Sugammadex: A Development that Modifies the Practice of Anesthesia

Authors

  • Girishkumar Modi Tawam Hospital, Tawam, Abu Dhabi, UAE
  • Vijay Kumar Tawam Hospital, Tawam, Abu Dhabi, UAE
  • Nagaraju Munagala Tawam Hospital, Tawam, Abu Dhabi, UAE

Keywords:

Cyclodextrin, Rocuronium, Selective relaxant binding agent, Neuromuscular blockade, Sugammadex

Abstract

Sugammadex is a modified form of gamma-cyclodextrin that reverses the effects of rocuronium and vecuronium, which are aminosteroid non-depolarizing muscle relaxants (NDMR). It is the first and only reversal agent in the class of selective relaxant binding agents (SRBA) that reverses any depth of neuromuscular blockade without the unwanted muscarinic side effects of neostigmine (bronchospasm, nausea, vomiting, bradycardia, diarrhea, etc.) and anti-muscarinic side effects of glycopyrrolate (dry mouth, palpitations, urinary retention, constipation, etc.). It is an Food and Drug Administration (FDA)-approved agent that is safe for the reversal of neuromuscular block (NMB) caused by rocuronium and is available worldwide. Sugammadex practical use is predicted to alleviate many of the faults in present anesthetic practice regarding the antagonistic effects of rocuronium and other aminosteroid muscle relaxants. Despite being a novel agent in the reversal of NMB, the cost of sugammadex may limit its use as a regular antagonist of neuromuscular-blocking drugs.

References

Hunter JM, Flockton EA. The doughnut and the hole: A new pharmacological concept for anesthetists. Br J Anaesth. 2006; 97(2): 123-126. doi: 10.1093/bja/ael158

Tarver GJ, Grove SJ, Buchanan K, et al. 2-O-substituted cy-clodextrins as reversal agents for the neuromuscular blocker ro-curonium bromide. Bioorg Med Chem. 2002; 10(6): 1819-1827. doi: 10.1016/s0968-0896(02)00026-3

Nicholson WT, Sprung J, Jankowski CJ. Sugammadex: A novel agent for the reversal of neuromuscular blockade. Pharmacotherapy. 2007; 27(8): 1181-1188. doi: 10.1592/phco.27.8.1181

Kim YH. Repeat dosing of rocuronium-sugammadex: Un-predictable. Korean J Anesthesiol. 2014; 67(1): 1-3. doi: 10.4097/ kjae.2014.67.1.1

Adam JM, Bennett DJ, Bom A, et al. Cyclodextrin-derived host molecules as reversal agents for the neuromuscular blocker ro-curonium bromide: Synthesis and structure-activity relationships. J Med Chem. 2002; 45(9): 1806-1816. doi: 10.1021/jm011107f

Nag K, Singh DR, Shetti AN, Kumar H, Sivashanmugam T, Parthasarathy S. Sugammadex: A revolutionary drug in neuromus-cular pharmacology. Anesth Essays Res. 2013; 7(3): 302-306. doi: 10.4103/0259-1162.123211

Naguib M. Sugammadex: Another milestone in clinical neuro-muscular pharmacology. Anesth Analg. 2007; 104(3): 575-581. doi: 10.1213/01.ane.0000244594.63318.fc

Akha AS, Rosa J, Jahr JS, Li A, Kiai K. Sugammadex: Cyclo-dextrins, development of selective binding agents, pharmacology, clinical development, and future directions. Anesthesiol Clin. 2010; 28(4): 691-708. doi: 10.1016/j.anclin.2010.08.014

Peeters P, Passier P, Smeets J, et al. Sugammadex is cleared rap-idly and primarily unchanged via renal excretion. Biopharm Drug Dispos. 2011; 32(3): 159-167. doi: 10.1002/bdd.747

Staals LM, de Boer HD, van Egmond J, et al. Reversal of ro-curonium-induced neuromuscular block by sugammadex is inde-pendent of renal perfusion in anesthetized cats. J Anesth. 2011; 25: 241-246. doi: 10.1007/s00540-010-1090-3

Schaller SJ, Fink H. Sugammadex as a reversal agent for neu-romuscular block: An evidence-based review. Core Evid. 2013; 8: 57-67. doi: 10.2147/CE.S35675

Yang LP, Keam SJ. Sugammadex: A review of its use in anes-thetic practice. Drugs. 2009; 69: 919-942. doi: 10.2165/00003495- 200969070-00008

Bom A, Bradley M, Cameron K, et al. A novel con-cept of reversing neuromuscular block: Chemical encapsu-lation of rocuronium bromide by a cyclodextrin-based syn-thetic host. Angew Chem Int Ed Engl. 2002; 41(2): 266-270. doi: 10.1002/1521-3773(20020118)41:2<265::aid-anie265>3.0.co;2-q

Zhang M-Q. Drug-specific cyclodextrins: The future of rapid neuromuscular block reversal? Drugs Future. 2003; 28(4): 347-354. doi: 10.1358/dof.2003.028.04.742715

Miller RD. Sugammadex: An opportunity to change the prac-tice of anesthesiology? Anesth Analg. 2007; 104(3): 477-478. doi: 10.1213/01.ane.0000255645.64583.e8

Gijsenbergh F, Ramael S, Houwing N, van Iersel T. First hu-man exposure of Org 25969, a novel agent to reverse the action of rocuronium bromide. Anesthesiology. 2005; 103(4): 695-703. doi: 10.1097/00000542-200510000-00007

Vanacker BF, Vermeyen KM, Struys MMR, et al. Reversal of rocuronium-induced neuromuscular block with the novel drug su-gammadex is equally effective under maintenance anesthesia with propofol or sevoflurane. Anesth Analg. 2007; 104(3): 563-568. doi: 10.1213/01.ane.0000231829.29177.8e

Groudine SB, Soto R, Lien C, et al. A randomized, dose-finding 13 Modi G, et al phase II study of the selective relaxant binding drug, sugamma-dex, capable of safely reversing profound rocuronium-induced neuromuscular block. Anesth Analg. 2007; 104(3): 555-562. doi: 10.1213/01.ane.0000260135.46070.c3

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- 884. doi: 10.1097/EJA.0b013e32832c605b

Pühringer FK, Rex C, Sielenkämper AW, et al. Reversal of pro-found, high-dose rocuronium-induced neuromuscular blockade by sugammadex at two different time points: An international, multicenter, randomized, dose-finding, safety assessor-blinded, phase II trial. Anesthesiology. 2008; 109: 188-197. doi: 10.1097/ ALN.0b013e31817f5bc7

Togioka BM, Yanez D, Aziz MF, Higgins JR, Tekkali P, Treggiari MM. Randomised controlled trial of sugammadex or neostigmine for reversal of neuromuscular block on the incidence of pulmo-nary complications in older adults undergoing prolonged surgery. Br J Anaesth. 2020; 124(5): 553-561. doi: 10.1016/j.bja.2020.01.016

Hunter JM, Naguib M. Sugammadex-induced bradycardia, and asystole: How great is the risk? Br J Anaesth. 2018; 121(1): 8-12. doi: 10.1016/j.bja.2018.03.003

Sungur Ulke Z, Yavru A, Camci E, Ozkan B, Toker A, Senturk M. Rocuronium and sugammadex in patients with myasthenia gra-vis undergoing thymectomy. Acta Anaesthesiol Scand. 2013; 57: 745- 748. doi: 10.1111/aas.12123

Saricicek V, Sahin L, Bulbul F, Ucar S, Sahin M. Does rocuroni-um-sugammadex reduce myalgia and headaches after electrocon-vulsive therapy in patients with major depression? J ECT. 2014; 30: 30-34. doi: 10.1097/YCT.0b013e3182972bd2

Lee HY, Jung KT. Advantages, and pitfalls of clinical applica-tion of sugammadex. Anesth Pain Med (Seoul). 2020; 15(3): 259-268. doi: 10.17085/apm.19099

Raghavendra T. Neuromuscular blocking drugs: Discovery and development. J R Soc Med. 2002; 95(7): 363-367. doi: 10.1258/ jrsm.95.7.363

Magorian T, Flannery KB, Miller RD. Comparison of rocuroni-um, succinylcholine, and vecuronium for rapid-sequence induction of anesthesia in adult patients. Anesthesiology. 1993; 79(5): 913-918. doi: 10.1097/00000542-199311000-00007

Harris A, Welliver M, Redfern R, Kalynych NM, McDonough J. Orthopaedic surgery implications of a novel encapsulation pro-cess that improves neuromuscular blockade and reversal. Internet J Orthop Surg. 2007; 7(2): e1-e12.

Reid JE, Breslin DS, Mirakhur RK, et al. Neostigmine antag-onism of rocuronium block during anesthesia with sevoflurane, isoflurane, or propofol. Can J Anesth. 2001; 48(4): 351-355. doi: 10.1007/BF03014962

Mirakhur RK. Sugammadex in clinical practice. Anaesthesia. 2009; 64 Suppl 1: 45-54. doi: 10.1111/j.1365-2044.2008.05870.x

Levano S, Ginz H, Siegemund M, et al. Genotyping the butyr-ylcholinesterase in patients with prolonged neuromuscular block after succinylcholine. Anesthesiology. 2005; 102(3): 531-535. doi: 10.1097/00000542-200503000-00009

White PF, Tufanogullari B, Sacan O, et al. The effect of re-sidual neuromuscular blockade on the speed of reversal with su-gammadex. Anesth Analg. 2009; 108(3): 846-851. doi: 10.1213/ ane.0b013e31818a9932

Donati F. Sugammadex: A cyclodextrin to reverse neuromus-cular blockade in anesthesia. Expert Opin Pharmacother. 2008; 9(8): 1375-1386. doi: 10.1517/14656566.9.8.1375

Mattila K, Toivonen J, Janhunen L, Rosenberg PH, Hynynen Submit your article to this journal | https://openventio.org/submit-manuscript/ Modi G, et al M. Postdischarge symptoms after ambulatory surgery: First-week incidence, intensity, and risk factors. Anesth Analg. 2005; 101(6): 1643-1650. doi: 10.1213/01.ANE.0000184189.79572.28

Donati F. Sugammadex: An opportunity for more thinking or more cookbook medicine? Can J Anesth. 2007; 54(9): 689-695. doi: 10.1007/BF03026865

Zhang B, Menzin J, Tran MH, et al. The potential savings in operating room time associated with the use of sugammadex to reverse selected neuromuscular blocking agents: Findings from a hospital efficiency model [abstract no. PHC9]. Value Health. 2008; 11(3): A244.

National Center for Biotechnology Information. Pub-Chem Substance Record for SID 135262074, Sugammadex [USAN:INN:BAN], Source: ChemIDplus. Website. https://pub-chem.ncbi.nlm.nih.gov/substance/135262074. Retrieved July 18, 2023.

Sugammadex. Website. https://en.wikipedia.org/wiki/Sugam-madex#. Accessed July 9, 2023.

Downloads

Published

2025-05-07

How to Cite

Girishkumar Modi, Vijay Kumar, & Nagaraju Munagala. (2025). Sugammadex: A Development that Modifies the Practice of Anesthesia. Research and Practice in Anesthesiology, 9(1), 8–14. Retrieved from https://openventio.us/index.php/RPA/article/view/1845