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 and 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.
Composition:
1 tabl powl. contains 5 mg or 10 mg of olanzapine.
Action:
Antipsychotic, anti-manic and stabilizing mood. Olanzapine has affinity for a number of receptor systems: serotonin (5HT2A / 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. The detailed mechanism of action is unknown, probably related to the 5-HT dopamine and serotonin receptor antagonists2. 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 P-450-2D6 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 is approximately 93% bound to plasma proteins. The blood concentration, 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.
Contraindications:
Hypersensitivity to olanzapine or other ingredients. Patients at risk of narrow-angle glaucoma.
Precautions:
There are no data on the safety and efficacy of olanzapine in children. Use with caution in patients with diabetes or risk factors for the development of diabetes mellitus; with prostatic hyperplasia, paralytic ileus and similar diseases; with increased ALT and / or AST, with signs and symptoms of hepatic impairment, in patients with pre-existing limited functional reserve of liver function and in patients using drugs with potential hepatotoxic effect (finding hepatitis is an indication for discontinuation of olanzapine treatment); in patients with low levels of leukocytes and / or neutrophils who are taking drugs that can induce neutropenia, with bone marrow suppression or damage caused by concomitant disease, radiotherapy or chemotherapy, and in patients with hypereosinophilia or myeloproliferative disease; in patients with a history of seizures or subjected to factors lowering the seizure threshold; with risk factors for clot in the venous system (eg immobilization) and in elderly patients (in the elderly, periodic measurements of blood pressure during treatment with olanzapine are recommended). Caution should be exercised when olanzapine is administered concomitantly with other centrally acting medicines and with alcohol. Caution should be exercised when olanzapine is used concomitantly with other QT prolonging agents, especially in elderly patients, patients with prolonged QT interval, congestive heart failure, hypertrophy, hypokalemia 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. Olanzapine should not be used to treat psychosis associated with dementia (increased mortality and increased risk of cerebrovascular events in this group of patients) and to treat psychosis associated with the intake of dopamine agonists in patients with Parkinson's disease (Parkinsonism and hallucinations were reported more frequently). The preparation contains lactose and should not be used in patients with hereditary galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose. The tablets contain soya lecithin and should not be used in patients who are hypersensitive to peanut or soya.
Pregnancy and lactation:
During pregnancy, use only in cases where the expected benefit to the mother outweighs the potential risk to the fetus. It should not be used during breast-feeding.
Side effects:
Very common: increased prolactin in the blood, drowsiness, weight gain, orthostatic hypotension. Common: eosinophilia, leukopenia, neutropenia; increased concentration of: cholesterol, Glucose, triglycerides; glycosuria, increased appetite, dizziness, akathisia, parkinsonism, dyskinesias, mild and transient anticholinergic effects (including constipation and dry mouth), transient, asymptomatic elevation of aminotransferases, especially in the initial phase of treatment, rash, joint pain, erection, decreased libido in men and women, asthenia, fatigue, edema, fever, increased alkaline phosphatase, high activity of creatinine phosphokinase and γ-glutamyltransferase, high concentration of uric acid. Uncommon: hypersensitivity, development of diabetes occasionally associated with ketoacidosis or coma, including fatal cases; convulsions, usually in patients with a history of convulsions or their occurrence factors; dystonia (including eye rotation), tardive dyskinesia, amnesia, dysarthria, bradycardia, QTc prolongation, thromboembolism (including pulmonary embolism and deep vein thrombosis), bloating, photosensitivity, alopecia, urinary incontinence, urinary retention , feeling of pressure on the bladder, lack of menstruation, breast enlargement, milk production in women beyond the breastfeeding period, gynecomastia or breast enlargement in men, increased total bilirubin. Rare: thrombocytopenia, hypothermia, neuroleptic malignant syndrome, withdrawal symptoms, ventricular tachycardia or ventricular fibrillation, sudden death, pancreatitis, hepatitis (including hepatocellular carcinoma, cholestatic liver injury or a mixed form of liver injury), rhabdomyolysis, priapism.
Dosage:
Orally. Schizophrenia: the recommended starting dose of olanzapine is 10 mg / day. Manic episode: the starting dose is 15 mg / day 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.Special groups of patients. In elderly patients a reduction of the initial dose (5 mg / day) should be considered, provided that this dose is sufficient to achieve clinical improvement. 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 carefully increased.If there is more than one factor that could cause a slower metabolism (female gender, old age, non-smoking), a reduction in the starting dose should be considered. In these patients, increasing the dose, if indicated, should be performed with caution.Way of giving. The tablets can be taken regardless of meals.