Merali S, Chin K, Grady R W, Weissberger L, Clarkson A B
Department of Medical and Molecular Parasitology, New York University School of Medicine, New York 10016, USA.
Antimicrob Agents Chemother. 1995 Jul;39(7):1442-4. doi: 10.1128/AAC.39.7.1442.
The iron-chelating drug deferoxamine mesylate (DFO) is active against Pneumocystis carinii in vitro and in rat and mouse models of P. carinii pneumonia. Because DFO has a short half-life, daily divided or continuous dosage was expected to improve the dose response, as is the case with DFO treatment of malaria. Therefore, results of single daily intraperitoneal injections were compared with results of an evenly divided four-times-daily dosage and the efficacy of delivery with implanted infusion pumps. The highest bolus dosage (1,000 mg kg-1 of body weight day-1) was as effective as the standard combination of trimethoprim with sulfamethoxazole. Unexpectedly, very little improvement was observed with the divided or continuous dosage, and several mechanisms that could account for this are discussed.
铁螯合剂甲磺酸去铁胺(DFO)在体外以及卡氏肺孢子虫肺炎的大鼠和小鼠模型中对卡氏肺孢子虫具有活性。由于DFO半衰期短,预计每日分次给药或持续给药会改善剂量反应,就如同DFO治疗疟疾的情况一样。因此,将每日单次腹腔注射的结果与每日均匀分四次给药的结果以及植入式输液泵给药的疗效进行了比较。最高推注剂量(1000 mg·kg-1体重·日-1)与甲氧苄啶联合磺胺甲恶唑的标准组合效果相当。出乎意料的是,分次给药或持续给药几乎没有观察到改善,文中讨论了几种可能解释此现象的机制。