olanzapine ZYPREXA

Class: Second Generation Antipsychotic/​Thienobenzodiazepine
FDA Indications: Bipolar I Disorder, Schizophrenia, Bipolar Depression (in Combination With Fluoxetine [Symbyax]), Treatment Resistant Depression (in Combination With Fluoxetine [Symbyax])
Off-Label Use: Behavioral Disturbances With Dementia, Impulse Control Disorders, Behavioral Disturbances In Children And Adolescents, Borderline Personality Disorder
Prescribing
Forms: 2.5, 5, 7.5, 10, 15, 20mg tablet; 5, 10, 15, 20mg ODT; 200, 210, 405mg LAI Relprevv; 10 mg/vial IM
Dose Range: 5-20 mg/day
Starting: Initial 5-10 mg qd, ↑ by 5mg/day weekly, max approved dose 20 mg qd however not unheard of to dose up to 30 mg qd in severe treatment-resistant cases
Stopping: Taper 6-8 weeks, rapid d/c can lead to rebound psychosis
Monitoring:

NAMI drug fact sheet

Precautions
Serious Side Effects: , , ,
Conditional Risk of TdP, Drugs to Avoid in Congenital Long QT
Side Effects: sedation/somnolence, dizziness, weight gain, anticholinergic side effects, EPS, dyspepsia, peripheral edema
Pharmacodynamics
1° MOA: 5HT2A–D2 antagonist
Target: Antagonism at:
Pharmacokinetics
t½: 33 (20-50)° TMAX:
Substrate of: 1A2, UGT; 2D6
Inhibits: ∅ ; Induces:
Active Metabolites:
DDIs
Misc
  • - chemical structure similar to clozapine
  • - the "pines" (clozapine, olanzapine, quetiapine, asenapine) all bind much more potently to the 5HT2A receptor than they do to the D2 receptor and also bind to α2 receptors to varying degrees
  • - high metabolic risk compared to others in its class due to its H1 & 5HT2C antagonism
  • - does not often raise prolactin levels
  • - low EPS
Special Populations

Category CGDM may be a problem with all SGAs; may cause extrapyramidal and/or withdrawal symptoms in neonates with third trimester exposure

RID 1-1.6%


All atypicals may increase mortality in elderly patients by 1.7 times greater than placebo.

No dosage adjustment necessary.


Little pharmacokinetic Δ in severe hepatic impairment, though recommend caution and starting at lower doses (5mg) due to its sedation & anticholinergic properties

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Last updated January 22 2018 19:18:05. Disclaimer: This website does not provide medical advice, nor is it a substitute for clinical judgment.