Pharmacodynamics and pharmacokinetics
Pharmacodynamics
The antipsychotic effect of the drug is associated with the blockade of dopamine D2 receptors in the brain, and the sedative effect is associated with the blockade of adrenergic receptors in the brain stem.
It also has an antiemetic effect , which is due to the blockade of D2 receptors of the vomiting center.
Influences m-cholino-, H1-histamine receptors. Eliminates productive symptoms (delusions, hallucinations), reduces emotional autism , hostility and suspicion. Does not cause extrapyramidal disorders .
Pharmacokinetics
Absorbed quickly. Eating does not affect absorption. After intramuscular administration, Cmax in the blood is determined after 15-45 minutes, and when taken orally after 5-8 hours. Up to 93% is bound to blood proteins. Metabolized in the liver to inactive metabolites. T1/2 within 21–54 hours. About 57% is excreted in the urine in the form of metabolites.
Indications for use of Zyprexa tablets
Olanzapine is indicated for the treatment of exacerbations and as maintenance therapy for schizophrenia and other psychoses with severe positive (delusions, hallucinations, thought disorders, hostility and suspiciousness) and/or negative symptoms (for example, flattened affect, emotional and social isolation, poverty of speech). Olanzapine also reduces the severity of secondary mood symptoms commonly associated with schizophrenia and similar disorders. Olanzapine is effective in maintaining clinical improvement with long-term therapy in patients who respond to initial therapy. Olanzapine, as monotherapy or in combination with lithium or valproate, is indicated for the treatment of acute manic or mixed episodes in bipolar disorder, with or without psychotic features, as well as rapid cycling. Olanzapine is indicated to reduce the severity of manic, mixed or depressive episodes in bipolar disorders and prolong the interictal period. Olanzapine in combination with fluoxetine is indicated for the treatment of depressive episodes occurring in bipolar disorder.
Zyprexa, instructions for use (Method and dosage)
The tablets are taken orally. The drug is started at 10 mg once a day. Subsequently, the dose can be increased to 20 mg/day.
The powder is dissolved with water for injection, the prepared solution is administered intramuscularly. Not administered intravenously or subcutaneously. The solution must be used within 1 hour. The recommended dose is 10 mg as a single injection, with a second injection given 2 hours later. To continue treatment, the drug is prescribed in tablets at a dose of 5-20 mg/day.
Instructions for use of Zyprexa contain a warning regarding the use of the drug in patients with prostate hypertrophy , a history of convulsive conditions angle-closure glaucoma , liver and kidney .
Overdose of Zyprexa tablets, symptoms and treatment
Symptoms: very common (≥10%) symptoms of olanzapine overdose are tachycardia, agitation/aggression, dysarthria, various extrapyramidal disorders and disturbances of consciousness of varying severity (from sedation to coma). Other clinically significant effects of olanzapine overdose included delirium, seizures, coma, potential for NMS, respiratory depression, aspiration, hypertension or hypotension, arrhythmias (≤2% of cases), and cardiopulmonary shock. The minimum dose for an acute overdose with a fatal outcome was 450 mg, the maximum for an overdose with a favorable outcome was 1500 mg. Treatment: there is no specific antidote. It is not recommended to prescribe drugs that cause vomiting. Gastric lavage and administration of activated charcoal are indicated (its use reduces the bioavailability of olanzapine when taken orally by 50–60%). Symptomatic treatment is recommended in accordance with the clinical condition and monitoring of vital organ functions, including the elimination of arterial hypotension, circulatory collapse and support of respiratory function. Dopamine, epinephrine and other sympathomimetics, which are β-adrenergic receptor agonists, should not be used, since β-adrenergic stimulation can aggravate the manifestations of arterial hypotension. Cardiac monitoring of the cardiovascular system is necessary for timely detection of possible arrhythmia. Careful medical observation should be carried out until the patient recovers.
Interaction
Zyprexa reduces the effects of Levodopa and dopamine agonists . There is no interaction with Cimetidine , Imipramine , antacids , Warfarin , Diazepam , Theophylline , or biperidenolithium . Carbamazepine increases the metabolism of the drug. Activated carbon reduces bioavailability by 50%.
Zyprexa®
Clinical improvement with antipsychotic treatment may take several days to several weeks and requires careful monitoring of the patient.
Suicide
The risk of suicide attempts in patients with schizophrenia and bipolar disorder type 1 is determined by these diseases themselves. In this regard, during pharmacotherapy, careful monitoring of those patients whose risk of suicide is especially high is required. When prescribing olanzapine, efforts should be made to minimize the number of tablets taken by the patient in order to reduce the risk of overdose.
Neuroleptic malignant syndrome
Neuroleptic malignant syndrome (NMS) can develop during treatment with any antipsychotic drug, including olanzapine. Clinical manifestations of neuroleptic malignant syndrome include significant increase in body temperature, muscle rigidity, changes in mental status and autonomic disturbances (unstable pulse or blood pressure, tachycardia, arrhythmias, increased sweating). Additional features may include increased creatine phosphokinase activity, myoglobinuria (rhabdomyolysis), and acute renal failure. Clinical manifestations of neuroleptic malignant syndrome or a significant unexplained increase in body temperature without other symptoms of neuroleptic malignant syndrome require discontinuation of all antipsychotics, including olanzapine.
Tardive dyskinesia
In comparative studies lasting more than 6 weeks, treatment with olanzapine was significantly less likely to be accompanied by the development of dyskinesia requiring drug correction than the use of haloperidol. However, the increased risk of tardive dyskinesia should be taken into account with long-term therapy with antipsychotics. If signs of tardive dyskinesia develop, it is recommended to reduce the dose or discontinue olanzapine. Symptoms of tardive dyskinesia may increase or manifest after discontinuation of the drug.
Psychosis associated with dementia and/or conduct disorders
Olanzapine is not indicated for the treatment of psychosis associated with dementia and/or behavioral disorders and is not recommended for use in this group of patients due to the high mortality rate and risk of cerebrovascular accidents. In placebo-controlled studies (duration 6-12 weeks) in elderly patients (mean age 78 years) with psychosis associated with dementia and/or conduct problems, there was a two-fold higher incidence of death in patients in the olanzapine group compared with those in the olanzapine group. placebo group (3.5% and 1.5%, respectively). The higher mortality rate was not associated with the dose of olanzapine (mean dose 4.4 mg) or duration of treatment. Risk factors that may predispose this group of patients to higher mortality when treated with olanzapine include age ≥ 65 years, dysphagia, sedation, malnutrition (wasting), dehydration, concomitant use with benzodiazepines, or the presence of pulmonary pathology (eg, pneumonia with with or without aspiration).
Cerebrovascular adverse events (eg, stroke, transient ischemic attack), including deaths, were observed in the same studies of olanzapine in elderly patients. In placebo-controlled studies, there was a threefold higher incidence of cerebrovascular adverse events in patients in the olanzapine group compared with the placebo group (1.3% versus 0.4%, respectively). All patients with cerebrovascular disorders had previous risk factors for the development of cerebrovascular adverse events: age ≥75 years, vascular or mixed dementia, a previous case of cerebrovascular adverse event or transient ischemic attack, arterial hypertension, smoking, as well as concomitant diseases and/or medications, temporally associated with cerebrovascular adverse events. The effectiveness of olanzapine was not established in these studies.
Parkinson's disease
The use of olanzapine is not recommended in the treatment of psychosis induced by dopamine receptor agonists in Parkinson's disease.
In clinical trials in patients with drug-induced psychosis (dopamine receptor agonist) for Parkinson's disease, increased parkinsonian symptoms and hallucinations were very common (≥10%) and at a higher frequency than in the placebo group. Olanzapine was not superior to placebo in treating psychotic symptoms in patients with Parkinson's disease. In these clinical studies, patients were required to take antiparkinsonian drugs (dopamine agonists) at the lowest effective dose and continue to take them at the same dose throughout the study. The starting dose of olanzapine was 2.5 mg per day and could be increased to 15 mg per day as recommended by the physician.
Liver dysfunction
In some cases, taking olanzapine, usually in the early stages of therapy, was accompanied by a transient, asymptomatic increase in hepatic aminotransferases (aspartate aminotransferase and alanine aminotransferase) in the blood serum. Rare cases of hepatitis have been reported. In very rare cases, hepatic cholestasis and other associated liver damage have been observed. Particular caution is required when serum aspartate aminotransferase and/or alanine aminotransferase activity increases in patients with impaired liver function, with limited liver functional reserve, or in patients receiving treatment with potentially hepatotoxic drugs.
Hyperglycemia and diabetes mellitus
Patients with schizophrenia have a higher prevalence of diabetes. As with some other antipsychotic drugs, cases of hyperglycemia, diabetes, exacerbation of pre-existing diabetes, ketoacidosis and diabetic coma have been reported. Close clinical monitoring of patients with diabetes and patients with risk factors for developing diabetes is recommended according to the following guidelines: measurement of blood glucose concentrations at baseline, 12 weeks after starting olanzapine, and annually thereafter. Patients taking antipsychotic drugs, including Zyprexa®, should be monitored for signs and symptoms of hyperglycemia (such as polydipsia, polyuria, polyphagia, weakness). Patients with diabetes mellitus or risk factors for diabetes mellitus require regular monitoring of blood glucose concentrations. Regular monitoring of body weight is necessary: before starting treatment, 4, 8 and 12 weeks after starting olanzapine, and subsequently every 3 months.
Change in lipid profile
During placebo-controlled studies, undesirable lipid changes were observed in patients receiving olanzapine (see Adverse Reactions), especially in patients with dyslipidemia and in patients with risk factors for developing lipid disorders. Patients taking antipsychotic medications, including Zyprexa, should have their lipid profiles monitored regularly as recommended: before starting treatment, 12 weeks after starting olanzapine, and every 5 years thereafter.
Sudden cardiac death
Sudden deaths have been reported in post-marketing surveillance of olanzapine. A retrospective observational study found an approximately twofold increase in the risk of sudden death in the olanzapine group compared with the group of patients not receiving antipsychotics. In this study, these results for olanzapine were comparable to those for the other atypical antipsychotics included in the analysis. Spontaneous reports of sudden death during post-marketing surveillance have been rare.
Convulsions
Olanzapine should be used with caution in patients with a history of seizures or exposure to factors that lower the seizure threshold. Cases of seizures were uncommon in patients taking olanzapine, and in most of these cases, the patients had a history of seizures or risk factors for seizures.
Hematological changes
As with the use of other antipsychotics, caution should be exercised when treating patients with olanzapine with a low number of leukocytes and/or neutrophils in the peripheral blood due to various reasons; with signs of suppression or toxic impairment of bone marrow function under the influence of drugs in the anamnesis; with suppression of bone marrow function due to concomitant disease, radiotherapy or chemotherapy in history; with hypereosinophilia or myeloproliferative disease.
In clinical studies, the use of olanzapine in patients with a history of clozapine-dependent neutropenia or agranulocytosis was not accompanied by relapses of these disorders.
Cancellation of therapy
In case of immediate withdrawal of olanzapine, sudden development of sweating, insomnia, tremor, anxiety, nausea and vomiting was rarely (≥ 0.01% and < 0.1%) reported.
QT interval duration
In clinical studies, clinically significant prolongation of the QT interval (QT interval adjusted by Fridericius [QTcF] > 500 ms in patients with baseline QTcF < 500 ms) was observed infrequently (0.1% to 1%) in patients receiving olanzapine, while no significant differences with placebo in the incidence of adverse cardiac events. However, as with other antipsychotics, caution is recommended when prescribing olanzapine in combination with drugs that can prolong the QT interval, especially in elderly patients with congenital prolongation of the QT interval, congestive heart failure, myocardial hypertrophy, hypokalemia and hypomagnesemia .
General activity in relation to the central nervous system (CNS)
Given the primary action of olanzapine on the central nervous system, caution should be exercised when using olanzapine in combination with other centrally acting drugs and alcohol.
Postural hypotension
Postural hypotension was observed infrequently in clinical studies of olanzapine in the elderly. As with other antipsychotics, periodic monitoring of blood pressure is recommended when olanzapine is prescribed to patients over 65 years of age.
Thromboembolism
Infrequently (≥ 0.1% and < 1%) cases of a temporal association between the development of venous thromboembolism and olanzapine therapy have been reported. The presence of a cause-and-effect relationship between olanzapine and venous thromboembolism has not been established. However, given that patients with schizophrenia often have acquired risk factors for venous thromboembolism, it is necessary to conduct a cumulative assessment of all possible risk factors for the development of this complication, including immobilization of patients, and take the necessary preventive measures.
Lactose
Zyprexa® tablets contain lactose. Patients with rare hereditary galactose intolerance, lactase intolerance and glucose-galactose malabsorption should not take olanzapine.
Anticholinergic activity
Although olanzapine exhibited anticholinergic activity in in vitro studies, olanzapine therapy was rarely associated with anticholinergic side effects in clinical studies. However, clinical experience with olanzapine in patients with comorbidities is limited, and caution is recommended when prescribing olanzapine to patients with clinically significant prostatic hypertrophy, paralytic ileus, angle-closure glaucoma, and similar conditions.
Dopaminergic antagonism
In vitro
Olanzapine exhibits dopamine antagonism and, like other antipsychotics, may theoretically inhibit the effects of levodopa and dopamine agonists.
Analogs
Level 4 ATX code matches:
Lakvel
Leponex
Zalasta
Quentiax
Closasten
Ketilept
Clozapine
Quetiapine
Seroquel
Azaleptin
Zalasta , Zyprexa Zidis , Ku-tab , Olanzapine , Normiton , Olanex , Olanzapin-Teva , Parnasan , Saphris , Egolanza .
Reviews of Zyprex
Looking through forums dedicated to the treatment of mental disorders, there are many positive reviews about the drug Zyprexa. Almost all patients noted the high effectiveness of the drug, which was prescribed long-term in maintenance doses on an outpatient basis.
Negative reviews about Zyprex on the forums relate primarily to adverse reactions. Metabolic disorders and the risk of developing diabetes mellitus come to the fore.
“Zyprexa gives me an increased appetite. Will Siofor or other drugs relieve this?”
“...the appetite is huge. Weight gain of 12 kilos in just 5 years.”
“...I took Zyprexa for six months. There was an increased appetite."
“Zyprexa causes weight gain.”
“I took Zyprexa and my periods disappeared for several months.”
“...the withdrawal syndrome was terrible. There were fears and anxieties.”
In men, enlargement of the mammary glands was observed, which occurred without discontinuation of the drug. Some patients complained of dizziness, dry mouth and constipation. There are complaints about the high cost of the drug.
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** The Drug Directory is intended for informational purposes only. For more complete information, please refer to the manufacturer's instructions. Do not self-medicate; You should consult your doctor before starting to use Zyprexa. EUROLAB is not responsible for the consequences caused by the use of information posted on the portal. Any information on the site does not replace medical advice and cannot serve as a guarantee of the positive effect of the drug.
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Zyprexa price, where to buy
You can buy it in many pharmacies in Moscow. The price of Zyprexa tablets 10 mg No. 28 in various pharmacies ranges from 2,407 rubles. up to 4950 rub.
- Online pharmacies in RussiaRussia
LuxPharma* special offer
- Zyprexa tablet.
10 mg 28 pcs 3400 rub. order
ZdravCity
- Zyprexa tablets p.p.o. 10 mg 28 pcs Eli Lilly SA Spain
RUR 4,238 order
- Zyprexa tablets p.p.o. 5 mg 28 pcs Lilly SA
RUB 2192 order
