Adajio (olanzapin) coated tablets 10 mg. №28

Composition

Active substance: olanzapine.

1 tablet contains:

• olanzapine 5 mg or 10 mg.

Excipients: lactose, monohydrate; hydroxypropyl cellulose; crospovidone; microcrystalline cellulose; magnesium stearate.

Film shell: hypromellose, Opadray White 13B28444 (hypromellose, titanium dioxide (E 171), macrogol, polysorbate 80), carnauba wax: beeswax (60:40).

Pharmacotherapeutic group

Antipsychotic drugs. ATX code N05A H03.

Pharmacological properties

Pharmacodynamics

Olanzapine is an antipsychotic, antimanic, mood-stabilizing drug with a broad pharmacological profile across multiple receptor systems. In preclinical studies, olanzapine showed affinity for a number of receptors (Ki; < 100 nM) of serotonin 5HT2A/2C, 5HT3, 5HT6; dopamine D1, D2, D3, D4, D5; cholinergic muscarinic receptors M1-M5; α1-adrenergic; histamine H1 receptors. Animal behavioral studies have revealed 5HT, dopamine and cholinergic antagonism consistent with the receptor binding profile of olanzapine. Olanzapine has demonstrated greater affinity for serotonin 5HT2 receptors than dopamine D2 in vitro and greater 5HT2 activity than D2 in vivo. Electrophysiological studies have shown that olanzapine selectively reduces the excitability of mesolimbic (A10) dopaminergic neurons, showing a slight effect on the striatal (A9) pathways associated with motor function. Olanzapine inhibits the conditioned avoidance reflex, suggesting its antipsychotic activity at doses below those that cause catalepsy, a sign of motor side effects. Unlike some other antipsychotic drugs, olanzapine enhances responses to stimuli in an anxiolytic test.

When taking a single oral dose of 10 mg of olanzapine in the course of positron emission tomography (PET) with the participation of healthy volunteers, it was found that olanzapine had a higher level of binding to 5 HT2A receptors than to dopamine D2 receptors. In addition, single-photon emission computed tomography (SPECT) analysis of schizophrenic patients revealed that olanzapine-sensitive patients had lower levels of binding to striatal D2- receptors than in other antipsychotic-sensitive and risperidone-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 achieved clinical effect during long-term therapy in patients who have responded to initial therapy.
• Olanzapine is indicated for the treatment of moderate to severe manic episodes.
• Olanzapine is indicated for the prevention of relapse in patients with bipolar disorder who have responded positively to olanzapine treatment for mania.

Contraindications of Adagio

Hypersensitivity to the active substance or to any of the auxiliary substances of the medicinal product. There is a known risk of angle-closure glaucoma.