What is Neostigmine?
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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
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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.