Hope William W, Shoham Shmuel, Walsh Thomas J
National Institutes of Health, 10 Center Dr, Bethesda, MD, 20892, USA.
Expert Opin Drug Metab Toxicol. 2007 Apr;3(2):263-74. doi: 10.1517/17425255.3.2.263.
Caspofungin was the first echinocandin to be licensed for the treatment of invasive fungal infections. Caspofungin has in vitro and in vivo activity against Candida spp. and Aspergillus spp., which constitute the majority of medically important opportunistic fungal pathogens. Caspofungin inhibits the synthesis of the 1,3-beta-glucan, with resultant osmotic instability and lysis. The pharmacology of caspofungin is relatively complex. Trafficking of drug into tissues is an important determinant of the shape of the concentration-time relationship. Caspofungin has demonstrated efficacy in experimental models of invasive candidiasis and aspergillosis, which reflect its activity in the treatment of oropharyngeal, esophageal and disseminated candidiasis, as well as salvage therapy for patients with invasive aspergillosis.
卡泊芬净是首个被批准用于治疗侵袭性真菌感染的棘白菌素。卡泊芬净在体外和体内对念珠菌属和曲霉属具有活性，而念珠菌属和曲霉属是大多数具有重要医学意义的机会性真菌病原体。卡泊芬净抑制1,3-β-葡聚糖的合成，导致渗透压不稳定和细胞溶解。卡泊芬净的药理学相对复杂。药物向组织中的转运是浓度-时间关系曲线形状的一个重要决定因素。卡泊芬净在侵袭性念珠菌病和曲霉病的实验模型中已显示出疗效，这反映了其在治疗口咽、食管和播散性念珠菌病以及对侵袭性曲霉病患者进行挽救治疗方面的活性。
