vi medicine informatics




Physostigmine and neostigmine, both of which are amines, are reversible anticholinesterases. Both compounds act as substrates for acetylcholinesterase, which prevent esterase from breaking down acetylcholine in the neuromuscular junction, therefore increasing the amount of acetylcholine in the synapse. Physostigmine is a tertiary amine and has better central nervous system penetration than neostigmine (a quaternary amine). Thus physostigmine is used as an antidote for anticholinergic toxicity because of its ability to cross the blood-brain barrier and treat central anticholinergic toxicity (delirium, agitation), as well as peripheral anticholinergic toxicity. Neostigmine has better peripheral action (especially on skeletal muscle). Neostigmine does not cross the blood-brain barrier,but can be used for post-operative and neurogenic ileus, urinary retention, and reversal of neuromuscular junction blockade.

tags: oneliner