Colistimethate

Cyclic Lipopeptide (polymyxin Antibiotic)Rx: PrescriptionCompound: Approved

Also known as: CMS, Colistimethate sodium, Colistin, Colistin methanesulfonate, Colistin methanesulfonate sodium, Coly-Myc, Coly-Mycin M, Polymyxin E methanesulfonate

Educational Only — Not medical advice. Consult a qualified clinician before using any peptide.

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Summary

Colistimethate sodium (colistin methanesulfonate) is a prodrug of colistin, a polymyxin E antibiotic used intravenously or by inhalation to treat infections caused by multidrug‑resistant Gram‑negative bacteria.

Mechanism of Action

Binds to lipopolysaccharide of Gram-negative bacterial outer membrane, displaces calcium and magnesium ions, increases membrane permeability and causes cell death.

Routes of Administration

InhalationIntramuscularIntrathecalIntravenous

Goals & Uses

  • Combination therapy for XDR infectionsAntimicrobialModerate
  • Manage chronic Pseudomonas lung infection in cystic fibrosisAntibacterialHigh
  • Treatment of MDR Gram-negative infectionsAntimicrobialHigh
  • Ventilator-associated pneumonia (VAP) treatmentAntimicrobialModerate
  • Pulmonary infection suppression in cystic fibrosisAntimicrobialModerate
  • Treat multidrug‑resistant Gram‑negative infectionsAntibacterialHigh

Contraindications

  • Severe pre-existing renal impairment (if alternatives exist)RenalHigh
  • Hypersensitivity to colistin or polymyxinsAllergyHigh
  • Severe renal impairment (creatinine clearance <30 mL/min) without dose adjustmentRenalModerate
  • Hypersensitivity to colistin or other polymyxinsAllergyHigh
  • Myasthenia gravisNeuromuscular DiseaseHigh

Adverse Effects

  • NeurotoxicityNeurologicalCommon
  • Injection site reactionsLocalCommon
  • OtotoxicityAuditory/vestibularUncommon
  • Electrolyte disturbancesMetabolicUncommon
  • BronchospasmRespiratoryUncommon
  • Neuromuscular blockadeNeuromuscularRare
  • NephrotoxicityRenalCommon
  • Superinfection / Clostridium difficileInfectiousUncommon

Drug Interactions

  • Non‑steroidal anti‑inflammatory drugs (NSAIDs)Moderate
  • AminoglycosidesModerate
  • Neuromuscular blocking agents (e.g., vecuronium)High
  • Non-depolarizing neuromuscular blocking agents (e.g., vecuronium)High
  • Aminoglycosides (e.g., gentamicin, tobramycin)High
  • VancomycinModerate
  • NSAIDsModerateMay increase renal risk in susceptible patients
  • Loop diuretics (e.g., furosemide)Moderate

Population Constraints

  • PregnancyReproductive SafetyRelative
  • Renal impairmentOrgan ImpairmentRelative
  • Pediatrics (<1 month)AgeRelative
  • Patients with neuromuscular disordersNeurologicalAbsolute
  • Pediatric patientsAgeRelative
  • Elderly patientsAgeRelative
  • Pregnancy (Category C/D)PregnancyRelative

Regulatory Status

  • European UnionApprovedApproved: Infections due to susceptible MDR Gram‑negative bacteriaEMA approval with similar restrictions.
  • United StatesApprovedApproved: Complicated urinary tract infections, Ventilator‑associated pneumonia, Bloodstream infections caused by MDR Gram‑negative bacteriaColistimethate sodium approved under FDA for limited indications; restricted use program.
  • United KingdomApprovedApproved: Serious infections due to susceptible Gram-negative organisms, Suppressive therapy of chronic pulmonary Pseudomonas aeruginosa infection in cystic fibrosisMHRA approved; available as Colomycin injection and Colobreathe inhalation powder; NICE guidelines support use in CF

Limited to severe infections due to high nephro‑ and neurotoxicity; dosing requires renal function monitoring; contraindicated in patients with known hypersensitivity to polymyxins.

Evidence & Sources

No sources recorded yet.

Frequently Asked Questions

What is Colistimethate?

Colistimethate sodium (colistin methanesulfonate) is a prodrug of colistin, a polymyxin E antibiotic used intravenously or by inhalation to treat infections caused by multidrug‑resistant Gram‑negative bacteria.

What is Colistimethate used for?

Colistimethate is educationally associated with: Combination therapy for XDR infections, Manage chronic Pseudomonas lung infection in cystic fibrosis, Treatment of MDR Gram-negative infections, Ventilator-associated pneumonia (VAP) treatment, Pulmonary infection suppression in cystic fibrosis, Treat multidrug‑resistant Gram‑negative infections. Educational only — not medical advice.

How is Colistimethate administered?

Recorded routes of administration: Inhalation, Intramuscular, Intrathecal, Intravenous.

What are the potential side effects of Colistimethate?

Reported adverse effects include: Neurotoxicity, Injection site reactions, Ototoxicity, Electrolyte disturbances, Bronchospasm, Neuromuscular blockade, Nephrotoxicity, Superinfection / Clostridium difficile. This list is not exhaustive — consult a qualified clinician.

Who should avoid Colistimethate?

Recorded contraindications: Severe pre-existing renal impairment (if alternatives exist), Hypersensitivity to colistin or polymyxins, Severe renal impairment (creatinine clearance <30 mL/min) without dose adjustment, Hypersensitivity to colistin or other polymyxins, Myasthenia gravis. Consult a qualified clinician before use.