Egolanza, 5 mg 28 pcs

Schizophrenia, Anxiety, Manic Depressive Psychosis

Schizophrenia (exacerbation, maintenance and long-term antiretroviral therapy). Bipolar affective disorder (monotherapy or in combination with Li+ drugs or valproic acid): acute manic or mixed episodes with/without psychotic manifestations and with/without rapid phase change.

Bipolar relapse and prevention of bipolar relapse (if the drug is effective in treating the manic phase).

Active ingredient

How to take, the dosage

Ingestion, regardless of meals, once, 5-20 mg/day. In schizophrenia in adults, the recommended initial dose is 10 mg/day. In acute mania associated with bipolar disorders in adults, 15 mg/day (1 time) as monotherapy or 10 mg/day (1 time) in combination with Li+ or valproic acid (maintenance therapy at the same dose).

Prevention of recurrence of bipolar disorder: The recommended starting dose is 10 mg daily. Patients who previously received olanzapine for treatment of a manic episode should continue treatment at the same dose to prevent relapse. In the presence of a new manic, mixed or depressive episode, olanzapine should be continued (adjusting the dose if necessary); if clinically indicated, mood medications should be prescribed additionally.

In the treatment of schizophrenia, manic episode, and for the prevention of recurrence of bipolar disorder, the daily dose may subsequently be adjusted between 5 and 20 mg, taking into account the clinical condition of the individual patient. Dose adjustments beyond the value recommended as the starting dose are recommended only after careful clinical review, and should generally occur at intervals of at least 24 hours.

The dose should be gradually reduced before discontinuing olanzapine. The maximum daily dose of olanzapine is 20 mg.

Interaction

CYP1A2 isoenzyme inducers or inhibitors may alter the metabolism of olanzapine. CYP1A2 isoenzyme inducers: clearance of olanzapine is increased in smoking patients and with concomitant use of carbamazepine, which leads to decreased plasma concentration of olanzapine. It may be necessary to increase the dose of the drug. CYP1A2 isoenzyme inhibitors: fluvoxamine significantly inhibits metabolism of olanzapine. By reducing clearance of olanzapine, it increases Csh of olanzapine by 54% in non-smoking women and by 77% in smoking men, AUC by 52% and 108%, respectively, so patients taking fluvoxamine or any other CYP1A2 inhibitor (such as ciprofloxacin) should consider using a lower starting dose of olanzapine.

Activated charcoal reduces the bioavailability of olanzapine by 50-60% and should be taken at least 2 hours before or 2 hours after olanzapine.

Fluoxetine (a CYP2D6 inhibitor), as well as single administration of antacids (aluminum or magnesium) or cimetidine, had no significant effect on the pharmacokinetics of olanzapine.

Ethanol had no effect on the pharmacokinetics of olanzapine in equilibrium; however, administration of ethanol together with olanzapine may be accompanied by an increase in the pharmacological effects of olanzapine (sedation).

Olanzanine slightly inhibits the formation of valproic acid glucuronide (the main metabolic pathway). Valproic acid slightly affects the metabolism of olanzapine. A clinically significant pharmacokinetic interaction between olanzapine and valproic acid is unlikely.

Caution is necessary when using olanzapine with drugs that prolong the QTc interval (amitriptyline, chlorpromazine. droperidol, thioridazine, pimozide, quinidine, procainamide, sotalol, ephedrine, adrenaline, terbutaline, erythromycin, trimethoprim/sulfamethoxazole, ketoconazole, fluconazole, etc) that disrupt electrolyte balance or inhibit hepatic metabolism of olanzapine.

The concomitant use of olanzapine and antiparkinsonian drugs in patients with Parkinson’s disease and dementia is not recommended.

Olanzapine is antagonistic to dopamine and may, in theory, inhibit the effects of levodopa and dopamine agonists.

Olanzapine does not inhibit the major CYP450 isoenzymes in vitro (e.g., 1A2, 2D6, 2C9, 2C19, ZA4), a clinically significant interaction is unlikely. No inhibition of metabolism of the following active substances has been found: tricyclic antidepressants (representing mainly CYP2D6 pathway), warfarin (CYP2C9), theophylline (CYP1A2) or diazepam (CYP3A4 and 2C19).

No interaction has been found with lithium or biperiden when used concomitantly.

Special Instructions

An improvement in the clinical condition of patients may occur over a period of days or weeks while on antipsychotic medication. During this period, patients need close monitoring.

Psychosis and/or behavioral disorders associated with dementia
Olanzapine is not approved for the treatment of psychosis and/or behavioral disorders associated with dementia, and this medication is not recommended for use in such patients because of increased mortality and risk of cerebrovascular events. Cerebrovascular disorders (stroke, transient ischemic attack), including fatal outcomes, have been reported in elderly patients with psychosis with dementia. These patients had previous risk factors (cerebrovascular disorders (history), transient ischemic attacks, arterial hypertension, smoking), as well as concomitant diseases and/or drug intake, in time associated with cerebrovascular disorders.

The use of olanzapine is not recommended for the treatment of psychosis associated with dopamine agonist administration in patients with Parkinson’s disease.

Malignant neuroleptic syndrome (MNS)
Malignant neuroleptic syndrome may develop during treatment with neuroleptics (including olanzapine). Clinical manifestations of MNS are fever, muscle rigidity, mental changes, instability of autonomic functions (unstable levels of heart rate and blood pressure, tachycardia, sweating, cardiac arrhythmia). Additional signs may include elevated levels of creatine phosphokinase, myoglobinuria (rhabdomyolysis), and acute renal failure. If a patient develops symptoms and signs of MNS or unexplained fever without additional clinical manifestations of MNS, all antipsychotics, including olanzapine, should be discontinued.

Hyperglycemia and diabetes mellitus
A higher prevalence of diabetes mellitus has been noted in patients with schizophrenia. Very rare cases of hyperglycemia, development of diabetes mellitus or exacerbation of pre-existing diabetes mellitus, ketoacidosis and diabetic coma have been reported. A causal relationship between antipsychotic medications and these conditions has not been established. Clinical monitoring of patients with diabetes mellitus or with risk factors for its development is recommended.

Changes in lipid levels
If lipid levels change with olanzapine, appropriate treatment should be prescribed, especially in patients with dyslipidemia or risk factors for fat metabolism disorders.

Anticholinergic activity
Although olanzapine has anticholinergic activity in vitro, due to limited clinical experience with olanzapine in patients with comorbidities, caution is recommended when prescribing this drug in patients with prostatic hypertrophy, paralytic ileus and other similar conditions.

Hepatic function
Particular caution is required when hepatic transaminases, ALT and/or ACT are elevated in patients with hepatic insufficiency or receiving treatment with potentially hepatotoxic drugs. Monitoring of the patient and, if necessary, dose reduction is required. If hepatitis (including hepatocellular, cholestatic or mixed liver disease) is detected, olanzapine should be discontinued.

Neutropenia
Olanzapine should be used with caution in patients with decreased number of leukocytes including neutrophils; with signs of inhibition or toxic dysfunction of bone marrow under the influence of drugs (in anamnesis); with suppression of bone marrow function due to concomitant disease, radio- or chemotherapy (history); with hypereosinophilia or myeloproliferative disease. Neutropenia is often seen with the combined use of olanzapine and valproate. The use of olanzapine in patients with clozapine-dependent neutropenia or agranulocytosis (history) was not accompanied by recurrence of these disorders.

The discontinuation of the drug
When olanzapine is discontinued abruptly in very rare cases (

The OT interval
As with other antipsychotic medications, caution should be exercised during treatment with olanzapine if this medication is prescribed concomitantly with QTc interval prolonging medications, especially in elderly patients, patients with congenital QT prolongation syndrome, congestive heart failure, cardiac hypertrophy, hypokalemia, hypomagnesemia, or a family history of QT prolongation.

The concomitant use of other neuroleptics or drugs that also prolong the QT interval or cause hypokalemia should be avoided.

Thromboembolism
Coincidence in the timing of taking olanzapine and venous thromboembolism has been reported in rare cases (less than 0.01%). A causal link between the symptoms of venous thromboembolism and olanzapine administration has not been established. However, because schizophrenic patients often have acquired risk factors for venous thromboembolism, all possible risk factors for venous thromboembolism, such as patient immobility, should be identified and preventive measures taken.

Convulsive seizures
Olanzapine should be used with caution in patients who have a history of seizures or are exposed to factors that lower the seizure threshold. Seizures in patients receiving olanzapine are rare. Most of these cases have a history of seizures or risk factors for seizures.

Late dyskinesia
If signs of tardive dyskinesia develop, dose reduction or cancellation of olanzapine is recommended. Symptoms of tardive dyskinesia may increase or manifest after drug withdrawal.

Ortostatic hypotension
In clinical trials of olanzapine, orthostatic hypotension was infrequently observed in elderly patients. As with other antipsychotic medications, periodic BP measurements are recommended in patients over 65 years of age.

Pediatric use
Olanzapine is not recommended for the treatment of children and adolescents. Studies in patients aged 13-17 years have found a variety of adverse reactions, including weight gain, altered metabolic parameters, and increased prolactin levels. The long-term outcomes of these events have not been studied and remain unknown.

Lactose
This drug contains lactose, so it should not be prescribed in patients with rare hereditary galactose tolerance disorders, hereditary Sami lactase deficiency or glucose-galactose malabsorption. Caution should be exercised when using olanzapine in combination with other centrally acting drugs and ethanol.

Contraindications

Hypersensitivity to the active ingredient or any of the ingredients of the drug. Closed angle glaucoma. Psychosis and/or behavioral disorders associated with dementia. Period of lactation. Childhood (under 18 years of age due to insufficient clinical data). Lactose intolerance, lactase deficiency or glucose-galactose malabsorption (the drug contains lactose).

With caution

Hepatic failure, renal failure, prostatic hyperplasia, epilepsy, seizure syndrome in anamnesis, myelosuppression (including leukopenia, neutropenia). myeloproliferative diseases, hypereosinophilic syndrome, paralytic intestinal obstruction, pregnancy, cardiovascular and cerebrovascular diseases or other conditions predisposing to arterial hypotension, congenital increased QT interval on electrocardiogram (ECG) (increased corrected QT interval (QTc) on ECG), or in 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 centrally acting drugs; immobilization.

Side effects

Nervous system and sense organs: dizziness, headache, migraine, weakness, asthenia, somnolence, insomnia, anxiety, hostility, agitation, euphoria, amnesia, depersonalization, phobia, obsessive-compulsive symptoms, neuralgia, facial paresis, hypoesthesia, extrapyramidal disorders, including. tardive dyskinesia, ataxia, neck muscle stiffness, muscle twitching, tremor, akathisia, dysarthria, stuttering, syncopal states, delirium, suicidal tendencies, stupor, coma, subarachnoid hemorrhage, stroke, nystagmus, diplopia, mydriasis, lens pigment deposition, cataracts, xerophthalmia, ocular hemorrhages, accommodation disorders, amblyopia, glaucoma, corneal damage, eye pain, keratoconjunctivitis, blepharitis, tinnitus and ear pain, deafness, and taste disorders.

The cardiovascular system and blood (hematopoiesis, hemostasis):orthostatic hypotension, tachy and bradycardia, palpitations, ventricular extrasystoles, ECG changes, cardiac arrest, cyanosis, vasodilation, transient leuko- and neutropenia, eosinophilia, leukocytosis, thrombocytopenia, hemorrhagic syndrome.

Respiratory system disorders: rhinitis, pharyngitis, laryngitis, voice changes, increased coughing, dyspnea, apnea, bronchial asthma, hyperventilation.

Gastrointestinal organs: increased appetite up to bulimia, thirst, dry mouth, increased salivation, aphthous stomatitis, gingivitis, glossitis, dysphagia, belching, esophagitis, nausea, vomiting, gastritis, gastroenteritis, enteritis, melena, rectal bleeding, constipation, flatulence, fecal incontinence, transient increase in activity of hepatic transaminases, gamma-glutamyl transpeptidase and creatine phosphokinase, hepatitis.

Metabolic disorders: hyperprolactinemia, weight gain (rarely decrease), diabetes mellitus, hyperglycemia, diabetic ketoacidosis, diabetic coma, goiter.

Urogenital system disorders: dysuria (including polyuria), hematuria, pyuria, albuminuria, urinary incontinence, urinary tract infections, cystitis, decreased libido, impotence, ejaculation disorders, priapism, gynecomastia, galactorrhea, breast pain, uterine fibrosis, premenstrual syndrome, meno- and metrorrhagia, amenorrhea.

Motor system disorders: arthritis, arthralgia, bursitis, myasthenia, myopathy, cramps of the calf muscles, bone pain.

Skin disorders: photosensitization, alopecia, hirsutism, dry skin, eczema, seborrhea, contact dermatitis, skin ulcers, skin color changes, maculopapular rash.

Allergic reactions: urticaria.

Others: fever, chills, flu-like syndrome, lymphoadenopathy, chest or abdominal pain, peripheral edema, withdrawal syndrome, possible abuse.

Overdose

Symptoms: tachycardia, agitation/aggression, articulation disorder, extrapyramidal disorders, depression of consciousness of varying severity (from sedation to coma), delirium, seizures, malignant neuroleptic syndrome, respiratory depression, aspiration, increased or decreased BP, arrhythmias, cardiac and respiratory arrest. The minimum dose in acute fatal overdose was 450 mg, the maximum dose with a favorable outcome (survival) was 1500 mg.

Treatment: gastric lavage, administration of activated charcoal, symptomatic treatment, maintenance of respiratory function. Sympathomimetics (including norepinephrine, dopamine), which are agonists of beta-adrenoreceptors should not be used (stimulation of these receptors may aggravate BP decrease). Close medical observation and monitoring should continue until the patient is well.

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