Absorption: Well absorbed but rapidly metabolized by first-pass effect, resulting in 60% bioavailability. Conventional tablets and orally disintegrating tablets (Zydis) are bioequivalent. IM administration results in significantly higher blood levels (5 times that of oral).
Distribution: Extensively distributed.
Protein Binding: 93%.
Metabolism/Excretion: Highly metabolized (primarily by the CYP1A2 isoenzyme); 7% excreted unchanged in urine.
Half-life: 2154 hr.
CV: orthostatic hypotension, bradycardia, chest pain, syncope, tachycardia.
Derm: DRUG REACTION WITH EOSINOPHILIA AND SYSTEMIC SYMPTOMS (DRESS), photosensitivity.
EENT: amblyopia, rhinitis, ↑ salivation, pharyngitis.
Endo: galactorrhea, goiter, gynecomastia, hyperglycemia, hyperprolactinemia.
GI: constipation, dry mouth, ↑liver enzymes, abdominal pain, dysphagia, nausea, ↑ thirst.
GU: amenorrhea, ↓ fertility (females), ↓ libido, impotence, urinary incontinence.
Hemat: AGRANULOCYTOSIS, leukopenia, neutropenia.
Metab: weight loss or gain, dyslipidemia, ↑ appetite.
MS: hypertonia, joint pain.
Neuro: tremor , NEUROLEPTIC MALIGNANT SYNDROME, SEIZURES, SUICIDAL THOUGHTS, agitation, delirium, dizziness, headache, restlessness, sedation, weakness, dystonia, falls, insomnia, mood changes, personality disorder, speech impairment, tardive dyskinesia.
Resp: cough, dyspnea.
Misc: aspiration, body temperature dysregulation, fever, flu-like syndrome.
Schizophrenia
- PO (Adults Most Patients): 510 mg/day initially; may ↑ at weekly intervals by 5 mg/day (target dose = 10 mg/day; not to exceed 20 mg/day).
- PO (Adults Debilitated or Nonsmoking Female Patients
65 yr): Initiate therapy at 5 mg/day. - PO (Children 1317 yr): 2.55 mg/day initially; may ↑ at weekly intervals by 2.55 mg/day (target dose = 10 mg/day; not to exceed 20 mg/day).
- IM (Adults): Oral olanzapine dose = 10 mg/day 210 mg every 2 wk or 410 mg every 4 wk for the first 8 wk, then 150 mg every 2 wk or 300 mg every 4 wk as maintenance therapy; Oral olanzapine dose = 15 mg/day 300 mg every 2 wk for the first 8 wk, then 210 mg every 2 wk or 405 mg every 4 wk as maintenance therapy; Oral olanzapine dose = 20 mg/day 300 mg every 2 wk for the first 8 wk, then 300 mg every 2 wk as maintenance therapy.
- IM (Adults Debilitated or Nonsmoking Female Patients
65 yr): Initiate therapy at 150 mg every 4 wk.
Acute Manic or Mixed Episodes Associated with Bipolar I Disorder
- PO (Adults): 1015 mg/day initially (use 10 mg/day when used with lithium or valproate); may ↑ every 24 hr by 5 mg/day (not to exceed 20 mg/day).
- PO (Children 1317 yr): 2.55 mg/day initially; may ↑ by 2.55 mg/day (target dose = 10 mg/day; not to exceed 20 mg/day).
Maintenance Treatment of Bipolar I Disorder
- PO (Adults): Continue at the dose required to maintain symptom remission (usual dose: 520 mg/day).
- PO (Children 1317 yr): Continue at the lowest dose required to maintain symptom remission.
Acute Agitation due to Schizophrenia or Bipolar I Mania
- IM (Adults): 10 mg, may repeat in 2 hr, then 4 hr later.
- IM (Adults >65 yr): Initiate therapy with 5 mg.
Depressive Episodes Associated with Bipolar I Disorder
- PO (Adults): 5 mg/day with fluoxetine 20 mg/day (both given in evening); may ↑ fluoxetine dose up to 50 mg/day and olanzapine dose up to 12.5 mg/day.
- PO (Children 1017 yr): 20 mg/day with olanzapine 2.5 mg/day (both given in evening); may ↑ fluoxetine dose up to 50 mg/day and olanzapine dose up to 12 mg/day.
Treatment-Resistant Depression
- PO (Adults): 5 mg/day with fluoxetine 20 mg/day (both given in evening); may ↑ fluoxetine dose up to 50 mg/day and olanzapine dose up to 20 mg/day.
ZyPREXA, ZyPREXA Relprevv, ZyPREXA Zydis
Therapeutic Classification: antipsychotics
Pharmacologic Classification: thienobenzodiazepines