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 |