Paliperidone 3-Month Injection for Treatment of Schizophrenia: A Narrative Review

Abstract

Given the typical age onset of schizophrenia, there are tremendous economic and social impacts that extend beyond the person and their families. One critical determinant of the diseases' impact is the patient's adherence to antipsychotic drug treatment. Approved in 2015 for the treatment of schizophrenia, paliperidone palmitate (Invega Trinza, a 3-month injection, noted as PP3M) is a second-generation long-acting injectable antipsychotic medication. Among the different formulations offered for palmitate paliperidone, including the 1 and 3-month formulations, the longer duration 3-month formulation was better at preventing relapse in schizophrenic patients. To date, different formulations of palmitate paliperidone that have been studied on relapse episodes of schizophrenia include once-daily extended-release oral paliperidone (ORAL paliperidone), once-monthly paliperidone palmitate (PP1M), and once-every-3-months paliperidone palmitate (PP3M). Post-hoc analyses show that patients who were withdrawn from PP1M paliperidone had the least risk of relapse, followed by patients withdrawn from PP3M and patients withdrawn from ORAL paliperidone. PP3M was better at preventing relapse compared to ORAL paliperidone. The results demonstrated that 50% of patients who were withdrawn from ORAL paliperidone, PP1M, or PP3M remained relapse-free for ~2, 6, and 13 months, respectively. Compared to PP1M, PP3M is just as safe and effective and has the added advantage of increased adherence related to a longer dose interval, decreasing the risk of relapse.

Structure-based discovery of an antipsychotic drug, paliperidone, as a modulator of human superoxide dismutase 1: a potential therapeutic target in amyotrophic lateral sclerosis

“…The crystal structure of the complex was refined using the phenix.refine module of the Phenix package (Liebschner et al, 2019). Model building was performed using Coot (Emsley et al, 2010). The X-ray data-collection, scaling and refinement statistics are shown in Table 1.…”

“…Paliperidone is a drug for the treatment of schizophrenia and schizoaffective disorders (Jones et al, 2010). It is a second-generation atypical antipsychotic agent with proposed therapeutic activity mediated through central dopamine type 2 and serotonin type 2 receptor antagonism (Edinoff et al, 2021). A biochemical assay using microscale thermophoresis (MST) confirms that the proposed drug binds to SOD1 with low-micromolar affinity.…”

Comparing Relapse Rates in Real-World Patients with Schizophrenia Who Were Adequately versus Not Adequately Treated with Paliperidone Palmitate Once-Monthly Injections Before Transitioning to Once-Every-3-Months Injections

“…Recent evidence highlights the potential benefits of transitioning from PP1M to PP3M, including improved adherence and persistence, 10 , 11 a lower likelihood of hospitalization, 11 and patient-provider preference for the 3-month formulation. 12 , 13 Optimization of the PP1M dose prior to transitioning to PP3M is essential to prevent relapse or adverse events that may result from doses that are too low or too high, respectively.…”