Drouhet E, Dupont B
Rev Infect Dis. 1987 Jan-Feb;9 Suppl 1:S4-14. doi: 10.1093/clinids/9.supplement_1.s4.
Important progress has been achieved in antifungal chemotherapy in recent years. Two groups of drugs are now used: those produced by various organisms and those made synthetically. In the first group, only amphotericin B (1956) administered systemically is active in numerous deep mycoses. Although toxicity limits the use of amphotericin B, it is still the drug of choice for systemic mycoses. Griseofulvin was the first agent used for oral treatment of dermatophytoses. The introduction of flucytosine began a new era in chemotherapy; however, although flucytosine is orally administered and rapidly distributed, its antifungal activity is limited to cryptococcosis and systemic candidosis. The rapid induction of flucytosine-resistant mutants led to the development of treatment regimens of amphotericin B plus flucytosine. With the development of imidazole derivatives in 1969, a new generation of azole antifungal agents has emerged. Of these, only ketoconazole was orally active. New azole derivatives and triazoles have been synthesized, but only itraconazole has been successful in the treatment of superficial and deep mycoses in humans. Future trends for the development of agents with fungicidal activity, wider spectra, and better distribution are proposed. The association of immunotherapy with antifungal chemotherapy may offer new treatments for fungal infections in immunocompromised patients.
近年来，抗真菌化疗取得了重要进展。目前使用两类药物：一类是由各种生物体产生的，另一类是合成的。在第一类中，只有全身给药的两性霉素B（1956年）对多种深部真菌病有效。尽管毒性限制了两性霉素B的使用，但它仍然是系统性真菌病的首选药物。灰黄霉素是第一种用于口服治疗皮肤癣菌病的药物。氟胞嘧啶的引入开启了化疗的新时代；然而，尽管氟胞嘧啶口服给药且分布迅速，但其抗真菌活性仅限于隐球菌病和系统性念珠菌病。氟胞嘧啶耐药突变体的快速诱导导致了两性霉素B加氟胞嘧啶治疗方案的发展。随着1969年咪唑衍生物的发展，新一代唑类抗真菌药物出现了。其中，只有酮康唑具有口服活性。新的唑类衍生物和三唑已被合成，但只有伊曲康唑成功用于治疗人类的浅表和深部真菌病。提出了开发具有杀菌活性、更广谱和更好分布的药物的未来趋势。免疫疗法与抗真菌化疗的联合可能为免疫受损患者的真菌感染提供新的治疗方法。
