Zalasta
Zalasta: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Zalasta
ATX code: N05AH03
Active ingredient: Olanzapine (Olanzapine)
Producer: KRKA POLSKA, Sp.zoo (Poland)
Description and photo update: 18.10.2018
Prices in pharmacies: from 950 rubles.
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Zalasta is an antipsychotic drug (neuroleptic).
Release form and composition
Tablets: round, slightly biconvex, light yellow, darker inclusions are possible; in a dose of 2.5 mg tablets without an inscription, on tablets 5; 7.5; ten; 15 and 20 mg the applied number corresponds to the dose of the active substance (7 pcs. In blisters, in a cardboard box of 4 or 8 blisters together with an instruction leaflet).
Composition of 1 tablet:
- active substance: olanzapine - 2.5; five; 7.5; ten; 15 or 20 mg;
- auxiliary ingredients: corn starch, pregelatinized starch, cell lactose (spray-dried compound containing α-lactose monohydrate - 75% and cellulose - 25%), magnesium stearate, anhydrous colloidal silicon dioxide.
Pharmacological properties
Pharmacodynamics
Olanzapine is a broad-spectrum neuroleptic with the following effects:
- antipsychotic: due to blockade of the mesocortical and mesolimbic systems, as well as dopamine D2 receptors;
- sedative: provided by blocking the adrenergic receptors of the reticular formation of the brain stem;
- antiemetic: caused by blockade of dopamine D2 receptors in the trigger zone of the vomiting center;
- hypothermic: due to blockage of dopamine receptors in the hypothalamus.
In addition, olanzapine affects adrenergic, H 1 -histamine, muscarinic and some subclasses of serotonin receptors.
Zalasta significantly reduces the negative (suspicion, hostility, social and emotional autism) and productive (hallucinations, delusions) symptoms of psychosis. At the same time, extrapyramidal disorders are rarely caused.
Pharmacokinetics
Olanzapine is well absorbed in the intestines, the absorption of the drug does not depend on food intake. The period of reaching C max (maximum plasma concentration of the drug) after oral administration is from 5 to 8 hours. With proteins (mainly albumin and α1-glycoprotein), olanzapine binds by 93% in the concentration range of 7-1000 ng / ml. The substance penetrates through the GGB (histohematogenous barrier), including the BBB (blood-brain barrier). Olanzapine is metabolized in the liver without the formation of active metabolites, glucuronide, the main circulating metabolite, does not penetrate the BBB.
Patient age, sex and smoking affect T 1/2 (half-life) and plasma clearance of olanzapine, but compared with individual variability of pharmacokinetics between individuals, the degree of such influence is negligible. The drug is excreted mainly by the kidneys (up to 60%) in the form of inactive metabolites.
Indications for use
- schizophrenia - the drug is used for therapy, effectively supporting the improvement of clinical symptoms during long-term treatment of patients with a positive initial response to olanzapine;
- mania - treating moderate to severe episodes;
- bipolar disorder - prevention of relapse of mania in patients with manic episodes with a good response to olanzapine therapy.
Contraindications
Absolute:
- angle-closure glaucoma;
- Lapp lactase deficiency, galactose intolerance, glucose-galactose malabsorption;
- lactation period;
- children and adolescents up to 18 years old;
- hypersensitivity to olanzapine and other ingredients of the drug.
According to the instructions, Zalasta is taken with caution in case of renal / hepatic insufficiency, prostatic hyperplasia, paralytic intestinal obstruction, epilepsy, immobilization, pregnancy, a history of convulsive syndrome, leukopenia / neutropenia of various origins, myelosuppression of various origins (including myeloproliferative diseases), hyperproliferative diseases cardiovascular and cerebrovascular diseases or conditions predisposing to arterial hypotension, concomitant use with other centrally acting drugs, in old age, as well as with a congenital increase in the QT interval on an ECG (electrocardiogram) with an increase in QT c (corrected QT interval) or in the presence of conditions that can cause an increase in the QT interval (for example, congestive heart failure, concomitant use of drugs that prolong the QT interval, hypomagnesemia, hypokalemia).
Instructions for use of Zalasta: method and dosage
Zalasta tablets are taken orally, regardless of food intake, 1 time per day.
Recommended starting doses:
- schizophrenia: 10 mg / day;
- episode of mania: with monotherapy - 15 mg / day; in combination therapy - 10 mg / day;
- bipolar disorders (prevention of relapse): in remission - 10 mg / day; for patients already receiving Zalasta for the treatment of an episode of mania, maintenance treatment is carried out in the same doses; against the background of taking the drug with the development of a new manic, depressive or mixed episode - if necessary, the dose is increased with an additional course of therapy for mood disorders, according to clinical indications.
The daily dose of the drug can vary within 5–20 mg, depending on clinical parameters. Its increase from the recommended initial is allowed after an adequate repeated clinical assessment of the patient's condition, usually carried out at intervals of ≥ 24 hours.
Dose changes are not required for women versus men, and for non-smokers versus smokers. But in the case of the presence of more than one factor potentially capable of influencing the absorption of olanzapine, for example, old age or female sex, a reduction in the initial dose may be required. In this case, a further increase in the dose, if necessary, is carried out with caution.
Cancellation of the drug should be carried out with a gradual dose reduction.
Side effects
Classification of the frequency of side effects from systems and organs in accordance with the scale of the World Health Organization (WHO): very often -> 0.1%; often - 0.1–0.01%; infrequently - 0.01–0.001%; rarely - 0.001–0.0001%; extremely rare - <0.0001% (including single messages):
- central and peripheral nervous system: very often - drowsiness; often - akathisia, dyskinesia, dizziness, parkinsonism; rarely - convulsive syndrome (mainly in the presence of data on convulsive syndrome in the anamnesis); extremely rarely - neuroleptic malignant syndrome (NMS), dystonia (including oculogyric crisis) and tardive dyskinesia; abrupt withdrawal of olanzapine rarely causes sweating, insomnia, tremors, anxiety, nausea or vomiting;
- cardiovascular system: often - arterial hypotension (including orthostatic); infrequently - bradycardia with or without collapse; extremely rare - an increase in the QT interval c on an ECG, thromboembolism (including deep vein thrombosis and pulmonary embolism), ventricular tachycardia / fibrillation, sudden death;
- Gastrointestinal tract (gastrointestinal tract): often - transient anticholinergic effects (including dry mouth and constipation); extremely rare - pancreatitis;
- metabolism and nutrition: very often - weight gain; often - improved appetite; extremely rarely - hyperglycemia / decompensation of diabetes mellitus (sometimes expressed by ketoacidosis or hypoglycemic coma up to a fatal outcome) hypercholesterolemia, hypertriglyceridemia, hypothermia;
- hematopoietic organs and lymphatic system: often - eosinophilia; rarely - leukopenia; extremely rare - thrombocytopenia, neutropenia;
- hepatobiliary system: often - asymptomatic transient increase in the levels of hepatic transaminases [aspartate aminotransferase (ACT), alanine aminotransferase (ALT)], especially at the initial stage of therapy; rarely - hepatitis (including cholestatic, hepatocellular or mixed liver damage);
- organs of the genitourinary system: extremely rarely - priapism, urinary retention;
- organs of the musculoskeletal system: extremely rare - rhabdomyolysis;
- skin and subcutaneous tissue: infrequently - photosensitization;
- hypersensitivity reactions: rarely - skin rash; extremely rarely - itching, urticaria, angioedema, anaphylactoid reactions;
- other reactions: often - peripheral edema, asthenia; extremely rare - alopecia;
- laboratory indicators: very often - hyperprolactinemia with rare clinical manifestations (galactorrhea, gynecomastia, enlargement of the mammary glands), the level of prolactin in most cases spontaneously normalized without discontinuation of the drug; infrequently - an increase in the level of creatine phosphokinase (CPK); extremely rarely - an increase in the level of total bilirubin and alkaline phosphatase (ALP).
The highest frequency of deaths and cerebrovascular disorders (transient ischemic attacks, stroke) were recorded in studies in elderly patients with dementia. Very often, this category of patients had gait disturbances and falls; hyperthermia, urinary incontinence, pneumonia, erythema, visual hallucinations, lethargy were often observed.
Worsening of parkinsonian symptoms with the development of hallucinations was often recorded among patients with drug-induced (dopamine agonist-induced) psychoses associated with Parkinson's disease.
In the treatment of bipolar mania, the development of neutropenia (4.1%) was recorded against the background of therapy in combination with valproic acid. Combined therapy with lithium or valproic acid preparations increases the frequency (> 10%) of side effects such as dry mouth, tremors, improved appetite and weight gain. With this combination, speech disorders were often observed (from 1 to 10%). Weight gain is also recorded in the first 6 weeks of combination therapy with lithium and with prolonged (up to 1 year) olanzapine therapy for the prevention of recurrence of bipolar disorders.
Overdose
Symptoms of an olanzapine overdose: very often (> 10%) - dysarthria, tachycardia, various symptoms of extrapyramidal disorders, agitation / aggression, switching off consciousness (from lethargy to coma); less than 2% - convulsions, coma, delirium, ZNS, aspiration, respiratory depression, increased or decreased blood pressure, cardiac arrhythmias; in very rare cases - cardiopulmonary insufficiency.
Registered: the minimum dose of olanzapine in case of an acute overdose with a fatal outcome - 450 mg; the maximum dose in case of an overdose with a favorable outcome (survival) is 1500 mg.
There is no specific antidote for the treatment of the condition and it is not recommended to induce vomiting. Gastric lavage should be performed, activated charcoal should be taken, which reduces the bioavailability of olanzapine by 60%, and a course of symptomatic therapy under the control of vital systems and organs should be carried out, including the maintenance of respiratory function, treatment of vascular collapse and arterial hypotension. The use of dopamine, epinephrine, other sympathomimetics with β-adrenomimetic activity is not recommended, since they can aggravate arterial hypotension. In order to identify possible arrhythmias, monitoring of cardiovascular activity is required. The patient should be kept under continuous medical supervision until the final recovery.
special instructions
Patients with diabetes mellitus, as well as in the presence of factors suggesting its development, are recommended to undergo regular examination (to monitor the clinical condition) and determine the blood glucose level. In such patients, rare cases of the development of hyperglycemia / decompensation of diabetes mellitus, sometimes with the concomitant development of ketoacidosis or ketoacidotic coma, up to death were recorded (isolated reports). In some episodes, there was an increase in the patient's body weight, preceding the development of decompensation, which could be the cause of the development of these side effects.
Changes in lipid levels require correction of the dosage regimen.
According to the experience of using olanzapine for the treatment of patients with psychosis in Parkinson's disease, due to the use of dopaminomimetics, an increase in the symptoms of parkinsonism and hallucinations was noted. At the same time, the effectiveness of olanzapine in the treatment of psychosis did not exceed that of placebo. Zalasta is not recommended for the treatment of this category of patients.
It is not recommended to use olanzapine for the treatment of psychoses / behavioral disorders associated with dementia, due to increased mortality and increased risk of cerebrovascular disorders (transient ischemic attacks, stroke). The association of increased mortality with olanzapine dosing or duration of therapy has not been established. Risk factors that predispose to increased mortality: sedation, dysphagia, malnutrition, dehydration, lung disease (pneumonia, including aspiration), concomitant use of benzodiazepines, age over 65 years. However, in the olanzapine groups, compared with placebo, the increased death rate was not related to these risk factors in the observational results.
Antipsychotic therapy is characterized by the onset of improvement in the patient's clinical condition in the period from several days to several weeks. Throughout this period, the patient requires careful monitoring.
Such a potentially life-threatening condition as NMS due to therapy with antipsychotic drugs (neuroleptics), inclusive of olanzapine, is extremely rare. Symptoms of NMS: impaired consciousness, muscle rigidity, fever, autonomic disorders [tachycardia, unstable pulse / labile blood pressure (BP), hyperhidrosis, arrhythmias]. Additionally, signs of NMS may be: myoglobinuria (against the background of rhabdomyolysis), increased CPK, acute renal failure. If any of these symptoms develop, with an increase in temperature for no apparent reason, all antipsychotics, including Zalasta, should be discontinued.
Tardive dyskinesia was observed much less frequently with olanzapine therapy than with haloperidol. The risk of its development increases with the duration of treatment. The appearance of signs of this condition in patients taking olanzapine requires a dose reduction or complete abolition of Zalasta, after which the symptoms of dyskinesia may increase for some time.
During therapy with olanzapine, special care is required when it is used together with other centrally acting drugs and alcohol.
Reception of olanzapine in very rare cases (less than 0.01%) may be accompanied by the development of venous thromboembolism, but the cause-and-effect relationship between these factors has not been established. Patients with schizophrenia often have acquired risks of venous thrombosis (eg, immobilization) that should be identified for preventive action.
Influence on the ability to drive vehicles and complex mechanisms
During treatment, it is important to be careful when engaging in potentially hazardous activities (including driving vehicles) that require quick psychomotor reactions and high concentration of attention.
Application during pregnancy and lactation
The experience of using Zalasta in pregnant women is limited, and therefore olanzapine during pregnancy is prescribed only in case of a significant excess of the expected benefit to the mother over the potential risks to the fetus. The woman should be informed about the need to inform the attending physician about the planned or coming pregnancy while taking olanzapine. Isolated episodes of tremor, arterial hypertension, drowsiness and lethargy were recorded in children whose mothers took olanzapine in the third trimester of pregnancy.
Studies have revealed the ingestion of olanzapine into breast milk at the average dose received by the child in case of reaching the equilibrium concentration in the mother, up to 1.8% of the maternal dose of olanzapine (mg / kg). Therefore, breastfeeding during therapy with Zalastaya is not recommended.
Pediatric use
The safety and efficacy of the drug in children and adolescents under 18 years of age have not been established, therefore, taking Zalasta in this category of patients is contraindicated.
With impaired renal function
For patients with kidney disease, it is recommended to reduce the initial dose to 5 mg / day; further increase in the dose is carried out with caution.
For violations of liver function
Patients with liver disease are advised to reduce the initial dose to 5 mg / day, since at the beginning of treatment, an asymptomatic increase in the level of hepatic transaminases (ALT and ACT) is possible. With initially elevated ACT / ALT levels, liver failure and conditions potentially limiting the functionality of the liver, as well as in the case of a combination with hepatotoxic drugs, Zalasta tablets are taken with caution. An increase in ALT / ACT during therapy requires monitoring the patient with a possible decrease in the dose of the drug. If hepatitis is diagnosed (including cholestatic, hepatocellular or mixed), olanzapine is canceled.
Use in the elderly
A decrease in the initial dose to 5 mg per day in elderly patients over 65 years of age is possible in the presence of the following risk factors: congestive heart failure, congenital long QT interval syndrome, myocardial hypertrophy, hypokalemia and hypomagnesemia. Zalasta is taken with caution.
Postural arterial hypotension in the elderly is rare, but patients in this age group are periodically recommended to monitor blood pressure.
Drug interactions
- CYP1A2 inhibitors: significantly reduce the clearance of olanzapine in combination with fluvoxamine, ciprofloxacin, and other CYP1A2 inhibitors (therapy with Zalastaya should be started with lower doses; also, a reduction in the olanzapine dose may be required when CYP1A2 inhibitors are added to therapy);
- CYP1A2 inducers: an increase in the clearance of olanzapine in smoking patients or in combination with carbamazepine is possible, as a result of which the plasma concentration of olanzapine decreases (clinical observation is recommended, since in some cases an increase in the dose of the drug may be required);
- activated charcoal: when taken orally, it reduces the absorption of olanzapine by 50-60%, so it is taken at least two hours before or after Zalasta;
- magnesium- or aluminum-containing antacids (in a single dose), cimetidine, fluoxetine: they do not affect the pharmacokinetics of olanzapine;
- direct and indirect dopamine agonists: olanzapine can weaken their effect;
- tricyclic antidepressants, warfarin, theophylline, diazepam: olanzapine was not found to inhibit their metabolism;
- lithium, biperiden: no interaction with olanzapine with simultaneous use has been identified;
- valproic acid: no dose changes are required;
- other drugs of central action: in combination with olanzapine, take with caution;
- ethanol-containing drugs, alcohol: a single dose of alcohol (45 mg / 70 kg) in combination with taking Zalasta does not have a pharmacokinetic effect, but may be accompanied by an increase in the depressive effect on the central nervous system.
Analogs
Zalasta's analogs are: Normiton, Zalasta Ku-tab, Olanex, Zyprexa, Zyprexa Zidis, Olanzapine, Egolanza, Parnasan, etc.
Terms and conditions of storage
Keep out of the reach of children.
Store at <30 ° C.
Shelf life: tablets 5 and 10 mg - 5 years; tablets 2.5; 7.5; 15 and 20 mg - 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Zalast
Reviews of Zalaste by practicing doctors are mostly positive. They note the pronounced antipsychotic effect of the drug, its high efficiency in relation to positive and negative symptoms. The drug is more effective in preventing exacerbations in schizophrenic patients compared to conventional antipsychotics. There is also a positive trend in the appointment of Zalasta for the prevention of bipolar affective disorders.
Patients in reviews of Zalast also talk about the positive effect of therapy on their well-being, but express dissatisfaction with the high price of the drug. A significant number of side effects are often noted, in particular a strong increase in appetite and, accordingly, subsequent weight gain.
Price for Zalasta in pharmacies
There is information about the availability of tablets in the network of pharmacies, mainly in doses of 5 and 10 mg. The approximate price of Zalasta: 5 mg tablets (28 pcs in a package) - about 1300 rubles; tablets 10 mg (28 pcs. in a package) - from 2500 rubles. and higher.
Zalasta: prices in online pharmacies
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Drug name Price Pharmacy |
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Zalasta KU-Tab tablets oral dispersion 5mg 28 pcs. RUB 950 Buy |
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Zalasta KU-Tab tablets dispersion 10mg 28 pcs. 1852 RUB Buy |
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Zalasta Ku-tab 10 mg orodispersible tablets 28 pcs. 1852 RUB Buy |
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Zalasta 10 mg tablets 28 pcs. RUB 2308 Buy |
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Zalasta tablets 10mg 28 pcs. 2340 RUB Buy |
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Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
