Rispolept solution for oral administration 1 mg/ml 30 ml

Dosage form

Oral solution

Composition

Risperidone

Excipients: tartaric acid; benzoic acid; sodium hydroxide; purified water

Packing

30 ml

Mechanism of action

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

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

It is also associated with α1-adrenergic receptors and somewhat weaker with H1-histaminergic and α2-adrenergic receptors.

Does not possess tropism for cholinergic receptors.

Antipsychotic action is due to the blockade of the D2-dopaminergic receptors of the mesolimbic and mesocortical system.

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

Antiemetic effect - blockade of dopamine D2-receptors of the trigger zone of the vomiting center.

Hypothermic effect - blockade of dopamine receptors of the hypothalamus.

Risperidone reduces the productive symptoms of schizophrenia (delusions, hallucinations), aggressiveness, automatism.It causes less suppression of motor activity and to a lesser extent induces catalepsy than classical 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.

May cause a dose-dependent increase in plasma prolactin concentration.

Indications and usage

Relief of acute attacks and long-term maintenance therapy of the following conditions:

acute and chronic schizophrenia and other psychotic disorders with productive and negative symptoms;

affective disorders in various mental illnesses;

behavioral disorders in patients with dementia with symptoms of aggressiveness (outbreak of anger, physical abuse), impaired activity (agitation, delirium) or psychotic symptoms;

behavioral disorders in adolescents from 15 years and adult patients with reduced intellectual level or mental retardation, in cases where destructive behavior (aggressiveness, impulsivity, auto-aggression) is leading in the clinical picture of the disease.

Stabilization of mood in the treatment of mania with bipolar disorders - as a means of adjuvant therapy.

Contraindications

individual hypersensitivity to the drug;

lactation period.

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

dehydration and hypovolemia;

disorders of cerebral circulation;

Parkinson's disease;

convulsions (including in history);

severe renal or hepatic impairment (see “Dosage and Administration”);

drug abuse or drug dependence (see “Dosage and administration”);

conditions predisposing to the development of tachycardia of the “pirouette” type (bradycardia, electrolyte imbalance, concomitant medication taking, extending the QT interval);

brain tumor, intestinal obstruction, cases of acute drug overdose, Reye's syndrome - the antiemetic effect of Risperidone may mask the symptoms of these conditions;

pregnancy;

children's age up to 15 years (efficiency and safety are not established).

Pregnancy and Breastfeeding

The positive effect justifies the possible risk.

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

Dosage and administration

Inside

A. Schizophrenia

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

Initial dose - 2 mg / day; on the second day, the dose should be increased to 4 mg / day. From this point on, the dose is either kept at the same level, or, if necessary, individually adjusted. 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 do not have a higher efficacy compared with smaller ones and can cause the appearance of extrapyramidal symptoms. Due to the fact that the safety of doses above 16 mg / day has not been studied, they cannot be used.

Benzodiazepines can be added to Rispolepit therapy if additional sedation is required.

Information on the use for the treatment of schizophrenia in children younger than 15 years old is not available.

Elderly patients: the recommended initial dose is 0.5 mg 2 times a day. The dosage can be individually increased by 0.5 mg 2 times a day to 1-2 mg 2 times a day.

Liver and kidney diseases: the recommended initial dose is 0.5 mg per dose 2 times a day. This dose can be gradually increased to 1-2 mg 2 times a day.

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

B. Behavioral disorders in patients with dementia

The recommended initial dose is 0.25 mg 2 times a day. The dosage, 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 2 times a day. However, some patients are shown taking a dose of 1 mg 2 times a day.

Upon reaching the optimal dose, it may be recommended to take the drug once a day.

B. Bipolar Disorders (Mania)

The recommended initial dose of the drug - 2 mg per day for 1 reception. If necessary, this dose can be increased by 2 mg per day, no more than a day.For most patients, the optimal dose is 2-6 mg / day.

D. Behavioral disorders in patients with mental retardation or with the dominance in the clinical picture of destructive tendencies

Patients weighing 50 kg or more: the recommended initial dose of the drug is 0.5 mg 1 time per day. If necessary, this dose can be increased by 0.5 mg per day, no more than every other day. For most patients, the optimal dose is 1 mg per day. However, for some patients, it is preferable to take 0.5 mg per day, while some require an increase in dose to 1.5 mg per day.

Patients weighing less than 50 kg: the recommended initial dose of the drug - 0.25 mg 1 time a day. If necessary, this dose can be increased by 0.25 mg per day, no more than every other day. For most patients, the optimal dose is 0.5 mg per day. However, for some patients it is preferable to take 0.25 mg per day, while some require an increase in the dose to 0.75 mg per day.

Long-term reception of Rispolept in adolescents should be carried out under the constant supervision of a physician.

Use in children under 15 is not recommended.

Adverse reactions

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 due to the syndrome of inadequate secretion of ADH), tardive dyskinesia (involuntary rhythmic movements mainly of the tongue and / or face), neuroleptic malignant syndrome (hyperthermia, muscle rigidity, instability of autonomous functions, impaired consciousness and increased creatine phosphokinase), thermoregulation disorders and epileptic seizures.

Gastrointestinal: constipation, dyspepsia, nausea or vomiting, abdominal pain, increased liver enzymes, dry mouth, hypo-or hypersalivation, anorexia, increased appetite, increased or decreased body weight.

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

From the side of blood-forming organs: neutropenia, thrombocytopenia.

On the part of the endocrine system: galactorrhea, gynecomastia, menstrual disorders and amenorrhea; in very rare cases, the occurrence of hyperglycemia and exacerbation of preexisting diabetes in patients has been reported.

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

Allergic reactions: rhinitis, rash, angioedema, photosensitization.

On the part of the skin: dry skin, hyperpigmentation, itching, seborrhea.

Other: arthralgia.

Given the fact that Rispolept® has an impact primarily on the central nervous system, it should be used with caution in combination with other drugs of central action and with alcohol.

Rispolept® reduces the effectiveness of levodopa and other dopamine agonists.

Clozapine reduces the clearance of risperidone.

When using Carbamazepine, a decrease in the concentration of active antipsychotic fraction of Rispolept in plasma was observed. Similar effects can be observed when using other hepatic enzyme inducers.

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

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

When using Rispolepta along with other drugs that are highly bound to plasma proteins, there is no clinically pronounced displacement of any drug from the plasma protein fraction.

Antihypertensive drugs - increased severity of blood pressure reduction on the background of risperidone.

Symptoms: These are already known pharmacological effects of the drug in an enhanced form - drowsiness, sedation, tachycardia, hypotension, extrapyramidal symptoms. It was reported about reception to 360 mg of a preparation. The data obtained suggest a wide range of drug safety.In rare cases, overdose was noted prolongation of the QT interval.

In the case of an acute overdose with a combination therapy, the possibility of involving the effects of several drugs in symptomatology should be analyzed.

Treatment: free airway should be achieved and maintained to ensure an adequate supply of oxygen and ventilation, gastric lavage (after intubation, if the patient is unconscious), and the appointment of Activated carbon with laxative. ECG monitoring should be immediately started to detect possible arrhythmias.

There is no specific antidote, appropriate symptomatic therapy should be carried out. Arterial hypotension and vascular collapse should be eliminated by IV fluids and / or sympathomimetic drugs. If acute extrapyramidal symptoms develop, anticholinergic drugs should be prescribed. Constant medical observation and monitoring should be continued until the symptoms of intoxication disappear.