Stenlake J B, Waigh R D, Urwin J, Dewar G H, Coker G G
Br J Anaesth. 1983;55 Suppl 1:3S-10S.
The rationale underlying the design of atracurium, a bis-quaternary ammonium neuromuscular blocking agent which incorporates the Hofmann elimination as a novel biodegradation pathway, is described. Destruction in vivo, of the bis-quaternary structure essential for neuromuscular blocking activity, by the combination of Hofmann elimination and a parallel ester hydrolysis leads to innocuous breakdown products that are without neuromuscular or cardiovascular effects and to a time-course of action which is unaffected by the level of plasma esterase activity, renal or hepatic function.
描述了阿曲库铵（一种双季铵神经肌肉阻滞剂）设计背后的基本原理，该药物引入霍夫曼消除反应作为一种新的生物降解途径。通过霍夫曼消除反应与平行的酯水解反应相结合，体内对神经肌肉阻滞活性至关重要的双季铵结构被破坏，产生无害的分解产物，这些产物无神经肌肉或心血管作用，且其作用时间不受血浆酯酶活性、肾功能或肝功能水平的影响。
