Sawyer P R, Brogden R N, Pinder R M, Speight T M
Drugs. 1975;9(6):424-47. doi: 10.2165/00003495-197509060-00003.
Clotrimazole 2, a synthetic imidazole derivative, is primarily used locally in the treatment of vaginal and skin infections due to yeasts and dermatophytes. In vitro, it is most active against Candida spp., Trichophyton spp., Microsporum spp. and Malazzesia fuffur (Pityrosporon orbiculare). In addition, it has some in vitro activity against certain Gram-positive bacteria, and at very high concentrations has activity against Trichomonas spp. In the treatment of vaginal candidiasis, clotrimazole vaginal tablets have produced cure rates comparable with those of conventional nystatin vaginal tablets. There have been no published comparisons with nystatin vaginal cream or foaming vaginal tablets - nystatin dosage forms preferred by some clinicians. Cootrimazole has also been successful in patients who had failed to respond to other antifungal agents such as nystatin and amphotericin B. Results in trichomonal vaginitis are not impressive. Skin infections caused by Candida or dermatophytes have been effectively treated with topical application of clotrimazole. In comparative trials, clotrimazole cream has been as effective as Whitfield's ointment and tolnaftate in the treatment of dermatophytoses, and as effective as nystatin in cutaneous candidiasis. Clotrimazole topical preparations are generally well tolerated, but local irritation has necessitated withdrawal of therapy in a few cases. Candidal septicemia and urinary and pulmonary candidiasis have been cured with oral clotrimazole therapy. Results in other types of serious fungal infections, including pulmonary aspergillosis, have been disappointing. A limiting factor in oral clotrimazole therapy is the high incidence of gastro-intestinal disturbances and neurological reactions.
克霉唑2是一种合成咪唑衍生物,主要用于局部治疗由酵母菌和皮肤癣菌引起的阴道及皮肤感染。在体外,它对念珠菌属、毛癣菌属、小孢子菌属和糠秕马拉色菌(圆形糠秕孢子菌)最为有效。此外,它对某些革兰氏阳性菌有一定的体外活性,在非常高的浓度下对滴虫属有活性。在治疗阴道念珠菌病时,克霉唑阴道片的治愈率与传统制霉菌素阴道片相当。尚未有与制霉菌素阴道乳膏或泡沫阴道片(一些临床医生更喜欢的制霉菌素剂型)的比较研究发表。克霉唑在对其他抗真菌药物如制霉菌素和两性霉素B治疗无效的患者中也取得了成功。在滴虫性阴道炎的治疗中,效果并不显著。由念珠菌或皮肤癣菌引起的皮肤感染通过局部应用克霉唑已得到有效治疗。在比较试验中,克霉唑乳膏在治疗皮肤癣菌病方面与惠菲尔德软膏和托萘酯效果相当,在皮肤念珠菌病方面与制霉菌素效果相当。克霉唑局部制剂一般耐受性良好,但在少数情况下,局部刺激导致治疗中断。口服克霉唑治疗已治愈念珠菌败血症、泌尿道和肺部念珠菌病。在其他类型的严重真菌感染,包括肺曲霉病的治疗中,结果令人失望。口服克霉唑治疗的一个限制因素是胃肠道紊乱和神经反应的发生率较高。