NEOSTIGMINE METHYLSULFATE

DistributionProtein binding of neostigmine to human serum albumin ranges from 15 to 25%. The observed volume of distribution is between 0.12 and 1.4 L/kg following intravenous injection.

EliminationNeostigmine is metabolized by microsomal enzymes in the liver and the observed elimination half-life reported is between 24 and 113 minutes.

MetabolismNeostigmine is metabolized by microsomal enzymes in the liver.

ExcretionThe observed elimination half-life reported is between 24 and 113 minutes f...

Data from published literature support the intravenous use of neostigmine methylsulfate for reversal of nondepolarizing neuromuscular blocking agents. Randomized, spontaneous-recovery-controlled or placebo-controlled studies using similar efficacy endpoints evaluated a total of 404 adult and 80 pediatric patients undergoing various surgical procedures. Patients had reductions in their recovery time from neuromuscular blockade with neostigmine methylsulfate treatment compared to spontaneous recovery and placebo treatments.

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 obs...

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. Hyp...

Bradycardia : Atropine or glycopyrrolate should be administered prior to administration of neostigmine methylsulfate injection to lessen risk of bradycardia ( 5.1 ) 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 suff...

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 Depolari...