Dupont B, Drouhet E
Ann Otolaryngol Chir Cervicofac. 1982;99(12):575-80.
Numerous progresses are realized in the chemotherapy of mycoses, particularly in the field of deep mycoses due to 3 categories of systemic antifungal agents: polyenes (oral nystatin, oral and intravenous amphotericin B), 5-fluorocytosine (oral and intravenous) and imidazole derivatives (oral and intravenous miconazole, oral ketoconazole). The old drugs as nystatin and amphotericin B per os continue to have a remarkable effect in oro-pharyngeal candidosis, chiefly after sufficient local contact with the mucos membranes; topical preparation are effective in fungal O.R.L. localizations (aspergillar or candidal otomycoses, glossitis). IV amphotericin B is indicated in naso-orbital-cerebral mucor mycosis, nasosinusal aspergillosis, candidosis, entomophthoromycoses and particularly systemic mycoses (histoplasmosis, blastomycosis, coccidioidomycosis) in spite of severe toxicity. 5-fluorocytosine (100-200 mg/kg) has a limited spectrum to Candida, Cryptococcus neoformans, Aspergillus fumigatus infections if the strains are sensitive to this agent (5% primary resistance). Among the new imidazole derivatives, ketoconazole (400 mg/day) represent a revolutionary antifungal agent due to a very large antifungal spectrum, absence of toxicity, rapid diffusion by oral way, and high therapeutic efficiency in candidosis, histoplasmosis, blastomycosis, rhino-entomophthoromycosis... Oral miconazole has a poor diffusion into the tissues and by intravenous way necessitates several injections daily to obtain therapeutic levels. Numerous imidazole derivatives (econazole, miconazole, clotrimazole etc...) can be successfully utilized by topical application, as well as numerous other local antifungal agents.
在真菌病的化疗方面取得了许多进展,特别是在深部真菌病领域,这得益于三类全身性抗真菌药物:多烯类(口服制霉菌素、口服及静脉用两性霉素B)、5-氟胞嘧啶(口服及静脉用)和咪唑衍生物(口服及静脉用咪康唑、口服酮康唑)。像制霉菌素和口服两性霉素B这类老药,在口腔念珠菌病中仍有显著疗效,主要是在与黏膜充分局部接触后;局部制剂对真菌性耳鼻喉局部感染(曲霉菌性或念珠菌性耳霉菌病、舌炎)有效。尽管毒性严重,但静脉用两性霉素B仍适用于鼻眶脑毛霉菌病、鼻窦曲霉菌病、念珠菌病、虫霉病,尤其是全身性真菌病(组织胞浆菌病、芽生菌病、球孢子菌病)。5-氟胞嘧啶(100 - 200mg/kg)对念珠菌、新型隐球菌、烟曲霉菌感染的抗菌谱有限,前提是菌株对此药敏感(5%的原发性耐药)。在新型咪唑衍生物中,酮康唑(400mg/天)是一种革命性的抗真菌药物,因其抗菌谱非常广、无毒性、口服吸收迅速且对念珠菌病、组织胞浆菌病、芽生菌病、鼻虫霉病等治疗效率高……口服咪康唑在组织中的扩散性差,静脉用药则需要每日多次注射才能达到治疗浓度。许多咪唑衍生物(益康唑、咪康唑、克霉唑等)以及许多其他局部抗真菌药物可通过局部应用成功发挥作用。