ベンズニダゾール 化学特性,用途語,生産方法
効能
抗原虫薬
説明
Benznidazole is the second of the drugs approved for treatment of Chagas' disease. Like
nifurtimox, it is effective against the circulating form of Trypanosoma cruzi during the acute phase
of the disease, but also like nifurtimox, it is ineffective during the chronic stage of the disease.
使用
Benznidazole (BNZ) is traditionally used to treat Chagas disease caused by Trypanosoma cruzi. The drugs used for the treatment of this disease, Nifurtimox and Benznidazole, are toxic and present sever
e side effects.
定義
ChEBI: A monocarboxylic acid amide obtained by formal condensation of the carboxy group of (2-nitroimidazol-1-yl)acetic acid with the aromatic amino group of benzylamine. Used for treatment of Chagas disease.
抗菌性
It exhibits antiprotozoal activity, particularly against Trypanosoma cruzi.
一般的な説明
N-Benzyl-2-nitro-1
H-imidazole-1-acetamide (Benznidazole) is a nitro-heterocyclic compound. It is widely employed drug for the treatment of Chagas disease. It exhibits three polymorphic forms..
応用例（製薬）
A synthetic 2-nitroimidazole, formulated for oral administration. Solubility in water 400 mg/L.
作用機序
Studies suggest that benznidazole does not catalyze the formation of ROS and, therefore, has a
mechanism of action different from that of nifurtimox. It has been proposed that benznidazole
undergoes an one-electron transfer to the nitro group, which in turn dismutates to give back the
nitroimidazole and a nitrosoimidazole. The latter product may then undergo an electrophilic
addition to trypanothione, which leads to depletion of trypanothione, an essential enzyme system
in the Trypanosoma cruzi.
薬物動態学
Oral bioavailability :High
Cmax 100 mg oral ：2.2–2.8 mg/L after 3–4 h
Plasma half-life：10.5–13.6 h
Volume of distribution：c. 0.56 L/kg
Plasma protein binding： c. 44%
The 2-nitro group undergoes reduction to the amine and hydrolysis to the hydroxy derivative.
臨床応用
Benznidazole is used in treatment of South American trypanosomiasis (Chagas disease).
副作用
Adverse effects are more common in the elderly and include nausea, vomiting, abdominal pain, peripheral neuropathy and severe skin reactions.
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