Sugammadex: a cyclodextrin to reverse neuromuscular blockade in anaesthesia.

Abstract

BACKGROUND:

Neuromuscular blocking agents are used to provide relaxation and immobility during surgery. To avoid residual paralysis after anaesthesia, reversal of blockade is commonly accomplished with anticholinesterase agents but these drugs have cardiovascular side effects and incomplete effectiveness. Sugammadex is a cyclodextrin that binds rocuronium and chemically similar neuromuscular blocking drugs.

OBJECTIVE:

Published data on the effectiveness of sugammadex as a reversal agent were examined.

METHODS:

Peer-reviewed articles on residual postoperative paralysis and sugammadex (ORG 25969) were analysed.

RESULTS:

Rocuronium-sugammadex complexes are formed and excreted via the kidney. The dissociation constant of the reaction is estimated at 0.1 microM. Sugammadex produces more rapid reversal of rocuronium- and vecuronium-induced blockade than current reversal agents. The dose required depends directly on intensity of blockade. To date, there appear to be few side effects. Inadequate dosage may lead to reparalysis.

CONCLUSION:

More data are needed, especially in patients with renal failure and those who require neuromuscular blockade again soon after receiving sugammadex.

• Authors: François Donati
• Journal: Expert opinion on pharmacotherapy (Expert Opin Pharmacother) Vol. 9 Issue 8 Pg. 1375-86 (Jun 2008) ISSN: 1744-7666 [Electronic] England
• PMID: 18473711 (Publication Type: Journal Article, Review)

Chemical References

• Androstanols
• Cholinesterase Inhibitors
• Neuromuscular Nondepolarizing Agents
• gamma-Cyclodextrins
• Sugammadex
• Rocuronium

Topics

• Androstanols (antagonists & inhibitors, pharmacokinetics, therapeutic use)
• Anesthesia, General (methods)
• Animals
• Cholinesterase Inhibitors (adverse effects, pharmacology)
• Dose-Response Relationship, Drug
• Humans
• Neuromuscular Blockade (methods)
• Neuromuscular Nondepolarizing Agents (antagonists & inhibitors, pharmacokinetics, therapeutic use)
• Rocuronium
• Sugammadex
• gamma-Cyclodextrins (administration & dosage, adverse effects, pharmacokinetics)