Ambenonium chloride explained

Ambenonium (as ambenonium dichloride, trade name Mytelase) is a cholinesterase inhibitor^[1] used in the management of myasthenia gravis.

It is classified as a reversible cholinesterase inhibitor.^[2]

Mechanism of action

Ambenonium exerts its actions against myasthenia gravis by competitive reversible inhibition of acetylcholinesterase, the enzyme responsible for the hydrolysis of acetylcholine. Myasthenia gravis occurs when the body produces antibodies against acetylcholine receptors, and thus inhibits signal transmission across the neuromuscular junction. Ambenonium reversibly binds acetylcholinesterase, inactivates it and therefore increases levels of acetylcholine. This, in turn, facilitates transmission of impulses across the myoneural junction and effectively treats the disease.

Indications

Ambenonium is used to treat muscle weakness due to disease or defect of the neuromuscular junction (myasthenia gravis).

Ambenonium was withdrawn from the market in the United States in 2010.^[3]

Notes and References

1. Bolognesi ML, Cavalli A, Andrisano V . Design, synthesis and biological evaluation of ambenonium derivatives as AChE inhibitors . Farmaco . 58 . 9 . 917–28 . September 2003 . 13679187 . 10.1016/S0014-827X(03)00150-2. etal.
2. Hodge AS, Humphrey DR, Rosenberry TL . Ambenonium is a rapidly reversible noncovalent inhibitor of acetylcholinesterase, with one of the highest known affinities . Mol. Pharmacol. . 41 . 5 . 937–42 . May 1992 . 1588924 .
3. Web site: Ambenonium . St. Elizabeth Healthcare . 2016-02-10 . https://web.archive.org/web/20150908065032/http://www.stelizabeth.com/ADAM/doc/Thomson%20DrugNotes/45/5103.htm . 2015-09-08 . dead .