A Universal Pharmacological-Based List of Drugs with Anticholinergic Activity

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.

Automated summary

This study aimed to provide a comprehensive list of drugs with documented affinity for muscarinic receptors, in order to address the gaps in anticholinergic burden tools. A literature review and database search were conducted to identify these tools and evaluate the drugs included in them. A universal list of 133 drugs with anticholinergic activity, categorized by their affinity for different subtypes of muscarinic receptors and their ability to cross the blood-brain barrier, was developed. The proportion of drugs with confirmed antagonism varied among the tools, highlighting the need for further validation in different clinical settings.