Neuromuscular Block and Reversal
Article information
J Korean Med Assoc. 2007;50(12):1072-1080
Publication date (electronic) : 2007 January 20
doi :
https://doi.org/10.5124/jkma.2007.50.12.1072
Abstract
Abstract
The Griffith and Johnson's report of the successful use of curare in 1942 brought a revolution in anesthetic care. The only depolarizing agent still in use is succinylcholine due to its rapid onset of action and rapid recovery. However, its use is limited by serious side effects (hyperkalemia, malignant hyperthermia, arrhythmia, etc). New non-depolarizing neuromuscular blocking agents have been studied to replace succinylcholine, which are still at a preclinical level. Rocuronium is an aminosteroid compound and has an intermediate duration of action, but the onset is shorter. A new method of reversing neuromuscular blockade has been advocated by the introduction of a cyclodextrin, sugammadex (Org 25969), which is still at the investigational stage in humans. It has a high affinity for rocuronium, with which it forms a complex. Sugammadex has a lower affinity for other steroidal neuromuscular blocking agents such as vecuronium and pancuronium, and does not bind benzylisoquinoline-type neuromuscular blocking agents. The ability to produce a rapid return of twitch height even at deep levels of paralysis and the lack of side effects make this compound a promising new agent for anesthesia.
Structure of sugammadex, a synthetic γ-cyclodextrin.
Complex formation of sugammadex and rocuronium as obtained by X-ray diffraction.
Train-of-four tracing from one volunteer. The blue line represents the height of the twitch, and the dashed red line is the value of the train-of-four ratio. The volunteer received 0.6 mg/kg rocuronium (Roc) followed by placebo at 3 min (A) in one treatment period, followed by 8 mg/kg Org 25969 in another treatment period (B). No recurarization was observed in the 90 min.
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