Polymyxin B

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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 nephrotoxic^4,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 aeruginosa^Label. Polymyxin B has a narrow therapeutic index and so its use is limited and unlikely to be used first line⁵.

Type

Biotech

Groups

Approved, Vet approved

Biologic Classification

Protein Based Therapies
Peptides

Protein Chemical Formula

Not Available

Protein Average Weight

Not Available

Sequences

Not Available

Synonyms

Polimixina B
Polymyxin B
Polymyxine B
Polymyxinum B

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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 aeruginosa^Label.

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Associated Conditions

Indication Type	Indication	Combined Product Details	Approval Level	Patient Characteristics	Dose Form
Used in combination to treat	Acute otitis media	Combination Product in combination with: Neomycin (DB00994), Lidocaine (DB00281)	••• •••		••••••••• •••••••• • •••••
Treatment of	Bacteremia caused by enterobacter aerogenes		••••••••••••
Used in combination to treat	Bacterial conjunctivitis	Combination Product in combination with: Neomycin (DB00994), Prednisolone acetate (DB15566)	••••••••••••
Treatment of	Bacterial infections		••••••••••••
Treatment of	Bacterial 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 processes^6,1. Polymyxin B is generally indicated for susceptible Gram negative infections of the urinary tract, meninges, and blood stream^Label.

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.

Target	Actions	Organism
ABacterial outer membrane	incorporation into and destabilization	Bacteria
ADihydropteroate synthase	binder	Escherichia coli (strain K12)

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 pathways^1,8. 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.

Drug	Interaction
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Aceclofenac	The risk or severity of adverse effects can be increased when Aceclofenac is combined with Polymyxin B.
Acemetacin	The risk or severity of adverse effects can be increased when Acemetacin is combined with Polymyxin B.
Acenocoumarol	The risk or severity of bleeding can be increased when Polymyxin B is combined with Acenocoumarol.
Acetophenazine	Acetophenazine may increase the neurotoxic activities of Polymyxin B.
Acetylsalicylic acid	The 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

Ingredient	UNII	CAS	InChI Key
Polymyxin B sulfate	19371312D4	1405-20-5	HFMDLUQUEXNBOP-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

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Aerosporin Sterile Powder	Powder, for solution	500000 unit / vial	Intramuscular; Intrathecal; Intravenous; Respiratory (inhalation); Topical	Glaxo Wellcome Indonesia	1952-12-31	1998-07-30
Polymyxin B for Injection USP	Powder, for solution	50 mg / vial	Intramuscular; Intrathecal; Intravenous; Ophthalmic	Sterimax Inc	2012-05-03	Not applicable

Generic Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Polymyxin B	Injection, powder, lyophilized, for solution	500000 [USP'U]/1	Intramuscular; Intravenous	X-GEN Pharmaceuticals, Inc.	2014-04-25	2020-02-25
Polymyxin B	Injection, powder, for solution	500000 [USP'U]/1	Intramuscular; Intrathecal; Intravenous; Ophthalmic	Xellia Pharmaceuticals USA LLC	2018-10-01	Not applicable
Polymyxin B	Injection, powder, lyophilized, for solution	500000 [iU]/1	Intramuscular; Intrathecal; Intravenous; Ophthalmic	Athenex Pharmaceutical Division, Llc.	2017-01-01	Not applicable
Polymyxin B	Injection, powder, for solution	500000 [iU]/1	Intramuscular; Intrathecal; Intravenous; Ophthalmic	Bedford Pharmaceuticals	1998-06-01	2014-03-31
Polymyxin B	Injection, powder, lyophilized, for solution	500000 [USP'U]/1	Intramuscular; Intrathecal; Intravenous; Ophthalmic	Fosun Pharma USA Inc	2016-06-10	Not applicable

Mixture Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End
0.9g Triple Antibiotic	Polymyxin B sulfate (5000 [USP'U]/1g) + Bacitracin zinc (400 [USP'U]/1g) + Neomycin sulfate (0.0035 g/1g)	Ointment	Topical	Sled Distribution, LLC	2022-03-24	Not applicable
10 Person ANSI	Polymyxin 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)	Kit	Ophthalmic; Oral; Topical	Genuine First Aid	2010-04-24	Not applicable
25 Person ANSI	Polymyxin 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)	Kit	Ophthalmic; Oral; Topical	Genuine First Aid	2010-04-25	Not applicable
4032 First Aid Kit	Polymyxin 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; Tablet	Ophthalmic; Oral; Respiratory (inhalation); Topical	Honeywell Safety Products USA, Inc	2018-10-18	Not applicable
4042 First Aid Kit	Polymyxin 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)	Kit	Topical	Honeywell Safety Products USA, Inc	2018-11-21	2019-10-18

Unapproved/Other Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End
4032 First Aid Kit	Polymyxin 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; Tablet	Ophthalmic; Oral; Respiratory (inhalation); Topical	Honeywell Safety Products USA, Inc	2018-10-18	Not applicable
4042 First Aid Kit	Polymyxin 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)	Kit	Topical	Honeywell Safety Products USA, Inc	2018-11-21	2019-10-18
4050 First Aid Kit	Polymyxin 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)	Kit	Topical	Honeywell Safety Products USA, Inc	2018-11-21	2019-10-18
4064 First Aid Kit	Polymyxin 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; Swab	Topical	Honeywell Safety Products USA, Inc	2018-11-21	2019-10-18
4065 First Aid Kit	Polymyxin 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; Swab	Topical	Honeywell Safety Products USA, Inc	2018-11-21	Not applicable

Chemical Identifiers

UNII: J2VZ07J96K
CAS number: 1404-26-8

References

General References

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]
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]
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]
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]
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]
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]
SteriMax Inc: Polymyxin B for Injection USP Monograph [Link]
Product Monograph: Polymyxin B For Injection USP [File]

External Links

ChemSpider: 25045120
BindingDB: 50410807
RxNav: 8536
ChEMBL: CHEMBL1201283
Wikipedia: Polymyxin_B

FDA label

Download (219 KB)

MSDS

Download (127 KB)

Clinical Trials

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Phase	Status	Purpose	Conditions	Count	Start Date	Why Stopped	100+ additional columns
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Not Available	Completed	Prevention	Infection / Surgery	1	somestatus	stop reason	just information to hide
Not Available	Completed	Treatment	Corneal Diseases	1	somestatus	stop reason	just information to hide
Not Available	Completed	Treatment	Herpes Simplex / Human Immunodeficiency Virus (HIV) Infections	1	somestatus	stop reason	just information to hide
Not Available	Completed	Treatment	Mastectomy Flap Necrosis	1	somestatus	stop reason	just information to hide
Not Available	Completed	Treatment	Nasal Carriers of Staphylococcus Aureus	1	somestatus	stop reason	just information to hide

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Not Available

Dosage Forms

Form	Route	Strength
Inhalant; kit; liquid; ointment; spray; tablet	Ophthalmic; Oral; Respiratory (inhalation); Topical
Cream; kit; liquid; ointment; swab	Topical
Gel; inhalant; kit; liquid; ointment	Ophthalmic; Respiratory (inhalation); Topical
Cream; kit; liquid; ointment; swab; tablet	Ophthalmic; Oral; Topical
Cream; kit; liquid; ointment; swab	Ophthalmic; Topical
Kit	Ophthalmic; Oral; Respiratory (inhalation); Topical
Kit	Ophthalmic; Respiratory (inhalation); Topical
Kit	Oral; Respiratory (inhalation); Topical
Kit; liquid; ointment; swab	Ophthalmic; Topical
Inhalant; kit; liquid; ointment; spray; swab; tablet	Ophthalmic; Oral; Respiratory (inhalation); Topical
Kit	Respiratory (inhalation); Topical
Gel; kit; liquid; ointment; swab	Ophthalmic; Topical
Inhalant; kit; liquid; ointment; spray; swab	Ophthalmic; Respiratory (inhalation); Topical
Kit; liquid; ointment; spray; swab	Ophthalmic; Topical
Cream; kit; liquid; ointment; spray; tablet	Ophthalmic; Oral; Topical
Cream; kit; liquid; ointment; swab; tablet	Oral; Topical
Cream; kit; liquid; ointment	Topical
Gel; kit; ointment; swab	Topical
Cream; kit; ointment; swab	Topical
Gel; kit; liquid; ointment	Ophthalmic; Topical
Kit; liquid; ointment; swab; tablet	Ophthalmic; Oral; Topical
Gel; kit; liquid; ointment; solution; swab	Ophthalmic; Topical
Kit; liquid; ointment; swab	Topical
Gel; kit; liquid; ointment	Topical
Gel; kit; liquid; ointment; swab	Topical
Cream; gel; kit; liquid; ointment; swab	Ophthalmic; Topical
Kit; liquid; ointment; spray; tablet	Ophthalmic; Oral; Topical
Cream; gel; kit; liquid; ointment; spray; swab	Ophthalmic; Topical
Kit; liquid; ointment	Topical
Gel; kit; liquid; ointment; swab; tablet	Oral; Topical
Kit; liquid; ointment	Ophthalmic; Topical
Kit	Irrigation; Ophthalmic; Respiratory (inhalation); Topical
Cream; irrigant; kit; liquid; ointment; swab	Irrigation; Ophthalmic; Topical
Kit	Irrigation; Oral; Respiratory (inhalation); Topical
Kit	Irrigation; Ophthalmic; Oral; Respiratory (inhalation); Topical
Kit	Oral; Topical
Kit	Topical
Powder, for solution	Intramuscular; Intrathecal; Intravenous; Respiratory (inhalation); Topical	500000 unit / vial
Solution	Other
Solution / drops	Oral
Solution	Auricular (otic); Ophthalmic
Ointment
Ointment	Cutaneous
Ointment; swab	Topical
Kit	Electro-osmosis
Cloth; kit; ointment; swab	Topical
Ointment	Ophthalmic	10 mg
Ointment	Ophthalmic	1 mg/g
Solution	Cutaneous
Solution / drops	Ophthalmic	5 mg/ml
Cream	Topical
Solution	Auricular (otic)
Suspension	Topical
Kit	Oral
Cream; kit; liquid; ointment; tablet; tablet, chewable; tablet, film coated	Oral; Topical
Kit	Ophthalmic; Topical
Liquid	Topical
Solution	Auricular (otic); Topical
Kit	Ophthalmic; Oral; Topical
Cream; kit; tablet, film coated	Oral; Topical
Cloth; cream; gel; kit; ointment; solution	Ophthalmic; Topical
Kit	Ophthalmic
Lozenge	Buccal
Stick	Topical
Suspension	Conjunctival; Ophthalmic	1 mg
Solution	Conjunctival; Ophthalmic
Solution	Intravenous	5 mg
Solution / drops	Auricular (otic)	1 mg/ml
Solution	Intraocular; Ophthalmic
Irrigant	Irrigation
Solution	Irrigation
Ointment	Ophthalmic
Suspension	Ophthalmic
Solution / drops	Ophthalmic
Solution / drops	Auricular (otic)
Suspension / drops	Auricular (otic)
Suspension / drops	Ophthalmic
Suspension / drops	Topical
Solution	Urethral
Kit; ointment	Topical
Ointment	Conjunctival; Ophthalmic
Gel	Topical
Solution / drops	Auricular (otic)	10000 IU/ml
Liquid	Auricular (otic)
Suspension	Auricular (otic)
Injection, powder, lyophilized, for solution	Intramuscular; Intrathecal; Intravenous	500000 IU
Solution	Ophthalmic	1.3 mg
Injection, solution	Intramuscular; Intrathecal; Intravenous	500000 iu
Injection, solution	Intramuscular; Intrathecal; Intravenous
Injection, powder, lyophilized, for solution	Intramuscular; Intrathecal; Intravenous	500000 units
Liquid	Auricular (otic); Ophthalmic
Solution	Auricular (otic)	0.1 g/100ml
Solution / drops	Ophthalmic	0.025 mg/ml
Capsule	Vaginal
Capsule	Vaginal	35000 iu
Injection	Intramuscular; Intrathecal; Intravenous	500000 1/1
Injection, powder, for solution	Intramuscular; Intrathecal; Intravenous; Ophthalmic	500000 [iU]/1
Injection, powder, for solution	Intramuscular; Intrathecal; Intravenous; Ophthalmic	500000 [USP'U]/1
Injection, powder, lyophilized, for solution	Intramuscular; Intrathecal; Intravenous	500000 [USP'U]/1
Injection, powder, lyophilized, for solution	Intramuscular; Intrathecal; Intravenous; Ophthalmic	500000 [iU]/1
Injection, powder, lyophilized, for solution	Intramuscular; Intrathecal; Intravenous; Ophthalmic	500000 [USP'U]/1
Injection, powder, lyophilized, for solution	Intramuscular; Intravenous	500000 [USP'U]/1
Injection, solution	Intramuscular; Intrathecal; Intravenous; Ophthalmic	500000 1/1
Powder, for solution	Intramuscular; Intrathecal; Intravenous; Ophthalmic	50 mg / vial
Injection, solution	Intramuscular; Intrathecal; Intravenous	500000 i.u.
Powder	Topical
Solution / drops	Auricular (otic); Ophthalmic
Ointment	Ophthalmic; Topical
Injection, powder, lyophilized, for solution	Intramuscular; Intrathecal; Intravenous	50000000000 IU
Lozenge	Oral
Cloth; kit; ointment	Topical
Solution	Intravenous	89.600 mg
Powder	Intramuscular; Intrathecal; Intravenous	500000 IU
Ointment	Topical
Solution	Ophthalmic
Jelly; kit; ointment	Topical
Suspension	Conjunctival; Ophthalmic
Swab	Topical
Liquid	Ophthalmic

Prices

Not Available

Patents

Not Available

Properties

State

Solid

Experimental Properties

Property	Value	Source
melting point (°C)	>203	MSDS
water solubility	Soluble	MSDS

Targets

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1. Bacterial outer membrane

Kind

Group

Organism

Bacteria

Pharmacological action

Yes

Actions

Incorporation into and destabilization

References

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]
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]

Details2. Dihydropteroate synthase

Kind: Protein
Organism: Escherichia coli (strain K12)
Pharmacological action: Yes
Actions: Binder

General Function: Catalyzes the condensation of para-aminobenzoate (pABA) with 6-hydroxymethyl-7,8-dihydropterin diphosphate (DHPt-PP) to form 7,8-dihydropteroate (H2Pte), the immediate precursor of folate derivatives.
Specific Function: dihydropteroate synthase activity
Gene Name: folP
Uniprot ID: P0AC13
Uniprot Name: Dihydropteroate synthase
Molecular Weight: 30614.855 Da

References

Zhou Y, Zhang Y, Zhao D, Yu X, Shen X, Zhou Y, Wang S, Qiu Y, Chen Y, Zhu F: TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res. 2024 Jan 5;52(D1):D1465-D1477. doi: 10.1093/nar/gkad751. [Article]

Transporters

Details1. Solute carrier family 15 member 2

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Curator comments: Mediates drug reabsorption in the kidney

General Function: Proton-coupled amino-acid transporter that transports oligopeptides of 2 to 4 amino acids with a preference for dipeptides (PubMed:16434549, PubMed:18367661, PubMed:7756356). Transports neutral and anionic dipeptides with a proton to peptide stoichiometry of 2:1 or 3:1 (By similarity). In kidney, involved in the absorption of circulating di- and tripeptides from the glomerular filtrate (PubMed:7756356). Can also transport beta-lactam antibiotics, such as the aminocephalosporin cefadroxil, and other antiviral and anticancer drugs (PubMed:16434549). Transports the dipeptide-like aminopeptidase inhibitor bestatin (By similarity). Also able to transport carnosine (PubMed:31073693). Involved in innate immunity by promoting the detection of microbial pathogens by NOD-like receptors (NLRs) (By similarity). Mediates transport of bacterial peptidoglycans across the plasma membrane or, in macrophages, the phagosome membrane: catalyzes the transport of certain bacterial peptidoglycans, such as muramyl dipeptide (MDP), the NOD2 ligand (PubMed:20406817)
Specific Function: dipeptide transmembrane transporter activity
Gene Name: SLC15A2
Uniprot ID: Q16348
Uniprot Name: Solute carrier family 15 member 2
Molecular Weight: 81782.77 Da

References

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 October 13, 2024 03:42

Polymyxin B

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