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      Sugammadex: A revolutionary drug in neuromuscular pharmacology

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          Abstract

          Sugammadex (ORG 25969) is a unique neuromuscular reversal drug; a novel cyclodextrin, the first in a new class of selective relaxant binding agents, which reverse neuromuscular blockade (NMB) with the aminosteroid non-depolarizing muscle relaxants rocuronium and vecuronium. Sugammadex can reverse moderate or deep NMB. The clinical use of sugammadex promises to eliminate many of the shortcomings in current anesthetic practice with regard to antagonism of rocuronium and other aminosteroid muscle relaxants.

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          Sugammadex: another milestone in clinical neuromuscular pharmacology.

          Mohamed Naguib (2007)
          Sugammadex is a revolutionary investigational reversal drug currently undergoing Phase III testing whose introduction into clinical practice may change the face of clinical neuromuscular pharmacology. A modified gamma-cyclodextrin, sugammadex exerts its effect by forming very tight water-soluble complexes at a 1:1 ratio with steroidal neuromuscular blocking drugs (rocuronium > vecuronium > pancuronium). During rocuronium-induced neuromuscular blockade, the IV administration of sugammadex creates a concentration gradient favoring the movement of rocuronium molecules from the neuromuscular junction back into the plasma, which results in a fast recovery of neuromuscular function. Sugammadex is biologically inactive, does not bind to plasma proteins, and appears to be safe and well tolerated. Additionally, it has no effect on acetylcholinesterase or any receptor system in the body. The compound's efficacy as an antagonist does not appear to rely on renal excretion of the cyclodextrin-relaxant complex. Human and animal studies have demonstrated that sugammadex can reverse very deep neuromuscular blockade induced by rocuronium without muscle weakness. Its future clinical use should decrease the incidence of postoperative muscle weakness, and thus contribute to increased patient safety. Sugammadex will also facilitate the use of rocuronium for rapid sequence induction of anesthesia by providing a faster onset-offset profile than that seen with 1.0 mg/kg succinylcholine. Furthermore, no additional anticholinesterase or anticholinergic drugs would be needed for antagonism of residual neuromuscular blockade, which would mean the end of the cardiovascular and other side effects of these compounds. The clinical use of sugammadex promises to eliminate many of the shortcomings in our current practice with regard to the antagonism of rocuronium and possibly other steroidal neuromuscular blockers.
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            A novel concept of reversing neuromuscular block: chemical encapsulation of rocuronium bromide by a cyclodextrin-based synthetic host.

            Douglas Rees, Jan van Lanschot, K. Clark … (2002)
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              First human exposure of Org 25969, a novel agent to reverse the action of rocuronium bromide.

              Francois Gijsenbergh, Natalie Houwing, Thijs van Montfort … (2005)
              Acetylcholinesterase inhibitors are widely used for the reversal of neuromuscular blocking agents. However, acetylcholinesterase inhibitors have several side effects and are not effective during profound block. Org 25969 is a modified gamma-cyclodextrin that encapsulates the neuromuscular blocking agent, rocuronium bromide (Esmeron/Zemuron, NV Organon, Oss, The Netherlands), forming a tightly bound complex with an association constant of approximately 10 m. Chemical encapsulation of rocuronium promotes dissociation of rocuronium from the acetylcholine receptor, thereby reversing the neuromuscular block without the side effects associated with acetylcholinesterase inhibitors. Twenty-nine healthy male volunteers were enrolled to investigate the safety, pharmacokinetics, and efficacy of Org 25969. In part 1, Org 25969 or placebo was administered to 19 subjects during one to three treatment periods each. In part 2, a further 10 subjects received general anesthesia on two separate occasions, using an intubating dose of 0.6 mg/kg rocuronium. Three minutes after rocuronium administration, Org 25969 or placebo was given in random order. Six doses of 0.1-8.0 mg/kg Org 25969 were evaluated. Neuromuscular block was measured using an acceleromyograph, the TOF-Watch-SX (NV Organon, Oss, The Netherlands). All adverse events related to Org 25969 treatment were of limited duration and mild intensity, except for a period of paresthesia, seen in one patient receiving 8 mg/kg Org 25969, which was of moderate intensity. No adverse events required any treatment, and all subjects recovered from them. When 8 mg/kg Org 25969 was given, the train-of-four ratio returned to 0.9 within 2 min after its administration. No signs of recurarization were observed. Org 25969 was both well tolerated and effective in reversing neuromuscular block induced by rocuronium in 29 human volunteers.
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                Author and article information

                Journal
                Journal ID (nlm-ta): Anesth Essays Res
                Journal ID (iso-abbrev): Anesth Essays Res
                Journal ID (publisher-id): AER
                Title: Anesthesia, Essays and Researches
                Publisher: Medknow Publications & Media Pvt Ltd (India )
                ISSN (Print): 0259-1162
                ISSN (Electronic): 2229-7685
                Publication date (Print): Sep-Dec 2013
                Volume: 7
                Issue: 3
                Pages: 302-306
                Affiliations
                [1]Department of Anaesthesiology and Critical Care, Mahatma Gandhi Medical College, Pillaiyarkuppam, Puducherry, India
                [1 ]Department of Anaesthesiology, Krishna Institute of Medical Sciences, Karad, Maharashtra, India
                Author notes
                Corresponding author: Dr. Dewan Roshan Singh, Department of Anaesthesiology and Critical Care, Mahatma Gandhi Medical College, Pillaiyarkuppam, Puducherry - 607 402, India. E-mail: droshansingh@ 123456yahoo.com
                Article
                Publisher ID: AER-7-302
                DOI: 10.4103/0259-1162.123211
                PMC ID: 4173552
                PubMed ID: 25885973
                SO-VID: 134fa219-ebf3-467a-b127-744107168199
                Copyright © Copyright: © Anesthesia: Essays and Researches
                License:

                This is an open-access article distributed under the terms of the Creative Commons Attribution-Noncommercial-Share Alike 3.0 Unported, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

                History
                Categories
                Subject: Review Article

                Keywords: encapsulation,residual paralysis,rocuronium,selective relaxant binding agent,sugammadex
                Data availability:
                Keywords: encapsulation, residual paralysis, rocuronium, selective relaxant binding agent, sugammadex

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