section name header

Pronunciation

eye-loe-PER-i-done

Classifications

Therapeutic Classification: antipsychotics

Pharmacologic Classification: benzisoxazoles

Indications

BEERS REMS


Action

  • May act by antagonizing dopamine and serotonin in the CNS.
Therapeutic effects:
  • Decreased symptoms of schizophrenia or bipolar mania.

Pharmacokinetics

Absorption: Well absorbed (96%) following oral administration.

Distribution: Unknown.

Metabolism/Excretion: Extensively metabolized by the liver, primarily by the CYP3A4 and CYP2D6 isoenzymes. The CYP2D6 enzyme system exhibits genetic polymorphism (7–10% of Caucasians and 3–8% of Black/African Americans are considered poor metabolizers [PM]). Two major metabolites (P88 and P95) may be partially responsible for pharmacologic activity. 58% excreted in urine as metabolites in extensive metabolizers (EM) and 45% in PM; 20% eliminated in feces in EM and 22.1% in PM.

Half-Life: EMs: iloperidone—18 hr, P88—26 hr, P95—23 hr; PMs: iloperidone—33 hr, P88—37 hr, P95—31 hr.

Time/Action Profile

(antipsychotic effect)

ROUTEONSETPEAKDURATION
PO2–4 wk2–4 hrunknown



Blood level.



Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects

CV: orthostatic hypotension, tachycardia, palpitations, QT interval prolongation

EENT: nasal congestion, intraoperative floppy iris syndrome

Endo: hyperglycemia, hyperprolactinemia

GI: dry mouth, nausea, abdominal discomfort, diarrhea

GU: priapism, urinary incontinence

Metab: weight gain, dyslipidemia, weight loss

MS: bone density, musculoskeletal stiffness

Neuro: dizziness, drowsiness, fatigue, agitation, cognitive impairment, delusions, extrapyramidal disorders, NEUROLEPTIC MALIGNANT SYNDROME, restlessness, tardive dyskinesia

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS AND ANGIOEDEMA)

Interactions

Drug-drug:

Route/Dosage

Schizophrenia

Acute Manic or Mixed Episodes Associated With Bipolar I Disorder

Availability

(Generic available)

Assessment

Lab Test Considerations:

Implementation

Patient/Family Teaching

Evaluation/Desired Outcomes

US Brand Names

Fanapt