Patterson T F, George D, Miniter P, Andriole V T
Department of Medicine, Yale University School of Medicine, New Haven, Connecticut 06510.
Antimicrob Agents Chemother. 1992 Dec;36(12):2681-5. doi: 10.1128/AAC.36.12.2681.
The efficacy of orally and intravenously administered saperconazole against Aspergillus fumigatus was assessed in an immunosuppressed temporarily leukopenic rabbit model of invasive aspergillosis and compared with that of amphotericin B. Oral saperconazole at dosages of 5, 10, and 15 mg/kg of body weight per day improved survival compared with that of controls. In addition, saperconazole at 10 and 15 mg/kg/day reduced the tissue burden and reduced levels of circulating antigen, which correlated with increasing dosages of saperconazole. Intravenous saperconazole produced levels in serum more than 10-fold that of oral therapy. Intravenous saperconazole not only improved survival and reduced antigen levels but also significantly eradicated A. fumigatus from tissues compared with those of controls and was as effective as amphotericin B in these studies. Saperconazole was effective in the treatment of experimental invasive aspergillosis and demonstrates the potential of the newer azoles in therapy for invasive aspergillosis.
在免疫抑制的暂时性白细胞减少兔侵袭性曲霉病模型中评估了口服和静脉注射沙泊康唑对烟曲霉的疗效，并与两性霉素B进行了比较。与对照组相比，每天口服5、10和15mg/kg体重的沙泊康唑可提高生存率。此外，每天10和15mg/kg的沙泊康唑可减轻组织负担并降低循环抗原水平，这与沙泊康唑剂量增加相关。静脉注射沙泊康唑在血清中的浓度比口服治疗高10倍以上。静脉注射沙泊康唑不仅提高了生存率并降低了抗原水平，而且与对照组相比还能显著从组织中清除烟曲霉，在这些研究中其效果与两性霉素B相当。沙泊康唑在治疗实验性侵袭性曲霉病方面有效，并证明了新型唑类药物在侵袭性曲霉病治疗中的潜力。
