Colistimethate

Table of contents

  • Brand Names
  • Drug Combinations
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Toxicological Effects
  • Drug Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Colistin; Belgium: Colistineb; Czech Republic: Colomycin; Denmark: Coliplus, Coliscour, Promixin; France: Colimycine; Germany: Colistin, Promixin; Greece: Colomycin, Promixin; Hungary: Colomycin; Ireland: Colomycin, Promixin; Malta: Colomycin, Promixin; Netherlands: Colistin; Poland: Colistin, Colomycin; Romania: Colistina; Slovakia: Colimycine, Kolimycin; Spain: Colistimetato, Promixin; UK: Colomycin, Promixin.

North America

Canada: Colistimethate, Coly-Mycin M; USA: Colistimethate, Coly-Mycin M.

Drug combinations

Colistimethate and Erythromycin

Chemistry

Colistimethate Sodium: C~58~H~105~N~16~Na~5~O~28~S~5~ (colistin A component). Mw: 1749.82; C~57~H~103~N~16~Na~5~O~28~S~5~ (colistin B component). Mw: 1735.80. Pentasodium colistinmethanesulfonate. CAS-8068-28-8 (1963).

Pharmacologic Category

Antibacterials; Polymyxins. (ATC-Code: A07AA10; J01XB01).

Mechanism of action

Inactive until hydrolyzed to colistin, which acts as a cationic detergent which damages the bacterial cytoplasmic membrane causing alteration of the osmotic barrier and leakage of essential intracellular metabolites and nucleosides. Usually bactericidal. Inactive against Gram-positive bacteria, fungi, and viruses.

Therapeutic use

Gram-negative infections due to susceptible organisms. Life-threatening infections caused by organisms resistant to the preferred drugs.

Pregnancy and lactiation implications

Adverse events observed in animal reproduction studies. Colistimethate crosses the placenta in humans. There are no adequate studies in pregnant women. Excretion in breast milk unknown (use caution).

Unlabeled use

Prevention of P. aeruginosa respiratory tract infections in immunocompromised patients. Treatment of P. aeruginosa infections in cystic fibrosis and other seriously ill or chronically ill patients.

Contraindications

Hypersensitivity to colistimethate, colistin, or any component of the formulation.

Warnings and precautions

Transient, reversible neurological disturbances (e.g. dizziness, numbness, paresthesia, tingling, vertigo) may occur. Dose-dependent nephrotoxicity reported (use with caution in pre-existing renal disease). Respiratory arrest reported (impaired renal function may increase the risk). Prolonged use may result in fungal or bacterial superinfection, including C. difficile-associated diarrhea and pseudomembranous colitis.

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