Lavrador Marta, Cabral Ana C, Veríssimo Manuel T, Fernandez-Llimos Fernando, Figueiredo Isabel V, Castel-Branco M Margarida
Pharmacology and Pharmaceutical Care Laboratory, Faculty of Pharmacy, University of Coimbra, 3000-548 Coimbra, Portugal.
Coimbra Institute for Clinical and Biomedical Research (iCBR), 3000-548 Coimbra, Portugal.
Pharmaceutics. 2023 Jan 10;15(1):230. doi: 10.3390/pharmaceutics15010230.
Anticholinergic burden tools have relevant pharmacological gaps that may explain their limited predictive ability for clinical outcomes. The aim of this study was to provide a universal pharmacological-based list of drugs with their documented affinity for muscarinic receptors. A comprehensive literature review was performed to identify the anticholinergic burden tools. Drugs included in these instruments were searched in four pharmacological databases, and the investigation was supplemented with PubMed. The evidence regarding the potential antagonism of the five muscarinic receptors of each drug was assessed. The proportion of drugs included in the tools with an affinity for muscarinic receptors was evaluated. A universal list of drugs with anticholinergic activity was developed based on their documented affinity for the different subtypes of muscarinic receptors and their ability to cross the blood-brain barrier. A total of 23 tools were identified, including 304 different drugs. Only 48.68%, 47.70%, 48.03%, 43.75%, and 42.76% of the drugs had an affinity to the M1, M2, M3, M4, and M5 receptor, respectively, reported in any pharmacological database. The proportion of drugs with confirmed antagonism varied among the tools (36.8% to 100%). A universal pharmacological-based list of 133 drugs is presented. It should be further validated in different clinical settings.
抗胆碱能负担工具存在相关的药理学空白,这可能解释了它们对临床结局的预测能力有限。本研究的目的是提供一份基于药理学的通用药物清单,列出已记录的它们对毒蕈碱受体的亲和力。进行了全面的文献综述以确定抗胆碱能负担工具。在四个药理学数据库中搜索这些工具中包含的药物,并通过PubMed进行补充调查。评估了每种药物对五种毒蕈碱受体潜在拮抗作用的证据。评估了工具中包含的对毒蕈碱受体有亲和力的药物比例。根据已记录的对毒蕈碱受体不同亚型的亲和力及其穿越血脑屏障的能力,制定了一份具有抗胆碱能活性的通用药物清单。共识别出23种工具,包括304种不同的药物。在任何药理学数据库中报告的药物中,分别只有48.68%、47.70%、48.03%、43.75%和42.76%的药物对M1、M2、M3、M4和M5受体有亲和力。具有确认拮抗作用的药物比例在不同工具中有所不同(36.8%至100%)。列出了一份包含133种药物的基于药理学的通用清单。应在不同临床环境中进一步验证。