Atracurium: conception and inception.
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.
D000818:Animals; D001279:Atracurium; D001711:Biotransformation; D006801:Humans; D007546:Isoquinolines / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D009466:Neuromuscular Blocking Agents / Q000138:chemical synthesis*; D013329:Structure-Activity Relationship
D007546:Isoquinolines; D009466:Neuromuscular Blocking Agents; D001279:Atracurium