Abstract
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.
Highlights
Residual neuromuscular block at the end of surgery may compromise the patient’s safety
Rocuronium required the highest concentration for effective suppression of single twitch (ST) force amplitude in our ex vivo system
Mechanism of neuromuscular blocking agents (NMBA) block reversal with CMGCD To evaluate the nature of the interaction between CMGCD and NMBAs, CMGCD was administered in a concentration of 13.3 μM to the buffer solution before incremental dosing of pipecuronium
Summary
Residual neuromuscular block at the end of surgery may compromise the patient’s safety. Effective reversal can be achieved with selective relaxant binding agents, sugammadex is the only clinically approved drug in this group. We investigated the concentration–response properties of a novel selective relaxant binding agent, carboxymethyl-γcyclodextrin for the reversal of neuromuscular block. The safe use of non-depolarizing neuromuscular blocking agents (NMBA) requires their rapid and reliable reversal from any depth of block following their administration, without the risk of postoperative re-paralysis or other sequelae. Sugammadex was able to rapidly reverse any depth of rocuronium-induced neuromuscular block within 3 to 5 min, depending on its dose [7, 8].
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