Polymyxin B

Polymyxin B

drugbox
IUPAC_name = N- [4-amino-1- [1- [4-amino-1-oxo-1- [6,9,18-tris(2-aminoethyl)-15-benzyl-3-(1-hydroxyethyl)-12-(2-methylpropyl)-2,5,8,11,14,17,20-heptaoxo-1,4,7,10,13,16,19-heptazacyclotricos-21-yl] amino] butan-2-yl] amino] -3-hydroxy-1-oxobutan-2-yl] amino] -1-oxobutan-2-yl] -6-methyloctanamide


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CAS_number = 1405-20-5
ATC_prefix = A07
ATC_suffix = AA05
ATC_supplemental = ATC|J01|XB02, ATC|S01|AA18, ATC|S02|AA11, ATC|S03|AA03
PubChem = 5702105
DrugBank = APRD01190
C=56 | H=100 | N=16 | O=17 | S=1
molecular_weight = 1301.56 g/mol
bioavailability =
protein_bound =
metabolism =
elimination_half-life =
pregnancy_category =
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routes_of_administration =

Polymyxin B is an antibiotic primarily used for resistant gram negative infections. Polymyxins bind to the cell membrane and alter its structure making it more permeable. The resulting water uptake leads to cell death. They are cationic, basic proteins that act like detergents. Side effects include neurotoxicity and acute renal tubular necrosis.

# Family of polypeptides with attached fatty acid; cationic detergent at physiological pH, both hydrophilic and hydrophobic properties
# Bactericidal for gram-negative; little to no effect on gram-positive since cell wall is too thick to permit access to membrane

Mechanism of action

# Alters cytoplasmic membrane permeability by binding to a negatively charged site in the lipopolysaccharide layer which has an electrostatic attraction for the positively charged amino groups in the cyclic peptide portion
# Fatty acid portion dissolves in hydrophobic region of membrane and disrupts membrane integrity
# Leakage of cellular molecules, inhibition of cellular respiration
# Binds and inactivates endotoxincite journal |author=Cardoso LS, Araujo MI, Góes AM, Pacífico LG, Oliveira RR, Oliveira SC |title=Polymyxin B as inhibitor of LPS contamination of Schistosoma mansoni recombinant proteins in human cytokine analysis |journal=Microb. Cell Fact. |volume=6 |issue= |pages=1 |year=2007 |pmid=17201926 |pmc=1766364 |doi=10.1186/1475-2859-6-1 |url=http://www.microbialcellfactories.com/content/6//1]
# Relative absence of selective toxicity: nonspecific for cell membranes of any type, highly toxic

Research application

# In addition to its antibiotic function, polymix B has been used to clear endotoxin contamination in reagents.

References


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Look at other dictionaries:

  • polymyxin B — n the least toxic of the polymyxins used in the form of its sulfate chiefly in the treatment of some localized, gastrointestinal, or systemic infections * * * an antibiotic used to treat severe infections caused by Gram negative bacteria.… …   Medical dictionary

  • polymyxin E — n COLISTIN …   Medical dictionary

  • polymyxin — [päl΄i mik′sin] n. [< ModL ( Bacillus) polymyx( a) (< poly , POLY + myxa < Gr myxa, MUCUS) + IN1] any of various antibiotics obtained from strains of a soil bacterium (Bacillus polymyxa), esp. effective against Gram negative bacteria …   English World dictionary

  • Polymyxin — Polymyxins are antibiotics,cite journal |author=Dixon RA, Chopra I |title=Polymyxin B and polymyxin B nonapeptide alter cytoplasmic membrane permeability in Escherichia coli |journal=J. Antimicrob. Chemother. |volume=18 |issue=5 |pages=557–63… …   Wikipedia

  • Polymyxin E — Strukturformel Allgemeines Freiname Colistin Summenformel …   Deutsch Wikipedia

  • polymyxin — /pol ee mik sin/, n. Pharm. any of various polypeptide antibiotics derived from Bacillus polymyxa. [1945 50; < NL polymyx(a) specific epithet ( < Gk poly POLY + mýxa mucus, slime) + IN2] * * * ▪ drug       any of five polypeptide antibiotics… …   Universalium

  • polymyxin — polimiksinas statusas T sritis chemija apibrėžtis Ciklinis peptidas, antibiotikas. atitikmenys: angl. polymyxin rus. полимиксин …   Chemijos terminų aiškinamasis žodynas

  • polymyxin A — noun see polymyxin …   Useful english dictionary

  • polymyxin B — noun see polymyxin …   Useful english dictionary

  • polymyxin B sulfate — [USP] the sulfate salt of the least toxic member of the polymyxin group; used in the treatment of various systemic, urinary tract, ophthalmic, otic, and cutaneous infections due to susceptible gram negative bacteria, especially Pseudomonas… …   Medical dictionary

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