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Drug intelligence / Profile preview
neostigmine methylsulfate
- Development stage
- Approved
- Lead developer
- ASPIRO PHARMA
- Modality
- Small Molecules
- Administration
- Parenteral, Intravenous, Intramuscular, Subcutaneous
01
Overview
Neostigmine methylsulfate is a quaternary ammonium compound that acts as a reversible acetylcholinesterase inhibitor. By competing with acetylcholine for binding to the enzyme acetylcholinesterase, it prevents the hydrolysis of acetylcholine, thereby increasing its concentration and duration of action at the neuromuscular junction. This enhancement of cholinergic activity is leveraged therapeutically to reverse the effects of non-depolarizing neuromuscular blocking agents (NMBAs) following surgery and to manage the symptoms of myasthenia gravis. Due to its quaternary ammonium structure, neostigmine methylsulfate is poorly absorbed from the gastrointestinal tract and does not cross the blood-brain barrier, which limits its pharmacological effects to the peripheral nervous system and reduces central nervous system side effects compared to tertiary amines like physostigmine.
- Brand names
- ProstigminBloxiverzVagostigmin
- Other names
- neostigmineneostigmine methyl sulfateneostigmine metilsulfate3-(dimethylcarbamoyloxy)-N,N,N-trimethylanilinium methyl sulfate
02
Targets
AcetylcholinesteraseButyrylcholinesteraseNicotinic Acetylcholine Receptor
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