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any compound containing a chlorine atom
any salt of hydrochloric acid (containing the chloride ion)

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塩化物

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/06/21 02:35:45」(JST)

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Edrophonium is a readily reversible acetylcholinesterase inhibitor. It prevents breakdown of the neurotransmitter acetylcholine and acts by competitively inhibiting the enzyme acetylcholinesterase, mainly at the neuromuscular junction. It is sold under the trade names Tensilon and Enlon (according to FDA Orange Book).

Clinical uses

Edrophonium (by the so-called Tensilon test) is used to differentiate myasthenia gravis from cholinergic crisis and Lambert-Eaton myasthenic syndrome. In myasthenia gravis, the body produces autoantibodies which block, inhibit or destroy nicotinic acetylcholine receptors in the neuromuscular junction. Edrophonium—an effective acetylcholinesterase inhibitor—will reduce the muscle weakness by blocking the enzymatic effect of acetylcholinesterase enzymes, prolonging the presence of acetylcholine in the synaptic cleft. It binds to a Serine-103 allosteric site, while pyridostigmine and neostigmine bind to the AchE active site for their inhibitory effects. In a cholinergic crisis, where a person has too much neuromuscular stimulation, edrophonium will make the muscle weakness worse by inducing a depolarizing block.

Lambert-Eaton myasthenic syndrome (LEMS), is similar to myasthenia gravis in that it is an autoimmune disease. However, in LEMS the neuron is unable to release enough acetylcholine for normal muscle function due to autoantibodies attacking P/Q-type calcium channel that are necessary for acetylcholine release. This means there is insufficient calcium ion influx into presynaptic terminal resulting in reduced exocytosis of acetylcholine containing vesicles. Consequently, there will typically be not as much increase in muscle strength observed after edrophonium injection, if any with LEMS.

The drug may also be used for postoperative decurarization.^[1]

Chemistry

Edrophonium, ethyl-(3-hydroxyphenyl)dimethylammonium chloride, is made by reacting 3-dimethylaminophenol with ethyl bromide, which forms ethyl(3-hydroxyphenyl)dimethylammonium bromide, the bromine atom of which is replaced with a chlorine atom by reacting it with silver chloride, giving edrophonium.

J.A. Aeschlimann, A. Stempel, U.S. Patent 2,647,924 (1953).

Pharmacokinetics

The drug has a brief duration of action, about 10–30 mins.^[1]

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

Reference

^ ^a ^b KD Tripati MD. Essentials of Medical Pharmacology (fifth ed.). Jaypee Brothers Medical Publishers(P) Ltd. p. 84. ISBN 81-8061-187-6.

UpToDate Contents

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3. 重症筋無力症の鑑別診断 differential diagnosis of myasthenia gravis
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5. 重症筋無力症の治療 treatment of myasthenia gravis

English Journal

Discordant thymectomy in identical twins concordant for myasthenia gravis.

Riggs KR, Gutmann L, Riggs JE.AbstractBACKGROUND: Thymectomy is standard therapy fornonthymomatousmyasthenia gravis despite the absence of randomized clinical trials (1). Myasthenia gravis is uncommonly reported in monozygous twins; disease concordance occurs in approximately one third of such identical twin pairs; and treatment for myasthenia gravis, when described,is usually concordant in identical twin pairs (2).OBJECTIVE: To report an 11-year clinical course of a pair of identical twins concordant for generalized acetylcholine receptor antibody–positive nonthymomatous myasthenia gravis in whom only 1 was treated with extended transsternal thymectomy. CASE REPORT: Twin A was a 19-year-old white woman who presented with an 8-week history of intermittent leg weakness, causing her to fall during activities, such as climbing stairs. On examination,she had moderately severe fatigable proximal muscle weakness and ptosis. Her weakness improved with intravenous edrophonium administration.Initial binding acetylcholine receptor antibody titer was 1.22 nmol/L (normal value, 0.03 nmol/L). Repetitive 2-Hz nerve(median, ulnar, and facial) stimulation studies demonstrated up to a 16% decremental response. Chest computed tomography showed residual thymic tissue without thymoma. An extended transsternal thymectomy was performed 11 weeks after the onset of symptoms.
Annals of internal medicine.Ann Intern Med.2011 Oct 4;155(7):478-9.
BACKGROUND: Thymectomy is standard therapy fornonthymomatousmyasthenia gravis despite the absence of randomized clinical trials (1). Myasthenia gravis is uncommonly reported in monozygous twins; disease concordance occurs in approximately one third of such identical twin pairs; and treatment for mya
PMID 21969350

[Therapy for anti-MuSK antibody positive myasthenia gravis].

Pál Z, Boczán J, Bereznai B, Lovas G, Molnár MJ.SourceSemmelweis Egyetem, Általános Orvostudományi Kar, Neurológiai Klinika, Molekuláris Neurológiai Központ, Budapest.
Orvosi hetilap.Orv Hetil.2011 Sep 25;152(39):1586-9.
The authors report the case of a 27-year-old woman with muscle-specific receptor tyrosine kinase antibody positive myasthenia with predominantly ocular and bulbar symptoms. Both edrophonium and low dose (4×30 mg/day) pyridostigmin resulted in cholinergic side effects including fasciculation mainly
PMID 21920845

Japanese Journal

重症筋無力症合併多発肺癌に同時手術を施行した1例

片岡和彦,藤原俊哉,松浦求樹,妹尾紀具
肺癌 49(3), 273-277, 2009
背景．重症筋無力症（MG）に合併した肺癌の報告は少ない．症例．76歳の女性で，主訴は眼瞼下垂と下肢の脱力．エドロフォニウムの注射により筋力の改善を認めた．Sero-negative MGと診断された．胸部X線写真にて，右上肺野に異常影が認められた．胸部CTにて，右S1に3 cmのmixed ground glass opacity（GGO），右S3に1 cmのGGO，左S10に5 mmのGGOの3 …
NAID 130000123209

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,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

Related Pictures

★リンクテーブル★

リンク元	「エドロホニウム」
拡張検索	「edrophonium chloride test」
関連記事	「chloride」

「エドロホニウム」

Edrophonium
Systematic (IUPAC) name
	N-Ethyl-3-hydroxy-N,N-dimethylbenzenaminium
Clinical data
Trade names	Tensilon
AHFS/Drugs.com	FDA Professional Drug Information
Identifiers
CAS Number	116-38-1
ATC code	none
PubChem	CID 8307
DrugBank	DB01010
ChemSpider	8006
UNII	QO611KSM5P
KEGG	D00994
ChEBI	CHEBI:4759
ChEMBL	CHEMBL1128
Chemical data
Formula	C10H16NO+
Molar mass	166.24 g/mol
	SMILES [Cl-].Oc1cccc(c1)[N+](C)(CC)C ;
	InChI InChI=1S/C10H15NO.ClH/c1-4-11(2,3)9-6-5-7-10(12)8-9;/h5-8H,4H2,1-3H3;1H ; Key:BXKDSDJJOVIHMX-UHFFFAOYSA-N ;
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　　[★]

英: edrophonium
化: 塩化エドロホニウム edrophonium chloride
同: エドロフォニウム
商: アンチレクス、Enlon, Reverso, Tensilon テンシロン
関: 抗コリンエステラーゼ薬コリンエステラーゼ阻害薬。コリンエステラーゼ、ネオスチグミン

[show details]

エドロホニウム : 約 2,450 件
エドロフォニウム : 約 1,110 件

四級アンモニウム塩
作用の持続時間はneostigmineに比して短い (SPC.158)
テンシロンテストに利用される

薬理作用

可逆的コリンエステラーゼ阻害薬
(1)抗コリンエステラーゼ作用、(2)ニコチン性受容体に対するアセチルコリン様の直接刺激作用
骨格筋の線維束性攣縮を示す

「edrophonium chloride test」

　　[★]

同: Tensiion

同: Tensiion

「chloride」

　　[★] 塩素イオン　　　

[trip-1] KD Tripati MD. Essentials of Medical Pharmacology (fifth ed.). Jaypee Brothers Medical Publishers(P) Ltd. p. 84. ISBN 81-8061-187-6.

匿名

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案内

案内

edrophonium chloride