CNS Drugs

, Volume 32, Issue 3, pp 241–257 | Cite as

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

  • Michael W. Jann
  • Scott R. Penzak
Review Article


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.


Compliance with Ethical Standards


No funds from any sources were used to assist with the preparation of this review article.

Conflict of interest

Michael W. Jann is on Janssen’s Speaker Bureau. Scott R. Penzak has no conflicts of interest.


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Copyright information

© Springer International Publishing AG, part of Springer Nature 2018

Authors and Affiliations

  1. 1.Department of PharmacotherapyUniversity of North Texas System College of Pharmacy (UNTSCP), University of North Texas Health Science Center (UNTHSC)Fort WorthUSA

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