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.