An update on the efficacy and safety of iloperidone as a schizophrenia therapy

Expert Opin Pharmacother. 2020 Oct;21(15):1793-1798. doi: 10.1080/14656566.2020.1798931. Epub 2020 Jul 31.

Abstract

Introduction: Schizophrenia has a prevalence of approximately 1% in the general population, with 15.2 per 100,000 persons affected. Iloperidone is a second-generation antipsychotic drug approved for the treatment of schizophrenia in adults. It acts primarily by D2/5HT2a receptor antagonism, with greater affinity for the 5HT2a receptor than for the D2 receptor.

Areas covered: This article discusses iloperidone and aims to provide useful information for clinicians to determine which circumstances would best suit the use of iloperidone to treat schizophrenic patients. In this review, the authors briefly discuss schizophrenia and its treatment, before they discuss properties of iloperidone, its indications, approval process, and adverse effects. Finally, the authors review the specific strengths and weaknesses of the medication.

Expert opinion: Iloperidone would be an attractive option in patients who are particularly prone to EPS, or who are showing prominent negative symptoms, as well as cognitive deficits. Its availability only in an oral formulation makes it a better option for patients with good medication adherence, and though it could be useful in patients prone to weight gain or hepatic dysfunction on other second generation antipsychotics, it should be used with caution in patients prone to side effects related to alpha adrenergic blockade.

Keywords: Iloperidone; antipsychotic; dopamine; serotonin.

Publication types

  • Review

MeSH terms

  • Antipsychotic Agents / administration & dosage
  • Antipsychotic Agents / adverse effects
  • Antipsychotic Agents / therapeutic use*
  • Humans
  • Isoxazoles / administration & dosage
  • Isoxazoles / adverse effects
  • Isoxazoles / therapeutic use*
  • Piperidines / administration & dosage
  • Piperidines / adverse effects
  • Piperidines / therapeutic use*
  • Receptor, Serotonin, 5-HT2A / metabolism
  • Receptors, Dopamine D2 / metabolism
  • Schizophrenia / drug therapy*
  • Schizophrenia / metabolism
  • Weight Gain / drug effects

Substances

  • Antipsychotic Agents
  • DRD2 protein, human
  • HTR2A protein, human
  • Isoxazoles
  • Piperidines
  • Receptor, Serotonin, 5-HT2A
  • Receptors, Dopamine D2
  • iloperidone