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QuickView for colistin (compound)

Summary
General Info

PubChem

PubChem Compound 11969072

PubChem Compound 11969072

Name:	Colistin
PubChem Compound ID:	11969072
Description:	Cyclic polypeptide antibiotic from Bacillus colistinus. It is composed of Polymyxins E1 and E2 (or Colistins A, B, and C) which act as detergents on cell membranes. Colistin is less toxic than Polymyxin B, but otherwise similar; the methanesulfonate is used orally.
Molecular formula:	C₅₂H₁₀₂N₁₆O₂₁S₂
Molecular weight:	1351.59 g/mol
Synonyms:	1264-72-8; Prestwick_787; Colistin sulfate

DrugBank

Identification

Name:	Colistin
Name (isomeric):	DB00803
Drug Type:	small molecule
Description:	Cyclic polypeptide antibiotic from Bacillus colistinus. It is composed of Polymyxins E1 and E2 (or Colistins A, B, and C) which act as detergents on cell membranes. Colistin is less toxic than Polymyxin B, but otherwise similar; the methanesulfonate is used orally.
Brand:	Polymyxin E. Sulfate, Polymyxin E sulfate, Colistin sulfate, Colistin sulfate, nonsterile, Colistin sulphate
Category:	Anti-Bacterial Agents
CAS number:	1264-72-8

Pharmacology

Indication:	For the treatment of acute or chronic infections due to sensitive strains of certain gram-negative bacilli, particularly <i>Pseudomonas aeruginosa</i>.
Pharmacology:	Colistin 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-resistan... show more » Colistin 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. show less «
Mechanism of Action:	Colistin is a surface active agent which penetrates into and disrupts the bacterial cell membrane. Colistin 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 precipit... show more » Colistin is a surface active agent which penetrates into and disrupts the bacterial cell membrane. Colistin 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. show less «
Absorption:	Very poor absorption from gastrointestinal tract.
Biotransformation:	As 80% of the dose can be recovered unchanged in the urine, and there is no biliary excretion, it can be assumed that the remaining drug is inactivated in the tissues, however the mechanism is unknown.
Half Life:	5 hours
Toxicity:	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.
Affected organisms:	Gram-negative bacilli

Targets

bacterial outer membrane