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NERVOUS SYSTEM › PSYCHOLEPTICS › ANTIPSYCHOTICS › Diazepines, oxazepines, thiazepines and oxepines
olanzapine
N05AH03
Forms & Strengths
- Tablet: 2.5 mg, 5 mg, 7.5 mg, 10 mg, 15 mg, 20 mg
- Orally Disintegrating Tablet (Zyprexa Zydis): 5 mg, 10 mg, 15 mg, 20 mg
- Intramuscular Solution (Reconstitution): 10 mg/vial
- Extended-Release Intramuscular Suspension (Zyprexa Relprevv): 210 mg, 305 mg, 405 mg
Adult Dosing
- Schizophrenia: Oral: Initial 5-10 mg once daily; target 10 mg/day within several days; range 10-20 mg/day.
- Bipolar Mania (Monotherapy): Oral: Initial 10-15 mg once daily; range 5-20 mg/day.
- Bipolar Mania (Adjunct to Lithium or Valproate): Oral: Initial 10 mg once daily; range 5-20 mg/day.
- Agitation associated with Schizophrenia or Bipolar Mania: IM: 10 mg (5 mg or 7.5 mg may be considered); max 30 mg/24 hours.
Pediatric Dosing
- Schizophrenia (Adolescents 13-17 years): Oral: Initial 2.5-5 mg once daily; target 10 mg/day; range 2.5-20 mg/day.
- Bipolar I Mania (Adolescents 13-17 years): Oral: Initial 2.5-5 mg once daily; target 10 mg/day; range 2.5-20 mg/day.
Indications
- Treatment of schizophrenia
- Acute treatment of manic or mixed episodes associated with bipolar I disorder
- Maintenance treatment of bipolar I disorder
- Adjunctive treatment of major depressive disorder with-resistant psychotic features
- Acute agitation associated with schizophrenia and bipolar mania
Mechanism of Action
- Second-generation (atypical) antipsychotic
- High affinity antagonism at serotonin 5-HT2A, 5-HT2C, and 5-HT6 receptors
- Dopamine D1, D2, D3, and D4 receptor antagonism
- Antagonism at histamine H1 receptors
- Antagonism at muscarinic M1, M2, M3, and M4 receptors
Contraindications
- Known hypersensitivity to olanzapine or any component of the formulation
- Patients with documented risk of narrow-angle glaucoma
Adverse Reactions
- Weight gain (frequent and often significant)
- Somnolence and sedation
- Metabolic syndrome (hyperglycemia, new-onset or exacerbation of type 2 diabetes mellitus, dyslipidemia)
- Orthostatic hypotension
- Extrapyramidal symptoms (akathisia, Parkinsonism, tardive dyskinesia)
- Elevated liver transaminases (ALT/AST)
- Hyperprolactinemia
Drug Interactions
- CYP1A2 inducers (e.g., carbamazepine, tobacco smoke) decrease olanzapine plasma concentrations.
- CYP1A2 inhibitors (e.g., fluvoxamine) increase olanzapine plasma concentrations.
- CNS depressants (e.g., alcohol, opioids, benzodiazepines) increase risk of profound sedation, respiratory depression, and hypotension.
- Antihypertensive agents: Increased risk of hypotension.
- Levodopa and dopamine agonists: Olanzapine may antagonize their effects.
Curated Content: Needs Vetting Before Put to Clinical Use