Carboxymethyl-γ-cyclodextrin, a novel selective relaxant binding agent for the reversal of neuromuscular block induced by aminosteroid neuromuscular blockers: an ex vivo laboratory study

BMC Anesthesiology

Tamás Sohajda¹  Lajos Szente¹  Ákos I. Fábián²  Vera Csernoch²  Edömér Tassonyi²  Marianna Fedor²  Béla Fülesdi² 

[1] Cyclolab Ltd, Budapest, Hungary;Department of Anaesthesiology and Intensive Care, University of Debrecen Clinical Center, Nagyerdei krt. 98, 4012, Debrecen, Hungary;

关键词: Neuromuscular blocking agent;    Selective relaxant binding agent;    Cyclodextrin;    Sugammadex;    Rocuronium;    Pipecuronium;    Vecuronium;    Phrenic nerve;    Hemidiaphragm;   

DOI  :  10.1186/s12871-021-01424-4

来源: Springer

【 摘 要 】

BackgroundResidual neuromuscular block at the end of surgery may compromise the patient’s safety. The risk of airway complications can be minimized through monitoring of neuromuscular function and reversal of neuromuscular block if needed. Effective reversal can be achieved with selective relaxant binding agents, however, sugammadex is the only clinically approved drug in this group.We investigated the concentration–response properties of a novel selective relaxant binding agent, carboxymethyl-γ-cyclodextrin for the reversal of neuromuscular block. We evaluated the hypothesis that it is equally potent for reversing neuromuscular block as sugammadex.MethodsPhrenic nerve – hemidiaphragm tissue preparations were isolated from male Wistar rats and suspended in a tissue holder allowing electrical stimulation of the nerve and monitoring of muscle contraction force. Concentration–response relationships were constructed for the neuromuscular blocking agents rocuronium, pipecuronium, and vecuronium. The half-effective concentrations of sugammadex and carboxymethyl-γ-cyclodextrin for reversal of neuromuscular block were determined.ResultsThe half effective concentrations (95% confidence interval, CI) were 7.50 (6.93–8.12) μM for rocuronium, 1.38 (1.33–1.42) μM for pipecuronium, and 3.69 (3.59–3.80) μM for vecuronium. The half effective concentrations (95% CI) of carboxymethyl-γ-cyclodextrin and sugammadex were 35.89 (32.67–39.41) μM and 3.67 (3.43–3.92) μM, respectively, for the reversal of rocuronium-induced block; 10.14 (9.61–10.70) μM and 0.67 (0.62–0.74) μM, respectively, for the reversal of pipecuronium-induced block; and 376.1 (341.9–413.8) μM and 1.45 (1.35–1.56) μM, respectively, for the reversal of vecuronium-induced block.ConclusionsCarboxymethyl-γ-cyclodextrin is an effective, but less potent agent for reversal of neuromuscular block than sugammadex.

【 授权许可】

CC BY