Bristol-Myers Squibb; patent expiration 2014.
Bipolar disorder, manic and mixed episodes.
Partial agonist at the D2 and 5HT 1A receptors, and full antagonist at the 5HT 2A receptor (vs. other atypicals which are D2 and 5 HT 2 antagonists).
Oral tablets at 5 mg, 10 mg, 15 mg, 20 mg, and 30 mg
Orally disintegrating “Abilify Discmelt” tablets in 10 mg and 15 mg strengths
Oral solution (1 mg/mL) in 150 ml bottles
Start most patients at 10 mg QD to prevent agitation/akathisia, gradually increase to target dose of 15-30 mg QD.
Can be dosed once daily because of long half life.
No dosage adjustments required in liver or renal impairment, elderly, or in smokers.
BLACK BOX WARNING: All atypicals may increase mortality in elderly patients by 1.7 times greater than placebo.
Most common are headache, anxiety/agitation/akithisia, insomnia, and nausea. Anecdotally, at 30 mg dose sedation becomes more common.
EPS: Minimal risk.
Weight gain: Minimal. In clinical trials in schizophrenia there was an average weight gain of about 1.5 pounds over 4-6 weeks, but no weight gain in bipolar patients over 3 weeks.
Glucose/Lipids: Minimal to no elevation.
EKG: No significant changes; QT interval showed a slight shortening (of no clinical significance).
Prolactin level: No elevation.
Pregnancy Category C.
Does not itself inhibit liver enzymes, so Abilify does not significantly affect the metabolism of other drugs.
Metabolized by CYP2D6 and CYP3A4, so Tegretol will decrease effective dose, while Prozac and Paxil will increase levels. Also, poor metabolizers of CYP2D6 (8% of Caucasians) will have a 60% higher effective dose.
Long half life of 4 days.