Egolanza

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Egolanza: 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: Egolanza

ATX code: N05AH03

Active ingredient: olanzapine (Olanzapine)

Producer: EGIS CJSC Pharmaceutical Plant (EGIS Pharmaceuticals PLC) (Hungary)

Description and photo updated: 30.11.2018

Prices in pharmacies: from 988 rubles.

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Egolanza is an antipsychotic drug.

Release form and composition

Dosage form - film-coated tablets: yellow, biconvex, almost odorless or odorless; 5 mg each - oblong, on one side with a line, on the other side engraving E 402; 7.5 each; ten; 15 or 20 mg - round, on one of the sides, in accordance with the dosage, engraved E 403, E 404, E 405 or E 406 (in a cardboard box 4 or 8 blisters of 7 tablets and instructions for use of Egolanza).

The composition of 1 tablet (5 / 7.5 / 10/15/20 mg) contains:

active substance: olanzapine - 5; 7.5; ten; 15 or 20 mg (olanzapine dihydrochloride trihydrate - 7.03; 10.55; 14.06; 21.09 or 28.12 mg);
auxiliary components, core: microcrystalline cellulose - 40.99 / 61.48 / 81.97 / 122.96 / 163.94 mg; hyprolosis - 5.0 / 7.5 / 10.0 / 15.0 / 20.0 mg; crospovidone - 5.0 / 7.5 / 10.0 / 15.0 / 20.0 mg; lactose monohydrate - 40.98 / 61.47 / 81.97 / 122.95 / 163.94 mg; magnesium stearate - 1.0 / 1.5 / 2.0 / 3.0 / 4.0 mg;
auxiliary components, shell: hypromellose - 1.4 / 1.9 / 2.4 / 3.1 / 3.8 mg; quinoline yellow dye - 0.014 / 0.019 / 0.023 / 0.031 / 0.038 mg; Opadry Y-1-7000 white (hypromellose - 62.5%; titanium dioxide - 31.25%; macrogol 400 - 6.25%) - 2.79 / 3.78 / 4.68 / 6.27 / 7, 66 mg.

Pharmacological properties

Pharmacodynamics

Olanzapine - the active component of Egolanza - is an antipsychotic substance (neuroleptic) with a wide pharmacological spectrum of influence on a number of receptor systems.

Receptors to which olanzapine has an affinity: serotonin (5-HT _{2A / C}, 5HT ₃, 5HT ₆), dopamine (D ₁, D ₂, D ₃, D ₄, D ₅), muscarinic (M _1-5), histamine (H ₁), adrenergic receptors (α ₁).

Antagonism of olanzapine to serotonin (5HT), cholinergic and dopamine receptors was established. The substance has a more pronounced affinity and activity in relation to serotonin 5HT ₂ -receptors in comparison with dopamine D ₂ -receptors.

Olanzapine selectively reduces the excitability of mesolimbic (A10) dopaminergic neurons, slightly affects the striatal (A9) nerve pathways that are involved in the regulation of motor functions.

In addition, olanzamine causes a decrease in the conditioned defense reflex at doses lower than those that cause catalepsy; potentiates the anti-anxiety effect during anxiolytic test and reliably reduces productive (including hallucinations, delirium) and negative symptoms.

Pharmacokinetics

Olanzapine is well absorbed after oral administration. The time to reach C _max (maximum concentration) after oral administration is from 5 to 8 hours. Food has no effect on the absorption of the substance.

In the dose range of 1–20 mg, the change in plasma concentration is linear.

Binding to proteins (mainly with alpha _1- acid glycoprotein and albumin) at a plasma concentration of 7-1000 ng / ml is 93%.

Metabolism occurs in the liver by conjugation and oxidation. The main circulating metabolite is 10-N-glucuronide, which does not cross the blood-brain barrier. The isoenzymes CYP1A2 and CYP2D6 are involved in the formation of N-desmethyl and 2-hydroxymethyl metabolites of olanzapine.

The main pharmacological activity of Egolanza is due to olanzapine, its metabolites are much less active.

Excretion of 57% of the dose is carried out by the kidneys (mainly in the form of metabolites).

T _{1/2 of} olanzapine in healthy volunteers with oral administration of Egolanza is 33 hours (from 21 to 54 hours), plasma clearance is 12–47 l / h (on average - 26 l / h).

The T _1/2 value can vary depending on gender and age, as well as smoking status (clearance; T _1/2):

men: 27.3 l / h; 32.3 hours;
women: 18.9 l / h; 36.7 hours;
patients under 65 years of age: 18.2 l / h; 33.8 hours;
patients over 65 years old: 17.5 l / h; 51.8 hours;
smokers: 27.7 l / h; 30.4 hours;
non-smokers: 18.6 l / h; 38.6 hours.

The degree of these changes is significantly lower than the degree of individual variability of these indicators. Significant differences between the mean values of T _1/2 and plasma clearance of olanzapine in patients without renal dysfunction and with severe renal impairment have not been established.

Indications for use

schizophrenia: treatment;
schizophrenia in patients who responded to initial treatment with Egolanza: maintenance and long-term anti-relapse therapy;
moderate to severe manic episodes: treatment;
bipolar disorders: use to prevent relapse in patients in whom the drug has been effective in treating a manic episode;
therapeutically resistant depression in adult patients (major depressive episodes in the presence of a history of the ineffectiveness of the use of two antidepressants, which in terms of dose and duration of the course of therapy correspond to this episode): treatment in combination with fluoxetine (for use as monotherapy, Egolanza is not used in this case);
depressive episodes in the structure of bipolar disorder: treatment in combination with fluoxetine (for use as monotherapy, Egolanza is not used in this case).

Contraindications

Absolute:

the presence of a risk of developing angle-closure glaucoma;
lactose intolerance, glucose-galactose malabsorption or lactase deficiency (lactose is part of Egolanza);
age up to 18 years;
lactation period;
individual intolerance to the components of the drug.

Relative (Egolanza tablets are prescribed under medical supervision):

hepatic and renal failure;
hyperplasia of the prostate;
burdened history of convulsive syndrome;
epilepsy;
paralytic intestinal obstruction;
myelosuppression (including leukopenia, neutropenia);
hypereosinophilic syndrome;
myeloproliferative diseases;
cerebrovascular and cardiovascular diseases or other conditions that predispose to the development of arterial hypotension;
immobilization;
congenital increase in the QT interval on the electrocardiogram (ECG) (increase in the corrected interval, adjusted for heart rate - QTc) or the presence of conditions that can potentially lead to its growth;
combination therapy with other centrally acting drugs;
elderly age;
pregnancy.

Egolanza, instructions for use: method and dosage

Egolanza tablets are taken orally, regardless of food intake, once in a daily dose of 5–20 mg. The maximum dose is 20 mg per day.

The initial daily dose for schizophrenia is 10 mg.

In the treatment of acute mania associated with bipolar disorders, Egolanza is prescribed:

monotherapy: 15 mg;
combination therapy with valproic acid and lithium preparations: 10 mg (maintenance therapy is carried out at the same dose).

The recommended starting dose for the prevention of recurrence of bipolar disorder is 10 mg daily. Patients who have previously received olanzapine for the treatment of a manic episode should continue taking Egolanza at the same dose to prevent relapse. If there is a new manic, depressive or mixed episode, the drug should be continued (dose adjustment may be required); if there is a clinical indication, drugs are additionally prescribed to eliminate mood disorders.

The daily dose in the treatment of a manic episode, schizophrenia, as well as in order to prevent relapses of bipolar disorder can subsequently be adjusted individually in the range of therapeutic doses (5-20 mg), taking into account the clinical condition of the patient. Dose adjustments above the recommended starting dose are only possible after careful clinical analysis. Such changes must take place with a break of at least 24 hours.

Before canceling Egolanza, the dose should be reduced gradually.

A lower starting daily dose (5 mg) is optional for all patients 65 years of age and older, but is possible if clinically indicated. Also, the use of Egolanza at an initial dose of 5 mg may be required for patients with renal and liver dysfunction.

Patients with moderate hepatic impairment (with cirrhosis, dysfunction of class A or B on the Child-Pugh scale) should be prescribed the drug in an initial dose of 5 mg, its increase in the future requires caution.

In the presence of two or more factors that can lead to a slowdown in metabolism (old age, female sex, non-smoking patients) at the beginning of therapy, Egolanza can be used in a daily dose of 5 mg. But if necessary, in the future, the dose can be increased with caution.

Side effects

Possible adverse reactions (> 10% - very common;> 1% and 0.1% and 0.01% and <0.1% - rarely; <0.01% - very rare):

cardiovascular system: often - arterial hypotension (including orthostatic); infrequently - bradycardia with / without collapse; very rarely - ventricular tachycardia / fibrillation, increased QTc interval on the ECG, sudden death; very rarely - thromboembolism (including deep vein thrombosis and pulmonary embolism);
nervous system: very often - drowsiness; often - akathisia, dizziness, asthenia, parkinsonism, dyskinesia; rarely - convulsive syndrome (in most cases in patients with a burdened history of convulsive syndrome); very rarely - dystonia (including oculogyric crisis and tardive dyskinesia; neuroleptic malignant syndrome develops very rarely);
digestive system: often - transient anticholinergic effects (including constipation, xerostomia), asymptomatic transient increase in the activity of hepatic transaminases (alanine aminotransferase, aspartate aminotransferase), especially at the beginning of treatment; rarely - hepatitis (including cholestatic, hepatocellular or mixed liver damage); very rarely - increased activity of alkaline phosphatase and total bilirubin, pancreatitis;
genitourinary system: very rarely - priapism, urinary retention;
musculoskeletal system: very rarely - rhabdomyolysis;
metabolism: very often - weight gain; often - hypertriglyceridemia, increased appetite; very rarely - decompensation of diabetes mellitus and / or hyperglycemia (sometimes manifested by ketoacidosis or coma, including death), hypothermia, hypercholesterolemia;
hematopoietic organs: often - eosinophilia; rarely - leukopenia; very rarely - neutropenia, thrombocytopenia; in isolated cases - asymptomatic eosinophilia;
skin: infrequently - photosensitivity reactions; very rarely - alopecia;
laboratory parameters: very often - hyperprolactinemia (while clinical manifestations such as gynecomastia, enlargement of the mammary glands and galactorrhea rarely develop; in most cases, the prolactin level normalizes spontaneously without discontinuation of therapy); infrequently - an increase in the activity of creatine phosphokinase; in isolated cases - an increase in the plasma concentration in the blood of glucose, cholesterol, triglycerides;
immune system: rarely - skin rash; very rarely - angioedema, anaphylactoid reactions, urticaria, pruritus;
other reactions: often - peripheral edema, asthenia; very rarely - withdrawal syndrome.

In studies in elderly patients with dementia, a high frequency of cerebrovascular pathologies (transient ischemic attacks, stroke) and deaths were recorded. Falls and gait disturbances were very common in this category of patients. The development of the following diseases / conditions was also often observed: erythema, lethargy, pneumonia, urinary incontinence, fever, visual hallucinations.

With abrupt withdrawal of Egolanza, insomnia, increased sweating, anxiety, tremors, vomiting, or nausea very rarely develop.

Among patients with drug psychoses (during therapy with dopamine agonists) against the background of Parkinson's disease, hallucinations and worsening of parkinsonian symptoms were often recorded.

There is information about the development of neutropenia in patients with bipolar mania (in 4.1% of cases) during combined treatment with valproic acid. Combined use with lithium or valproic acid increases the frequency (> 10%) of tremors, xerostomia, increased appetite or weight gain. Cases (1-10%) of various disorders of speech activity were also recorded.

Overdose

The main symptoms: convulsions, delirium, aspiration, respiratory depression, neuroleptic malignant syndrome, decreased / increased blood pressure, arrhythmias, articulation disorder, agitation / aggressiveness, tachycardia, extrapyramidal disturbances, depression of consciousness of varying severity (from sedation to coma), deterioration breathing and cardiac arrest.

In acute overdose, the lowest fatal dose was 450 mg, the maximum dose, the adoption of which ended in a favorable outcome (survival) - 1500 mg.

Therapy: gastric lavage, intake of activated carbon, maintenance of respiratory function, symptomatic treatment. Sympathomimetics (including norepinephrine, dopamine), which are among the β-adrenergic receptor agonists, should not be used, since the stimulation of these receptors can lead to an increase in the decrease in blood pressure. Careful medical monitoring should be established for the patient's condition until he recovers.

special instructions

Clinical improvement during antipsychotic therapy can occur over days or weeks. During this period, patients require close monitoring.

Olanzapine is not approved for the treatment of psychosis and / or dementia-related behavioral abnormalities, which is associated with increased mortality and the risk of impaired cerebral circulation. When using Egolanza in elderly patients with psychosis against the background of dementia, the development of cerebrovascular diseases (in the form of stroke, transient ischemic attack), including deaths, was noted. These patients had pre-existing risk factors (aggravated history of cerebrovascular pathologies, arterial hypertension, transient ischemic attacks, smoking), as well as concomitant diseases and / or drug therapy, in time associated with cerebrovascular disorders.

Egolanza is not recommended for patients with Parkinson's disease for the treatment of psychosis associated with the use of dopamine agonists.

When using antipsychotics (including olanzapine), NNS (neuroleptic malignant syndrome) may develop. Its clinical manifestations include muscle stiffness, fever, changes in mental state, sweating, tachycardia, instability of autonomic functions (cardiac arrhythmia, irregular heart rate and blood pressure levels). Increased creatine phosphokinase levels, acute renal failure and myoglobinuria (rhabdomyolysis) may be considered additional symptoms. In the event of signs and symptoms of NNS or when an unexplained fever occurs, not accompanied by additional clinical manifestations of NNS, all antipsychotic drugs, including Egolanza, should be discontinued.

Patients with schizophrenia have a higher prevalence of diabetes. In very rare cases, the development of hyperglycemia, diabetes mellitus or exacerbation of pre-existing diabetes mellitus, diabetic coma and ketoacidosis has been noted. A causal relationship has not been established between antipsychotic drugs and these conditions. Clinical monitoring of the condition is recommended for patients with diabetes mellitus or risk factors for its occurrence.

While taking Egolanza, when lipid levels change, appropriate therapy is required, especially in patients with dyslipidemia or risk factors for fat metabolism disorders.

In case of prostate hypertrophy, paralytic intestinal obstruction and other similar conditions, the appointment of Egolanza requires caution, which is associated with the limited clinical experience of using olanzapine in such situations.

Patients who have an increase in the activity of hepatic transaminases, alanine aminotransferase and / or aspartate aminotransferase on the background of liver failure, or therapy with potentially hepatotoxic drugs, need special care. The condition of such patients should be monitored, if necessary, the dose should be reduced. In case of detection of hepatitis (including cholestatic, hepatocellular or mixed liver damage), Egolanza is canceled.

Olanzapine should be used with caution in patients with a decrease in the number of leukocytes (including neutrophils); with signs of toxic disorders or suppression of bone marrow function associated with exposure to certain drugs (in history); with depression of bone marrow function, which develops due to concomitant diseases, radio or chemotherapy (in history); with myeloproliferative disease or hypereosinophilia. Often, the diagnosis of neutropenia is noted with the combined use of olanzapine with valproate. Egolanza in patients with agranulocytosis or clozapine-dependent neutropenia (in history) did not cause recurrence of these disorders.

In very rare cases (with a frequency of <0.01%), acute symptoms, including insomnia, tremors, anxiety, vomiting, or nausea, have been reported with abrupt discontinuation of Egolanza.

As with therapy with other antipsychotic drugs, during the course of taking Egolanza, care must be taken in cases of its combined use with drugs that prolong the QTc interval. In particular, this caution applies to elderly patients, patients with congestive heart failure, congenital long QT syndrome, cardiac hypertrophy, hypomagnesemia, hypokalemia, or a family history of QT prolongation.

The combined use of Egolanza with other antipsychotics or drugs that also prolong the QT interval or cause hypokalemia should be avoided.

The timing of olanzapine therapy and venous thromboembolism was rare (<0.01%). The causal relationship has not been reliably confirmed. However, it must be borne in mind that patients with schizophrenia often have acquired risk factors for venous thromboembolism, and therefore all possible risk factors for venous thromboembolism (including immobility of patients) should be identified and preventive measures taken.

In patients who have a history of seizures, or in patients exposed to factors that lower the seizure threshold, Egolanza should be used with caution. Seizures are rare during treatment. Most often, they were observed in patients with a burdened history of seizures or in the presence of risk factors for seizures.

If signs of tardive dyskinesia develop, it is recommended to reduce the dose or cancel the drug. After discontinuation of Egolanza, the symptoms of tardive dyskinesia may manifest or worsen.

Orthostatic hypotension has rarely been observed in elderly patients in clinical trials of olanzapine. As with therapy with other antipsychotics, it is recommended that blood pressure be monitored periodically over the age of 65.

Olanzapine is not recommended for the treatment of children and adolescents. In studies involving patients aged 13–17 years, the development of various adverse reactions, including weight gain, increased prolactin levels and changes in metabolic parameters, was revealed. The long-term outcomes of these disorders have not been studied and remain unknown.

Egolanza in combination with other centrally acting drugs and ethanol should be taken with caution.

Influence on the ability to drive vehicles and complex mechanisms

Patients during the period of therapy with Egolanza should be careful while driving.

Application during pregnancy and lactation

pregnancy: Egolanza can only be used in cases where the expected benefit is higher than the possible risk;
lactation period: it is not recommended to take the drug (olanzapine is excreted in breast milk).

The experience of using Egolanza in pregnant women is insufficient. When planning or occurring pregnancy during therapy, you must inform your doctor about it.

There is spontaneous rare data that in newborns whose mothers took olanzapine in the third trimester of pregnancy, the development of disorders such as tremor, lethargy, muscle hypertonia, and drowsiness was noted.

The effect of olanzapine on fertility is unknown.

Pediatric use

Due to the lack of clinical data, it is contraindicated to take Egolanza to patients under 18 years of age.

With impaired renal function

Egolanza for renal failure is prescribed with caution.

For violations of liver function

Egolanza with hepatic failure is prescribed with caution.

Use in the elderly

To carry out therapy in elderly patients should be under medical supervision.

Drug interactions

inhibitors or inducers of the isoenzyme CYP1A2: olanzapine metabolism may change;
inducers of the CYP1A2 isoenzyme: the clearance of olanzapine increases with simultaneous use with carbamazepine and in smoking patients, which causes a decrease in the plasma concentration of olanzapine in the blood; if necessary, the dose of Egolanza is increased;
inhibitors of the isoenzyme CYP1A2 (fluvoxamine, ciprofloxacin): there is a significant suppression of olanzapine metabolism, with a decrease in its clearance, the values of C _max and AUC increase; if it is necessary to carry out combined therapy, it is possible to prescribe a lower initial dose of Egolanza;
activated carbon: the bioavailability of olanzapine is significantly reduced; the recommended interval between taking these medicines is 2 hours;
ethanol: the equilibrium pharmacokinetics of olanzapine does not change, but an increase in its sedative effect may be noted;
drugs that prolong the QTc interval (trimethoprim / sulfamethoxazole, ketoconazole, droperidol, amitriptyline, terbutaline, chlorpromazine, erythromycin, thioridazine, quinidine, pimozide, procainamide, adrenaline, sotalol, ephedrine and other electrolyte metabolites, fluconazole) or olzapine liver: when carrying out combination therapy, caution is required;
antiparkinsonian medications in patients with dementia and Parkinson's disease: the combination is not recommended;
dopamine: olanzapine is antagonistic to it, so it is theoretically possible to suppress the action of dopamine and levodopa agonists.

Analogs

The analogues of Egolanza are Zyprexa, Normiton, Zalasta, Parnasan, Olanex, Olanzapine.

Terms and conditions of storage

Store at temperatures up to 25 ° C. Keep out of the reach of children.

The shelf life is 5 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Egolanze

In most reviews of Egolanza, patients, as well as their relatives, note the high efficiency and good tolerance of the drug. There are practically no reports of adverse reactions.

The cost of the drug is estimated to be high, but many prefer it to cheaper analogues.

Price for Egolanza in pharmacies

Approximate price for Egolanza, film-coated tablets, per pack 28 pcs. is:

dosage 5 mg 1015-1100 rubles;
dosage of 10 mg - 1761-2032 rubles.

Egolanza: prices in online pharmacies

Drug name

Price

Pharmacy

Egolanza 5 mg film-coated tablets 28 pcs.

988 RUB

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Egolanza tablets p.p. 5mg 28 pcs.

1062 RUB

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Egolanza 10 mg film-coated tablets 28 pcs.

1749 RUB

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Egolanza tablets p.p. 10mg 28 pcs.

2058 RUB

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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!