Description

Pharmacodynamics

Olanzapine is an antipsychotic, antimanic medication that stabilizes mood. It has a wide spectrum of pharmacological action due to its effect on various receptors. Binding to serotonin receptors 5 HT _{2A / 2C,} 5 HT _3, 5 HT _6, dopamine receptors D _1, D _2, D _3, D _4, D _5, muscarinic receptors M ₁ – M _5, blockers a ₁ and histamine H ₁receptor. Behavioral studies of animals administered olanzapine revealed antagonism of olanzapine both to serotonin 5HT receptors and to dopamine and cholinergic receptors. Olanzapine has a high level of binding to serotonin 5HT ₂ receptors than to dopamine D _{2 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. Olanzapine inhibits the conditioned avoidance reflex, suggesting its antipsychotic activity at doses lower than those causing catalepsy, which is a sign of adverse motor effects. Unlike some other antipsychotic drugs, olanzapine enhances responses to stimuli during an anxiolytic test.

With a single dose of 10 mg of olanzapine to volunteers during positron emission tomography (PET), it was established that olanzapine had a higher level of binding to 5 HT _2A receptors than to dopamine D ₂ receptors. In addition, as a result of the analysis of the images obtained during the studies of schizophrenic patients, by the emission computed tomography (SPECT) method, it was found that olanzapine-sensitive patients had a lower level of binding to striatal D ₂ receptors than in other antipsychotic- and risperidone-sensitive patients, compared to such in clozapine-sensitive patients.

Clinical effectiveness.

When treating schizophrenic patients with positive and negative symptoms with olanzapine, statistically reliable data on the improvement of both negative and positive symptoms were obtained.

In patients with manic or mixed episodes in bipolar disorder, olanzapine has been shown to be highly effective in reducing manic symptoms.

Children.

The experience of use in adolescents (aged 13 to 17 years) is limited.

Indications for use

Olanzapine is indicated for the treatment of schizophrenia.

It is effective in maintaining the achieved clinical effect with long-term therapy in patients who have responded to initial therapy.

It is indicated for the treatment of moderate to severe manic episodes.

Adajio tablets are indicated for the prevention of relapse in patients with bipolar disorder who have responded positively to olanzapine treatment for mania.

Contraindication

Hypersensitivity to the active substance or to any of the auxiliary substances of the drug is a known risk of glaucoma.

Method of application and dosage

Adults

Schizophrenia. The recommended starting dose 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 disorders. The recommended starting dose is 10 mg per day. Patients with bipolar disorder who have received Adajio Tablets for the treatment of manic episodes should continue to receive olanzapine at the same dosage and for the prevention of recurrent episodes. When a new manic, depressive, or mixed episode develops, treatment should be continued (with dose optimization if necessary) along with supportive therapy for mood disorder symptoms, if clinically indicated.

Treatment of schizophrenia, manic episodes and prevention of relapses of bipolar disorder. The daily dose is determined based on the clinical status in the range from 5 to 20 mg per day. An increase in the recommended initial dose is carried out at intervals of at least 24 hours only after a clinical examination. The tablets are used regardless of food intake, as food does not affect the absorption of the drug. When withdrawing the drug, the completion of therapy should be carried out gradually.

Children. The use of the drug in children and adolescents (up to 18 years) is not recommended due to insufficient data on safety and effectiveness. In the course of short-term studies, an increase in body weight, changes in prolactin and lipid levels were noted in adolescent patients compared to adults.