Buy Zalasta tablets 10 mg 28 pcs

Zalasta pills 10 mg 28 pcs

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Active ingredients


Release form



Active ingredient: Olanzapine (Olanzapinum) Active substance concentration (mg): 10

Pharmacological effect

Antipsychotic, neuroleptic.


Olanzapine absorption is high, does not depend on food intake; Tmax after oral administration is 5–8 h. Protein binding is 93% in the concentration range from 7 to 1000 ng / ml. Olanzapine binds mainly albumin and α1-glycoprotein. Penetrates histohematogenous barriers, incl. BBB. Metabolized in the liver, active metabolites are not formed, the main circulating metabolite - glucuronide - does not penetrate through the BBB. Smoking, sex and age affect T1 / 2 and plasma clearance. In persons older than 65 years, T1 / 2 is 51.8 h and plasma clearance is 17.5 l / h; in persons younger than 65 years old - 33.8 h and plasma clearance - 18.2 l / h. Plasma clearance is lower in patients with hepatic insufficiency, women and non-smoking patients in comparison with the respective groups of individuals. However, the degree of influence of age, gender or smoking on clearance and T1 / 2 of olanzapine is insignificant compared with the individual variability of pharmacokinetics between individuals. Excreted mainly by the kidneys (60%) as metabolites.


Symptomatic therapy of painful and inflammatory processes of various origins, including: - inflammatory and degenerative diseases of the musculoskeletal system: • rheumatoid arthritis; • seronegative arthritis: ankylosing spondylitis - ankylosing spondylitis, psoriatic arthritis, reactive arthritis (Reiter's syndrome); • gout, pseudogout; • osteoarthritis; - pain syndrome: • headache; • tendonitis, bursitis, myalgia, neuralgia, sciatica; • post-traumatic and postoperative pain syndrome; • pain syndrome in oncological diseases; • algomenorrhea.


Angle-closure glaucoma; - children up to 18 years of age (efficacy and safety have not been established); - lactation period; - galactose intolerance, lapp lactase deficiency or glucose-galactose absorption disorder; - hypersensitivity to olanzapine or other components of the drug.

Use during pregnancy and lactation

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 There are reports of several fatal cases. In some cases, an increase in body weight preceding decompensation was noted, which could become a predisposing factor. Patients with diabetes mellitus and risk factors for the development of this disease are recommended to have regular clinical monitoring and control of blood glucose levels. If you change lipid levels, therapy must be adjusted. If you suddenly stop taking olanzapine, very rarely (less than 0.01%) may develop the following symptoms: insomnia, tremor, anxiety, nausea or vomiting. With the abolition of the drug, a gradual reduction in dose is recommended. Anti-cholinergic activity. Since clinical experience with olanzapine in people with comorbidities is limited, the drug should be used with caution in patients with prostatic hyperplasia and paralytic intestinal obstruction. Experience using olanzapine in patients with Parkinson's psychoses caused by dopaminomimetic drugs. 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 was not superior to placebo in the treatment of psychosis. Olanzapine is not indicated for the treatment of psychoses and / or behavioral disorders in dementia due to increased mortality and an 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, the patient’s clinical condition improves from a few days to a few weeks. During this period, the patient needs careful observation. Liver function disorders.At the beginning of therapy, an asymptomatic increase in liver transaminases (ALT and ACT) is possible. In patients with initially elevated levels of ACT and / or ALT, 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 ACT during drug therapy, medical observation of the patient is recommended, and possibly a reduction in the dose of the drug. When diagnosing hepatitis (including hepatocellular, cholestatic, or mixed), olanzapine must be canceled. 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 has often been observed with the simultaneous use of olanzapine and valproic acid (see “Side effects”). Malignant neuroleptic syndrome. Potentially life-threatening condition associated with therapy with antipsychotics (neuroleptics), incl. olanzapine. It is characterized by the following clinical manifestations: fever, muscle stiffness, impaired consciousness, autonomic disturbances (unstable pulse or labile blood pressure, tachycardia, increased sweating, arrhythmias). Additional symptoms of NNS: increased CPK, myoglobinuria (in the presence 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. Congestive 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. General 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. 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 hypomagnesemia. . The causal relationship between olanzapine therapy and vein thrombosis has not been established. Since patients with schizophrenia often have acquired risk factors for venous thrombosis, all possible other factors (such as immobilization) should be identified and preventive measures taken. Zalast pills contain lactose. The drug should not be taken in patients with rare hereditary problems of intolerance to galactose, Lappa lactase deficiency or impaired glucose-galactose absorption. Influence on the ability to drive a car or perform work requiring increased speed of physical and mental reactions. During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and psychomotor reactions.
Dosage and administration
The drug is administered orally, 1 time / day. Since food does not affect the absorption of the drug, pills can be taken regardless of the meal. In case of drug withdrawal, a gradual dose reduction is recommended. In schizophrenia, the recommended initial dose of the drug is 10 mg / day. In episodes of mania, the initial dose is 15 mg per dose with monotherapy or 10 mg / day as part of combination therapy. The recommended initial dose of the drug in remission is 10 mg / day.For patients already receiving Zalasta for the treatment of an episode of mania, supportive therapy is carried out in the same doses. With Zalast treatment, if a new manic, mixed or depressive episode develops, the dose of the drug should be increased with additional treatment for mood disorders, in accordance with clinical indications. -20 mg / day, depending on the clinical condition of the patient. 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. In elderly patients, a reduction in the initial dose (up to 5 mg / day) is usually not recommended, but it is possible in patients over 65 years of age with risk factors. Patients with liver and / or kidney diseases are recommended to reduce the initial dose to 5 mg / day. In moderate liver failure (cirrhosis, class A or B according to Child-Pugh hepatocellular insufficiency in patients with cirrhosis of the liver), the initial dose is 5 mg / day, a further increase in dose with caution is possible. Women do not need changes in dosing compared to men In non-smoking patients, dose adjustment is not required compared with smoking patients. If the patient has more than one factor that can affect the absorption of the drug (female, old age, non-smoker), it is possible buet lowering initial dosage. If necessary, a further dose increase with caution is possible.

Side effects

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 can affect the pharmacokinetic parameters of olanzapine. taking carbamazepine, which leads to a decrease in the concentration of olanzapine in the blood plasma. Clinical observation is recommended, sincesome cases require an increase in the dose of the drug. CYP1A2 inhibitors: fluvoxamine - a specific inhibitor of CYP1A2 - 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 average increase in olanzapine AUC in these categories of patients was 5 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 treatment. Drug interactions that affect / do not affect the bioavailability of olanzapine. Activated carbon reduces the absorption of olanzapine when taken orally by 50–60%, so it should be taken no less than 2 hours before or after taking olanzapine. Fluoxetine (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 influence other drugs. Olanzapine can weaken the effect of direct and indirect dopamine agonists. In vitro, olanzapine does not inhibit the major isoenzymes of CYP450 (for example, 1A2, 2D6, 2C9, 2C19, ZA4). In vivo metabolism of the following active substances was not found to be inhibited: tricyclic antidepressants (CYP2D6), warfarin (CYP2C9), theophylline (CYP1A2) and diazepam (CYP3A4 and 2C19). There were no interactions with simultaneous use with lithium or biperiden. Therapeutic monitoring of plasma valproic acid showed that, while prescribing olanzapine, changes in valproic acid doses are not required (see the “Side Effects” section). Care should be taken when using other centrally acting drugs. Despite the fact that a single dose of alcohol (45 mg / 70 kg) does not have a pharmacokinetic effect, taking alcohol with olanzapine may be accompanied by an increase in the depressive effect on the central nervous system.


Classification of the incidence of side effects (WHO): very often (more than 1/10), often (from more than 1/100 to less than 1/10), infrequently (from more than 1/1000 to less than 1/100), rarely from (more than / 10 000 to less 1 / 1000), very rarely from (less than 1/10 000, including individual messages). From the CNS and peripheral nervous system: very often - drowsiness; often - dizziness, akathisia, parkinsonism,dyskinesia; seldom - a convulsive syndrome (more often against the background of a convulsive syndrome in the anamnesis); very rarely, malignant neuroleptic syndrome, dystonia (including oculogy crisis) and tardive dyskinesia. With abrupt cancellation of olanzapine, symptoms such as sweating, insomnia, tremor, anxiety, nausea, or vomiting are very rare. From the cardiovascular system: often - arterial hypotension (including orthostatic); infrequently - bradycardia with or without collapse; very rarely - an increase in the QTc interval on the ECG, ventricular tachycardia / fibrillation and sudden death, thromboembolism (including pulmonary artery embolism and deep vein thrombosis). On the part of the digestive system: often - transient anticholinergic effects, including constipation and dry mouth, transient, asymptomatic elevation of hepatic transaminase (ALT, ACT), especially at the beginning of treatment; rarely, hepatitis (including hepatocellular, cholestatic, or mixed liver damage); very rarely - pancreatitis, increased levels of alkaline phosphatase and total bilirubin. On the metabolic side: very often - an increase in body weight often - increased appetite; very rarely, hyperglycemia and / or decompensation of diabetes mellitus, sometimes manifested by ketoacidosis or coma, including a fatal outcome; hypertriglyceridemia, hypercholesterolemia, hypothermia. For the blood-forming organs: often - eosinophilia; rarely, leukopenia; very rarely - thrombocytopenia, neutropenia. From the musculoskeletal system: very rarely - rhabdomyolysis. From the urogenital system: very rarely - urinary retention, priapism. From the skin and subcutaneous tissue: rarely - photosensitization reactions. Allergic reactions: rarely - skin rash; very rarely - anaphylactoid reactions, angioedema, pruritus or urticaria. Other: often - asthenia, peripheral edema; very rarely - alopecia. Laboratory parameters: very often - hyperprolactinemia, but clinical manifestations (for example, gynecomastia, galactorrhea and an increase in the mammary glands) are rare. In most patients, the level of prolactin spontaneously normalized without discontinuation of therapy. Infrequently - an increase in the level of creatine phosphokinase (CPK). In elderly patients with dementia, a high frequency of deaths and cerebrovascular disorders (stroke, transient ischemic attacks) was recorded in studies. Very often, this category of patients had gait disturbances and falls.Pneumonia, fever, lethargy, erythema, visual hallucinations and urinary incontinence were also often observed. Among patients with medicinal (against the background of dopamine agonists) psychosis against Parkinson's disease, there was often a worsening of parkinsonian symptoms and hallucinations. There are data on the development of neutropenia ( 4.1%) in combination with valproic acid in patients with bipolar mania. Simultaneous therapy with valproic acid or lithium increases the frequency (more than 10%) of tremor, dry mouth, increased appetite and increased body weight. Speech disorders were also often recorded (from 1 to 10%). In the first 6 weeks of combination therapy with lithium, the frequency of weight gain increases. Long-term therapy with olanzapine (up to 12 months) in order to prevent recurrence in patients with bipolar disorder was accompanied by an increase in body weight.

Interaction with other drugs

Precautionary measures

special instructions

Symptoms: very often (more than 10%) - tachycardia, agitation / aggression, dysarthria, various extrapyramidal symptoms, a decrease in the level of consciousness from lethargy to coma; in less than 2% of cases, delirium, convulsions, coma, neuroleptic malignant syndrome (MNS), respiratory depression, aspiration, increased or decreased blood pressure, cardiac arrhythmia; in very rare cases, cardiopulmonary failure. The minimum dose of olanzapine for acute overdose with a fatal outcome is 450 mg, the maximum dose for overdose with a favorable outcome (survival) is 1500 mg. Treatment: gastric lavage, taking activated carbon (reduces the bioavailability of olanzapine by 60%), symptomatic treatment under the control is vital important functions, including the 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-adreno-mimetic activity, since the latter may aggravate hypotension. To identify possible arrhythmias, monitoring of cardiovascular activity is necessary. The patient must be under continuous medical supervision until full recovery.