Overview
11 DESCRIPTION Neostigmine Methylsulfate Injection, USP, a cholinesterase inhibitor, has an empirical formula of C 13 H 22 N 2 O 6 S, a molecular weight of 334.39 g/mol and the following structural formula: Neostigmine Methylsulfate Injection is formulated with neostigmine methylsulfate, a white crystalline powder, chemically designated as (m-hydroxyphenyl) trimethylammonium methylsulfate...
Mechanism of Action
12 CLINICAL PHARMACOLOGY 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. 12.2 Pharmacodynamics Neostigmine is an anticholinesterase agent, and inhibits the hydrolysis of acetylcholine by competing with acetylcholine for binding to acetylcholinesterase at sites of cholinergic transmission. By reducing the breakdown of acetylcholine, neuromuscular transmission is facilitated.
Indications
- 1 INDICATIONS AND USAGE Neostigmine Methylsulfate Injection, a cholinesterase inhibitor, is indicated for reversal of the effects of nondepolarizing neuromuscular blocking agents (NMBA) after surgery. Neostigmine Methylsulfate, a cholinesterase inhibitor, is indicated for reversal of the effects of nondepolarizing neuromuscular blocking agents (NMBA) after surgery ( 1 ).
Common Doses
- 0.03 mg
- 0.07 mg
- 5 mg
- 15 mcg
Dosage
2 DOSAGE AND ADMINISTRATION Dosage Should be administered by trained healthcare providers ( 2.1 ) Recommend use of a peripheral nerve stimulator to determine whether neostigmine methylsulfate should be administered and to monitor recovery from neuromuscular blockade ( 2.1 ). 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) ( 2.2 , 2.3 , 2.
Contraindications
- 4 CONTRAINDICATIONS Neostigmine 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 urinary or intestinal tracts. Hypersensitivity to neostigmine ( 4 ) Peritonitis or mechanical obstruction of urinary or intestinal tracts ( 4 )
Side Effects
- 6 ADVERSE REACTIONS The most common adverse reactions include bradycardia and nausea and vomiting. ( 6 ) To report SUSPECTED ADVERSE REACTIONS, contact Fresenius Kabi USA, LLC at 1-800-551-7176 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trial Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.
Interactions
- 7 DRUG INTERACTIONS The pharmacokinetic interaction between neostigmine methylsulfate and other drugs has not been studied. Neostigmine methylsulfate is metabolized by microsomal enzymes in the liver. Closely monitor patients for a longer period of time when using Neostigmine Methylsulfate Injection with other drugs which may alter the activity of metabolizing enzymes or transporters. 7.1 Depolarizing Muscle relaxants Use of neostigmine to reverse the effects of depolarizing muscle relaxants such as succinylcholine is not recommended, because it may prolong the phase-1 block. 7.