Sugammadex: A revolutionary drug in neuromuscular pharmacology

Kusha Nag, Dewan Roshan Singh, Akshaya N Shetti, Hemanth Kumar, T Sivashanmugam, S Parthasarathy, Kusha Nag, Dewan Roshan Singh, Akshaya N Shetti, Hemanth Kumar, T Sivashanmugam, S Parthasarathy

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.

Keywords: Encapsulation; residual paralysis; rocuronium; selective relaxant binding agent; sugammadex.

Conflict of interest statement

Conflict of Interest: None declared.

Figures

Figure 1
Figure 1
Structure of sugammadex

References

    1. Kovac AL. Sugammadex: The first selective binding reversal agent for neuromuscular block. J Clin Anesth. 2009;21:444–53.
    1. Hemmerling TM, Zaouter C, Geldner G, Nauheimer D. Sugammadex: A short review and clinical recommendations for the cardiac anesthesiologist. Ann Card Anaesth. 2010;13:206–16.
    1. Bhaskar SB. Emergence from anaesthesia: Have we got it all smoothened out? Indian J Anaesth. 2013;57:1–3.
    1. Lee C, Jahr JS, Candiotti KA, Warriner B, Zornow MH, Naguib M. Reversal of profound neuromuscular block by sugammadex administered three minutes after rocuronium: A comparison with spontaneous recovery from succinylcholine. Anesthesiology. 2009;110:1020–5.
    1. Gijsenbergh F, Ramael S, Houwing N, van Iersel T. First human exposure of Org 25969, a novel agent to reverse the action of rocuronium bromide. Anesthesiology. 2005;103:695–703.
    1. Nicholson WT, Sprung J, Jankowski CJ. Sugammadex: A novel agent for the reversal of neuromuscular blockade. Pharmacotherapy. 2007;27:1181–8.
    1. Cameron KS, Fletcher L, Clark JK, Zhang MQ, Orbons LPM. Chemical chelation as a novel method of NMB reversal characterization of the Org 25969 NMB complex: 15. 2001;18:99.
    1. Zhang MQ. Drug specific cyclodextrins: The future of rapid neuro-muscular block reversal? Drugs Future. 2003;28:347–54.
    1. Naguib M. Sugammadex: Another milestone in clinical neuromuscular pharmacology. Anesth Analg. 2007;104:575–81.
    1. Bom A, Bradley M, Cameron K, Clark JK, Van Egmond J, Feilden H, et al. A novel concept of reversing neuromuscular block: Chemical encapsulation of rocuronium bromide by a cyclodextrin-based synthetic host. Angew Chem Int Ed Engl. 2002;41:266–70.
    1. Adam JM, Bennett DJ, Bom A, Clark JK, Feilden H, Hutchinson EJ, et al. Cyclodextrin-derived host molecules as reversal agents for the neuromuscular blocker rocuronium bromide: Synthesis and structure-activity relationships. J Med Chem. 2002;45:1806–16.
    1. Tarver GJ, Grove SJ, Buchanan K, Bom A, Cooke A, Rutherford SJ, et al. 2-O-substituted cyclodextrins as reversal agents for the neuromuscular blocker rocuronium bromide. Bioorg Med Chem. 2002;10:1819–27.
    1. Cameron KS, Clark JK, Cooper A, Fielding L, Palin R, Rutherford SJ, et al. Modified gamma-cyclodextrins and their rocuronium complexes. Org Lett. 2002;4:3403–6.
    1. Epemolu O, Bom A, Hope F, Mason R. Reversal of neuromuscular blockade and simultaneous increase in plasma rocuronium concentration after the intravenous infusion of the novel reversal agent Org 25969. Anesthesiology. 2003;99:632–7.
    1. Sparr HJ, Vermeyen KM, Beaufort AM, Rietbergen H, Proost JH, Saldien V, et al. Early reversal of profound rocuronium-induced neuromuscular blockade by sugammadex in a randomized multicenter study: Efficacy, safety, and pharmacokinetics. Anesthesiology. 2007;106:935–43.
    1. Yang LP, Keam SJ. Sugammadex: A review of its use in anaesthetic practice. Drugs. 2009;69:919–42.
    1. Schering-Plough; 2008. Jul 29, BRIDION(R) (Sugammadex) Injection-First and Only Selective Relaxant Binding Agent-Approved in European Union.
    1. Sacan O, White PF, Tufanogullari B, Klein K. Sugammadex reversal of rocuronium-induced neuromuscular blockade: A comparison with neostigmine-glycopyrrolate and edrophonium-atropine. Anesth Analg. 2007;104:569–74.
    1. Kovac AL. Sugammadex: A selective relaxant binding agent for neuromuscular block reversal. Formulary. 2009;44:13–21.
    1. Schering-Plough (press release); 2008. Aug 01, US FDA Issues Action Letter for Sugammadex.
    1. Naguib M, Mohamed, Brull, Sorin J. Update on neuromuscular pharmacology. Curr Opin Anaesthesiol. 2009;26:874–84.
    1. Staals LM, Snoeck MM, Driessen JJ, Flockton EA, Heeringa M, Hunter JM. Multicentre, parallel-group, comparative trial evaluating the efficacy and safety of sugammadex in patients with end-stage renal failure or normal renal function. Br J Anaesth. 2008;101:492–7.
    1. Dahl V, Pendeville PE, Hollmann MW, Heier T, Abels EA, Blobner M. Safety and efficacy of sugammadex for the reversal of rocuronium-induced neuromuscular blockade in cardiac patients undergoing noncardiac surgery. Eur J Anaesthesiol. 2009;26:874–84.
    1. Hemmerling TM, Russo G, Bracco D. Neuromuscular blockade in cardiac surgery: An update for clinicians. Ann Card Anaesth. 2008;11:80–90.
    1. Jones RK, Caldwell JE, Brull SJ, Soto RG. Reversal of profound rocuronium-induced blockade with sugammadex: A randomized comparison with neostigmine. Anesthesiology. 2008;109:816–24.
    1. Chambers D, Paulden M, Paton F, Heirs M, Duffy S, Hunter JM, et al. Sugammadex for reversal of neuromuscular block after rapid sequence intubation: A systematic review and economic assessment. Br J Anaesth. 2010;105:568–75.
    1. Bajaj P. Reversal by sugammadex. Indian J Anaesth. 2009;53:399–400.
    1. Groudine SB, Soto R, Lien C, Drover D, Roberts K. A randomized, dose-finding, phase II study of the selective relaxant binding drug, Sugammadex, capable of safely reversing profound rocuronium-induced neuromuscular block. Anesth Analg. 2007;104:555–62.
    1. Abrishami A, Ho J, Wong J, Yin L, Chung F. Cochrane corner: Sugammadex, a selective reversal medication for preventing postoperative residual neuromuscular blockade. Anesth Analg. 2010;110:1239.
    1. Miller RD. Sugammadex: An opportunity to change the practice of anesthesiology? Anesth Analg. 2007;104:477–8.
    1. Suy K, Morias K, Cammu G, Hans P, van Duijnhoven WG, Heeringa M, et al. Effective reversal of moderate rocuronium- or vecuronium-induced neuromuscular block with sugammadex, a selective relaxant binding agent. Anesthesiology. 2007;106:283–8.
    1. Eleveld DJ, Kuizenga K, Proost JH, Wierda JM. A temporary decrease in twitch response during reversal of rocuronium-induced muscle relaxation with a small dose of sugammadex. Anesth Analg. 2007;104:582–4.
    1. Ledowski T, Hillyard S, O’Dea B, Archer R, Vilas-Boas F, Kyle B. Introduction of sugammadex as standard reversal agent: Impact on the incidence of residual neuromuscular blockade and postoperative patient outcome. Indian J Anaesth. 2013;57:46–51.
    1. Tayal G, Kundra S, Grewal A. Sugammadex-New neuromuscular block reversal. J Anaesth Clin Pharmacol. 2008;24:211–4.
    1. Naguib M, Magboul MM. Adverse effects of neuromuscular blockers and their antagonists. Drug Saf. 1998;18:99–116.
    1. Duvaldestin P, Kuizenga K, Saldien V, Claudius C, Servin F, Klein J, et al. A randomized, dose-response study of sugammadex given for the reversal of deep rocuronium- or vecuronium-induced neuromuscular blockade under sevoflurane anesthesia. Anesth Analg. 2010;110:74–82.

Source: PubMed

3
Prenumerera