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Manufacturers: Patheon Italia (Italy)
Active ingredients
- Olanzapine
Disease class
- Schizophrenia
- Chronic delusional disorders
- Schizoaffective disorders
Clinical and pharmacological group
- Not indicated. See instructions
Pharmacological action
- Antipsychotic
Pharmacological group
- Neuroleptics
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.
Drug interactions Zyprexa tablets
The metabolism of olanzapine may be influenced by inhibitors or inducers of cytochrome P450 isoforms, especially CYP 1A2. Smoking or concomitant administration of carbamazepine increases the clearance of olanzapine. Smoking and treatment with carbamazepine stimulate CYP 1A2 activity. Inhibitors of CYP1A2 activity may reduce the clearance of olanzapine. Olanzapine is a weak inhibitor of CYP1A2 activity; it does not alter the pharmacokinetics of theophylline, which is predominantly metabolized by CYP 1A2. Clinical studies have found that the use of olanzapine during therapy with the following drugs is not accompanied by inhibition of the metabolism of such drugs: imipramine or its metabolite desipramine (CYP 2D6, CYP 3A, CYP 1A2), warfarin (CYP 2C19), theophylline (CYP 1A2), diazepam ( CYP 3A4, CYP 2C19). There was no interaction of olanzapine when administered concomitantly with lithium salts or biperiden. When steady state concentrations were reached, olanzapine did not affect the pharmacokinetics of ethanol. However, when ethanol is used concomitantly with olanzapine, additive pharmacological effects, such as increased sedation, may occur. Single doses of cimetidine or aluminum/magnesium-containing antacids did not affect the oral bioavailability of olanzapine. Additional administration of activated charcoal reduced the oral bioavailability of olanzapine by 50–60%. Fluoxetine (60 mg as a single dose or 60 mg daily for 8 days) resulted in an average increase in the maximum concentration of olanzapine by 16% and an average decrease in olanzapine clearance by 16%. The variation of these factors is small compared to the overall individual variability, so dosage adjustments are usually not required. Fluvoxamine, a CYP1A2 inhibitor, reduces the clearance of olanzapine. This results in an average increase in fluvoxamine Cmax: 54% among non-smoking women and 77% among male smokers. The mean increase in olanzapine AUC was 52% and 108%, respectively. Patients taking fluvoxamine should have their dosage of olanzapine reduced. In vitro experiments with human liver microsomes revealed that olanzapine has a slight ability to suppress the process of glucuronidation of valproic acid (the main route of its metabolization). In addition, a negligible effect of valproate on the metabolism of olanzapine in vitro . Daily additional in vivo of 10 mg olanzapine for 2 weeks did not affect the steady-state plasma concentration of valproate. Therefore, when valproate and olanzapine are used in combination, no additional adjustment of the dose of valproate is required. With a single intramuscular injection of olanzapine at a dose of 5 mg 1 hour before the administration of 2 mg of lorazepam, the pharmacokinetics of these drugs did not change. However, the administration of this combination of drugs was accompanied by increased drowsiness, which is typical when each drug is administered separately. Olanzapine has antagonistic activity against α1-adrenergic receptors. The drug should be prescribed with caution to patients taking antihypertensive drugs. Because olanzapine is metabolized by CYP 1A2, substances that can stimulate or inhibit this isoenzyme may affect the pharmacokinetics of olanzapine.
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 .
Description of the drug ZYPREXA® (ZYPREXA®)
Use with extreme caution when increasing the activity of AST and ALT in patients with insufficiency of liver function, limited functional reserve of the liver, or in patients receiving treatment with potentially hepatotoxic drugs. If the activity of AST and/or ALT increases during treatment with olanzapine, careful monitoring of the patient is required and, if necessary, dose reduction.
Use with caution in patients with a history of epileptic seizures or exposed to factors that lower the seizure threshold.
Use with caution in patients with a low number of leukocytes and/or neutrophils due to various reasons; with signs of suppression/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.
Use with caution in patients with clinical manifestations of prostatic hyperplasia, paralytic ileus, angle-closure glaucoma and similar conditions.
When treated with antipsychotics, including olanzapine, the development of NMS is possible. Clinical manifestations of NMS or a significant increase in body temperature without other symptoms of this syndrome require the abolition of all antipsychotics, including olanzapine.
With long-term therapy with antipsychotics, there is a risk of developing tardive dyskinesia. If signs of tardive dyskinesia develop, it is recommended to reduce the dose or discontinue olanzapine. Symptoms of tardive dyskinesia may appear or worsen after discontinuation of therapy.
Given the nature of the action of olanzapine on the central nervous system, it should be used with caution in combination with other centrally acting drugs and ethanol.
The safety and effectiveness of olanzapine in patients under 18 years of age have not been studied.
Impact on the ability to drive vehicles and operate machinery
During the treatment period, caution should be exercised in engaging in activities that require concentration and high speed of psychomotor reactions.
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%.
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.
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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** Attention! The information presented in this medication guide is intended for medical professionals and should not be used as a basis for self-medication. The description of Zyprexa is provided for informational purposes only and is not intended for prescribing treatment without the participation of a physician. Patients need to consult a specialist!
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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 Zidis tab. dispers. 5mg n28Katalent/Eli Lilly
RUB 2,386 order
- 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
