What is olanzapine
OlanzapineDrug groupsAtypical neuroleptics Olanzapine is an antipsychotic, antimanic and mood-stabilizing agent from the group of atypical neuroleptics for the treatment of schizophrenia or bipolar disorder. The effects are based on the interaction with various neurotransmitter receptors. Olanzapine is an antagonist at dopamine and serotonin receptors. The tablets are taken once a day with or without meals. Possible adverse effects include tiredness, weight gain, changes in blood parameters and movement disorders. Olanzapine is a substrate for CYP450 isozymes.
Olanzapine is commercially available in the form of film-coated tablets, orodispersible tablets and as a powder for the preparation of a solution for injection (Zyprexa®, generics). It has been approved in the USA and the EU since 1996 and in Switzerland since 1997. Generics came on the market in 2012.Structure and properties
Olanzapine (C.17H20N4S, Mr = 312.4 g / mol) belongs to the thienobenzodiazepine derivatives. It is a yellow, crystalline powder that is practically insoluble in water. Olanzapine is structurally closely related to clozapine (Leponex®, generics).
Olanzapine (ATC N05AH03) has antipsychotic, antimanic and mood stabilizing properties. The effects are based on the antagonism of serotonin receptors, dopamine receptors, cholinergic muscarinic receptors, α1 adrenoceptors and histamine H1 receptors. The half-life is between 29 and 55 hours, depending on age and gender.
Mechanism of action of neuroleptics, click to enlarge. Illustration © PharmaWikiIndications
- Bipolar disorder
According to the specialist information. The tablets are taken once a day with or without meals. The orodispersible tablets are allowed to dissolve in the mouth and the solution for injection is injected intramuscularly.Contraindications
- Patients at known risk of narrow-angle glaucoma
- Children and young people under 18 years of age
The complete precautionary measures can be found in the product information sheet.Interactions
Olanzapine is conjugated and oxidized. It is a substrate of CYP1A2 and, to a lesser extent, CYP2D6. Interactions can occur with central depressant drugs and alcohol, among others.unwanted effects
The most common possible adverse effects include:
- Drowsiness, dizziness, weakness, fatigue
- Increased appetite, weight gain
- Eosinophilia, leukopenia, neutropenia
- Elevated prolactin, cholesterol, glucose, uric acid, creatine phosphokinase and triglyceride levels, glucosuria
- Increase in liver enzymes
- Sitting restlessness, Parkinsonism, movement disorders
- Orthostatic hypotension
- Anticholinergic side effects
- Rash, edema
- Fever, joint pain
- Pharmaceutical product information (CH, D, USA)
- Duggan L., Fenton M., Dardennes R.M., El-Dosoky A., Indran S. Olanzapine for schizophrenia. Cochrane Database Syst Rev, 2000, 2 Pubmed
- European Pharmacopoeia PhEur
- Green B. Focus on olanzapine. Curr Med Res Opin, 1999, 15 (2), 79-85 Pubmed
- Kantrowitz J.T., Citrome L. Olanzapine: review of safety 2008. Expert Opin Drug Saf, 2008, 7 (6), 761-9 Pubmed
- Kruger S. Olanzapine in the treatment of bipolar disorder. Psychiatr Prax, 2006, 33 (1), 18-26 Pubmed
- Lund B.C., Perry P.J. Olanzapine: an atypical antipsychotic for schizophrenia. Expert Opin Pharmacother, 2000, 1 (2), 305-23 Pubmed
- Rao M.L., Hiemke C., Grasmäder K., Baumann P. Olanzapine: pharmacology, pharmacokinetics and therapeutic drug monitoring. Fortschr Neurol Psychiatr, 2001, 69 (11), 510-7 Pubmed
- Wittköpper K., El-Armouche A., Eschenhagen T. Olanzapine. Dtsch Med Wochenschr, 2008, 133 (39), 1958-62 Pubmed
Conflicts of Interest: None / Independent. The author has no relationships with the manufacturers and is not involved in the sale of the products mentioned.additional Information
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This article was last changed on 5/21/2020.
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