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.

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.

Related Concept Videos

Combined Effects of Drugs: Synergism01:27

Combined Effects of Drugs: Synergism

Synergism is a useful mechanism where combining two or more drugs is more effective than each constituent used alone. Such combinations are also called supra-additive interactions. The drugs collectively enhance the final therapeutic effect by acting on different targets. Another advantage is that the low dose of each constituent drug is sufficient to achieve the desired effect. This helps reduce the duration of therapy and lower the adverse effects of these drugs.
Such synergistic combinations...
6.2K
Inhibitors of Bacterial Protein Synthesis01:25

Inhibitors of Bacterial Protein Synthesis

Aminoglycosides constitute a highly potent class of bactericidal antibiotics that exert their antimicrobial effects by targeting the bacterial ribosome, specifically disrupting protein synthesis. These polycationic molecules consist of amino-modified sugars linked via glycosidic bonds to an aminocyclitol core such as 2-deoxystreptamine or streptamine. Their strong positive charges facilitate tight binding to the negatively charged phosphate backbone of ribosomal RNA (rRNA), primarily at the 16S...
106
Inhibitors of Gram-positive Cell Wall Synthesis01:23

Inhibitors of Gram-positive Cell Wall Synthesis

Bacterial cell walls are typically rigid structures composed mainly of peptidoglycan, a mesh-like polymer that provides mechanical strength and maintains cell shape. The synthesis of peptidoglycan is a crucial process in bacterial growth and serves as a primary target for many antibiotics.Mechanism of Action of Beta-Lactam AntibioticsBeta-lactam antibiotics, such as penicillin, inhibit peptidoglycan synthesis in actively growing cells. These antibiotics share a characteristic four-membered...
191
Clinical Significance of Antibiotic Resistance01:25

Clinical Significance of Antibiotic Resistance

Methicillin-resistant Staphylococcus aureus (MRSA) presents a critical public health threat, arising from its capacity to resist β-lactam antibiotics due to acquisition of the mecA gene within the staphylococcal cassette chromosome mec (SCCmec). This gene encodes penicillin-binding protein 2a (PBP2a), which impairs binding efficacy of methicillin and other β-lactams. MRSA has evolved into distinct clonal lineages impacting humans and animals alike, reinforcing its significance within...
90
Antibiotic Selection00:57

Antibiotic Selection

Overview
48.9K
Drugs that Destabilize Microtubules01:10

Drugs that Destabilize Microtubules

Microtubules are dynamic structures and can be regulated by microtubule targeting agents (MTAs). Microtubule destabilizing drugs are a class of MTAs that destabilize and prevent microtubules' polymerization. Both natural and synthetic chemicals can be found under this class of drugs. Vincristine and vinblastine, two vinca alkaloids, and colchicine were among the first to be discovered. These drugs can affect cells in various ways, either by inducing a change in cell morphology, preventing...
3.2K