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抗胆碱能负担与老年人抗胆碱能不良反应的关系:其预测不良结局的药理学基础。

Association between anticholinergic burden and anticholinergic adverse outcomes in the elderly: Pharmacological basis of their predictive value for adverse outcomes.

机构信息

University of Coimbra, Pharmacology and Pharmaceutical Care Laboratory, Faculty of Pharmacy, Pólo das Ciências da Saúde, Azinhaga de Santa Comba, 3000-548 Coimbra, Portugal; Coimbra Institute for Clinical and Biomedical Research (iCBR), Pólo das Ciências da Saúde, Azinhaga de Santa Comba, 3000-548 Coimbra, Portugal.

University of Coimbra, Pharmacology and Pharmaceutical Care Laboratory, Faculty of Pharmacy, Pólo das Ciências da Saúde, Azinhaga de Santa Comba, 3000-548 Coimbra, Portugal.

出版信息

Pharmacol Res. 2021 Jan;163:105306. doi: 10.1016/j.phrs.2020.105306. Epub 2020 Nov 25.

Abstract

The use of anticholinergic drugs and other drugs with anticholinergic activity is highly prevalent in older people. Cumulative anticholinergic effects, known as anticholinergic burden, are associated with important peripheral and central adverse effects and outcomes. Several methods have been developed to quantify anticholinergic burden and to estimate the risk of adverse anticholinergic effects. Serum anticholinergic activity (SAA) and anticholinergic burden scoring systems are the most commonly used methods to predict the occurrence of important negative outcomes. These tools could guide clinicians in making more rational prescriptions to enhance patient safety, especially in older people. However, the literature has reported conflicting results about the predictive ability of these tools. The majority of these instruments ignore relevant pharmacologic aspects such as the doses used, differential muscarinic receptor subtype affinities, and blood-brain barrier permeability. To increase the clinical relevance of these tools, mechanistic and clinical pharmacology should collaborate. This narrative review describes the rational and pharmacological basis of anticholinergic burden tools and provides insight about their predictive value for adverse outcomes.

摘要

抗胆碱能药物和其他具有抗胆碱能活性的药物在老年人中广泛使用。累积的抗胆碱能效应,即抗胆碱能负担,与重要的外周和中枢不良反应和结局有关。已经开发了几种方法来量化抗胆碱能负担并估计不良抗胆碱能作用的风险。血清抗胆碱能活性(SAA)和抗胆碱能负担评分系统是最常用的预测重要不良结局发生的方法。这些工具可以指导临床医生制定更合理的处方,以提高患者安全性,尤其是在老年人中。然而,文献报道了这些工具的预测能力存在矛盾的结果。这些工具中的大多数都忽略了相关的药理学方面,如使用的剂量、不同的毒蕈碱受体亚型亲和力和血脑屏障通透性。为了提高这些工具的临床相关性,机制和临床药理学应该合作。本叙述性综述描述了抗胆碱能负担工具的合理和药理学基础,并提供了关于它们对不良结局预测价值的见解。

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