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Olanzapine

Zyprexa

Second-Generation AntipsychoticGeneric availableTDM data

The mechanism of action of olanzapine, in the listed indications is unclear. However, the efficacy of olanzapine in schizophrenia could be mediated through a combination of dopamine and serotonin type 2 (5HT2) antagonism.

Compare Olanzapine

FDA-Approved Indications

  • Schizophrenia (adults; adolescents 13–17 years)
  • Acute manic or mixed episodes in Bipolar I — mono or adjunct with lithium/valproate
  • Bipolar I maintenance (adults)
  • Treatment-resistant depression — combination with fluoxetine (adults)
  • Acute agitation in schizophrenia/bipolar mania (IM, adults)

Common Off-Label Uses

  • Anorexia nervosa
  • Chemotherapy-induced nausea
  • Delirium
  • Agitation in dementia
  • Treatment-resistant OCD (adjunct)

What Sets This Drug Apart

  • Among the most effective SGAs for overall symptom reduction in NMA data, with very low EPS (akathisia and parkinsonism risk ratios ~1.0 vs placebo)
  • Highest or co-highest weight gain among SGAs: ~22% exceed 7% gain at 6 weeks, rising to ~64% by 12 months per FDA label
  • FDA-approved combination with fluoxetine (Symbyax) for bipolar depression and treatment-resistant unipolar depression
  • CYP1A2 substrate — smokers often need 1.5-2x higher doses than non-smokers; dose adjustment required with smoking changes
  • Sedation is early-onset (median ~4 days) but often self-limited: 50% resolve within 1 week, 75% within 1 month
  • Higher-dose strategy (20-40 mg/day, plasma level target 125-200 ng/mL) shows benefit in TRS when clozapine is not feasible
  • Available as long-acting injectable (olanzapine pamoate) requiring 3-hour post-injection observation for rare delirium/sedation syndrome (0.2%)
Boxed Warning
WARNING: INCREASED MORTALITY IN ELDERLY PATIENTS WITH DEMENTIA-RELATED PSYCHOSIS Elderly patients with dementia-related psychosis treated wi