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利培酮 ISM 作为精神分裂症临床治疗的新选择:一项叙述性综述。

Risperidone ISM as a New Option in the Clinical Management of Schizophrenia: A Narrative Review.

机构信息

Department of Biomedical Sciences, Alcalá University. Alcalá de Henares. , C/ Serrano Galvache 42, 9ºC , 28033, Madrid, Spain.

出版信息

Adv Ther. 2022 Nov;39(11):4875-4891. doi: 10.1007/s12325-022-02299-8. Epub 2022 Sep 1.

DOI:10.1007/s12325-022-02299-8
PMID:36048404
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9525356/
Abstract

Antipsychotics are the cornerstone of schizophrenia treatment. Lack of treatment adherence encouraged the development of injectable long-acting antipsychotics. However, second-generation or atypical antipsychotics require a loading dose at the start of treatment and eventually oral supplementation to achieve therapeutic plasma levels. This review discusses the evidence emerging from studies evaluating the pharmacokinetics, efficacy and safety of the intramuscular formulation of risperidone based on in situ microparticles (ISM). ISM® technology applied to risperidone allows therapeutic levels of the active moiety to be achieved within 2 h of intramuscular administration without the need for loading doses or oral supplementation, leading to a constant release over the whole dosing period. Risperidone ISM showed significant antipsychotic efficacy versus placebo in the Positive and Negative Syndrome Scale (PANSS) total score (p < 0.0001) and on the subscales of positive symptoms after 8 days, negative symptoms in 8 weeks, and general psychopathology during the 12 weeks of treatment. The improvement was also statistically significant (p < 0.0001) against placebo in the Clinical Global Impressions-Severity of Illness scale (CGI-S) score at the end of the treatment. Risperidone ISM was generally well tolerated and the most frequently reported adverse events were similar to those observed with other risperidone formulations. There is clinical evidence that these results are maintained in the long term. In conclusion, four-weekly risperidone ISM (75 mg and 100 mg) is an adequate antipsychotic for treating schizophrenia, both in the short term when an exacerbation has recently occurred and for long-term maintenance, since it provides rapid onset of action and sustained efficacy, as well as being safe and well tolerated.

摘要

抗精神病药是精神分裂症治疗的基石。由于缺乏治疗依从性,促使开发了可注射长效抗精神病药。然而,第二代或非典型抗精神病药在开始治疗时需要负荷剂量,最终需要口服补充以达到治疗性血浆水平。本文综述了评估利培酮原位微颗粒(ISM)肌肉内制剂的药代动力学、疗效和安全性的研究结果。将 ISM®技术应用于利培酮,可以在肌肉内给药后 2 小时内达到治疗水平的活性成分,而无需负荷剂量或口服补充,从而在整个给药期间实现持续释放。利培酮 ISM 在阳性和阴性综合征量表(PANSS)总分(p<0.0001)和阳性症状(第 8 天)、阴性症状(第 8 周)和一般精神病理学(第 12 周)的亚量表上与安慰剂相比,显示出显著的抗精神病疗效。在治疗结束时,临床总体印象-疾病严重程度量表(CGI-S)评分也显著优于安慰剂(p<0.0001)。利培酮 ISM 通常具有良好的耐受性,最常报告的不良反应与其他利培酮制剂观察到的不良反应相似。有临床证据表明,这些结果在长期内得到维持。总之,每周 4 次利培酮 ISM(75mg 和 100mg)是一种有效的抗精神病药物,适用于近期恶化的精神分裂症短期治疗和长期维持治疗,因为它具有快速起效和持续疗效,且安全耐受良好。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba4b/9525356/496277ca42bf/12325_2022_2299_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba4b/9525356/fe4b5ba91985/12325_2022_2299_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba4b/9525356/9c345401d970/12325_2022_2299_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba4b/9525356/496277ca42bf/12325_2022_2299_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba4b/9525356/fe4b5ba91985/12325_2022_2299_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba4b/9525356/9c345401d970/12325_2022_2299_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba4b/9525356/496277ca42bf/12325_2022_2299_Fig3_HTML.jpg

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Neuropsychiatr Dis Treat. 2022 Jan 26;18:111-123. doi: 10.2147/NDT.S326299. eCollection 2022.
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