Colistin Methanesulfonate (sodium salt)

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Background

Colistin methanesulfonate is an inactive prodrug of colistin (also known as polymyxin E), which is an antibiotic with effect against most Gram-negative bacteria, but also causes nephro- and neurotoxicity [1]. Colistin is produced by certain strains of the bacteria Paenibacillus polymyxa, and belongs to the class of polypeptide antibiotics known as polymyxins. In Vitro: Studying the time-kill kinetics of Colistin methanesulfonate against a type culture of pseudomonas aeruginosa found that 8.0 or 32 mg/l Colistin methanesulfonate began killing at approximately 90 or 30 min, and the mean AUC0-240 values were 186.3±6.0 and 90.4±4.1, respectively [2]. Besides, by investigation among mucoid and nonmucoid strains of Pseudomonas aeruginosa isolated from patients with cystic fibrosis, Colistin methanesulfonate was found to require a concentration of 16 times the MIC to achieve complete killing within 24 h [3]. In Vivo: no data available. Clinical trial: no data available.

[1] Nation R L, Li J. Colistin in the 21st century.[J]. Current Opinion in Infectious Diseases, 2009, 22(6): 535-543.
[2] Bergen P J, Li J, Rayner C R, et al. Colistin methanesulfonate is an inactive prodrug of colistin against Pseudomonas aeruginosa.[J]. Antimicrobial Agents and Chemotherapy, 2006, 50(6): 1953-1958.
[3] Li J, Turnidge J D, Milne R W, et al. In Vitro Pharmacodynamic Properties of Colistin and Colistin Methanesulfonate against Pseudomonas aeruginosaIsolates from Patients with Cystic Fibrosis[J]. Antimicrobial Agents and Chemotherapy, 2001, 45(3): 781-785.