Use of Chemical Chelators as Reversal Agents for Drug-Induced Neuromuscular Block

Abstract

The invention relates to the use of chemical chelators for the preparation of a medicament for the reversal of drug-induced neuromuscular block, to a kit for providing neuromuscular block and its reversal, and to cyclophane derivatives having the general formula A wherein R is (CH 2 ) 5 , or or the general formula B wherein X is (CH 2 ) 5 , or or a pharmaceutically acceptable salt thereof.

1 - 11 . (canceled) 
   
   
       12 . A method for reversal of drug-induced neuromuscular block in a patient caused by clinically-used neuromuscular blocking agent which acts by reversible binding to the acetylcholine receptor, comprising parenterally administering to said patient an effective amount of a chemical chelator capable of forming a guest-host complex with the neuromuscular blocking agent, wherein the association constant of said guest-host in an aqueous medium at ambient temperature is higher than 10.000 M-1. 
   
   
       13 . The method according to  claim 12 , wherein the neuromuscular blocking agent is selected from the group consisting of rocuronium, vecuronium, pancuronium, rapacuronium, mivacurium, (cis)atracurium and tubocurarine. 
   
   
       14 . The method according to  claim 12 , wherein the chemical chelator is selected from the group consisting of cyclic oligosaccharides and cyclophanes. 
   
   
       15 . The method according to  claim 12 , wherein the chemical chelator is gamma-cyclodextrin or a derivative thereof. 
   
   
       16 . The method according to  claim 12 , wherein the neuromuscular blocking agent is selected from the group consisting of rocuronium and vecuronium and the chemical chelator is gamma-cyclodextrin or a derivative thereof.