アセタゾラミド 化学特性,用途語,生産方法
解説
アセタゾラミド，白色の結晶性粉末．分解点255 ℃．pKa 7.2．エタノール，水，エーテルに難溶，アルカリに可溶．炭酸脱水酵素阻害剤，利尿薬，妊娠中毒症，および緑内障治療薬として使用される．
森北出版「化学辞典（第2版）
用途
炭酸脱水酵素阻害剤です。炭 酸脱水酵素阻害作用を示します。
用途
炭酸脱水酵素阻害剤です。炭
酸脱水酵素阻害作用を示します。
用途
医薬(炭酸脱水素酵素抑制剤)
効能
抗緑内障薬, 炭酸脱水酵素阻害薬
製造
アセタゾラミド，5-アミノ-1,3,4-チアジアゾール-2-チオールをアセチル化後，塩素ガス，ついでアンモニアを作用させてスルホンアミドとして合成する．
毒性
LD50 3～6 g/kg(マウス，静注)．
商品名
ダイアモックス (三和化学研究所)
説明
Acetazolamide is a weak diuretic with limited use in edema associated with cardiac
insufficiency, glaucoma, minor epileptic attacks, and altitude sickness.
化学的特性
White Solid
使用
Acetazolamide is used for epilepsy in the absence of attacks and also in conjunction with
other antiepileptic drugs.
一般的な説明
White to yellowish-white fine crystalline powder. No odor or taste.
空気と水の反応
Insoluble in water.
反応プロフィール
A weak acid and a diazo derivative. Azo, diazo, azido compounds can detonate. This applies in particular to organic azides that have been sensitized by the addition of metal salts or strong acids. Toxic gases are formed by mixing materials of this class with acids, aldehydes, amides, carbamates, cyanides, inorganic fluorides, halogenated organics, isocyanates, ketones, metals, nitrides, peroxides, phenols, epoxides, acyl halides, and strong oxidizing or reducing agents. Flammable gases are formed by mixing materials in this group with alkali metals. Explosive combination can occur with strong oxidizing agents, metal salts, peroxides, and sulfides.
火災危険
Flash point data for Acetazolamide are not available; however, Acetazolamide is probably combustible.
作用機序
Acetazolamide is an aromatic sulfonamide used as a carbonic anhydrase inhibitor. It facilitates
production of alkaline urine with an elevated biocarbonate, sodium, and potassium ion concentrations.
By inhibiting carbonic anhydrase, the drug suppresses reabsorption of sodium ions
in exchange for hydrogen ions, increases reflux of bicarbonate and sodium ions and reduces
reflux of chloride ions. During this process, chloride ions are kept in the kidneys to cover of
insufficiency of bicarbonate ions, and for keeping an ion balance. Electrolytic contents of fluid
secreted by the kidneys in patients taking carbonic anhydrase inhibitors are characterized by
elevated levels of sodium, potassium, and bicarbonate ions and a moderate increase in water
level. Urine becomes basic, and the concentration of bicarbonate in the plasma is reduced.
臨床応用
Acetazolamide was the first of the carbonic anhydrase inhibitors to be introduced as an orally effective diuretic, with a diuretic effect that lasts approximately 8 to 12
hours. As mentioned earlier, its diuretic action is limited because of the systemic acidosis it produces. Acetazolamide
reduces the rate of aqueous humor formation and is used primarily for reducing intraocular pressure in the treatment of glaucoma. The dose is 250 mg to 1 g per day.
安全性プロファイル
Poison by subcutaneous and intravenous routes. Moderately toxic by intraperitoneal route. Human systemic effects by ingestion: dyspnea. An experimental teratogen by many routes. Other experimental reproductive effects. When heated to decomposition it emits very toxic fumes of NOx, and SOx,. A carbonic anhydrase inhibitor and dmretic used to treat glaucoma.
純化方法
It is recrystallised from water. [Roblin & Clapp J Am Chem Soc 72 4890 1950, Beilstein 27 III/IV 8219.]
アセタゾラミド 上流と下流の製品情報
原材料
アセチルクロリド
チオシアン酸アンモニウム
塩化スルフリル
N-(5-メルカプト-1,3,4-チアジアゾール-2-イル)アセトアミド
二亜硫酸二ナトリウム
Butanedioic acid,1-[1-[[(1-methylethyl)amino]methyl]-2-(1-naphthalenyloxy)ethyl] ester
Benzoic acid, 2-[[[[5-(acetylamino)-1,3,4-thiadiazol-2-yl]sulfonyl]amino]carbonyl]-, 1-[[(1-methylethyl)amino]methyl]-2-(1-naphthalenyloxy)ethyl ester
2-アミノ-1,3,4-チアジアゾール-5-スルホンアミド
N-[5-(フェニルメチルチオ)-1,3,4-チアジアゾール-2-イル]アセトアミド
2-(ACETAMIDO)-5-(CHLOROSULFONYL)-1,3,4-THIADIAZOLE
準備製品