Neostigmine

Trade Names: generic, Prostigmin ®

Drug Class: Carbamate Anticholinesterase, Cholinomimetic
Mechanism of Action:
Inhibits the hydrolysis of acetylcholine by competing with acetylcholine for attachment to acetylcholinesterase at sites
of cholinergic transmission
It enhances cholinergic action by facilitating the transmission of impulses across neuromuscular junctions
It also has a direct cholinomimetic effect on skeletal muscle and possibly on autonomic ganglion cells
Because it contains a quaternary ammonium group it does not cross the blood-brain barrier
Indications:
For symptomatic treatment of myasthenia gravis
Its greatest usefulness is in prolonged therapy where no difficulty in swallowing is present
In acute myasthenic crisis where difficulty in breathing and swallowing is present, the parenteral form (neostigmine
methylsulfate) should be used. The patient can be transferred to the oral form as soon as it can be tolerated.
Off label: non-obstructive ileus (paralysis of the bowel) (Thompson & Magnuson, 2012; Kasi, 2013)
Contraindications:
Patients with known hypersensitivity to the drug
Contraindicated in patients with peritonitis or mechanical obstruction of the intestinal or urinary tract
Side Effects:
Generally due to an exaggeration of pharmacological effects of which salivation and fasiculation are the most common
Bowel cramps and diarrhea may also occur
For a more complete list, see the rxlist.com [http://www.rxlist.com/prostigmin-drug.htm] reference
Pharmacokinetics:
Neostigmine bromide is poorly absorbed from the gastrointestinal tract following oral administration
As a rule, 15 mg of neostigmine bromide given orally is equivalent to 0.5 mg of neostigmine methylsulfate given
parenterally
Major drug Interactions:
Certain aminoglycoside antibiotics, especially neomycin, streptomycin and kanamycin, have a mild but definite
nondepolarizing blocking action which may accentuate neuromuscular block. These antibiotics should be used in the
myasthenic patient only where definitely indicated.
References:
Kasi PM (2013): The use of intravenous neostigmine in palliation of severe ileus. Case Reports in Gastrointestinal
Medicine Volume 2013 Article ID 796739, 4 pages. http://dx.doi.org/10.1155/2013/796739
[http://dx.doi.org/10.1155/2013/796739]
Pappano AJ (2012) [http://libproxy.tulane.edu:2048/login?url=http://www.accessmedicine.com/content.aspx?aID=55820947]
Cholinoceptor-Activating & Cholinesterase-Inhibiting Drugs (Chapter 7). In: Basic & Clinical Pharmacology. 12e. Katzung
BG, Masters SB, Trevor AJ (Editors). McGraw-Hill / Lange. (Access-Medicine)
Thompson M, Magnuson B (2012): Management of postoperative ileus. Orthopedics 35(3):213-217. DOI:
10.3928/01477447-20120222-08
rxlist.com [http://www.rxlist.com/prostigmin-drug.htm] (Prostigmin ®)

Keywords

neostigmine
neostigmine.txt · Last modified: 2015/09/16 14:46 by cclarks