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: 5.88). 02/2007; 106(2):283-8. DOI: 10.1097/00000542-200702000-00016
Source: PubMed


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
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    • "The main study finding was that recovery to a TOF ratio of 0.9 was significantly faster after administration of sugammadex 2 mg/kg compared with neostigmine 50 μg/kg (geometric mean 1.6 min vs 9.1 min, respectively). Geometric mean time to a TOF ratio of 0.9 in Caucasian subjects was 1.4 min and 6.7 min for sugammadex and neostigmine, respectively, confirming the efficacy of sugammadex 2 mg/kg for reversal of moderate rocuronium NMB in Caucasian subjects as demonstrated in previous studies [3,11,12]. Furthermore, equivalence of efficacy of sugammadex (i.e. time to recovery of the TOF ratio to 0.9) was demonstrated between Chinese and Caucasian subjects. "
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    ABSTRACT: This study compared efficacy and safety of the selective relaxant binding agent sugammadex (2 mg/kg) with neostigmine (50 μg/kg) for neuromuscular blockade (NMB) reversal in Chinese and Caucasian subjects. This was a randomized, active-controlled, multicenter, safety-assessor-blinded study (NCT00825812) in American Society of Anesthesiologists Class 1-3 subjects undergoing surgery with propofol anesthesia. Rocuronium 0.6 mg/kg was administered for endotracheal intubation, with 0.1–0.2 mg/kg maintenance doses given as required. NMB was monitored using TOF-Watch® SX. At second twitch reappearance, after last rocuronium dose, subjects received sugammadex 2 mg/kg or neostigmine 50 μg/kg plus atropine 10–20 μg/kg, according to randomization. Primary efficacy variable was time from sugammadex/neostigmine to recovery of the train-of-four (TOF) ratio to 0.9. Overall, 230 Chinese subjects (sugammadex, n = 119, neostigmine, n = 111); and 59 Caucasian subjects (sugammadex, n = 29, neostigmine, n = 30) had evaluable data. Geometric mean (95% CI) time to recovery to TOF ratio 0.9 was 1.6 (1.5–1.7) min with sugammadex vs 9.1 (8.0–10.3) min with neostigmine in Chinese subjects. Corresponding times for Caucasian subjects were 1.4 (1.3–1.5) min and 6.7 (5.5–8.0) min, respectively. Sugammadex 2 mg/kg was generally well tolerated, with no serious adverse events reported. There was no residual NMB or recurrence of NMB. Both Chinese and Caucasian subjects recovered from NMB significantly faster after sugammadex 2 mg/kg vs neostigmine 50 μg/kg, with a ~5.7 times (p < 0.0001) faster recovery with sugammadex vs neostigmine in Chinese subjects. Sugammadex was generally well tolerated. Trial registration Identifier: NCT00825812.
    Full-text · Article · Jul 2014 · BMC Anesthesiology
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    • "Although sugammadex was developed to antagonize rocuronium-induced block; it is also effective in reversing 0.1 mg/kg vecuronium-induced block [14]. When given at reappearance of T2, recovery of a 0.9 TOF ratio was obtained in 2.3 min and 1.5 min following 2.0 and 4.0 mg/kg respectively [15]. "
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    ABSTRACT: Sugammadex is belonging to a new class of drugs: the selective relaxant binding agents. Sugammadex can reverse residual paralysis by encapsulating free circulating non depolarizing muscle relaxants. The mains advantages of sugammadex when compared with conventional anticholinesterase agents are a much faster recovery time and the unique ability, for the first time, to reverse rapidly and efficiently deep levels of neuromuscular blockade. However it only works for reversal of rocuronium or vecuronium-induced neuromuscular blockade. When administered 3 min after rocuronium the use of a large dose (16 mg/kg) can even reverse rocuronium significantly faster than the spontaneous recovery after succinylcholine.
    Full-text · Article · Dec 2013 · Korean journal of anesthesiology
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    • "There is no dose recommendation for the immediate reversal of a vecuronium-induced neuromuscular block. The sugammadex doses to reverse a deep (posttetanic count [PTC] of 1–2) or a moderate (TOF count >2) vecuronium-induced neuromuscular block are the same as for rocuronium; however, due to the lower affinity, the speed of recovery from the neuromuscular block is slightly slower (3.3 minutes after 4 mg/kg sugammadex, at a PTC of 1–2,16 and 2.3 min after 2 mg/kg, at a TOF count >217). "
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    ABSTRACT: Sugammadex is the first clinical representative of a new class of drugs called selective relaxant binding agents. It has revolutionized the way anesthesiologists think about drug reversal. Sugammadex selectively binds rocuronium or vecuronium, thereby reversing their neuromuscular blocking action. Due to its 1:1 binding of rocuronium or vecuronium, it is able to reverse any depth of neuromuscular block. So far, it has been approved for use in adult patients and for pediatric patients over 2 years. Since its approval in Europe, Japan, and Australia, further insight on its use in special patient populations and specific diseases have become available. Due to its pharmacodynamic profile, sugammadex, in combination with rocuronium, may have the potential to displace succinylcholine as the "gold standard" muscle relaxant for rapid sequence induction. The use of rocuronium or vecuronium, with the potential of reverse of their action with sugammadex, seems to be safe in patients with impaired neuromuscular transmission, ie, neuromuscular diseases, including myasthenia gravis. Data from long-term use of sugammadex is not yet available. Evidence suggesting an economic advantage of using sugammadex and justifying its relatively high cost for an anesthesia-related drug, is missing.
    Full-text · Article · Sep 2013 · Core Evidence
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