Clinical utility of the risperidone formulations in the management of schizophrenia

Abstract

Risperidone is one of the early second-generation antipsychotics that came into the limelight in the early 1990s. Both the oral and long-acting injectable formulations have been subject to numerous studies to assess their safety, efficacy, and tolerability. Risperidone is currently one of the most widely prescribed antipsychotic medications, used for both acute and long-term maintenance in schizophrenia. Risperidone has better efficacy in the treatment of psychotic symptoms than placebo and possibly many first-generation antipsychotics. Risperidone fares better than placebo and first-generation antipsychotics in the treatment of negative symptoms. Risperidone’s long acting injectable preparation has been well tolerated and is often useful in patients with medication nonadherence. Risperidone has a higher risk of hyperprolactinemia comparable to first-generation antipsychotics (FGAs) but fares better than many second-generation antipsychotics with regards to metabolic side effects. In this article, we briefly review the recent literature exploring the role of risperidone formulations in schizophrenia, discuss clinical usage, and highlight the controversies and challenges associated with its use.

Changes in prolactin levels and sexual function in young psychotic patients after switching from long-acting injectable risperidone to paliperidone palmitate

“…It has been suggested that hyperprolactinaemia in patients treated with risperidone-LAI or PP is driven by 9-hydroxyrisperidone and the higher occupancy of D2 at the pituitary level compared with the striatum (Madaan et al, 2011). It has been suggested that hyperprolactinaemia in patients treated with risperidone-LAI or PP is driven by 9-hydroxyrisperidone and the higher occupancy of D2 at the pituitary level compared with the striatum (Madaan et al, 2011).…”

Blonanserin vs risperidone in Japanese patients with schizophrenia: A post hoc analysis of a phase 3, 8‐week, multicenter, double‐blind, randomized controlled study

“…The range is in line with the current Japanese label of risperidone recommending 2‐6 mg/d and the US FDA current label not recommending doses above 6 mg/d, although both labels also allow a higher dose of risperidone. Several clinical studies indicated that risperidone at a dose higher than 6 mg/d might induce side effects such as extrapyramidal symptoms . The dose was increased by 4 mg/d for blonanserin and 1 mg/d for risperidone if the change from baseline in the Brief Psychiatric Rating Scale (BPRS, see Section 2.4) total score at the study visit was −5 or higher and no major safety concern was observed.…”

“…Several clinical studies indicated that risperidone at a dose higher than 6 mg/d might induce side effects such as extrapyramidal symptoms. 8,9 The dose was increased by 4 mg/d for blonanserin and 1 mg/d for risperidone if the change from baseline in the Brief Psychiatric Rating Scale (BPRS, see Section 2.4) total score at the study visit was −5 or higher and no major safety concern was observed. If a major safety concern was found, a dose reduction was allowed.…”

Prolactin regulates TRPV1, TRPA1, and TRPM8 in sensory neurons in a sex-dependent manner: Contribution of prolactin receptor to inflammatory pain

“…Overall, we demonstrate a sex-dependent regulation of peripheral inflammatory hyperalgesia by the PRL system. prolactin receptor; transient receptor potential V1; transient receptor potential A1; transient receptor potential M8; female; inflammation; pain MANY HUMAN CHRONIC INFLAMMATORY conditions are associated with hyperprolactinemia, and this increase in prolactin (PRL) levels can lead to serious health issues related to cancer, infertility, inflammatory diseases, and body weight (11,42,48,73). Human inflammatory conditions with increased PRL serum levels include the severe form of progressive systemic sclerosis (34, 69), the active phase of systemic lupus erythematosus (37, 74), rheumatoid arthritis (44), polymyalgia rheumatica (68), and autoimmune thyroid diseases (26).…”