Polymyxin B

Identification

Summary

Polymyxin B is a polymyxin antibiotic used to treat a wide variety of infections in the body.

Brand Names
Casporyn HC, Cortisporin, Dioptrol, Diosporin, Diphen, Maxitrol, Neo-polycin, Neo-polycin HC, Neosporin Ointment, Neosporin Plus Maximum Strength, Neosporin Plus Maximum Strength Cream, Neosporin Solution, Polycin-B, Polysporin, Polytrim, Procomycin, Statrol, Triple Antibiotic
Generic Name
Polymyxin B
DrugBank Accession Number
DB00781
Background

Polymyxin B was discovered in the 1940s5. They are basic polypeptides of about eight amino acids and have cationic detergent action on cell membranes4. Polymyxin B is used for infections with gram-negative organisms, but may be neurotoxic and nephrotoxic4,Label. All gram-positive bacteria, fungi, and the gram-negative cocci, are resistant4. It is appropriate for treatment of infections of the urinary tract, meninges, and blood stream, caused by susceptible strains of Pseudomonas aeruginosaLabel. Polymyxin B has a narrow therapeutic index and so its use is limited and unlikely to be used first line5.

Type
Small Molecule
Groups
Approved, Vet approved
Structure
Weight
Average: 1203.499
Monoisotopic: 1202.74992728
Chemical Formula
C56H98N16O13
Synonyms
  • Polimixina B
  • Polymyxin B
  • Polymyxine B
  • Polymyxinum B

Pharmacology

Indication

Polymyxin B is indicated for the treatment of infections of the urinary tract, meninges, and blood stream, caused by susceptible strains of Pseudomonas aeruginosaLabel.

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Used in combination to treatAcute otitis mediaCombination Product in combination with: Neomycin (DB00994), Lidocaine (DB00281)••• •••••••••••• •••••••• • •••••
Treatment ofBacteremia caused by enterobacter aerogenes••••••••••••
Used in combination to treatBacterial conjunctivitisCombination Product in combination with: Neomycin (DB00994), Prednisolone acetate (DB15566)••••••••••••
Treatment ofBacterial infections••••••••••••
Treatment ofBacterial meningitis••••••••••••••••••••••• ••••••••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

Polymyxin B is an antibiotic that disrupts the outer cell membrane of Gram negative bacteria, binds and neutralizes lipopolysaccharide, and inhibits respiration of Gram-negative bacterial cells4. Polymyxin B can be given by a number of routes to treat susceptible Gram negative bacterial infections4. Absorption of the drug is poor (though not necessary for most of its activity) and the excreted drug is unchanged by metabolic processes6,1. Polymyxin B is generally indicated for susceptible Gram negative infections of the urinary tract, meninges, and blood streamLabel.

Mechanism of action

The alpha and gamma diaminobutyric acid of a positively charged polymyxin B forms an electrostatic interaction with the phosphate groups of a negatively charged lipid A on the outer membrane of a Gram negative bacterium4. Calcium and Magnesium ions are displaced from phosphates of the membrane lipids, destabalising the lipopolysaccharide (LPS), increasing membrane permeability, causing cytoplasmic leaking, and killing the cell4.

Polymyxin B can also bind and neutralize LPS released during bacterial lysis, preventing reactions to endotoxin4.

A third activity of polymyxin B is the inhibition of type II NADH-quinone oxidoreductases in the bacterial inner membrane, which are essential for respiration4.

Polymyxin is active against common Gram negative bacteria but not Gram negative cocci, Gram positive bacteria, or anaerobic bacteria4.

TargetActionsOrganism
ABacterial outer membrane
incorporation into and destabilization
Bacteria
Absorption

Administration by the oral route does not lead to absorption4.

Volume of distribution

1 compartment models estimate the volume of distribution to be 34.3L to 47.2L1. However, the general consensus is that the volume of distribution is yet to be determined8.

Protein binding

Polymyxin B is 79% to 92% bound to proteins8. Polymyxin B is likely 92 to 99% protein bound in circulation, though the exact proteins have not been identified3.

Metabolism

There is little data available for the metabolism of polymyxin B6. In one study, <1% of polymyxin B was eliminated through the kidneys and it had not been metabolised6. Polymyxin B has also been found in bile, not having undergone metabolic processes1.

Route of elimination

Polymyxin B is proposed to be primarily eliminated through renal tubular reabsorption and non-renal pathways1,8. Urine collection in humans and animals show <5% of polymyxin B eliminated from the kidneys1. However, a Canadian product monograph states the drug is primarily eliminated through the kidneys and that 60% of polymyxin B is recovered in the urine8. This discrepancy can be explained by the 12 to 24 hour lag time between administration and significant elimination of polymyxin B8. Non-renal elimination is not well understood but all 4 components of polymyxin B have been detected in bile1.

Half-life

In one study the half life was 9 to 11.5 hours1. However, a Canadian monograph states the half life to be 6 hours, and 48-72 hours in patients with renal insufficiency8.

Clearance

1 compartment models estimate clearance to be 2.37L/h to 2.5L/h1.

Adverse Effects
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Toxicity

Nephrotoxicity can occur in patients as polymyxin B is thought to accumulate in renal cells after renal tubular reabsorption1. This accumulation can lead to apoptosis of renal cells and decrease in renal function2. In recent studies, acute kidney injury (AKI) has been seen in 31.3% to 39.4% of patients receiving polymyxin B2.

Overdose cases can cause neuromuscular block leading to apnea, muscular weakness, vertigo, transient facial parasthesia, slurred speed, vasomotor instability, visual disturbance, confusion, psychosis, and respiratory arrest8. Renal failure has also been seen through decreased urine output, and increased serum concentrations of blood urea nitrogen8.

Overdose of polymyxin B is treated by stopping the drug and beginning symptomatic treatment8. Intravenous administration of mannitol may enhance renal clearance, and hemodialysis may manage renal complications8.

Safety of polymyxin B has not been established in pregnancy, breast feeding, pediatrics, and geriatrics8. Polymyxin B should no be used in pregnancy unless the benefit outweighs the risk8. Nursing mothers should either stop nursing or stop polymyxin B treatment depending on the risks to both the mother and child8. Pediatric patients should be frequently monitored for renal function and no dosing information is available in children under 2 years of age8. Geriatric patients should have renal function assessed before and regularly during therapy8.

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AceclofenacThe risk or severity of adverse effects can be increased when Aceclofenac is combined with Polymyxin B.
AcemetacinThe risk or severity of adverse effects can be increased when Acemetacin is combined with Polymyxin B.
AcenocoumarolThe risk or severity of bleeding can be increased when Polymyxin B is combined with Acenocoumarol.
AcetophenazineAcetophenazine may increase the neurotoxic activities of Polymyxin B.
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Acetylsalicylic acid is combined with Polymyxin B.
Food Interactions
No interactions found.

Products

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Product Ingredients
IngredientUNIICASInChI Key
Polymyxin B sulfate19371312D41405-20-5HFMDLUQUEXNBOP-OLYKAHIFSA-N
International/Other Brands
Aerosporin (GlaxoSmithKline) / Metamyxin (Pola Pharma) / Polomyxin B (Fuji Yakuhin) / Poly-Rx (X-Gen) / Polyfax (Intra) / Polyxx (Celon)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Aerosporin Sterile PowderPowder, for solution500000 unit / vialIntramuscular; Intrathecal; Intravenous; Respiratory (inhalation); TopicalGlaxo Wellcome1952-12-311998-07-30Canada flag
Polymyxin B for Injection USPPowder, for solution50 mg / vialIntramuscular; Intrathecal; Intravenous; OphthalmicSterimax Inc2012-05-03Not applicableCanada flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Polymyxin BInjection, powder, lyophilized, for solution500000 [USP'U]/1Intramuscular; Intrathecal; Intravenous; OphthalmicFosun Pharma USA Inc2016-06-10Not applicableUS flag
Polymyxin BInjection, powder, lyophilized, for solution500000 [USP'U]/1Intramuscular; Intrathecal; Intravenous; OphthalmicFresenius Kabi USA, LLC2009-11-17Not applicableUS flag
Polymyxin BInjection, powder, lyophilized, for solution500000 [USP'U]/1Intramuscular; Intrathecal; IntravenousFresenius Kabi USA, LLC2015-09-09Not applicableUS flag
Polymyxin BInjection, powder, lyophilized, for solution500000 [iU]/1Intramuscular; Intrathecal; Intravenous; OphthalmicAlvogen Inc.2017-09-23Not applicableUS flag
Polymyxin BInjection, powder, lyophilized, for solution500000 [USP'U]/1Intramuscular; Intrathecal; Intravenous; OphthalmicEugia US LLC2016-04-04Not applicableUS flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
0.9g Triple AntibioticPolymyxin B sulfate (5000 [USP'U]/1g) + Bacitracin zinc (400 [USP'U]/1g) + Neomycin sulfate (0.0035 g/1g)OintmentTopicalSled Distribution, LLC2022-03-24Not applicableUS flag
10 Person ANSIPolymyxin B sulfate (5000 [iU]/1g) + Acetaminophen (325 mg/1) + Acetylsalicylic acid (325 mg/1) + Bacitracin zinc (400 [iU]/1g) + Benzalkonium chloride (0.13 g/100g) + Benzalkonium chloride (0.40 mL/100mL) + Benzocaine (6 mL/100mL) + Ethanol (60 mL/100mL) + Ibuprofen (200 mg/1) + Lidocaine (0.5 1/100g) + Neomycin sulfate (5 mg/1g) + Water (98.6 mL/100mL)KitOphthalmic; Oral; TopicalGenuine First Aid2010-04-24Not applicableUS flag
25 Person ANSIPolymyxin B sulfate (5000 [iU]/1g) + Acetaminophen (325 mg/1) + Acetylsalicylic acid (325 mg/1) + Bacitracin zinc (400 [iU]/1g) + Benzalkonium chloride (0.13 g/100g) + Benzalkonium chloride (0.40 mL/100mL) + Benzocaine (6 mL/100mL) + Ethanol (60 mL/100mL) + Ethanol (62 g/100g) + Ibuprofen (200 mg/1) + Isopropyl alcohol (70 mL/100mL) + Lidocaine (0.5 g/100g) + Neomycin sulfate (5 mg/1g) + Water (98.6 mL/100mL)KitOphthalmic; Oral; TopicalGenuine First Aid2010-04-25Not applicableUS flag
4032 First Aid KitPolymyxin B sulfate (5000 [iU]/1g) + Acetylsalicylic acid (325 mg/1) + Ammonia (0.045 g/0.3mL) + Bacitracin zinc (400 [iU]/1g) + Benzalkonium chloride (1.3 mg/1mL) + Lidocaine hydrochloride (24.64 mg/1mL) + Neomycin sulfate (3.5 mg/1g) + Water (98.6 mL/100mL)Inhalant; Kit; Liquid; Ointment; Spray; TabletOphthalmic; Oral; Respiratory (inhalation); TopicalHoneywell Safety Products USA, Inc2018-10-18Not applicableUS flag
4042 First Aid KitPolymyxin B sulfate (5000 [iU]/1g) + Bacitracin zinc (400 [iU]/1g) + Benzalkonium chloride (0.13 g/100g) + Lidocaine hydrochloride (0.5 g/100g) + Neomycin sulfate (3.5 mg/1g) + Povidone-iodine (10 mg/1mL)KitTopicalHoneywell Safety Products USA, Inc2018-11-212019-10-18US flag
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
4032 First Aid KitPolymyxin B sulfate (5000 [iU]/1g) + Acetylsalicylic acid (325 mg/1) + Ammonia (0.045 g/0.3mL) + Bacitracin zinc (400 [iU]/1g) + Benzalkonium chloride (1.3 mg/1mL) + Lidocaine hydrochloride (24.64 mg/1mL) + Neomycin sulfate (3.5 mg/1g) + Water (98.6 mL/100mL)Inhalant; Kit; Liquid; Ointment; Spray; TabletOphthalmic; Oral; Respiratory (inhalation); TopicalHoneywell Safety Products USA, Inc2018-10-18Not applicableUS flag
4042 First Aid KitPolymyxin B sulfate (5000 [iU]/1g) + Bacitracin zinc (400 [iU]/1g) + Benzalkonium chloride (0.13 g/100g) + Lidocaine hydrochloride (0.5 g/100g) + Neomycin sulfate (3.5 mg/1g) + Povidone-iodine (10 mg/1mL)KitTopicalHoneywell Safety Products USA, Inc2018-11-212019-10-18US flag
4050 First Aid KitPolymyxin B sulfate (5000 [iU]/1g) + Bacitracin zinc (400 [iU]/1g) + Benzalkonium chloride (0.13 g/100g) + Lidocaine hydrochloride (0.5 g/100g) + Neomycin sulfate (3.5 mg/1g) + Povidone-iodine (10 mg/1mL)KitTopicalHoneywell Safety Products USA, Inc2018-11-212019-10-18US flag
4064 First Aid KitPolymyxin B sulfate (5000 [iU]/1g) + Bacitracin zinc (400 [iU]/1g) + Benzalkonium chloride (0.13 g/100g) + Lidocaine hydrochloride (0.5 g/100g) + Neomycin sulfate (3.5 mg/1g) + Povidone-iodine (10 mg/1mL)Cream; Kit; Ointment; SwabTopicalHoneywell Safety Products USA, Inc2018-11-212019-10-18US flag
4065 First Aid KitPolymyxin B sulfate (5000 [iU]/1g) + Bacitracin zinc (400 [iU]/1g) + Benzalkonium chloride (0.13 g/100g) + Lidocaine hydrochloride (0.5 g/100g) + Neomycin sulfate (3.5 mg/1g) + Povidone-iodine (10 mg/1mL)Cream; Kit; Ointment; SwabTopicalHoneywell Safety Products USA, Inc2018-11-21Not applicableUS flag

Categories

ATC Codes
S02AA11 — Polymyxin bS03AA03 — Polymyxin bJ01XB02 — Polymyxin bA07AA05 — Polymyxin bS01AA18 — Polymyxin b
Drug Categories
Classification
Not classified
Affected organisms
Not Available

Chemical Identifiers

UNII
J2VZ07J96K
CAS number
1404-26-8
InChI Key
WQVJHHACXVLGBL-BPJDFBQWSA-N
InChI
InChI=1S/C56H98N16O13/c1-7-32(4)13-11-12-16-44(75)63-36(17-23-57)51(80)72-46(34(6)74)56(85)68-39(20-26-60)48(77)67-41-22-28-62-55(84)45(33(5)73)71-52(81)40(21-27-61)65-47(76)37(18-24-58)66-53(82)42(29-31(2)3)69-54(83)43(30-35-14-9-8-10-15-35)70-49(78)38(19-25-59)64-50(41)79/h8-10,14-15,31-34,36-43,45-46,73-74H,7,11-13,16-30,57-61H2,1-6H3,(H,62,84)(H,63,75)(H,64,79)(H,65,76)(H,66,82)(H,67,77)(H,68,85)(H,69,83)(H,70,78)(H,71,81)(H,72,80)/t32?,33-,34-,36+,37+,38-,39+,40+,41+,42+,43-,45+,46+/m1/s1
IUPAC Name
N-[(1S)-3-amino-1-{[(1S,2R)-1-{[(1S)-3-amino-1-{[(3S,6S,9S,12S,15R,18R,21S)-6,9,18-tris(2-aminoethyl)-15-benzyl-3-[(1R)-1-hydroxyethyl]-12-(2-methylpropyl)-2,5,8,11,14,17,20-heptaoxo-1,4,7,10,13,16,19-heptaazacyclotricosan-21-yl]carbamoyl}propyl]carbamoyl}-2-hydroxypropyl]carbamoyl}propyl]-6-methyloctanamide
SMILES
[H][C@]1(NC(=O)[C@H](CCN)NC(=O)[C@H](CCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC2=CC=CC=C2)NC(=O)[C@@H](CCN)NC(=O)[C@H](CCNC1=O)NC(=O)[C@H](CCN)NC(=O)[C@@H](NC(=O)[C@H](CCN)NC(=O)CCCCC(C)CC)[C@@H](C)O)[C@@H](C)O

References

General References
  1. Avedissian SN, Liu J, Rhodes NJ, Lee A, Pais GM, Hauser AR, Scheetz MH: A Review of the Clinical Pharmacokinetics of Polymyxin B. Antibiotics (Basel). 2019 Mar 22;8(1). pii: antibiotics8010031. doi: 10.3390/antibiotics8010031. [Article]
  2. Nation RL, Rigatto MHP, Falci DR, Zavascki AP: Polymyxin Acute Kidney Injury: Dosing and Other Strategies to Reduce Toxicity. Antibiotics (Basel). 2019 Mar 14;8(1). pii: antibiotics8010024. doi: 10.3390/antibiotics8010024. [Article]
  3. Abodakpi H, Gohlke J, Chang KT, Chow DS, Tam VH: Analytical and functional determination of polymyxin B protein binding in serum. Antimicrob Agents Chemother. 2015 Nov;59(11):7121-3. doi: 10.1128/AAC.01815-15. Epub 2015 Aug 31. [Article]
  4. Poirel L, Jayol A, Nordmann P: Polymyxins: Antibacterial Activity, Susceptibility Testing, and Resistance Mechanisms Encoded by Plasmids or Chromosomes. Clin Microbiol Rev. 2017 Apr;30(2):557-596. doi: 10.1128/CMR.00064-16. [Article]
  5. Velkov T, Roberts KD, Nation RL, Thompson PE, Li J: Pharmacology of polymyxins: new insights into an 'old' class of antibiotics. Future Microbiol. 2013 Jun;8(6):711-24. doi: 10.2217/fmb.13.39. [Article]
  6. Zavascki AP, Goldani LZ, Cao G, Superti SV, Lutz L, Barth AL, Ramos F, Boniatti MM, Nation RL, Li J: Pharmacokinetics of intravenous polymyxin B in critically ill patients. Clin Infect Dis. 2008 Nov 15;47(10):1298-304. doi: 10.1086/592577. [Article]
  7. SteriMax Inc: Polymyxin B for Injection USP Monograph [Link]
  8. Product Monograph: Polymyxin B For Injection USP [File]
ChemSpider
25045120
BindingDB
50410807
RxNav
8536
ChEMBL
CHEMBL1201283
Wikipedia
Polymyxin_B
FDA label
Download (219 KB)
MSDS
Download (127 KB)

Clinical Trials

Clinical Trials

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Inhalant; kit; liquid; ointment; spray; tabletOphthalmic; Oral; Respiratory (inhalation); Topical
Cream; kit; liquid; ointment; swabTopical
Gel; inhalant; kit; liquid; ointmentOphthalmic; Respiratory (inhalation); Topical
Cream; kit; liquid; ointment; swab; tabletOphthalmic; Oral; Topical
Cream; kit; liquid; ointment; swabOphthalmic; Topical
KitOphthalmic; Oral; Respiratory (inhalation); Topical
KitOphthalmic; Respiratory (inhalation); Topical
KitOral; Respiratory (inhalation); Topical
Kit; liquid; ointment; swabOphthalmic; Topical
Inhalant; kit; liquid; ointment; spray; swab; tabletOphthalmic; Oral; Respiratory (inhalation); Topical
KitRespiratory (inhalation); Topical
Gel; kit; liquid; ointment; swabOphthalmic; Topical
Inhalant; kit; liquid; ointment; spray; swabOphthalmic; Respiratory (inhalation); Topical
Kit; liquid; ointment; spray; swabOphthalmic; Topical
Cream; kit; liquid; ointment; spray; tabletOphthalmic; Oral; Topical
Cream; kit; liquid; ointment; swab; tabletOral; Topical
Cream; kit; liquid; ointmentTopical
Gel; kit; ointment; swabTopical
Cream; kit; ointment; swabTopical
Gel; kit; liquid; ointmentOphthalmic; Topical
Kit; liquid; ointment; swab; tabletOphthalmic; Oral; Topical
Gel; kit; liquid; ointment; solution; swabOphthalmic; Topical
Kit; liquid; ointment; swabTopical
Gel; kit; liquid; ointmentTopical
Gel; kit; liquid; ointment; swabTopical
Cream; gel; kit; liquid; ointment; swabOphthalmic; Topical
Kit; liquid; ointment; spray; tabletOphthalmic; Oral; Topical
Cream; gel; kit; liquid; ointment; spray; swabOphthalmic; Topical
Kit; liquid; ointmentTopical
Gel; kit; liquid; ointment; swab; tabletOral; Topical
Kit; liquid; ointmentOphthalmic; Topical
KitIrrigation; Ophthalmic; Respiratory (inhalation); Topical
Cream; irrigant; kit; liquid; ointment; swabIrrigation; Ophthalmic; Topical
KitIrrigation; Oral; Respiratory (inhalation); Topical
KitIrrigation; Ophthalmic; Oral; Respiratory (inhalation); Topical
KitOral; Topical
KitTopical
Powder, for solutionIntramuscular; Intrathecal; Intravenous; Respiratory (inhalation); Topical500000 unit / vial
SolutionOther
Solution / dropsOral
SolutionAuricular (otic); Ophthalmic
Ointment
OintmentCutaneous
Ointment; swabTopical
KitElectro-osmosis
Cloth; kit; ointment; swabTopical
SolutionCutaneous
CreamTopical
SolutionAuricular (otic)
SuspensionTopical
KitOral
Cream; kit; liquid; ointment; tablet; tablet, chewable; tablet, film coatedOral; Topical
KitOphthalmic; Topical
LiquidTopical
SolutionAuricular (otic); Topical
KitOphthalmic; Oral; Topical
Cream; kit; tablet, film coatedOral; Topical
Cloth; cream; gel; kit; ointment; solutionOphthalmic; Topical
KitOphthalmic
LozengeBuccal
StickTopical
SuspensionConjunctival; Ophthalmic1 mg
SolutionConjunctival; Ophthalmic
SolutionIntravenous5 mg
SolutionIntraocular; Ophthalmic
IrrigantIrrigation
SolutionIrrigation
OintmentOphthalmic
SuspensionOphthalmic
Solution / dropsOphthalmic
Solution / dropsAuricular (otic)
Suspension / dropsAuricular (otic)
Suspension / dropsOphthalmic
Suspension / dropsTopical
SolutionUrethral
Kit; ointmentTopical
OintmentConjunctival; Ophthalmic
GelTopical
LiquidAuricular (otic)
SuspensionAuricular (otic)
Injection, powder, lyophilized, for solutionIntramuscular; Intrathecal; Intravenous500000 IU
SolutionOphthalmic1.3 mg
Injection, solutionIntramuscular; Intrathecal; Intravenous500000 iu
Injection, solutionIntramuscular; Intrathecal; Intravenous
Injection, powder, lyophilized, for solutionIntramuscular; Intrathecal; Intravenous
LiquidAuricular (otic); Ophthalmic
SolutionAuricular (otic)0.1 g/100ml
CapsuleVaginal
CapsuleVaginal35000 iu
InjectionIntramuscular; Intrathecal; Intravenous500000 1/1
Injection, powder, for solutionIntramuscular; Intrathecal; Intravenous; Ophthalmic500000 [USP'U]/1
Injection, powder, for solutionIntramuscular; Intrathecal; Intravenous; Ophthalmic500000 [iU]/1
Injection, powder, lyophilized, for solutionIntramuscular; Intrathecal; Intravenous500000 [USP'U]/1
Injection, powder, lyophilized, for solutionIntramuscular; Intrathecal; Intravenous; Ophthalmic500000 [USP'U]/1
Injection, powder, lyophilized, for solutionIntramuscular; Intrathecal; Intravenous; Ophthalmic500000 [iU]/1
Injection, powder, lyophilized, for solutionIntramuscular; Intravenous500000 [USP'U]/1
Injection, solutionIntramuscular; Intrathecal; Intravenous; Ophthalmic500000 1/1
Powder, for solutionIntramuscular; Intrathecal; Intravenous; Ophthalmic50 mg / vial
Injection, solutionIntramuscular; Intrathecal; Intravenous500000 i.u.
PowderTopical
Solution / dropsAuricular (otic); Ophthalmic
OintmentOphthalmic; Topical
Injection, powder, lyophilized, for solutionIntramuscular; Intrathecal; Intravenous50000000000 IU
LozengeOral
Cloth; kit; ointmentTopical
SolutionIntravenous89.600 mg
PowderIntramuscular; Intrathecal; Intravenous500000 IU
OintmentTopical
SolutionOphthalmic
Jelly; kit; ointmentTopical
SuspensionConjunctival; Ophthalmic
SwabTopical
LiquidOphthalmic
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)>203MSDS
water solubilitySolubleMSDS
pKa8.9https://www.chemicalbook.com/ChemicalProductProperty_US_CB8666707.aspx
Predicted Properties
PropertyValueSource
Water Solubility0.0744 mg/mLALOGPS
logP-0.89ALOGPS
logP-7.2Chemaxon
logS-4.2ALOGPS
pKa (Strongest Acidic)11.57Chemaxon
pKa (Strongest Basic)10.23Chemaxon
Physiological Charge5Chemaxon
Hydrogen Acceptor Count18Chemaxon
Hydrogen Donor Count18Chemaxon
Polar Surface Area490.66 Å2Chemaxon
Rotatable Bond Count29Chemaxon
Refractivity313.22 m3·mol-1Chemaxon
Polarizability127.4 Å3Chemaxon
Number of Rings2Chemaxon
Bioavailability0Chemaxon
Rule of FiveNoChemaxon
Ghose FilterNoChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleNoChemaxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-0udi-3390000000-364cd3f5c051fd282948
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-0ue9-0590000000-d0de5c17c416192b5e85
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-00ri-7920000020-754c2b9c3b89f80133a6
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-0a4r-3934000016-60010377a089e5b17dc9
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-00di-9400100021-f6058a5805e8cf3cec90
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-054n-9640100170-187ee07831c4d7d57b5b
Chromatographic Properties
Collision Cross Sections (CCS)
Not Available

Targets

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1. Bacterial outer membrane
Kind
Group
Organism
Bacteria
Pharmacological action
Yes
Actions
Incorporation into and destabilization
References
  1. Yuan Z, Tam VH: Polymyxin B: a new strategy for multidrug-resistant Gram-negative organisms. Expert Opin Investig Drugs. 2008 May;17(5):661-8. doi: 10.1517/13543784.17.5.661 . [Article]
  2. Zavascki AP, Goldani LZ, Li J, Nation RL: Polymyxin B for the treatment of multidrug-resistant pathogens: a critical review. J Antimicrob Chemother. 2007 Dec;60(6):1206-15. Epub 2007 Sep 17. [Article]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Curator comments
Mediates drug reabsorption in the kidney
General Function
Peptide:proton symporter activity
Specific Function
Proton-coupled intake of oligopeptides of 2 to 4 amino acids with a preference for dipeptides.
Gene Name
SLC15A2
Uniprot ID
Q16348
Uniprot Name
Solute carrier family 15 member 2
Molecular Weight
81782.77 Da
References
  1. Lu X, Chan T, Xu C, Zhu L, Zhou QT, Roberts KD, Chan HK, Li J, Zhou F: Human oligopeptide transporter 2 (PEPT2) mediates cellular uptake of polymyxins. J Antimicrob Chemother. 2016 Feb;71(2):403-12. doi: 10.1093/jac/dkv340. Epub 2015 Oct 22. [Article]

Drug created at February 28, 2019 16:07 / Updated at March 28, 2024 03:23