Olanzapine
Olanzapine (sold under the trade name Zyprexa among others) is an atypical antipsychotic primarily used to treat schizophrenia and bipolar disorder. For schizophrenia, it can be used for both new-onset disease and long-term maintenance. It is taken by mouth or by injection into a muscle.
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Trade names | Zyprexa, Zypine, others |
AHFS/Drugs.com | Monograph |
MedlinePlus | a601213 |
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Routes of administration | By mouth, intramuscular injection |
Drug class | Atypical antipsychotic |
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Bioavailability | 60-65% |
Protein binding | 93% |
Metabolism | Liver (direct glucuronidation and CYP1A2 mediated oxidation) |
Elimination half-life | 33 hours, 51.8 hours (elderly) |
Excretion | Urine (57%; 7% as unchanged drug), faeces (30%) |
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ECHA InfoCard | 100.125.320 |
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Formula | C17H20N4S |
Molar mass | 312.44 g·mol−1 |
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Melting point | 195 °C (383 °F) |
Solubility in water | Practically insoluble in water mg/mL (20 °C) |
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Common side effects include weight gain, movement disorders, dizziness, feeling tired, constipation, and dry mouth. Other side effects include low blood pressure with standing, allergic reactions, neuroleptic malignant syndrome, high blood sugar, seizures, and tardive dyskinesia. In older people with dementia, its use increases the risk of death. Use in the later part of pregnancy may result in a movement disorder in the baby for some time after birth. Although how it works is not entirely clear, it blocks dopamine and serotonin receptors.
Olanzapine was patented in 1991 and approved for medical use in the United States in 1996. It is available as a generic medication. In 2020, it was the 164th most commonly prescribed medication in the United States, with more than 3 million prescriptions. Eli Lilly also markets olanzapine in a fixed-dose combination with fluoxetine as olanzapine/fluoxetine (Symbyax). It is on the World Health Organization's List of Essential Medicines.