A Universal Pharmacological-Based List of Drugs with Anticholinergic Activity

Abstract

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.

Role of antidepressant receptor antagonism and the development of gestational diabetes: a nested case-control study

“…The antagonistic properties of AD drugs were retrieved from DrugBank Online, PDSP Ki database, and other relevant literature [18][19][20]. The mean pKi from human cloned receptors were used to classify individual ADs as an antagonist (+, ++, and +++), a strongantagonist (+++) and a non-antagonist (-) on each receptor of interest.…”

Cholinergic Antagonists and Behavioral Disturbances in Neurodegenerative Diseases

“…As far as possible, a cholinergic antagonist whose indication is indisputable should be replaced by another molecule of the same class using the anticholinergic load estimation scales. The Anticholinergic Risk Scale [ 99 ] seems to date to have the best correlation with pharmacokinetic parameters [ 23 ]. Moreover, in a situation of overuse, cholinergic antagonist cannot be renewed.…”

“…The distribution of muscarinic receptors across many physiological systems leads to a wide range of peripheral (e.g., dry mouth, dry eyes, urinary retention, constipation, and tachycardia) and central (e.g., cognitive impairment, delirium, and confusion) adverse effects. Affinity for muscarinic receptors varies from one therapeutic class to another, and from one molecule to another within the same therapeutic class [ 23 ].…”

Análise das escalas de fármacos com atividade anticolinérgica

“…The current trend is to develop scales with an international perspective and covering more drugs, as was the case with CALS 1 . An important strategy to improve the predictive power of anticholinergic action scales is to include in their structure drugs whose antagonistic action on muscarinic receptors has been proved 22 .…”

“…In 2023, a universal list of drugs with anticholinergic activity was published by Lavrador et al, based on the available documentation regarding the activity of drugs on muscarinic receptors and their ability to cross the blood-brain barrier 22 . The universal list does not present the anticholinergic action scores; therefore, it is not considered a scale.…”