Colistimethate is a methanesulfonate of polymyxin antibacterial colistin. Colistimethate is a nonactive prodrug. In aqueous solutions, colistimethate is hydrolyzed and forms a complex mixture of partially sulfomethylated derivatives and colistin. The antimicrobial activity of colistin is similar to that of polymyxin B and is restricted to gram-negative bacteria, including P aeruginosa, Acinetobacter species, Enterobacter-Klebsiella tribe, Escherichia coli, Salmonella and Shigella species, Citrobacter species, Yersinia pseudotuberculosis, Morganella morganii and Haemophilus influenzae. Colistin has also been shown to possess considerable in vitro activity against Stenotrophomonas maltophilia. Colistin and polymyxin B, however, do not have activity against Proteus, Providencia, Serratia species, Pseudomonas mallei, Burkholderia cepacia, Brucella species, most gram-positive bacteria, gram-negative cocci, anaerobes, fungi and parasites. Parenteral or nebulized colistimethate is indicated for the treatment of acute or chronic infections due to sensitive strains of certain gram-negative bacilli. It is particularly indicated when the infection is caused by sensitive strains of Pseudomonas aeruginosa.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: CHEMBL4229 Sources: https://www.ncbi.nlm.nih.gov/pubmed/27670739 |
2.3 µM [IC50] | ||
Target ID: GO:0009276 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Curative | COLY-MYCIN M Approved UseColistimethate for injection is indicated for the treatment of acute or chronic infections due to sensitive strains of certain gram-negative bacilli. It is particularly indicated when the infection is caused by sensitive strains of Pseudomonas aeruginosa. This antibiotic is not indicated for infections due to Proteus or Neisseria. Colistimethate for injection has proven clinically effective in treatment of infections due to the following gram-negative organisms: Enterobacter aerogenes, Escherichia coli, Klebsiella pneumoniae and Pseudomonas aeruginosa. Colistimethate for injection may be used to initiate therapy in serious infections that are suspected to be due to gram-negative organisms and in the treatment of infections due to susceptible gram-negative pathogenic bacilli. To reduce the development of drug-resistant bacteria and maintain the effectiveness of colistimethate for injection and other antibacterial drugs, colistimethate for injection should be used only to treat or prevent infections that are proven or strongly suspected to be caused by susceptible bacteria. When culture and susceptibility information are available, they should be considered in selecting or modifying antibacterial therapy. In the absence of such data, local epidemiology and susceptibility patterns may contribute to the empiric selection of therapy. Launch Date1970 |
Substance Class |
Mixture
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CFR |
21 CFR 522.468
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EU-Orphan Drug |
EU/3/02/088
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NCI_THESAURUS |
C52588
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FDA ORPHAN DRUG |
672418
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EMA ASSESSMENT REPORTS |
COLOBREATHE (AUTHORIZED: CYSTIC FIBROSIS)
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