スルファチアゾール 化学特性,用途語,生産方法
外観
白色, 結晶性粉末〜粉末
溶解性
アセトンに溶け、水及びエタノールにほとんど溶けない。
解説
スルファチアゾール,融点200～204 ℃(柱状晶)，175 ℃(六角板状晶)．pKa1 2.1，pKa2 7.43(20 ℃)．効力は強いが全身的な毒性もやや強く，使用法が制限されている．
森北出版「化学辞典（第2版）
応用
肺炎菌，淋(りん)菌，ぶどう状球菌などの感染症に内服またはナトリウム塩を注射する．
効能
抗菌薬, 葉酸合成阻害薬
製造
スルファチアゾール,2-アミノチアゾールとアセチルスルファニルクロリドから合成する．
化学的特性
white to cream powder
使用
Sulfonamide antibacterial.
定義
ChEBI: A 1,3-thiazole compound having a 4-aminobenzenesulfonamido group at the 2-position.
世界保健機関（WHO）
Sulfathiazole, a sulfonamide anti-infective agent, was introduced
more than 25 years ago for the treatment of bacterial infections. The importance of
sulfonamides has subsequently decreased as a result of increasing bacterial
resistance and their replacement by antibiotics which are generally more active
and less toxic. The sulfonamides are known to cause serious adverse effects such
as renal toxicity, sometimes fatal exfoliative dermatitis and erythema multiforma
and dangerous adverse reactions affecting blood formation such as
agranulocytosis and haemolytic or aplastic anaemia. Although preparations remain
available, use of the drug has been discontinued in many countries.
一般的な説明
White crystalline powder. Is dimorphous: form I is consists of prismatic rods and form II of six-sided plates and prisms. Insoluble in water and soluble in dil aqueous acid and aqueous base.
空気と水の反応
May be sensitive to heat, air and light during long-term storage . Insoluble in water.
反応プロフィール
Sulfathiazole is an amino acid.
火災危険
Flash point data for Sulfathiazole are not available, but Sulfathiazole is probably combustible.
応用例（製薬）
2-Sulfanilamidothiazole. A short-acting compound (half-life
c. 4 h) with relatively high activity. Protein binding is c. 75%.
Its use has declined because of a high incidence of side effects.
It is one of the constituents of triple sulfonamide mixtures, of
which local preparations are still available.
Two compounds, phthalylsulfathiazole (sulfathalidine) and
succinylsulfathiazole (sulfasuxidine) owe their activity to the
slow liberation of sulfathiazole in the bowel. They are poorly
soluble and very little is absorbed after oral administration.
They were formerly used in the treatment of intestinal infections
and in bowel preparation before surgery. They are available
in multi-ingredient preparations in some countries.
安全性プロファイル
Human poison by
unspecified route. Experimental poison by
intraperitoneal route, Moderately toxic by
intravenous, subcutaneous, and parenteral
routes. Mildly toxic by ingestion. Human
systemic effects by unspecified route:
conjunctiva irritation, tubule changes, and
allergic skin dermatitis. Experimental
reproductive effects. Questionable
carcinogen with experimental tumorigenic
data, Mutation data reported. When heated
to decomposition it emits very toxic fumes
of NOx and SOx.
スルファチアゾール 上流と下流の製品情報
原材料
準備製品