Olanzapine
Olanzapine
Zyprexa (oral, IM acute), Zyprexa Zydis (ODT), Zyprexa Relprevv (LAI), Lybalvi (with samidorphan)
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Summary
Common uses
Schizophrenia (FDA)0, Bipolar I mania and mixed episodes (FDA)0, Bipolar I maintenance (FDA)0, Bipolar depression (FDA, in combination with fluoxetine as Symbyax)0, Acute agitation in schizophrenia or bipolar disorder (FDA, IM)0, Treatment-resistant depression adjunct (off-label)0, Anorexia nervosa (off-label, evidence-supported)0
Pharmacy
Starting dose
Schizophrenia / acute mania: 5-10 mg PO once daily, target 10-15 mg/day. Acute agitation IM: 10 mg, may repeat in 2 hours. Relprevv LAI: 150-300 mg every 4 weeks after oral overlap
Preparations
Tablets 2.5, 5, 7.5, 10, 15, 20 mg; ODT (Zydis) 5, 10, 15, 20 mg; acute IM injection 10 mg/vial; Relprevv LAI 210, 300, 405 mg vials
US FDA Max
20 mg/day (oral)
Pharmacology
Routes
Oral, intramuscular (acute and long-acting)
Onset
Sedation from first dose; neuroleptic effect emerges over days to weeks
Duration
24 hours (oral); 2-4 weeks (LAI)
Half-life
21-54 hours[1]
Bioavailability
~60% (oral); ~100% (IM)[1]
Pregnancy
Signal for gestational diabetes and metabolic syndrome with maternal exposure; the metabolic load can be substantial during pregnancy.[citation needed]
Legal status
Rx-only in US. Carries the atypical-neuroleptic Boxed Warning for increased mortality in elderly patients with dementia-related psychosis. Zyprexa Relprevv LAI additionally carries a Boxed Warning for post-injection delirium/sedation syndrome requiring 3-hour monitored observation after each injection[1]
Purported mechanism
Multi-receptor antagonist with broad activity at D1, D2, D3, D4 dopamine receptors (D2/D3 mediating the neuroleptic effect), 5-HT2A and 5-HT2C serotonin receptors (the atypical-neuroleptic feature, reducing extrapyramidal burden), H1 histamine (mediating sedation and weight gain), M1-M5 muscarinic (anticholinergic effects), and α1-adrenergic (orthostatic hypotension) receptors.0 The marquee tolerability concern is severe metabolic burden: weight gain often exceeding 10 kg in the first year, insulin resistance, hyperlipidemia, and elevated type 2 diabetes risk, among the worst in the second-generation class. Routine metabolic monitoring (weight, fasting glucose, lipid panel) is standard. The Lybalvi formulation combines olanzapine with samidorphan, an opioid antagonist, to mitigate weight gain[1].
References
- ↑ 1.0 1.1 1.2 1.3 FDA Prescribing Information, Zyprexa (olanzapine), Eli Lilly, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/020592s062,021086s041,021253s048lbl.pdf