Index of drugs

Treatment of schizophrenia - the preparation 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 treatment in the treatment of a manic episode, the preparation is indicated for the prevention of relapse of bipolar disorder.

1 tabl orally disintegrating contains 5 mg, 10 mg, 15 mg or 20 mg olanzapine. The preparation contains 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 (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 C_max 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 is approximately 93% bound to 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 at risk of glaucoma with closed-angle glaucoma.

Olanzapine is not indicated for use in children and adolescents (no data on the safety and efficacy of treatment, shorter-term studies in adolescents have shown a significantly higher increase in body mass and greater changes in blood lipids and prolactin levels than in studies with adults). Olanzapine is not approved for the treatment of patients with symptoms of psychosis and / or behavioral disorders due to dementia (increased mortality and an increased risk of cerebrovascular accidents) and for the treatment of psychosis induced by dopamine agonists in patients with Parkinson's disease (Parkinsonism and hallucinations have been observed ). Use with caution in patients with: diabetes or risk factors for diabetes (regular glycemic control and body weight are recommended); with disturbances of lipid metabolism or with risk factors for the development of such disorders; with prostatic hyperplasia, paralytic ileus and similar diseases; 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, bone marrow suppression and / or marrow depletion, co-existing disease, radiotherapy 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 people over 65 years it is recommended to periodically measure blood pressure during treatment with olanzapine); 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 used if olanzapine is prescribed in combination with other medicines known to prolong the QT interval, especially in elderly patients, patients with congenital long QT syndrome, congestive heart failure, hypertrophy of the heart, 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, the preparation may be dangerous for people with phenylketonuria.

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. Olanzapine is excreted in breast milk - patients should be advised against breast-feeding while taking olanzapine.

Very common: weight gain, drowsiness, increased prolactin in the blood, which was rarely accompanied by clinical symptoms (eg gynaecomastia, mycotox and breast enlargement) - in most patients the level of prolactin normalized and did not require discontinuation of treatment. Common: eosinophilia, increased cholesterol, Glucose, triglycerides, glycosuria, increased appetite, dizziness, akathisia, parkinsonism, dyskinesias, orthostatic hypotension, mild and transient anticholinergic effects (including constipation and dry mouth), transient asymptomatic elevation of hepatic transaminases, rash, erectile dysfunction in men, decreased libido in men and women, asthenia, fatigue, edema. Uncommon: leukopenia, neutropenia, bradycardia, QT prolongation, thromboembolism (including pulmonary embolism and deep vein thrombosis), photosensitivity reactions, alopecia, urinary retention, amenorrhea, breast enlargement in men and women, amlectomy women, gynecomastia, increased creatinine phosphokinase, increased total bilirubin. Not known: thrombocytopenia, hypersensitivity reactions, onset or worsening of diabetes with ketoacidosis or coma (including fatal cases), hypothermia, seizures, neuroleptic malignant syndrome (VEGA), dystonia (including ocular rotations), tardive dyskinesias, acute discontinuation symptoms in case of abrupt discontinuation of olanzapine (sweating, insomnia, tremor, anxiety, nausea or vomiting), ventricular tachycardia, ventricular fibrillation, sudden death, thromboembolic events (deep vein thrombosis, pulmonary embolism), pancreatitis, inflammation liver (including hepatocellular and cholestatic liver damage and mixed form of liver damage), rhabdomyolysis, urinary bladder feeling, withdrawal syndrome in the newborn, priapism, increased alkaline phosphatase. In elderly patients with dementia, more frequent deaths and unwanted cerebrovascular events have been observed. 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. Patients receiving olanzapine in combination with valproate had 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 (13-17 years) 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 liver transaminases, total bilirubin, increased GGT, increased prolactin in the blood, increased cholesterol in the blood and dry mouth - the preparation is not indicated for use in children and adolescents.

Orally. Adults. 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 (≥ 65 years), the initial dose reduction is not routinely recommended, however, it should be considered as the clinical factors suggest. 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.Way of giving. The orodispersible tablet should be placed in the mouth, where it rapidly disintegrates in the saliva; take the tablet immediately after opening the package; alternatively, it can be dissolved in a full glass of water or another drink (orange juice, apple juice, milk, coffee) just before taking.