Neuromuscular transmission: new concepts and agents.
Sugammadex is the first selective relaxant binding agent which was originally designed to reverse the steroidal NMB drug rocuronium. The results of recent studies demonstrate that sugammadex is effective for reversal of rocuronium and vecuronium-induced neuromuscular block without apparent side-effects. This is in contrast to the currently available cholinesterase inhibitors used to reverse neuromuscular block and which are even ineffective against profound neuromuscular block and have a number of undesirable side-effects. Sugammadex-rocuronium complexes are highly hydrophilic and it has been demonstrated that sugammadex is excreted in a rapid and dose-dependent manner in urine, resulting in a complete elimination from the body. The ability of sugammadex to reverse rocuronium and vecuronium-induced neuromuscular block may have major implications for routine anesthetic practice. Once sugammadex becomes commercially available, anesthesiologists will be capable of maintaining the desired depth of neuromuscular block at any time, thereby assuring optimal surgical conditions. The mechanism by which sugammadex encapsulates rocuronium and vecuronium appears to be superior to currently used neuromuscular block reversal strategies in terms of speed, efficacy and side effects. In this article, clinical studies of sugammadex are discussed.
de Boer
Hans D
HD
Department of Anesthesiology, Radboud University Medical Center Nijmegen, Nijmegen, The Netherlands. HD.de.boer@mzh.nl
D000732:Androstanols / Q000037:antagonists & inhibitors*; D000762:Anesthesia Recovery Period; D002626:Chemistry, Pharmaceutical; D002800:Cholinesterase Inhibitors / Q000009:adverse effects / Q000627:therapeutic use; D004305:Dose-Response Relationship, Drug; D016903:Drug Monitoring; D006801:Humans; D008657:Metabolic Clearance Rate; D016343:Monitoring, Intraoperative; D018727:Muscarinic Antagonists / Q000627:therapeutic use; D019148:Neuromuscular Blockade / Q000009:adverse effects / Q000379:methods; D009469:Neuromuscular Junction / Q000187:drug effects*; D003473:Neuromuscular Nondepolarizing Agents / Q000037:antagonists & inhibitors*; D018579:Patient Selection; D000077123:Rocuronium; D012449:Safety; D000077122:Sugammadex; D009435:Synaptic Transmission / Q000187:drug effects*; D016896:Treatment Outcome; D014673:Vecuronium Bromide / Q000037:antagonists & inhibitors*; D047408:gamma-Cyclodextrins / Q000378:metabolism / Q000494:pharmacology / Q000627:therapeutic use*
D000732:Androstanols; D002800:Cholinesterase Inhibitors; D018727:Muscarinic Antagonists; D003473:Neuromuscular Nondepolarizing Agents; D047408:gamma-Cyclodextrins; D000077122:Sugammadex; D014673:Vecuronium Bromide; D000077123:Rocuronium