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.
| Molecular Weight | 1253.51 |
| Formula | C52H100N16O17S |
| CAS Number | 1264-72-8 |
| Solubility (25°C) | Water: ≥ 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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