Expiration date: 07/2025

Structure and Composition:

Film-coated tablets. 1 tablet contains risperidone 1, 2, 3 or 4 mg

Excipients: Table. 1 mg - lactose, starch corn Valium MCC magnesium stearate silica colloidal anhydrous sodium lauryl sulfate, propylene glycol,

additionally: Table. 2 mg - titanium dioxide, talc, orange-yellow S Table. 3 mg - titanium dioxide talc quinoline yellow table. 4 mg - titanium dioxide talc quinoline yellow indigotindisulfonat

in blister 10 pcs. in box 2 or 6 blisters.

Description pharmaceutical form:

Tablets 1 mg: white, oblong, biconvex, film-coated, with Valium, with the words "Ris" and "1" - on one side. Color on a break - white.

Tablets 2 mg: light orange, oblong, biconvex, film-coated, with Valium, with the words "Ris" and "2" - on one side. Color on a break - white.

Tablets 3 mg: Yellow, oblong, biconvex, film-coated, with Valium, with the words "Ris" and "3" - on one side. Color on a break - white.

Tablets 4 mg: Green, oblong, biconvex, film-coated, with Valium, with the words "Ris" and "4" on - one side. Color on a break - white.

Pharmacokinetics:

Risperidone after oral completely absorbed, reaching Cmax plasma within 1-2 hours. Food does not affect the absorption of the drug, so risperidone can be administered independently from the meal.

It is rapidly distributed in the body. The volume of distribution of 1.2 l / kg. The plasma is associated with albumin and alpha-1-glycoprotein. Risperidone 88% bound plasma proteins, 9-hydroxy-risperidone - 77%.

The equilibrium concentration of risperidone in the body is achieved in most patients within one day. The equilibrium concentration of 9-hydroxy-risperidone achieved after 4-5 days. Risperidone plasma concentrations are proportional to the dose of the drug (in the range of therapeutic doses).

Risperidone is metabolized by cytochrome P450 enzyme CYP2D6 and 9-hydroxy-risperidone, which has a similar pharmacological action of risperidone. Risperidone and 9-hydroxy-risperidone constitute antipsychotic active fraction. Another way rispolept metabolism is N-dealkylation.

Following oral administration in patients with psychotic risperidone is released from T1 / 2 of about three hours. The T1 / 2 of 9-hydroxy-risperidone, and the active antipsychotic fraction is 24 hours.

After 1 week receive 70% of the dose is excreted in the urine, 14% - with the feces. In urine, risperidone and 9-hydroxy-risperidone constitute 35-45% of the dose. The remaining amount up inactive metabolites.

Study a single dose of the drug showed a higher plasma concentration and a slower elimination in the elderly and in patients with renal insufficiency. Risperidone plasma concentrations in patients with hepatic failure were normal.

Description of the pharmacological actions:

Rispolept (risperidone) - antipsychotic, benzisoxazole derivative, also has a sedative, antiemetic and hypothermic effect.

Risperidone - is a selective monoaminergic antagonist has a high affinity for 5-HT2 serotonergic and dopaminergic D2-receptors.

Associated also with & alpha1-adrenergic receptors and somewhat weaker with H1-histaminergic and alpha2-adrenergic & receptors.

It has no affinity for cholinergic receptors.

Antipsychotic effect due to blockade of dopamine D2-receptors and mesolimbic system Mesocortical.

Sedative effect due to blockade of adrenergic receptors of the reticular formation of the brain.

Antiemetic action - blockade of dopamine D2-receptor trigger zone of the vomiting center.

Hypothermic action - blockade of dopamine receptors of the hypothalamus.

Risperidone reduces the productive symptoms of schizophrenia (delusions, hallucinations), aggressiveness, automatism. It causes minimal suppression of motor activity and to a lesser extent induces catalepsy than classic antipsychotics. Balanced central antagonism of serotonin and dopamine may reduce the propensity for extrapyramidal side effects and enhance the therapeutic effects of the drug, covering the negative and affective symptoms of schizophrenia.

It may cause a dose-dependent increase in plasma prolactin concentration.

Testimony:

Mild acute and long-term maintenance therapy:

• acute and chronic schizophrenia and other psychotic disorders with productive and negative symptoms
  
• affective disorders in a variety of mental illnesses
  
• behavioral disturbances in patients with dementia with aggressive manifestation of symptoms (angry outbursts, physical violence), activity disturbances (agitation, delirium) or psychotic symptoms
  
• behavioral disorders in adolescents from 15 years and adult patients with reduced intellectual level or mental retardation, if the destructive behavior (aggressiveness, impulsivity, autoaggression) is leading the clinical picture of the disease.
  

Mood stabilization in treating mania in bipolar disorders - as a means of adjuvant therapy.

Contraindications:

• individual hypersensitivity to the drug
  
• lactation.
  

Carefully:

• diseases of the cardiovascular system (chronic heart failure, myocardial infarction, conduction disorders of the heart muscle)
  
• Dehydration and hypovolemia
  
• cerebrovascular accidents
  
• Parkinson's disease
  
• seizures (including history)
  
• severe renal or hepatic insufficiency (see. "Dosage and administration")
  
• drug abuse or drug dependence (see. "Dosage and administration")
  
• conditions that predispose to the development of tachycardia type "pirouette" (bradycardia, electrolyte imbalance, concomitant drugs prolonging the QT interval)
  
• brain tumor, intestinal obstruction, acute cases of drug overdose, Reye's syndrome - an antiemetic effect of risperidone may mask the symptoms of these conditions
  
• pregnancy
  
• Children up to age 15 years (effectiveness and safety have been established).
  

Application of pregnancy and breastfeeding:

Rispolept Safety in pregnant women has not been studied. Rispolept can be used during pregnancy only when the positive effect justifies the potential risk.

Since risperidone and 9-hydroxy-risperidone passes into breast milk, women using Rispolept should not breastfeed.

Side effect:

From the nervous system: insomnia, agitation, anxiety, headache, sometimes - drowsiness, fatigue, dizziness, impaired concentration, blurred vision, rarely - extrapyramidal symptoms: tremor, rigidity, hypersalivation, bradykinesia, akathisia, acute dystonia.

In patients with schizophrenia: hypervolemia (either due to polydipsia or because the syndrome of inappropriate secretion of ADH), tardive dyskinesia (involuntary rhythmic movements mainly language and / or persons), neuroleptic malignant syndrome (hyperthermia, muscle rigidity, instability of the autonomous functions, violation consciousness and awareness CPK), thermoregulation disorders and seizures.

From the digestive system: constipation, dyspepsia, nausea or vomiting, abdominal pain, elevated liver enzymes, dry mouth, hypo- or hypersalivation, anorexia, increased appetite, increased or decreased body weight.

Since the cardiovascular system: orthostatic hypotension, reflex tachycardia, increased blood pressure. Against the background described rispolept therapy for stroke, mostly in elderly patients with predisposing factors.

From the side of hematopoiesis: neutropenia, thrombocytopenia.

From endocrine system: galactorrhea, gynaecomastia, menstrual disorders and amenorrhea in very rare cases have been reported of the occurrence of hyperglycemia and exacerbation of preexisting diabetes mellitus patients.

With the genitourinary system: priapism, erectile dysfunction, abnormal ejaculation, anorgasmia, urinary incontinence.

Allergic reactions: rhinitis, rash, angioedema, fotosensebilizatsiya.

For the skin: dry skin, hyperpigmentation, itching, seborrhea.

Other: arthralgia.

Drug Interactions:

Given that Rispolept affects primarily the central nervous system, it should be used with caution in combination with other centrally acting drugs and alcohol.

Rispolept reduces the effectiveness of levodopa or other dopamine agonists.

Clozapine decreases clearance of risperidone.

When using carbamazepine marked reduction in the concentration of the active antipsychotic fraction plasma rispolept. Similar effects may be observed with other hepatic enzyme inducers.

Phenothiazines, tricyclic antidepressants and some blockers & beta-can increase the plasma concentrations of risperidone, but this does not affect the concentration of the active antipsychotic fraction.

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

When using rispolept together with other drugs that are highly bound to plasma proteins, clinically pronounced displacement of a drug from the plasma protein fraction is observed.

Antihypertensive drugs - enhanced the severity of blood pressure lowering on the background of risperidone.

Dosage and administration:

Inside.

A. Schizophrenia

Adults and children over 15 years - 1 or 2 times a day.

Initial dose - 2 mg / day on the second day the dose should be increased to 4 mg / day. Since then, the dose or remain at the same level, either individually adjusted if necessary. Usually the optimum dose is 4-6 mg / day. In some cases, it may be justified by a slower increase in the dose and lower initial and maintenance doses.

Doses above 10 mg / day did not have a higher efficiency as compared with smaller and may cause the appearance of extrapyramidal symptoms. Due to the fact that the safety of doses above 16 mg / day has not been studied, they can not be used.

For therapy rispolept benzodiazepines can add, if required additional sedation.

For information on the use for the treatment of schizophrenia in children under 15 years are not available.

Elderly patients: The recommended initial dose - 0.5 mg 2 times a day. The dosage can be individually increased by 0.5 mg 2 times per day to 1.2 mg two times a day.

Diseases of the liver and kidneys: The recommended initial dose - 0.5 mg per reception 2 times a day. This dose can be gradually increased to 2.1 mg 2 times a day.

Abuse of drugs or drug dependence: the recommended dose - 2-4 mg / day.

B. Behavioral disorders in patients with dementia

The recommended starting dose - 0.25 mg 2 times a day. If necessary dosage can be individually increased by 0.25 mg 2 times a day, no more than a day. For most patients, the optimal dose is 0.5 mg two times a day. However, some patients are shown receiving 1 mg 2 times a day.

On reaching the optimum dose of the drug can be recommended 1 time per day.

B. bipolar disorder (mania with)

The recommended initial dose - 2 mg per day for 1 admission. If necessary, this dose may be increased to 2 mg per day, no more than a day. For most patients the optimal dose is 2-6 mg / day.

D. Conduct disorders in patients with mental retardation or dominance in the clinical picture of the destructive trends

Patients weighing 50 kg and over: The recommended initial dose - 0.5 mg 1 time a day. If necessary, this dose may be increased to 0.5 mg per day, no more than a day. For most patients, the optimal dose is 1 mg per day. However, preferred for some patients receiving 0.5 mg per day, whereas some require increasing doses up to 1.5 mg per day.

Patients weighing less than 50 kg: the recommended initial dose - 0.25 mg 1 time a day. If necessary, this dose may be increased by 0.25 mg per day, no more than a day. For most patients, the optimal dose is 0.5 mg per day. However, preferred for some patients receiving 0.25 mg per day, whereas some require increasing doses up to 0.75 mg per day.

Long-term use rispolept adolescents should be carried out under the constant supervision of a physician.

Use in children under 15 years is not recommended.

Overdose:

Symptoms are the known pharmacological effects of the drug in a stronger form - drowsiness, sedation, tachycardia, hypotension, extrapyramidal symptoms. Reported receiving up to 360 mg. These data suggest a wide range of drug safety. In rare cases, the overdose was noted lengthening of the QT interval.

In case of acute overdose in combination therapy should examine the possibility of drawing in the symptoms of the effects of several drugs.

Treatment: should achieve and maintain a free airway to ensure adequate oxygen supply and ventilation, gastric lavage (after intubation if the patient is unconscious) and the appointment of activated charcoal together with a laxative. It is necessary to immediately begin ECG monitoring to detect possible arrhythmias.

There is no specific antidote, should carry out appropriate symptomatic therapy. Hypotension and circulatory collapse should be dealt with on / in the liquid infusions and / or sympathomimetic agents. In the case of severe extrapyramidal symptoms, anticholinergic agents should be appointed. Constant medical supervision and monitoring should continue until the disappearance of symptoms of intoxication.

Special instructions:

Transition from other antipsychotic therapy. In schizophrenia the beginning of treatment is recommended to gradually abolish rispolept previous therapy, if clinically justified. At the same time, if patients are transferred from the depot forms of therapy antipsychotics, it is recommended to start therapy rispolept instead of the next scheduled injection. Periodically evaluate the need to continue current therapy antiparkinsonian drugs.

In connection with the & alpha-blocking action may occur rispolept orthostatic hypotension, especially during the initial dose adjustment. In the event of hypotension should consider lowering the dose. In patients with diseases of the cardiovascular system, as well as dehydration, hypovolemia, or cerebrovascular disorders, the dose should be increased gradually, as recommended (see. "Dosage and administration").

It has been reported that the occurrence of extrapyramidal symptoms is a risk factor for the development of tardive dyskinesia. Rispolept rarely causes extrapyramidal symptoms than classical neuroleptics. If you have signs and symptoms of tardive dyskinesia should consider abolishing all antipsychotics.

In the case of development of neuroleptic malignant syndrome, characterized by hyperthermia, muscle rigidity, autonomic instability functions, impairment of consciousness and increased CPK level is necessary to cancel all antipsychotics, including Rispolept.

In case of cancellation of carbamazepine and other hepatic enzyme inducers rispolept dose should be reduced.

Patients should be advised to refrain from eating because of the possibility of weight gain.

Rispolept may have an impact on activities that require quick response: patients should be advised not to drive a car or operate machinery until they determine individual sensitivity to the drug.