Rispolept, oral solution 1mg/ml, 30ml

Composition

Active ingredient:

risperidone 1 mg;

Auxiliary substances:

tartaric acid;

benzoic acid;

sodium hydroxide;

purified water;

Pharmacological action

Rispolept is an antipsychotic drug derived from benzisoxazole. It also has sedative, antiemetic and hypothermic effects.

Risperidone is a selective monoaminergic antagonist with high affinity for serotonin 5-HT2 and dopamine D2 receptors. It binds to α1-adrenergic receptors and is slightly weaker-to histamine H1-receptors and α2-adrenergic receptors. It has no tropicity to cholinergic receptors.

The antipsychotic effect is due to the blockade of dopamine D2-receptors of the mesolimbic and mesocortical systems. Sedative effect is caused by blockade of adrenoreceptors of the reticular formation of the brain stem; antiemetic effect – blockade of dopamine D2-receptors of the trigger zone of the emetic center; hypothermic effect – blockade of dopamine receptors of the hypothalamus.

Risperidone reduces the productive symptoms of schizophrenia (delusions, hallucinations), aggressiveness, automatism, to a lesser extent causes suppression of motor activity and to a lesser extent induces catalepsy than classical antipsychotics. Balanced central antagonism to serotonin and dopamine can reduce the propensity for extrapyramidal side effects and expand the therapeutic effect of the drug on the negative and affective symptoms of schizophrenia.

Risperidone may cause a dose-dependent increase in plasma prolactin concentrations.

Pharmacokinetics

Suction

After oral use, risperidone is completely absorbed from the gastrointestinal tract. Cmax in plasma is reached after 1-2 hours. Food does not affect the absorption of the drug, so Rispolept can be prescribed regardless of food intake.

Distribution

Risperidone is rapidly distributed in the body. Vd is 1-2 l/kg. In plasma, risperidone binds to albumin and alpha-1-glycoprotein. Risperidone binds to plasma proteins by 88%,9-hydroxy-risperidone-by 77%.

Css of risperidone in the body in most patients is reached within 1 day.

Css of 9-hydroxy-risperidone is achieved within 4-5 days. Plasma concentrations of risperidone are proportional to the dose of the drug (within therapeutic doses).

Metabolism

Risperidone is metabolized in the liver with the participation of the CYP2D6 isoenzyme to form 9-hydroxy-risperidone, which has a pharmacological effect similar to risperidone. Risperidone and 9-hydroxy-risperidone constitute the active antipsychotic fraction. Another route of risperidone metabolism is N-dealkylation.

Deduction

After oral use in patients with psychosis, T1 / 2 of risperidone from plasma is about 3 hours. T1 / 2 of 9-hydroxy-risperidone 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 the urine, risperidone plus 9-hydroxy-risperidone account for 35-45% of the dose. The remaining amount is made up of inactive metabolites.

Pharmacokinetics in special clinical cases

In elderly patients and in patients with renal insufficiency, higher plasma concentrations and delayed elimination of risperidone were observed after a single oral use of the drug.

In patients with hepatic insufficiency, the concentration of risperidone in plasma did not change.

Indications

Relief of acute attacks and long-term maintenance therapy:

• acute and chronic schizophrenia and other psychotic disorders with productive and negative symptoms;
• affective disorders in various mental disorders,
• behavioral disorders in patients with dementia in the manifestation of symptoms of aggression (angry outbursts, physical violence), the impaired activity (agitation, delirium) or psychotic symptoms;
• behavioral disorders in adolescents 15 years and adult patients with reduced intellectual level or retardation in cases where destructive behavior (aggression, impulsivity, autoaggression) is leading to the clinical picture of the disease.

To stabilize mood in the treatment of mania in bipolar disorders (as an adjunct therapy).

Contraindications

• lactation period (breastfeeding);
• hypersensitivity to the components of the drug.

With caution, the drug should be used in patients with diseases of the cardiovascular system (including chronic heart failure, myocardial infarction, conduction disorders), dehydration, hypovolemia, impaired cerebral circulation, Parkinson’s disease, convulsions (including in the anamnesis), severe renal or hepatic insufficiency, drug abuse or drug dependence, with conditions predisposing to the development of tachycardia of the “pirouette” type (bradycardia, electrolyte imbalance, concomitant use of drugs that prolong the QT interval), in brain tumors, intestinal obstruction, in cases of acute drug overdose, in Reye’s syndrome (since the antiemetic effect of risperidone can mask the symptoms of these conditions), during pregnancy, in patients under 15 years of age (since the safety and effectiveness of the drug have not been established).

Side effects

From the central nervous system:  insomnia, agitation, anxiety, headache; sometimes-drowsiness, fatigue, dizziness, impaired concentration, visual clarity; rarely-extrapyramidal symptoms (tremor, rigidity, hypersalivation, bradykinesia, akathisia, acute dystonia). In patients with schizophrenia, hypervolemia (either due to polydipsia or due to the syndrome of inadequate ADH secretion), tardive dyskinesia (involuntary rhythmic movements mainly of the tongue and/or face), NMS (hyperthermia, muscle rigidity, instability of autonomic functions, impaired consciousness and increased CPK levels), thermoregulation disorders and convulsive seizures are possible.

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

From the cardiovascular system:  orthostatic hypotension and reflex tachycardia, increased blood pressure. Against the background of Rispolept therapy, the development of strokes is described mainly in elderly patients with predisposing factors.

From the hematopoietic system:  neutropenia, thrombocytopenia.

From the endocrine system:  galactorrhea, gynecomastia, menstrual disorders, amenorrhea are possible; in some cases, the development of hyperglycemia or worsening of the course of diabetes mellitus.

From the genitourinary system:  priapism, erectile dysfunction, ejaculation disorders, anorgasmia, urinary incontinence.

Allergic reactions:  rhinitis, skin rash, angioedema.

Dermatological reactions:  dry skin, hyperpigmentation, itching, seborrhea, photosensitization.

Other services:  arthralgia.

How to take, course of use and dosage

Inside, regardless of food intake.

Schizophrenia

Adults. Rispolept® can be prescribed 1 or 2 times a day. The initial dose of Rispolept® is 2 mg / day. On the second day, the dose should be increased to 4 mg / day. From this point on, 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 increase in the dose and lower initial and maintenance doses may be justified.

Doses higher than 10 mg / day do not show higher efficacy compared to lower 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.

Benzodiazepines may be added to Rispolept therapy if additional sedation is required.

Elderly patients. An initial dose of 0.5 mg twice daily is recommended. The dose can be individually increased by 0.5 mg 2 times a day to 1-2 mg 2 times a day.

Teenagers over the age of 13. An initial dose of 0.5 mg once daily in the morning or evening is recommended. If necessary, the dose can be increased after at least 24 hours by 0.5-1 mg per day to the recommended dose of 3 mg / day if well tolerated. The safety of doses above 6 mg / day has not been studied.

Patients with persistent drowsiness are recommended to take half the daily dose 2 times a day.

There is no information on the use of the drug for the treatment of schizophrenia in children under 13 years of age.

Behavioral disorders in patients with dementia

The recommended starting dose is 0.25 mg 2 times a day. The dose, if necessary, can be individually increased by 0.25 mg 2 times a day, no more than every other day. For most patients, the optimal dose is 0.5 mg 2 times a day. However, some patients are shown to take 1 mg 2 times a day.

When the optimal dose is reached, it may be recommended to take the drug once a day.

Bipolar disorders in mania

Adults. The recommended starting dose of the drug is 2 or 3 mg / day in one dose. If necessary, this dose can be increased by at least 1 mg/day after 24 hours. For most patients, the optimal dose is 1-6 mg / day.

Teenagers and children over 10 years old. An initial dose of 0.5 mg once daily in the morning or evening is recommended.If necessary, the dose can be increased at least 24 hours later by 0.5-1 mg/day to the recommended dose of 2.5 mg / day if well tolerated. For most patients, the optimal dose is 0.5-6 mg / day.

The safety of doses above 6 mg / day has not been studied.

Patients with persistent drowsiness are recommended to take half the daily dose 2 times a day.

There is no information on the use of the drug for the treatment of bipolar disorders in children under 10 years of age.

Behavioral disorders

Patients with a body weight of 50 kg or more. The recommended initial dose of the drug is 0.5 mg once a day. If necessary, this dose can be increased by 0.5 mg / day no more than every other day. For most patients, the optimal dose is 1 mg / day. However, for some patients,0.5 mg/day is preferable, while some require an increase in the dose to 1.5 mg / day.

Patients with a body weight of less than 50 kg. The recommended initial dose of the drug is 0.25 mg once a day. If necessary, this dose can be increased by 0.25 mg / day no more than every other day. For most patients, the optimal dose is 0.5 mg / day. However, for some patients,0.25 mg/day is preferable, while some require an increase in the dose to 0.75 mg / day.

Long-term use of Rispolept® in adolescents should be carried out under the constant supervision of a doctor.

Use in children under 5 years of age has not been studied.

Autism in children and adolescents

The dose of Rispolept® should be selected individually. The recommended starting dose of the drug is 0.25 mg / day for patients with a body weight of less than 20 kg and 0.5 mg / day for patients with a body weight of 20 kg or more. On the 4th day of use, the dose can be increased by 0.25 mg / day for patients with a body weight of less than 20 kg and by 0.5 mg / day per day for patients with a body weight of 20 kg or more.

This dose should be applied until approximately day 14 of treatment, when it is necessary to evaluate the effectiveness. A further increase in the dose is carried out only if there is no effectiveness. The dose can be increased at intervals of 2 weeks or more by 0.25 mg / day for patients weighing less than 20 kg and by 0.5 mg / day for patients weighing 20 kg or more.

In clinical trials, the maximum daily dose did not exceed 1.5 mg / day for patients weighing less than 20 kg and 2.5 mg / day for patients weighing 20 kg or more, and 3.5 mg / day for patients weighing more than 45 kg.

Overdose

Symptoms: drowsiness, sedation, tachycardia, hypotension, extrapyramidal symptoms. Up to 360 mg of the drug has been reported. The obtained data suggest a wide range of drug safety. In rare cases of overdose, prolongation of the QT interval was noted.

In the case of acute overdose with combination therapy, the possibility of involving other drugs should be analyzed.

Treatment: the airway should be kept clear to ensure adequate oxygen supply and ventilation. Gastric lavage is indicated (after intubation, if the patient is unconscious) and the appointment of activated charcoal along with a laxative. ECG monitoring should be started immediately to detect possible cardiac arrhythmias.

There is no specific antidote, and appropriate symptomatic therapy should be performed. In case of arterial hypotension and vascular collapse, intravenous infusion solutions should be administered and / or sympathomimetic drugs should be used. In case of acute extrapyramidal symptoms, anticholinergic drugs should be prescribed. Continuous medical supervision and monitoring should be continued until the symptoms of intoxication disappear.

Form of production

solution for oral use

Storage conditions

At a temperature of 15-30 °C. Do not freeze

Shelf life

3 years

Active ingredient

Risperidone

Conditions of release from pharmacies

By prescription

Dosage form

oral solution