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Pharmaceutics
Volume 15
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10.3390/pharmaceutics15010230
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Article

A Universal Pharmacological-Based List of Drugs with Anticholinergic Activity

by
Marta Lavrador
1,2,
Ana C. Cabral
1,2,
Manuel T. Veríssimo
2,3,
Fernando Fernandez-Llimos
4,5,
Isabel V. Figueiredo
1,2 and
M. Margarida Castel-Branco
1,2,*
1
Pharmacology and Pharmaceutical Care Laboratory, Faculty of Pharmacy, University of Coimbra, 3000-548 Coimbra, Portugal
2
Coimbra Institute for Clinical and Biomedical Research (iCBR), 3000-548 Coimbra, Portugal
3
Faculty of Medicine, University of Coimbra, 3000-548 Coimbra, Portugal
4
Laboratory of Pharmacology, Department of Drug Sciences, Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal
5
Center for Health Technology and Services Research (CINTESIS), University of Porto, 4200-450 Porto, Portugal
*
Author to whom correspondence should be addressed.
Pharmaceutics 2023, 15(1), 230; https://doi.org/10.3390/pharmaceutics15010230
Submission received: 28 November 2022 / Revised: 1 January 2023 / Accepted: 7 January 2023 / Published: 10 January 2023
(This article belongs to the Section Pharmacokinetics and Pharmacodynamics)
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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.
Keywords: aged; anticholinergic burden; receptors; muscarinic; cholinergic antagonists; clinical practice aged; anticholinergic burden; receptors; muscarinic; cholinergic antagonists; clinical practice
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MDPI and ACS Style

Lavrador, M.; Cabral, A.C.; Veríssimo, M.T.; Fernandez-Llimos, F.; Figueiredo, I.V.; Castel-Branco, M.M. A Universal Pharmacological-Based List of Drugs with Anticholinergic Activity. Pharmaceutics 2023, 15, 230. https://doi.org/10.3390/pharmaceutics15010230

AMA Style

Lavrador M, Cabral AC, Veríssimo MT, Fernandez-Llimos F, Figueiredo IV, Castel-Branco MM. A Universal Pharmacological-Based List of Drugs with Anticholinergic Activity. Pharmaceutics. 2023; 15(1):230. https://doi.org/10.3390/pharmaceutics15010230

Chicago/Turabian Style

Lavrador, Marta, Ana C. Cabral, Manuel T. Veríssimo, Fernando Fernandez-Llimos, Isabel V. Figueiredo, and M. Margarida Castel-Branco. 2023. "A Universal Pharmacological-Based List of Drugs with Anticholinergic Activity" Pharmaceutics 15, no. 1: 230. https://doi.org/10.3390/pharmaceutics15010230

APA Style

Lavrador, M., Cabral, A. C., Veríssimo, M. T., Fernandez-Llimos, F., Figueiredo, I. V., & Castel-Branco, M. M. (2023). A Universal Pharmacological-Based List of Drugs with Anticholinergic Activity. Pharmaceutics, 15(1), 230. https://doi.org/10.3390/pharmaceutics15010230

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