Universal reference book for medicines
Name of the preparation: ZALASTA ® KU-TAB (ZALASTA Q-TAB)

Active substance: olanzapine

Type: Antipsychotic drug (antipsychotic)

Manufacturer: KRKA (Slovenia) manufactured by KRKA POLSKA (Poland)
Composition, form of production and packaging
Tablets dispersible in the oral cavity
1 tab.

olanzapine 10 mg

7 pcs.
- blisters (4) - packs of cardboard.
7 pcs.
- blisters (8) - packs of cardboard.
Tablets dispersible in the oral cavity 1 tab.

olanzapine 15 mg

7 pcs.
- blisters (4) - packs of cardboard.
7 pcs.
- blisters (8) - packs of cardboard.
Tablets dispersible in the oral cavity 1 tab.

olanzapine 20 mg

7 pcs.
- blisters (4) - packs of cardboard.
7 pcs.
- blisters (8) - packs of cardboard.
Tablets dispersible in the oral cavity 1 tab.

olanzapine 5 mg

7 pcs.
- blisters (4) - packs of cardboard.
7 pcs.
- blisters (8) - packs of cardboard.
Tablets dispersible in the oral cavity 1 tab.

olanzapine 7.5 mg

7 pcs.
- blisters (4) - packs of cardboard.
7 pcs.
- blisters (8) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2014.

PHARMACHOLOGIC EFFECT

Olanzapine is an antipsychotic agent (neuroleptic) with a broad pharmacological spectrum of action.
The antipsychotic effect is due to blockade of dopamine D2 receptors of the mesolimbic and mesocortical system; sedative effect - adrenoreceptor blockade of the reticular formation of the brainstem; antiemetic effect - blockade of dopamine D2 receptors in the trigger zone of the vomiting center; hypothermic action - blockade of dopamine receptors of the hypothalamus. In addition, it affects muscarinic, adrenergic, H1-histamine and some subclasses of serotonin receptors.
Olanzapine significantly reduces productive (delusions, hallucinations) and negative symptoms (hostility, suspicion, emotional and social autism) of psychoses.
Rarely causes extrapyramidal disorders.
PHARMACOKINETICS

Absorption of olanzapine is high, does not depend on food intake;
the time required to reach the maximum concentration of the drug in the blood plasma (TC max)after oral administration is 5-8 hours. It penetrates through the histogematic barriers, including blood-brain barrier (BBB). Metabolized in the liver, active metabolites are not formed, the main circulating metabolite is glucuronide, does not penetrate the GEB. Smoking, sex and age affect T 1/2 and plasma clearance. In persons over 65 years, T 1/2 is 51.8 hours and plasma clearance is 17.5 l / h; in persons younger than 65 years - 33.8 h and plasma clearance - 18.2 l / h. Plasma clearance is lower in patients with hepatic insufficiency, women and non-smokers in comparison with the corresponding groups of individuals. It is excreted mainly by 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 in long-term treatment in patients with initial positive reaction to the drug.

- Zalast ® Cu-tab is indicated for the treatment of moderate or severe episodes of mania.

In patients with manic episodes with a good effect of olanzapine therapy, the drug is indicated for the prevention of recurrence of mania in bipolar disorder.

DOSING MODE

Tablets for resorption Zalasta ® Ku-tab quickly dissolve in the oral cavity under the influence of saliva, after which they are easily swallowed.
Because the tablets are fragile, they should be taken immediately after removal from the blister. Alternatively, just before use, the tablet can be dissolved in a full glass of water. Tablets for resorption Zalasta ® Ku-tab are bioequivalent to simple Zalast ® tablets, speed and degree of absorption, dose and dosage regimen are also equivalent. Zalasta ® Cu-tab can be used as an alternative to Zalast ® tablets.
Because
food does not affect the absorption of the drug, tablets for resorption Zalasta ® Ku-tab can be taken regardless of food intake. In case of cancellation, a gradual dose reduction is recommended.
Schizophrenia: the recommended initial dose of the drug is 10 mg per day.

The episode of mania: the initial dose is 15 mg in one dose with monotherapy or 10 mg per day as part of a combination therapy.

Prophylaxis of relapses in bipolar disorder: the recommended initial dose of the drug in a state of remission is 10 mg per day.
For patients already receiving Zalast ®Cu-tab for the treatment of a manic episode, maintenance therapy is administered in the same doses. On the background of therapy with Zalast ® Cu-tab, if a new manic, mixed or depressive episode develops, if necessary, increase the dose of the drug with additional treatment of mood disorders, in accordance with clinical indications.
The daily dose of the drug in the treatment of schizophrenia, a manic episode or the prevention of recurrence of bipolar disorder may be 5-20 mg / day, depending on the clinical condition of the patient.
An increase in the dose above the recommended initial dose is only possible after an adequate repeated clinical assessment of the patient's condition and is usually performed with an interval of at least 24 hours.
Special patient groups:

In elderly patients, a reduction in the initial dose (up to 5 mg per day) is usually not recommended, but it is possible in patients older than 65 years with risk factors (see section "Special instructions").

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

In non-smoking patients, dose adjustments compared to smokers (see "Interactions with other drugs") are not required.

If the patient has more than one factor that can influence the absorption of the drug (female, elderly, non-smokers), it may be necessary to reduce the initial dose.
If necessary, further increase in dose with caution.
SIDE EFFECT

Classification of the incidence of adverse events (WHO):

very often> 1/10

often from> 1/100 to <1/10

infrequently from> 1/1000 to <1/100

rarely from> 1/10000 to <1/1000

very rarely from <1/10000, including individual messages.

From the central (CNS) and peripheral nervous system: very often - drowsiness;
often - dizziness, akathisia, parkinsonism, dyskinesia; rarely - convulsive syndrome (more often in the background of convulsive syndrome in anamnesis); very rarely - malignant neuroleptic syndrome (see section "Special instructions"), dystonia (including oculogic crisis) and tardive dyskinesia. With a sharp abolition of olanzapine, symptoms such as sweating, insomnia, tremor, anxiety, nausea, or vomiting are very rarely noted.
From the side of the cardiovascular system: often - arterial hypotension (including orthostatic);
infrequently - a bradycardia with a collapse or without; very rarely - an 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 artery embolism and deep vein thrombosis).
From the gastrointestinal tract: often - transitory anticholinergic effects, incl.
constipation and dry mouth; very rarely - pancreatitis.
Disorders of metabolism and nutrition: 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; hypertriglyceridemia, hypercholesterolemia, hypothermia.
Hepatobiliary disorders: often - transient, asymptomatic increase in the level of "liver" transaminases (alanine aminotransferase (ART), aspartate aminotransferase (ACT)), especially at the beginning of treatment (see "Special instructions");
rarely - hepatitis (including hepatocellular, cholestatic or mixed liver damage).
On the part of the organs of hematopoiesis and lymphatic system: often - zosinophilia;
rarely - leukopenia; very rarely - thrombocytopenia, neutropenia.
On the part of the organs of the musculoskeletal system: very rarely - rhabdomyolysis.

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

From the skin and subcutaneous tissue: infrequently - the reaction of photosensitization.

Allergic reactions: rarely - skin rash;
very rarely - anaphylactoid reactions, angioedema, skin itching or urticaria.
Other: often - asthenia, peripheral edema;
very rarely - alopecia.
Laboratory parameters: very often hyperprolactinemia, but clinical manifestations (for example, gynecomastia, galactorrhea and breast enlargement) are rare.
In most patients, the level of prolactin spontaneously normalized without the abolition of therapy. Infrequent - increase in the level of creatine phosphokinase (CK); very rarely - an increase in the level of alkaline phosphatase (APF) and total bilirubin.
In elderly patients with dementia, a large incidence of deaths and cerebrovascular disorders (stroke, transient ischemic attacks) is documented in studies.
Very frequent in this category of patients were violations of gait and fall. Also often observed pneumonia, fever, lethargy, erythema, visual hallucinations and urinary incontinence.
Among patients with drug (against the background of dopamine agonists) psychoses on the background of Parkinson's disease often recorded worsening of parkinsonian symptoms and the development of hallucinations.

There are data on the development of neutropenia (4.1%) against a combination therapy with valproic acid in patients with bipolar mania.
Simultaneous therapy with valproic acid or lithium helps to increase the frequency (> 10%) of tremors, dry mouth, increase appetite and weight gain. Violations of speech were often recorded (from 1 to 10%). In the first 6 weeks of combined therapy with lithium, the incidence of weight gain increases. Long-term therapy with olanzapine (up to 12 months) in order to prevent relapse in patients with bipolar disorder was accompanied by an increase in body weight.
CONTRAINDICATIONS

- hypersensitivity to olanzapine or other components of the drug;

- an angle-closure glaucoma;

- Children under 18 years of age (effectiveness and safety not established);

lactation period.

With caution: renal insufficiency, hepatic insufficiency, prostatic hyperplasia, paralytic intestinal obstruction, epilepsy, history of convulsive syndrome, leukopenia and / or neutropenia of various genesis, myelosuppression of various genesis, incl.
myeloproliferative diseases, hypereosinophilic syndrome, cardiovascular and cerebrovascular diseases or other conditions predisposing to arterial hypotension, congenital increase in the QT interval on the ECG (increase in the QT interval corrected on the ECG) or in the presence of conditions potentially capable of causing an increase in the QT interval (for example, simultaneous administration of drugs that extend the QT interval, congestive heart failure, hypokalemia, hypomagnesemia), advanced age, and simultaneous administration rugih centrally acting drugs; phenylketonuria, immobilization, pregnancy.
PREGNANCY AND LACTATION

Due to the limited experience of 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 the doctor about the onset or planned pregnancy with olanzapine therapy. There are isolated reports of tremors, arterial hypertension, lethargy and drowsiness in children born to mothers who took olanzapine in the third trimester of pregnancy. The study found that olanzapine is excreted in breast milk. The average dosage (mg / kg) received by a child when the mother's equilibrium concentration reached equilibrium was 1.8% of the mother's olanzapine dose (mg / kg). It is not recommended to breast-feed on the background of olanzapine therapy.
APPLICATION FOR FUNCTIONS OF THE LIVER

Take with caution patients suffering from kidney failure.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

Take with caution patients suffering from liver failure.

APPLICATION FOR CHILDREN

The drug is contraindicated in children under the age of 18 years (efficacy and safety not established).

SPECIAL INSTRUCTIONS

There are very few 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 a previous decompensation of weight gain, which could become a predisposing factor. Patients with diabetes or with risk factors for the development of this disease are recommended regular clinical control and monitoring of blood glucose levels. When the level of lipids changes, correction of therapy is required.
With a sharp discontinuation of olanzapine, it is very rare (less than 0.01%) to develop the following symptoms: sweating, insomnia, tremor, anxiety, nausea, or vomiting.
With the withdrawal of 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 used with caution in patients with prostatic hyperplasia, paralytic intestinal obstruction.
Experience with olanzapine in patients with psychosis in Parkinson's disease caused by dopaminomimetic treatment.
Olanzapine is not recommended for the treatment of psychoses in Parkinson's disease caused by dopaminomimetic treatment. The symptoms of parkinsonism and hallucinations increase. However, olanzapine was not superior to placebo in the treatment of psychoses.
Olanzapine is not indicated for the treatment of psychoses and / or behavioral disorders in dementia , due to increased mortality and increased risk of cerebrovascular disorders (stroke, transient ischemic attacks).
The increase in mortality does not depend on the dose of olanzapine or the duration of therapy. Risk factors predisposing to increased mortality include: age over 65 years, dysphagia, sedation, malnutrition and dehydration, lung diseases (eg, pneumonia, including aspiration), simultaneous reception of benzodiazepines. However, the increased incidence of death in olanzapine compared with placebo did not depend on these risk factors.
With antipsychotic therapy, the improvement in the clinical state of the patient occurs in the period from several days to several weeks.
During this period, the patient needs careful observation.
Dysfunction of the liver.
At the beginning of therapy, an asymptomatic increase in liver transaminases (ALT and ACT) is possible. Patients with initially elevated levels of ACT and / or ALT, with hepatic insufficiency and conditions potentially limiting the functionality of the liver, as well as those taking hepatotoxic drugs, caution should be exercised when prescribing olanzapine. When ALT and / or ACT are increased against the background of drug therapy, it is recommended that medical supervision of the patient and, possibly, a reduction in the dose of the drug be recommended. When diagnosing hepatitis (including hepatocellular, cholestatic or mixed), olanzapine should be discarded.
Hematologic changes.
The drug should be used with caution in patients with leukopenia and / or neutropenia of any genesis, myelosuppression of drug origin, as well as radiation or chemotherapy, due to concomitant diseases, in patients with hypereosinophilic conditions or myeloproliferative diseases. Neutropenia has often been noted with the simultaneous use of olanzapine and valproic acid (see the "Side effect" section).
Malignant neuroleptic syndrome (CNS).
ZNS is a potentially life-threatening condition associated with antipsychotic medication (neuroleptics), incl. olanzapine.Clinical manifestations of ZNS: fever, rigidity of muscles, impaired consciousness, vegetative disorders (unstable pulse or labile blood pressure, tachycardia, increased sweating, arrhythmias). Additional symptoms of ZNS: increased CK, myoglobinuria (against rhabdomyolysis) and acute renal failure. With the development of symptoms of the ZNS, as well as an increase in body temperature for no apparent reason, it is necessary to cancel all neuroleptics, including. olanzapine.
Convulsive syndrome.
Olanzapine should be carefully prescribed to patients with a history of seizures or the presence of factors that reduce the threshold of convulsive readiness. On the background of taking olanzapine, seizures were rarely recorded.
Late dyskinesia.
The therapy with olanzapine was accompanied by a significantly lower incidence of late dyskinesia, in comparison with haloperidol. The risk of developing tardive dyskinesia increases with increasing duration of treatment. If there are signs of this condition, the patient taking olanzapine should cancel the drug or reduce its dose. Symptoms of dyskinesia may temporarily increase after the drug is discontinued.
General activity in relation to the central nervous system.
Care should be taken when using other drugs of central action and alcohol.
Cerebrovascular adverse events, including stroke in elderly patients with dementia.
In elderly people, postural arterial hypotension is not often observed. Patients over 65 years of age are recommended to periodically monitor blood pressure. Olanzapine should be administered with caution to patients with an established QTc interval, 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%) recorded cases of development of venous thromboembolism.
The causal relationship between olanzapine treatment and venous thrombosis has not been established. Since patients with schizophrenia often present acquired risk factors for venous thrombosis, should identify all possible other factors (for example, immobilization) and take preventive measures.
Tablets Zalasta ® Ku tab contain aspartame - phenylalanine source. The drug may not be safe for people suffering from phenylketonuria.
Effect on the driving ability and other mechanical means:
Because olanzapine may cause drowsiness and dizziness, patients should be exercised when working with technical devices, including while driving.
OVERDOSE

Symptoms: very frequent (> 10%) with an overdose of olanzapine are tachycardia, agitation / aggression, dysarthria, various extrapyramidal symptoms, decreased level of consciousness from the retardation to coma; less than 2% of the cases arise: delirium, seizures, coma, neuroleptic malignant syndrome, respiratory depression, aspiration, hypertension or hypotension, cardiac arrhythmias; in very rare cases - cardio-pulmonary insufficiency. The minimum dose of olanzapine in acute lethal overdose - 450 mg, maximum registered dose overdose with a favorable outcome (survival) - 1500 mg.
Treatment: there is no specific antidote.
It is not recommended to provoke vomiting. Necessary to: gastric lavage, activated charcoal (reduces the bioavailability of olanzapine by 60%), symptomatic treatment under the control of vital functions, including treatment of hypotension and circulatory collapse, maintaining respiratory function. We do not recommend the use of epinephrine, dopamine, or other sympathomimetic agents with beta-Adrenomimeticalkie activity because the latter may worsen hypotension. To detect possible arrhythmias requires monitoring of cardiovascular activity. The patient should be under continuous medical supervision until complete recovery.
DRUG INTERACTION

Potential drug interactions affecting the metabolism of olanzapine: olanzapine metabolizing enzymes CYP1A2, therefore, inhibitors, or inducers of cytochrome P450 isoenzymes, exhibiting specific activity towards CYP1A2 can affect the pharmacokinetic parameters of olanzapine.
Inducers of CYP1A2: olanzapine clearance may be increased in patients who smoke or while taking carbamazepine, leading to a decrease in olanzapine plasma concentrations. Recommended clinical observation, because Some cases require increasing doses of the drug.
Inhibitors of CYP1A2: Fluvoxamine, a specific inhibitor of CYP1A2 - significantly reduces the clearance of olanzapine. The average increase in C maxolanzapine after administration of fluvoxamine in nonsmoking women was 54%, while male smokers - 77%. The average increase in the area under curve AUC of olanzapine in these categories of patients was 52% and 108%. Patients taking fluvoxamine or any other inhibitors of CYP1A2 (eg, ciprofloxacin), olanzapine therapy is recommended to start with smaller doses. Reducing the dose of olanzapine may also be required in the case of adherence to therapy CYP1A2 inhibitors.
Drug interactions affecting / not affecting the bioavailability of olanzapine: activated charcoal reduces the absorption of olanzapine orally 50-60%, however it should be taken at least 2 hours before or after olanzapine.
Fluoxetine inhibitor (CYP450), a single dose of magnesium or aluminum containing antacids or cimetidine did not affect the pharmacokinetics of olanzapine.
The potential ability of olanzapine to affect other medicinal products
Olanzapine may weaken the effect of direct and indirect dopamine agonists. Under conditions in vitro olanzapine does not inhibit the major isoenzymes CYP450 (e.g., 1A2, 2D6, 2C9, 2C19, ZA4). In vivo it found no inhibition of metabolism of the following active substances: the tricyclic antidepressants (CYP2D6), warfarin (CYP2C9), theophylline (CYP1A2) and diazepam (CYP3A4 and 2C19).
There were no interaction while the use of lithium or biperidenom. The therapeutic monitoring of valproic acid content in plasma showed that at a simultaneous administration with doses of olanzapine changes of valproic acid is not required (see. "Side effect" section).
Caution must be exercised while the use of other drugs central action. Despite the fact that a single dose of alcohol (45 mg / 70 kg) has no effect pharmacokinetic, alcohol together with olanzapine may be accompanied by increased depressive effect on the central nervous system.
TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

Store at a temperature not higher than 25 ° C, in the original package.
Keep out of the reach of children. Shelf life - 5 years.
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