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colistin (colistimethate sodium, Coly Mycin M)

 

Classes: Antibiotics, Other

Dosing and uses of Colistimethate sodium, Coly Mycin M (colistin)

 

Adult dosage forms and strengths

powder for injection

  • 150mg/vial

 

Susceptible Infections

Dosage expressed in terms of colistin base

2.5-5 mg/kg/day divided q6-12hr IV/IM; not to exceed 5 mg/kg/day

 

Renal Impairment

CrCl >80 mL/min: No dosage adjustment required

CrCl 50-79 mL/min: 2.5-3.8 mg/kg/day IV/IM divided q12hr

CrCl 30-49 mL/min: 2.5 mg/kg/day IV/IM qDay or divided q12hr

CrCl 10-29 mL/min: 1.5 mg/kg IV/IM q36hr

 

Other Indications & Uses

Gram-neg. infection (e.g., Enterobacter aerogenes, E. coli, Klebsiella, Pseudomonas) unresponsive to other antibiotics

Multi-drug resistant gram-neg. infection

 

Pediatric dosage forms and strengths

powder for injection

  • 150 mg/vial

 

Susceptible Infections

Dosage expressed in terms of colistin bas

<12 years old: Safety and efficacy not established

 

Colistimethate sodium, Coly Mycin M (colistin) adverse (side) effects

1-10%

Dizziness

Paresthesia, tingling sensation

 

<1%

Neurotoxicity

Nephrotoxicity

Acute respiratory failure (inhalation route)

Respiratory tract paralysis

 

Warnings

Contraindications

Hypersensitivity

 

Caution

Do not exceed 5 mg/kg/day (as colistin base) with normal renal function (see Dosing for renal impairment)

Not indicated for infections by Proteus or Neisseria (most strains are resistant)

Risk of nephrotoxicity, neurotoxicity; discontinue if elevated BUN/creatinine

Risk of respiratory arrest in myasthenia gravis or concomitant anesthetics or neuromuscular blocking drugs

Risk of C. difficile-associated pseudomembranous colitis

Sedative effects may impair driving, operating machinery

 

Pregnancy and lactation

Pregnancy category: C

Lactation: unknown; use caution

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Colistimethate sodium, Coly Mycin M (colistin)

Half-Life

Normal renal function: 2-3hr

CrCl < 20 mL/min: 10-20 hr

 

Peak Plasma

IV: 10 min

Time: 2 hr (IM)

Concentration: 5-7.5 mcg/mL (IM); higher IV

 

Other Information

Protein Bound: 50%

Metabolism: colistimethate sodium hydrolyzed in vivo

Metabolites: colistin (active)

Excretion: urine

Dialyzable: unknown

 

Mechanism of action

Structurally similar to polymyxin B; colistimethate hydrolyzed to colistin in vitro or in vivo

Cationic detergent that damages bacterial cytoplasmic membrane, causing cell death

 

Administration

IV Incompatibilities

Additive: erythromycin, hydrocortisone Na-succinate, kanamycin, cefazolin

 

IV Compatibilities

Additive: amikacin, ascorbic acid, chlormaphenicol, diphenhydramine, heparin, penicillin G Na/K, phenobarbital, polymyxin B, ranitidine, vit B/C

Syringe: ampicillin, penicillin G Na

 

IV Preparation

Reconstitute with 2 mL SWI to obtain a 75 mg/mL solution

 

IV/IM Administration

IM or

IV push: half of daily dose injected over 3-5 min q12 hr

IV infusion: half of daily dose injected over 3-5 min; other half mixed with compatible IV solution and administered 1-2 hr later at 5-6 mg/hr