a 1 Department of Pharmacy, Singapore General Hospital, Outram Rd 169608, Singapore.
c 3 Department of Pharmacy, National University of Singapore, 21 Lower Kent Ridge Rd 119077, Singapore.
Expert Rev Anti Infect Ther. 2015;13(12):1481-97. doi: 10.1586/14787210.2015.1093933. Epub 2015 Oct 21.
Polymyxin B and colistin (polymyxin E) are polypeptide antibiotics that were developed in the 1940s, but fell into disfavor due to their high toxicity rates. These two antibiotics were previously regarded to be largely equivalent, due to similarities in their chemical structure and spectrum of activity. In recent years, several pertinent differences, especially in terms of potency and disposition, have been revealed between polymyxin B and colistin. These differences are mainly attributed to the fact that polymyxin B is administered parenterally in its active form, while colistin is administered parenterally as an inactive pro-drug, colistimethate. In this review, we summarize the similarities and differences between polymyxin B and colistin. We also discuss the potential clinical implications of these findings, and provide our perspectives on how polymyxins should be employed to preserve their utility in this era of multi-drug resistance.
黏菌素和多黏菌素 B(多黏菌素 E)是两种在 20 世纪 40 年代开发的多肽类抗生素,但由于其高毒性而失宠。这两种抗生素以前被认为基本等效,因为它们在化学结构和活性谱上具有相似性。近年来,人们发现多黏菌素 B 和黏菌素之间存在一些相关的差异,特别是在效力和分布方面。这些差异主要归因于多黏菌素 B 以其活性形式经肠胃外给药,而黏菌素则以无活性的前体药物,即黏菌素甲磺酸钠经肠胃外给药。在这篇综述中,我们总结了多黏菌素 B 和黏菌素之间的异同。我们还讨论了这些发现的潜在临床意义,并就如何在这个多药耐药的时代使用多黏菌素来保持其效用提出了我们的看法。