Org 25969 (sugammadex), a selective relaxant binding agent for antagonism of prolonged rocuronium-induced neuromuscular block

Br J Anaesth. 2006 Jan;96(1):36-43. doi: 10.1093/bja/aei314.

Abstract

Background: Org 25969 is a cyclodextrin compound designed to reverse a rocuronium-induced neuromuscular block. The aim of this study was to explore the efficacy, dose-response relation and safety of Org 25969 for reversal of a prolonged rocuronium-induced neuromuscular block.

Methods: Thirty anaesthetized adult patients received rocuronium 0.6 mg kg(-1) as an initial dose followed by increments to maintain a deep block at a level of <10 PTCs (post-tetanic counts) recorded every 6 min. Neuromuscular monitoring was carried out using accelerometry, in a train-of-four (TOF) mode using TOF-WatchSX. At recovery of T2, following at least 2 h of neuromuscular block, patients received their randomly assigned dose of 0.5, 1.0, 2.0, 4.0 or 6.0 mg kg(-1) of Org 25969. Anaesthesia and neuromuscular monitoring were continued for a minimum period of 30 min after Org 25969 administration. The main end-point of the study was the time to achieve a sustained recovery of TOF ratio to 0.9. Patients were followed up for 7 days after anaesthesia.

Results: The results showed a dose-related decrease in the average time taken to attain a TOF ratio of 0.9 from 6:49 (min:s) with the 0.5 mg kg(-1) dose to 1:22 with the 4.0 mg kg(-1) dose. Weighted non-linear regression analysis showed the fastest achievable time to TOF ratio of 0.9 to be 1:35. Org 25969 produced no major adverse effects.

Conclusion: Org 25969 effectively reversed a deep and prolonged neuromuscular block induced by rocuronium. The effective reversal dose appears to be 2-4 mg kg(-1).

Publication types

  • Clinical Trial, Phase II
  • Multicenter Study
  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Aged
  • Androstanols / antagonists & inhibitors*
  • Androstanols / pharmacology
  • Anesthesia Recovery Period
  • Anesthesia, General
  • Dose-Response Relationship, Drug
  • Double-Blind Method
  • Electric Stimulation
  • Female
  • Humans
  • Male
  • Middle Aged
  • Monitoring, Intraoperative / methods
  • Myography
  • Neuromuscular Blockade
  • Neuromuscular Junction / drug effects
  • Neuromuscular Junction / physiology
  • Neuromuscular Nondepolarizing Agents / antagonists & inhibitors*
  • Neuromuscular Nondepolarizing Agents / pharmacology
  • Rocuronium
  • Sugammadex
  • gamma-Cyclodextrins / adverse effects
  • gamma-Cyclodextrins / pharmacology*

Substances

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