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直到1970年两性霉素B(Amphotericin B)仍是唯一疗效可靠的广谱抗真菌药。氟胞嘧啶进入临床实践则表明两性霉素B与其它药物合用可产生更高的疗效。霉可乃除(双氯苯咪唑,Miconazole)在70年代中进入临床试验,由于脂质性溶剂引起相当严重的毒性,治疗球孢子菌病时易复发。70年代末酮康唑(Ketoconazole)研制成功,该药具有口服易吸收、毒性小的优点;近年在美、英等许多国家已获批准。本文仅限讨论这些治疗全身真菌感染有价值的药物,简述其抗菌活性、药物动力学和临床应用进展。
Amphotericin B remained the only broad-spectrum antifungal agent with proven efficacy until 1970. Flucytosine into clinical practice shows that amphotericin B and other drugs can produce higher efficacy. Miconazole (Miconazole) enters clinical trials in the 1970s and is prone to relapse in the treatment of coccidioidomycosis due to the rather severe toxicity caused by the lipidic solvents. Ketoconazole was successfully developed in the late 1970s. It has the advantages of oral absorption and little toxicity. In recent years, it has been approved in many countries such as the United States and Britain. This article discusses only those drugs that are valuable in the treatment of systemic fungal infections and briefly reviews their antibacterial activity, pharmacokinetics, and clinical application.