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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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English Journal

Effect of reversible ligands on oxime-induced reactivation of sarin- and cyclosarin-inhibited human acetylcholinesterase.

Scheffel C1, Thiermann H1, Worek F2.
Toxicology letters.Toxicol Lett.2015 Feb 3;232(3):557-65. doi: 10.1016/j.toxlet.2014.12.009. Epub 2014 Dec 15.
Poisoning by organophosphorus compounds (OP) used as pesticides and nerve agents is due to irreversible inhibition of the enzyme acetylcholinesterase (AChE). Oximes have been widely recognized for their potency to reactivate the inhibited enzyme. The limited efficacy of currently available oximes ag
PMID 25522658

Predominant Glandular Cholinergic Dysautonomia in Patients with Primary Sjögren's Syndrome.

Imrich R1, Alevizos I, Bebris L, Goldstein DS, Holmes CS, Illei GG, Nikolov NP.
Arthritis & rheumatology (Hoboken, N.J.).Arthritis Rheumatol.2015 Jan 26. doi: 10.1002/art.39044. [Epub ahead of print]
Objectives: The autonomic nervous system (ANS) modulates exocrine gland function. Available data show poor correlation between the degree of exocrine gland function and destruction in primary Sjögren's syndrome (pSS) suggesting other mechanisms, such as autonomic dysfunction may be important in the
PMID 25622919

To Evaluate the Effect of Edrophonium on Blood Glucose Levels in Euglycemic Albino Rats Through OGTT.

Amoghimath S1, Suresha RN2, Jayanthi MK3, Shruthi SL1, Vaibhavi P1, Satish AM4, Pushpa VH4, Kalabharathi HL4.
Journal of clinical and diagnostic research : JCDR.J Clin Diagn Res.2015 Jan;9(1):FF04-7. doi: 10.7860/JCDR/2015/11073.5452. Epub 2015 Jan 1.
OBJECTIVE: To evaluate the effect of Edrophonium on blood glucose levels in euglycemic albino rats through OGTT.MATERIALS AND METHODS: Twelve Swiss albino rats weighing around 150-200 gms of either sex were randomly selected from the central animal facility, JSSMC, Mysore and divided into two groups
PMID 25738004

Japanese Journal

抗MuSK抗体陽性全身型重症筋無力症の抗コリンエステラーゼ薬の効果

小西哲郎,高坂雅之,山川健太郎,松井大,太田潔江
臨床神経学 49(10), 660-663, 2009-10-01
NAID 10026290576

閉口障害を契機に診断された重症筋無力症の2例

齋藤高,浅田洸一,臼井弘幸,豊田長隆,栃原しほみ,石橋克禮
日本口腔外科学会雑誌 54(5), 339-343, 2008-05-20
… Finally, they were given a diagnosis of MG by a neurologist on the basis of the Tensilon test.<BR>Oral surgeons have to consider MG in patients who have masticatory dysfunction with ocular symptoms. …
NAID 10027088726

Related Pictures

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★リンクテーブル★

リンク元

「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
CASRN	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 ;
(verify)

　　[★]

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

[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

検索

案内

案内

Tensilon