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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/06/15 10:58:26」(JST)

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

It is classified as reversible.^[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 myoneural 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Ambenonium was withdrawn from the market in the United States in 2010.^[3]

References

^ Bolognesi ML, Cavalli A, Andrisano V, et al. (September 2003). "Design, synthesis and biological evaluation of ambenonium derivatives as AChE inhibitors". Farmaco 58 (9): 917–28. doi:10.1016/S0014-827X(03)00150-2. PMID 13679187.
^ Hodge AS, Humphrey DR, Rosenberry TL (May 1992). "Ambenonium is a rapidly reversible noncovalent inhibitor of acetylcholinesterase, with one of the highest known affinities". Mol. Pharmacol. 41 (5): 937–42. PMID 1588924.
^ "Ambenonium". St. Elizabeth Healthcare.

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English Journal

Long-Lasting Inhibitory Effects of Distigmine on Recombinant Human Acetylcholinesterase Activity.

Obara K1, Chino D1,2, Tanaka Y1.
Biological & pharmaceutical bulletin.Biol Pharm Bull.2017;40(10):1739-1746. doi: 10.1248/bpb.b17-00351.
PMID 28966245

The Long-Lasting Enhancing Effect of Distigmine on Acetylcholine-Induced Contraction of Guinea Pig Detrusor Smooth Muscle Correlates with Its Anticholinesterase Activity.

Obara K1, Ogawa T1, Chino D1, Tanaka Y1.
Biological & pharmaceutical bulletin.Biol Pharm Bull.2017;40(7):1092-1100. doi: 10.1248/bpb.b17-00175.
PMID 28674252

Spontaneous Synaptic Activation of Muscarinic Receptors by Striatal Cholinergic Neuron Firing.

Mamaligas AA1, Ford CP2.
Neuron.Neuron.2016 Aug 3;91(3):574-86. doi: 10.1016/j.neuron.2016.06.021. Epub 2016 Jun 30.
PMID 27373830

Japanese Journal

多発筋炎に重症筋無力症を同時期に合併した1症例

櫻木志津,三谷紀之,田中芳紀 [他],松井久末子,松田万幸,篠原健次,平田郁雄
山口医学 54(2・3), 57-61, 2005-06-30
68歳, 女性.2ヵ月前より両大腿筋肉痛, 筋力低下, 両肩・両膝関節痛が出現し, 立ち上がり, 歩行が困難になった.同時期より眼瞼下垂, 上下肢の易疲労性を認めた.抗核抗体は陽性, 抗アセチルコリンレセプター抗体は著明に高値, 抗Jo-1抗体は陰性であった.エドロフォニウムテストにより眼瞼下垂は改善したが, 上下肢の筋力は改善しなかった.一方CKは上昇し大腿筋生検では筋線維の不揃いの変性, 著明 …
NAID 110002774399

9)コリンエステラーゼ阻害薬(マイテラーゼ:Ambenonium Chloride)による重症筋無力症の治療中に顕性化した冠攣縮性狭心症の1例

吉井豊史,鈴木誠,大木元明義,大塚知明,佐々木修,長岡祥宣,日浅豪,池田俊太郎,橋田英俊,原裕二,大蔵隆文,重松裕二,濱田希臣,日和田邦男
Japanese circulation journal 63(supple2), 776, 1999-08-20
NAID 110002559061

Comparative Pharmacokinetics of Four Cholinesterase Inhibitors in Rats

山本康次郎,澤田康文,伊賀立二
Biological & pharmaceutical bulletin 18(9), 1292-1295, 1995-09-15
… Pharmacokinetics of a very short-acting, a short-acting and two long-acting cholinesterase (ChE) inhibitors, edrophonium, neostigmine, pyridostigmine and ambenonium, respectively, were compared to elucidate the major determinant of their pharmacokinetics. … No dose-dependency in pharmacokinetic behavior was observed within the range of 2-10 μmol/kg for edrophonium, 0.5-2 μmol/kg for pyridostigmine, 0.1-0.5 μmol/kg for neostigmine and 0.3-3 μmol/kg for ambenonium, respectively. …
NAID 110003641043

Related Pictures

★リンクテーブル★

リンク元	「アンベノニウム」
拡張検索	「ambenonium chloride」

「アンベノニウム」

Ambenonium chloride
Systematic (IUPAC) name
	2,2'-[(1,2-Dioxoethane-1,2-diyl)diimino]bis[N-(2-chlorobenzyl)-N,N-diethylethanaminium]
Clinical data
Drugs.com	Consumer Drug Information
MedlinePlus	a699058
Routes of; administration	Oral
Pharmacokinetic data
Bioavailability	Low
Identifiers
CAS Number	7648-98-8
ATC code	N07AA30 (WHO)
PubChem	CID 8288
DrugBank	DB01122
ChemSpider	7987
UNII	L16PUN799N
KEGG	D01001
ChEBI	CHEBI:2628
ChEMBL	CHEMBL1652
Chemical data
Formula	C28H42Cl2N4O2+2
Molar mass	537.564 g/mol
	SMILES [Cl-].[Cl-].Clc1ccccc1C[N+](CC)(CC)CCNC(=O)C(=O)NCC[N+](Cc2ccccc2Cl)(CC)CC ;
	InChI InChI=1S/C28H40Cl2N4O2.2ClH/c1-5-33(6-2,21-23-13-9-11-15-25(23)29)19-17-31-27(35)28(36)32-18-20-34(7-3,8-4)22-24-14-10-12-16-26(24)30;;/h9-16H,5-8,17-22H2,1-4H3;2*1H ; Key:DXUUXWKFVDVHIK-UHFFFAOYSA-N ;
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