Messer Thomas, Bernardo Miquel, Anta Lourdes, Martínez-González Javier
Danuviusklinik GmbH, Pfaffenhofen an der Ilm, Klinik für Psychiatrie, Psychotherapie und Psychosomatik, Akademisches Lehrkrankenhaus der Technischen Universität München, München, Germany.
Barcelona Clinic Schizophrenia Unit, Hospital Clínic de Barcelona, Departament de Medicina, Institut de Neurociències (UBNeuro), Universitat de Barcelona (UB), Institut d'Investigacions Biomèdiques August Pi I Sunyer (IDIBAPS), CIBERSAM, ISCIII, Barcelona, Spain.
Ther Adv Psychopharmacol. 2024 Oct 4;14:20451253241280046. doi: 10.1177/20451253241280046. eCollection 2024.
One of the most important challenges in the management of patients with schizophrenia is to ensure adherence to antipsychotic treatment. The contribution of long-acting injectables (LAI) is undeniable in this matter, but there are still some unmet medical needs not covered by these drugs (e.g. quick onset of action for patients with acute exacerbation of schizophrenia). This article summarises the pharmacokinetics, efficacy and safety of Risperidone ISM ( microparticles). The aim of this review is to provide information about the potential uses of this new LAI formulation of risperidone for the treatment of schizophrenia, contextualising and diving into the published evidence. Risperidone ISM shows a rapid release which allows achieving within 12 h risperidone active moiety levels similar to those observed in the steady-state for oral risperidone treatment, achieving a mean average concentration of 38.63 ng/mL. The plasma concentration of active moiety achieved by Risperidone ISM comes with a predictable dopamine D2 receptor occupancy above 65% throughout the 28-day dosing period, which is accepted as a threshold for the efficacy of the antipsychotic treatment. This can be associated with the positive efficacy findings throughout its clinical development. In the short term, it provides an early and progressive reduction of symptoms in adult patients with acute exacerbation of schizophrenia without the need for loading doses or oral risperidone supplementation, which could contribute to reinforcing the therapeutic alliance between the patient and the psychiatrist. In addition, long-term treatment was effective, safe and well tolerated regardless of the initial disease severity or whether patients were previously treated with Risperidone ISM during an acute exacerbation or switched from stable doses of oral risperidone. Improvement and maintenance of personal and social functioning and health-related quality of life were observed in each setting, respectively. All these findings endorse Risperidone ISM as a useful and valuable treatment for the acute and maintenance management of patients with schizophrenia.
精神分裂症患者管理中最重要的挑战之一是确保患者坚持抗精神病药物治疗。长效注射剂（LAI）在这方面的作用不可否认，但这些药物仍存在一些未满足的医疗需求（例如，精神分裂症急性加重患者的起效迅速）。本文总结了利培酮ISM（微粒）的药代动力学、疗效和安全性。本综述的目的是提供关于这种新型利培酮长效注射剂在精神分裂症治疗中的潜在用途的信息，并结合并深入探讨已发表的证据。利培酮ISM显示出快速释放，在12小时内可使利培酮活性部分水平达到与口服利培酮治疗稳态时相似的水平，平均浓度为38.63 ng/mL。在整个28天的给药期内，利培酮ISM达到的活性部分血浆浓度伴随着可预测的多巴胺D2受体占有率高于65%，这被认为是抗精神病治疗疗效的阈值。这可能与整个临床开发过程中的阳性疗效结果相关。在短期内，它可使精神分裂症急性加重的成年患者早期且逐渐减轻症状，无需负荷剂量或补充口服利培酮，这有助于加强患者与精神科医生之间的治疗联盟。此外，无论初始疾病严重程度如何，也无论患者在急性加重期之前是否接受过利培酮ISM治疗或是否从稳定剂量的口服利培酮转换而来，长期治疗都是有效、安全且耐受性良好的。在每种情况下，分别观察到个人和社会功能以及与健康相关的生活质量得到改善和维持。所有这些发现都支持利培酮ISM作为精神分裂症患者急性和维持治疗的一种有用且有价值的治疗方法。
