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Colistimethate (Colistimethate Sodium) - Description and Clinical Pharmacology

 
 



Rx only

To reduce the development of drug-resistant bacteria and maintain the effectiveness of Colistimethate for Injection, USP and other antibacterial drugs, Colistimethate for Injection, USP should be used only to treat or prevent infections that are proven or strongly suspected to be caused by bacteria.

FOR INTRAMUSCULAR AND INTRAVENOUS USE

DESCRIPTION

Colistimethate for Injection, USP is a sterile parenteral antibiotic product which, when reconstituted (see Reconstitution ) is suitable for intramuscular or intravenous administration.  The color of the reconstituted solution is colorless to light yellow.

Each vial contains colistimethate sodium or pentasodium colistinmethanesulfonate (150 mg colistin base activity) as a white to slightly yellow lyophilized cake.  The sodium content is approximately 0.07 mg (0.003 mEq) of sodium per milligram of Colistin.

Colistimethate sodium is a polypeptide antibiotic with an approximate molecular weight of 1750.  The molecular formula is C58H105N16Na5O28S5 and the structural formula is represented below:

 

pentasodium colistinmethanesulfonate (colistimethate sodium) Dbu is 2, 4-diaminobutanoic acid, R is 5-methylheptyl in colistin A and 5-methylhexyl in colistin B


CLINICAL PHARMACOLOGY

Typical serum and urine levels following a single 150 mg dose of colistimethate IM or IV in normal adult subjects are shown in Figure 1. 




Higher serum levels were obtained at 10 minutes following IV administration.  Serum concentration declined with a half-life of 2 to 3 hours following either intravenous or intramuscular administration in adults and in the pediatric population, including premature infants.

Average urine levels ranged from about 270 mcg/mL at 2 hours to about 15 mcg/mL at 8 hours after intravenous administration and from 200 to about 25 mcg/mL during a similar period following intramuscular administration.

Microbiology

Colistimethate sodium is a surface  active agent which penetrates into and disrupts the bacterial cell membrane.  It has been shown to have bactericidal activity against most strains of the following microorganisms, both in vitro and in clinical infections as described in INDICATIONS AND USAGE :

Aerobic gram-negative microorganisms

Enterobacter aerogenes, Escherichia coli, Klebsiella pneumoniae and Pseudomonas aeruginosa .

Susceptibility Tests

Colistimethate sodium is no longer listed as an antimicrobial for routine testing and reporting by clinical microbiology laboratories.

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