Risperidone tablets 2mg, # 20

• Treatment of schizophrenia (including acute psychosis for the first time, acute attack of schizophrenia, chronic schizophrenia);

• psychotic states with pronounced productive (hallucinations, delusions, thought disorders, hostility, suspicion) and / or negative (dull affect, emotional and social detachment, poor speech) symptoms;

• to reduce affective symptoms (depression, guilt, anxiety) in patients with schizophrenia;

• prevention of relapses (acute psychotic conditions) in the chronic course of schizophrenia;

• treatment of behavioral disorders in patients with dementia with symptoms of aggression (outbursts of anger, physical violence), mental disorders (agitation, delirium) or psychotic symptoms;

• treatment of manias in bipolar disorder (as a mood stabilizer as an adjuvant therapy).

Individual. For oral administration, the initial dose for adults is 0.25-2 mg / day, on the 2nd day - 4 mg / day. Further, the dose can either be kept at the same level, or, if necessary, adjusted. Usually, the optimal therapeutic dose, depending on the indications, is in the range of 0.5-6 mg / day. In some cases, a slower dose increase and lower initial and maintenance doses may be justified.

In schizophrenia for elderly patients, as well as with concomitant liver and kidney diseases, an initial dose of 500 mcg 2 times / day is recommended. If necessary, the dose can be increased to 1-2 mg 2 times / day.

Maximum dose: when using risperidone at a dose of more than 10 mg / day, there is no increase in efficacy compared to lower doses, but the risk of developing extrapyramidal symptoms increases. The safety of using risperidone in doses exceeding 16 mg / day has not been studied, therefore, further excess of the dose is not allowed.

White or almost white film-coated tablets

1 tab.

risperidone 2 mg

Hypersensitivity to risperidone.

pharmachologic effect

An antipsychotic agent (neuroleptic), a benzisoxazole derivative. It has a high affinity for serotonin 5-HT2 and dopamine D2 receptors. It binds to ? 1-adrenergic receptors and, with slightly lower affinity, to histamine H1 receptors and ? 2-adrenergic receptors. Has no affinity for cholinergic receptors. Although risperidone is a potent D2 antagonist (which is believed to be the main mechanism for improving the productive symptoms of schizophrenia), it causes less pronounced suppression of motor activity and induces less catalepsy than classical antipsychotics. Due to the balanced antagonism to serotonin and dopamine receptors in the central nervous system, the likelihood of developing extrapyramidal side effects decreases.

Risperidone can induce a dose-dependent increase in plasma prolactin concentration.

Pharmacokinetics

After oral administration, risperidone is completely absorbed from the gastrointestinal tract, Cmax in plasma is achieved within 1-2 hours. Food does not affect the absorption of risperidone.

The Css of risperidone in the body in most patients is reached within 1 day. The css of 9-hydroxyrisperidone is reached within 4-5 days. Plasma concentrations of risperidone are dose-proportional (in the therapeutic dose range).

Risperidone is rapidly distributed in the body, Vd is 1-2 l / kg. In plasma, risperidone binds to albumin and alpha1-glycoprotein. Plasma protein binding of risperidone is 88%, 9-hydroxyrisperidone - 77%.

Risperidone is metabolized in the liver with the participation of the isoenzyme CYP2D6 to form 9-hydroxyrisperidone, which has a pharmacological effect similar to risperidone. The antipsychotic effect is due to the pharmacological activity of risperidone and 9-hydroxyrisperidone. Another metabolic pathway for risperidone is N-dealkylation.

After oral administration in patients with psychosis, T1 / 2 of risperidone from plasma is 3 hours. T1 / 2 of 9-hydroxyrisperidone and the active antipsychotic fraction is 24 hours.

After 1 week of admission, 70% is excreted in the urine, 14% in the feces. In urine, the total content of risperidone and 9-hydroxyrisperidone is 35-45%. The rest is inactive metabolites.

In elderly patients and in patients with renal insufficiency, after a single oral administration, increased plasma concentrations and delayed excretion of risperidone were observed.

Side effect

From the side of the central nervous system: often - insomnia, agitation, anxiety, headache; possible - drowsiness, fatigue, dizziness, impaired ability to concentrate, impaired clarity of vision; rarely - extrapyramidal symptoms (including tremor, rigidity, hypersalivation, bradykinesia, akathisia, acute dystonia). Patients with schizophrenia may have tardive dyskinesia, NNS, impaired thermoregulation, and seizures.

From the digestive system: constipation, dyspeptic symptoms, nausea, vomiting, abdominal pain, increased activity of liver enzymes.

From the reproductive system: priapism, erectile dysfunction, ejaculation disorders, orgasm disorders.

From the side of the cardiovascular system: rarely - orthostatic hypotension and reflex tachycardia, arterial hypertension.

From the endocrine system: galactorrhea, gynecomastia, menstrual irregularities, amenorrhea, weight gain.

From the hematopoietic system: a slight decrease in the number of neutrophils and / or platelets.

Allergic reactions: rhinitis, skin rash, angioedema.

Others: urinary incontinence.

Application during pregnancy and lactation

Use during pregnancy is possible if the expected benefit of therapy to the mother outweighs the potential risk to the fetus. If necessary, use during lactation, breastfeeding should be discontinued.

Application for violations of liver function

In schizophrenia with concomitant liver diseases, an initial dose of 500 mcg 2 times / day is recommended. If necessary, the dose can be increased to 1-2 mg 2 times / day.

Application for impaired renal function

In schizophrenia with concomitant kidney disease, an initial dose of 500 mcg 2 times / day is recommended. If necessary, the dose can be increased to 1-2 mg 2 times / day.

Application in children

There are no data on the safety of using risperidone in children under 15 years of age.

Use in elderly patients

In schizophrenia, for elderly patients, an initial dose of 500 mcg 2 times / day is recommended. If necessary, the dose can be increased to 1-2 mg 2 times / day.

special instructions

Use with caution in patients with diseases of the cardiovascular system (including heart failure, myocardial infarction, cardiac muscle conduction disorders), as well as dehydration, hypovolemia or cerebrovascular disorders. In this category of patients, the dose should be increased gradually.

The risk of developing orthostatic hypotension is especially increased during the initial period of dose selection. If hypotension occurs, dose reduction should be considered.

With the use of drugs with the properties of dopamine receptor antagonists, the occurrence of tardive dyskinesia, characterized by involuntary rhythmic movements (mainly of the tongue and / or face), was noted. There are reports that the occurrence of extrapyramidal symptoms is a risk factor for the development of tardive dyskinesia. Risperidone causes the appearance of extrapyramidal symptoms to a lesser extent than classical antipsychotics. If symptoms of tardive dyskinesia appear, consideration should be given to discontinuing all antipsychotics.

If NMS develops, it is necessary to discontinue all antipsychotics, including risperidone.

Risperidone should be used with caution in patients with Parkinson's disease, since it is theoretically possible to worsen this disease.

It is known that classical antipsychotics reduce the seizure threshold. With this in mind, risperidone is recommended to be used with caution in patients with epilepsy.

Risperidone should be used with caution in combination with other centrally acting drugs.

With the abolition of carbamazepine and other inducers of hepatic enzymes, the dose of risperidone should be reviewed and, if necessary, reduced.

During the period of treatment, patients should be advised to refrain from overeating due to the possibility of increasing body weight.

There are no data on the safety of using risperidone in children under 15 years of age.

Influence on the ability to drive vehicles and use mechanisms

During the period of treatment, until the individual sensitivity to risperidone is ascertained, patients should avoid driving vehicles and other activities that require high concentration of attention and speed of psychomotor reactions.

Drug interactions

With the simultaneous use of inducers of microsomal liver enzymes, it is possible to reduce the concentration of risperidone in the blood plasma.

With simultaneous use with phenothiazine derivatives, tricyclic antidepressants and beta-blockers, an increase in the concentration of risperidone in blood plasma is possible.

With simultaneous use with carbamazepine, the concentration of risperidone in the blood plasma is significantly reduced.

With the simultaneous use of risperidone reduces the effects of levodopa and other dopamine receptor agonists.

With simultaneous use with fluoxetine, an increase in the concentration of risperidone in blood plasma is possible.