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酮康唑(Ketoconazole)具有广泛的抗真菌作用。它是一种与克霉唑及益康唑有关的咪唑类衍生物,其特点是可以口服,效果显著。据最近报告,酮康唑对治疗晚期前列腺癌具有重要的潜在意义。它能使某些前列腺癌患者的癌瘤消失,其效果同切除双侧睾丸的晚期前列腺癌患者有极相似的临床缓解表现。酮康唑抗真菌作用的机理,据认为:药物干扰了真菌细胞膜上的麦角醇或其它甾醇类的生物合成使细胞膜通透性增加,从而容易进入细胞抑制核酸前体的合成。而且酶(氧化酶及过氧化酶)的合成和脂的代谢也受到抑制或障碍,最终变性以至死亡。
Ketoconazole has a wide range of antifungal effects. It is an imidazole derivative related to clotrimazole and econazole, which is characterized by its oral effect and remarkable effect. According to recent reports, ketoconazole has important potential for the treatment of advanced prostate cancer. It can make the cancer of some prostate cancer patients disappear, the effect of resection of bilateral testes with advanced prostate cancer patients have very similar clinical remission performance. The mechanism of anti-fungal action of ketoconazole is believed to be that the drug interferes with the biosynthesis of ergotol or other sterols on the cell membrane of the fungus to increase cell membrane permeability and thus facilitate the entry of cells into the cell to inhibit the synthesis of nucleic acid precursors. Moreover, the synthesis of enzymes (oxidase and peroxidase) and the metabolism of lipids are also inhibited or impeded, eventually degeneration and even death.