A Comprehensive Monograph on Penequinine (Penehyclidine): Pharmacology, Clinical Evidence, and Therapeutic Potential

Executive Summary

Penequinine, more commonly encountered in its clinical hydrochloride salt form as Penehyclidine (DrugBank ID: DB16287), is a potent anticholinergic agent developed and primarily utilized in China. It represents a significant pharmacological advancement over traditional anticholinergics like atropine. The molecule's therapeutic efficacy is rooted in a dual mechanism of action that combines selective antagonism of muscarinic (M1, M3) and nicotinic acetylcholine receptors with a distinct, secondary anti-inflammatory and cytoprotective function mediated through the negative regulation of the Toll-like receptor 4 (TLR4) and nuclear factor-kappa B (NF-kB) signaling pathways. This unique pharmacological profile translates into a broad spectrum of clinical applications, most notably in the management of acute organophosphorus pesticide poisoning (AOPP), where it has demonstrated marked superiority over atropine in large-scale meta-analyses, significantly reducing mortality, morbidity, and adverse effects.