Expiration date: 12/2025
Structure and Composition:
1 film-coated tablet contains olanzapine 5, 7.5 or 10 mg in a blister pack 7 pcs., In box 4 of the blister.
Pharmachologic effect:
As the serotonin ligand (2A / 2C, 3, 6), dopamine (D1-D5), m-choline (m1-m5), histamine H1- and alpha1-adrenoceptor selective effect on limbic system.
Pharmacokinetics:
Well absorbed, Cmax in plasma - in 5-8 hours, is metabolized in the liver (by conjugation and oxidative pathways) to inactive metabolites.. The main metabolite - 10-N-glucuronide - does not pass through the BBB. The average T1 / 2 varies (depending on age and sex) within 21-54 hours.
Indications:
The acute form of schizophrenia and others. Psychosis, accompanied by a pronounced positive (delusions, hallucinations, thought disorder, hostility, suspiciousness), and / or negative (blunted affect, emotional and social withdrawal, poverty of speech activity) symptoms. The secondary affective symptoms on a background of schizophrenia and related disorders.
Contraindications:
Hypersensitivity.
Application of pregnancy and breastfeeding:
If necessary, the appointment during pregnancy should carefully correlate the expected benefit to the mother and the risk to the fetus. During lactation nursing mothers should stop breast-feeding.
Side effect:
Frequent (more than 10%) - drowsiness, weight gain rare (less than 10%) - dizziness, dry mouth, constipation, peripheral edema, orthostatic hypotension, akathisia, dystonia, eosinophilia (asymptomatic), a small and temporary increase in prolactin levels (gynecomastia , laktoreya), liver transaminases.
Drug Interactions:
It reduces the effects of levodopa and dopamine agonists. Activated charcoal reduces the bioavailability of 50-60% when administered orally. Smoking and carbamazepine accelerates metabolism. There was no apparent interaction with antacids, cimetidine, imipramine, warfarin, diazepam, lithium, theophylline, biperidenom.
Dosage and administration:
Inside, regardless of meals. The initial dose - 10 mg / day dose. Then, the daily dose can range - from 5 to 20 mg / day, depending on the clinical condition.
Overdose:
Symptoms: Nausea, muddled speech, drowsiness. Mydriasis, respiratory depression, hypotension, extrapyramidal disorders were observed in animal studies.
Treatment: No specific antidote. Treatment is symptomatic, with obligatory use of activated carbon, providing good ventilation and oxygenation in the case of the collapse - in / in the introduction of norepinephrine (but not agonists with beta-stimulating activity - adrenaline, dopamine and others.).
Precautionary measures:
Used with caution in patients with prostatic hypertrophy, narrow-angle glaucoma, paralytic ileus, the presence of convulsive states in history, liver disease and kidney failure in patients with altered haematological parameters as well as in combination with others. CNS depressants (including with alcohol). It is not recommended during treatment to control potentially dangerous machinery (vehicles, etc.).
