Olanzapine Canon pills 10mg, 28pcs

Composition

1 film-coated tablet,10 mg contains:

Active ingredient:

olanzapine 10 mg;

excipients:

hyprolose (hydroxypropylcellulose) low-substituted 3.5 mg,

calcium hydrophosphate 58 mg,

croscarmellose sodium 1.5 mg,

mannitol 75.5 mg, magnesium stearate 1.5 mg;

composition of the film shell:

 opadray II yellow 5 mg, including: polyvinyl alcohol 2 mg, macrogol (polyethylene glycol) 1.01 mg, talc 0.74 mg, titanium dioxide 1.175 mg, iron oxide yellow dye 0.075 mg

Pharmacological action

Pharmacotherapy group:

antipsychotic (neuroleptic)

ATX code: N05AH03

Indications

• Schizophrenia in adults. Olanzapine Canon is indicated for the treatment of exacerbations, maintenance and long-term anti-relapse therapy in patients with schizophrenia.
• Bipolar affective disorder in adults. Olanzapine Canon alone or in combination with lithium or valproic acid is indicated for the treatment of acute manic or mixed episodes in bipolar affective disorder with / without psychotic manifestations and / without rapid phase change. Olanzapine Canon is indicated for preventing relapses in patients with bipolar disorder in whom olanzapine has been effective in treating the manic phase.
• In combination with fluoxetine, Olanzapine Canon is indicated for the treatment of depressive states associated with bipolar disorder.
• Therapeutically resistant depression
• In combination with fluoxetine, Olanzapine Canon is indicated for the treatment of therapeutically resistant depression in adult patients (major depressive episodes with a history of ineffective use of two antidepressants in the dose and duration of therapy adequate for this episode

Contraindications

• Hypersensitivity to any of the components of the drug
• If you are at risk of developing glaucoma
• Angle-closure glaucoma
• Age up to 18 years (efficacy and safety not proven)
• Breast-feeding period

Side effects

Classification of the frequency of side effects (WHO): very common > 10%common>< 10%and > 1%infrequent< 10%and >< 1%and>0.1%rare< 1%and><0.1%and>0.01%very rare – <0.1%and>< 0.01% including individual messages

Blood and lymphatic system disorders often: eosinophilia; Infrequently: leukopenia, neutropenia; rarely: thrombocytopenia; Immune system disorders Very rarely: allergic reactions (anaphylactic shock, angioedema, pruritus, urticaria);

Metabolic disorders are very rare: the development or decompensation of diabetes mellitus, in some cases accompanied by ketoacidosis and diabetic coma, including with a fatal outcome; after discontinuation of therapy, after 9-12 months of treatment, a decrease in blood glucose concentration may occur;

Metabolic and nutritional disorders very common: weight gain; often: increased cholesterol, triglycerides, glucosuria, increased appetite; Changes in glucose concentration from normal values on an empty stomach (<5.5 b mmol / l) to an increase in gx (>7 mmol/l) observed frequently. Changes in glucose concentration from borderline values (>5.5 b mmol/l – ><7 mmol/L) to elevated values (>7 mmol/l) very common; very rare: hypertriglyceridemia, hypercholesterolemia; frequency unknown: bloating;

Violations of the nervous system is very frequent: drowsiness;often: dizziness, akathisia, parkinsonism, dyskinesia;infrequent: cramps (often on a background of seizures in the anamnesis);very rare: neuroleptic malignant syndrome, dystonia (including oculogyric crisis), tardive dyskinesia, a syndrome of “cancellation” (sweating, insomnia, tremor, anxiety, nausea or vomiting);

Cardiac disorders often: bradycardia, prolongation of the QT interval; very rarely: ventricular tachycardia/ ventricular fibrillation, sudden death;

Vascular disorders common: orthostatic hypotension; very rare: pulmonary embolism, deep vein thrombosis;

Gastrointestinal disorders often: transient anticholinergic effects, including dry mouth, constipation; rarely: pancreatitis;

Liver and biliary tract disorders often: transient increase in the activity of” hepatic ” transferases (alanine aminotransferase (ALT), aspartate aminotransferase (ACT)), especially in the early study period;rarely: hepatitis (including hepatic-cellular, hepatocellular or mixed).

Skin and subcutaneous tissue disorders Infrequently: skin rash; Infrequently: photosensitization reactions; very rarely: alopecia;

Musculoskeletal and connective tissue disorders Rare: rhabdomyolysis; frequency unknown: arthralgia;

Renal and urinary tract disorders often: urinary incontinence; rare: delayed urination; Frequency unknown: increased uric acid;

Disorders of the genitals and mammary gland rarely: priapism.

General disorders and disorders at the injection site often: asthenia, fatigue, edema; rare: hypothermia; frequency not known: fever;

Laboratory and instrumental data are very common: an increase in plasma prolactin concentration, but clinical manifestations (for example, gynecomastia, galactorrhea, and breast enlargement) are rare. In most patients, prolactin levels spontaneously returned to normal without discontinuation of the drug; often: increased creatine phosphokinase (CPK) activity, total bilirubin;very rarely: increased alkaline phosphatase activity.

Undesirable effects in special treatment groups A very common (> 10%) undesirable effect when using olanzapine in patients with psychosis on the background of dementia is a violation of gait and fall. Frequent (<10% and > 1%) adverse effects of olanzapine in elderly patients with psychosis and dementia are urinary incontinence and pneumonia.

Patients with psychosis induced by taking a dopamine receptor agonist drug in Parkinson’s disease often have increased symptoms of Parkinsonism. Hallucinations are also very common in this group of patients. In patients with bipolar mania who receive olanzapine in combination with lithium or valproic acid, very common adverse effects are weight gain, dry mouth, increased appetite, tremor, and often speech disorders.

Data on the side effect of the drug based on the results of clinical studies:

In clinical trials, cases of parkinsonism and dystonia were more frequent in patients taking olanzapine, but the difference with the placebo group was not statistically significant.

In patients taking olanzapine, cases of parkinsonism, akathisia, and dystonia were observed less frequently than in patients receiving titrated doses of haloperidol. Due to the lack of similar information about the presence of acute and tardive dyskinesias in patients, it is currently impossible to conclude that olanzapine is less likely to cause the development of tardive dyskinesias or other late extrapyramidal syndromes.

In 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 most of these patients, the increase in prolactin concentration was moderate, and less than 2 times higher than the upper limit of normal.

In patients taking olanzapine, genital and breast disorders that may be associated with olanzapine use (aminorrhea, breast enlargement, galactorrhea in women, gynecomastia, and breast enlargement in men) were uncommon. Sexual dysfunction, possibly related to olanzapine use (erectile dysfunction in men, decreased libido in men and women), was often observed.

Interaction

Olanzapine metabolism can be altered by inhibitors or inducers of cytochrome P450 isoenzymes that exhibit specific activity against the CYP1A2 isoenzyme. Olanzapine clearance is increased in smoking patients and in patients taking carbamazepine (due to an increase in the activity of the CYP1A2 isoenzyme). Known potential inhibitors of the CYP1A2 isoenzyme may reduce the clearance of olanzapine. Olanzapine is not a potential inhibitor of the activity of the CYP1A2 isoenzyme, so when taking olanzapine, the pharmacokinetics of drugs such as theophylline, mainly metabolized with the participation of the CYP1A2 isoenzyme, do not change.

Clinical studies have shown that a single dose of olanzapine during therapy with the following drugs is not accompanied by suppression of the metabolism of the following drugs: imipramine or its metabolite desipramine (CYP2D6, CYP3A, CYP1A2), warfarin (CYP2C19), theophylline (CYP1A2) or diazepam (CYP3A4, CYP2C19). There were no signs of drug interaction when olanzapine was used in combination with lithium or biperiden. No changes in the pharmacokinetics of ethanol were observed against the background of stable olanzapine concentrations. However, taking ethanol together with olanzapine. It may be accompanied by an increase in the pharmacological effects of olanzapine, for example, sedation. A single dose of an aluminum – or magnesium-containing antacid or cimetidine does not interfere with the oral bioavailability of olanzapine.Simultaneous use of activated charcoal reduces the oral bioavailability of olanzapine by up to 50-60%. Fluoxetine (60 mg once or 60 mg daily for 8 days) causes an increase in the maximum concentration of olanzapine by an average of 16% and a decrease in the clearance of olanzapine by an average of 16%. The degree of influence of this factor is significantly lower than the severity of individual differences in these indicators, so it is usually not recommended to change the dose of olanzapine when it is prescribed in combination with fluoxetine.

Fluvoxamine, an inhibitor of the CYP1A2 isoenzyme, reduces the clearance of olanzapine. The result is an average increase in olanzapine Cmax with fluvoxamine use by 54% in non-smoking women and 77% in smoking men, and an average increase in the area under the olanzapine pharmacokinetic curve (AUC) by 52% and 108%, respectively. Small doses of olanzapine should be given to patients receiving co-treatment with fluvoxamine.

In vitro studies using human liver microsomes have shown that olanzapine slightly inhibits the formation of valproate glucuronide (the main pathway of valproic acid metabolism). Valproic acid also has little effect on olanzapine metabolism in vitro, so a clinically significant pharmacokinetic interaction between olanzapine and valproic acid is unlikely.

According to in vitro studies using human liver microsomes, olanzapine also showed extremely low potential in suppressing the activity of the following cytochrome P 450 isoenzymes: CYP1A2, CYP2C9, CYP2C19, CYP2D6 and CYP3A. As with other antipsychotic medications, caution should be exercised when using olanzapine concomitantly with medications that prolong the QTc interval, as well as affect the central nervous system.

How to take, course of use and dosage

Inside, regardless of food intake.

The recommended therapeutic dose of Olanzapine Canon is 5 mg to 20 mg per day. The daily dose should be selected individually, depending on the patient’s clinical condition.

Schizophrenia in adults. The recommended starting dose of Olanzapine Canon is 10 mg once daily. Acute mania in bipolar disorder in adults. The recommended starting dose of Olanzapine Canon is 15 mg once daily as monotherapy or 10 mg once daily in combination with lithium or valproic acid. Maintenance therapy for bipolar disorder in adults. The recommended starting dose of Olanzapine Canon is 10 mg once daily. Patients receiving Olanzapine Canon for the treatment of acute mania are advised to continue maintenance therapy at the same dose.

Depression within bipolar disorder in adults. Olanzapine Canon in combination with fluoxetine should be administered once a day, in the evening. The initial dose is 5 mg olanzapine and 20 mg fluoxetine.

Antidepressant activity was confirmed with the use of olanzapine at a dose of 6-12 mg (average daily dose-7.4 mg) and fluoxitine at a dose of 25-30 mg (average daily dose -39.3 mg). If necessary, you can change the dosage of both olanzapine and fluoxetine.

Therapeutic resistant depression. Olanzapine Canon should be given in combination with fluoxetine once a day, in the evening. The initial dose is 5 mg olanzapine and 20 mg fluoxetine. If necessary, you can change the dosage of both olanzapine and fluoxetine.

Special patient groups

In elderly patients, reducing the initial dose (up to 5 mg per day) is usually not recommended, but it is possible in patients over 65 years of age with risk factors (see the section “Special instructions”).

Patients with liver and/or kidney diseases are recommended to reduce the initial dose to 5 mg / day. In moderate hepatic insufficiency (cirrhosis of the liver, class A and B according to the Child-Pugh classification of hepatic cell insufficiency in patients with cirrhosis of the liver), the initial dose is 5 mg / day, further dose increase is possible with caution. Women do not need to change the dosage compared to men.

In non-smoking patients, no dose adjustment is required in comparison with smokers. Reducing the initial dose may be recommended for patients with a combination of factors (female, elderly, non-smoker) that may slow down olanzapine metabolism.

Overdose

Common symptoms: tachycardia, agitation / aggressiveness, articulation disorders, various extrapyramidal disorders and consciousness disorders of varying severity (from sedation to coma).

Other clinically significant consequences: delirium, seizures, neuroleptic malignant syndrome, respiratory depression, aspiration, arterial hypertension or hypotension, cardiac arrhythmias ( The minimum dose for acute overdose with a fatal outcome according to studies is 450 mg, the maximum dose for overdose with a favorable outcome (survival) is 2000 mg.

Treatment: There is no specific antidote for olanzapine. It is not recommended to provoke vomiting. Standard procedures for overdose may be indicated (gastric lavage, use of activated charcoal). Co-use of activated charcoal reduces the oral bioavailability of olanzapine by up to 50-60%. Symptomatic treatment is indicated in accordance with the clinical condition and control over the functions of vital organs, including the treatment of arterial hypotension, circulatory disorders and maintenance of respiratory function. Do not use epinephrine, dopamine, or other sympathomimetics that are beta-adrenergic agonists, as stimulation of these receptors may worsen hypotension.

Special instructions

Clinical improvement can take several days and requires monitoring of the patient.

Neuroleptic malignant syndrome Neuroleptic malignant syndrome (NMS) (a potentially fatal symptom complex) can develop during treatment with any neuroleptics, including Olanzapine Canon, but to date there are no data confirming a reliable association between olanzapine use and the development of this condition. Clinical manifestations of neuroleptic malignant syndrome include a significant increase in body temperature, muscle rigidity, changes in mental status and vegetative disorders (unstable pulse or blood pressure, tachycardia, cardiac arrhythmias, increased sweating). Additional signs may include increased creatinine phosphokinase, myoglobinuria (rhabdomyolysis), and acute renal failure. Clinical manifestations of neuroleptic malignant syndrome or a significant increase in body temperature without other symptoms of neuroleptic malignant syndrome require the withdrawal of all neuroleptics, including Olanzapine Canon.

Tardive dyskinesia

Treatment with olanzapine is less frequently associated with the development of dyskinesia, which requires drug correction, than with the use of haloperidol. However, the risk of tardive dyskinesia should be considered during long-term neuroleptic therapy. If signs of tardive dyskinesia develop, it is recommended to reduce the dose or discontinue Olanzapine Canon. It should be borne in mind that when switching to Olanzapine Canon, symptoms of tardive dyskinesia may develop due to simultaneous discontinuation of previous therapy. Symptoms of tardive dyskinesia may increase or manifest after discontinuation of the drug. Parkinson’s disease

Efficacy in Parkinson’s disease does not exceed placebo (for the treatment of iatrogenic psychoses). The use of Olanzapine Canon is not recommended in the treatment of psychoses induced by taking dopamine receptor agonists in Parkinson’s disease, in such patients there is an increase in Parkinsonism symptoms and hallucinations.

Experience of use in elderly patients with psychosis on the background of dementia

Cerebrovascular adverse events (for example, stroke, transient ischemic attack), including fatal outcomes, are observed in elderly patients with psychosis on the background of dementia. In placebo-controlled studies, there was a higher incidence of cerebrovasular adverse events in patients in the olanzapine group compared to the placebo group. These patients had previous risk factors (history of cerebrovascular disorders, transient ischemic attack, arterial hypertension, smoking), as well as concomitant diseases and / or medication intake that were associated with time. with cerebrovascular disorders.

The efficacy of olanzapine in elderly patients with psychosis and dementia has not been established. The main risk factors for increased mortality in this group of patients treated with olanzapine are age > 80 years, sedation, concomitant use with benzodiazepines, or the presence of lung pathology (for example, pneumonia with or without aspiration). There are insufficient data to establish differences in the incidence of cerebrovascular disorders and / or mortality (compared to placebo), and in the risk factors in this group of patients with oral and intramuscular injections of olanzapine. Olanzapine Canon is not recommended for the treatment of patients with psychosis and dementia.

Developing the risk of sudden death

Clinical experience with all neuroleptics, including olanzapine, has shown a similar, dose-dependent, twofold increase in the risk of death due to acute heart failure compared to deaths due to acute heart failure in patients not taking neuroleptics.

Duration of the QT interval

Infrequently, clinically significant increases in the QT interval were observed in patients treated with olanzapine, while there were no significant differences with placebo in the incidence of cardiac adverse events. However, as with other antipsychotic agents, caution is recommended when prescribing Olanzapine Canon in combination with drugs that can prolong the QT interval, especially in elderly patients with congenital QT prolongation, congestive heart failure, myocardial hypertrophy, hypokalemia and hypomagnesemia.

Postural hypotension

Postural hypotension is infrequently observed in elderly patients. As with other antipsychotics, if Olanzapine Canon is prescribed to patients over 65 years of age, it is recommended to monitor blood pressure.

Thromboembolism

Venous thromboembolism is extremely rare during olanzapine therapy. No causal relationship has been established between olanzapine and venous thromboembolism. However, given that patients with schizophrenia often have acquired risk factors for venous thromboembolism, it is necessary to conduct a combined assessment of all possible risk factors for the development of this complication, including patient immobilization, and take the necessary preventive measures.

Liver function disorders

In some cases, taking olanzapine, as a rule, at the early stages of therapy is accompanied by a transient, asymptomatic increase in the indicators of” hepatic ” transaminases (ACT and ALT) in the blood serum. Rare cases of hepatitis have been reported. In very rare cases, hepatic cholestasis and other mixed liver damage were observed. Special precautions should be taken when increasing serum ACT and/or ALT values in patients with hepatic insufficiency, with a limited functional reserve of the liver, or in patients receiving treatment with potentially hepatotoxic drugs. If there is an increase in ACT and/or ALT values during olanzapine treatment, careful monitoring of the patient is required and, if necessary, a reduction in the dose of Olanzapine Canon. If hepatitis is detected, including hepatocellular, cholestatic or mixed, Olanzapine Canon should be discontinued.

Hyperglycemia and diabetes mellitus

There is a higher prevalence of diabetes mellitus in patients with schizophrenia. As with some other antipsychotic medications, very rare cases of hyperglycemia, diabetes mellitus, exacerbation of pre-existing diabetes mellitus, ketoacidosis, and diabetic coma have been reported. No causal relationship has been established between antipsychotic medications and these conditions. Careful clinical monitoring of patients with diabetes mellitus and patients with risk factors for developing diabetes mellitus is recommended. For all groups of patients, regardless of body mass index, there was a clinically significant increase in body weight. An increase of 7% or more from the average value after a short course of treatment (average duration-47 days) was observed very often (22.2%), an increase of 15% or more was frequent (4.2%) and an increase of 25% or more was infrequent (0.8%). In patients receiving longer treatment (at least 48 weeks), increases of > 7%, > 15%, and >25% were very frequent (64.4%,31.7%, and 12.3%, respectively).

Changes in the lipid profile

In patients treated with olanzapine, undesirable changes in the lipid spectrum are observed. Monitoring of the lipid profile and clinical follow-up are recommended. Epileptic seizures Olanzapine Canon should be used with caution in patients with a history of epileptic seizures or who are exposed to factors that reduce the threshold of convulsive readiness. In such patients, convulsive seizures are rarely observed during treatment with olanzapine. Hematological alterationsas with other antipsychotics, caution should be exercised when using olanzapine in patients with a reduced number of leukocytes and/or neutrophils in the peripheral blood due to various causes; with signs of inhibition or toxic impairment of bone marrow function under the influence of drugs in the anamnesis; with suppression of bone marrow function due to concomitant disease, radiotherapy or chemotherapy in the anamnesis; with hypereosinophilia or myeloproliferative a medical condition. In clinical studies, the use of olanzapine in patients with a history of clozapine-dependent neutropenia or agranulocytosis was not accompanied by relapses of these disorders. Neutropenia has been reported mainly in combination therapy with olanzapine and valproic acid. Anticholinergic activityolanzapine therapy is rarely accompanied by anticholinergic side effects. However, clinical experience with olanzapine in patients with concomitant diseases is limited, so caution is recommended when prescribing Olanzapine Canon to patients with clinically significant prostatic hypertrophy, paralytic bowel obstruction, and similar conditions. Dopaminergic Antagonismin vitro, olanzapine is antagonistic to dopamine receptors and, like other neuroleptics, can theoretically inhibit the action of levodopa and dopamine agonists. General activity in relation to the central nervous system. Due to the main effect of olanzapine on the central nervous system, caution should be exercised when using olanzapine in combination with other centrally acting drugs and alcohol. Suicid Risk of making a suicide attempt in patients with schizophrenia and bipolar disorder of the first type is due to these diseases themselves. In this regard, against the background of pharmacotherapy, careful monitoring of those patients with a particularly high risk of suicide is required. When prescribing Olanzapine Canon, care should be taken to minimize the number of tablets taken by the patient in order to reduce the risk of overdose. Discontinuation of therapy If olanzapine is abruptly discontinued, sweating, insomnia, tremor, nausea and vomiting are rare (0.01 – 0.1%). When the drug is discontinued, a gradual dose reduction is recommended. Children and adolescents under 18 years of age Olanzapine is not recommended for use in children and adolescents under 18 years of age, due to the lack of sufficient data on efficacy and safety. In short-term studies conducted in adolescents aged 13-17 years, there was a more significant increase in body weight and changes in the concentration of lipids and prolactin than in similar studies in adults.

Impact on the ability to drive vehicles Patients taking Olanzapine Canon should be careful when driving vehicles and working at work that requires rapid psychomotor reactions, as olanzapine can cause drowsiness and dizziness.

Form of production

Round, biconvex tablets, covered with a yellow film coating. The cross-section is yellow.

Active ingredient

Olanzapine

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Schizophrenia, Manic-depressive psychosis