Long-Acting Injectable Second-Generation Antipsychotics: An Update and Comparison Between Agents

Michael W. Jann, Scott Robert Penzak

Research output: Contribution to journalReview articlepeer-review

36 Scopus citations


Schizophrenia is a chronic medical condition with periods of remission and relapses over a patient’s lifetime. Antipsychotic medications represent the mainstay of treatment for this disease. Long-acting injectable (LAI) formulations of antipsychotics are an attractive alternative to their oral counterparts, as they enhance patient adherence. A number of second-generation antipsychotics (SGAs) are available in LAI formulations. These include paliperidone, aripiprazole, olanzapine, and risperidone. This article reviews the most recently developed and approved of these formulations—aripiprazole monohydrate, aripiprazole lauroxil, and paliperidone palmitate. While all were initially available as once-monthly formulations, a paliperidone palmitate 3-monthly injection formulation has been approved and is the first LAI agent to extend the dosing administration beyond the typical monthly time period. In addition, aripiprazole lauroxil every 6-week and 8-week administration preparations have been developed. LAI preparations of the SGAs have all demonstrated superiority over placebo and are comparable to their oral counterparts in terms of safety and tolerability, if injection site reactions are not taken into account. First-generation antipsychotic LAI preparations (e.g., haloperidol decanoate) have recently been compared with SGA LAI agents, and both formulations demonstrated comparable efficacy with the expected adverse events seen with each drug. Despite their availability, barriers to the use of LAIs remain. Education of both patients and clinicians on the use of LAI formulations and the continued development of these agents are important steps in ensuring these medications are available to the patients they would be most likely to benefit.

Original languageEnglish
Pages (from-to)241-257
Number of pages17
JournalCNS Drugs
Issue number3
StatePublished - 1 Mar 2018


Dive into the research topics of 'Long-Acting Injectable Second-Generation Antipsychotics: An Update and Comparison Between Agents'. Together they form a unique fingerprint.

Cite this