Olanzapine
From Pharmacopedia
More actions
Olanzapine
Zyprexa (oral, IM acute), Zyprexa Zydis (ODT), Zyprexa Relprevv (LAI), Lybalvi (with samidorphan)
Experience
No personal reports yet
No clinical reports yet
Log in to add your own experience.
Problems
No problems yet. Be the first to suggest one.
+ Add a problemTitration strategies
No titration strategies yet. Be the first to suggest one.
Effects
No effects listed yet. Be the first to suggest one.
Relevant anecdote
No anecdotes yet. Share a relevant one.
Relevant Literature
No literature entries yet.
Log in to submit relevant literature.
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