フラゾリドン 化学特性,用途語,生産方法
外観
黄色, 結晶性粉末～粉末
溶解性
N,N -ジメチルホルムアミドに溶け、水にほとんど溶けない。
用途
フラゾリドンは細菌や原虫感染による下痢や腸炎の治療に使用される。
フラゾリドンは養殖業で使用される。
効能
抗菌薬, 抗原虫薬
説明
Furazolidone belongs to the group of nitro furans. This
antimicrobal (antibacterial and antiprotozoal) agent is
used in veterinary medicine both topically and orally,
particularly in animal feed. Reactions have been
reported in workers exposed to it by contact with
animal feed. Cross reactions with other nitrofuran
derivatives are rare.
化学的特性
solid
使用
The minimum inhibitory concentration of furazolidone was assessed to study the nonreplicating persistence of
M. tuberculosis in aerobic and anaerobic conditions using luminescence-based low-oxygen-recovery assay.
定義
ChEBI: A member of the class of oxazolidines that is 1,3-oxazolidin-2-one in which the hydrogen attached to the nitrogen is replaced by an N-{[(5-nitro-2-furyl)methylene]amino} group. It has antibacterial and antiprotozoal properties, and is us
d in the treatment of giardiasis and cholera.
世界保健機関（WHO）
Furazolidone, a nitrofuran derivative with antibacterial and
antiprotozoal activity, was introduced in 1954. In the 1970s it was shown to have a
carcinogenic potential following long-term administration to experimental animals.
However, the relevance of this to short-term therapy in man has not been
established. The risk-benefit assessment varies and furazolidone remains widely
available in many countries for the treatment of diarrhoea and enteritis.
抗菌性
It is active against a wide range of enteric pathogens,
including Salmonella enterica, Shigella spp., enterotoxigenic
Escherichia coli, Campylobacter jejuni, Aeromonas hydrophila,
Plesiomonas shigelloides, Vibrio cholerae and V. parahaemolyticus.
Yersinia enterocolitica is intrinsically resistant. Furazolidone
is also active against the protozoa Giardia lamblia
and
Trichomonas vaginalis.
獲得抵抗性
Acquired resistance has been observed in V. cholerae O1
and O139, S. enterica serotypes Typhi and Enteritidis,
A. hydrophila and Shigella spp. Such resistance may be
transferable, and there is cross-resistance with nitrofurantoin.
Many of these reports come from the Indian subcontinent,
where furazolidone is used widely for treating
diarrheal diseases.
一般的な説明
Furazolidone is an effective antiprotozoal and antibacterial agent.
危険性
A questionable carcinogen, use has been
restricted.
応用例（製薬）
A non-ionic synthetic compound, available for oral use only.
It is poorly soluble in water (40 mg/L) and ethanol (90 mg/L),
but dissolves well in dimethylformamide (10 g/L). It decomposes
in the presence of alkali.
接触アレルゲン
Furazolidone belongs to the group of nitrofurans. This
antimicrobial (antibacterial and antiprotozoal) agent is
used in veterinary medicine both topically and orally,
particularly in animal feed. Reactions are reported in
workers exposed to it in animal feeds. Cross-reactions
with other nitrofuran derivatives are rare.
薬物動態学
There is substantial absorption (65–70%) after oral administration,
but the drug is heavily metabolized, so that only
about 5% of the material excreted is microbiologically active.
A dose of 5 mg/kg achieves a maximum plasma concentration
of around 1 mg/L. Protein binding is about 30%. Intact drug
can be found in various body fluids in concentrations approximating
to the minimum inhibitory concentration (MIC)
for various intestinal pathogens. Less than 1% of the drug is
excreted into urine.
臨床応用
Furazolidone is used in gastrointestinal infections and vaginitis.
It is mainly used in developing countries to treat diarrheal
diseases of varying etiology, but it is not the drug of choice
if a specific pathogen has been identified. Use as a secondline
agent in giardiasis and as part of multidrug regimens in
Helicobacter infection has been advocated.
副作用
Most reported side effects are mild and only rarely cause discontinuation
of treatment. Nausea and vomiting are experienced
by around 8% of patients. Other adverse events include
neurological reactions (mainly headache; 1.3% of patients),
‘systemic’ reactions such as fever and malaise (0.6%) and skin rashes (0.54%). Administration of furazolidone may give rise
to inhibition of monoamine oxidase, and disulfiram-like reactions
have been reported.
安全性プロファイル
Poison by ingestion and
intraperitoneal routes. Human systemic
effects by ingestion: dyspnea, respiratory
depression, and eosinophilta. Experimental
reproductive effects. Human mutation data
reported. Questionable carcinogen. When
heated to decomposition it emits toxic
fumes of NOx.
フラゾリドン 上流と下流の製品情報
原材料
準備製品