de Marie S, Janknegt R, Bakker-Woudenberg I A
Department of Bacteriology, University Hospital Rotterdam, The Netherlands.
J Antimicrob Chemother. 1994 May;33(5):907-16. doi: 10.1093/jac/33.5.907.
Encapsulation of amphotericin B in liposomes or complexing of the compound with other lipid carriers brings about a major reduction in toxicity. Although animal experimental studies have shown an increased therapeutic index for a variety of such lipid formulations resulting in higher dose-dependent efficacy rates, clinical data on pharmacokinetics and efficacy are still scanty. AmBisomeR, Amphotericin B Lipid Complex (ABLC) and AmphocilR (Amphotericin B Colloidal Dispersion, ABCD) have quite different structural and pharmacokinetic characteristics; however, it is not clear whether these differences are important with respect to tolerance and efficacy. At this moment, most published clinical data are available for AmBisomeR, which shows encouraging results in a variety of invasive fungal infections. AmBisomeR has been safely administered in high dosages up to 5 mg/kg/day. Randomized comparative trials with liposomal and other lipid-complexed amphotericin B formulations versus conventional amphotericin B are urgently needed to assess their respective clinical values.
两性霉素B包裹于脂质体中或与其他脂质载体复合可使毒性大幅降低。尽管动物实验研究表明,多种此类脂质制剂的治疗指数有所提高,导致剂量依赖性疗效更高,但关于药代动力学和疗效的临床数据仍然匮乏。安必素(AmBisomeR)、两性霉素B脂质复合物(ABLC)和两性霉素B胶体分散体(ABCD,商品名安浮特克,AmphocilR)具有截然不同的结构和药代动力学特征;然而,尚不清楚这些差异对于耐受性和疗效是否重要。目前,关于安必素(AmBisomeR)的已发表临床数据最多,它在多种侵袭性真菌感染中显示出令人鼓舞的结果。安必素(AmBisomeR)已安全地以高达5毫克/千克/天的高剂量给药。迫切需要进行脂质体和其他脂质复合两性霉素B制剂与传统两性霉素B的随机对照试验,以评估它们各自的临床价值。