ZALASTA Q-TAB PILLS 10MG

QUALITY AND QUANTITATIVE COMPOSITION

1 pill dispersed in the mouth, contains:

Active substance:

Olanzapine 5 mg and 10 mg

PHARMACEUTICAL FORM

Tablets 5 mg and 10 mg: round slightly biconvex pills of yellow color. The presence of minor individual inclusions and marbling.

CLINICAL DATA

Therapeutic indications

The drug is indicated for the treatment of schizophrenia.

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

The drug Zalasta Q-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 relapses of mania in bipolar disorder.

Dosage and administration

Tablets that are dispersed in the mouth, Zalasta Q-Tab quickly dissolve in the oral cavity under the action of saliva, and then easily swallowed. Since the pills are fragile, they should be taken immediately after removal from the blister. Alternatively, immediately before taking the pill can be dissolved in a full glass of water.

Tablets that are dispersed in the mouth, Zalasta Q-Tab are bioequivalent to Zalasta® simple tablets,the rate and extent of absorption, doses and dosing regimen are also equivalent. Zalasta Q-Tab can be used as an alternative to Zalasta® tablets.

Since food does not affect the absorption of the drug, pills that are dispersed in the mouth, Zalasta® Koo-tab can be taken regardless of the meal. In case of drug withdrawal, gradual reduction of the dose is recommended.

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

Episode Mania: the initial dose is 15 mg in a single dose for 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 the drug Zalasta Q-Tab for the treatment of an episode of mania, supportive therapy is carried out in the same doses. Against the background of therapy with Zalasta Q-Tab, if a new manic, mixed or depressive episode develops, if necessary, increase the dose of the drug with additional treatment for mood disorders, in accordance with clinical indications.

The daily dose of the drug in the treatment of schizophrenia, manic episode or prevention of relapses of bipolar disorder can be 5 to 20 mg / day, depending on the patient’s clinical condition. Increasing the dose over the recommended initial dose is possible only after an adequate re-clinical assessment of the patient’s condition and is usually performed at intervals 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 over 65 years of age with risk factors (see the section "Special Instructions").

Patients with liver and / or kidney disease recommended reduction of the initial dose to 5 mg / day. In moderate hepatic insufficiency (cirrhosis, class A or B according to the Child-Pugh hepatocellular insufficiency in patients with liver cirrhosis), the initial dose is 5 mg / day, a further increase in the dose with caution is possible.

For women no change in dosage required compared to by men.

In non-smoking patients dose adjustment compared with smoking patients (see section "Interaction with other drugs") is not required.

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

Special instructions and precautionary measures

There are very rare developmental messages. hyperglycemia and / or decompensation of diabetesoccasionally accompanied by the development of ketoacidosis or ketoacid coma, including several fatal cases. In some cases, an increase in body weight preceding decompensation was noted, which could become a predisposing factor. Patients with diabetesor with risk factors for the development of this disease, regular clinical monitoring and control of blood glucose levels are recommended.

At change of level of lipids correction of therapy is required.

With a sharp cessation of reception olanzapine very rarely (less than 0.01%) may develop the following symptoms: sweating, insomnia, tremor, anxiety, nausea or vomiting. With the abolition of the drug is recommended gradual dose reduction.

Anticholinergic activity. Since clinical experience with olanzapine in people with comorbidities is limited, the drug should be carefully prescribed to patients with prostatic hyperplasia, paralytic intestinal obstruction.

Experience of using olanzapine in patients with psychosis in Parkinson's disease, caused by taking dopaminomimetik. Olanzapine is not recommended for the treatment of psychosis in Parkinson's disease caused by taking dopaminomimetic. Symptoms of parkinsonism and hallucinations are increasing. At the same time, olanzapine did not exceed placebo in terms of the effectiveness of treatment of psychosis.

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 an increase in mortality include: age over 65, dysphagia, sedation, malnutrition and dehydration, lung diseases (for example, pneumonia, including aspiration), simultaneous administration of benzodiazepines.However, the increased frequency of death in the olanzapine groups compared with placebo did not depend on these risk factors.

With antipsychotic therapy, an improvement in the patient’s clinical condition occurs in a period from several days to several weeks. During this period, the patient needs careful observation.

Liver dysfunction. At the beginning of therapy, an asymptomatic increase in liver transaminases (ALT and AST) is possible. In patients with initially elevated levels of AST and / or ALT, with liver failure and conditions that potentially limit the functionality of the liver, as well as taking hepatotoxic drugs, caution should be exercised when prescribing olanzapine. With increasing ALT and / or AST during therapy with a drug, medical observation of the patient and, possibly, a reduction in the dose of the drug are recommended. When diagnosing hepatitis (including hepatocellular, cholestatic or mixed), olanzapine should be canceled.

Hematologic 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 has often been observed with the simultaneous use of olanzapine and valproic acid (see the “Side Effects” section).

Malignant neuroleptic syndrome (SNS). MNS is a potentially life-threatening condition associated with antipsychotic therapy (antipsychotics), including 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 NNS: increased CPK, myoglobinuria (against the background of rhabdomyolysis) and acute renal failure. With the development of symptoms of ZNS, as well as an increase in body temperature for no apparent reason, it is necessary to cancel all antipsychotics, including olanzapine.

Convulsive syndrome. Olanzapine should be carefully prescribed to patients with a history of convulsions or the presence of factors that reduce the threshold of convulsive readiness. With olanzapine, seizures were rarely recorded.

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

Total activity against the central nervous system. Caution should be exercised while using other drugs of central action and alcohol.

Cerebrovascular adverse events, including stroke in elderly patients with dementia. Older people rarely observed postural hypotension. In patients older than 65 years, it is recommended to periodically monitor blood pressure (BP). Olanzapine should be used with caution in patients with an established increase in the QTc interval, especially the elderly, with congenital syndrome of prolonged QT interval, congestive heart failure, myocardial hypertrophy, hypokalemia and hypomagnesia.

When olanzapine is taken very rarely (less than 0.01%), cases of venous thromboembolism have been reported. The causal relationship between olanzapine therapy and venous thrombosis has not been established. Since 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 Q-Tab pills contain aspartame - a source of phenylalanine. The drug may not be safe for people suffering from phenylketonuria.

Interaction with other drugs

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

Inductors CYP1A2: clearance of olanzapine can be increased in patients who smoke or while taking Carbamazepine, which leads to a decrease in plasma concentration of olanzapine. Clinical observation is recommended, since some cases require an increase in the dose of the drug.

Inhibitors of CYP1A2: Fluvoxamine, a specific inhibitor of CYP1A2 - significantly reduces the clearance of olanzapine. The average increase in the maximum concentration (Cmax) of olanzapine after taking fluvoxamine in non-smoking women was 54%, and in smoking men, 77%. The average increase in the area under the concentration-time curve (AUC) of olanzapine in these categories of patients was 52% and 108%, respectively. In patients taking fluvoxamine or any other CYP1A2 inhibitor (for example, ciprofloxacin), olanzapine therapy is recommended to start with smaller doses. A reduction in the dose of olanzapine may also be required if CYP1A2 inhibitors are added to therapy.

Drug interactions that affect / not affect the bioavailability of olanzapine: Activated carbon reduces the absorption of olanzapine when taken orally by 50-60%, so it should be taken at least 2 hours before or after taking olanzapine.

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

Potential ability of olanzapine to affect other drugs

Olanzapine may weaken the effects of direct and indirect dopamine agonists.

In conditions in vitro olanzapine does not inhibit the major isoenzymes of CYP450 (for example, 1A2, 2D6, 2C9, 2C19, 3A4). In vivo, no metabolism of the following active substances was detected: tricyclic antidepressants (CYP2D6), Warfarin (CYP2C9), theophylline (CYP1A2) and diazepam (CYP3A4 and 2C19).

No interaction was found when used simultaneously with lithium or biperiden.

Therapeutic monitoring of the content of valproic acid in plasma showed that, when administered simultaneously with olanzapine, changes in the doses of valproic acid are not required (see the “Adverse Effects” section).

Caution should be exercised while using other drugs of central action. Despite the fact that a single dose of alcohol (45 mg / 70 kg) does not have a pharmacokinetic effect, alcohol intake with olanzapine may be accompanied by an increase in the depressive effect on the central nervous system.

Pregnancy and breastfeeding

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 about the need to inform the doctor about the occurrence or planned pregnancy during olanzapine therapy. There are isolated reports of tremor, 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 secreted in breast milk. The average dosage (mg / kg) received by the child upon reaching the equilibrium concentration in the mother was 1.8% of the dose of mother olanzapine (mg / kg).Breast-feeding during olanzapine therapy is not recommended.

Influence on ability to drive a car and other mechanisms

Since olanzapine can cause drowsiness and dizziness, patients should exercise caution when working with technical devices, including when driving.

Side effects

From the central (CNS) and peripheral nervous system: very often drowsiness; often - dizziness, akathisia, parkinsonism, dyskinesia; rarely, convulsive syndrome (more often with a history of convulsive syndrome); very rarely - neuroleptic malignant syndrome (see section "Special instructions"), dystonia (including oculograptic crisis) and tardive dyskinesia. With the abrupt cancellation of olanzapine, symptoms such as sweating, insomnia, tremor, anxiety, nausea, or vomiting are very rarely noted.

Since the cardiovascular system: often - arterial hypotension (including orthostatic); infrequently - bradycardia with or without collapse; very rarely, an increase in the QTs 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 (GIT): often - transient anticholinergic effects, incl. constipation and dry mouth; very rarely - pancreatitis.

Metabolism and nutrition disorders: very often - weight gain; often - increased appetite; very rarely - hyperglycemiaand / or decompensation of diabetes mellitus, sometimes manifested by ketoacidosis or coma, including fatal outcome; hypertriglyceridemia, hypercholesterolemia, hypothermia.

Hepato-biliary disorders: often - transient, asymptomatic elevation of “liver” transaminases (alanine aminotransferase (ALT), aspartate aminotransferase (AST)), especially at the beginning of treatment (see “Special instructions”); rarely, hepatitis (including hepatocellular, cholestatic, or mixed liver damage).

From the side of blood-forming organs and lymphatic system: often - eosinophilia; rarely, leukopenia; very rarely - thrombocytopenia, neutropenia.

From the organs of the musculoskeletal system: very rarely - rhabdomyolysis.

On the part of the genitourinary system: very rarely - urinary retention, priapism.

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

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

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