Development and potential clinical impairment of ultra-short-acting neuromuscular blocking agents

Br J Anaesth. 2011 Dec:107 Suppl 1:i60-71. doi: 10.1093/bja/aer341.

Abstract

Developing a non-depolarizing neuromuscular blocking agent that, like succinylcholine, has a rapid onset and a short duration of effect remains a goal of ongoing research. While rocuronium fills a portion of this need, the large doses required for rapid intubation render it a much longer-acting neuromuscular blocking agent. Postoperative residual neuromuscular block (NMB) is an increasingly recognized complication of non-depolarizing neuromuscular blocking agents. This occurs because of dosing choices for neuromuscular blocking agents and anticholinesterases as well as insensitivity of typically used monitors of depth of NMB. While antagonism of NMB is necessary with partial recovery, it is unnecessary with more complete recovery. Even when monitoring with an accelerograph, reversal of NMB is complicated. In addition to the pharmacodynamics of the individual neuromuscular blocking agents, factors such as timing of anticholinesterase administration, dose of anticholinesterase, concomitant medications, electrolyte abnormalities, and hepatic or renal disease can influence the degree of reversal. Sugammadex works differently than anticholinesterases and, when administered in appropriate doses, can reverse even profound block induced with vecuronium or rocuronium. Two new fumarate neuromuscular blocking agents have a rapid onset of effect and can be reversed at any time by administration of cysteine, which could significantly reduce the risk of postoperative residual NMB.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Androstanols / pharmacokinetics
  • Anesthesia Recovery Period
  • Cholinesterase Inhibitors / pharmacology
  • Cysteine / pharmacology
  • Dose-Response Relationship, Drug
  • Humans
  • Isoquinolines / pharmacokinetics
  • Neuromuscular Blocking Agents / pharmacokinetics*
  • Postoperative Complications / chemically induced
  • Postoperative Complications / prevention & control
  • Rocuronium
  • Sugammadex
  • Time Factors
  • Vecuronium Bromide / pharmacokinetics
  • gamma-Cyclodextrins / pharmacology

Substances

  • Androstanols
  • CW 002
  • Cholinesterase Inhibitors
  • Isoquinolines
  • Neuromuscular Blocking Agents
  • gamma-Cyclodextrins
  • Sugammadex
  • Vecuronium Bromide
  • Cysteine
  • gantacurium
  • Rocuronium