Understanding Anesthesiology - The Global Regional Anesthesia ...

NEOSTIGMINE
Class
Anticholinesterase. In anesthesia practice, neostigmine
is used for the reversal of neuromuscular blockade. Internal
Internal Medicine specialists use neostigmine (or its
relative, pyridostigmine) for the treatment of myasthenia
gravis.
Mechanism of Action
Anticholinesterases inhibit the breakdown of acetylcholine
(Ach) in the synaptic cleft by inhibiting the cholinesterase
enzyme. As a result, Ach concentrations in the
synaptic cleft are increased. Ach is then better able to
compete with muscle relaxants for the Ach receptors
and achieve depolarization of the muscle cell.
Dose
For reversal of neuromuscular blockade: 0.05 mg/kg
Dose should not exceed 5 mg
Effects
Most of neostigmine’s effects are related to its cholinergic
action. It must be given with an anticholinergic (atropine
or more commonly glycopyrrolate) in order to
minimize these effects.
CNS
Seizures
CVS
Bradycardia, AV block, nodal rhythm, hypotension
Respiratory
Increased oral and bronchial secretions, bronchospasm
GI/GU
Increased peristalsis, urinary frequency
Misc.
Overdose may produce cholinergic crisis. Neostigmine
does not antagonize succinylcholine and may prolong
phase 1 block of succinylcholine.
Must be administered with with atropine 0.015 mg/kg
or glycopyrrolate 0.01 mg/kg
Onset
5 minutes
Duration
55-75 minutes
Elimination
Hepatic, plasma esterases
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