Zolafren (olanzapine) coated tablets 5 mg. №30

Description

Zolafren (olanzapine) coated tablets 5 mg. №30

Composition

active substance: 1 tablet contains 5 mg or 10 mg of olanzapine;

Excipients: lactose monohydrate, microcrystalline cellulose, sodium starch glycolate (type A), magnesium stearate; shell: hydroxypropylmethylcellulose (hypromellose), polyethylene glycol (Macrogol) 400, dye Yellow No.6 Al-Lake (E 110), titanium dioxide (E 171), iron oxide yellow (E 172), lactose monohydrate.

Dosage form

Coated tablets.

Main physical and chemical properties:

• 5 mg tablets: beige tablets, coated, biconvex, with a dividing line on one side, 7 mm in diameter;
• 10 mg tablets: beige, coated, biconvex, 7 mm diameter tablets.

Pharmacotherapeutic group

Antipsychotics. ATX code N05A H03.

Pharmacological properties

Zolafren coated tablets (olanzapine) is an antipsychotic, antimanic, mood-stabilizing drug with a broad spectrum of pharmacological action due to exposure to various receptors. Binding to serotonin receptors 5 HT2A / 2C, 5 HT3, 5 HT6, dopamine receptors D1, D2, D3, D4, D5, muscarinic receptors M1-M5, adrenergic receptor a1 and histamine H1-receptor has been identified. Behavioral studies in olanzapine have revealed antagonism of olanzapine to both 5HT serotonin receptors and dopamine and cholinergic receptors. Olanzapine has a higher level of binding to serotonin 5HT2 receptors than to dopamine D2 receptors in both in vitro and in vivo models. Electrophysiological studies have shown that olanzapine selectively reduces the excitability of mesolimbic (A10) dopaminergic neurons, with little effect on striatal (A9) pathways associated with motor function. Zolafren coated tablets (olanzapine) inhibits the conditioned avoidance reflex, indicating its antipsychotic activity at doses lower than those causing catalepsy, which is a sign of motor side effects. Unlike some other antipsychotic drugs, olanzapine enhances responses to stimuli during an anxiolytic test.

A single dose of 10 mg olanzapine in positron emission tomography (PET) with volunteers showed that olanzapine had a higher level of binding to 5 HT2A receptors than to dopamine D2 receptors. In addition, an analysis of images obtained from studies of patients with schizophrenia by single-photon emission computed tomography (SPECT) revealed that olanzapine-sensitive patients had lower levels of binding to striatal D2- receptors than in other antipsychotic and respiridon-sensitive patients, which is comparable to that in clozapine-sensitive patients.

Indication:

• Olanzapine is indicated for the treatment of schizophrenia.
• Olanzapine is effective in maintaining the clinical effect achieved during long-term therapy in patients who respond to initial therapy.
• Olanzapine is indicated for the treatment of moderate to severe manic episodes.
• Olanzapine is indicated for the prevention of relapses in patients with bipolar disorder who have received a positive response to olanzapine mania.

Contraindication

Hypersensitivity to the active substance or to any of the excipients; known risk of angle-closure glaucoma.

Method of application and dosage

• Schizophrenia. The recommended starting dose of olanzapine is 10 mg once daily.
• Manic episodes. The recommended starting dose of olanzapine as monotherapy is 15 mg per day or 10 mg per day in combination therapy.
• Prevention of recurrent attacks in patients with bipolar disorder. The recommended starting dose is 10 mg per day. Patients with bipolar disorder who received olanzapine for the treatment of manic episodes continue to receive olanzapine at the same dosage and to prevent recurrence. If a new manic, depressive, or mixed episode develops, treatment should be continued (dose-optimized if necessary) with maintenance therapy to treat mood symptoms if clinically necessary.
• Treatment of schizophrenia, manic episodes and prevention of recurrence of bipolar disorder. The daily dose is determined on the basis of clinical status in the range from 5 to 20 mg per day. Increase the recommended starting dose at intervals of at least 24 hours only after a clinical examination. Olanzapine should be used with or without food, as food intake does not affect the absorption of the drug. Withdrawal of the drug should be completed gradually.

Children

Zolafren coated tablets (olanzapine) is not recommended for use in children and adolescents.

Studies of patients aged 13-17 years have shown various side effects, namely: weight gain, changes in metabolic parameters and increased prolactin levels. The results of these side effects have not been studied and remain unknown.

Overdose

Tachycardia, agitation / aggression, dysarthria, various extrapyramidal symptoms and decreased level of consciousness, ranging from sedation to coma.

Other significant complications of overdose are delirium, convulsions, coma, the possibility of neuroleptic malignant syndrome, respiratory depression, aspiration, hypertension or hypotension, cardiac arrhythmia and cardiopulmonary shock. Fatalities have been reported in acute overdoses of 450 mg, but there have been cases of survival after acute overdose after taking 2 g of olanzapine orally.

Side effects

The most common adverse reactions (observed in ≥ 1% of patients) associated with olanzapine in clinical trials were drowsiness, weight gain, eosinophilia, elevated prolactin, cholesterol (cholesterol), glucose and triglycerides, glucosuria. , increased appetite, dizziness, akathisia, parkinsonism, leukopenia, neutropenia, dyskinesia, orthostatic hypotension, anticholinergic effects, transient asymptomatic increase in hepatic transaminases, rash, asthenia, asthenia, increased fatigue, hyperglyphata creatine phosphokinase and edema.