テルコナゾール 化学特性,用途語,生産方法
効能
抗真菌薬, エルゴステロール合成酵素阻害薬
説明
Terconazole is an antifungal agent somewhat more potent than clotrimazole and
useful in the topical treatment of vaginal dermatophytosis and candidiasis.
化学的特性
White or almost white powder.
使用
Terconazole belongs to a new chemical class of antifungal agents, the triazoles. Terconazole has a far greater selectively for yeast cytochrome P-450 than for mammalian microsomal cytochrome P-450 and is used as topical treatment of mycotic vaginitis. Terconazole may also be used in vitro as a potent antifungal agent to prevent the morphogenetic transformation of yeast into (pseudo-)mycelium form of Candida albicans.
適応症
Terconazole (Terazol) is a fungicidal triazole topical preparation effective
against many Candida strains. It is used as either a 3-day or a 7-day course
(Terazol 7—0.4% cream for 7 days or Terazol 3—0.8% cream for 3 days).
世界保健機関（WHO）
Terconazole, an antifungal agent, was introduced into medicine in
1980. It is indicated for the treatment of vaginal candidiasis. It is not yet clear
whether the adverse effects associated with high dose formulations are due to
terconazole itself, to an excipient in the preparation or to fungal constituent.
作用機序
Terconazole is effective for fungistatic action for many strains of Candida and dermatophytes. The exact mechanism of its action is unknown, although it inhibits the action of
the enzyme lanosterol 1-demethylase of cytochrome P-450 of sensitive fungi (similar to
other azols described above), causing a reduction in the amount of ergosterin, which is
necessary for the organisms to construct membranes and to retain the appropriate permeability. It is only used externally for treating vulvovaginal candidoses. Synonyms of this
drug are terazol, tercospor, and others.
臨床応用
cis-1-[4-[[2-(2,4-Dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl)methoxy]phenyl]-4-(1methylethyl)piperazine (Terazol), or terconazole, is a triazolederivative that is used exclusively for the control ofvulvovaginal moniliasis caused by C. albicans and otherCandida species. It is available in creams containing 0.4%and 0.8% of the free base intended for 7-day and 3-day treatmentperiods, respectively. Suppositories containing 80 mgof the free base are also available.
テルコナゾール 上流と下流の製品情報
原材料
準備製品