Unlabeled Use:
Absorption: Well absorbed but rapidly metabolized by first-pass effect, resulting in 60% bioavailability. Conventional tablets and orally disintegrating tablets (Zydis) are bioequivalent. IM administration results in significantly higher blood levels (5 times that of oral).
Distribution: Extensively distributed.
Protein Binding: 93%.
Metabolism/Excretion: Highly metabolized (primarily by the CYP1A2 isoenzyme); 7% excreted unchanged in urine.
Half-life: 2154 hr.
Contraindicated in:
Use Cautiously in:
CV: orthostatic hypotension, bradycardia, chest pain, syncope, tachycardia.
Derm: DRUG REACTION WITH EOSINOPHILIA AND SYSTEMIC SYMPTOMS (DRESS), photosensitivity.
EENT: amblyopia, rhinitis, ↑ salivation, pharyngitis.
Endo: galactorrhea, goiter, gynecomastia, hyperglycemia, hyperprolactinemia.
GI: constipation, dry mouth, ↑liver enzymes, abdominal pain, dysphagia, nausea, ↑ thirst.
GU: amenorrhea, ↓ fertility (females), ↓ libido, impotence, urinary incontinence.
Hemat: AGRANULOCYTOSIS, leukopenia, neutropenia.
Metab: weight loss or gain, dyslipidemia, ↑ appetite.
MS: hypertonia, joint pain.
Neuro: tremor , NEUROLEPTIC MALIGNANT SYNDROME, SEIZURES, SUICIDAL THOUGHTS, agitation, delirium, dizziness, headache, restlessness, sedation, weakness, dystonia, falls, insomnia, mood changes, personality disorder, speech impairment, tardive dyskinesia.
Resp: cough, dyspnea.
Misc: aspiration, body temperature dysregulation, fever, flu-like syndrome.
Drug-Drug:
Schizophrenia
65 yr): Initiate therapy at 5 mg/day.
65 yr): Initiate therapy at 150 mg every 4 wk.Acute Manic or Mixed Episodes Associated with Bipolar I Disorder
Maintenance Treatment of Bipolar I Disorder
Acute Agitation due to Schizophrenia or Bipolar I Mania
Depressive Episodes Associated with Bipolar I Disorder
Treatment-Resistant Depression
(Generic available)
NDC Code*