Neurispin

Neurispin is an antipsychotic with the active ingredient risperidone.

Indications Neurispina

It is used in various types of schizophrenia (including new-onset psychosis, which is acute in nature, acute or chronic stage of schizophrenia) and other psychotic conditions accompanied by intense productive (including hallucinations, delusions, feelings of suspicion or aggression and thought disorders) or negative (including social and emotional alienation, dulling affect and speech impoverishment) symptoms.

Reduces affective manifestations (feelings of anxiety or fear and depression) in people with schizophrenia and schizoaffective disorders.

Used in long-term maintenance treatment to prevent relapses during the chronic stage of schizophrenia (acute psychotic states).

It is prescribed for behavioral forms of disorders in people with dementia and signs of aggression (use of physical violence and outbursts of strong anger), behavioral disorders (agitation and feelings of anxiety), or in cases of predominance of psychotic manifestations.

Behavioral disorders in situations where antisocial or aggressive behavior are the main symptoms of the pathology.

Elimination of manic reactions in bipolar disorder.

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Release form

The drug is released in tablets (volume 0.5, 1, 2, and 4 mg), 10 pieces in a plate, 2 plates in a box. It can also be released in plastic containers - 100 tablets of 1, 2 or 4 mg.

Pharmacodynamics

The drug belongs to the group of antipsychotics, is a derivative of benzisoxazole, a selective monoaminergic antagonist. It has a pronounced affinity for 5-HT2-endings of serotonin and D2-endings of dopamine. In addition, it is synthesized with α1-adrenoreceptors and, with slightly lower affinity, with α2-adrenoreceptors and H1-endings of histamine. It has no affinity for cholinergic receptors.

As a very strong D2-antagonist, risperidone has a weaker depressant effect on motor activity and also significantly weaker induces catalepsy processes (in comparison with standard neuroleptics). The balanced central antagonism exerted by risperidone on serotonin with dopamine reduces the intensity of extrapyramidal negative manifestations and expands the medicinal effect of the drug on the negative and affective signs of schizophrenia.

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Pharmacokinetics

Risperidone absorption is complete, without reference to food intake. Plasma Cmax values are noted after 1-2 hours. Synthesis with intraplasmic protein (albumin, as well as α1-acid glycoprotein) is 88%.

It undergoes rapid distribution and penetrates into the tissues of the central nervous system; the distribution volume index is 1-2 ml/kg. Intrahepatic metabolic processes involving the isoenzyme P450IID6 lead to the formation of the active element 9-hydroxyrisperidone, which is synthesized with protein by 77%. Partially, metabolic processes develop through N-dealkylation. Equilibrium values for the active component are recorded after 24 hours, and for 9-hydroxyrisperidone - after 4-5 days.

The half-life of risperidone is 3 hours, the component 9-hydroxyrisperidone is 24 hours. After 7 days of use, 70% of the drug is excreted in the urine, and another 14% through the gastrointestinal tract. 35-45% is excreted in the form of active ingredients.

In elderly people or people with renal insufficiency, with a single use of the drug, increased plasma levels and slow excretion of risperidone are observed.

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Dosing and administration

The medication should be taken orally, without regard to food intake, 1-2 times a day.

Treatment of schizophrenia: on the 1st day – 2 mg, on the 2nd – 4 mg. Later, the dosage is maintained at 4 mg or, if necessary, adjusted individually for the patient. Often, 4-6 mg of the drug per day is prescribed. It should be taken into account that when using the drug in a daily dose exceeding 10 mg, there is no increase in therapeutic efficacy, but the likelihood of extrapyramidal symptoms increases.

For people with kidney or liver failure, as well as for the elderly, therapy begins with a dosage of 0.5 mg 2 times a day, and then gradually increases it to 1-2 mg 2 times a day.

Behavioral disorders in people with dementia: the initial dosage is 0.25 mg, taken twice a day; if necessary, the dosage can be increased by +0.25 mg twice a day, but this is allowed at least every other day. The usual dosage is 0.5 mg twice a day, but some patients may require 1 mg of the substance twice a day.

Associated with manias BAR: the initial dose is 2 mg per day in 1 use; if necessary, the dosage is increased by +2 mg per day, but this is done at least every other day. Basically, the intake of 2-6 mg per day is prescribed.

Behavioral disorders in people with intellectual disabilities or with dominant destructive reactions: people weighing more than 50 kg should use 0.5 mg per day once, and then increase the dosage by +0.5 mg per day (every other day), if necessary. People weighing less than 50 kg are initially prescribed 1-time use of 0.25 mg per day; the dosage can be increased every other day by +0.25 mg per day. The optimal dose is 0.5 mg of the drug per day.

After achieving the optimal result, the use of the drug can be reduced to 1 dose per day. The maximum daily dose is 16 mg.

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Use Neurispina during pregnancy

Neurispin is prescribed during pregnancy only in situations where the benefits of treatment are more likely than the risks of complications for the fetus.

Contraindications

Contraindicated for use in case of personal intolerance, as well as during breastfeeding.

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Side effects Neurispina

Side effects include:

• damage to the central nervous system function together with the sensory organs: agitation, headaches, insomnia and anxiety often occur. Sometimes dizziness, fatigue or drowsiness, visual acuity and concentration disorders may occur. Extrapyramidal symptoms (rigidity, akathisia, tremor with bradykinesia, hypersalivation and acute dystonia) occasionally occur, thermoregulation disorders, seizures, NMS and dyskinesia may appear in the late stage;
• digestive disorders: dyspepsia, vomiting, abdominal pain, nausea, constipation and increased liver enzyme levels;
• problems with the functioning of the cardiovascular system and the blood system: occasionally observed are reflex tachycardia, hypervolemia, orthostatic collapse, some decrease in the level of platelets or neutrophils and stroke (in elderly people with predisposing factors);
• disorders affecting the endocrine system: gynecomastia, amenorrhea with galactorrhea, weight gain and menstrual cycle disorders. Occasionally, diabetes worsens or hyperglycemia develops;
• lesions of the reproductive system: occasionally problems with ejaculation, erection and orgasm appear, as well as priapism;
• allergy symptoms: occasionally observed Quincke's edema, runny nose and rashes on the epidermis;
• Others: urinary incontinence sometimes occurs.

Overdose

Signs of poisoning include: development of a strong sedative effect, feeling of drowsiness, decreased blood pressure, tachycardia and extrapyramidal manifestations. Increased QT interval readings on ECG are occasionally observed.

Treatment involves ensuring unimpeded air flow through the respiratory tract to maintain adequate oxygen supply and ventilation. Gastric lavage and administration of a laxative with activated charcoal are also performed, and ECG values are monitored to detect possible cardiac arrhythmias. Symptomatic measures are also taken to support the functioning of vital organs.

If vascular collapse develops and blood pressure values decrease, infusion or sympathomimetics are administered. If extrapyramidal signs appear, anticholinergic agents are prescribed.

Neurispin has no anthrax. Regular monitoring of the victim's condition is necessary until all signs of poisoning disappear.

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Interactions with other drugs

The combined use of risperidone and agents that are antagonists of dopamine endings leads to the appearance of late-onset dyskinesia (involuntary rhythmic movements - mainly of the face or tongue), which is why it is necessary to cancel the administration of any antipsychotics.

Risperidone may exhibit antagonistic effects on levodopa.

Tricyclics with phenothiazines, fluoxetine and β-blockers can increase blood levels of risperidone without affecting the level of the active antipsychotic fraction.

Combination with carbamazepine, as well as other agents that induce liver enzymes, leads to a decrease in the activity of the antipsychotic fraction of the drug in the blood. After discontinuing the administration of such substances, it is necessary to review the dosage of Neurispin.

If additional sedative effect is required, benzodiazepine derivatives are prescribed along with the medication.

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Storage conditions

Neurispin should be stored in a dark and dry place, out of the reach of small children. Temperature indicators are in the range of 15-30°C.

Shelf life

Neurispin can be used within a 24-month period from the date of manufacture of the pharmaceutical product.

Application for children

There is insufficient information regarding the effectiveness and safety of the drug in pediatrics. Do not prescribe to persons under 15 years of age.

Analogues

The analogs of the drug are Rileptid, Risset with Rispaksol, and also Rispolept with Risperone and Eridon with Rispertrile.

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