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Neostigmine chemical structure
|ATC code |
|Molecular weight||223.294 g/mol|
|Bioavailability||Unclear, probably less than 5%|
|Metabolism||Slow hydrolysis by acetylcholinesterase and also by plasma esterases|
|Elimination half-life||50-90 minutes|
|Excretion||Unchanged drug (up to 70%) and alcoholic metabolite (30%) are excreted in the urine|
|Routes of administration|
Neostigmine is a parasympathomimetic, specifically, a reversible cholinesterase inhibitor. By interfering with the breakdown of acetylcholine, neostigmine indirectly stimulates both nicotinic and muscarinic receptors. It does cross the blood-brain barrier albeit poorly. Neostigmine binds to the anionic site of cholinesterase. The drug blocks the active site of acetylcholinesterase so the enzyme can no longer break down the acetylcholine molecules before they reach the postsynaptic membrane receptors. This allows for the threshold to be reached so a new impulse can be triggered in the next neuron. In myasthenia gravis there are too few acetylcholine receptors so with the acetylcholinesterase blocked, acetylcholine can bind to the few receptors and trigger a muscular contraction.
Clinical Uses[edit | edit source]
It is used to improve muscle tone in people with myasthenia gravis and routinely, in anesthesia at the end of an operation, to reverse the effects of non-depolarizing muscle relaxants such as vecuronium.
Neostigmine is available under several trade names such as Prostigmin®.
Neostigmine was first synthesized by Aeschlimann and Reinert in 1931.
See also[edit | edit source]
References[edit | edit source]
- Brenner, G. M. (2000). Pharmacology. Philadelphia, PA: W.B. Saunders Company. ISBN 0-7216-7757-6
- Canadian Pharmacists Association (2000). Compendium of Pharmaceuticals and Specialties (25th ed.). Toronto, ON: Webcom. ISBN 0-919115-76-4
Anticholinesterases (N06DA, N07AA)
Ophthalmologicals: antiglaucoma preparations and miotics (S01E)
|Carbonic anhydrase inhibitors|
|Beta blocking agents|
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