Rispaksole, pills 4mg, 20pcs

Composition

Active ingredient:

risperidone 4 mg;

Auxiliary substances:

lactose anhydrous;

corn starch,

magnesium stearate,

colloidal anhydrous silicon dioxide;

microcrystalline cellulose

Pharmacological action

Rispaksole is an antipsychotic (neuroleptic), a derivative of benzisoxazole; it also has a sedative, antiemetic and hypothermic effect.

Risperidone is a selective monoaminergic antagonist with a pronounced affinity for serotonergic 5-HT2 and dopaminergic D2 receptors, also binds to alpha-1-adrenergic receptors and, with a slightly lower affinity, to Hl-histaminergic and alpha-2-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.

Reduces productive symptoms (delusions, hallucinations, aggressiveness), automatism. It causes less suppression of motor activity and induces catalepsy to a lesser extent than classical antipsychotics (neuroleptics).

Balanced central antagonism to serotonin and dopamine may reduce the risk of extrapyramidal symptoms. Risperidone may cause a dose-dependent increase in plasma prolactin concentrations.

Pharmacokinetics

When taken orally, risperidone is completely absorbed (regardless of food intake) and maximum plasma concentrations are observed after 1-2 hours.

Risperidone is metabolized by the P-450 IID6 cytochrome to form 9-hydroxyrisperidone, which has a similar pharmacological effect. Risperidone and 9-hydroxyrisperidone represent an effective antipsychotic fraction. When taken orally, risperidone is eliminated with a half-life of about 3 hours. The half-life of 9-hydroxyrisperidone and the active antipsychotic fraction was found to be 24 hours.

In most patients, the steady-state concentration of risperidone is observed one day after the start of treatment. In most cases, the equilibrium state of 9-hydroxyrisperidone is reached 3-4 days after the start of treatment. The concentration of risperidone in plasma is proportional to the dose of the drug (within therapeutic doses).

Risperidone is rapidly distributed in the body. The volume of distribution is 1-2 l/kg. In plasma, risperidone binds to albumin and a-1-glycoprotein. The binding of risperidone to plasma proteins is 88%,9-hydroxyrisperidone -77%.

Excreted by the kidneys-70% (35-45% of them in the form of a pharmacologically active fraction) and 14% – with bile. The remaining amount is accounted for by inactive metabolites.

In elderly patients, after a single oral dose of the drug, increased plasma concentrations of the active fraction were observed up to 30%, and in patients with renal insufficiency – up to 60%, as well as reduced clearance of the antipsychotic fraction. The presence of hepatic insufficiency does not affect the concentration of risperidone in plasma, but in such patients the average amount of free fraction in plasma was 35% higher.

Indications

• Schizophrenia (acute and chronic) and other psychotic states with a predominance of productive (delusions, hallucinations, aggressiveness), negative (blunted affect, emotional and social detachment, scarcity of speech) or affective (anxiety depression) symptoms; 
• behavioral disorders on the background of dementia (when symptoms of aggressiveness, activity disorders or psychotic symptoms appear) or mental retardation or reduced intelligence (when destructive behavior dominates);
• mania in bipolar disorders (auxiliary therapy).

Use during pregnancy and lactation

During pregnancy, it is possible if the intended benefit to the mother exceeds the potential risk to the fetus.

Category of action on the fetus according to the FDA-C.

Breast-feeding should be discontinued for the duration of treatment.

Contraindications

Hypersensitivity

Side effects

Nervous system and sensory disorders:  sleep disorders, including insomnia or drowsiness, increased excitability, fatigue, attention disorders, restlessness, anxiety, headache, dizziness, extrapyramidal disorders (rigidity, hypokinesia, hypersalivation, akathisia, acute dystonia), tardive dyskinesia, neuroleptic malignant syndrome, thermoregulation disorders, convulsive seizures, stroke (in predisposed elderly patients), blurred vision.

Cardiovascular and blood disorders (hematopoiesis, hemostasis):  orthostatic hypotension, reflex tachycardia, arterial hypertension, neutro-and thrombopenia, thrombocytopenic purpura.

From the digestive tract:  nausea, vomiting, dyspeptic symptoms, abdominal pain, constipation, increased levels of hepatic transaminases.

From the genitourinary system:  dysmenorrhea, amenorrhea, impotence, erectile and ejaculatory disorders, anorgasmia, decreased libido, priapism, polyuria, urinary incontinence, edema.

Allergic reactions:  skin rash, angioedema.

Other services:  rhinitis, galactorrhea, gynecomastia, weight gain, hypervolemia (due to polydipsia or inadequate secretion syndrome ADH), hyperglycemia (in patients with diabetes mellitus).

Interaction

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

Rispaksole reduces the effectiveness of levodopa and other dopamine agonists.

Clozapine reduces the clearance of risperidone.

Concomitant use of Rispaksole and carbamazepine resulted in a decrease in the concentration of the active antipsychotic fraction of risperidone in plasma. Similar effects can be observed with the use of other inducers of liver enzymes.

When used concomitantly with Rispaksole, phenothiazines, tricyclic antidepressants, and some beta-blockers may increase plasma concentrations of risperidone, but this does not affect the concentration of the active antipsychotic fraction.

When used concomitantly with Rispaksole, fluoxetine may increase the concentration of risperidone in plasma, but to a lesser extent the concentration of the active antipsychotic fraction.

When using Rispaksole together with other drugs that are highly bound to plasma proteins, clinically expressed displacement of any drug from the plasma protein fraction is not observed.

Antihypertensive drugs increase the severity of the decrease in blood pressure against the background of taking Rispaksole.

How to take, course of use and dosage

Rispaksole can be taken with a meal or in between meals; tablets can be washed down with a small amount of water.

Schizophrenia Adults and children over 15 years of age. Risperidone can be given once or twice a day. The initial dose is 2 mg per day. On the second day, the dose should be increased to 4 mg per 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 per 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 have not been shown to be more effective than lower doses and may cause extrapyramidal symptoms. Due to the fact that the safety of doses above 16 mg per day has not been studied, doses above this level should not be used. There is no information on use for the treatment of schizophrenia in children under 15 years of age.

Elderly patients.

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

Diseases of the liver and kidneys. An initial dose of 0.5 mg twice daily is recommended. This dose can be gradually increased to 1-2 mg taken twice a day. Drug abuse or drug dependence -the recommended daily dose of the drug is 2-4 mg.

Behavioral disorders in patients with dementia.

An initial dose of 0.25 mg twice daily is recommended (an adequate dosage form should be used). If necessary, the dosage 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 twice daily. 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.

Mania in bipolar disorders The recommended starting dose of the drug is 2 mg per day in one dose. If necessary, this dose can be increased by 2 mg per day, no more than every other day. For most patients, the optimal dose is 2-6 mg per day.

Behavioral disorders in patients with intellectual disability

Patients weighing 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 per day, no more than every other day. For most patients, the optimal dose is 1 mg per day.However, for some patients,0.5 mg per day is preferable, while some require an increase in the dose to 1.5 mg per day.

Patients weighing 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 per day, no more than every other day. For most patients, the optimal dose is 0.5 mg per day. However, for some patients, a dose of 0.25 mg per day is preferable, while some require an increase in the dose to 0.75 mg per day.

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

Use in children under 15 years of age is not recommended.

Overdose

Symptoms: drowsiness, sedation, depression of consciousness, tachycardia, hypotension, extrapyramidal disorders, in rare cases prolongation of the QT interval.

Treatment: it is necessary to ensure free airway patency to ensure adequate oxygenation and ventilation, gastric lavage (after intubation, if the patient is unconscious) and the appointment of activated charcoal in combination with laxatives. Symptomatic therapy aimed at maintaining vital body functions.

For timely diagnosis of possible cardiac arrhythmias, it is necessary to start ECG monitoring as soon as possible. Careful medical monitoring and ECG monitoring are performed until the symptoms of intoxication completely disappear. There is no specific antidote.

Composition

Tablet Form of production

Storage conditions

In a dark place, at a temperature not exceeding 25 °C

Shelf life

2 years

Active ingredient

Risperidone

Conditions of release from pharmacies

By prescription

Dosage form

Tablets