Discovery, development, and clinical application of sugammadex sodium, a selective relaxant binding agent

Abstract

Neuromuscular blockade, induced by neuromuscular blocking agents, has allowed prescribed immobility, improved surgical exposure, optimal airway management conditions, and facilitated mechanical ventilation. However, termination of the effects of neuromuscular blocking agents has, until now, remained limited. A novel cyclodextrin encapsulation process offers improved termination of the paralytic effects of aminosteroidal non-depolarizing neuromuscular blocking agents. Sugammadex sodium is the fi rst in a new class of drug called selective relaxant binding agents. Currently, in clinical trials, sugammadex, a modifi ed gamma cyclodextrin, has shown consistent and rapid termination of neuromuscular blockade with few side effects. The pharmacology of cyclodextrins in general and sugammadex in particular, together with the results of current clinical research are reviewed. The ability of sugammadex to terminate the action of neuromuscular blocking agents by direct encapsulation is compared to the indirect competitive antagonism of their effects by cholinesterase inhibitors. Also discussed are the clinical implications that extend beyond fast, effective reversal, including numerous potential peri-operative benefi ts.

Sugammadex use can decrease the incidence of post-operative urinary retention by avoiding anticholinergics: a retrospective study

“…Anticholinergics such as atropine and glycopyrrolate used to prevent the muscarinic effect of anticholinesterases can block detrusor contractions and cause bladder hypotonia, resulting in urinary retention [9]. On the other hand, sugammadex reverses neuromuscular blockade by selectively binding with a steroidal non-depolarizing neuromuscular blocking agent [12]. In this study, the incidence of POUR and daily residual urine volume from POD 1 to POD 4 were significantly lower in the sugammadex group.…”

“…However, anticholinergics have an inhibitory effect on bladder contraction in the presence of outlet obstruction, an effect achieved primarily by antagonizing postjunctional excitatory muscarinic receptors in the detrusor muscle, thereby increasing the frequency of POUR [1,9,12]. Recently, a selective relaxant binding agent, sugammadex, has been introduced into clinical practice.…”

Double blind Comparison of Rocuronium and Succinylcholine for endotracheal intubation in adult patients for elective surgeries

“…A "can't ventilate, can't intubate" scenario may be prolonged when rocuronium is administered 15,16 .…”

Sugammadex: A neuromuscular blockade agent encapsulator

“…On average, dose-dependent intravenous administration of sugammadex results in full reversal of NMB within three minutes, even in circumstances of deep neuromuscular block, and avoids the possibility of recurarization. 3,27 This makes it a possible rescue strategy in "can't intubate, can't ventilate" scenarios to recover spontaneous ventilation and airway tone. However, analysis of the cause of inability to intubate as well as correct timing of sugammadex administration must be considered.…”