Identification

Name
Polymyxin B
Accession Number
DB00781
Description

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
Thumb
Weight
Average: 1203.499
Monoisotopic: 1202.74992728
Chemical Formula
C56H98N16O13
Synonyms
  • Polimixina B
  • Polymyxin B
  • Polymyxine B
  • Polymyxinum B

Pharmacology

Pharmacology
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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.

Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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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
Medicalerrors
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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.

Affected organisms
Not Available
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.
AcyclovirThe risk or severity of adverse effects can be increased when Acyclovir is combined with Polymyxin B.
Adefovir dipivoxilThe risk or severity of adverse effects can be increased when Adefovir dipivoxil is combined with Polymyxin B.
AlclofenacThe risk or severity of adverse effects can be increased when Alclofenac is combined with Polymyxin B.
AlimemazineAlimemazine may increase the neurotoxic activities of Polymyxin B.
AmikacinThe risk or severity of adverse effects can be increased when Amikacin is combined with Polymyxin B.
Interactions
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Food Interactions
No interactions found.

Products

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 solutionIntramuscular; Intrathecal; Intravenous; Respiratory (inhalation); TopicalGlaxo Wellcome1952-12-311998-07-30Canada flag
Polymyxin B for Injection USPPowder, for solutionIntramuscular; Intrathecal; Intravenous; OphthalmicSterimax Inc2012-05-03Not applicableCanada flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Polymyxin BInjection, powder, lyophilized, for solution500000 1/1Intramuscular; Intrathecal; Intravenous; OphthalmicGland Pharma Limited2016-06-01Not applicableUS flag
Polymyxin BInjection, powder, lyophilized, for solution500000 [iU]/1Intramuscular; Intrathecal; Intravenous; OphthalmicAthenex Pharmaceutical Division, Llc.2017-01-01Not applicableUS flag
Polymyxin BInjection, powder, for solution500000 [iU]/1Intramuscular; Intrathecal; Intravenous; OphthalmicSagent Pharmaceuticals2011-08-012014-03-31US flag
Polymyxin BInjection, powder, lyophilized, for solution500000 [USP'U]/1Intramuscular; Intrathecal; Intravenous; OphthalmicX-GEN Pharmaceuticals, Inc.2014-01-152020-02-25US flag
Polymyxin BInjection, powder, lyophilized, for solution500000 [USP'U]/1Intramuscular; Intrathecal; Intravenous; OphthalmicX-GEN Pharmaceuticals, Inc.1994-09-30Not 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; OphthalmicAuroMedics Pharma LLC2016-04-04Not applicableUS flag
Polymyxin BInjection500000 1/1Intramuscular; Intrathecal; IntravenousXellia Pharmaceuticals ApS2014-01-24Not applicableUS flag
Polymyxin BInjection, powder, lyophilized, for solution500000 [USP'U]/1Intramuscular; IntravenousX-GEN Pharmaceuticals, Inc.2014-04-252020-02-25US flag
Polymyxin BInjection, powder, for solution500000 [USP'U]/1Intramuscular; Intrathecal; Intravenous; OphthalmicXellia Pharmaceuticals USA LLC2018-10-01Not applicableUS flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
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)KitOphthalmic; 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)KitTopicalHoneywell 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)KitTopicalHoneywell Safety Products USA, Inc2018-11-21Not applicableUS flag
4066 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, Inc2018-11-21Not applicableUS flag
4067 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, Inc2018-11-21Not applicableUS flag
4125 First Aid KitPolymyxin B sulfate (5000 [iU]/1g) + Ammonia (0.045 g/0.3mL) + Bacitracin zinc (400 [iU]/1g) + Benzalkonium chloride (1.3 mg/1mL) + Benzethonium chloride (0.2 g/100g) + Benzethonium chloride (0.2 g/100g) + Benzocaine (10 g/100g) + Benzocaine (10 g/100g) + Isopropyl alcohol (0.7 mL/1mL) + Levomenthol (0.33 g/100g) + Neomycin sulfate (3.5 mg/1g) + Water (98.6 mL/100mL)KitOphthalmic; Respiratory (inhalation); TopicalHoneywell Safety Products USA, Inc2018-10-18Not applicableUS 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)KitOphthalmic; 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)KitTopicalHoneywell 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)KitTopicalHoneywell Safety Products USA, Inc2018-11-21Not applicableUS flag
4066 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, Inc2018-11-21Not applicableUS flag
4067 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, Inc2018-11-21Not applicableUS flag
4125 First Aid KitPolymyxin B sulfate (5000 [iU]/1g) + Ammonia (0.045 g/0.3mL) + Bacitracin zinc (400 [iU]/1g) + Benzalkonium chloride (1.3 mg/1mL) + Benzethonium chloride (0.2 g/100g) + Benzethonium chloride (0.2 g/100g) + Benzocaine (10 g/100g) + Benzocaine (10 g/100g) + Isopropyl alcohol (0.7 mL/1mL) + Levomenthol (0.33 g/100g) + Neomycin sulfate (3.5 mg/1g) + Water (98.6 mL/100mL)KitOphthalmic; Respiratory (inhalation); TopicalHoneywell Safety Products USA, Inc2018-10-18Not applicableUS flag
4135 First Aid KitPolymyxin B sulfate (5000 [iU]/1g) + Ammonia (0.045 g/0.3mL) + Bacitracin zinc (400 [iU]/1g) + Benzalkonium chloride (1.3 mg/1mL) + Neomycin sulfate (3.5 mg/1g) + Povidone-iodine (10 mg/1mL) + Water (98.6 mL/100mL)KitOphthalmic; Respiratory (inhalation); TopicalHoneywell Safety Products USA, Inc.2018-09-13Not applicableUS flag
4138 First Aid KitPolymyxin B sulfate (5000 [iU]/1g) + Bacitracin zinc (400 [iU]/1g) + Benzalkonium chloride (1.3 mg/1mL) + Ethanol (0.5 mL/1mL) + Isopropyl alcohol (0.7 mL/1mL) + Lidocaine hydrochloride (2 g/100g) + Lidocaine hydrochloride (20 mg/1mL) + Neomycin sulfate (3.5 mg/1g) + Water (98.6 mL/100mL)KitOphthalmic; TopicalHoneywell Safety Products USA, Inc.2018-09-13Not applicableUS flag

Categories

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

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. [PubMed:30909507]
  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. [PubMed:30875778]
  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. [PubMed:26324262]
  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. [PubMed:28275006]
  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. [PubMed:23701329]
  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. [PubMed:18840079]
  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
AHFS Codes
  • 08:12.28.28 — Polymyxins
FDA label
Download (219 KB)
MSDS
Download (127 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedPreventionAntibiotic Allergy / Antibiotic Side Effect / Eyelid Diseases / Eyelid; Wound / Postoperative Wound Infection / Skin Cancer Face / Surgical Incision / Surgical Site Infections / Surgical Wound, Recent1
4CompletedPreventionEnd Stage Renal Disease (ESRD)1
4CompletedPreventionUrinary Tract Infection1
4CompletedTreatmentActinic Keratosis (AK)1
4CompletedTreatmentConjunctivitis1
4Unknown StatusTreatmentHospital Infection1
3CompletedTreatmentDermatitis, Eczematous1
3RecruitingTreatmentIllness, Critical / Resistant Infection / Traumas1
3Unknown StatusTreatmentAcute / Bacterial Conjunctivitis1
3Unknown StatusTreatmentHordeolum1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
KitOphthalmic; Oral; Respiratory (inhalation); Topical
KitOphthalmic; Respiratory (inhalation); Topical
KitOral; Respiratory (inhalation); Topical
KitRespiratory (inhalation); Topical
KitIrrigation; Ophthalmic; Respiratory (inhalation); Topical
KitIrrigation; Ophthalmic; Topical
KitIrrigation; Oral; Respiratory (inhalation); Topical
KitIrrigation; Ophthalmic; Oral; Respiratory (inhalation); Topical
KitOral; Topical
KitTopical
Powder, for solutionIntramuscular; Intrathecal; Intravenous; Respiratory (inhalation); Topical
OintmentOphthalmic1 mg
Solution / dropsOral1000000 IU
Ointment500 IU/g
OintmentCutaneous12.5 mg
Ointment; swabTopical
KitElectro-osmosis
OintmentOphthalmic1 mg/g
SolutionCutaneous200 U
SuspensionOphthalmic3.5 mg
SuspensionOphthalmic1 mg
CreamTopical
SolutionAuricular (otic)
SuspensionTopical
KitOral
SolutionConjunctival; Ophthalmic1 mg
Ointment5 mg
Solution / dropsOphthalmic1 mg/ml
SolutionAuricular (otic); Topical1 mg
OintmentTopical30 mg/g
KitOphthalmic; Oral; Topical
KitOphthalmic
KitOphthalmic; Topical
LozengeBuccal
StickTopical
OintmentOphthalmic3.5 mg/g
Suspension / dropsAuricular (otic)50 mg/vial
SolutionIntraocular; Ophthalmic1 mg
IrrigantIrrigation
SolutionIrrigation
OintmentOphthalmic
SuspensionOphthalmic
Solution / dropsOphthalmic
Solution / dropsAuricular (otic)
Suspension / dropsAuricular (otic)
Suspension / dropsOphthalmic
SolutionConjunctival; Ophthalmic5 mg
SolutionAuricular (otic); Ophthalmic
SolutionUrethral
Solution / dropsOphthalmic25 IU
SolutionOphthalmic1.3 mg
Solution / dropsOphthalmic5 mg
Solution / dropsOphthalmic1 mg
SolutionConjunctival; Ophthalmic10000 IU
GelTopical
SolutionConjunctival; Ophthalmic1.3 mg
Solution / dropsAuricular (otic)2 %w/v
SolutionAuricular (otic)1 mg
Solution / dropsAuricular (otic)1 mg/ml
LiquidAuricular (otic)
SuspensionAuricular (otic)
Suspension / dropsAuricular (otic)10000 u
OintmentTopical10000 U
OintmentOphthalmic10000 U
InjectionIntramuscular; Intrathecal; Intravenous500000 iu
Injection, powder, lyophilized, for solutionIntramuscular; Intrathecal; Intravenous500000 units
OintmentTopical3.5 mg/g
LiquidAuricular (otic); Ophthalmic
OintmentOphthalmic0.025 mg
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; Intravenous; Ophthalmic500000 [iU]/1
Injection, powder, lyophilized, for solutionIntramuscular; Intrathecal; Intravenous; Ophthalmic500000 [USP'U]/1
Injection, powder, lyophilized, for solutionIntramuscular; Intrathecal; Intravenous; Ophthalmic500000 1/1
Injection, powder, lyophilized, for solutionIntramuscular; Intravenous500000 [USP'U]/1
Injection, solutionIntramuscular; Intrathecal; Intravenous; Ophthalmic500000 1/1
Powder, for solutionIntramuscular; Intrathecal; Intravenous; Ophthalmic
InjectionIntramuscular; Intrathecal; Intravenous500000 i.u.
PowderTopical
Solution / dropsAuricular (otic); Ophthalmic
OintmentOphthalmic; Topical
Injection, powder, lyophilized, for solutionIntramuscular; Intrathecal; Intravenous500000 IU
OintmentOphthalmic5 mg/ml
LozengeOral
OintmentTopical
SolutionOphthalmic
OintmentOphthalmic0.5 g
OintmentOphthalmic5 mg/G
OintmentConjunctival; Ophthalmic0.5 g
Ointment500 IU
SolutionOphthalmic1 mg
SwabTopical
OintmentOphthalmic1 g
SuspensionConjunctival; Ophthalmic1 mg
OintmentConjunctival; Ophthalmic0.1 g
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
Not Available

Targets

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 . [PubMed:18447592]
  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. [PubMed:17878146]

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. [PubMed:26494147]

Drug created on February 28, 2019 16:07 / Updated on February 24, 2021 19:34