Risperidone pills 4mg №30

Risperidone

risperidone

Dosage form

film-coated tablets.

Composition

1 tablet, film coated, contains:

For dosage of 1 mg

active ingredient risperidone -1 mg

Auxiliary substances (core):

lactose monohydrate (milk sugar) - 83.0 mg;

microcrystalline cellulose - 12.0 mg; pregelatinized corn starch (Starch 1500) - 2.0 mg; Magnesium stearate - 1.0 mg; potato starch - 7.0 mg; Povidone (medium molecular weight polyvinylpyrrolidone)

- 4.0 mg.

Shell composition:

Opadry II - 3.0 mg (polyvinyl alcohol, partially hydrolyzed - 1.2000 mg; talc - 0.4440 mg; macrogol (polyethylene glycol 3350) - 0.6060 mg; titanium dioxide E 171 - 0.7500 mg).

For dosage 2 mg

active ingredient risperidone - 2 mg

Auxiliary substances (core):

lactose monohydrate (milk sugar) - 82.0 mg; microcrystalline cellulose - 12.0 mg; corn starch pregelatinized (Starch 1500) - 2.0 mg; magnesium stearate - 1.0 mg; potato starch - 7.0 mg; Povidone (medium molecular weight polyvinylpyrrolidone) - 4.0 mg.

Shell composition:

Opadry II -3 mg (polyvinyl alcohol, partially hydrolyzed - 1.2000 mg; talc

- 0,4440 mg; macrogol (polyethylene glycol 3350) - 0.6060 mg; titanium dioxide E 171 - 0.6561 mg; yellow lacquer based on quinoline yellow - 0.0903 mg;

aluminum varnish on the basis of yellow sundown - 0.0021 mg; iron dye oxide (II) yellow E 172 - 0.0009 mg; Indigo Carmine Aluminum Varnish - 0.0006 mg).

For dosage 4 mg

active ingredient risperidone - 4 mg

Auxiliary substances (core):

lactose monohydrate (milk sugar) -114.0 mg; microcrystalline cellulose - 19.7 mg; pregelatinized corn starch (Starch 1500) - 3.0 mg; magnesium stearate - 1.0 mg; potato starch - 11.0 mg; Povidone (medium molecular weight polyvinylpyrrolidone) - 7.3 mg.

Shell composition:

Opadry II - 5 mg (polyvinyl alcohol, partially hydrolyzed - 2.2000 mg; talc - 1.0000 mg; macrogol (polyethylene glycol 3350) - 0.6175 mg; titanium dioxide E 171 - 0.6545 mg; soy lecithin E 322 - 0.1750 mg; aluminum based varnish

Quinoline Yellow - 0.1010 mg; Indigo Carmine Aluminum Varnish - 0.2520 mg).

Mechanism of action

Pharmacodynamics

Risperidone is an antipsychotic agent, a benzisoxazole derivative, also has a sedative, anti-emetic and hypothermic effect.

Risperidone is a selective monoaminergic antagonist,

gives high affinity for serotonergic 5-HT2 and dopaminergic D2

-receptors. Risperidone is also associated with α1-adrenergic receptors and, somewhat weaker, with H1-histaminergic and α2-adrenergic receptors. Risperidone has no tropichnost to cholinergic receptors.

Antipsychotic action due to D2-dopaminergic blockade

mesolimbic and mesocortical receptors.

Risperidone reduces the productive symptoms of schizophrenia (delusions, hallucinations), aggressiveness, automatism, and to a lesser extent induces catalepsy than typical antipsychotics. Balanced central antagonism to serotonin and dopamine may reduce the propensity for extrapyramidal side effects and extend the therapeutic effect of the drug to cover the negative and affective symptoms of schizophrenia.

Clinical data

Schizophrenia

The effectiveness of risperidone in the short-term treatment of schizophrenia was

demonstrated in four studies with a duration of 4 to 8 weeks, in which 2500 patients were included, meeting the criteria for schizophrenia with the DSM-IV system. In a 6-week, placebo-controlled study, when titrated to a dose of 10 mg / day, 2 times a day, risperidone was superior to placebo on a brief psychiatric rating scale (BPRS). In a 6-week placebo-controlled study using risperidone in

four fixed doses (2, 6, 10, and 16 mg / day, 2 times a day), in the 4th group, risperidone was more effective than placebo on the scale of positive and negative syndromes (PANSS). In an 8-week comparative study of five fixed doses of risperidone (1, 4, 8, 12, and 16 mg / day, 2 times a day), risperidone in groups 4, 8, and 16 mg / day was more effective than risperidone 1 mg / day on a scale PANSS. In a 4-week comparative placebo-controlled study of two fixed doses of risperidone (4 and 8 mg / day, once a day), risperidone in both groups was more effective than placebo on several points of the PANSS scale.

Manic episodes in bipolar disorder

The effectiveness of risperidone in monotherapy for acute manic episodes with

Type I bipolar disorder was demonstrated in three double-blind, placebo-controlled studies involving about 820 patients with bipolar type I disorder, in accordance with the DSM-IV scale. In these three studies, risperidone in doses of 1-6 mg / day (initial dose of 3 mg in two studies and 2 mg in one study) statistically exceeded placebo in the primary endpoint, that is, change in the sum of points on the Yang mania rating scale (YMRS) after 3 weeks compared to baseline. The results for the secondary endpoints of effectiveness are generally consistent with those for the primary endpoint. The percentage of patients with a decrease of> 50% of the score on the YMRS scale after 3 weeks compared with baseline was significantly higher for risperidone than in the placebo group. The effectiveness of risperidone in combination with mood regulators in the treatment of mania was demonstrated in two three-week double-blind studies in approximately 300 patients who met the criteria of bipolar disorder of the first type on the DSM-IV system. In a 3-week study, risperidone in doses from 1 to 6 mg / day, initial dose 2

mg / day, in combination with lithium or valproate, was more effective than lithium or valproate only at the end of the study on the primary specified criterion, that is, on a change in the amount of points on the YMRS scale compared to baseline in the third week.

Prolonged aggression in dementia

The effectiveness of risperidone in the treatment of psycho-behavioral symptoms of dementia, including behavioral problems such as aggression, agitation, psychosis, activity and affective disorders, was demonstrated in three double-blind, placebo-controlled studies in 1,150 patients with moderate and severe dementia. One study was conducted in fixed doses of 0.5, 1 and 2 mg / day. In two studies, non-fixed doses were studied, including groups with doses of risperidone from 0.5 to 4 mg / day and from 0.5 to 2 mg / day, respectively. Risperidone showed clinically and statistically high efficacy in the treatment of aggression, and, to a lesser extent, arousal and psychosis.

in elderly patients with dementia (according to the scale of behavioral pathology during illness

Alzheimer (BEHAVE-AD) and on the questionnaire Kogen Mansfield for excitation (CMAI)).

Behavior disorders

The effectiveness of risperidone in the short-term treatment of aggressive behavior was

demonstrated in placebo-controlled studies in approximately 240 patients aged 5 to 12 years with devastating behavioral disorders in accordance with the DSM-IV system and below-average intellectual functioning or with mild mental retardation or moderate impairment in learning. In both studies, risperidone in doses from 0.02 to 0.06 mg / kg / day was significantly more effective than placebo with the preset primary efficacy endpoint.

Pharmacokinetics

Risperidone after oral administration is completely absorbed, reaching maximum plasma concentrations after 1-2 hours. The absolute oral bioavailability of risperidone is 70%.

Food does not affect the absorption of risperidone, so it can be administered regardless of the meal.

Risperidone is rapidly distributed in the body. The volume of distribution is 1-2 l / kg. In plasma, risperidone binds to albumin and alpha1-acid glycoprotein.

Risperidone is 90% bound to plasma proteins, 9-hydroxyrisperidone - 77%.

The equilibrium concentration of risperidone in the body in most patients is achieved within 1 day. Equilibrium concentration of 9-hydroxyrisperidone is reached after 4-5 days. Plasma concentrations of risperidone are proportional to the dose of the drug (within therapeutic doses).

Risperidone is metabolized by the isoenzyme of CYP2D6 to 9-hydroxy-risperidone, which has a pharmacological action similar to risperidone. Risperidone and 9-hydroxyrisperidone constitute the active antipsychotic fraction. Metabolism depends on the genetic polymorphism of the isoenzyme, CY2D6.

Another route of metabolism of risperidone is N-dealkylation.

After oral administration in patients with psychosis, risperidone is eliminated from the body with a half-life (T1 / 2) of about 3 hours. T1 / 2 9-hydroxyrisperidone and the active antipsychotic fraction are 24 hours.

After a week of taking the drug, 70% of the dose is excreted in the urine, 14% in the feces.In urine, risperidone plus 9-hydroxyrisperidone accounts for 35-45% of the dose. The rest is inactive metabolites.

Special patient groups

The study of a single dose of the drug revealed a higher concentration in plasma and a slower elimination in the elderly and in patients with renal insufficiency. Plasma risperidone concentrations in patients with hepatic insufficiency were normal.

The pharmacokinetics of risperidone and 9-hydroxyrisperidone in pediatric patients are similar to the pharmacokinetics in adult patients.

There is no effect of gender, nationality or smoking on the pharmacokinetics of risperidone.

Treatment of schizophrenia.

Treatment of manic episodes in the structure of moderate and severe bipolar disorder.

Short-term (up to 6 weeks) treatment of ongoing aggression in patients with

moderate to severe Alzheimer's disease -

with the ineffectiveness of non-pharmacological methods of correction and the threat of harm to the patient or others. Short-term (up to 6 weeks) symptomatic treatment of ongoing aggression in behavioral disorder in children 5-16 years of age with moderate and severe mental retardation, due to the severity of which pharmacological correction methods are required (as part of complex therapy).

-individual hypersensitivity to risperidone or any other

an ingredient of this drug;

-lactase deficiency, lactose intolerance, glucose-galactose malabsorption;

in the treatment of ongoing aggression in behavior disorder in children with

moderate and severe mental retardation; children under 5 years old (experience

application is insufficient);

-with other indications, children up to 18 years old.

Carefully

Use with caution in the following conditions:

- diseases of the cardiovascular system (chronic heart failure, myocardial infarction, cardiac muscle conduction disturbances);

dehydration and hypovolemia;

- disorders of cerebral circulation;

-Parkinson's disease;

- spasms and epilepsy (including in the anamnesis);

- heavy renal or hepatic failure (see the section "Route of administration and doses");

-use of drugs or drug dependence (see section "Dosage and administration");

-states

predisposing to the development of tachycardia type "pirouette" (bradycardia,

electrolyte imbalance, concomitant medication,

extending the interval QT);

- brain tumor, intestinal obstruction, cases of acute overdose of drugs,

Reis syndrome (the anti-emetic effect of risperidone may mask the symptoms of these conditions);

Pregnancy and lactation.

Use during pregnancy and lactation

There are no data on the safety of risperidone in pregnant women. AT

In animal experiments, risperidone had no direct toxic effect on the reproductive system, but it did produce some indirect effects mediated through prolactin and the central nervous system. None of the studies had risperidone teratogenic effects. If a woman took antipsychotic drugs (including risperidone) in the third trimester of pregnancy, newborns are at risk of extrapyramidal disorders and / or withdrawal symptoms of varying severity. These symptoms may include agitation, hypertension, hypotension, tremor, drowsiness, respiratory disorders and feeding disorders. The drug risperidone can be used during pregnancy only in cases where the potential benefits to a woman outweigh the possible risk to the fetus.

Since risperidone and 9-hydroxyrisperidone penetrate into breast milk, women who use risperidone should not be breastfed.

Inside, regardless of the meal.

Schizophrenia

Adults.

Risperidone may be administered once or twice a day.

The initial dose of risperidone is 2 mg per day. On the second day, the dose should be

increase to 4 mg per day. From this point on, the dose can either be maintained at the same level, or individually adjusted if necessary. Usually the optimal dose is from 4 to 6 mg per day. In some cases, a slower dose increase and lower initial and maintenance doses may be justified.

Doses above 10 mg per day did not show higher efficacy.

compared with smaller doses and can cause extrapyramidal symptoms. Due to the fact that the safety of doses above 16 mg per day has not been studied, doses above this level cannot be used.

Elderly patients.

An initial dose of 0.5 mg per dose is recommended twice a day. The dose can be individually increased by 0.5 mg twice a day to a dose of 1 to 2 mg twice a day.

day.

Children

Information on the use of the drug for the treatment of schizophrenia in children under 18 years old is not available.

Manic episodes in the structure of moderate to severe bipolar disorder

degrees

Adults.

The recommended initial dose of the drug -2 mg per day at a time. At

If necessary, this dose can be increased by at least 24 hours at 1 mg per day. For most patients, the optimal dose is from 1-6 mg per day.

Elderly patients.

An initial dose of 0.5 mg per dose is recommended twice a day. If necessary, the dose can be individually increased by 0.5 mg twice a day to a dose of 1 to 2 mg twice a day. In prescribing the drug in elderly patients, care must be taken.

Children

Information on the use of the drug for the treatment of manic episodes in the structure

bipolar disorder of moderate and severe in children under 18 years of age are absent.

Persistent aggression in patients with dementia due to illness

Moderate and severe alzheimer's

An initial dose of 0.25 mg per dose twice a day is recommended.The dose, if necessary, can be individually increased by 0.25 mg 2 times a day, not more often than every other day. For most patients, the optimal dose is 0.5 mg twice a day. However, some patients are shown taking 1 mg 2 times a day. Risperidone should not be used for longer than 6 weeks in the treatment of ongoing aggression in patients with moderate to severe Alzheimer's disease.

Continuing aggression in behavior disorder in children 5-16 years of age with moderate and severe mental retardation

Influence on ability to drive motor transport and control mechanisms

Risperidone may affect activity that requires a quick response:

patients should be advised not to drive a car or work with appliances until

finding out their individual sensitivity to the drug.

In a dry, dark place, at a temperature not higher than 25 ° C.

Keep out of the reach of children