Understanding Anesthesiology - The Global Regional Anesthesia ...

Neostigmine
Class
Anticholinesterase. In anesthesia practice, neostigmine is used for the reversal of neuromuscular
blockade. Internal Medicine specialists use neostigmine 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
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
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.
Related Glossary Terms
Anticholinergic, Anticholinesterase, Cholinesterase, Neuromuscular junction, Nondepolarizing
muscle relaxants
Index
Find Term
Chapter 3 - General Anesthesia
Chapter 4 - Recovery
Chapter 6 - Drug Finder
Chapter 6 - Anticholinesterase and Anticholinergics