Selective relaxant binding agents for reversal of neuromuscular blockade.
Traditionally, reversal of neuromuscular blockade during anaesthesia was achieved by increasing the acetylcholine concentration in the neuromuscular junction using acetylcholinesterase inhibitors. However, this is ineffective against profound blockade. Furthermore, the increase in acetylcholine level is not limited to the neuromuscular junction, resulting in unwanted side effects requiring co-treatment with muscarinic antagonists. Selective relaxant binding agents offer a new approach for the reversal of neuromuscular blockade: encapsulation of the neuromuscular blocking agent, resulting in inactivation. As part of this new approach, cyclodextrin molecules have been designed that selectively encapsulate steroidal neuromuscular blocking agents. Both animal and human experiments have demonstrated that fast, effective and complete recovery from both normal and profound neuromuscular blockade is now possible. Furthermore, these cyclodextrin derivatives do not have the unwanted side effects of acetylcholinesterase inhibitors.
Bom
Anton
A
Organon Laboratories Ltd, Department of Pharmacology, Newhouse ML1 5SH, UK. a.bom@organon.co.uk
Epemolu
Ola
O
Hope
Frank
F
Rutherford
Samantha
S
Thomson
Karen
K
D000818:Animals; D002986:Clinical Trials as Topic; D003505:Cyclodextrins / Q000627:therapeutic use*; D006801:Humans; D019148:Neuromuscular Blockade; D003473:Neuromuscular Nondepolarizing Agents / Q000037:antagonists & inhibitors*
D003505:Cyclodextrins; D003473:Neuromuscular Nondepolarizing Agents