查看Ch61 Antifungal Agents的源代码

== Topical Antifungal Agents (外用抗真菌药) ==

* '''Topical Imidazoles and Triazoles''' (外用咪唑类和三唑类)
** Clotrimazole (克霉唑)
** Econazole (益康唑)
** Efinaconazole (艾氟康唑)
** Miconazole (咪康唑)
** Luliconazole (卢立康唑)
** Terconazole and Butoconazole (特康唑和布托康唑)
** Tioconazole (噻康唑)
** Oxiconazole, Sulconazole, and Sertaconazole (奥昔康唑、磺康唑和舍他康唑)
** Ketoconazole (酮康唑)
* '''Structurally Diverse Antifungal Agents''' (结构多样的抗真菌剂)
** Ciclopirox Olamine (环吡酮乙醇胺)
** Haloprogin （盐丙蛋白）
** Tolnaftate (托萘酯)
** Naftifine (萘替芬)
** Terbinafine (特比萘芬)
** Butenafine (布特萘芬)
** Tavaborole (他伐硼罗)
** Nystatin (制霉菌素)
** Undecylenic Acid (十一烯酸)
** Benzoic and Salicylic Acids (苯甲酸和水杨酸)

=== Miconazole (咪康唑) ===

Miconazole readily penetrates the stratum corneum of the skin and persists for more than 4 days after application. Adverse effects from topical application to the vagina include burning, itching, or irritation in about 7% of recipients, as well as infrequent pelvic cramps (0.2%), headache, hives, or skin rash. Irritation, burning, and maceration are rare after cutaneous application. Miconazole is considered safe for use during pregnancy, although some experts advocate avoiding vaginal use during the first trimester.

咪康唑很容易渗透皮肤的角质层，并在应用后持续 4 天以上。局部应用于阴道的不良反应包括约 7% 的受者灼热、瘙痒或刺激，以及不频繁的盆腔痉挛 （0.2%）、头痛、荨麻疹或皮疹。皮肤应用后刺激、灼痛和浸渍很少见。咪康唑被认为在怀孕期间可以安全使用，尽管一些专家主张在妊娠早期避免阴道使用。

<b style=color:#0cf>【注】</b>咪康唑属咪唑类抗真菌药，咪唑类药物原理皆为：使14 - 脱甲基酶系失活，导致麦角固醇（真菌细胞膜重要成分）合成受阻。


'''Therapeutic Uses''': Miconazole nitrate is available as a 2% cream, ointment, lotion, powder, gel, aerosol powder, and aerosol solution. To avoid maceration, only the lotion should be applied to intertriginous areas. Miconazole is available as a 2% and 4% vaginal cream and as 100-, 200-, or 1200-mg vaginal suppositories to be applied high in the vagina at bedtime for 7 or 3 days or 1 day, respectively. In the treatment of tinea pedis, tinea cruris, and tinea versicolor, the cure rate exceeds 90%. In the treatment of vulvovaginal candidiasis, the mycological cure rate at the end of 1 month is about 80% to 95%. Pruritus sometimes is relieved after a single application. Some vaginal infections caused by C. glabrata also respond to this drug.

'''治疗用途'''：硝酸咪康唑以 2% 乳膏、软膏、化妆水、粉末、凝胶、气雾剂粉末和气雾剂溶液的形式提供。为避免浸渍，只能将化妆水涂抹在擦伤区域。咪康唑有 2% 和 4% 阴道乳膏以及 100、200 或 1200 mg 阴道栓剂两种，睡前涂抹于阴道高位，分别持续 7 天或 3 天或 1 天。在治疗足癣、股癣和花斑癣时，治愈率超过 90%。在治疗外阴阴道念珠菌病时，1个月结束时的真菌学治愈率约为80%至95%。瘙痒有时会在一次应用后缓解。一些由 C. glabrata 引起的阴道感染也对这种药物有反应。

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=== Naftifine (萘替芬) ===

Naftifine is a synthetic allylamine that inhibits squalene-2,3-epoxidase, a key enzyme in the fungal biosynthesis of ergosterol. The drug has broad-spectrum fungicidal activity in vitro. Naftifine hydrochloride is available as a 1% cream or gel. It is effective for the topical treatment of tinea cruris and tinea corporis; twice-daily application is recommended. The drug is well tolerated, although local irritation in 3% of treated patients and allergic contact dermatitis have been reported. Naftifine also may be efficacious for cutaneous candidiasis and tinea versicolor, although the drug is not approved for these uses.

Naftifine (萘替芬) 是一种合成的烯丙胺，可抑制角鲨烯-2,3-'''环氧化物酶'''，角鲨烯-2,3-环氧化物酶是''麦角固醇''真菌生物合成中的关键酶。该药物在体外具有广谱杀真菌活性。盐酸萘替芬有 1% 乳膏或凝胶形式。它对股癣和体癣的局部治疗有效；建议每天使用两次。该药物耐受性良好，尽管已报道 3% 的接受治疗的患者出现局部刺激和过敏性接触性皮炎。萘替芬也可能对皮肤念珠菌病和花斑癣有效，尽管该药物未被批准用于这些用途。

<b style=color:#0cf>【注】</b>烯丙胺类抗真菌药物原理为：其抑制真菌<b style='color:#f80'>角鲨烯环氧化酶</b>，从而减少<b style='color:#f80'>麦角固醇</b>（<b style='color:#0b0'>真菌细胞膜重要成分，其与磷脂结合增加膜的稳定性，缺乏则膜会破损</b>）的生物合成。

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=== Terbinafine (特比萘芬) ===

Like naftifine, terbinafine is an allylamine that targets ergosterol biosynthesis. Terbinafine 1% cream or spray, applied twice daily, is effective in tinea corporis, tinea cruris, and tinea pedis. Terbinafine is less active against Candida species and Malassezia furfur, but the cream also can be used in cutaneous candidiasis and tinea versicolor.

与萘替芬一样，特比萘芬是一种靶向'''麦角固醇'''生物合成的烯丙胺。1% 特比萘芬乳膏或喷雾剂，每天两次，对体癣、股癣和足癣有效。特比萘芬对念珠菌属和糠秕马拉色菌的活性较低，但该乳膏也可用于皮肤念珠菌病和花斑癣。

<b style=color:#0cf>【注】</b>典型烯丙胺类抗真菌药

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