Chemical formula: C₁₂H₁₉N₂O₂⁺ Molecular mass: 223.292 g/mol PubChem compound: 4456
Neostigmine inhibits cholinesterase activity and prolongs and intensifies the muscarinic and nicotinic effects of acetylcholine. The anticholinesterase actions of neostigmine are reversible. It is used mainly for its action on skeletal muscle and less frequently to increase the activity of smooth muscle. Neostigmine is used in the treatment of Myasthenia Gravis.
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. The half-life of neostigmine is only one to two hours.
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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