Schaffner A, Böhler A
Department of Medicine, University of Zürich Medical School, Switzerland.
Mycoses. 1993 Nov-Dec;36(11-12):421-4. doi: 10.1111/j.1439-0507.1993.tb00732.x.
Failure of amphotericin B to halt aspergillosis in a patient previously treated with itraconazole raised the question of whether amphotericin B lost its activity as a result of antagonism between the two antifungal drugs. Azoles exhaust the target of amphotericin B on the fungal cell membrane. Accordingly amphotericin B in vitro lost its activity against six isolates of Aspergillus fumigatus after exposure to subfungicidal concentrations of itraconazole. Prior treatment of mice with itraconazole abolished the protective effect of amphotericin B, even when itraconazole was stopped before starting amphotericin B therapy. These observations raise concern about sequential therapy of aspergillosis with itraconazole followed by amphotericin B.
两性霉素B无法阻止一名先前接受过伊曲康唑治疗的患者发生曲霉病，这引发了一个问题，即两性霉素B是否由于两种抗真菌药物之间的拮抗作用而失去了活性。唑类药物耗尽了两性霉素B在真菌细胞膜上的靶点。因此，在暴露于亚杀菌浓度的伊曲康唑后，两性霉素B在体外对六株烟曲霉失去了活性。即使在开始两性霉素B治疗前停用伊曲康唑，用伊曲康唑预先治疗小鼠也会消除两性霉素B的保护作用。这些观察结果引发了对曲霉病先采用伊曲康唑治疗、随后采用两性霉素B治疗的序贯疗法的担忧。
