title: Sugammadex: a novel agent for the reversal of neuromuscular blockade.
abstract: To achieve spontaneous ventilation after completion of surgery, the nondepolarizing effects on skeletal muscle relaxation are often reversed by administration of an acetylcholinesterase inhibitor. However, these agents increase acetylcholine at both the neuromuscular junction and the muscarinic receptors. Therefore, coadministration of an anticholinergic agent is required to prevent parasympathetic adverse effects. In addition, a relative pharmacologic ceiling effect is seen with inhibition of acetylcholinesterase, necessitating some recovery of neuromuscular function before an acetylcholinesterase inhibitor is administered. Sugammadex is a new modified gamma-cyclodextrin compound under clinical investigation in the United States. It does not interact with cholinergic mechanisms to elicit reversal. Instead, it is a selective relaxant binding agent and acts by forming a 1:1 complex with steroidal nondepolarizing neuromuscular blockers in the plasma, lowering the effective concentration available at the receptor. Due to its selectivity, sugammadex does not inhibit the effects of nondepolarizing agents of the benzylisoquinolinium class. In contrast to acetylcholinesterase inhibition, sugammadex is effective even when administered during profound blockade, and it does not require coadministration of an anticholinergic agent. It provides a novel mechanism of action for reversal of the neuromuscular block induced by nondepolarizing aminosteroidal agents.
authors.affiliation: Department of Anesthesiology, Mayo Clinic College of Medicine, Rochester, Minnesota 55905, USA. nicholson.wayne@mayo.edu
authors.forename: Wayne T
authors.initials: WT
authors.lastname: Nicholson
authors.forename: Juraj
authors.initials: J
authors.lastname: Sprung
authors.forename: Christopher J
authors.initials: CJ
authors.lastname: Jankowski
mesh_terms: D000732:Androstanols / Q000037:antagonists & inhibitors; D002800:Cholinesterase Inhibitors / Q000008:administration & dosage / Q000627:therapeutic use; D002986:Clinical Trials as Topic; D005260:Female; D006801:Humans; D008297:Male; D009388:Neostigmine / Q000008:administration & dosage / Q000627:therapeutic use; D019148:Neuromuscular Blockade; D009469:Neuromuscular Junction / Q000187:drug effects; D003473:Neuromuscular Nondepolarizing Agents / Q000037:antagonists & inhibitors*; D012121:Respiration, Artificial; D000077123:Rocuronium; D000077122:Sugammadex; D047408:gamma-Cyclodextrins / Q000009:adverse effects / Q000493:pharmacokinetics* / Q000627:therapeutic use
chemical_list: D000732:Androstanols; D002800:Cholinesterase Inhibitors; D003473:Neuromuscular Nondepolarizing Agents; D047408:gamma-Cyclodextrins; D000077122:Sugammadex; D009388:Neostigmine; D000077123:Rocuronium