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Neostigmine inhibits the hydrolysis of acetylcholine by competing with acetylcholine for attachment to acetylcholinesterase at sites of cholinergic transmission. It enhances cholinergic action by facilitating the transmission of impulses across neuromuscular junctions. It also has a direct cholinomimetic effect on skeletal muscle and possibly on autonomic ganglion cells and neurons of the central nervous system. Neostigmine undergoes hydrolysis by cholinesterase and is also metabolized by microsomal enzymes in the liver. Protein binding to human serum albumin ranges from 15 to 25 percent.
Neostigmine bromide is poorly absorbed from the gastrointestinal tract following oral administration. As a rule, 15 mg of neostigmine bromide orally is equivalent to 0.5 mg of neostigmine methylsulfate parenterally, due to poor absorption of the tablet from the intestinal tract. In a study in fasting myasthenic patients, the extent of absorption was estimated to be 1 to 2 percent of the ingested 30 mg single oral dose. Peak concentrations in plasma occurred 1 to 2 hours following drug ingestion, with considerable individual variations. The half-life ranged from 42 to 60 minutes with a mean half-life of 52 minutes.
Last reviewed on RxList: 3/26/2009
This monograph has been modified to include the generic and brand name in many instances.
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