Polymyxin E sulfate
Polymyxin E sulfate - General Information
Cyclic polypeptide antibiotic from Bacillus colistinus. It is composed of Polymyxins E1 and E2 (or Polymyxin E sulfates A, B, and C) which act as detergents on cell membranes. Polymyxin E sulfate is less toxic than Polymyxin B, but otherwise similar; the methanesulfonate is used orally. [PubChem]
Pharmacology of Polymyxin E sulfate
Polymyxin E sulfate is a polymyxin antibiotic agent. Polymyxins are cationic polypeptides that disrupt the bacterial cell membrane through a detergentlike mechanism. With the development of less toxic agents, such as extended-spectrum penicillins and cephalosporins, parenteral polymyxin use was largely abandoned, except for the treatment of multidrug-resistant pulmonary infections in patients with cystic fibrosis. More recently, however, the emergence of multidrug-resistant gram-negative bacteria, such as Pseudomonas aeruginosa and Acinetobacter baumannii, and the lack of new antimicrobial agents have led to the revived use of the polymyxins.
Additional information about Polymyxin E sulfate
Polymyxin E sulfate Indication: For the treatment of acute or chronic infections due to sensitive strains of certain gram-negative bacilli, particularly Pseudomonas aeruginosa.
Mechanism Of Action: Polymyxin E sulfate is a surface active agent which penetrates into and disrupts the bacterial cell membrane. Polymyxin E sulfate is polycationic and has both hydrophobic and lipophilic moieties. It interacts with the bacterial cytoplasmic membrane, changing its permeability. This effect is bactericidal. There is also evidence that polymyxins enter the cell and precipitate cytoplasmic components, primarily ribosomes.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Colistin
Synonyms: Not Available
Drug Category: Anti-Bacterial Agents
Drug Type: Small Molecule; Approved
Other Brand Names containing Colistin: Colistin sulfate; Colistin sulfate, nonsterile; Colistin sulphate; Coly-mycin S; Polymyxin E sulfate; Polymyxin E. Sulfate;
Absorption: Very poor absorption from gastrointestinal tract.
Toxicity (Overdose): Oral LD50 in rats is 5450 mg/kg. Overdosage with colistimethate can cause neuromuscular blockade characterized by paresthesia, lethargy, confusion, dizziness, ataxia, nystagmus, disorders of speech and apnea. Respiratory muscle paralysis may lead to apnea, respiratory arrest and death.
Protein Binding: Not Available
Biotransformation: Not Available
Half Life: 5 hours
Dosage Forms of Polymyxin E sulfate: Powder, for solution Intravenous
Chemical IUPAC Name: N-[(2S)-4-amino-1-[[(2S,3R)-1-[[(2S)-4-amino-1-oxo-1-[[(3S,6S,9S,12S,15R,18S,21S)-6,9,18-tris(2-aminoethyl)-3-(1-hydroxyethyl)-12,15-bis(2-methylpropyl)-2,5,8,11,14,17,20-heptaoxo-1,4,7,10,13,16,19-heptazacyclotricos-21-yl]amino]butan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxobutan-2-yl]-5-methylheptanamide
Chemical Formula: C52H98N16O13
Colistin on Wikipedia: https://en.wikipedia.org/wiki/Colistin
Organisms Affected: Gram-negative bacilli
