Advances in long-acting injectable antipsychotics: Focus on paliperidone palmitate

Abstract

Long-acting injectable antipsychotics (LAIAs) have emerged as a critical advancement in the treatment of schizophrenia and related psychotic disorders, offering a solution to the common issue of nonadherence associated with oral antipsychotics. Among these, paliperidone palmitate has gained prominence due to its favorable efficacy, safety profile, and flexible dosing options, available in both monthly and 3-month formulations. This review provides a comprehensive examination of the pharmacology, clinical efficacy, safety, and economic implications of paliperidone palmitate, highlighting its advantages over oral antipsychotics and first-generation LAIAs. Paliperidone palmitate exerts its effects through dopamine (D2) and serotonin (5HT2A) receptor antagonism, which helps in managing both the positive and negative symptoms of schizophrenia. Clinical trials and real-world studies demonstrate its effectiveness in reducing relapse rates, preventing hospitalizations, and improving treatment adherence compared to oral formulations. Furthermore, the availability of a 3-month dosing option has further enhanced patient satisfaction by reducing the frequency of administration. Despite its benefits, challenges such as initial loading doses and potential side effects, including weight gain and metabolic disturbances, require careful management. This review also explores the economic benefits of paliperidone palmitate, including its cost-effectiveness in reducing healthcare utilization. Finally, emerging research on its use in early intervention for schizophrenia and potential future advancements in LAIA formulations are discussed. This review underscores the critical role of paliperidone palmitate in enhancing treatment outcomes and advancing the long-term management of schizophrenia.