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Sections

History and Discovery | Structure–Activity Relations and Pharmacological Profile | Pharmacokinetics and Disposition | Indications and Efficacy | Side Effects and Toxicology | Conclusion | References

Excerpt

Iloperidone was approved by the U.S. Food and Drug Administration (FDA) in 2009 for the treatment of schizophrenia. It meets the now generally appreciated profile of second-generation antipsychotics (SGAs), in that it has a complex pharmacology (with a predilection for dopamine and serotonin antagonism) and little propensity for extrapyramidal side effects (EPS), as well as efficacy against key symptoms of schizophrenia, as shown in placebo-controlled clinical trials (Rado and Janicak 2010; Weiden 2012). Iloperidone’s efficacy has been demonstrated at a dosage range of 12–24 mg/day, with no clear advantage evident at higher dosages. To minimize the risk of dizziness and postural hypotension consequent to iloperidone’s antagonism of noradrenergic α1 receptors, it is recommended that the drug be initiated and titrated upward with caution. Clinical experience with iloperidone is accruing, as is comparative information for iloperidone in relation to other SGAs (Potkin et al. 2013; Rado and Janicak 2014; Tarazi and Stahl 2012). Additional clinical trials of iloperidone are ongoing (see www.clinicaltrials.gov).

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