Zalasta Ku-tab
Zalasta Ku-tab: 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 Q-tab
ATX code: N05AH03
Active ingredient: olanzapine (Olanzapine)
Producer: KRKA Polska Sp.z.o. (KRKA Polska Sp.z oo) (Poland)
Description and photo update: 2019-11-07
Prices in pharmacies: from 950 rubles.
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Zalasta Ku-tab is an antipsychotic drug (neuroleptic) with a wide pharmacological spectrum of action.
Release form and composition
The drug is available in the form of tablets dispersed in the oral cavity: slightly biconvex, round, yellow, marbling and minor structural inclusions are allowed (7 pcs. In blisters, in a cardboard box of 4 or 8 blisters and instructions for use of Zalasta Ku-tab) …
1 tablet contains:
- active substance: olanzapine - 5; 7.5; ten; 15 or 20 mg;
- auxiliary components: mannitol, calcium silicate, crospovidone, aspartame, low-substituted hypromellose LH-21, microcrystalline cellulose, magnesium stearate.
Pharmacological properties
Pharmacodynamics
Zalasta Ku-tab is a neuroleptic, antipsychotic drug. Its active ingredient - olanzapine - has a wide spectrum of pharmacological activity. The antipsychotic effect is due to the blockade of the dopamine D 2 receptors of the mesolimbic and mesocortical systems, the sedative effect is due to the blockade of adrenergic receptors of the reticular formation of the brain stem, the hypothermic effect is the blockade of the dopamine receptors of the hypothalamus, the antiemetic effect is due to the blockade of the D 2 -herreceptor zone of the dopamine receptor zone.
Olanzapine affects several subclasses of serotonin receptors and adrenergic, muscarinic, H 1 -histamine receptors.
Against the background of the use of olanzapine, the productive (hallucinations, delusions) and negative (suspicion, hostility, emotional and social autism) symptomatology of psychosis significantly decrease, extrapyramidal disorders rarely occur.
Pharmacokinetics
After taking Zalasta Ku-tab, olanzapine is well absorbed inside; simultaneous food intake does not affect the degree and rate of absorption. The maximum plasma concentration (C max) of olanzapine is reached within 5-8 hours.
Plasma protein binding (mainly albumin and alpha 1 acid glycoprotein) is 93%.
Overcomes the blood-brain and other histohematological barriers, penetrates into breast milk.
Olanzapine is metabolized in the liver through conjugation and oxidation. The main circulating metabolite is 10-N-glucuronide; it does not penetrate the blood-brain barrier. With the participation of isoenzymes CYP1A2 and CYP2D6, N-desmethyl and 2-hydroxymethyl metabolites are formed, the pharmacological activity of which is significantly lower than that of the parent compound.
Approximately 57% of the dose of olanzapine taken is excreted through the kidneys, mainly in the form of metabolites.
The half-life (T 1/2) is 33.8 hours, in men the average T 1/2 is less than in women. T 1/2 in old age (65 years and older) - 51.8 hours. Plasma clearance - 18.2 l / h, in the elderly - 17.5 l / h.
The use of olanzapine in patients with schizophrenia over the age of 65 years in daily doses of 5–20 mg does not cause differences in the profile of adverse events compared with younger people.
The safety profile of olanzapine (in a daily dose of 5 to 20 mg) is comparable in men and women.
In renal failure with creatinine clearance (CC) less than 10 ml / min, the pharmacokinetic parameters of olanzapine do not change significantly.
In smoking patients with mild hepatic impairment (Child-Pugh class A), the mean T 1/2 increases and the clearance decreases.
The dependence of T 1/2 and plasma clearance of olanzapine on age, sex and smoking is small.
Pharmacokinetic parameters in adolescents 13–17 years old and adult patients are similar. The average exposure of olanzapine in adolescents exceeds that in adults by about 27%.
The effect of race on olanzapine pharmacokinetics has not been established.
Indications for use
Zalasta Ku-tab is prescribed for the following diseases / conditions:
- schizophrenia;
- moderate to severe manic episodes;
- depressive episode in the structure of bipolar disorder - combination therapy with fluoxetine;
- therapeutically resistant depression in adult patients (major depressive episodes with a history of the lack of effect of the use of two antidepressants, according to the duration of the course of treatment and the dose corresponding to this episode) - combination therapy with fluoxetine.
In addition, Zalasta Ku-tab is indicated to maintain clinical improvement in the long-term treatment of schizophrenic patients who respond to initial treatment and to prevent relapse of mania in patients with bipolar disorder if olanzapine is effective for manic episodes.
Contraindications
Absolute:
- angle-closure glaucoma;
- lactation period;
- age up to 18 years;
- hypersensitivity to the components of the drug.
Zalasta Ku-tab should be prescribed with caution in case of epilepsy, a history of convulsive syndrome, hepatic failure, renal failure, paralytic intestinal obstruction, leukopenia and / or neutropenia of various origins, prostatic hyperplasia, myelosuppression of various origins (including myeloproliferative pathologies), cerebral and cerebral pathologies. diseases, a predisposition to arterial hypotension, congenital increase in the QT interval on the electrocardiogram (ECG), the presence of conditions that potentiate an increase in the QT interval (including congestive heart failure, the simultaneous use of drugs that prolong the QT interval, hypokalemia, hypomagnesemia), phenylketonuria, hypereosinophilic mobilization syndrome taking other drugs of central action, during pregnancy,in the elderly patient.
Zalasta Ku-tab, instructions for use: method and dosage
The tablets are taken orally, leaving in the mouth until completely dissolved under the influence of saliva, regardless of the meal. Due to the fragile structure of the tablets, they should be placed on the tongue immediately after being removed from the blister. If necessary, the tablet can be dissolved immediately before taking it in 200 ml of water.
Tablets for resorption of Zalasta Ku-tab are bioequivalent to ordinary Zalasta tablets, therefore, when switching from one drug to another, a change in the dosage regimen is not required.
Recommended dosage:
- schizophrenia: the initial dose of Zalasta Ku-tab is 10 mg once a day;
- manic or mixed episodes of bipolar disorder: the initial dose for monotherapy is 15 mg once a day, as part of a combination therapy - 10 mg once a day;
- prevention of recurrence of bipolar disorder: the initial dose of Zalasta Ku-tab is 10 mg once a day. If the patient is already taking olanzapine for the treatment of a manic episode, the dose should be maintained to prevent relapse. If a new manic, mixed or depressive episode occurs, treatment should be continued at the original or adjusted dose. Taking into account the clinical picture, the use of additional agents for the treatment of mood disorders is shown;
- combination therapy with fluoxetine for therapeutically resistant depression: the initial dose is 5 mg of olanzapine and 20 mg of fluoxetine once a day, in the evening. If necessary, dose adjustment should be done in parallel for each of the drugs. The antidepressant effect is usually achieved with the use of 6–12 mg olanzapine and 25–30 mg fluoxetine. Requires a regular assessment of the feasibility of continuing therapy;
- combination therapy with fluoxetine of a depressive episode in the structure of bipolar disorder: the initial dose of Zalasta Ku-tab is 5 mg, fluoxetine is 20 mg. The tablets are taken once a day, in the evening. In the absence of a sufficient clinical effect, it is allowed to increase the dose of olanzapine to 6–12 mg and the dose of fluoxetine to 25–30 mg. It is necessary to regularly evaluate the antidepressant activity of therapy and the need for its continuation.
It should be noted that for the maintenance therapy of schizophrenia, a manic episode or prevention of recurrence of bipolar disorder, it is allowed to select an individual dose of Zalasta Ku-tab in the dose range from 5 to 20 mg once a day, taking into account the patient's clinical condition. The initial dose can be increased only after evaluating the clinical picture, observing an interval of 1 day.
In patients 65 years of age and older, a reduced starting daily dose of 5 mg is generally not indicated, but should be considered in light of the patient's clinical condition.
The initial dose for renal failure, hepatic failure of classes A and B according to the Child-Pugh classification and / or cirrhosis is recommended to be used in the amount of 5 mg. Increasing the initial dose in such patients should be done with caution.
Taking into account the results of clinical monitoring, it is possible to consider the need to increase the dose of Zalasta Ku-tab in smoking patients.
In female patients, in the elderly or non-smokers, olanzapine metabolism may slow down, therefore, if necessary, consider reducing the dose. Increasing the dose in these categories of patients should be done with great caution.
Side effects
Unwanted disorders from systems and organs (classified as follows: very often - ≥ 1/10, often - ≥ 1/100 and <1/10, infrequently - ≥ 1/1000 and <1/100, rarely - ≥ 1/10 000 and <1/1000, very rarely - <1/10 000, including isolated cases):
- from the nervous system: very often - drowsiness; often - akathisia, dizziness, dyskinesia, parkinsonism; rarely - convulsive syndrome (usually with a history of convulsive syndrome); very rarely - neuroleptic malignant syndrome, dystonia (including oculogyric crisis), tardive dyskinesia; against the background of a sharp cancellation of Zalasta Ku-tab - nausea or vomiting, sweating, anxiety, insomnia, tremor;
- on the part of the cardiovascular system: often - arterial hypotension (including orthostatic arterial hypotension); infrequently - bradycardia (including with collapse); very rarely - an increase on the ECG of the QTc interval (corrected value of the QT interval relative to heart rate), thromboembolism (including deep vein thrombosis and pulmonary embolism), ventricular tachycardia or fibrillation, sudden death;
- on the part of the hepatobiliary system: often - a transient increase in the level of alanine aminotransferase and aspartate aminotransferase (asymptomatic, more often at the beginning of treatment); rarely - hepatitis (including cholestatic, hepatocellular or mixed liver damage);
- from the lymphatic system and hematopoietic organs: often - eosinophilia; rarely - leukopenia; very rarely - neutropenia;
- from the musculoskeletal system: very rarely - rhabdomyolysis;
- from the urinary system: very rarely - urinary retention;
- from the reproductive system: very rarely - priapism;
- from the gastrointestinal tract: often - dry mouth, constipation and other transient anticholinergic effects; very rarely - pancreatitis;
- metabolic and nutritional disorders: very often - an increase in body weight; often - increased appetite; very rarely - decompensation of diabetes mellitus, hyperglycemia, ketoacidosis, coma (including with a fatal outcome), hypothermia, hypertriglyceridemia, hypercholesterolemia;
- dermatological reactions: infrequently - photosensitivity;
- allergic reactions: rarely - skin rash; very rarely - itching, urticaria, angioedema, anaphylactoid reactions;
- laboratory parameters: very often - hyperprolactinemia; infrequently - an increase in the level of creatine phosphokinase; rarely - breast enlargement, gynecomastia, galactorrhea; very rarely - an increase in the level of total bilirubin and alkaline phosphatase;
- others: often - peripheral edema, asthenia; very rarely - alopecia.
In addition, in the course of clinical studies, a high incidence of cerebrovascular disorders (stroke, transient ischemic attacks), pneumonia, fever, lethargy, erythema, visual hallucinations, urinary incontinence and deaths in elderly patients with dementia was recorded.
In patients with Parkinson's disease and drug psychosis while taking dopamine agonists, hallucinations and worsening of symptoms of the disease are often observed.
The simultaneous use of Zalasta Ku-tab with valproic acid or lithium contributes to a significant (more than 10%) increase in appetite, body weight, the incidence of dry mouth, speech disorders, and tremors. In patients with bipolar mania, the combination of the drug with valproic acid causes neutropenia.
Significant weight gain is noted during the first 6 weeks of combination therapy with lithium.
Overdose
Symptoms: very often - tachycardia, agitation, dysarthria, aggression, extrapyramidal symptoms, a decrease in the level of consciousness up to coma. Less commonly, delirium, neuroleptic malignant syndrome, convulsions, respiratory depression, arterial hypertension or hypotension, aspiration, cardiac arrhythmias, coma occur. In very rare cases, the condition worsens to the development of cardiopulmonary failure. Acute fatal overdose may occur after taking olanzapine at a dose of 450 mg. At the same time, there are cases with a favorable outcome after a single dose of the drug at a dose of 1500 mg.
Treatment: a specific antidote has not been established, so it is necessary to immediately wash the stomach, take activated charcoal. Do not induce artificial vomiting. Further, symptomatic therapy is carried out under close control of the functional state of the respiratory system and other vital functions. Monitoring of cardiovascular activity is required in order to identify possible arrhythmias; if necessary, treatment of arterial hypotension and vascular collapse is prescribed. The use of sympathomimetics with beta-adrenomimetic activity (including epinephrine, dopamine) is not recommended in order to avoid aggravation of arterial hypotension. The patient needs close medical supervision until complete recovery.
special instructions
In schizophrenia and bipolar disorders, a tendency to suicide is observed, therefore, during therapy, this category of patients needs careful monitoring, including for a deliberate overdose of the drug.
Due to the increased mortality and the risk of cerebrovascular complications, it is not recommended to prescribe Zalastu Ku-tab to patients with psychosis and / or behavioral disorders caused by dementia. The frequency of deaths in this category of patients does not depend on the dose of olanzapine or the duration of treatment. Risk factors may include the patient's age over 65 years, sedation, dysphagia, dehydration, malnutrition, lung disease, or concomitant benzodiazepine therapy.
There is a significant increase in the incidence of cerebrovascular adverse events (including transient ischemic attack, stroke), including fatal ones, in patients over the age of 75 and with vascular or mixed dementia.
The use of olanzapine is not recommended for the treatment of psychosis, which are caused by the use of dopamine receptor agonists in Parkinson's disease. This is associated with an increased risk of worsening Parkinsonian symptoms and hallucinations.
The clinical manifestations of neuroleptic malignant syndrome (NMS) include: hyperthermia, tachycardia, unstable pulse or blood pressure (BP), arrhythmias, muscle rigidity, increased sweating, changes in mental status, increased serum creatine phosphokinase activity, myoglobinuria (rhabdomyolysis), acute myoglobinuria (rhabdomyolysis). If the patient develops an unexplained fever (even in the absence of other signs of NNS), immediate withdrawal of olanzapine is required.
It is recommended to carefully monitor the blood glucose concentration, including measuring the baseline concentration, 3 months after the start of therapy and then once every 12 months. Patients with diabetes mellitus or risk factors for its development should be regularly examined for a decrease in glycemic control, including checking body weight (before starting treatment, after 1, 2 and 3 months, then every 3 months).
Due to the negative effect of Zalasta Q-tab on the lipid profile, it is necessary to regularly monitor and correct lipid metabolism disorders, especially in case of dyslipidemia and the presence of factors that increase the risk of lipid metabolism disorders.
If hepatitis is diagnosed, treatment with olanzapine should be discontinued.
In the case of abrupt termination of olanzapine therapy, in rare cases, insomnia, tremors, increased sweating, anxiety, nausea and vomiting may occur.
Risk factors for the development of venous thromboembolism include immobilization of patients.
With prolonged therapy with olanzapine, the risk of developing tardive dyskinesia increases, therefore, when symptoms of this disease appear, it is necessary to consider reducing the dose of Zalasta Ku-tab or canceling it.
It is recommended to periodically monitor blood pressure in patients over 65 years of age due to the increased risk of postural hypotension in the elderly.
Consideration should be given to the presence of aspartame in the preparation, which is a source of phenylalanine and may be hazardous to people with phenylketonuria.
Influence on the ability to drive vehicles and complex mechanisms
The use of Zalasta Ku-tab can cause such undesirable phenomena as drowsiness and dizziness, which negatively affect the speed of psychomotor reactions and attention. Therefore, patients should be warned about the increased danger associated with driving vehicles or working with complex mechanisms.
Application during pregnancy and lactation
The use of Zalasta Ku-tab during gestation is indicated only in exceptional cases, if the expected clinical effect for the mother justifies the potential threat to the fetus. When the drug is taken by the mother in the third trimester of pregnancy, the effect of olanzapine can be manifested by tremors, arterial hypertension, drowsiness and lethargy in the child after birth.
Women taking Zalastu Ku-tab must inform the doctor about planning pregnancy or conception.
The use of tablets during breastfeeding is contraindicated.
Pediatric use
The safety and efficacy of olanzapine in children and adolescents have not been established, therefore, the appointment of Zalasta Ku-tab is contraindicated under the age of 18 years.
With impaired renal function
Zalasta Ku-tab should be taken with caution in patients with renal insufficiency.
For violations of liver function
Zalasta Ku-tab should be used with caution to treat patients with hepatic insufficiency.
Use in the elderly
With caution, Zalasta Ku-tab should be prescribed for the treatment of elderly patients.
Drug interactions
- CYP1A2 isoenzyme inducers: combination with carbamazepine and smoking cause a decrease in the concentration of olanzapine in the blood plasma, which is a consequence of an increase in its clearance. It is necessary to carry out clinical observation, since an increase in the dose of Zalasta Ku-tab may be required;
- inhibitors of the isoenzyme CYP1A2: during concomitant therapy with fluvoxamine, ciprofloxacin or other inhibitors of CYP1A2, olanzapine should be started with reduced doses. In cases where CYP1A2 inhibitors are prescribed during drug therapy, a reduction in the dose of olanzapine may be required;
- activated charcoal: affects the bioavailability of olanzapine, causing a decrease in its absorption by 50-60%, therefore activated charcoal should be taken before or after olanzapine intake with an interval of at least 2 hours;
- direct and indirect dopamine agonists: their effects may be weakened;
- tricyclic antidepressants, warfarin, theophylline, diazepam: the metabolism of the listed pharmaceutical substances is not inhibited;
- fluoxetine, cimetidine: do not affect olanzapine pharmacokinetics;
- aluminum and magnesium-containing antacids: single doses of these drugs do not interfere with the bioavailability of olanzapine;
- biperiden, lithium preparations: no interaction detected;
- valproic acid: no change in the dose of valproic acid is required;
- ethanol: alcohol consumption may be accompanied by an aggravation of the depressive effect on the central nervous system.
Analogs
Zalasta Ku-tab analogs are: Zalasta, Egolanza, Parnasan, Zyprexa, Zyprexa Zidis, Olaneks, Olanzapine Medisorb, Olanzapine-Vial, Olanzapine, Olanzapine-Teva, Olanzapine Canon, Olanzapine-ALSI, Olanzapin-TL, Normazapin-ALSI
Terms and conditions of storage
Keep out of the reach of children.
Store at temperatures up to 25 ° C.
The shelf life is 5 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Zalaste Ku-tab
Reviews about Zalasta Ku-tab are mostly positive. Patients note a mild clinically pronounced effect of the drug, a good comfortable state against the background of its use. Some adverse events (including drowsiness, anxiety, fear) have been reported that are transient.
Price for Zalasta Ku-tab in pharmacies
The price of Zalasta Ku-tab 5 mg can be 906–992 rubles, 10 mg - 1797–2028 rubles. per pack of 28 tablets.
Zalasta Ku-tab: 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 5 mg oral dispersible tablets 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 |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, 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!
