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効能
解毒薬 (クラーレ原理), 診断薬 (重症筋無力症)
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商品名
アンチレクス (杏林製薬)
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化学的特性
White or almost white, crystalline powder
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使用
Pharmacologically, edrophonium is also similar to neostigmine; however, it begins to act
quicker and is shorter lasting.
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使用
A reversible Acetylcholinesterase inhibitor.
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定義
ChEBI: The chloride salt of edrophonium. A reversible inhibitor of cholinesterase with a rapid onset (30-60 seconds after injection) but a short duration of action (5-15 minutes), it is used in myasthenia gravis both diagnostically and to distinguish between unde
- or over-treatment with other anticholinesterases. It has also been used for the reversal of neuromuscular blockade in anaesthesia, and for the management of poisoning due to tetrodotoxin, a neuromuscular blocking toxin found in puffer fish and other mari
e animals.
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一般的な説明
Edrophonium chloride,ethyl(m-hydroxyphenyl)dimethylammonium chloride(Tensilon), is a reversible anticholinesterase agent. It isbitter and very soluble in water and alcohol. Edrophoniumchloride injection has a pH of 5.2 to 5.5. On parenteral administration,edrophonium has a more rapid onset andshorter duration of action than neostigmine, pyridostigmine,or ambenonium. It is a specific anticurare agent andacts within 1 minute to alleviate overdose of d-tubocurarine,dimethyl d-tubocurarine, or gallamine triethiodide.
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臨床応用
Edrophonium Chloride is also used to terminate the action of any one ofthese drugs when the physician so desires. It is of no value,however, in terminating the action of the depolarizing (i.e.,noncompetitive) blocking agents, such as decamethoniumand succinylcholine. In addition to inhibiting AChE, edrophoniumchloride has a direct cholinomimetic effect onskeletal muscle, which is greater than that of most otheranticholinesterase drugs.
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合成
Edrophonium, ethyl-(3-hydroxyphenyl)dimethylammonium chloride
(13.2.13), is made by reacting 3-dimethylaminophenol with ethylbromide, which forms
ethyl(3-hydroxyphenyl)dimethylammonium bromide (13.2.12), the bromine atom of
which is replaced with a chlorine atom by reacting it with silver chloride, giving edrophonium (13.2.13) [45].
