モメタゾンフランカルボン酸エステル 化学特性,用途語,生産方法
外観
白色～うすい黄色粉末～結晶
効能
喘息治療薬, 抗炎症薬, グルココルチコイド受容体作動薬
商品名
アズマネックス (MSD); フルメタ (シオノギファーマ)
説明
Mometasone furoate is a topical steroidal antiinflammatory useful in the treatment of
corticosteroid-responsive dermatoses. As a steroidal antiinflammatory of grade II
potency, mometasone furoate is characterized by a once-daily dose regimen and a
relatively wide safety margin.
化学的特性
White-to-Off-White Solid
使用
Mometasone furoate is a deuterated topical corticosteroid used as an anti-inflammatory. Mometasone furoate has been used to study its effect on Leishmania major amastigotes. It could as labeled Mometasone, intended for use as an internal standard for the quantification of Mometasone by GC- or LC-mass spectrometry. Formulations containing mometasone furoate have been used in the treatment of allergic rhinitis, atopic dermatitis, and asthma. Intranasal administration of mometasone furoate (1 μg/nostril) reduces the frequency of sneezing and nasal rubbing in a rat model of histamine-induced allergic rhinitis. Topical application of mometasone furoate reduces croton oil-induced ear edema in mice (ED50 = 0.31 μg/ml).
生物学の機能
Mometasone furoate has strong local
anti-inflammatory activity equivalent to that of fluticasone propionate. It has a quick onset of action relative to
the other inhaled/intranasal steroids with the least systemic availability and, consequently, the fewest systemic
side effects.
一般的な説明
Mometasone furoate (Asmanex,Nasonex) undergoes extensive metabolism to multiplemetabolites. No major metabolites are detectable in humanplasma after oral administration, but the 6β-hydroxy metaboliteis detectable by use of human liver microsomes. Thismetabolite is formed via the CYP3A4 pathway.
作用機序
Mometasone furoate is the most recent glucocorticoid to be developed and commercialized. It has
a number of unique functional groups that confer enhanced glucocorticoid activity as well as
pharmacokinetic advantages. The combination of the C-21 chloro and the furoic acid ester at
C-17 results in the highest glucocorticoid receptor affinity of any topical corticosteroid. The 16α-
methyl decreases the mineralocorticoid effects, and the 9α-chloro group increases both
glucocorticoid and mineralocorticoid activities. Inhaled mometasone furoate acts locally as an
anti-inflammatory treatment for asthma and has the least systemic bioavailability of all the
inhaled glucocorticoids (<1%).
臨床応用
Mometasone furoate was originally marketed as a topically applied corticosteroid, but because of its low
systemic bioavailability, it was found to be more useful in the treatment of allergic disorders and lung diseases
(107).
代謝
It is extensively metabolized, with 6β-hydroxymometasone and
21-hydroxymometasone being found among the metabolites. Inhaled mometasone furoate in
mainly excreted in the feces (~74%) as metabolites and only minimally excreted in the urine
(~8%). It has a relatively long half-life in the lung and is administered once daily, usually in the
evening.
モメタゾンフランカルボン酸エステル 上流と下流の製品情報
原材料
準備製品