Products
Olanzapine is commercially available as film-coated tablets, meltable tablets, and powder for solution for injection (Zyprexa, generics). It has been approved in the U.S. and EU since 1996 and in many countries since 1997. Generic versions entered the market in 2012.
Structure and properties
Olanzapine (C17H20N4S, Mr = 312.4 g/mol) belongs to the thienobenzodiazepine derivatives. It exists as a yellow crystalline powder that is practically insoluble in water. Olanzapine is structurally closely related to clozapine (Leponex, generics).
Effects
Olanzapine (ATC N05AH03) has antipsychotic, antimanic, and mood-stabilizing properties. The effects are due to antagonism at serotonin receptors, dopamine receptors, cholinergic muscarinic receptors, α1-adrenoceptors, and histamine H1 receptors. Half-life ranges from 29 to 55 hours depending on age and gender.
Indications
- Schizophrenia
- Bipolar disorders
Dosage
According to the professional information. The tablets are taken once a day, regardless of meals. The melting tablets are melted in the mouth and the injection solution is injected intramuscularly.
Contraindications
- Hypersensitivity
- Patients at known risk for narrow-angle glaucoma
- Children and adolescents under 18 years of age
For complete precautions, see the drug label.
Interactions
Olanzapine is conjugated and oxidized. It is a substrate of CYP1A2 and, to a lesser extent, CYP2D6. Interactions may occur with central depressant drugs and alcohol, among others.
Adverse effects
The most common potential adverse effects include:
- Drowsiness, dizziness, weakness, fatigue.
- Increased appetite, weight gain
- Eosinophilia, leukopenia, neutropenia.
- Increased prolactin, cholesterol, glucose, uric acid, creatine phosphokinase and triglyceride levels, glucosuria.
- Increase in liver enzymes
- Sit restlessness, parkinsonism, movement disorders.
- Orthostatic hypotension
- Anticholinergic side effects
- Rash, edema
- Fever, joint pain