Neostigmine Methylsulfate

What it is and how it works

12.1. Mechanism of Action 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.

Indications

1. INDICATIONS AND USAGE Neostigmine Methylsulfate Injection, USP is a cholinesterase inhibitor indicated for the reversal of the effects of non-depolarizing neuromuscular blocking agents after surgery. Neostigmine Methylsulfate Injection, USP, a cholinesterase inhibitor, is indicated for the reversal of the effects of non-depolarizing neuromuscular blocking agents (NMBAs) after surgery.

Dosage and administration (summary)

2. DOSAGE AND ADMINISTRATION Should be administered by trained healthcare providers Peripheral nerve stimulator and monitoring for twitch responses should be used to determine when Neostigmine Methylsulfate Injection, USP should be initiated and if additional doses are needed 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 Maximum total dosage is 0.07 mg/kg or up to a total of 5 mg (whichever is less) An anticholinergic…

Contraindications

4. CONTRAINDICATIONS Neostigmine Methylsulfate Injection, USP is contraindicated in patients with: known hypersensitivity to neostigmine methylsulfate (known hypersensitivity reactions have included urticaria, angioedema, erythema multiforme, generalized rash, facial swelling, peripheral edema, pyrexia, flushing, hypotension, bronchospasm, bradycardia and anaphylaxis). peritonitis or mechanical obstruction of the intestinal or urinary tract.

Warnings and precautions

5. WARNINGS AND PRECAUTIONS Bradycardia: Atropine or glycopyrrolate should be administered prior to Neostigmine Methylsulfate Injection, USP to lessen risk of bradycardia. Serious Reactions with Coexisting Conditions: Use with caution in patients with coronary artery disease, cardiac arrhythmias, recent acute coronary syndrome or myasthenia gravis. Neuromuscular Dysfunction: Can occur if large doses of Neostigmine Methylsulfate Injection, USP are administered when neuromuscular blockade is minimal; reduce dose if recovery from neuromuscular blockade is nearly complete. 5.1.

Pregnancy

8.1. Pregnancy Risk Summary There are no adequate or well-controlled studies of Neostigmine Methylsulfate Injection, USP in pregnant women. It is not known whether Neostigmine Methylsulfate Injection, USP can cause fetal harm when administered to a pregnant woman or can affect reproductive capacity.

Storage and supply

16. HOW SUPPLIED/STORAGE AND HANDLING Neostigmine Methylsulfate Injection, USP is a clear, colorless liquid available in the following: NDC No. Strength Vial Size 0641-6264-10 0.5 mg/mL 10 mL multiple dose vials supplied in packages of 10 0641-6265-10 1 mg/mL 10 mL multiple dose vials supplied in packages of 10 The vial stopper is not made with nat…

Source: Neostigmine Methylsulfate (Neostigmine Methylsulfate) — US FDA prescribing information, 2024-04-10, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.