Ryley J F, McGregor S, Wilson R G
ICI Pharmaceuticals Division, Mereside, Alderley Park, Macclesfield, Cheshire, England.
Ann N Y Acad Sci. 1988;544:310-28. doi: 10.1111/j.1749-6632.1988.tb40416.x.
ICI 195,739 shows superior potency to other azoles in eliminating vaginal candidosis or dermatophyte infections in animal models of infection by both oral dosing and topical application; effective doses are in the range of 0.5-5.0 mg/kg/day or 0.01-0.30% in a topical formulation. ICI 195,739 is likewise effective in models of systemic fungal infection; 1, 10, 25 mg/kg/day will protect animals given a lethal inoculum of C. albicans, C. neoformans, or A. fumigatus, respectively, as long as dosing is continued, showing activity in this respect superior to that of other azoles tested. ICI 195,739 will suppress infections in mice with T. cruzi and prevent mortality with five daily doses of 1 mg/kg; cure rather than suppression of patent infections has been achieved with 35 daily doses of 10 mg/kg.
ICI 195,739在通过口服给药和局部应用消除动物感染模型中的阴道念珠菌病或皮肤癣菌感染方面，显示出比其他唑类更强的效力；有效剂量在0.5 - 5.0毫克/千克/天范围内，或局部制剂中为0.01 - 0.30%。ICI 195,739在系统性真菌感染模型中同样有效；只要持续给药，每天1、10、25毫克/千克将分别保护接受致死剂量白色念珠菌、新型隐球菌或烟曲霉接种的动物，在这方面显示出优于其他测试唑类的活性。ICI 195,739将抑制克氏锥虫感染的小鼠，并通过每日5次剂量为1毫克/千克预防死亡；通过每日35次剂量为10毫克/千克已实现治愈而非抑制显性感染。
