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. 2022 Nov 3;12(12):2705–2714. doi: 10.1007/s13555-022-00838-3

Table 2.

Clinical properties of topical anticholinergics

Agent Clinical properties Absorption Long-term use concern Trials assessing concern
Glycopyrronium tosylate (GT) Permanently charged quaternary amine therefore minimizes oral bioavailability and blood–brain barrier permeability. [35] The diffusion of the active drug is insufficient for the induction of the systemic response, which significantly reduces the possible adverse reactions. [9] In particular, CNS-related adverse effects [36] Minimal None A safety analysis showed no phototoxic, genotoxic, or carcinogenic effect [9]
Oxybutynin Tertiary amine structure provides ability to cross the blood–brain barrier given its lipophilic nature [34] Moderate Neurotoxicity (dementia should be considered) None
Sofpironium bromide Similar in chemical structure to glycopyrronium bromide. It has a high binding affinity for the M3 cholinergic receptor at the local site of administration, but is hydrolyzed at the ester linkage to less active metabolites upon entry into blood [31] Minimal Unknown Phase II and III studies completed, currently approved in Japan
Umeclidinium (UMEC) Long-acting muscarinic antagonist with minimal ability to cross the blood–brain barrier Minimal Unknown Limited studies, one phase II and III study