Neyrispin

Neuryspin is an antipsychotic. Contains element risperidone.

Indications Neuryspin

It is used in a variety of types of schizophrenia (among them, the first emerging psychosis, which is acute, acute or chronic stage of schizophrenia) and other psychotic states accompanied by intense productive (among them hallucinations, delusions, sense of suspicion or aggressiveness and mental disorders) or negative ( such social and emotional alienation, affect dullness and impoverishment of speech) signs.

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

It is used for long-term maintenance treatment to prevent recurrences during the chronic stage of schizophrenia (acutely psychotic states).

It is prescribed for behavioral forms of disorders in people with dementia and signs of aggressiveness (use of physical violence and an outbreak of strong anger), behavioral disorders (agitation and anxiety), or in the case of the prevalence of psychotic manifestations.

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

Elimination of manic reactions with BAR.

[1], [2]

Release form

The release of the element is made in tablets (volume 0.5, 1, 2, as well as 4 mg), 10 pieces per plate, 2 plates per box. It can also be produced inside plastic containers - 100 tablets of 1, 2 or 4 mg each.

Pharmacodynamics

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

As a very strong D2-antagonist, risperidone has a weaker inhibitory effect on motor activity, and also significantly less induces catalepsy processes (in comparison with standard antipsychotics). A balanced central antagonism of risperidone regarding serotonin with dopamine reduces the intensity of extrapyramidal negative manifestations and extends the drug's drug effect on negative and affective signs of schizophrenia.

[3], [4]

Pharmacokinetics

The absorption of risperidone is complete, without reference to the use of food. Plasma Cmax values are noted after 1-2 hours. Synthesis with intraplasma protein (albumin, as well as α1-acid glycoprotein) is 88%.

It is subject to rapid distribution and passes inside the tissues of the central nervous system; distribution volume is 1-2 l / 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-desalkylation. Equilibrium values for the active component are recorded after a day, and for 9-hydroxyrisperidone - after 4-5 days.

The half-life of risperidone is 3 hours, and the 9-hydroxyrisperidone component is 24 hours. After 7 days of use, 70% of drugs are excreted in the urine, and another 14% - through the digestive tract. 35-45% is derived in the form of existing items.

Older people or people with kidney failure with 1-time use of the drug have elevated plasma levels and delayed excretion of risperidone.

[5], [6],

Dosing and administration

It is necessary to apply a medicine orally, without binding to food intake, 1-2 times a day.

Treatment of schizophrenia: on the 1st day - taking 2 mg, on the 2nd - 4 mg. Later, the dosage is kept at a rate of 4 mg or, if necessary, adjusted personally for the patient. Often prescribed use 4-6 mg medication per day. It should be borne in mind that when using drugs in a daily portion in excess of 10 mg, there is no increase in therapeutic efficacy, but this increases the likelihood of extrapyramidal signs.

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

Behavioral disorders in people with dementia: the size of the initial dosage portion is 0.25 mg with 2 times daily use; if necessary, the portion can be increased by +0.25 mg 2 times per day, but this is allowed at least in a day. Basically, it is prescribed in a dose of 0.5 mg 2 times per day, but individual patients may require the use of 1 mg of the substance 2 times a day.

Related to mania 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 appoint 2-6 mg per day.

Behavioral dysfunctions in people with a delay in intellectual development or with the predominance of destructive reactions: individuals with a weight of more than 50 kg should use 0.5 mg per day 1-fold, and further increase the dosage by + 0.5 mg per day (after day), if required. People with a weight below 50 kg are first prescribed 1-fold use of 0.25 mg per day; The dosage may be increased every day by +0.25 mg per day. The size of the optimal portion is 0.5 mg of the drug per day.

After obtaining an optimal result, the use of a drug can be reduced to 1-fold intake per day. The maximum daily serving is 16 mg.

[10]

Use Neuryspin during pregnancy

During pregnancy, neuryspine is prescribed only in situations where the benefits of treatment are more likely than the risks of developing complications for the fetus.

Contraindications

Contraindicated use in personal intolerance, as well as during breastfeeding.

[7], [8], [9]

Side effects Neuryspin

Among the side effects:

• damage to the central nervous system along with the senses: often agitation, headaches, insomnia and anxiety. Sometimes it may cause dizziness, fatigue or drowsiness, disorders of visual clarity and concentration. Occasionally, extrapyramidal symptoms (rigidity, akathisia, tremor with bradykinesia, hypersalivation and acute dystonia) occur, thermoregulatory disorders, seizures, CSN and dyskinesia may occur in the late stage;
• disorders of digestive activity: dyspepsia, vomiting, pain in the abdominal area, nausea, constipation and an increase in the values of liver enzymes;
• problems with the work of the cardiovascular system and the blood system: rarely there is tachycardia of a reflex nature, hypervolemia, orthostatic collapse, some decrease in the level of platelets or neutrophils and stroke (in elderly people with the presence of predisposing factors);
• endocrine disorders: gynecomastia, amenorrhea with galactorrhea, weight gain and menstrual cycle disorder. Occasionally, diabetes is exacerbated or hyperglycemia develops;
• lesions of the reproductive system: rarely there are problems with ejaculation, erection and orgasm, as well as priapism;
• allergy symptoms: Quincke edema, runny nose and rash on the epidermis are occasionally observed;
• others: urinary incontinence sometimes occurs.

Overdose

Signs of poisoning include the development of a strong sedative effect, drowsiness, a decrease in blood pressure values, tachycardia, and extrapyramidal manifestations. The increase in the QT-interval indications on the ECG is noted individually.

During treatment, it is necessary to ensure the unimpeded passage of air through the respiratory tract in order to maintain the required oxygen supply and adequate ventilation. At the same time, gastric lavage and the introduction of a laxative with activated carbon are carried out, and in addition, ECG values are monitored to detect possible heart rhythm disorders. Also carried out symptomatic activities that support the work of important organs for life.

If vascular collapse develops and blood pressure values decrease, infusion or sympathomimetics are administered. If extrapyramidal signs appear, prescribe the use of anticholinergic substances.

Neuryspin does not have an antdot. It is necessary to conduct regular monitoring of the condition of the victim until all signs of poisoning disappear.

[11]

Interactions with other drugs

The combined use of risperidone and agents that are antagonists of dopamine endings, leads to the appearance of dyskinesia of a late nature (having involuntary rhythmic movements, mainly of a person or tongue), due to which the introduction of any antipsychotics is necessary.

Risperidone may have an antagonistic effect on levodopa.

Tricyclics with phenothiazines, fluoxetine and β-blockers are capable of increasing the blood levels of risperidone, while not affecting the level of active antipsychotic fraction.

The combination with carbamazepine, as well as other means that induce liver enzymes, leads to a decrease in the activity of the antipsychotic fraction of the drug inside the blood. After the abolition of the introduction of such substances is required to revise the size of the dosage of Neuryspin.

If additional sedation is required, the use of benzodiazepine derivatives is prescribed together with the medication.

[12], [13]

Storage conditions

Neuryspin is required to be stored in a dark and dry place, closed from access of young children. Temperature indicators - in the range of marks 15-30 ° C.

Shelf life

Neuryspin can be used within a 24-month term from the time the pharmaceutical product is manufactured.

Application for children

There is not enough information regarding the effectiveness and safety of the use of the drug in pediatrics. Not prescribed to persons under the age of 15.

Analogs

Analogues of drugs are the drugs Rileptid, Risset with Rispaxol, and in addition Rispolept with Risperon and Aridon with Rispetril.

[14], [15], [16]