スルファドキシン 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。
用途
高速液体クロマトグラフ法によるスルファドキシン定量用標準品。
効能
抗菌薬, 抗マラリア薬, 葉酸合成阻害薬
説明
Sulfadoxin is a sulfonamide antibiotic that inhibits dihydropteroate synthetase (DHPS), an enzyme involved in folic acid synthesis. Sulfadoxin competes with 4-aminobenzoate (PABA), the native substrate of DHPS, and inhibits PABA incorporation into folic acid. Folate is essential for purine and pyrimidine synthesis, therefore, sulfadoxin has antiproliferative activity in non-resistant
P. falciparum. Sulfadoxin inhibits growth of
P. falciparum in vitro, but potency varies between non-resistant (IC
50 = 4 ng/ml) and resistant strains (IC
50 = 3,970 ng/ml).
化学的特性
White Crystalline Solid
定義
ChEBI: A sulfonamide consisting of pyrimidine having methoxy substituents at the 5- and 6-positions and a 4-aminobenzenesulfonamido group at the 4-position. In combination with the antiprotozoal pyrimethamine (CHEBI:8673) it is used as an antimalarial.
抗菌性
Its antibacterial activity is relatively poor. Used alone it has a
slow and uncertain effect against malaria parasites. Resistance
of malaria parasites to the combination with pyrimethamine is
common in many endemic areas.
応用例（製薬）
An ultra-long-acting sulfonamide. It is no longer prescribed alone,
but is used in combination with pyrimethamine as the antimalarial
agent Fansidar. It is poorly soluble in water.
薬理学
In terms of antibacterial action, this drug is analogous to other sulfanilamides; however, it
possesses very prolonged action. Its half-life is from 120 to 200 h. Sulfadoxine is used for
infectious diseases caused by microorganisms that are sensitive to the sulfanilamide drugs,
such as infections of respiratory organs, gastric and urinary tracts; purulent infections of
various localization, osteomyelitis, sinusitis, and other infections. It is used in combination
with antimalarial drugs. Synonyms of this drug are sulfarmethoxine, fanasil, and fansidar.
薬物動態学
Oral absorption ：Extensive
C
max 500 mg oral： c. 60 mg/L after 3–4 h
Plasma half-life：c.6 days
Volume of distribution：0.13 L/kg
Plasma protein binding：94%
The extremely long half-life allows administration at weekly
intervals. The acetyl metabolite has a similarly long half-life,
but sulfadoxine is less extensively metabolized than many
other sulfonamides.
臨床応用
Sulfadoxine is used only in combination with pyrimethamine.
副作用
Side effects are those common to the group. There have been
many reports of Stevens–Johnson syndrome following its use
and the combination with pyrimethamine is no longer recommended
for the prophylaxis of malaria.
スルファドキシン 上流と下流の製品情報
原材料
準備製品