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| {{drugbox
| | #REDIRECT [[Pyridostigmine (patient information)]] |
| | IUPAC_name = (1-methylpyridin-5-yl) dimethylaminoformate
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| | image = Pyridostigmine.png
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| | CAS_number = 155-97-5
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| | ATC_prefix = N07
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| | ATC_suffix = AA02
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| | ATC_supplemental =
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| | PubChem = 4991
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| | DrugBank = APRD00380
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| | C = 9 | H = 13 | N = 2 | O = 2
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| | molecular_weight = 181.212 g/mol
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| | bioavailability = 7.6 +/- 2.4%
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| | protein_bound =
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| | metabolism =
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| | elimination_half-life = 1.78 +/- 0.24hrs
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| | excretion = [[Kidney|Renal]]
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| | pregnancy_AU = C
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| | pregnancy_US = C
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| | legal_UK = POM
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| | legal_US = Rx-only
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| | routes_of_administration = Oral, [[Intravenous therapy|intravenous]]
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| }}
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| '''Pyridostigmine''' is a [[parasympathomimetic]] and a reversible [[cholinesterase inhibitor]]. Since it is a quaternary amine, it is poorly absorbed in the gut and doesn't cross the [[blood-brain barrier]], except in stressful conditions[2].
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| ==Mode of action==
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| ''In order to understand the mode of action, a quick outline of a synapse is given below. For more information, look up [[synapse]].''
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| Action potentials are conducted along motor nerves to their terminals where they initiate a Ca2+ influx and the release of [[acetylcholine]] (ACh). The ACh diffuses across the synaptic cleft and binds to receptors on the post synaptic membrane, causing an influx of [[sodium|Na]]+ and [[potassium|K]]+ ions, resulting in depolarisation. If large enough, this depolarisation results in an action potential. In order to prevent constant stimulation once the ACh is released, an enzyme called [[acetylcholinesterase]] is present in the endplate membrane close to the receptors on the post synaptic membrane, and quickly hydrolises ACh.
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| Pyridostigmine inhibits acetylcholinesterase in the [[synaptic cleft]], thus slowing down the hydrolysis of [[acetylcholine]].
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| ==Clinical uses==
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| Pyridostigmine is used to treat muscle weakness in people with [[myasthenia gravis]] and to combat the effects of [[curare|curariform]] drug toxicity. It also has a military use as a [[nerve gas]] [[antidote]] (it has been used in particular during the first [[Gulf War]]).
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| Pyridostigmine is now also used to treat [[orthostatic hypotension]].<ref name="Singer-2003">{{cite journal | author=Singer W, Opfer-Gehrking TL, McPhee BR, Hilz MJ, Bharucha AE, Low PA. | title=Acetylcholinesterase inhibition: a novel approach in the treatment of neurogenic orthostatic hypotension. | journal=J Neurol Neurosurg Psychiatry | year=2003 | volume=74 | issue=9 | pages=1294-8 | id=PMID 12933939}}</ref>
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| Pyridostigmine bromide is available under the trade names '''Mestinon®''' ([[Valeant Pharmaceuticals International|Valeant Pharmaceuticals]]) and '''Regonol®'''.
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| ==References==
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| <references/>
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| 2. Journal Watch Psychiatry, Vol. 1997, Issue 201, 21 February 1, 1997
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| ==Related Publications==
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| #Brenner, G. M. (2000). ''Pharmacology.'' Philadelphia, PA: W.B. Saunders Company. ISBN 0-7216-7757-6
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| #Canadian Pharmacists Association (2000). ''Compendium of Pharmaceuticals and Specialties'' (25th ed.). Toronto, ON: Webcom. ISBN 0-919115-76-4
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| #Neal, M.J. (2002). ''Medical Pharmacology at a Glance'' (5th ed.). London, England: Blackwell Publishing. ISBN 1405133600
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| {{Parasympathomimetics}}
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| {{Anticholinesterases}}
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| [[Category:Anticholinesterases]]
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| [[ru:Пиридостигмина бромид]]
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