Neostigmine methylsulfate is a competitive cholinesterase inhibitor. By reducing the breakdown of acetylcholine, neostigmine methylsulfate induces an increase in acetylcholine in the synaptic cleft which competes for the same binding site as nondepolarizing neuromuscular blocking agents, and reverses the neuromuscular blockade.

Neostigmine Methylsulfate, a cholinesterase inhibitor, is indicated for reversal of the effects of nondepolarizing neuromuscular blocking agents (NMBA) after surgery.

Dosage:
•Should be administered by trained healthcare providers.
•Recommend use of a peripheral nerve stimulator to determine whether neostigmine methylsulfate should be administered and to monitor recovery from neuromuscular blockade.
•Recommended dosage range is 0.03 mg/kg to 0.07mg/kg for reversing nondepolarizing neuromuscular block when administered with an anticholinergic agent (atropine or glycopyrrolate) ○ For reversal of NMBAs with shorter half-lives, when first twitch response is substantially greater than 10% of baseline, or when a second twitch is present: 0.03 mg/kg by intravenous route. ○For reversal of NMBAs with longer half-lives or when first twitch response is close to 10% of baseline: 0.07 mg/kg by intravenous route. See package insert for complete information.

The most common adverse reactions include bradycardia and nausea and vomiting.

•Hypersensitivity to neostigmine.
•Peritonitis or mechanical obstruction of urinary or intestinal tracts.

•Bradycardia: Atropine or glycopyrrolate should be administered prior to administration of neostigmine methylsulfate injection to lessen risk of bradycardia.
•Coexisting Conditions: Patients with known cardiac disease, cardiac arrhythmias, or recent coronary artery occlusion may be particularly sensitive to the hemodynamic effects of neostigmine; their blood pressure and electrocardiogram should be continuously monitored with the initiation of neostigmine treatment and for a duration sufficient to assure hemodynamic stability.
•Neuromuscular Dysfunction: Can occur if large doses of neostigmine methylsulfate are administered when there is minimal neuromuscular blockade; reduce the dose if recovery from neuromuscular blockade is nearly complete.