Zyprexa Fact Sheet
Eli Lilly; patent expiration 2011.
Schizophrenia, both short-term and maintenance treatment.
- Bipolar disorder, including manic or mixed episodes, and maintenance monotherapy. Approval specifically includes both monotherapy and combination treatment with lithium or Depakote.
- IM formulation indicated for treatment of agitation associated with schizophrenia and bipolar mania.
- Off-label use for a variety of disorders, including treatment-resistant depression, anxiety disorders, PTSD, general impulsivity/agitation, and insomnia.
D2 and 5HT 2 receptor antagonist.
- Oral tablets at 2.5 mg, 5 mg, 10 mg, 15 mg, and 20 mg
- Orally disintegrating “Zyprexa Zydis” tablets in 5 mg, 10 mg, 15 mg and 20 mg
- Intramuscular injectible Zyprexa in 10 mg vials
- Start most patients at 5-10 mg QD, may need to increase up to 30 mg per day or more.
- Recommended IM dose for treatment of acute agitation is 10 mg.
BLACK BOX WARNING: All atypicals may increase mortality in elderly patients by 1.7 times greater than placebo.
- Most common are somnolence, dry mouth, constipation, and weight gain.
- Weight gain: Substantial; 10-30 pounds weight gain is common.
- EPS: Akithisia and parkinsonism in 10-20% of patients, depending on dosing.
- Glucose/Lipids: Associated with new onset diabetes and hyperlipidemia; worse in this regard than all atypicals except for clozapine.
- EKG: No concerns.
- Prolactin level: Transient increase only.
- Pregnancy Category C.
Does not affect hepatic enzymes and thus does not affect metabolism of other drugs.
- However, the metabolism of Zyprexa is affected in the following ways:
- Smoking and Tegretol increase clearance by 40%-50%, decreasing effective dose.
- Luvox decreases clearance by 50-70%, increasing blood levels of Zyprexa.
- Half-life 1-2 days, greater in elderly patients.
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