Source: Medicines & Healthcare Products Regulatory Agency (GB) Revision Year: 2015 Publisher: Alliance Pharmaceuticals Limited, Avonbridge House, Bath Road, Chippenham, Wiltshire, SN15 2BB, United Kingdom
Neostigmine bromide is an antagonist to cholinesterase, the enzyme which normally destroys acetylcholine. The action of neostigmine bromide can briefly be described, therefore, as the potentiation of naturally occurring acetylcholine.
Neostigmine bromide is a quaternary ammonium compound and is poorly absorbed from the gastro-intestinal tract. Following parenteral administration as the methylsulphate, neostigmine is rapidly eliminated with a plasma half-life of 50-90 minutes and is excreted in the urine both as unchanged drug and metabolites. It is metabolised partly by hydrolysis of the ester linkage.
Neostigmine has not been reported to have mutagenic or carcinogenic potential. In rats, acute and chronic exposure causes changes in the fine structure at the end-plate region of muscle.
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