Olanzapine, 5 mg 28 pcs

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Indications

Active ingredient

Composition

1 tablet contains:

The active ingredient: olanzapine benzoate 6.95 mg, corresponding to olanzapine 5.0 mg,

Auxiliary substances: calcium hydrophosphate 141.05 mg, microcrystalline cellulose 40.00 mg, sodium carboxymethyl starch (type A) 10.00 mg, magnesium stearate 2.00 mg.

How to take, the dosage

Schizophrenia: The recommended starting dose of the drug is 10 mg per day.

Therapeutic doses of olanzapine are indicated in the range of 5 mg to 20 mg per day. The daily dose should be adjusted individually depending on the clinical condition of the patient. Increasing the dose beyond the standard daily dose (10 mg) is recommended only after appropriate clinical examination of the patient.

Episode mania: the recommended starting dose of olanzapine is 15 mg once daily as monotherapy or 10 mg once daily in combination therapy with lithium or valproic acid.

Therapeutic doses of olanzapine are indicated in the range of 5 mg to 20 mg daily. The daily dose should be adjusted individually, depending on the clinical condition of the patient. Increasing the dose beyond the standard daily dose is recommended only after an appropriate clinical examination of the patient. The dose should be increased gradually, at intervals of at least 24 hours.

Prevention of relapses in bipolar disorder: the recommended starting dose of the drug in remission is 10 mg per day. For patients already receiving the drug for treatment of a mania episode, maintenance therapy is given in the same doses.

On background therapy with Olanzapine, if a new manic, mixed or depressive episode develops, the drug dose should be increased with additional treatment of mood disorders, if necessary, according to clinical indications.

Maintenance therapy for bipolar disorder. Patients who have taken olanzapine for the treatment of acute mania should continue maintenance therapy at the same dose. In patients in remission, the recommended initial dose of olanzapine is 10 mg once daily. Thereafter, the daily dose should be adjusted individually, depending on the clinical condition of the patient, ranging from 5 mg to 20 mg per day.

Olanzapine in combination with fluoxetine for the treatment of bipolar depression should be prescribed once daily, in the evening, regardless of meals. Typically, the starting dose is 5 mg of olanzapine and 20 mg of fluoxetine. Antidepressant activity has been confirmed with olanzapine at a dose of 6-12 mg (mean daily dose-7.4 mg) and fluoxetine at a dose of 25-30 mg (mean daily dose-39.3 mg). If necessary, it is possible to change the dose of both olanzapine and fluoxetine.

Olanzapine in combination with fluoxetine for treatment-resistant depression should be administered once daily, in the evening, regardless of meals. Typically, the starting dose is 5 mg olanzapine and 20 mg fluoxetine. If necessary, it is allowed to change the doses of both olanzapine and fluoxetine. Antidepressant activity has been confirmed with olanzapine at a dose of 6-12 mg and fluoxetine at a dose of 25-30 mg.

Special patient groups

In elderly patients, reduction of the starting dose (to 5 mg daily) is not usually recommended, but is possible in patients over 65 years of age if risk factors are present (see section on “Special Precautions”).

The general rules for choosing a daily oral dose for patients in special groups. Reduction of the starting dose to 5 mg daily is recommended in patients with clinical risk factors, including severe renal insufficiency or moderate hepatic insufficiency. Reducing the starting dose may be recommended for patients with a combination of factors (female patients, elderly, nonsmokers) that may slow down olanzapine metabolism.

Interaction

Special Instructions

Hyperglycemia and diabetes mellitus

There is a higher prevalence of diabetes mellitus in patients with schizophrenia. There are very rare reports of the development of hyperglycemia and/or decompensation of diabetes mellitus, sometimes accompanied by the development of ketoacidosis or ketoacidotic coma, including reports of several fatal cases. In some cases there was an increase in body weight prior to decompensation, which may have been a predisposing factor. In patients with diabetes mellitus and risk factors of this disease, regular clinical control and monitoring of blood glucose concentration is recommended.

Change in lipid concentrations

In therapy with olanzapine, plasma lipid concentrations should be monitored in patients with dyslipidemia and in patients with risk factors for lipid metabolism disorders. Patients receiving olanzapine therapy require monitoring of lipidogram values. If lipid concentrations change, correction of therapy is required.

Anticholinergic activity

In clinical trials, therapy with olanzapine has rarely had adverse reactions due to M-cholinoreceptor blockade. Because clinical experience with olanzapine in subjects with comorbidities is limited, the drug should be used with caution in patients with clinically significant prostatic hyperplasia, paralytic ileus, closed-angle glaucoma and similar conditions.

The use of olanzapine in patients with Parkinson’s disease

Olanzapine is not recommended for the treatment of psychosis caused by dopamine mimetics in Parkinson’s disease. Parkinsonian symptoms and hallucinations are increased. However, olanzapine was not superior to placebo for the treatment of psychosis.

Dopaminergic antagonism

In vitro olanzapine is antagonistic to dopamine receptors and, like other antipsychotics (neuroleptics), can theoretically inhibit the effects of levodopa and other dopamine receptor agonists.

The experience of olanzapine in elderly patients with psychosis associated with dementia. Efficacy of olanzapine in elderly patients with psychosis associated with dementia has not been established. In placebo-controlled clinical trials (lasting 6-12 weeks) in elderly patients (mean age 78 years) with psychosis and behavioral disorders associated with dementia, increased mortality was observed in patients treated with olanzapine compared to the placebo group (3.5% versus 1.5%, respectively). The increase in lethality was independent of the dose of olanzapine or the duration of therapy. Risk factors predisposing to increased mortality include: age over 75 years, dysphagia, sedation, malnutrition and dehydration, lung disease (e.g., pneumonia, including aspiration), concurrent administration of benzodiazepines.

Cerebrovascular adverse events, including stroke in elderly patients with dementia

Cerebrovascular adverse events (stroke, transient ischemic attack), including fatal outcomes, have been reported in studies of olanzapine in elderly patients with psychosis associated with dementia. In placebo-controlled trials, a higher incidence of cerebrovascular adverse events was noted in patients in the olanzapine group compared to the placebo group (1.3% vs. 0.4%, respectively). All patients had prior risk factors for cerebrovascular adverse events (smoking, arterial hypertension, a previous history of a cerebrovascular adverse event or transient ischemic attack), and comorbidities with drug intake that were temporally associated with cerebrovascular adverse events.

Postural hypotension

Postural hypotension was not frequently observed in elderly patients during clinical trials of olanzapine. As with therapy with other antipsychotics, periodic blood pressure monitoring is recommended in patients over 65 years of age.

The QT interval

In clinical trials, clinically significant prolongation of the QT interval (Friederick formula QT correction [QTcF] ≥500 milliseconds in patients with a baseline QTcF< 500 msec) only (0.1%-1%) in patients treated with olanzapine against the background of no significant difference with placebo for associated cardiac events. However, as with other neuroleptic drugs, caution should be exercised when prescribing olanzapine simultaneously with drugs that can prolong the QT interval, especially in elderly patients, patients with QT interval prolongation syndrome, congestive heart failure, cardiac hypertrophy, hypokalemia or hypomagnesemia. An electrocardiogram should be monitored during therapy with olanzapine.

Hepatic disorders

Hematological changes

The drug should be used with caution in patients with leukopenia and/or neutropenia of any genesis, myelosuppression of drug genesis, as well as against the background of radiation or chemotherapy, due to concomitant diseases, in patients with hypereosinophilic states or myeloproliferative diseases. Neutropenia has often been noted with concomitant use of olanzapine and valproic acid (see section “Side effects”).

Malignant neuroleptic syndrome (MNS)

MNS is a potentially life-threatening condition associated with therapy with antipsychotics (neuroleptics), including olanzapine. Clinical manifestations of MNS: fever, muscle rigidity, impaired consciousness, autonomic disorders (unstable pulse or labile blood pressure, tachycardia, increased sweating, arrhythmias).

Contraindications

– Hypersensitivity to olanzapine or other drug components;

– Established risk of closed angle glaucoma;

– Closed-angle glaucoma;

– Childhood under 18 years of age (efficacy and safety not established).

Renal failure, hepatic failure, prostatic hyperplasia, paralytic intestinal obstruction, epilepsy, seizure syndrome in the history, leukopenia and/or neutropenia of various genesis, myelosuppression of various genesis, including.ч. myeloproliferative diseases, hypereosinophilic syndrome, cardiovascular and cerebrovascular diseases or other conditions predisposing to arterial hypotension, congenital increased QT interval on electrocardiogram (ECG) (increased correlated QT interval (QTc) on ECG), or in the presence of conditions that may potentially cause QT interval prolongation (e.g., concomitant administration of QT interval prolongers, congestive heart failure, hypokalemia, hypomagnesemia), elderly age, as well as concomitant administration of other drugs of central action; immobilization.

Side effects

The table below summarizes the major adverse effects and their frequency that have been reported during spontaneous reports, clinical trials, and/or in the post-registration period. Within each group, adverse reactions are presented in descending order of significance.

Very common (≥10%)

Often (≥1 and < 10%)

Infrequent (≥0.1 and < 1%)

Frequency unknown

(frequency cannot be determined from available data)

Disorders of the blood and lymphatic system

Eosinophilia

Amenorrhea

Breast enlargement in women

Galactorrhea in women

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Gynecomastia and breast enlargement in men

Musculoskeletal disorders

Arthralgia

General disorders

Asthenia

Fatigue

Peripheral edema

Hyperthermia

Respiratory system side

Nosebleeds

Pregnancy, prenatal and postnatal period

Newborn “withdrawal” syndrome

Laboratory indicators

Increased plasma prolactin concentration8

Increased alkaline phosphatase activity

Elevated creatine phosphokinase activity

Elevated uric acid concentration

Elevated total bilirubin concentration

1In all patient groups, regardless of BMI, there was a clinically significant increase in body weight.

A 7% or greater increase in body weight from the mean after a short course of therapy (median duration of 47 days) was observed very frequently (22.2%), an increase of 15% or greater was frequent (4.2%), and an increase of 25% or greater was infrequent (0.8%). With a prolonged course of olanzapine therapy (more than 48 weeks), increases of ≥7%, ≥15%, and ≥25% of baseline body weight were very frequent (64.4%), 31.7%, and 12.3%, respectively).

2 Mean increases in fasting lipid concentrations (total cholesterol, low-density lipoproteins (LDL), and triglycerides) were most pronounced in patients without baseline signs of lipid metabolism disorders.

3Often there was an increase in cholesterol concentration from normal fasting (< 5.17 mmol/L), to high values (≥6.2 mmol/L). Changes in cholesterol concentration from borderline fasting (≥5.17 to < 6.2 mmol/L) to elevated (≥6.2 mmol/L) were very frequent.

4Frequent increases in glucose concentration from normal fasting (< 5.56 mmol/L), to elevated (≥7 mmol/L) were observed. Changes in glucose concentration from borderline fasting values (≥5.56 to < 7 mmol/L) to elevated values (≥7 mmol/L) were very frequent.

5Frequent increases in triglyceride concentration from normal fasting (< 1.69 mmol/L) to elevated values (≥2.26 mmol/L) were observed. Changes in triglyceride concentration from borderline values (≥1.69 to < 2.26 mmol/L) to elevated (≥2.26 mmol/L) were very frequent.

7Symptoms such as sweating, insomnia, tremors, anxiety, nausea, and vomiting have been observed with abrupt withdrawal of olanzapine.

8In clinical trials lasting up to 12 weeks, plasma prolactin concentrations exceeded the upper limit of normal in approximately 30% of patients with normal baseline prolactin values. In the majority of such patients, the increase in prolactin concentrations was moderate, and less than 2 times the upper limit of the norm. There were also cases where patients’ prolactin concentrations spontaneously normalized without withdrawal of therapy.

Indesirable Effects in Special Patient Groups

In clinical trials, gait disturbances and falls have been reported as a very frequent (≥10%) adverse effect of olanzapine therapy in elderly patients with psychosis with dementia. Pneumonia, lethargy, erythema, visual hallucinations, and urinary incontinence were observed frequently (< 10% and ≥1%).

In clinical studies in patients with drug-induced (dopamine agonist-induced) Parkinsonian psychosis, an increase in Parkinsonian symptoms was observed very frequently (≥10%) and with a higher frequency than in the placebo group. Hallucinations were also very common in this group of patients.

In patients with bipolar mania, on combination therapy with valproic acid, the incidence of neutropenia was (4.1%), a contributing factor being the high plasma concentration of valproate.

Overdose

Symptoms. Very common (>10%) in olanzapine overdose are: tachycardia, agitation/aggressiveness, speech impairment, various extrapyramidal disorders and impaired consciousness of varying severity (from sedation to coma); in less than 2% of cases occur: Delirium, convulsions, coma, malignant neuroleptic syndrome, respiratory depression, aspiration, increased or decreased blood pressure, cardiac arrhythmias; in very rare cases, cardiopulmonary failure. The minimum dose of olanzapine in acute fatal overdose is 450 mg; a maximum dose in benign overdose (survival) of 2 g has been reported.

Pregnancy use

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