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Abstract
Since the introduction of nondepolarizing neuromuscular blocking agents, acetylcholinesterase
inhibitors have been used to increase the speed of recovery from neuromuscular blockade.
The major disadvantages of acetylcholinesterase inhibitors are their lack of activity
against profound neuromuscular blockade and their activity outside the neuromuscular
junction resulting in unwanted side effects, requiring cotreatment with a muscarinic
antagonist. An alternative to acetylcholinesterase inhibitors is the encapsulating
agent sugammadex. This agent has been specifically designed to encapsulate the steroidal
neuromuscular blocking agents rocuronium and vecuronium. This review describes the
effects of sugammadex in in vitro tissue and in vivo animal experiments. The encapsulation
approach allows reversal of any degree of neuromuscular blockade because the dose
of sugammadex can be adjusted to encapsulate sufficient neuromuscular blocking molecules
to cause effective reversal. Because this interaction is a drug-drug interaction,
reversal can be achieved very fast but is limited by the circulation time. Sugammadex
is also effective against neuromuscular blockade under conditions with reduced acetylcholine
release, which potentiate the action of neuromuscular blocking agents. Sugammadex
does not cause cholinergic side effects, preventing the need of coadministration of
muscarinic antagonists. Because of these properties, sugammadex has the potential
to become a very useful drug for the management of neuromuscular blockade.