药品信息:
--------------------------------------------------------------- 部分中文卓兰处方资料(仅供参考)
【药品名称】
通用名:硝酸舍他康唑乳膏
商品名:卓兰Zalain
英文名:Sertaconazole Nitrate Cream 卓兰
汉语拼音:Xiaosuan Shetakangzuo Rugao
【成 份】本品主药成份为硝酸舍他康唑
【有 效 期】 36个月。
【性 状】本品为白色或类白色乳膏
【适 应 症】由皮真菌、酵母菌、念珠菌、曲霉菌引起的皮肤感染,如:体股癣、足癣。
【规 格】10g:0.2g 硝酸舍他康唑
【用法用量】每日两次,把药膏适量涂于患病的皮肤部位,一般应连续用28天。
【不良反应】极少数病人用药后可出现皮肤发红、瘙痒、灼烧感,停药后自行消失。发生不良反应时应告知医生。
【禁 忌】对硝酸舍他康唑对本品任何成份或本品任何成份过敏者禁用。
【贮 藏】避光,密闭保存。
Sertaconazole nitrate (Ertaczo, Dermofix) is an antifungal medication of the imidazole class. It is available as a cream to treat skin infections such as athlete's foot.
It is also available in a vaginal tablet form. The most popular of these is Gyno-Dermofix.
Mechanism of action
Sertaconazole has several known mechanisms of action. It is considered fungistatic, fungicidal, antibacterial, antiinflammatory, antitrichomonal, and antipruritic.
Like other imidazole antifungals, sertaconazole blocks the synthesis of ergosterol by inhibiting the 14α-demethylase enzyme. Ergosterol is a critical component of the fungal cell membrane. Inhibition of ergosterol synthesis prevents fungal cells from multiplying and impairs hyphae growth.
Chemically, sertaconazole contains a benzothiophene ring which makes it unique from other imidazole antifungals. A benzothiophene ring is a sulfur analogue of the indole ring found in the amino acid tryptophan. Tryptophan is found in the fungal membrane in addition to lipids such as ergosterol. The benzothiophene ring in sertaconazole mimics tryptophan and increases the drugs ability to form pores in the fungal cell membrane. If the cell membrane is made sufficiently leaky by these pores the fungal cell will die from loss of ATP and other effects which can include calcium disregulation. These pores are believed to open at about 10 minutes following topical application of sertaconazole. One hour following topical application, approximately 90% of fungal cells die from lack of energy (due to ATP loss) and general loss of homeostasis. Sertaconazole is thought to be the only imidazole antifungal with this mechanism of action.
Sertaconazole has also antiinflammatory and antipruritic action. It inhibits the release of proinflammatory cytokines from activated immune cells. It has been shown that sertaconazole activatates of the p38/COX2/PGE2 pathway. PGE2 can have a variety of important effects in the body including activation of the body's fever response.
Sertaconazole also has antibacterial action. It is hypothesized that the mechanism of action again involves sertaconazole's ability to form pores by mimicking tryptophan.
It has also been shown that sertaconazole can kill Trichomonas vaginalis in vitro. The exact mechanism of action is as yet unknown.
Sertaconazole also appears to inhibit the dimorphic transformation of Candida albicans into pathogenic fungi.
Side effects
Side effects were rarely reported with sertaconazole therapy, but may include contact dermatitis, burning on application site and skin dryness.
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