Paliperidone palmitate three-month depot formulation: a helpful innovation with practical pitfalls

• Published in: Australasian psychiatry : bulletin of the Royal Australian and New Zealand College of Psychiatrists Vol. 26; no. 2; p. 206
• Main Authors: Hope, Judith D, Keks, Nicholas A
• Format: Journal Article
• Language: English
• Published: England 01.04.2018
• Subjects: Antipsychotic Agents - administration & dosage; Antipsychotic Agents - adverse effects; Antipsychotic Agents - pharmacokinetics; Antipsychotic Agents - pharmacology; Delayed-Action Preparations; Humans; Outcome Assessment (Health Care); Paliperidone Palmitate - administration & dosage; Paliperidone Palmitate - adverse effects; Paliperidone Palmitate - pharmacokinetics; Paliperidone Palmitate - pharmacology; Schizophrenia - drug therapy; paliperidone; injectable; antipsychotic; schizophrenia; pharmacotherapy
• DOI: 10.1177/1039856217751986

Paliperidone palmitate is now available as a three-month depot injection. This paper will review the pharmacokinetics, pharmacodynamics, efficacy and tolerability, as well as practical issues and pitfalls for clinicians with this innovative treatment for schizophrenia. The three-month depot formulation of paliperidone for the treatment of schizophrenia is not a new compound. The nanocrystalline structure of the three-month formulation is larger and takes longer to disperse than the one-month formulation, hence its extended depot action. As expected, it is non-inferior to one-month depot paliperidone, and superior to placebo, for the treatment of schizophrenia. The side effect profile of three-month paliperidone is identical to the one-month formulation. The relapse rate on treatment is low, and the median time to relapse after ceasing the drug is 395 days. An understanding of half-life and kinetics is crucial for clinicians using this compound, and the loading strategy is important to ensure effectiveness. There are significant challenges: ensuring timely administration and switching a three-month depot treatment to another antipsychotic may be problematic. Paliperidone palmitate three-month depot injection represents an advance for both convenience and effectiveness in the long term psychopharmacological treatment of schizophrenia.