Sugammadex: A novel agent for the reversal of neuromuscular blockade

Wayne T. Nicholson, Juraj Sprung, Christopher J. Jankowski

Research output: Contribution to journalArticle

28 Citations (Scopus)

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 γ-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.

Original languageEnglish (US)
Pages (from-to)1181-1188
Number of pages8
JournalPharmacotherapy
Volume27
Issue number8
DOIs
StatePublished - Aug 2007

Fingerprint

Neuromuscular Blockade
Cholinesterase Inhibitors
Cholinergic Antagonists
Acetylcholinesterase
Cholinergic Agents
Neuromuscular Nondepolarizing Agents
Neuromuscular Blocking Agents
Muscle Relaxation
Neuromuscular Junction
Recovery of Function
Cyclodextrins
Muscarinic Receptors
Ventilation
Skeletal Muscle
Sugammadex

Keywords

  • Cholinesterase inhibitor
  • Cyclodextrin
  • Org 25969
  • Rocuronium
  • Sugammadex

ASJC Scopus subject areas

  • Pharmacology (medical)
  • Pharmacology, Toxicology and Pharmaceutics(all)

Cite this

Sugammadex : A novel agent for the reversal of neuromuscular blockade. / Nicholson, Wayne T.; Sprung, Juraj; Jankowski, Christopher J.

In: Pharmacotherapy, Vol. 27, No. 8, 08.2007, p. 1181-1188.

Research output: Contribution to journalArticle

Nicholson, WT, Sprung, J & Jankowski, CJ 2007, 'Sugammadex: A novel agent for the reversal of neuromuscular blockade', Pharmacotherapy, vol. 27, no. 8, pp. 1181-1188. https://doi.org/10.1592/phco.27.8.1181
Nicholson, Wayne T. ; Sprung, Juraj ; Jankowski, Christopher J. / Sugammadex : A novel agent for the reversal of neuromuscular blockade. In: Pharmacotherapy. 2007 ; Vol. 27, No. 8. pp. 1181-1188.
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