Neostigmine

What is Neostigmine?

  • Neostigmine is a cholinesterase inhibitor generally used to reverse non-depolarizing muscle relaxants like DrugLibrary/Rocuronium Rocuronium Private or Broken Links
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Mechanism of Action & Pharmacokinetics 12

  • Mechanism of Action: Neostigmine inhibits acetylcholinesterase, preventing the breakdown of acetylcholine => Leads to enhanced stimulation of nicotinic and muscarinic receptors.
  • Secondary Effects: Leads to muscarinic receptor stimulation, which can lead to bradycardia, increased secretions, and bronchospasm. Glycopyrrolate can reduce these effects.

Pharmacodynamics 12

Cardiovascular

  • Bradycardia due to its stimulation of the parasympathetic nervous system.

Respiratory

  • Can cause bronchospasm due to stimulation of muscarinic receptors in the bronchial smooth muscles.

Indications 12

Reversal of Neuromuscular Blockade

  • Used to reverse the effects of non-depolarizing neuromuscular blocking agents (NDMRs) like DrugLibrary/Rocuronium Rocuronium Private or Broken Links
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    and vecuronium.
  • Works by increasing the concentration of acetylcholine at the neuromuscular junction, outcompeting the NDMRs

Dosing 12

  • Reversal of NDMR: 0.03 - 0.07 mg/kg IV, usually administered with glycopyrrolate to mitigate muscarinic side effects.
  • Due to the side effects of neostigmine, often the dose does not exceed 3mg.
  • The ratio of neostigmine to Glycopyrrolate is 5:1.

Complications 12

  • Bradycardia: Often requires co-administration of an anticholinergic agent like glycopyrrolate.
  • Bronchospasm: Due to stimulation of muscarinic receptors.
  • Gastrointestinal: Nausea, vomiting, and increased gastrointestinal motility.

References

  1. Sullivan, P. (2012). Ottawa Anesthesia Primer. Echo Book Publishing.  2 3 4 5

  2. Shafer SL, Rathmell JP, Flood P. (2015). Stoelting’s Pharmacology and Physiology in Anesthetic Practice. Fifth edition. Philadelphia: Wolters Kluwer Health.  2 3 4 5