Neostigmine
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Neostigmine
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| Systematic (IUPAC) name | |
| 3-(dimethylcarbamoyloxy)-N,N,N-trimethylbenzenaminium | |
| Identifiers | |
| CAS number | |
| ATC code | N07 S01EB06 |
| PubChem | |
| Chemical data | |
| Formula | C12H19N2O2 |
| Mol. mass | 223.294 g/mol |
| Pharmacokinetic data | |
| Bioavailability | Unclear, probably less than 5% |
| Metabolism | Slow hydrolysis by acetylcholinesterase and also by plasma esterases |
| Half life | 50-90 minutes |
| Excretion | Unchanged drug (up to 70%) and alcoholic metabolite (30%) are excreted in the urine |
| Therapeutic considerations | |
| Pregnancy cat. |
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| Legal status | |
| Routes | ? |
Neostigmine is a parasympathomimetic, specifically, a reversible cholinesterase inhibitor. By interfering with the breakdown of acetylcholine, neostigmine indirectly stimulates both nicotinic and muscarinic receptors.
[edit] Clinical Uses
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-depolarising muscle relaxants such as vecuronium.
It can also be used for urinary retention resulting from general anaesthetia and to treat curariform drug toxicity.
Another indication for use is the Ogilvie syndrome which is a pseudoobstruction of the colon in critically ill patients.
Neostigmine will cause slowing of the heart rate (bradycardia), for this reason it is usually given along with a parasympatholytic drug such as atropine or glycopyrrolate.
Neostigmine is available under several trade names such as Prostigmin®.
[edit] Sources
- 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
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| Anticholinesterases (N06DA, N07AA) edit |
| Metrifonate - Physostigmine - Neostigmine - Pyridostigmine - Ambenonium - Demarcarium - Rivastigmine - Galantamine - Donepezil - Tacrine - Edrophonium |
| Antiglaucoma preparations and miotics (S01E) | |
|---|---|
| Sympathomimetics | Apraclonidine, Brimonidine, Clonidine, Dipivefrine, Epinephrine |
| Parasympathomimetics | Aceclidine, Acetylcholine, Carbachol, Demecarium, Echothiophate, Fluostigmine, Neostigmine, Paraoxon, Physostigmine, Pilocarpine |
| Carbonic anhydrase inhibitors | Acetazolamide, Brinzolamide, Diclofenamide, Dorzolamide, Methazolamide |
| Beta blocking agents | Befunolol, Betaxolol, Carteolol, Levobunolol, Metipranolol, Timolol |
| Prostaglandin analogues | Bimatoprost, Latanoprost, Travoprost, Unoprostone |
| Other agents | Dapiprazole, Guanethidine |
