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Colistin and polymyxin B: peas in a pod, or chalk and cheese?
Roger L Nation1, Tony Velkov1, Jian Li1
1Drug Delivery, Disposition, and Dynamics, Monash Institute of Pharmaceutical Sciences, Monash University, Melbourne, Australia.
Abstract:
Colistin and polymyxin B have indistinguishable microbiological activity in vitro, but they differ in the form administered parenterally to patients. Polymyxin B is administered directly as the active antibiotic, whereas colistin is administered as the inactive prodrug, colistin methanesulfonate (CMS). CMS must be converted to colistin in vivo, but this occurs slowly and incompletely. Here we summarize the key differences between parenteral CMS/colistin and polymyxin B, and highlight the clinical implications. We put forth the view that overall polymyxin B has superior clinical pharmacological properties compared with CMS/colistin. We propose that in countries such as the United States where parenteral products of both colistin and polymyxin B are available, prospective studies should be conducted to formally examine their relative efficacy and safety in various types of infections and patients. In the meantime, where clinicians have access to both polymyxins, they should carefully consider the relative merits of each in a given circumstance.
Insights
Polymyxin B offers better clinical and pharmacological properties than colistin methanesulfonate (CMS)/colistin. Further studies are needed to compare their efficacy and safety in treating infections.
Area of Science:
- Pharmacology
- Infectious Diseases
- Clinical Microbiology
Background:
- Colistin and polymyxin B exhibit similar in vitro antimicrobial activity.
- Parenteral administration differs: polymyxin B is active, while colistin is a prodrug (colistin methanesulfonate, CMS).
- CMS requires in vivo conversion to active colistin, which is slow and incomplete.
Purpose of the Study:
- To summarize key differences between parenteral CMS/colistin and polymyxin B.
- To highlight the clinical implications of these differences.
- To propose comparative studies on efficacy and safety.
Main Methods:
- Review and comparison of pharmacological properties.
- Analysis of clinical administration routes and in vivo conversion.
- Literature synthesis on existing data.
Main Results:
- Polymyxin B is administered as the active drug, whereas CMS is an inactive prodrug requiring conversion.
- The conversion of CMS to colistin in vivo is inefficient.
- Polymyxin B demonstrates superior clinical pharmacological properties compared to CMS/colistin.
Conclusions:
- Polymyxin B appears to have advantages over CMS/colistin in parenteral administration.
- Prospective studies are recommended in the US to compare the efficacy and safety of both agents.
- Clinicians should carefully weigh the benefits of each polymyxin based on the clinical scenario.
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