Colistin sulfate

cell wall

1253.51

Water : ≥ 32 mg/mL (25.53 mM)

白色或类白色粉末

Colistin (2 μg/mL) is active against most strains of Escherichia coli and P. aeruginosa, and all species of Enterobacter, Salmonella, Shigella, Pasteurella, Brucella, and Bordetella. Proteus, Serratia, Providencia. Colistin inhibits 225 strains of P.aeruginosa with MIC90 and MIC50 of 6.3 μg/mL and 1.6μg/mL, respectively. Colistin sulfate is approved only for topical and oral use because of its toxicity. Colistin sulfate is administered orally (tablets or syrup) for bowel decontamination and topically as a powder for the treatment of bacterial skin infections. Colistin interacts with the bacterial membrane through electrostatic interactions between the cationic polypeptide (colistin) and anionic lipopolysaccharide (LPS) molecules in the outer membrane of the gram-negative bacteria, leading to derangement of the cell membrane. Colistin displaces magnesium (Mg+2) and calcium (Ca+2), which normally stabilize the LPS molecules, from the negatively charged LPS, leading to a local disturbance of the outer membrane. Colistin has also potent anti-endotoxin activity. Colistin sulfate produces a strong postantibiotic effects against Acinetobacter baumannii ranging from 2.5 hours to 7.0 hours in a concentration-dependent manner.

Colistin sulfate (5%, i.m.) causes the muscle circumference to appear erythematic in mice. Colistin sulfate (i.m., 15 mg/kg/day for 5 days) causes obvious neurotoxicity to piglets with moderate granular degenerations in the epithelial tissues from kidney and liver of mice. Colistin sulfate (i.m.) at dose of 2.5 mg/kg and 5.0 mg/kg results in Cmax of 3.73 mg/mL and 6.40 mg/mL, Tmax of 32 min and 34 min, t(1/2beta) of 256 min and 264 min, and absolute bioavailability of 95.94% and 88.45% in mice.

硫酸粘杆菌素；Polymyxin E Sulfate

C₅₂H₁₀₀N₁₆O₁₇S 

1264-72-8