Index of drugs

Adults. Treatment of schizophrenia - olanzapine is effective in long-term supportive care for patients who have a good response to treatment in the initial phase of therapy. Treatment of moderate to severe manic episodes. In patients with a good response to olanzapine therapy in the treatment of a manic episode, the drug is indicated to prevent the recurrence of bipolar disorder.

1 tabl powl. contains 5 mg or 10 mg of olanzapine. The tablets contain lactose and soy lecithin.

Antipsychotic, anti-manic and stabilizing mood. Olanzapine has affinity for numerous receptors: serotonin (5HT_{2A / 2C}, 5HT₃, 5HT₆), Dopamine (D.₁, D₂, D₃, D₄, D₅), cholinergic muscarinic receptors (m₁-m₅), α₁-renergic and histamine H-receptors₁. It has greater affinity for the 5-HT receptor₂ than to the D-receptor₂. Olanzapin selectively reduces the stimulatory activity of dopaminergic neurons of the mesolimbic system (A10), while having little effect on the striatum (A9) involved in motor function. After oral administration, olanzapine is well absorbed from the gastrointestinal tract, reaching a maximum concentration in the blood within 5-8 h (food does not affect the absorption of the drug). It is metabolized in the liver via conjugation and oxidation. The main circulating metabolite of olanzapine is 10-N-glucuronide, which does not cross the blood-brain barrier. Cytochromes P-450 CYP1A2 and 2D6 are involved in the formation of N-desmethyl and 2-hydroxymethyl metabolites, which show significantly less activity than olanzapine. Pharmacological activity depends mainly on the parent compound - olanzapine. Olanzapine binds approximately 93% of plasma proteins. The half-life and clearance of olanzapine may vary depending on age and sex, and smoking. The drug is excreted in about 57% in the urine, mainly in the form of metabolites.

Hypersensitivity to olanzapine or other ingredients. Patients with narrow-angle glaucoma or with a known risk of it.

When using antipsychotics, improvement of the patient's clinical condition may occur after a few days or weeks - during this time patients should be carefully monitored. The drug is not indicated for use in children under 18 years. Caution in patients with: diabetes or risk factors for diabetes (regular monitoring of the clinical condition, glycaemia and body weight is recommended); with disorders of lipid metabolism and in patients with risk factors for such disorders (lipid levels should be regularly tested); with prostatic hyperplasia, paralytic ileus and similar diseases; with increased ALT and / or AST (dose reduction should be considered), with signs and symptoms of hepatic impairment with pre-existing limited functional reserve and liver and hepatotoxic patients (finding hepatitis is an indication for discontinuation of olanzapine ); with low numbers of leukocytes and / or neutrophils, drugs that can induce neutropenia, with drug-induced suppression and / or toxic medication, in patients with bone marrow suppression caused by concomitant disease, radiation or chemotherapy, and in patients with hypereosinophilia or myeloproliferative disease; with convulsive seizures or subjected to factors lowering the seizure threshold; in the elderly (in patients over 65 years, it is recommended to periodically measure blood pressure); with risk factors for clots with blockages in the venous system (eg immobilization). Caution should be exercised when olanzapine is used concomitantly with other drugs affecting o.u.n. or alcohol.Caution should be exercised when olanzapine is used concomitantly with other QT prolonging agents, especially in elderly patients, patients with congenital long QT syndrome, congestive heart failure, hypertrophy of the heart, hypokalaemia or hypomagnesaemia. Olanzapine is not recommended for the treatment of psychosis caused by the intake of dopamine agonists in patients with Parkinson's disease (worsening parkinsonism and hallucinations has been observed). It is not recommended for patients with symptoms of psychosis and / or behavioral disorders due to dementia due to increased mortality (risk factors were: age> 65 years, dysphagia, sedation, malnutrition and dehydration, lung disease and concomitant use of benzodiazepines) and increased risk of the risk of cerebrovascular accidents (risk factors are: age> 75 years, vascular dementia or mixed dementia). In case of symptoms of malignant neuroleptic syndrome (manifested by very high fever, muscle stiffness, consciousness disorders and symptoms of instability of the autonomic nervous system) or high unexplained fever, no other clinical symptoms of RH should be discontinued all antipsychotics, also olanzapine. In the event of tardive dyskinesia, a dose reduction or discontinuation of olanzapine should be considered. The drug contains lactose; should not be used in patients with rare hereditary galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose.

During pregnancy, use only in cases where the expected benefit to the mother outweighs the potential risk to the fetus. In newborns whose mothers took olanzapine in the third trimester of pregnancy, there was observed: tremor, increased tension, slowing and drowsiness. Patients should be advised not to breastfeed when taking olanzapine.

Very common: weight gain; somnolence; increased prolactin in the blood, which was rarely accompanied by clinical symptoms (eg gynecomastia, milk secretion outside the breastfeeding period and breast enlargement) - in the majority of patients, these symptoms subsided and did not require discontinuation of treatment. Common: eosinophilia; increase in appetite, increase in cholesterol, Glucose, triglycerides in the blood, glycosuria; dizziness, akathisia, parkinsonism, dyskinesia; orthostatic hypotension; mild, transient anticholinergic effects (including constipation and dryness of the oral mucosa); transient asymptomatic increases in ALT and AST, especially in the initial phase of treatment; rash; asthenia, fatigue, edema. Uncommon: leukopenia, neutropenia; bradycardia, prolongation of the QT interval; hypersensitivity to light, alopecia; high activity of creatinine phosphokinase, increase in total bilirubin. Not known: thrombocytopenia; Allergic reaction; development or worsening of diabetes occasionally associated with ketoacidosis or coma (including fatal cases), hypothermia; convulsive seizures in the majority of cases in patients with convulsions or risk factors for their occurrence, history of neuroleptic malignant syndrome (NMS), dystonia (including ocular rotations), tardive dyskinesia, withdrawal symptoms (acute symptoms in case of abrupt withdrawal of olanzapine - sweating , insomnia, tremor, anxiety, nausea or vomiting), ventricular tachycardia, ventricular fibrillation and sudden death; thromboembolic events (including deep vein thrombosis, pulmonary embolism), pancreatitis, hepatitis (including hepatocellular and cholestatic liver damage or a mixed form of liver injury); disintegration of striated muscles; feeling of pressure on the bladder; priapism; increase in alkaline phosphatase. In elderly patients with dementia, more frequent deaths and adverse cerebrovascular events were observed than in the placebo group. In this group of patients, abnormal gait and falls were very common; common: pneumonia, increased body temperature, lethargy, erythema, visual hallucinations and urinary incontinence. In Parkinson's patients with drug-induced psychosis (caused by dopamine agonists) Parkinsonism and hallucinations have been reported more frequently. In patients with a diagnosis of a manic episode in the course of bipolar disorder, the combined use of olanzapine and valproate induced neutropenia.When olanzapine was used with lithium or valproate, more frequent tremors, dry mouth, increased appetite and weight gain were observed; Speech disorder was also commonly reported. In adolescents (aged from 13 to 17 years) side effects were reported more frequently. Very common - weight gain, increased triglycerides, increased appetite, sedation (including excessive need for sleep, lethargy, drowsiness), increased ALT and AST, reduced total bilirubin, increased GGT, increased prolactin levels plasma; often - increase in cholesterol, dryness of the oral mucosa. Olanzapine is not indicated for the treatment of children and adolescents <18 years.

Orally. Adults.SchizophreniaThe recommended starting dose of olanzapine is 10 mg / day.Manic episodes: the starting dose is 15 mg given as a single dose in monotherapy or 10 mg / day in combination therapy.Prevention of relapse of bipolar disorder: the recommended starting dose is 10 mg / day. In patients receiving olanzapine to treat a manic episode, to prevent relapse, treatment with the same dose should be continued. In the case of a new mania, mixed episode or depression episode, olanzapine should be continued (if necessary optimizing the dose) and if there are clinical indications - additional treatment of affective symptoms. During the treatment of schizophrenia, manic episodes and for the prevention of recurrence of bipolar disorder, the daily dose may be set depending on the clinical condition of the patient in the range of 5-20 mg / day. Increasing the dose above the recommended starting dose is only recommended after a re-evaluation of the clinical condition and should be made no more frequently than every 24 hours. In elderly patients a lower starting dose (5 mg / day) is not routinely recommended, but should be considered if this is supported by clinical factors. In patients with impaired renal and / or hepatic function, a lower starting dose (5 mg) should be considered. In cases of moderate hepatic failure (cirrhosis, Child-Pugh class A or B) the starting dose should be 5 mg and be increased cautiously. If there is more than one factor that could slow down the metabolism of olanzapine (female gender, old age, non-tobacco use), a reduction of the starting dose should be considered. In these patients, increasing the dose, if indicated, should be performed with caution.
The preparation can be taken regardless of meals.