Zalasta Ku-tab, 5 mg, tablets, dispersible in the oral cavity, 28 pcs.: instructions for use, reviews and analogues, prices in pharmacies. Buy and deliver to the nearest pharmacy or home in Moscow. Produce

Zalasta Ku-tab, 5 mg, tablets, dispersible in the oral cavity, 28 pcs.

Orally dispersible tablets Zalasta® Ku-tab quickly dissolve in the oral cavity under the influence of saliva, after which they are easily swallowed. Since the tablets are fragile, they should be taken immediately after removal from the blister. Alternatively, the tablet may be dissolved in a full glass of water immediately before use.

Orally dispersible tablets Zalasta® Ku-tab are bioequivalent to simple Zalasta® tablets, the rate and extent of absorption, dose and dosage regimen are also equivalent. Zalasta® Ku-tab can be used as an alternative to Zalasta® tablets.

Because food does not affect the absorption of the drug; Zalasta® Ku-tab tablets can be taken regardless of meals. If the drug is discontinued, a gradual dose reduction is recommended

Schizophrenia

. The recommended initial dose of the drug is 10 mg/day.

Episode of mania.

The initial dose is 15 mg in 1 dose for monotherapy or 10 mg/day as part of combination therapy.

Relapse prevention in bipolar disorder.

The recommended initial dose of the drug in remission is 10 mg/day. For patients already receiving Zalasta® Qu-tab for the treatment of an episode of mania, maintenance therapy is carried out in the same doses. During therapy with Zalasta® Qu-tab, in the event of a new manic, mixed or depressive episode, the dose of the drug should be increased, if necessary, with additional treatment of mood disorders, in accordance with clinical indications.

The daily dose of the drug for the treatment of schizophrenia, a manic episode, or the prevention of relapses of bipolar disorder can be 5–20 mg/day, depending on the clinical condition of the patient. Increasing the dose above the recommended initial dose is possible only after an adequate re-clinical assessment of the patient’s condition and is usually carried out at intervals of at least 24 hours.

Special patient groups

Elderly patients.

A reduction in the initial dose (to 5 mg/day) is usually not recommended, but is possible in patients over 65 years of age if there are risk factors.

Liver and/or kidney diseases.

For patients with liver and/or kidney diseases, it is recommended to reduce the initial dose to 5 mg/day. For moderate liver failure (cirrhosis, class A or B according to the Child-Pugh classification of hepatic cell failure in patients with liver cirrhosis), the initial dose is 5 mg/day, further dose increases are possible with caution.

Women

no change in dosage is required compared to men.

Smoking.

In non-smoking patients, no dose adjustment is required compared to smokers.

If the patient has more than one factor that can affect the absorption of the drug (female gender, elderly age, non-smokers), a reduction in the initial dose may be necessary. If necessary, further increase in dose is possible with caution.

Zalasta Ku-tab, dissolved tablet 5 mg No. 28

Compound.


active substance:
olanzapine	5 mg
10 mg
excipients: mannitol - 41.5/83 mg; MCC - 6/12 mg; crospovidone - 6/12 mg; low-substituted hypromellose LH-21 - 4.5/9 mg; aspartame - 0.5/1 mg; calcium silicate - 10/20 mg; magnesium stearate - 1.5/3 mg

Pharmachologic effect. Antipsychotic.

Method of administration and dose.

Because food does not affect the absorption of the drug; Zalasta® Ku-tab tablets can be taken regardless of meals. If the drug is discontinued, a gradual dose reduction is recommended

Schizophrenia

. The recommended initial dose of the drug is 10 mg/day.

Episode of mania.

The initial dose is 15 mg in 1 dose for monotherapy or 10 mg/day as part of combination therapy.

Relapse prevention in bipolar disorder.

Special patient groups

Elderly patients.

A reduction in the initial dose (to 5 mg/day) is usually not recommended, but is possible in patients over 65 years of age if there are risk factors.

Liver and/or kidney diseases.

Women

no change in dosage is required compared to men.

Smoking.

In non-smoking patients, no dose adjustment is required compared to smokers.

Release form.

Oral dispersible tablets, 5 mg, 10 mg.

7 tablets each in a blister. 4 bl. placed in a cardboard box.

Manufacturer.

KRKA Polska Sp. h. o.o., st. Ruwnolegla 5, 02-235 Warsaw, Poland.

Representative office of JSC "KRKA, d.d., Novo Mesto" in the Russian Federation/organization receiving consumer complaints: 125212, Moscow, Golovinskoye Shosse, 5, bldg. 1, fl. 22.

Tel.; Fax.

When packaging and/or packaging at a Russian enterprise, the following is indicated: KRKA-RUS LLC, 143500, Russia, Moscow region, Istra, st. Moskovskaya, 50.

Tel.; Fax.

Conditions for dispensing from pharmacies.

On prescription.

Zalasta Ku-tab KRKA TB orally dispersible 10mg N 28

Zalasta Qu-tab TB diperg in the mouth 10 mg N 28

Release form

Lozenges

Package

28 pcs.

pharmachologic effect

Zalasta Ku-tab has antipsychotic and neuroleptic effects.

Olanzapine is an antipsychotic drug (neuroleptic) with a wide pharmacological spectrum of action. The antipsychotic effect is due to the blockade of dopamine D2 receptors of the mesolimbic and mesocortical systems; sedative effect - blockade of adrenergic receptors of the reticular formation of the brain stem; antiemetic effect - blockade of dopamine D2 receptors in the trigger zone of the vomiting center; hypothermic effect - blockade of dopamine receptors of the hypothalamus. In addition, it has an effect on muscarinic, adrenergic, H1-histamine and some subclasses of serotonin receptors.

Olanzapine significantly reduces productive (delusions, hallucinations) and negative symptoms (hostility, suspiciousness, emotional and social autism) of psychosis. Rarely causes extrapyramidal disorders.

Pharmacokinetics

The absorption of olanzapine is high and does not depend on food intake; the time required to achieve the maximum concentration of the drug in the blood plasma (TCmax) after oral administration is 5-8 hours. Penetrates histohematic barriers, incl. blood-brain barrier (BBB). Metabolized in the liver, no active metabolites are formed, the main circulating metabolite is a glucuronide, does not penetrate the BBB. Smoking, gender and age affect T1/2 and plasma clearance. In persons over 65 years of age, T1/2 is 51.8 hours and plasma clearance is 17.5 l/hour; in persons under 65 years of age - 33.8 hours and plasma clearance - 18.2 l/hour. Plasma clearance is lower in patients with liver failure, women and non-smokers compared with corresponding groups of individuals. It is excreted mainly by the kidneys (60%) in the form of metabolites.

Indications

— the drug is indicated for the treatment of schizophrenia.

Zalasta Ku-tab effectively supports the improvement of clinical symptoms during long-term treatment in patients with an initial positive reaction to the drug.

- Zalasta Qu-tab is indicated for the treatment of moderate to severe episodes of mania.

In patients with manic episodes who have responded well to olanzapine therapy, the drug is indicated for the prevention of relapses of mania in bipolar disorder.

Contraindications

hypersensitivity to olanzapine or other components of the drug;
angle-closure glaucoma;
children under 18 years of age (efficacy and safety have not been established);
lactation period.

With caution: renal failure, liver failure, prostatic hyperplasia, paralytic ileus, epilepsy, history of convulsive syndrome, leukopenia and/or neutropenia of various origins, myelosuppression of various origins, incl. myeloproliferative diseases, hypereosinophilic syndrome, cardiovascular and cerebrovascular diseases or other conditions predisposing to hypotension, congenital prolongation of the QT interval on the ECG (increased corrected QT interval (QTc) on the ECG), or in the presence of conditions that can potentially cause prolongation of the QT interval (eg, simultaneous administration of drugs that prolong the QT interval, congestive heart failure, hypokalemia, hypomagnesemia), old age, as well as simultaneous use of other centrally acting drugs; phenylketonuria, immobilization, pregnancy.

Use during pregnancy and breastfeeding

Due to limited experience with the drug in pregnant women, olanzapine should be used only if the expected benefit to the mother justifies the potential risk to the fetus. Women should be informed of the need to inform their doctor about an existing or planned pregnancy during olanzapine therapy. There are isolated reports of tremor, arterial hypertension, lethargy and drowsiness in children born to mothers taking olanzapine in the third trimester of pregnancy. The study found that olanzapine is excreted into breast milk. The mean dosage (mg/kg) the child received when maternal steady-state concentrations were reached was 1.8% of the maternal olanzapine dose (mg/kg). Breastfeeding is not recommended during olanzapine therapy.

special instructions

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 preceding decompensation, which could become a predisposing factor. For patients with diabetes mellitus or with risk factors for developing this disease, regular clinical monitoring and monitoring of blood glucose levels is recommended. If lipid levels change, therapy adjustments are required.

When olanzapine is stopped abruptly, very rarely (less than 0.01%) the following symptoms may develop: sweating, insomnia, tremor, anxiety, nausea or vomiting. When discontinuing the drug, a gradual dose reduction is recommended.

Experience with the use of olanzapine in patients with psychosis in Parkinson's disease caused by taking dopaminomimetics. Olanzapine is not recommended for the treatment of psychosis in Parkinson's disease caused by dopaminomimetics. Symptoms of parkinsonism and hallucinations increase. However, olanzapine was not superior to placebo in treating psychosis.

Olanzapine is not indicated for the treatment of psychosis and/or behavioral disorders in dementia due to increased mortality and increased risk of cerebrovascular events (stroke, transient ischemic attack). The increase in mortality was independent of olanzapine dose or duration of therapy. Risk factors predisposing to increased mortality include: age over 65 years, dysphagia, sedation, malnutrition and dehydration, lung diseases (for example, pneumonia, including aspiration), concomitant use of benzodiazepines. However, the increased incidence of death in the olanzapine groups compared with placebo was independent of these risk factors.

With antipsychotic therapy, improvement in the patient's clinical condition occurs within a period of several days to several weeks. During this period, the patient needs careful monitoring.

Liver dysfunction. At the beginning of therapy, an asymptomatic increase in liver transaminases (ALT and AST) is possible. Caution should be exercised when prescribing olanzapine in patients with initially elevated AST and/or ALT levels, hepatic impairment and conditions potentially limiting liver function, and those taking hepatotoxic drugs. If ALT and/or AST increase during drug therapy, medical monitoring of the patient and, possibly, a reduction in the dose of the drug are recommended. If hepatitis (including hepatocellular, cholestatic or mixed) is diagnosed, olanzapine should be discontinued.

Hematological changes. The drug should be used with caution in patients with leukopenia and/or neutropenia of any origin, myelosuppression of drug origin, as well as during radiation or chemotherapy, due to concomitant diseases, in patients with hypereosinophilic conditions or myeloproliferative diseases. Neutropenia was often observed with simultaneous use of olanzapine and valproic acid (see section "Side effects").

Neuroleptic malignant syndrome (NMS). NMS is a potentially life-threatening condition associated with treatment with antipsychotic drugs (neuroleptics), incl. olanzapine. Clinical manifestations of NMS: fever, muscle rigidity, impaired consciousness, autonomic disorders (unstable pulse or labile blood pressure, tachycardia, increased sweating, arrhythmias). Additional symptoms of NMS: increased CPK, myoglobinuria (against the background of rhabdomyolysis) and acute renal failure. If symptoms of NMS develop, as well as an increase in body temperature for no apparent reason, it is necessary to discontinue all antipsychotics, incl. olanzapine.

Tardive dyskinesia. Olanzapine therapy was associated with a significantly lower incidence of tardive dyskinesia compared with haloperidol. The risk of developing tardive dyskinesia increases with increasing duration of treatment. If signs of this condition occur in a patient taking olanzapine, the drug should be discontinued or the dose reduced. Symptoms of dyskinesia may temporarily increase after discontinuation of the drug.

General activity in relation to the central nervous system. Caution should be exercised when using other centrally acting drugs and alcohol simultaneously.

Cerebrovascular adverse events including stroke in elderly patients with dementia. Postural hypotension is uncommon in older adults. In patients over 65 years of age, it is recommended to periodically monitor blood pressure. Olanzapine should be administered with caution to patients with established QTc prolongation, especially the elderly, with congenital long QT syndrome, congestive heart failure, myocardial hypertrophy, hypokalemia and hypomagnesemia.

When taking olanzapine, very rarely (less than 0.01%) cases of venous thromboembolism have been reported. A cause-and-effect relationship between olanzapine therapy and venous thrombosis has not been established. Because patients with schizophrenia often have acquired risk factors for venous thrombosis, all possible other factors (eg, immobilization) should be identified and preventive measures taken.

Zalasta Ku-tab tablets contain aspartame, a source of phenylalanine. The drug may not be safe for people with phenylketonuria.

Impact on the ability to drive a car and other mechanical means:

Since olanzapine may cause drowsiness and dizziness, patients should exercise caution when operating technical devices, incl. when driving a car.

Compound

1 tablet contains: active substance: olanzapine 10 mg; excipients: cellactose (a spray-dried compound consisting of 75% alpha-lactose monohydrate and 25% cellulose powder), pregelatinized starch; corn starch; anhydrous colloidal silicon dioxide; magnesium stearate

Directions for use and doses

Zalasta Ku-tab lozenges quickly dissolve in the oral cavity under the influence of saliva, after which they are easily swallowed. Since the tablets are fragile, they should be taken immediately after removal from the blister. Alternatively, the tablet may be dissolved in a full glass of water immediately before use. Zalasta Qu-tab lozenges are bioequivalent to simple Zalasta tablets, the speed and extent of absorption, doses and dosage regimen are also equivalent. Zalasta Ku-tab can be used as an alternative to Zalasta tablets.

Because food does not affect the absorption of the drug; Zalasta Ku-tab lozenges can be taken regardless of meals. If the drug is discontinued, a gradual dose reduction is recommended.

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

Episode of mania: the initial dose is 15 mg in one dose in monotherapy or 10 mg per day in combination therapy.

Prevention of relapse in bipolar disorder: the recommended initial dose of the drug in remission is 10 mg per day. For patients already receiving Zalasta Qu-tab to treat an episode of mania, maintenance therapy is carried out at the same doses. During therapy with Zalasta Ku-tab, in the event of a new manic, mixed or depressive episode, the dose of the drug should be increased, if necessary, with additional treatment of mood disorders, in accordance with clinical indications.

The daily dose of the drug for the treatment of schizophrenia, a manic episode or the prevention of relapses of bipolar disorder can be 5-20 mg/day, depending on the clinical condition of the patient. Increasing the dose above the recommended initial dose is possible only after an adequate re-clinical assessment of the patient's condition and is usually carried out at intervals of at least 24 hours.

Special patient groups:

In elderly patients, a reduction in the initial dose (to 5 mg per day) is usually not recommended, but is possible in patients over 65 years of age if there are risk factors (see section "Special Instructions").

Women do not require any changes in dosage compared to men.

In non-smoking patients, no dose adjustment is required compared to smoking patients.

If the patient has more than one factor that can affect the absorption of the drug (female gender, old age, non-smoker), it may be necessary to reduce the initial dose. If necessary, further increase in dose is possible with caution.

Side effects

From the central (CNS) and peripheral nervous system: very often - drowsiness; often - dizziness, akathisia, parkinsonism, dyskinesia; rarely - convulsive syndrome (usually against the background of a history of convulsive syndrome); very rarely - neuroleptic malignant syndrome, dystonia (including oculogyric crisis) and tardive dyskinesia. When olanzapine is abruptly discontinued, symptoms such as sweating, insomnia, tremor, anxiety, nausea or vomiting are very rarely observed.

From the cardiovascular system: often - arterial hypotension (including orthostatic); infrequently - bradycardia with or without collapse; very rarely - increased QTc interval on ECG, ventricular tachycardia/fibrillation and sudden death, thromboembolism (including pulmonary embolism and deep vein thrombosis).

From the gastrointestinal tract: often - transient anticholinergic effects, incl. constipation and dry mouth; very rarely - pancreatitis.

Metabolic and nutritional disorders: very often - weight gain; often - increased appetite; very rarely - hyperglycemia and/or decompensation of diabetes mellitus, sometimes manifested by ketoacidosis or coma, including fatal outcome; hypertritlyceridemia, hypercholesterolemia, hypothermia.

Hepato-biliary disorders: often - transient, asymptomatic increase in the level of “liver” transaminases (alanine aminotransferase (ART), aspartate aminotransferase (AST)), especially at the beginning of treatment; rarely - hepatitis (including hepatocellular, cholestatic or mixed liver damage).

From the hematopoietic organs and lymphatic system: often - zosinophilia; rarely - leukopenia; very rarely - thrombocytopenia, neutropenia.

From the musculoskeletal system: very rarely - rhabdomyolysis.

From the genitourinary system: very rarely - urinary retention, priapism.

From the skin and subcutaneous tissue: rarely - photosensitivity reactions.

Allergic reactions: rarely - skin rash; very rarely - anaphylactoid reactions, angioedema, itching or urticaria.

Other: often - asthenia, peripheral edema; very rarely - alopecia.

Laboratory parameters: hyperprolactinemia is very common, but clinical manifestations (for example, gynecomastia, galactorrhea and breast enlargement) are rare. In most patients, prolactin levels spontaneously normalized without discontinuation of therapy. Uncommon: increased levels of creatine phosphokinase (CPK); very rarely - increased levels of alkaline phosphatase (ALP) and total bilirubin.

In older patients with dementia, studies have shown a higher incidence of death and cerebrovascular events (stroke, transient ischemic attacks). Gait disturbances and falls were very common in this category of patients. Pneumonia, fever, lethargy, erythema, visual hallucinations, and urinary incontinence were also common.

Among patients with drug-induced (while taking dopamine agonists) psychoses associated with Parkinson's disease, worsening of parkinsonian symptoms and the development of hallucinations were often recorded.

There is evidence of the development of neutropenia (4.1%) during combination therapy with valproic acid in patients with bipolar mania. Concomitant therapy with valproic acid or lithium increases the frequency (> 10%) of tremor, dry mouth, increased appetite and weight gain. Speech impairments were also frequently reported (from 1 to 10%). In the first 6 weeks of combination therapy with lithium, the incidence of weight gain increases. Long-term therapy with olanzapine (up to 12 months) for the purpose of preventing relapses in patients with bipolar disorder was accompanied by an increase in body weight.

Drug interactions

Potential drug interactions affecting the metabolism of olanzapine: Olanzapine is metabolized by the CYP1A2 enzyme, therefore inhibitors or inducers of cytochrome P450 isoenzymes that exhibit specific activity against CYP1A2 may affect the pharmacokinetic parameters of olanzapine.

CYP1A2 inducers: The clearance of olanzapine may be increased in patients who smoke or when taking carbamazepine concomitantly, resulting in decreased olanzapine plasma concentrations. Clinical observation is recommended because some cases require increasing the dose of the drug.

CYP1A2 inhibitors: fluvoxamine, a specific CYP1A2 inhibitor, significantly reduces the clearance of olanzapine. The average increase in Cmax of olanzapine after taking fluvoxamine in non-smoking women was 54%, and in smoking men - 77%. The mean increase in olanzapine AUC in these patient categories was 52% and 108%, respectively. In patients taking fluvoxamine or any other CYP1A2 inhibitor (eg, ciprofloxacin), it is recommended that olanzapine therapy be initiated at lower doses. A dose reduction of olanzapine may also be required if CYP1A2 inhibitors are added to therapy.

Drug interactions that do/do not affect the bioavailability of olanzapine: Activated charcoal reduces the oral absorption of olanzapine by 50-60% and should therefore be taken at least 2 hours before or after taking olanzapine.

Fluoxetine (a CYP450 inhibitor), single doses of magnesium or aluminum-containing antacids, or cimetidine do not affect the pharmacokinetics of olanzapine.

The potential for olanzapine to interfere with other medications

Olanzapine may reduce the effects of direct and indirect dopamine agonists. In vitro, olanzapine does not inhibit the main isoenzymes of CYP450 (for example, 1A2, 2D6, 2C9, 2C19, 3A4). In vivo, no inhibition of the metabolism of the following active substances was found: tricyclic antidepressants (CYP2D6), warfarin (CYP2C9), theophylline (CYP1A2) and diazepam (CYP3A4 and 2C19).

No interaction was detected when used simultaneously with lithium or biperiden. Therapeutic monitoring of plasma valproic acid levels showed that no changes in valproic acid doses are required when administered concomitantly with olanzapine.

Caution should be exercised when using other centrally acting drugs simultaneously. Although a single dose of alcohol (45 mg/70 kg) does not have a pharmacokinetic effect, taking alcohol with olanzapine may be accompanied by an increased depressive effect on the central nervous system.

Overdose

Symptoms: very often (>10%) - tachycardia, agitation/aggression, dysarthria, various extrapyramidal symptoms, decreased level of consciousness from lethargy to coma; in less than 2% of cases - delirium, convulsions, coma, neuroleptic malignant syndrome (NMS), respiratory depression, aspiration, increased or decreased blood pressure, cardiac arrhythmia; in very rare cases - cardiopulmonary failure. The minimum dose of olanzapine for an acute overdose with a fatal outcome is 450 mg; the maximum dose for an overdose with a favorable outcome (survival) is 1500 mg. Treatment: gastric lavage, taking activated charcoal (reduces the bioavailability of olanzapine by 60%), symptomatic treatment under the control of vital functions, including treatment of arterial hypotension and vascular collapse, maintaining respiratory function. There is no specific antidote. It is not recommended to induce vomiting, use epinephrine, dopamine or other sympathomimetics with beta-adrenomimetic activity, because the latter can aggravate arterial hypotension. To identify possible arrhythmias, monitoring of cardiovascular activity is necessary. The patient should be under continuous medical supervision until complete recovery.

Storage conditions

Store at a temperature not exceeding 25°C, in the original packaging. Keep out of the reach of children.

Best before date

5 years.

Conditions for dispensing from pharmacies

Dispensed with a doctor's prescription

Zalasta Qu-tab tablet dispersion in the oral cavity 5 mg x28

ATX code: N05AH03 (Olanzapine) Active substance: olanzapine (olanzapine) Rec.INN registered by WHO Dosage form ZALASTA® KU-TAB tab. dispersible in the oral cavity 5 mg: 28 or 56 pcs. reg. No.: LSR-005803/09 dated 07/17/09 - Registration period. beat not limited Release form, composition and packaging Tablets dispersible in the oral cavity 1 tab. olanzapine 5 mg

7 pcs. - blisters (4) - cardboard packs. 7 pcs. - blisters (8) - cardboard packs.

Clinical and pharmacological group: Antipsychotic drug (neuroleptic) Pharmacotherapeutic group: Antipsychotic (neuroleptic) drug Pharmacological action Olanzapine is an antipsychotic drug (neuroleptic) with a wide pharmacological spectrum of action. The antipsychotic effect is due to the blockade of dopamine D2 receptors of the mesolimbic and mesocortical system, the sedative effect is due to the blockade of adrenergic receptors of the reticular formation of the brain stem, the antiemetic effect is due to the blockade of dopamine D2 receptors of the trigger zone of the vomiting center, the hypothermic effect is due to the blockade of dopamine receptors of the hypothalamus. In addition, it has an effect on muscarinic, adrenergic, H1-histamine and some subclasses of serotonin receptors.

Pharmacokinetics The absorption of olanzapine is high, does not depend on food intake, the time required to achieve the maximum concentration of the drug in the blood plasma (TCmax) after oral administration is 5-8 hours. Penetrates histohematic barriers, incl. blood-brain barrier (BBB). Metabolized in the liver, no active metabolites are formed, the main circulating metabolite is a glucuronide, does not penetrate the BBB. Smoking, gender and age affect T1/2 and plasma clearance. In persons over 65 years of age, T1/2 is 51.8 hours and plasma clearance is 17.5 l/hour, in persons under 65 years of age it is 33.8 hours and plasma clearance is 18.2 l/hour. Plasma clearance is lower in patients with liver failure, women and non-smokers compared with corresponding groups of individuals. It is excreted mainly by the kidneys (60%) in the form of metabolites.

Indications - the drug is indicated for the treatment of schizophrenia.

Zalasta® Qu-tab effectively supports the improvement of clinical symptoms during long-term treatment in patients with an initial positive reaction to the drug.

— Zalasta® Qu-tab is indicated for the treatment of moderate to severe episodes of mania.

In patients with manic episodes who have responded well to olanzapine therapy, the drug is indicated for the prevention of relapses of mania in bipolar disorder.

ICD-10 codes ICD-10 code Indication F20 Schizophrenia F21 Schizotypal disorder F22 Chronic delusional disorders F23 Acute and transient mental disorders F25 Schizoaffective disorders F29 Non-organic psychosis, unspecified F30 Manic episode F31 Bipolar affective disorder

Dosage regimen Zalasta® Ku-tab lozenges quickly dissolve in the oral cavity under the influence of saliva, after which they are easily swallowed. Since the tablets are fragile, they should be taken immediately after removal from the blister. Alternatively, the tablet may be dissolved in a full glass of water immediately before use. Zalasta® Ku-tab lozenges are bioequivalent to simple Zalasta® tablets, the speed and extent of absorption, doses and dosage regimen are also equivalent. Zalasta® Ku-tab can be used as an alternative to Zalasta® tablets.

Because food does not affect the absorption of the drug; Zalasta® Ku-tab lozenges can be taken regardless of meals. If the drug is discontinued, a gradual dose reduction is recommended.

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

Episode of mania: the initial dose is 15 mg in one dose in monotherapy or 10 mg per day in combination therapy.

Prevention of relapse in bipolar disorder: the recommended initial dose of the drug in remission is 10 mg per day. For patients already receiving Zalasta® Qu-tab for the treatment of an episode of mania, maintenance therapy is carried out in the same doses. During therapy with Zalasta® Qu-tab, in the event of a new manic, mixed or depressive episode, the dose of the drug should be increased, if necessary, with additional treatment of mood disorders, in accordance with clinical indications.

Special patient groups:

Women do not require any changes in dosage compared to men.

In non-smoking patients, no dose adjustment is required compared to smoking patients (see section “Interaction with other drugs”).

Side effects Classification of the frequency of side effects (WHO):

very often >1/10

often from > 1/100 to infrequently from > 1/1000 to rarely from >1/10000 to very rarely from From the central (CNS) and peripheral nervous system: very often - drowsiness, often - dizziness, akathisia, parkinsonism, dyskinesia, rarely - convulsive syndrome (usually against the background of a history of convulsive syndrome), very rarely - neuroleptic malignant syndrome (see section "Special Instructions"), dystonia (including oculogyric crisis) and tardive dyskinesia. When olanzapine is abruptly discontinued, symptoms such as sweating, insomnia, tremor, anxiety, nausea or vomiting are very rarely observed.

From the cardiovascular system: often - arterial hypotension (including orthostatic), infrequently - bradycardia with or without collapse, very rarely - increase in the QTc interval on the ECG (see section "Special Instructions"), ventricular tachycardia/fibrillation and sudden death (see section "Special Instructions"), thromboembolism (including pulmonary embolism and deep vein thrombosis).

From the gastrointestinal tract: often - transient anticholinergic effects, incl. constipation and dry mouth, very rarely - pancreatitis.

Metabolic and nutritional disorders: very often - weight gain, often - increased appetite, very rarely - hyperglycemia and/or decompensation of diabetes mellitus, sometimes manifested by ketoacidosis or coma, including fatal outcome, hypertritlyceridemia, hypercholesterolemia, hypothermia.

Hepato-biliary disorders: often - transient, asymptomatic increase in the level of "liver" transaminases (alanine aminotransferase (ART), aspartate aminotransferase (AST)), especially at the beginning of treatment (see "Special Instructions"), rarely - hepatitis (incl. hepatocellular, cholestatic or mixed liver damage).

From the hematopoietic organs and lymphatic system: often - zosinophilia, rarely - leukopenia, very rarely - thrombocytopenia, neutropenia.

From the musculoskeletal system: very rarely - rhabdomyolysis.

From the genitourinary system: very rarely - urinary retention, priapism.

From the skin and subcutaneous tissue: rarely - photosensitivity reactions.

Allergic reactions: rarely - skin rash, very rarely - anaphylactoid reactions, angioedema, itching or urticaria.

Other: often - asthenia, peripheral edema, very rarely - alopecia.

Laboratory parameters: hyperprolactinemia is very common, but clinical manifestations (for example, gynecomastia, galactorrhea and breast enlargement) are rare. In most patients, prolactin levels spontaneously normalized without discontinuation of therapy. Uncommon: increased levels of creatine phosphokinase (CPK); very rare: increased levels of alkaline phosphatase (ALP) and total bilirubin.

Contraindications for use: hypersensitivity to olanzapine or other components of the drug,

- angle-closure glaucoma,

- children under 18 years of age (efficacy and safety have not been established),

- lactation period.

Use during pregnancy and lactation Due to limited experience with the drug in pregnant women, olanzapine should be used during pregnancy only if the expected benefit justifies the potential risk to the fetus. Women should be informed of the need to inform their doctor about an existing or planned pregnancy during olanzapine therapy. There are isolated reports of tremor, hypertension, lethargy and somnolence in children born to mothers taking olanzapine in the third trimester of pregnancy. The study found that olanzapine is excreted into breast milk. The mean dosage (mg/kg) the child received when maternal steady-state concentrations were reached was 1.8% of the maternal olanzapine dose (mg/kg). Breastfeeding is not recommended during olanzapine therapy.

Use for liver dysfunction Take with caution in patients suffering from liver failure. Use for impaired renal function Take with caution in patients suffering from renal failure. Use in children The drug is contraindicated in children under 18 years of age (efficacy and safety have not been established). Special instructions 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 preceding decompensation, which could become a predisposing factor. For patients with diabetes mellitus or with risk factors for developing this disease, regular clinical monitoring and monitoring of blood glucose levels is recommended. If lipid levels change, therapy adjustments are required.

With antipsychotic therapy, improvement in the patient's clinical condition occurs within a period of several days to several weeks. During this period, the patient needs careful monitoring.

General activity in relation to the central nervous system. Caution should be exercised when using other centrally acting drugs and alcohol simultaneously.

Zalasta® Ku-tab tablets contain aspartame, a source of phenylalanine. The drug may not be safe for people with phenylketonuria.

Impact on the ability to drive a car and other mechanical means:

Since olanzapine may cause drowsiness and dizziness, patients should exercise caution when operating technical devices, incl. when driving a car.

Overdose Symptoms: very common (> 10%) with olanzapine overdose are: tachycardia, agitation/aggression, dysarthria, various extrapyramidal symptoms, decreased level of consciousness from lethargy to coma, in less than 2% of cases occur: delirium, convulsions, coma, malignant neuroleptic syndrome, respiratory depression, aspiration, arterial hypertension or hypotension, cardiac arrhythmias, and in very rare cases, cardiopulmonary failure. The minimum dose of olanzapine for an acute overdose with a fatal outcome is 450 mg; the maximum dose for an overdose with a favorable outcome (survival) is 1500 mg.

Treatment: There is no specific antidote. It is not recommended to induce vomiting. It is necessary to carry out: gastric lavage, taking activated charcoal (reduces the bioavailability of olanzapine by 60%), symptomatic treatment under the control of vital functions, including treatment of arterial hypotension and vascular collapse, maintaining respiratory function. The use of epinephrine, dopamine or other sympathomimetics with beta-adrenomimetic activity is not recommended, because the latter can aggravate arterial hypotension. To identify possible arrhythmias, monitoring of cardiovascular activity is necessary. The patient should be under continuous medical supervision until complete recovery.

Drug interactions Potential drug interactions affecting the metabolism of olanzapine: Olanzapine is metabolized by the CYP1A2 enzyme, therefore inhibitors or inducers of cytochrome P450 isoenzymes that exhibit specific activity against CYP1A2 may affect the pharmacokinetic parameters of olanzapine.

Fluoxetine (a CYP450 inhibitor), single doses of magnesium or aluminum-containing antacids, or cimetidine do not affect the pharmacokinetics of olanzapine.

The potential for olanzapine to interfere with other medications

Olanzapine may reduce the effects of direct and indirect dopamine agonists. In vitro, olanzapine does not inhibit the main CYP450 isoenzymes (for example, 1A2, 2D6, 2C9, 2C19, 3A4). In vivo, no inhibition of the metabolism of the following active substances was found: tricyclic antidepressants (CYP2D6), warfarin (CYP2C9), theophylline (CYP1A2) and diazepam (CYP3A4 and 2C19).

No interaction was detected when used simultaneously with lithium or biperiden. Therapeutic monitoring of valproic acid levels in plasma has shown that no changes in valproic acid doses are required when administered concomitantly with olanzapine (see section “Side Effects”).

Conditions for dispensing from pharmacies The drug is dispensed with a prescription. Storage conditions and periods Store at a temperature not exceeding 25°C, in the original packaging. Keep out of the reach of children. Shelf life: 5 years.

ZALASTA KU-TAB TAB. DISPERS. IN THE ORAL CAVITY 5MG No. 28

For patients with diabetes mellitus or with risk factors for developing this disease, regular clinical monitoring and monitoring of blood glucose levels is recommended. If lipid levels change, therapy adjustments are required. When olanzapine is stopped abruptly, very rarely (less than 0.01%) the following symptoms may develop: sweating, insomnia, tremor, anxiety, nausea or vomiting. When discontinuing the drug, a gradual dose reduction is recommended.

Anticholinergic activity. Since clinical experience with olanzapine in people with concomitant diseases is limited, the drug should be prescribed with caution to patients with prostatic hyperplasia, paralytic ileus. Experience with olanzapine in patients with psychosis in Parkinson's disease caused by taking dopaminomimetics. Olanzapine is not recommended for the treatment of psychosis in Parkinson's disease caused by dopaminomimetics. Symptoms of parkinsonism and hallucinations increase. However, olanzapine was not superior to placebo in treating psychosis.

Risk factors predisposing to increased mortality include: age over 65 years, dysphagia, sedation, malnutrition and dehydration, lung diseases (for example, pneumonia, including aspiration), concomitant use of benzodiazepines. However, the increased incidence of death in the olanzapine groups compared with placebo was independent of these risk factors. With antipsychotic therapy, improvement in the patient's clinical condition occurs within a period of several days to several weeks. During this period, the patient needs careful monitoring. Liver dysfunction. At the beginning of therapy, an asymptomatic increase in liver transaminases (ALT and AST) is possible.

In patients with initially elevated AST and/or ALT levels, with liver failure and conditions that potentially limit liver function, and those taking hepatotoxic drugs, caution should be exercised when prescribing olanzapine. If ALT and/or AST increase during drug therapy, medical monitoring of the patient and, possibly, a reduction in the dose of the drug are recommended. If hepatitis (including hepatocellular, cholestatic or mixed) is diagnosed, olanzapine should be discontinued. Hematological changes.

The drug should be used with caution in patients with leukopenia and/or neutropenia of any origin, myelosuppression of drug origin, as well as during radiation or chemotherapy, due to concomitant diseases, in patients with hypereosinophilic conditions or myeloproliferative diseases. Neutropenia was often observed with simultaneous use of olanzapine and valproic acid (see section "Side effects").

Convulsive syndrome. Olanzapine should be used cautiously in patients with a history of seizures or the presence of factors that lower the seizure threshold. Seizures were rarely reported while taking olanzapine. Tardive dyskinesia. Olanzapine therapy was associated with a significantly lower incidence of tardive dyskinesia compared with haloperidol.

The risk of developing tardive dyskinesia increases with increasing duration of treatment. If signs of this condition occur in a patient taking olanzapine, the drug should be discontinued or the dose reduced. Symptoms of dyskinesia may temporarily increase after discontinuation of the drug. General activity in relation to the central nervous system.

Caution should be exercised when using other centrally acting drugs and alcohol simultaneously. Cerebrovascular adverse events including stroke in elderly patients with dementia. Postural hypotension is uncommon in older adults.

In patients over 65 years of age, it is recommended to periodically monitor blood pressure (BP). Olanzapine should be administered with caution to patients with established QTc prolongation, especially the elderly, with congenital long QT syndrome, congestive heart failure, myocardial hypertrophy, hypokalemia and hypomagnesemia. Cases of venous thromboembolism have been reported very rarely (less than 0.01%) when taking olanzapine. A cause-and-effect relationship between olanzapine therapy and venous thrombosis has not been established.

Because patients with schizophrenia often have acquired risk factors for venous thrombosis, all possible other factors (eg, immobilization) should be identified and preventive measures taken. Zalasta Ku-tab tablets contain aspartame, a source of phenylalanine. The drug may not be safe for people with phenylketonuria.