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Neostigmine is a drug used to treat the disease myasthenia gravis. The drug binds to the active site of acetylcholinesterase preventing breakdown of acetylcholine. This drug is a competitive inhibitor.
Neostigmine is water-soluble. It is an ionized compound which reversibly inhibits the enzyme acetylcholinesterase. Its FDA indication is for the reversal of the effects of non-depolarizing neuromuscular blocking agents after surgery.
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.
Neostigmine, unlike physostigmine, does not cross the blood-brain barrier.
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