iloperidone; hoperidone (Fanapt)

Introduction

FDA-approved in 2009

Indications

• treatment of schizophrenia
• depression
• psychosis & agitation in the elderly

Contraindications

• not approved for patients with dementia-related psychosis

Dosage

• usual dose 6-12 mg PO BID
• 4-day titration pack to get to 6 mg BID, then increase by 2 mg BID each day up to 12 mg BID if needed

Pharmacokinetics

• metabolized in the liver by CYP2D6 & CYP3A4

Adverse effects

• most common: dizziness, dry mouth, fatigue, nasal congestion, orthostatic hypotension, drowsiness, tachycardia
• weight gain mid-range for atypical antipsychotics
• sedation about same as risperidone
• tardive dyskinesia,
• seems to cause less restlessness & movement disorders than risperidone or olanzapine
• minimal effects on glucose & lipids
• cardiovascular events, stroke
• sleep disturbance
• hyperglycemia
• hyperprolactinemia
• priapism,
• hyperthermia,
• neuroleptic malgnant syndrome
• QT prolongation
• agranulocytosis
• seizures
• aspiration pneumonia
• cognitive impairment
• black box warning
  • increased risk of hyperglycemia
  • increased risk of cerebrovascular events
  • increased risk of mortality in patients with dementia

• drug adverse effects of antipsychotic agents
• drug adverse effects of atypical antipsychotic agents
• drug adverse effects of psychotropic agents

Drug interactions

• drugs that inhibit CYP2D6 or CYP3A4 may increase levels of iloperidone

• drug interaction(s) of antipsychotics & dopamine receptor agonists
• drug interaction(s) of antipsycotics with benzodiazepines

Mechanism of action

• dopamine receptor anagonist
• alpha-adrenergic receptor anagonist
• serotonin receptor antagonist

More general terms

• atypical antipsychotic agent; second generation antipsychotic

Database

• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=71360