Effective reversal of moderate rocuronium- or vecuronium-induced neuromuscular block with sugammadex, a selective relaxant binding agent

University of Liège, Luik, Walloon, Belgium
Anesthesiology (Impact Factor: 6.17). 02/2007; 106(2):283-8. DOI: 10.1097/00000542-200702000-00016
Source: PubMed

ABSTRACT Sugammadex rapidly reverses rocuronium-induced neuromuscular block. This study explored the dose-response relation of sugammadex given as a reversal agent at reappearance of the second muscle twitch after rocuronium- and vecuronium-induced block. A secondary objective was to investigate the safety of single doses of sugammadex.
In this two-center, phase II, dose-finding study, 80 patients (age >or= 18 yr, American Society of Anesthesiologists physical status I or II, surgery >or= 60 min requiring muscle relaxation for intubation) were randomly assigned to receive rocuronium (0.60 mg/kg) or vecuronium (0.10 mg/kg). Sugammadex or placebo was administered at reappearance of the second muscle twitch. The primary efficacy endpoint was time from starting sugammadex administration until recovery of the train-of-four ratio to 0.9.
Compared with placebo, sugammadex produced dose-dependent decreases in mean time to recovery for all train-of-four ratios in the rocuronium and vecuronium groups. The mean time for recovery of the train-of-four ratio to 0.9 in the rocuronium group was 31.8 min after placebo compared with 3.7 and 1.1 min after 0.5 and 4.0 mg/kg sugammadex, respectively. The mean time for recovery of the train-of-four ratio to 0.9 in the vecuronium group was 48.8 min after placebo, compared with 2.5 and 1.4 min after 1.0 and 8.0 mg/kg sugammadex, respectively. Sugammadex was well tolerated.
Sugammadex rapidly reversed rocuronium- or vecuronium-induced neuromuscular block at reappearance of the second muscle twitch and was well tolerated. A dose-response relation was observed with sugammadex for reversal of both rocuronium- and vecuronium-induced neuromuscular block.

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Available from: Ignace Demeyer, Jul 14, 2015
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    • "Few adverse effects have been attributed to sugammadex. One study reported abdominal discomfort as " defi nitely related " to study drug (Suy et al 2007). Movement after sugammadex was observed in several studies which may be expected with rapid restoration of motor function and lighter anesthetic levels towards the conclusion of surgery (Sorgenfrei et al 2006; de Boer et al 2007). "
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    ABSTRACT: Summary One of the elements of triad anesthesia is myorelaxation. It is induced by the muscle relaxing agents. In majo- rity of cases of general anesthesia non-depolarizing block inducing agents are administered. The occurrence of the non-depolarizing block is caused by binding of the muscle relaxant to the nicotine receptors in postsynaptic membrane and competition with acetylcholine. Relaxants that belong to this group also bind to the presynaptic receptors. Even a small dose of muscle relaxant bound to presynaptic receptors inhibits acetylcholine release from the presynaptic part vesicle in response to the tetanus stimulation. Binding of nondepolarizing agents to presynaptic receptors plays a leading role in the occurrence of Post-Operative Residual Curarisation phenomenon (PORC), since administration of cholinesterase inhibitors (at the end of anesthesia) - does not affect these receptors at all, thus it does not prevent the PORC. The drug that can "extract" a nondepolarizing muscle relaxation agent (from the aminosteroid group) from the complex with both pre- and postsynaptic receptors, is cyclodextrin (Sugammadex). After its administration, neuromuscular transmission is fully restored. The dose of Sugammadex administered in order to stop the neuromuscular block depends on depth of the blockade. The authors have presented observations on administration of sugammadex in several patients undergoing urgent or elective surgical procedures - attempting to categorize indication for the administration of, needless to say, quite an expensive drug. Indications for elective administration of sugammadex would be: severe patient's general condition, extreme age bracket, morbid obesity, muscle relaxants overdose, too rapid end of the surgical procedure, neuromuscular diseases, prolonged time of anesthesia. Urgent indications for administering of sugammadex, the authors considered the lack of restoration of neuromuscular transmission in spite of going out of the timeframe of the muscle relaxant action and the need for immediate reversal of neuromuscular block. Anestezjologia i Ratownictwo 2009; 3: 440-454.
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