Therapeutic Effects: Nondepolarizing neuromuscular blockade reversal

Anesthesia Implications

Uses – good for reversal of nondepolarizing neuromuscular blockers (eg. rocuronium, vecuronium, atracurium, cisatracurium)

Bradycardia – this is the primary concern when giving neostigmine. Neostigmine causes an increased quantity of acetylcholine at the synapse. This effectively competes with the neuromuscular blocker, but also causes an increase in muscarinic affects (such as bradycardia). To counter this affect, glycopyrrolate (0.01 mg/kg) is given with neostigmine (0.05 mg/kg).

OB – Must be given slowly in the parturient. If given rapidly, neostigmine can increase uterine tone and thereby cause preterm labor and/or fetal distress.

Reduced affects – aminoglycoside antibiotics, hypothermia, hypokalemia, and acidosis all weaken the reversal affects of neostigmin

Succinylcholine – should not be used to reverse succinylcholine. In fact, neostigmine will prolong its affects.

Cholinergic crisis – Excessive neostigmine can contribute to a cholinergic crisis. The symptoms are nausea, vomiting, brady/tachycardia, excessive salivation, sweating, bronchospasm, weakness, and paralysis.
Treatment: 10 mcg/kg IV every 3-10 minutes until muscarinic symptoms subside. Pralidoxime (15 mg/kg) IV over 2 minutes will reverse nicotinic symptoms. Supportive treatment (eg. ventilator support) as needed.

Contraindications

Peritonitis
Mechanical obstruction of the intestines or urinary tract

Use with caution in patients with: Bradycardia, bronchial asthma, peptic ulcers, epilepsy, and arrhythmias

IV push dose

Neuromuscular Blockade Reversal: 0.05 mg/kg with glycopyrrolate (0.01 mg/kg). MAX: 5 mg.

Classification: Acetylcholinesterase Inhibitor

Time to Onset: less than 3 minutes

Time to Peak: 3-14 minutes

Duration: 40-60 minutes

Method of Action: Competes with acetylcholine in binding to acetylcholinesterase and thereby prevents hydrolysis of acetylcholine. Additional acetylcholine at the postsynaptic receptors leads to improved transmission of impulses across the neuromuscular junction. Additional acetylcholine also leads to muscarinic affects such as bradycardia and salivation – which is countered, or decreased by co-administration of glycopyrrolate or atropine.

Metabolism: Hepatic and plasma esterase