Index of drugs

Adults. Treatment of schizophrenia. olanzapine is effective in long-term supportive care for patients who have responded to treatment early in treatment. Treatment of moderate to severe manic episodes. In patients who respond to treatment with olanzapine in the treatment of a manic episode, it is indicated to prevent the recurrence of bipolar disorder.

1 tabl submissive. in the mouth contains 5 mg, 10 mg, 15 mg or 20 mg olanzapine; tablets contain aspartame.

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 (M.₁-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. Olanzapine in the form of tabl. submissive. in the oral version is bioequivalent to olanzapine in the form of area, showing a similar rate and extent of absorption (both forms can be used interchangeably). Olanzapine is well absorbed from the gastrointestinal tract, reaching C_max within 5-8 h (food does not affect the absorption of the drug). It is 93% bound to plasma proteins. 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. 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 to any of the excipients. Patients at risk of narrow-angle glaucoma.

When using antipsychotics, improvement of the clinical condition may occur after a few days or weeks; during this time, the patient should be carefully monitored. Do not use olanzapine in children and adolescents <18 years (no data on the safety and efficacy of treatment in this age group, during short-term studies in adolescents aged 13-17 years, a significantly higher increase in body mass and greater changes in blood lipids and prolactin levels were observed , than in studies involving adults - the long-term effects of these side effects have not been studied and they remain unknown). Olanzapine should not be used for the treatment of psychosis and / or behavioral disorders caused by dementia (increased mortality and increased risk of cerebrovascular accidents) and for the treatment of psychosis induced by dopamine agonists in patients with Parkinson's disease (Parkinsonism and hallucinations were observed, and olanzapine was not more effective than placebo in the treatment of psychotic symptoms). Olanzapine-treated patients should be monitored in accordance with accepted guidelines for antipsychotic treatment: control of blood Glucose - before treatment, after 12 weeks of treatment with olanzapine and then once a year, and patients should be monitored for symptoms of hyperglycaemia (excessive thirst and hunger, polyuria and weakness); systematically check body weight - before starting treatment, 4, 8 and 12 weeks after starting treatment with olanzapine, and then once a quarter; control the level of lipids in the blood - before starting treatment, after 12 weeks of treatment with olanzapine and then every 5 years.If the risk profile of metabolic changes (changes in body weight, Glucose, lipids in the blood) deteriorates, the clinical guidelines should be followed and appropriate treatment should be given. Olanzapine should be used with caution in patients with: diabetes or risk factors for developing diabetes (regularly examine patients to detect deterioration in glycemic control); with dyslipidemia or with risk factors for the development of lipid disorders; with prostatic hyperplasia, paralytic bowel obstruction and similar diseases (due to the anticholinergic activity of olanzapine); with increased ALT and / or AST, with signs and symptoms of hepatic impairment, with pre-existing limited functional reserve of liver function and in patients using drugs with potential hepatotoxic effects (finding hepatitis is an indication for discontinuation of olanzapine treatment); with a low number of leukocytes and / or neutrophils, drugs that can induce neutropenia, with myelosuppression and / or bone marrow failure induced by a history of medication, by co-existing disease, radiation or chemotherapy, and in patients with hypereosinophilia or myeloproliferative disease (combination therapy olanzapine and valproate increases the risk of neutropenia); with convulsive seizures or subjected to factors lowering the seizure threshold; in the elderly (in patients> 65 years, periodic measurements of blood pressure during treatment with olanzapine are recommended). Before and during treatment with olanzapine, all possible risk factors for venous thromboembolism should be identified and appropriate preventive measures should be taken. Caution should be exercised when olanzapine is used concomitantly with other drugs affecting o.u.n. or alcohol. Caution should be used if olanzapine is prescribed in combination with other medicines known to prolong the QTc interval, particularly in elderly patients, patients with congenital long QT syndrome, congestive heart failure, hypertrophy, hypokalaemia or hypomagnesaemia. If you have symptoms of a neuroleptic malignant syndrome (NMS) or high fever with an unexplained reason, all other antipsychotics, including olanzapine, should be discontinued without other clinical symptoms of RH. In the event of tardive dyskinesia, a dose reduction or discontinuation of olanzapine should be considered. Due to the content of aspartame, tabl. submissive. in the mouth can be harmful for people with phenylketonuria.

During pregnancy, use only if 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 is a risk of adverse reactions, including extrapyramidal and / or withdrawal symptoms of varying severity and duration - newborns should be carefully monitored. Patients should be advised not to breastfeed when taking olanzapine.

Very common: weight gain, drowsiness, orthostatic hypotension, increased prolactin in the blood (in most patients, mild, not exceeding the 2-fold upper limit of normal). Common: eosinophilia, leukopenia and neutropenia, increased glucose, triglycerides and cholesterol in the blood, glycosuria, increased appetite, dizziness, akathisia, parkinsonism, dyskinesias, mild, transient anticholinergic effects (including constipation and dry mouth), transient asymptomatic transaminase elevation, rash, arthralgia, erectile dysfunction in men and decreased libido in both sexes, asthenia, fatigue, edema, fever, increased alkaline phosphatase, creatine phosphokicase, GGT, increased uric acid. Uncommon: hypersensitivity, development or worsening of diabetes (occasionally associated with ketoacidosis or coma, including fatal cases), seizures (mostly in patients with convulsions or risk factors for a seizure disorder), dystonia (including ocular rotation) , tardive dyskinesia, amnesia, dysarthria, epistaxis, bradycardia, QTc prolongation, thromboembolism (deep vein thrombosis, pulmonary embolism), flatulence, photosensitivity reaction, alopecia, urinary incontinence, urinary retention, urge bladder, amenorrhea, breast enlargement, milk secretion in women outside the lactation period, gynecomastia or breast enlargement in men, increased total bilirubin.Rare: thrombocytopenia, hypothermia, neuroleptic malignant syndrome, withdrawal symptoms (insomnia, tremor, anxiety, sweating, nausea or vomiting), ventricular tachycardia or ventricular fibrillation, sudden cardiac death, pancreatitis, hepatitis (including hepatocellular and cholestatic hepatic injury) and mixed form of liver damage), rhabdomyolysis, priapism. Not known: neonatal withdrawal syndrome. In adolescents an increased incidence of certain side effects was observed than in the adult group, weight gain, increased triglycerides in the blood, increased appetite, sedation, increased hepatic transaminases, total bilirubin, increased GGT, increased prolactin in the blood, increased cholesterol in the blood and dry mouth - no preparation it is indicated for use in children and adolescents.

Orally. Adults. Schizophrenia: the recommended starting dose of olanzapine is 10 mg / day. Manic episodes: the starting dose is 15 mg / day as 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.Special groups of patients. In elderly patients (≥65 years old), a reduction in the initial dose of up to 5 mg is not routinely recommended, however, it should be considered if there are clinical factors for this. In patients with impaired renal and / or hepatic function, a lower starting dose of 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 advisable, should be performed with caution.Way of giving. The preparation can be taken regardless of meals. Table. submissive. in the oral version are bioequivalent from the table powl. and can be used interchangeably. Table. submissive. begin in mouth should be placed in the mouth, where they are rapidly disintegrated in the saliva. The tablet should be taken immediately after opening the package; alternatively, it can be dissolved in a full glass of water or other suitable drink (orange juice, apple juice, milk) just before taking.