Rispaxol, 4 mg 20 pcs.

Rispaxol is an antipsychotic (neuroleptic), a benzisoxazole derivative; it also has sedative, antiemetic and hypothermic effects.

Risperidone is a selective monoaminergic antagonist with strong affinity for serotonergic 5-HT2 and dopaminergic D2 receptors, also binds to alpha1-adrenoceptors and, with some less affinity, to Hl-histaminergic and alpha2-adrenergic receptors. It has no tropinity to cholinoreceptors

Antipsychotic action is caused by blockade of dopamine D2-receptors of mesolimbic and mesocortical system.
Sedative action is caused by the blockade of adrenoreceptors of reticular formation of brain stem; antiemetic action – by the blockade of dopamine D2-receptors of trigger zone of the vomiting center; hypothermic action – by the blockade of dopamine receptors of hypothalamus.

Reduces productive symptomatology (delirium, hallucinations, aggression), automatism. Causes less suppression of motor activity and is less likely to induce catalepsy than classical antipsychotics (neuroleptics).

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

Pharmacokinetics

In oral administration, risperidone is completely absorbed (regardless of food intake) and maximum plasma concentrations are observed after 1-2 hours.

Risperidone is metabolized with participation of P-450 IID6 cytochrome to form 9-hydroxyrisperidone, which has similar pharmacological effects. Risperidone and 9-hydroxyrisperidone constitute an effective antipsychotic fraction.
When administered orally, risperidone is excreted with a half-life of about 3 hours. The half-life of 9-hydroxysperidone and the active antipsychotic fraction has been found to be 24 hours.

In most patients the equilibrium concentration of risperidone is observed one day after initiation of treatment. The equilibrium state of 9-hydroxysperidone in most cases 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 the 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-hydroxirisperidone -77%.

Extracted by the kidneys – 70% (of which 35 – 45% in the form of pharmacologically active fraction) and 14% – in the bile. The remaining amount falls on inactive metabolites.

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

Indications

Active ingredient

Composition

Active ingredient:

Spiridone 4 mg;

Supplements:

Lactose anhydrous;

Corn starch,

Magnesium stearate,

How to take, the dosage

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

Schizophrenia
Adults and children over 15 years of age.
Risperidone may be prescribed once or twice daily. The initial dose is 2 mg per day. On the second day, the dose should be increased to 4 mg per day. From then on, the dose can either be maintained at the same level or individually adjusted if necessary. Usually the optimal dose is 4-6 mg per day. In some cases, a slower dose increase and lower starting and maintenance doses may be warranted.

Doses above 10 mg daily have not been shown to be more effective than lower doses and may cause extrapyramidal symptoms. Because 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 less than 15 years of age.

Elderly patients.

The initial dose of 0.5 mg per dose twice daily is recommended. The dosage can be increased individually at 0.5 mg twice daily to 1 to 2 mg twice daily.

Hepatic and renal diseases.
The initial dose of 0.5 mg per dose 2 times a day is recommended. This dose can be gradually increased to 1 – 2 mg per dose twice a day.
Drug abuse or drug addiction – the recommended daily dose of the drug is 2-4 mg.

Behavioral disorders in patients with dementia.

The initial dose of 0.25 mg per dose twice daily is recommended (adequate dosage form should be used). The dosage can be increased individually to 0.25 mg twice daily if necessary, no more often than every other day. For most patients, the optimal dose is 0.5 mg twice a day. However, some patients are indicated to take 1 mg twice a day.

Once the optimal dose has been reached, once daily dosing may be recommended.

Mania in bipolar disorders
The recommended starting dose of the drug is 2 mg daily at a single dose. If necessary, this dose may be increased by 2 mg per day, no more often than every other day. For most patients the optimal dose is 2 to 6 mg per day.

Behavioral disorders in patients with mental retardation

Patients weighing 50 kg or more – the recommended starting dose of the drug is 0.5 mg once daily. If necessary, this dose may be increased by 0.5 mg daily, no more often than every other day. For most patients, the optimal dose is 1 mg daily. However, some patients prefer to take 0.5 mg daily, while some need to increase the dose to 1.5 mg daily.

Patients weighing less than 50 kg – the recommended starting dose of the drug is 0.25 mg once daily. If necessary, this dose may be increased by 0.25 mg daily, no more often than every other day. For most patients, the optimal dose is 0.5 mg daily. However, some patients prefer to take 0.25 mg daily, while some need to increase the dose to 0.75 mg daily.

Long-term administration of Risperidone in adolescents should be done under the constant supervision of a physician.

The use in children younger than 15 years is not recommended.

Interaction

Given that Rispaxol primarily affects the CNS, it should be used with caution in combination with other centrally acting drugs and ethanol.

Rispaxol decreases the effectiveness of levodopa and other dopamine agonists.

Clozapine decreases the clearance of risperidone.

In concomitant use of Rispaxol and carbamazepine, a decrease in the concentration of the active antipsychotic fraction of risperidone in plasma has been observed. Similar effects may be observed with other hepatic enzyme inducers.

Phenothiazines, tricyclic antidepressants and some beta-adrenoblockers may increase plasma concentrations of risperidone when used concomitantly with rispaxol, but this does not affect the concentration of the active antipsychotic fraction.

In concomitant use with rispaxol, fluoxetine may increase plasma concentrations of risperidone, but to a lesser extent the concentration of the active antipsychotic fraction.

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

Antihypertensive drugs increase the severity of BP reduction with Ripaxol.

Contraindications

Hypersensitivity

Side effects

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

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

Gastrointestinal system disorders: nausea, vomiting, dyspeptic complaints, abdominal pain, constipation, increased liver transaminases.

Hyrogenital system disorders: dysmenorrhea, amenorrhea, impotence, erection and ejaculation disorders, anorgasmia, decreased libido, priapism, polyuria, urinary incontinence, edema.

Allergic reactions: skin rash, angioedema.

Others: rhinitis, galactorrhea, gynecomastia, weight gain, hypervolemia (due to polydipsia or inadequate ADH secretion syndrome), hyperglycemia (in diabetic patients).

Overdose

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

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

For timely diagnosis of possible cardiac rhythm disturbances, ECG monitoring should be initiated as soon as possible. Close medical observation and ECG monitoring is carried out until symptoms of intoxication have completely disappeared. There is no specific antidote.

Pregnancy use

In pregnancy, it is possible if the estimated benefit to the mother outweighs the potential risk to the fetus.

The FDA fetal category is C.

Breastfeeding should be avoided during treatment.

Similarities