Egolanza pills 5 mg 28 pcs
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Active ingredients
Olanzapine
Release form
Pills
Composition
Olanzapine dihydrochloride trihydrate is 7.03 mg, which corresponds to the content of olanzapine 5 mg; Excipients: microcrystalline cellulose - 40.99 mg, lactose monohydrate - 40.98 mg, hyperrol (hydroxypropylcellulose) - 5 mg, crospovidone - 5 mg, magnesium stearate - 1 mg., Mg. shell: hypromellose - 1.4 mg, quinoline yellow dye - 0.014 mg, opadry Y-1-7000 white - 2.79 mg (hypromellose - 62.5%, titanium dioxide - 31.25%, macrogol 400 - 6.25%).
Pharmacological effect
Olanzapine is an antipsychotic (neuroleptic) with a wide pharmacological spectrum of effects on a number of receptor systems. It has affinity for serotonin (5-НТ2А / С, 5НТ3, 5НТ6), dopamine (D1, D2, D3, D4, D5, muscarinic (M1 -5) receptors, adrenoreceptors (1) and histamine (H1) receptors.; Antagonism has been revealed towards serotonin (5HT), dopamine and cholinergic receptors. It has a more pronounced affinity and activity against serotonin 5HT2 receptors, compared to dopamine D2 receptors.; Selectively reduces the excitability of mesolimbic (A10) dopaminergic neurons, has little effect on striatal (A9) nerve pathways involved in the regulation of motor functions. Reduces the conditioned protective reflex in lower doses than the doses causing catalepsy. Enhances anti-anxiety effect when conducting anxiolytic test. Reliably reduces productive (including delirium, hallucinations) and negative symptoms.
Pharmacokinetics
Absorption and distribution; Olanzapine is well absorbed after oral administration. Cmax after oral administration is achieved after 5-8 hours. Food does not affect the absorption of the drug. When taken in the dose range of 1-20 mg, the concentration in plasma changes linearly, proportionally to the dose.; At a plasma concentration of 7-1000 ng / ml, binding to proteins - 93%; mainly with albumin and alpha1-acid glycoprotein.; Metabolism and excretion; Metabolized in the liver by conjugation and oxidation. The main circulating metabolite - 10-N-glucuronide, does not penetrate the BBB. CYP1A2 and CYP2D6 isoenzymes are involved in the formation of N-desmethyl and 2-hydroxymethyl metabolites of olanzapine.; The main pharmacological activity of the drug is due to olanzapine, its metabolites are less pronounced.; Derived by the kidneys - 57% (mostly in the form of metabolites) .; In healthy volunteers after oral administration, T1 / 2 of olanzapine is 33 h (21-54 h), and the average plasma clearance is 26 l / h (12-47 l / h).T1 / 2 olanzapine can vary depending on age and sex, as well as the status of smoking: non-smokers (clearance - 18.6 l / h, T1 / 2 - 38.6 h), smokers (clearance - 27.7 l / h, T1 / 2 - 30.4 h), women (clearance - 18.9 l / h, T1 / 2 - 36.7 h), men (clearance - 27.3 l / h, T1 / 2 - 32.3 h), patients 65 years and older (clearance - 17.5 l / h, T1 / 2 - 51.8 h), patients under 65 years old (clearance - 18.2 l / h, T1 / 2 - 33.8 h); The degree of changes in T1 / 2 and plasma clearance under the influence of each of these factors is significantly inferior to the degree of individual differences of these indicators. Significant differences between the mean T1 / 2 and plasma clearance of olanzapine in patients with severe impaired renal function and in patients with normal renal function has not been established.
Indications
- treatment of schizophrenia; - supportive and long-term contraceptive therapy in patients with schizophrenia who responded to the initial treatment; - treatment of a manic episode of moderate and severe; - prevention of relapse in patients with bipolar disorder, in whom the drug was effective in treating a manic episode; - in combination with fluoxetine for the treatment of therapeutically resistant depression in adult patients (major depressive episodes with a history of ineffective use of two antidepressants in terms of the dose and duration of the course of therapy corresponding to this episode). The drug Egolanza as monotherapy is not indicated for the treatment of therapeutically resistant depression; - in combination with fluoxetine for the treatment of a depressive episode in the structure of bipolar disorder. The drug Egolanza as monotherapy is not indicated for the treatment of a depressive episode in the structure of bipolar disorder.
Contraindications
- risk of development of angle-closure glaucoma; - children and adolescents up to 18 years (due to the lack of clinical data); - lactose intolerance, lactase deficiency or glucose-galactose malabsorption (the product contains lactose); - hypersensitivity to the drug components.; With caution; Liver failure, renal failure, prostatic hyperplasia, epilepsy, a history of convulsions, myelosuppression (including leukopenia, neutropenia), myeloproliferative diseases, hypereosinophilic syndrome, intestinal chromositypregnancy, cardiovascular and cerebrovascular diseases or other conditions predisposing to arterial hypotension, congenital increase in the QT interval on the ECG (increase in the QTc interval on the ECG), or in the presence of conditions potentially capable of increasing the QT interval (for example, simultaneous administration of drugs that extend the QT interval , congestive heart failure, hypokalemia, hypomagnesemia), old age, and the simultaneous use of other drugs of central action; immobilization.
Use during pregnancy and lactation
Due to insufficient experience with pregnant women, the drug should be prescribed during pregnancy only if the intended benefit to the mother significantly exceeds the potential risk to the fetus. Patients should be warned that in the event of an onset or planning of pregnancy during the period of treatment with olanzapine, they should be notified of this to their physician. Very rare spontaneous reports were received that newborns whose mothers took olanzapine in the third trimester of pregnancy were noted tremor, muscle hypertonus, lethargy, drowsiness. In studies it was found that olanzapine is excreted in breast milk. The average dose received by the child (mg / kg) upon reaching Css in the mother was 1.8% of the dose of mother olanzapine (mg / kg). Breastfeeding during olanzapine therapy is not recommended.; Effect on fertility is unknown.
Dosage and administration
Inside, regardless of food intake, once - 5-20 mg / day; In schizophrenia in adults, the recommended initial dose is 10 mg / day; In acute mania associated with bipolar disorders, in adults - 15 mg / day (1 times) as monotherapy or 10 mg / day (1 time) in combination with lithium preparations or valproic acid (maintenance therapy at the same dose); Prevention of relapses of bipolar disorder: the recommended initial dose is 10 mg / day. Patients who have previously received olanzapine for the treatment of a manic episode should continue treatment at the same dose to prevent recurrence. If there is a new manic, mixed or depressive episode, olanzapine intake should be continued (if necessary, specifying the dose); in the presence of clinical indications, additional drugs should be prescribed to eliminate mood disorders.; In the treatment of schizophrenia, a manic episode, and also to prevent the recurrence of bipolar disorder,the daily dose can be subsequently adjusted in the range from 5 to 20 mg, taking into account the clinical condition of the individual patient. Dose adjustment in excess of the value recommended as the initial dose is recommended only after careful clinical analysis, and should usually occur at intervals of at least 24 hours; Before discontinuing olanzapine, the dose should be gradually reduced. The maximum daily dose of olanzapine is 20 mg. A lower initial dose (5 mg / day) is not necessary for all patients, but it is possible for patients aged 65 and older if clinically indicated. For patients with impaired liver function / or kidney may require a decrease in the initial dose (up to 5 mg / day). With moderate hepatic insufficiency (cirrhosis, class A or B on Child-Pugh) should be prescribed an initial dose of 5 mg and increase it with caution.; Women should prescribe the drug in the same doses as men.; Smoking patients should prescribe the drug in those same doses as non-smoking patients. If there is more than one factor capable of causing a slowdown in metabolism (female gender, old age, non-smoking patients), the need to reduce the initial dose to 5 mg / day should be considered. If necessary, a further dose increase with caution is possible.
Side effects
The frequency of side effects noted when taking the drug is given in accordance with the WHO classification: very often (> 1/10), often (> 1/100 and less than 1/10), infrequently (> 1/1000 and less than 1/100) , rarely (> 1/10 000 and less than 1/1000), very rarely (less than 1/10 000, including individual messages); From the nervous system: very often - drowsiness; often - dizziness, akathisia, parkinsonism, asthenia, dyskinesia; seldom - a convulsive syndrome (more often against the background of a convulsive syndrome in the anamnesis); very rarely - dystonia (including ocular crisis) and tardive dyskinesia. Very rarely can an SNS develop. Clinical manifestations of ZNS are fever, muscle rigidity, changes in mental state, instability of autonomic functions (non-constant levels of heart rate and blood pressure, tachycardia, sweating, cardiac arrhythmia). Additional signs may be increased levels of CPK, myoglobinuria (rhabdomyolysis) and acute renal failure.If the patient develops symptoms and signs of MNS or the appearance of unexplained fever without additional clinical manifestations of MNS, all antipsychotics should be canceled, incl. olanzapine. With abrupt drug withdrawal, symptoms such as increased sweating, insomnia, tremor, anxiety, nausea or vomiting are very rarely noted. Cardiovascular: often - 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; very rarely - thromboembolism (including pulmonary embolism and deep vein thrombosis); On the part of the digestive system: often - transient anticholinergic effects, including constipation and dryness of the oral mucosa, transient, asymptomatic increased activity of hepatic transaminases (ALT, ACT), especially at the beginning of therapy; rarely, hepatitis (including hepatocellular, cholestatic, or mixed liver damage); very rarely - pancreatitis, increased activity of alkaline phosphatase and total bilirubin. From the side of metabolism: very often - an increase in body mass often - increased appetite, hypertriglyceridemia; very rarely, hyperglycemia and / or decompensation of diabetes mellitus, sometimes manifested by ketoacidosis or coma, including death; hypercholesterolemia, hypothermia. From the side of blood-forming organs: often - eosinophilia; rarely, leukopenia; very rarely - thrombocytopenia, neutropenia; in isolated cases - asymptomatic eosinophilia.; From the musculoskeletal system: very rarely - rhabdomyolysis.; From the urogenital system: very rarely - urinary retention, priapism. From the skin: rarely - photosensitization reaction; very rarely - alopecia.; Allergic reactions: rarely - skin rash; very rarely - anaphylactoid reactions, angioedema, pruritus or urticaria. Laboratory findings: very often - hyperprolactinemia, but clinical manifestations (for example, gynecomastia, galactorrhea and enlargement of the mammary glands) are rare; in most patients, prolactin levels spontaneously normalize without discontinuing therapy. Infrequently - increased activity of CPK; in isolated cases there was an increase in plasma glucose concentration, triglycerides,cholesterol.; Other: often - asthenia, peripheral edema; very rarely - withdrawal syndrome. In elderly patients with dementia, a high frequency of deaths and cerebrovascular disorders (stroke, transient ischemic attacks) has been reported in studies. Very frequent in this category of patients were gait disturbances and falls. Also, pneumonia, fever, lethargy, erythema, visual hallucinations and urinary incontinence were often observed. Among patients with medicinal (against the background of dopamine agonists) psychosis with Parkinson's, worsening of parkinsonian symptoms and the development of hallucinations were often recorded; neutropenia (4.1%) on the background of combination therapy with valproic acid in patients with bipolar mania. Simultaneous therapy with valproic acid or lithium increases the frequency (more than 10%) of tremor, dryness of the oral mucosa, increase appetite or increase body weight. Speech disorders were also recorded (from 1 to 10%).
Overdose
Symptoms: tachycardia, agitation / aggressiveness, articulation disorder, extrapyramidal disorders, depression of consciousness of varying severity (from sedation to coma), delirium, convulsions, neuroleptic malignant syndrome, respiratory depression, aspiration, increased or decreased blood pressure, arrhythmias, cardiac arrest and respiration. The minimum dose for acute overdose with a fatal outcome was 450 mg, the maximum dose with a favorable outcome (survival) - 1500 mg; Treatment: gastric lavage, the appointment of activated carbon, si Automatic treatment, maintenance of respiratory function. You should not use sympathomimetics (including norepinephrine, dopamine), which are β-adrenoreceptor agonists (stimulation of these receptors may aggravate the decrease in blood pressure). Careful medical observation and monitoring should be continued until the patient recovers.
Interaction with other drugs
Inductors or inhibitors of the CYP1A2 isoenzyme can alter the metabolism of olanzapine.; CYP1A2 isoenzyme inducers: olanzapine clearance is increased in smoking patients and with simultaneous use of carbamazepine, which leads to a decrease in the concentration of olanzapine in the blood plasma.It may be necessary to increase the dose of the drug.; CYP1A2 isoenzyme inhibitors: fluvoxamine significantly inhibits the metabolism of olanzapine. Decreasing olanzapine clearance increases olmanzapine Cmax in non-smoking women by 54% and 77% in male smokers, AUC by 52% and 108%, respectively, so patients taking fluvoxamine or any other CYP1A2 isoenzyme inhibitor (for example, ciprofloxacin) should be considered the possibility of using a lower initial dose of olanzapine.; Activated carbon reduces the bioavailability of olanzapine by 50-60% and should be taken at least 2 hours before or 2 hours after olanzapine.; Fluoxetine (CYP2D6 inhibitor), as well as a single dose of antacid drugs ( aluminum or magnesium) or cimetidine, did not have a significant effect on the pharmacokinetics of olanzapine.; Ethanol did not affect the pharmacokinetics of olanzapine in an equilibrium state, however, ethanol intake with olanzapine may be accompanied by increased pharmacological effects of olanzapine (sedative effect) .; valproic acid glucuronide (main metabolic pathway). Valproic acid has little effect on olanzapine metabolism. Clinically important pharmacokinetic sulfamethoxazole, ketoconazole, fluconazole and others) that disrupt the electrolyte balance or inhibit the metabolism of olanzapine in the liver.; Simultaneous It is not recommended to use olanzapine and antiparkinsonian drugs in patients with Parkinson's disease and dementia.; Olanzapine exhibits antagonism against dopamine and, theoretically, can inhibit the action of levodopa and dopamine agonists; 2C9, 2C19, 3A4), a clinically significant interaction is unlikely. No suppression of the metabolism of the following active substances was found: tricyclic antidepressants (representing mainly the CYP2D6 pathway), warfarin (CYP2C9), theophylline (CYP1A2) and diazepam (CYP3A4 and 2C19); no interaction was detected when used simultaneously with lithium or biperiden.
special instructions
While taking antipsychotic drugs, an improvement in the clinical status of patients can occur within a few days or weeks. Patients need to be carefully monitored throughout this period. Psychosis and / or dementia-related behavioral disorders; Olanzapine is not approved for use in treating psychosis and / or dementia-related behaviors and is not recommended for use in these patients from due to increased mortality and risk of cerebral circulation. When taking olanzapine in elderly patients with psychosis on the background of dementia, cerebrovascular disorders (stroke, transient ischemic attack), including deaths, were noted. These patients had previous risk factors (cerebrovascular disorders (in history), transient ischemic attacks, arterial hypertension, smoking), as well as concomitant diseases and / or medication associated with cerebrovascular disorders. The use of olanzapine is not recommended for the treatment of psychosis, associated with the administration of dopamine agonists in patients with Parkinson's disease. Malignant neuroleptic syndrome (NNS); When treated with neuroleptics (including olanzapine), NNS may develop. Clinical manifestations of ZNS are fever, muscle rigidity, changes in mental state, instability of vegetative functions (unstable levels of heart rate and blood pressure, tachycardia, sweating, cardiac arrhythmia). Additional signs may be increased levels of CPK, myoglobinuria (rhabdomyolysis) and acute renal failure. If the patient develops symptoms and signs of MNS or the appearance of unexplained fever without additional clinical manifestations of MNS, all antipsychotics should be canceled, incl. olanzapine; hyperglycemia and diabetes; there is a higher prevalence of diabetes in patients with schizophrenia. Cases of hyperglycemia, development of diabetes mellitus or exacerbation of pre-existing diabetes mellitus, ketoacidosis and diabetic coma have been very rarely observed. The causal relationship between antipsychotic drugs and these conditions has not been established.Clinical monitoring of patients with diabetes mellitus or with risk factors for its development is recommended.; Changes in lipid levels; If lipid levels change while receiving olanzapine, appropriate treatment should be prescribed, especially in patients with dyslipidemia or risk factors for the development of fat metabolism disorders; that olanzapine in vitro has anticholinergic activity, due to the limited clinical experience of using olanzapine in patients with concomitant diseases , caution is recommended when prescribing this drug to patients with prostatic hypertrophy, paralytic intestinal obstruction and other similar conditions. means. Patient monitoring and dose reduction are required. If hepatitis is detected (including hepatocellular, cholestatic, or mixed liver damage), olanzapine should be stopped.; Neutropenia; Olanzapine should be used with caution in patients with a decrease in white blood cell count, including neutrophils; with signs of depression or toxic impairment of bone marrow function under the influence of drugs (in history); with inhibition of bone marrow function due to concomitant disease, radio or chemotherapy (in history); with hypereosinophilia or myeloproliferative disease. Neutropenia is often observed with the combined use of olanzapine and valproate. The use of olanzapine in patients with clozapine-dependent neutropenia or agranulocytosis (in history) was not accompanied by a recurrence of these disorders. Termination of the drug administration ; nausea or vomiting; QT interval; As with other antipsychotic drugs, caution should be exercised during olanzapine treatment if this drug is given at the same time as Reparata, prolong the QTc interval,especially in elderly patients, patients with congenital QT lengthening syndrome, congestive heart failure, cardiac hypertrophy, hypokalemia, hypomagneemia, or QT lengthening in the family history. Simultaneous use of other neuroleptics or drugs that also prolong the QT interval or cause hypokalemia should be avoided; ; The coincidence of olanzapine and venous thromboembolism was registered in rare cases (less than 0.01%). The causal relationship between the symptoms of vein thromboembolism and olanzapine intake has not been established. However, since schizophrenic patients often have acquired risk factors for venous thromboembolism, all possible risk factors for venous thromboembolism, such as immobility of patients, should be identified and preventive measures taken; Convulsive seizures; Olanzapine should be used with caution in patients with a history of seizures or undergoing the effects of factors that reduce the threshold of convulsive readiness. Seizures in patients receiving olanzapine are rare. In most of these cases, a history of convulsive seizures or risk factors of convulsive seizures have been reported. Late dyskinesia; With the development of signs of tardive dyskinesia, a dose reduction or elimination of olanzapine is recommended. Symptoms of tardive dyskinesia may increase or manifest after discontinuation of the drug. Orthostatic hypotension; In clinical trials of olanzapine, orthostatic hypotension was not often observed in elderly patients. As in the case of taking other antipsychotic drugs, it is recommended to periodically measure blood pressure in patients over 65 years of age.; Use in pediatrics; Olanzapine is not recommended for use in the treatment of children and adolescents. Studies conducted in patients aged 13-17 years, revealed a variety of adverse reactions, including weight gain, changes in metabolic parameters and increased prolactin levels. The long-term outcomes of these phenomena have not been studied and remain unknown.; Lactose; This drug contains lactose, so it should not be given to patients with rare hereditary disorders of tolerance to galactose, hereditary Saami lactase deficiency or glucose-galactose malabsorption.; Additionalinformation; Caution should be exercised when using olanzapine in combination with other centrally acting drugs and ethanol. Influencing the ability to drive vehicles and control mechanisms; During treatment, care must be taken when driving and engaging in potentially hazardous activities that require increased concentration and the speed of psychomotor reactions.