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非典型抗精神病药物的治疗药物监测

Therapeutic drug monitoring of atypical antipsychotics.

作者信息

Urban Anna Emilia, Cubała Wiesław Jerzy

机构信息

Klinika Psychiatrii Dorosłych Gdańskiego Uniwersytetu Medycznego.

出版信息

Psychiatr Pol. 2017 Dec 30;51(6):1059-1077. doi: 10.12740/PP/65307.

Abstract

The paper presents an overview and analysis of the results of research on therapeutic ranges of concentrations and receptor occupancy, mainly D2 receptors, in the treatment with some atypical antipsychotic drugs. Amisulpride, aripiprazole, clozapine, quetiapine, olanzapine, risperidone, paliperidone, sertindole, and ziprasidone were taken into account. The benefits of therapeutic drug monitoring to optimize the effectiveness of treatment and avoid side effects or toxicity were shown. The safety of patients, with the possibility to use the lowest effective dose, is an undoubted profit of TDM. This helps to avoid overdosing resulting in adverse events (with particular emphasis on extrapyramidal symptoms and seizures).The need and desirability of TDM is due to the inter -and intraindividual differences in the pharmacokinetics of drugs, because only some of them have a close correlation between dose and plasma concentration. The plasma concentration correlates well with the occupancy of D2 receptors. The efficient and safe level is determined at 60-80%. Based on the knowledge of the indications for TDM and therapeutic concentration ranges, amisulpride, clozapine and olanzapine have the highest level of recommendation to use TDM. Therapeutic ranges of plasma concentrations of the analyzed drugs were determined to be 200-320 ng/ml for amisulpride, 150-210 ng/ml for aripiprazole, over 350-500 ng/ml for clozapine, 50-500 ng/ml for quetiapine, 20-40 ng/ml for olanzapine, 20-60 ng/ml for risperidone and paliperidone, 50-100 ng/ml for sertindole and 50-130 ng/ml for ziprasidone.

摘要

本文概述并分析了一些非典型抗精神病药物治疗中浓度治疗范围和受体占有率(主要是D2受体)的研究结果。研究考虑了氨磺必利、阿立哌唑、氯氮平、喹硫平、奥氮平、利培酮、帕利哌酮、舍吲哚和齐拉西酮。研究表明了治疗药物监测对于优化治疗效果以及避免副作用或毒性的益处。患者的安全性以及使用最低有效剂量的可能性是治疗药物监测的一项无疑的益处。这有助于避免因用药过量导致不良事件(尤其强调锥体外系症状和癫痫发作)。治疗药物监测的必要性和可取性归因于药物药代动力学的个体间和个体内差异,因为只有部分药物的剂量与血浆浓度之间存在密切相关性。血浆浓度与D2受体占有率密切相关。有效且安全的水平确定为60 - 80%。基于对治疗药物监测的适应证和治疗浓度范围的了解,氨磺必利、氯氮平和奥氮平在使用治疗药物监测方面的推荐级别最高。所分析药物的血浆浓度治疗范围确定为:氨磺必利200 - 320 ng/ml,阿立哌唑150 - 210 ng/ml,氯氮平超过350 - 500 ng/ml,喹硫平50 - 500 ng/ml,奥氮平20 - 40 ng/ml,利培酮和帕利哌酮20 - 60 ng/ml,舍吲哚50 - 100 ng/ml,齐拉西酮50 - 130 ng/ml。

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