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益康唑:其抗真菌活性与治疗效果综述

Econazole: a review of its antifungal activity and therapeutic efficacy.

作者信息

Heel R C, Brogden R N, Speight T M, Avery G S

出版信息

Drugs. 1978 Sep;16(3):177-201. doi: 10.2165/00003495-197816030-00001.

Abstract

Econazole1 is a recently introduced imidazole antifungal agent which is very closely related structurally to another imidazole derivative, miconazole. For local application the nitrate salt of econazole is used, while in preliminary investigations of systemic use in a few patients econazole base has been administered orally or intravenously. In uncontrolled studies in large numbers of patients, econazole nitrate has been administered topically in the treatment of dermatomycoses due to a wide variety of fungi, and vaginally in the treatment of vaginal candidosis; but it has not been compared with any other antifungal drug in controlled therapeutic trials in mycoses of the skin and has only been compared with nystatin in a few patients with vaginal candidosis. Until adequate comparative studies are done the relative place of econazole in the treatment of dermatomycoses and vaginal condidosis, compared with traditional antifungal agents and with other imidazole derivatives such as miconazole or clotrimazole, cannot be clearly stated. Nevertheless, econazole nitrate is an effective antifungal drug. In dermatological studies about 90% of a large number of patients were cured, often after a relatively short treatment period (2 to 6 weeks, as occurs with other imidazole antifungal agents). The cure rate was only slightly lower (about 85%) in patients with severe mycoses of many years' duration than in those whose infections were of more recent onset. In vaginal candidosis a 3-day treatment regimen using a 150mg suppository once daily was only slightly less effective (85% mycological cure rate) than a 15-day regimen using a 50mg dose (suppository or cream) once daily (90% cure rate). A 3 to 5 day 'higher' dose regimen was slightly more effective than a standard 15-day regimen of nystatin vaginal inserts in a small group of patients with vaginal candidosis. The convenience of the higher-dose shorter term regimen would likely be an important advantage to most patients. Whether other agents useful in vaginal candidosis would be as effective as econazole were they to be used in this way, has not been determined. Topical or intravaginal econazole nitrate has usually been well tolerated, side effects being limited to local irritation in about 1 to 4% of patients in most studies.

摘要

益康唑1是一种最近推出的咪唑类抗真菌药,在结构上与另一种咪唑衍生物咪康唑密切相关。局部应用时使用益康唑硝酸盐,而在少数患者的全身应用初步研究中,益康唑碱已通过口服或静脉给药。在大量患者的非对照研究中,硝酸益康唑已局部用于治疗由多种真菌引起的皮肤癣菌病,以及阴道给药治疗阴道念珠菌病;但在皮肤真菌病的对照治疗试验中,它尚未与任何其他抗真菌药物进行比较,在少数阴道念珠菌病患者中仅与制霉菌素进行了比较。在与传统抗真菌药物以及其他咪唑衍生物(如咪康唑或克霉唑)进行比较的充分研究完成之前,无法明确益康唑在治疗皮肤癣菌病和阴道念珠菌病中的相对地位。然而,硝酸益康唑是一种有效的抗真菌药物。在皮肤病学研究中,大量患者中约90%得到治愈,通常在相对较短的治疗期后(2至6周,其他咪唑类抗真菌药物也如此)。病程长达数年的严重真菌病患者的治愈率仅略低于近期感染患者(约85%)。在阴道念珠菌病中,每天使用一次150mg栓剂的3天治疗方案的疗效(真菌治愈率85%)仅略低于每天使用一次50mg剂量(栓剂或乳膏)的15天治疗方案(治愈率90%)。在一小部分阴道念珠菌病患者中,3至5天的“高剂量”方案比制霉菌素阴道栓剂的标准15天方案略有效。高剂量短期方案的便利性对大多数患者来说可能是一个重要优势。其他对阴道念珠菌病有用的药物以这种方式使用是否会与益康唑一样有效,尚未确定。局部或阴道内使用硝酸益康唑通常耐受性良好,在大多数研究中,副作用仅限于约1%至4%的患者出现局部刺激。

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