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 numerous 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 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.
Contraindications:
Hypersensitivity to olanzapine or other ingredients. Patients at risk of glaucoma with closed-angle glaucoma.
Precautions:
There are no data on the safety and efficacy of olanzapine in children. Caution in patients with: diabetes or risk factors for diabetes (regular monitoring of the clinical condition, glycaemia and body weight is recommended); 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.Olanzapine is not recommended 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 ). 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 its lactose content, the preparation should not be used in patients with hereditary galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose.
Pregnancy and lactation:
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.
Side effects:
Very common: drowsiness, weight gain, increased prolactin in the blood, which was rarely accompanied by clinical symptoms (eg gynaecomastia, mycotox and enlarged nipples), in most patients the level of prolactin normalized and did not require discontinuation of treatment. Common: eosinophilia, dizziness, akathisia, parkinsonism, dyskinesias, mild, transient anticholinergic effects (including constipation and dry mouth), increased appetite, increased Glucose, triglycerides in the blood, orthostatic hypotension, asthenia, edema, transient asymptomatic elevation of liver transaminases. Uncommon: elevation of creatinine phosphokinase, bradycardia with or without hypotension, syncope, prolongation of QT interval, photosensitivity reactions. In addition, after the marketing, the following side effects were observed - rarely: leukopenia, seizures, rash, hepatitis (including hepatocellular and cholestatic liver damage and mixed form of liver damage); very rare: ventricular tachycardia, ventricular fibrillation, sudden death, thrombocytopenia, neutropenia, neuroleptic malignant syndrome, dystonia, tardive dyskinesia, pancreatitis, inability to urinate despite pressure, rhabdomyolysis, hyperglycemia, onset or worsening of diabetes with sometimes with ketoacidosis or coma ( including fatalities), hypothermia, thromboembolic events (deep vein thrombosis, pulmonary embolism), hypersensitivity reactions (eg anaphylactoid reaction, angioneurotic edema, pruritus, urticaria), priapism. 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. Very rarely, discontinuation symptoms such as sweating, insomnia, tremor, anxiety, nausea or vomiting have been reported with abrupt discontinuation of treatment.
Dosage:
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. In elderly patients, a lower starting dose (5 mg / day) is not routinely recommended, but should be considered if there are clinical factors for this. 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.