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Drug

D0296 | Polymyxin B

Molecular Formula C56H98N16O13
Molecular Weight 1203.5
Structure
State solid
Clearance 1 compartment models estimate clearance to be 2.37L/h to 2.5L/h[A176390].
Volume of distribution 1 compartment models estimate the volume of distribution to be 34.3L to 47.2L[A176390]. However, the general consensus is that the volume of distribution is yet to be determined[F4151].
Route of elimination Polymyxin B is proposed to be primarily eliminated through renal tubular reabsorption and non-renal pathways[A176390,F4151]. Urine collection in humans and animals show <5% of polymyxin B eliminated from the kidneys[A176390]. However, a Canadian product monograph states the drug is primarily eliminated through the kidneys and that 60% of polymyxin B is recovered in the urine[F4151]. This discrepancy can be explained by the 12 to 24 hour lag time between administration and significant elimination of polymyxin B[F4151]. Non-renal elimination is not well understood but all 4 components of polymyxin B have been detected in bile[A176390].
Protein binding Polymyxin B is 79% to 92% bound to proteins[F4151]. Polymyxin B is likely 92 to 99% protein bound in circulation, though the exact proteins have not been identified[A176420].
Half life In one study the half life was 9 to 11.5 hours[A176390]. However, a Canadian monograph states the half life to be 6 hours, and 48-72 hours in patients with renal insufficiency[F4151].
Absorption Administration by the oral route does not lead to absorption[A176426].

S

J

A

S03AA03 Polymyxin b


[S03AA] Antiinfectives


[S03A] ANTIINFECTIVES


[S03] OPHTHALMOLOGICAL AND OTOLOGICAL PREPARATIONS


[S] Sensory organs

S02AA11 Polymyxin b


[S02AA] Antiinfectives


[S02A] ANTIINFECTIVES


[S02] OTOLOGICALS


[S] Sensory organs

S01AA18 Polymyxin b


[S01AA] Antibiotics


[S01A] ANTIINFECTIVES


[S01] OPHTHALMOLOGICALS


[S] Sensory organs

J01XB02 Polymyxin b


[J01XB] Polymyxins


[J01X] OTHER ANTIBACTERIALS


[J01] ANTIBACTERIALS FOR SYSTEMIC USE


[J] Antiinfectives for systemic use

A07AA05 Polymyxin b


[A07AA] Antibiotics


[A07A] INTESTINAL ANTIINFECTIVES


[A07] ANTIDIARRHEALS, INTESTINAL ANTIINFLAMMATORY/ANTIINFECTIVE AGENTS


[A] Alimentary tract and metabolism

Toxicity Dose Time Species Model Method Action Positive criterion Reference
ELECTRON TRANSPORT CHAIN rat isolated liver mitochondria measurements of mitochondrial respiration; RST inhibition assay, RST uncoupling assay; IC 50ratio of glucose/galactose assay decrease 53
ELECTRON TRANSPORT CHAIN 1.6 μg/ml Mycobacterium smegmatis membrane-bound dehydrogenases decrease IC50 76
TCA 1.6 μg/ml Mycobacterium smegmatis membrane-bound dehydrogenases affect IC50 76

Target Dose Time Species Model Method Action Positive criterion Reference
NADH:ubiquinone reductase 1.6 μg/ml Mycobacterium smegmatis membrane-bound dehydrogenases inhibitor IC50 76
Malate:quinone oxidoreductase 1.6 μg/ml Mycobacterium smegmatis membrane-bound dehydrogenases inhibitor IC50 76

Pictogram Signal Statements Precautionary Statement Codes
Warning

Aggregated GHS information provided by 38 companies from 1 notifications to the ECHA C&L Inventory.


H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]


Information may vary between notifications depending on impurities, additives, and other factors. The percentage value in parenthesis indicates the notified classification ratio from companies that provide hazard codes. Only hazard codes with percentage values above 10% are shown.


 P264, P270, P301+P312, P330, and P501; (The corresponding statement to each P-code can be found at the GHS Classification page.)


  • A807660 BDBM50410807 CHEMBL1201283
    N-[(2S)-4-amino-1-[[(2S,3R)-1-[[(2S)-4-amino-1-oxo-1-[[(3S,6S,9S,12S,15R,18R,21S)-6,9,18-tris(2-aminoethyl)-3-[(1R)-1-hydroxyethyl]-12-(2-methylpropyl)-2,5,8,11,14,17,20-heptaoxo-15-(phenylmethyl)-1,4,7,10,13,16,19-heptazacyclotricos-21-yl]amino]butan-2-y N-[(2S)-4-azanyl-1-[[(2S,3R)-1-[[(2S)-4-azanyl-1-oxidanylidene-1-[[(3S,6S,9S,12S,15R,18R,21S)-6,9,18-tris(2-azanylethyl)-12-(2-methylpropyl)-3-[(1R)-1-oxidanylethyl]-2,5,8,11,14,17,20-heptakis(oxidanylidene)-15-(phenylmethyl)-1,4,7,10,13,16,19-heptazacycl POLUMYXIN B
    Polymixin B WQVJHHACXVLGBL-BPJDFBQWSA-N polymyxin b

    DrugBank Name Polymyxin B
    DrugBank DB00781
    CAS Number 1404-26-8, 1405-20-5
    PubChem Compound 49800004
    KEGG Compound ID C11612
    KEGG Drug D08401
    ChEBI 8309
    ChemSpider 25045120
    BindingDB 50410807.0
    Wikipedia Polymyxin_B
    DPD 8520|8519