Neostigmine

PROSTIGMIN

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Neostigmine ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Neostigmine ballicule

What it isPeripheral acetylcholinesterase inhibitor; reversal of neuromuscular blockade and treatment of myasthenia.

Why this oneIt restores neuromuscular transmission after surgery without entering the CNS.

What limits it⚑ Give with glycopyrrolate or atropine to prevent bradycardia and bronchospasm; it cannot reliably reverse deep blockade.

Neostigmine molecular structure (skeletal formula) — Molecular structure: Neostigmine

FDA-approved for

myasthenia/reversal (~1955)

FDA label

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FDA dosing	Population	Start	Target	Max
Reversal of non-depolarizing NMBA — shorter-acting (e.g., rocuronium) or twitch >10% baseline/2nd twitch present	Adults & peds (all ages)	0.03 mg/kg IV	0.03 mg/kg IV	0.07 mg/kg or 5 mg total, whichever is less
Reversal of non-depolarizing NMBA — longer-acting (e.g., vecuronium, pancuronium) or twitch near 10% baseline	Adults & peds (all ages)	0.07 mg/kg IV	0.07 mg/kg IV	0.07 mg/kg or 5 mg total, whichever is less

Renal No dose adjustment; half-life prolonged in renal impairment — monitor longer

Hepatic No dose adjustment in hepatic impairment

Maximum total dose 0.07 mg/kg or 5 mg, whichever is less

Instructions

IV use only; inject slowly over at least 1 minute
Give an anticholinergic (atropine or glycopyrrolate) prior to or concomitantly to lessen bradycardia
Use peripheral nerve stimulator (train-of-four) monitoring to time dosing and assess recovery
Maintain ventilation and patent airway until full recovery

Available strengths

inj 0.5, 0.51, 1, 1.02 mg/mL

Contraindications

Peritonitis or mechanical obstruction of the intestinal or urinary tract

Cautions

Bradycardia — pretreat with anticholinergic
Caution in coronary artery disease, cardiac arrhythmias, recent acute coronary syndrome, or myasthenia gravis
Neuromuscular dysfunction with large doses when blockade is minimal
Differentiate cholinergic crisis from myasthenic crisis
Hypersensitivity/anaphylaxis — have atropine and anaphylaxis treatment available

Adverse reactions

Bradycardia
Nausea
Vomiting
Hypotension
Tachycardia
Dry mouth
Dizziness
Headache

Pregnancy No adequate human data; anticholinesterases may cause uterine irritability/premature labor near term; use only if clearly needed

Lactation Not studied; unknown whether present in human milk

Cost

Neostigmine (PROSTIGMIN)

Strength		#/mo	CostPlus
0.5 mg/mL	inj	per unit	not offered
0.51 mg/mL	inj	per unit	not offered
1 mg/mL	inj	per unit	not offered
1.02 mg/mL	inj	per unit	not offered

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Neostigmine is administered under clinical supervision and dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

NO BOXED WARNINGS

Principal riskBradycardia unless an antimuscarinic is co-given

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4

Overdose danger3 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Defining liabilityCholinergic crisis with respiratory weakness and bradycardia

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