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QuickView for Colistimethate (compound)

Summary
General Info

PubChem

PubChem Compound 216258

PubChem Compound 216258

Name:	colistimethate
PubChem Compound ID:	216258
Molecular formula:	C₅₈H₁₀₅N₁₆Na₅O₂₈S₅
Molecular weight:	1749.82 g/mol
Synonyms:	Colistrimethate sodium; 12705-41-8; 8068-28-8; Colistimethate sodium; 11033-40-2; 21362-08-3; W 1929; Sodium colistimethate; 11048-71-8; 12768-67-1. show more » Colistrimethate sodium; 12705-41-8; 8068-28-8; Colistimethate sodium; 11033-40-2; 21362-08-3; W 1929; Sodium colistimethate; 11048-71-8; 12768-67-1; Coly-Mycin M; Coly-mycin injectable; EINECS 232-516-9; 8068-37-9; Sodium colistin methanesulfonate; 155704-91-9; Sodium colistinemethanesulfonate; 37196-55-7; Coly-Mycin M parenteral; 2680-63-9; Colistinmethanesulfonic acid, sodium salt; Colistimethate sodium [USAN:INN]; Colistinemethanesulfonate sodique; Colistin sulfomethate sodium; 1867-68-1; Colimycin M; Colistimethate sodium methanesulfonate; Pentasodium colistinmethanesulfonate; 12676-33-4; Colistin sodium methanesulfonate show less «

DrugBank

Identification

Name:	colistimethate
Name (isomeric):	DB01111
Drug Type:	small molecule
Synonyms:	Colistin sodium methanesulfonate from bacillus colistinus; Colistimethate sodium; Colistin sodium methanesulfonate; Colistimethale Sodium; Colistin methanesulfonate sodium salt
Brand:	Coly-Mycin, Coly-Mycin M
Category:	Antibacterial Agents
CAS number:	8068-28-8

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:	Colistimethate is a polymyxin antibiotic agent. Originally, colistimethate sodium was thought to be less toxic than polymyxin B; however, if the drugs are administered at comparable doses, their toxicities may be similar. Polymyxins are cationic polypeptides that disrupt the bacterial cell membrane through a detergentlike mechanism. With the develo... show more » Colistimethate is a polymyxin antibiotic agent. Originally, colistimethate sodium was thought to be less toxic than polymyxin B; however, if the drugs are administered at comparable doses, their toxicities may be similar. 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:	Colistimethate is a surface active agent which penetrates into and disrupts the bacterial cell membrane. Colistimethate 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 ... show more » Colistimethate is a surface active agent which penetrates into and disrupts the bacterial cell membrane. Colistimethate 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:	2-3 hours following either intravenous or intramuscular administration in adults and in the pediatric population, including premature infants.
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

Interactions

Drug interaction:

Atracurium	Colistimethate may enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents. If possible, avoid concomitant use of these products. Monitor for deeper, prolonged neuromuscular-blocking effects (respiratory paralysis) in patients receiving concomitant neuromuscular-blocking agents and polymyxin antibiotics (e.g., colistimethate, polymyxin B).
Gentamicin	Aminoglycosides may enhance the nephrotoxic effect of Colistimethate. Aminoglycosides may enhance the neuromuscular-blocking effect of Colistimethate. Due to the potential for additive or synergistic toxicities (including both nephrotoxicity and neuromuscular blockade) between colistimethate and the aminoglycoside antibiotics, this combination should be avoided whenever possible. If these agents must be used together, patients' renal and neuromuscular function should be monitored closely.
Amphotericin B	Amphotericin B may enhance the nephrotoxic effect of Colistimethate. Due to the potential for additive or synergistic nephrotoxicity between colistimethate and other nephrotoxic drugs, such as amphotericin B, this combination should be avoided whenever possible. If these agents must be used together, patients' renal function should be monitored closely.
Streptomycin	Aminoglycosides may enhance the nephrotoxic effect of Colistimethate. Aminoglycosides may enhance the neuromuscular-blocking effect of Colistimethate. Due to the potential for additive or synergistic toxicities (including both nephrotoxicity and neuromuscular blockade) between colistimethate and the aminoglycoside antibiotics, this combination should be avoided whenever possible. If these agents must be used together, patients' renal and neuromuscular function should be monitored closely.
Pancuronium	Colistimethate may enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents. If possible, avoid concomitant use of these products. Monitor for deeper, prolonged neuromuscular-blocking effects (respiratory paralysis) in patients receiving concomitant neuromuscular-blocking agents and polymyxin antibiotics (e.g., colistimethate, polymyxin B).

Atracurium	Colistimethate may enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents. If possible, avoid concomitant use of these products. Monitor for deeper, prolonged neuromuscular-blocking effects (respiratory paralysis) in patients receiving concomitant neuromuscular-blocking agents and polymyxin antibiotics (e.g., colistimethate, polymyxin B).
Gentamicin	Aminoglycosides may enhance the nephrotoxic effect of Colistimethate. Aminoglycosides may enhance the neuromuscular-blocking effect of Colistimethate. Due to the potential for additive or synergistic toxicities (including both nephrotoxicity and neuromuscular blockade) between colistimethate and the aminoglycoside antibiotics, this combination should be avoided whenever possible. If these agents must be used together, patients' renal and neuromuscular function should be monitored closely.
Amphotericin B	Amphotericin B may enhance the nephrotoxic effect of Colistimethate. Due to the potential for additive or synergistic nephrotoxicity between colistimethate and other nephrotoxic drugs, such as amphotericin B, this combination should be avoided whenever possible. If these agents must be used together, patients' renal function should be monitored closely.
Streptomycin	Aminoglycosides may enhance the nephrotoxic effect of Colistimethate. Aminoglycosides may enhance the neuromuscular-blocking effect of Colistimethate. Due to the potential for additive or synergistic toxicities (including both nephrotoxicity and neuromuscular blockade) between colistimethate and the aminoglycoside antibiotics, this combination should be avoided whenever possible. If these agents must be used together, patients' renal and neuromuscular function should be monitored closely.
Pancuronium	Colistimethate may enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents. If possible, avoid concomitant use of these products. Monitor for deeper, prolonged neuromuscular-blocking effects (respiratory paralysis) in patients receiving concomitant neuromuscular-blocking agents and polymyxin antibiotics (e.g., colistimethate, polymyxin B).
Cisatracurium Besylate	Colistimethate may enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents. If possible, avoid concomitant use of these products. Monitor for deeper, prolonged neuromuscular-blocking effects (respiratory paralysis) in patients receiving concomitant neuromuscular-blocking agents and polymyxin antibiotics (e.g., colistimethate, polymyxin B).
Vecuronium	Colistimethate may increase the neuromuscular blocking action of Vecuronium. Risk of respiratory depression and apnea. Consider alternate therapy or monitor for prolonged neuromuscular blocking effects, such as respiratory paralysis.
Amikacin	Aminoglycosides may enhance the nephrotoxic effect of Colistimethate. Aminoglycosides may enhance the neuromuscular-blocking effect of Colistimethate. Due to the potential for additive or synergistic toxicities (including both nephrotoxicity and neuromuscular blockade) between colistimethate and the aminoglycoside antibiotics, this combination should be avoided whenever possible. If these agents must be used together, patients' renal and neuromuscular function should be monitored closely.
Rocuronium	Colistimethate may enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents. If possible, avoid concomitant use of these products. Monitor for deeper, prolonged neuromuscular-blocking effects (respiratory paralysis) in patients receiving concomitant neuromuscular-blocking agents and polymyxin antibiotics (e.g., colistimethate, polymyxin B).
Neomycin	Aminoglycosides may enhance the nephrotoxic effect of Colistimethate. Aminoglycosides may enhance the neuromuscular-blocking effect of Colistimethate. Due to the potential for additive or synergistic toxicities (including both nephrotoxicity and neuromuscular blockade) between colistimethate and the aminoglycoside antibiotics, this combination should be avoided whenever possible. If these agents must be used together, patients' renal and neuromuscular function should be monitored closely.
Kanamycin	Aminoglycosides may enhance the nephrotoxic effect of Colistimethate. Aminoglycosides may enhance the neuromuscular-blocking effect of Colistimethate. Due to the potential for additive or synergistic toxicities (including both nephrotoxicity and neuromuscular blockade) between colistimethate and the aminoglycoside antibiotics, this combination should be avoided whenever possible. If these agents must be used together, patients' renal and neuromuscular function should be monitored closely.
Tobramycin	Increased risk of nephrotoxicity
Vancomycin	Additive nephrotoxic effects may occur. Consider alternate therapy or monitor for renal function during concomitant therapy.

Targets

bacterial outer membrane