seborrheic dermatitis, skin disease, skin disorders; rare - rash caused by the drug, dandruff; very rarely - angioedema.
On the part of the musculoskeletal system: often - muscle spasm, pain in bones and muscles, arthralgia, back pain; infrequently - raising activity of CK in the blood plasma, bad posture, joint stiffness, joint swelling, muscle weakness, pain in the neck; rarely - rhabdomyolysis.
Impact on the course of pregnancy, postpartum and perinatal conditions:seldom - a withdrawal syndrome in newborns.
Injury, poisoning and complications of manipulation: often - fall; rarely - pain associated with medical interventions.
Other: often - edema 4 , pyrexia, in the area of chest pain, asthenia, fatigue; infrequently - facial edema, chills, fever, gait disturbance, thirst, discomfort in the chest, feeling unwell, discomfort; rarely - hypothermia, decreased body temperature, cold extremities, withdrawal, induration 3 .
1 - Hyperprolactinemia can in some cases lead to gynaecomastia, menstrual disorders, amenorrhea and galaktoree.
2- in the placebo studies kontrolirumyh diabetes was observed in 0.18% of patients treated with risperidone compared with 0.11% in the placebo group. The overall incidence of diabetes based on the results of all clinical trials was 0.43% of all patients treated with risperidone.
3 - adverse reactions were not observed during the clinical trials but have been reported in the post-registration period.
4- extrapyramidal disorders may manifest as parkinsonism (hypersalivation, musculoskeletal stiffness, parkinsonism, drooling, rigidity of the type "gear", bradykinesia, hypokinesia, maskopodobnoe face, muscle stiffness, akinesia, stiff neck, muscle rigidity, parkinsonian gait, disorders glabellar reflex), akathisia (akathisia, restlessness, hyperkinesia and restless leg syndrome), tremor, dyskinesia (which term includes diskeneziju, muscle twitching, choreoathetosis, athetosis and miokl ЕЌnusa), dystonia.
The term includes dystonia itself dystonia, muscle spasms, hypertension, torticollis, involuntary muscle contractions, muscle contracture, blepharospasm, movement of the eyeball, tongue paralysis, facial spasm, laryngospasm, myotonia, opisthotonos, oropharyngeal spasm plevrototonus, tongue spasm and lockjaw. Tremor includes tremor and parkinsonian rest tremor. It should be noted, that was included a wider range of symptoms, which do not always have the extrapyramidal origin.
The term insomnia include: disturbance of sleep and sleep disorders.
The term convulsions denotes grand mal seizure (grand mal).
The term includes menstruation violation: irregular menstruation and oligomenorrhea.
The term edema include: generalized edema, peripheral edema, swelling, keeping track finger pressure.
Adverse reactions due paliperidone
Paliperidone is an active metabolite of risperidone, however should be considered the profile of adverse reactions of these active substances (including forms of drugs for oral administration, and for injection). Besides the above reactions, the following adverse reactions were observed at application paliperidone, but they can also develop when using risperidone.
With the cardiovascular system: orthostatic tachycardia syndrome.
Class-effects
With the cardiovascular system:as well as the use of other antipsychotics, very rare cases lengthening QT interval observed in the post-registration surveillance period. Other class-effects to the cardiovascular system, seen with antipsychotic drugs that prolong QT interval include ventricular arrhythmia, ventricular fibrillation, ventricular tachycardia, sudden death, cardiac arrest and ventricular tachycardia type "pirouette".
Venous thromboembolism: cases of venous thromboembolism, including cases of pulmonary embolism and deep vein thrombosis observed with antipsychotics (the frequency is unknown).
Weight gain:in the placebo-controlled studies in patients with schizophrenia, a statistically significant increase in body weight is not less than 7% was observed after 6-8 weeks in 18% of patients taking risperidone and 9% of patients receiving placebo. In placebo-controlled clinical studies in patients with manic episodes incidence of weight gain of 7% or more after 3 weeks of treatment was comparable to the group receiving risperidone (2.5%) and in the group receiving the placebo (2.4%), and active control group was slightly higher (3.5%). Children with behavior disorders during long-term clinical trials of body weight increased by an average of 7.3 kg after 12 months of therapy. The expected increase in body weight in children aged 5-12 years with normal development of 3-5 kg ​​/ year.From 12-16 years the value of weight gain should be 3-5 kg ​​/ year for girls and about 5 kg / year for the boys.
Additional information on special populations of patients
Side effects that occurred with greater frequency in elderly patients with dementia and in children rather than in adults, are described below.
Elderly patients with dementia: a transient ischemic attack and stroke have been observed in clinical trials with a frequency of 1.4% and 1.5%, respectively. In addition, the following adverse effects were observed in elderly patients with dementia with a frequency of 5% and a frequency at least 2 times greater than that in other patient populations - urinary tract infection, peripheral edema, lethargy, and cough.
Children:The following side effects were seen in children (aged 5 to 17 years) with a frequency of 5% and a frequency of at least 2 times greater than that in other populations of patients in clinical trials - drowsiness / sedation, fatigue, headache, , increased appetite, vomiting, upper respiratory tract infection, nasal congestion, abdominal pain, dizziness, cough, fever, tremors, diarrhea, and enuresis.
Reported adverse reactions suspected of being related to treatment
Notice of suspects in connection with the treatment of adverse reactions occurring after the registration of the drug, it is very important. These measures allow to monitor the ratio benefits and risks of the drug. Health care providers should report any suspects in connection with the treatment of adverse reactions through the pharmacovigilance system.
CONTRAINDICATIONS
- phenylketonuria;
- Lactase deficiency, lactose intolerance, glucose-galactose malabsorption;
- Hypersensitivity to risperidone or any subsidiary component of the drug.
With cautionshould be used on patients with diseases of the cardiovascular system (including chronic heart failure, myocardial infarction, conduction disturbances of the heart muscle), during dehydration, hypovolemia, cerebrovascular disease, Parkinson's disease, convulsions (incl . history), severe renal or hepatic failure, with drug abuse or drug addiction, in conditions predisposing to tachycardia type "pirouette" (bradycardia, nar ushenie electrolyte balance, concomitant drugs, prolonging the interval QT), in tumors of the brain, intestinal obstruction, in cases of acute drug overdose, with Reye's syndrome (b.p. antiemetic effect of risperidone may mask symptoms of these conditions),the presence of risk factors for thromboembolism, venous vascular disease diffuse Lewy bodies, hyperglycemia, pregnancy, as well as in conjunction with furosemide.
PREGNANCY AND LACTATION
Full use of risperidone studies in pregnant women have been conducted. According to observations in the postmarketing period with risperidone in the III trimester of pregnancy, the newborn appeared reversible extrapyramidal symptoms, so the newborns whose mothers took risperidone in the III trimester of pregnancy, should be under close medical supervision. In animal studies, risperidone did not have a teratogenic effect, but there were other types of toxic effects on the reproductive system. The potential risk to humans is unknown. Rileptid В® can be used during pregnancy only if the expected benefits of the drug for a pregnant woman outweighs the potential risk to the fetus. If necessary, stop taking the drug during pregnancy should be the abolition of the drug gradually.
In studies in animals, risperidone and 9-hydroxyrisperidone are excreted with breast milk. It has also been demonstrated that risperidone and 9-hydroxyrisperidone in small amounts into breast milk of lactating women. Information about side effects in infants who are breastfed are missing, so the issue of breast-feeding should be resolved taking into account the possible risk to the child.
APPLICATION FOR FUNCTIONS OF THE LIVER
When renal impairment initial dose of 500 mg 2 times / day. The dose can be gradually increased to 1-2 mg of 2 times / sut.S care use in patients with severe renal failure.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With care use in patients with severe hepatic insufficiency.
In human liver initial dose of 500 mg 2 times / day. The dose can be gradually increased to 1-2 mg of 2 times / day.
APPLICATION FOR CHILDREN
Use of the drug in children under the age of 5 years is not recommended due to lack of data.
APPLICATION IN ELDERLY PATIENTS
Elderly patients preparation administered in an initial dose of 500 ug to receive 2 times / day. The dose can be individually increased by 500 mg 2 times / day of 1-2 mg of 2 times / day. Care must be taken in connection with the limited experience of the drug in elderly patients.
SPECIAL INSTRUCTIONS
Use in elderly patients with dementia
In elderly patients with dementia in the treatment of atypical antipsychotics observed increased mortality compared to placebo in studies of atypical antipsychotics, including risperidone. In applying risperidone frequency for a given population of deaths was 4% for patients treated with risperidone, compared to 3.1% for placebo. The average age of patients who died was 86 years (range 67-100 years). The data collected from two large observational studies showed that elderly patients with dementia being treated typical antipsychotic drugs, also have a slightly increased risk of death compared with patients not undergoing treatment. At the moment, was not enough data to accurately assess this risk. Unknown and the cause of increasing this risk.Also not determined the extent to which increased mortality can be applied to antipsychotic drugs, but not to the characteristics of this group of patients.
In placebo-controlled trials with risperidone in elderly patients with dementia there was increased mortality, while the use of furosemide and risperidone orally (7.3%; mean age 89 years, range 75-97 years) compared with the group treated with risperidone alone (3.1%; mean age 84 years old, range 70-96 years) and the group treated with furosemide alone (4.1%; mean age 80 years, range 67-90 years). Increased mortality of patients receiving furosemide together with risperidone was observed during 2 out of 4 clinical trials. The combined use of risperidone with other diuretics (mainly with thiazide diuretics at low doses) was not accompanied by increased mortality.
Not assigned pathophysiological mechanisms explaining this observation. However, you should be very careful when administering the drug in such cases. The appointment should carefully evaluate the risk / benefit ratio. It was found to increase mortality in patients concurrently taking other diuretics together with risperidone. Irrespective of treatment, dehydration is a common risk factor for mortality and should be carefully monitored in elderly patients with dementia.
Side effects associated with cerebrovascular
In elderly patients with dementia, an increase of side effects from cerebrovascular system (acute and transient ischemic attacks), including fatalities in patients (mean age 85 years, range 73-97 years) with risperidone compared with placebo.
In a randomized, placebo-controlled clinical trials in patients with dementia, taking some atypical antipsychotics, there was an increased risk of cerebrovascular adverse events in approximately 3 times. Pooled data from six placebo-controlled studies involving mostly elderly patients with dementia (age over 65 years) show that cerebrovascular adverse effects (serious and carried
