Rispolux 4 mg, 20 pcs.

Rispolux has neuroleptic and antipsychotic effects.

Pharmacodynamics

Antipsychotic (neuroleptic), a benzisoxazole derivative; also has sedative, antiemetic and hypothermic effects.

A selective monoaminergic antagonist, has high tropism to serotonergic 5-NT₂– and dopaminergic D₂-receptors, also binds to alpha₁-adrenoceptors and somewhat weaker to H₁-histaminergic and alpha₂-adrenergic receptors. It has no tropism to cholinergic receptors.

Risperidone is particularly effective in the treatment of schizophrenia with productive symptoms (delirium, hallucinations, aggression), also has a positive effect in negative symptoms.

The balanced central antagonism to serotonin and dopamine may reduce the propensity for extrapyramidal side effects and extend the therapeutic effects of the drug to include negative and affective symptoms of schizophrenia. Causes less suppression of motor activity and is less likely to induce catalepsy than classical antipsychotic neuroleptics.

Pharmacokinetics

Risperidone is completely absorbed after oral administration, reaching C_max in plasma after 1-2 h. Food intake has no effect on the completeness and rate of absorption.

Metabolism is via cytochrome P450 CYP2D6 to form 9-hydroxyrisperidone, which has pharmacological activity comparable to that of risperidone. Risperidone and 9-hydroxysperidone constitute the so-called neuroleptic fraction. Risperidone also undergoes an N-dealkylation reaction.

T_1/2 is about 24 h for 9-hydroxyrisperidone and the neuroleptic fraction as a whole.

In oral administration, 70% of the dose of risperidone is excreted by the kidneys (35-45% as a pharmacologically active fraction), 14% – in the bile.

Plasma clearance with oral administration is 1.667 ml/s.

Stable concentrations of risperidone in blood of the majority of patients are achieved within the first day of treatment, 9-hydroxirisperidone – on the 4th-5th day. Plasma concentrations of risperidone are proportional to the dose of the drug (within the therapeutic doses).

In elderly patients, as well as in patients with renal insufficiency, plasma concentrations of the drug are increased and the elimination half-life is longer. Plasma concentrations of risperidone in patients with hepatic impairment do not change.

Indications

Active ingredient

Composition

Active ingredient: risperidone 4 mg;

Excipients: lactose monohydrate; MCC; pregelatinized starch; croscarmellose sodium; sodium lauryl sulfate; anhydrous colloidal silica; magnesium stearate

How to take, the dosage

Ingestion, regardless of meals, with water.

Adults and children over 15 years of age.

The initial dose of Rispolux® for all patients (in acute and chronic cases) is 2 mg/day (in 1 or 2 doses), on the second day to 4 mg/day; further, if necessary, the dose may be increased or decreased in 1-2 mg at weekly intervals. Doses above 10 mg/day have not been shown to be more effective than lower doses and may cause extrapyramidal symptoms. The maximum daily dose is 16 mg.

Benzodiazepines may be administered concomitantly with Rispolux® if sedation is required.

Hepatic and/or renal impairment and elderly patients.The recommended starting dose of Rispolux® is 0.5 mg 2 times daily. This dose can be gradually (0.5 mg) increased to 1-2 mg per dose 2 times a day.

When switching to Rispolux® treatment, a gradual withdrawal of the previously taken neuroleptic drug is recommended. If a depot neuroleptic for parenteral administration was previously used, the first dose of Rispolux® should be taken instead of an injection according to the depot neuroleptic administration regimen.

Interaction

Antacids decrease absorption of oral neuroleptics.

Risperidone decreases the effectiveness of levodopa and other dopamine agonists.

Hypotensive drugs increase the severity of BP reduction during administration of risperidone.

Phenothiazine neuroleptics, tricyclic antidepressants and some beta-adrenoblockers when concomitantly administered with risperidone may increase its plasma concentration without affecting the concentration of the neuroleptic fraction.

Carbamazepine and other hepatic enzyme inducers decrease the plasma concentration of the active fraction of risperidone.

Concomitant administration of fluoxetine increases plasma concentrations of risperidone, but levels of the neuroleptic fraction increase only slightly.

Neuroleptics increase the effects of alcohol, antihistamines, benzodiazepines and other drugs that depress the CNS.

Special Instructions

Because Risolux®® administration may result in weight gain, dietary advice should be given to the patient.

If orthostatic hypotension occurs, especially at the beginning of treatment, dose reduction should be considered. In patients with cardiac disease, as well as in dehydration, hypovolemia, or cerebrovascular disorders, the dose should be increased gradually.

The dose of Rispolux® should be reduced when carbamazepine and other hepatic enzyme inducers are withdrawn.

If symptoms of tardive dyskinesia or malignant neuroleptic syndrome occur, all antipsychotic medications, including Rispolux®, should be considered for withdrawal.

A gradual withdrawal of the drug is recommended because withdrawal syndrome (vomiting, nausea, increased sweating, insomnia) may develop after abrupt discontinuation of high-dose neuroleptic treatment.

When treating with risperidone, caution should be exercised when driving motor vehicles and engaging in other potentially hazardous activities requiring increased attention and rapid psychomotor reactions.

Contraindications

Hypersensitivity to risperidone or other components of the drug; period of lactation.

With caution:

Side effects

Allergic reactions: skin rash, rhinitis, pruritus, angioedema, anaphylactic shock,

CCC: orthostatic hypotension, reflex tachycardia, arterial hypertension, sinus bradycardia, 1st degree AV block, atrial fibrillation, syncope, peripheral edema.

Gastrointestinal disorders: dry mouth, nausea, vomiting, dyskinesia, dyspepsia, anorexia, abdominal pain, constipation, hypo- or hypersalivation, jaundice, dysphagia, gastritis, pancreatitis.

Nervous system disorders: Insomnia, headache, dizziness, agitation, restlessness, drowsiness, fatigue, decreased ability to concentrate, seizures; rarely, extrapyramidal disorders (tremor, rigidity, hypersalivation, bradykinesia, akathisia, acute dystonia), coordination disorders, speech disorders, hypersensitivity, sleep disorders; cerebral circulatory disorders (in older patients with predisposing factors).

In patients with schizophrenia: tardive dyskinesia (involuntary tongue movements and facial muscle contractions), malignant neuroleptic syndrome (hyperthermia, extreme muscle rigidity, impaired consciousness, autonomic disorders, increased creatine phosphokinase activity, tachypnea), epileptic seizures.

Urogenital system disorders: priapism, erectile dysfunction, anorgasmia, urinary incontinence, ejaculation disorders.

Endocrine system disorders: galactorrhea, gynecomastia, menstrual cycle disorders, hyperglycemia, hyperprolactinemia, disruption of antidiuretic hormone production.

Laboratory parameters: neutropenia, thrombocytopenia, anemia, granulocytopenia, agranulocytosis, increased ALT level, eosinophilia, leukopenia, increased AST level.

Others: dry skin, hyperpigmentation, photosensitization, hyperkeratosis, increased sweating, weight gain, arthralgia, myalgia, visual disturbances, mania, nasal congestion, nasal bleeding, sleep apnea, increased susceptibility to infection in elderly patients with dementia, polydipsia.

Overdose

Symptoms: drowsiness, sedation, tachycardia, arterial hypotension, extrapyramidal symptoms, rarely – QT interval prolongation.

Treatment: in acute overdose, ensure free airway patency to ensure adequate oxygen supply and ventilation, ECG monitoring, gastric lavage, administration of activated charcoal and laxatives; symptomatic therapy aimed at maintaining vital body functions; in the development of extrapyramidal symptoms – prescription of anticholinergic drugs. Continuous medical observation should be continued until complete disappearance of intoxication symptoms. There is no specific antidote.

Pregnancy use

The use of risperidone during pregnancy is possible only if the estimated benefit to the mother exceeds the potential risk to the fetus.

The drug is excreted in breast milk, therefore breastfeeding should be stopped when taking the drug.

Similarities