Polymyxin B

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 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

Small Molecule

Groups

Approved, Vet approved

Structure

Similar Structures

Weight: Average: 1203.499
Monoisotopic: 1202.74992728
Chemical Formula: C₅₆H₉₈N₁₆O₁₃

Synonyms

Polimixina B
Polymyxin B
Polymyxine B
Polymyxinum B

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 aeruginosa^Label.

Associated Conditions

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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

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.

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.

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.
Acyclovir	The risk or severity of adverse effects can be increased when Acyclovir is combined with Polymyxin B.
Adefovir dipivoxil	The risk or severity of adverse effects can be increased when Adefovir dipivoxil is combined with Polymyxin B.
Alclofenac	The risk or severity of adverse effects can be increased when Alclofenac is combined with Polymyxin B.
Alimemazine	Alimemazine may increase the neurotoxic activities of Polymyxin B.
Amikacin	The risk or severity of adverse effects can be increased when Amikacin is combined with Polymyxin B.

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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		Intramuscular; Intrathecal; Intravenous; Respiratory (inhalation); Topical	Glaxo Wellcome	1952-12-31	1998-07-30
Polymyxin B for Injection USP	Powder, for solution		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 1/1	Intramuscular; Intrathecal; Intravenous; Ophthalmic	Gland Pharma Limited	2016-06-01	Not applicable
Polymyxin B	Injection, powder, for solution	500000 [iU]/1	Intramuscular; Intrathecal; Intravenous; Ophthalmic	Sagent Pharmaceuticals	2011-08-01	2014-03-31
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, lyophilized, for solution	500000 [USP'U]/1	Intramuscular; Intrathecal; Intravenous; Ophthalmic	X-GEN Pharmaceuticals, Inc.	2014-01-15	2020-02-25
Polymyxin B	Injection, powder, lyophilized, for solution	500000 [USP'U]/1	Intramuscular; Intrathecal; Intravenous; Ophthalmic	X-GEN Pharmaceuticals, Inc.	1994-09-30	Not applicable
Polymyxin B	Injection, powder, lyophilized, for solution	500000 [iU]/1	Intramuscular; Intrathecal; Intravenous; Ophthalmic	Alvogen Inc.	2017-09-23	Not applicable
Polymyxin B	Injection	500000 1/1	Intramuscular; Intrathecal; Intravenous	Xellia Pharmaceuticals ApS	2014-01-24	Not applicable
Polymyxin B	Injection, powder, lyophilized, for solution	500000 [USP'U]/1	Intramuscular; Intrathecal; Intravenous; Ophthalmic	AuroMedics Pharma LLC	2016-04-04	Not applicable
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

Mixture Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End
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)	Kit	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)	Kit	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)	Kit	Topical	Honeywell Safety Products USA, Inc	2018-11-21	Not applicable
4066 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	Not applicable
4067 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	Not applicable
4125 First Aid Kit	Polymyxin 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)	Kit	Ophthalmic; Respiratory (inhalation); Topical	Honeywell Safety Products USA, Inc	2018-10-18	Not applicable

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)	Kit	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)	Kit	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)	Kit	Topical	Honeywell Safety Products USA, Inc	2018-11-21	Not applicable
4066 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	Not applicable
4067 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	Not applicable
4125 First Aid Kit	Polymyxin 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)	Kit	Ophthalmic; Respiratory (inhalation); Topical	Honeywell Safety Products USA, Inc	2018-10-18	Not applicable
4135 First Aid Kit	Polymyxin 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)	Kit	Ophthalmic; Respiratory (inhalation); Topical	Honeywell Safety Products USA, Inc.	2018-09-13	Not applicable
4138 First Aid Kit	Polymyxin 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)	Kit	Ophthalmic; Topical	Honeywell Safety Products USA, Inc.	2018-09-13	Not applicable

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

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]
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]
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]
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]
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]
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]
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

AHFS Codes

08:12.28.28 — Polymyxins

FDA label

Download (219 KB)

MSDS

Download (127 KB)

Clinical Trials

Clinical Trials

Phase	Status	Purpose	Conditions	Count
4	Completed	Prevention	Antibiotic Allergy / Antibiotic Side Effect / Eyelid Diseases / Eyelid; Wound / Postoperative Wound Infection / Skin Cancer Face / Surgical Incision / Surgical Site Infections / Surgical Wound, Recent	1
4	Completed	Prevention	End Stage Renal Disease (ESRD)	1
4	Completed	Prevention	Urinary Tract Infection	1
4	Completed	Treatment	Actinic Keratosis (AK)	1
4	Completed	Treatment	Conjunctivitis	1
4	Unknown Status	Treatment	Hospital Infection	1
3	Completed	Treatment	Dermatitis, Eczematous	1
3	Recruiting	Treatment	Illness, Critical / Resistant Infection / Traumas	1
3	Unknown Status	Treatment	Acute / Bacterial Conjunctivitis	1
3	Unknown Status	Treatment	Hordeolum	1

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Not Available

Dosage Forms

Form	Route	Strength
Kit	Ophthalmic; Oral; Respiratory (inhalation); Topical
Kit	Ophthalmic; Respiratory (inhalation); Topical
Kit	Oral; Respiratory (inhalation); Topical
Kit	Respiratory (inhalation); Topical
Kit	Irrigation; Ophthalmic; Respiratory (inhalation); Topical
Kit	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
Solution / drops	Oral
Ointment
Ointment	Cutaneous
Ointment; swab	Topical
Kit	Electro-osmosis
Solution	Cutaneous
Cream	Topical
Solution	Auricular (otic)
Suspension	Topical
Kit	Oral
Solution	Auricular (otic); Topical
Kit	Ophthalmic; Oral; Topical
Kit	Ophthalmic
Kit	Ophthalmic; Topical
Lozenge	Buccal
Stick	Topical
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
Solution	Auricular (otic); Ophthalmic
Solution	Urethral
Gel	Topical
Solution	Conjunctival; Ophthalmic
Liquid	Auricular (otic)
Suspension	Auricular (otic)
Injection, solution	Intramuscular; Intrathecal; Intravenous
Liquid	Auricular (otic); Ophthalmic
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; Ophthalmic	500000 [iU]/1
Injection, powder, lyophilized, for solution	Intramuscular; Intrathecal; Intravenous; Ophthalmic	500000 [USP'U]/1
Injection, powder, lyophilized, for solution	Intramuscular; Intrathecal; Intravenous; Ophthalmic	500000 1/1
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
Powder	Topical
Solution / drops	Auricular (otic); Ophthalmic
Ointment	Ophthalmic; Topical
Injection, powder, lyophilized, for solution	Intramuscular; Intrathecal; Intravenous
Lozenge	Oral
Ointment	Topical
Solution	Ophthalmic
Swab	Topical
Suspension	Conjunctival; Ophthalmic
Ointment	Conjunctival; Ophthalmic
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
pKa	8.9	https://www.chemicalbook.com/ChemicalProductProperty_US_CB8666707.aspx

Predicted Properties

Property	Value	Source
Water Solubility	0.0744 mg/mL	ALOGPS
logP	-0.89	ALOGPS
logP	-7.2	ChemAxon
logS	-4.2	ALOGPS
pKa (Strongest Acidic)	11.57	ChemAxon
pKa (Strongest Basic)	10.23	ChemAxon
Physiological Charge	5	ChemAxon
Hydrogen Acceptor Count	18	ChemAxon
Hydrogen Donor Count	18	ChemAxon
Polar Surface Area	490.66 Å²	ChemAxon
Rotatable Bond Count	29	ChemAxon
Refractivity	313.22 m³·mol^-1	ChemAxon
Polarizability	127.4 Å³	ChemAxon
Number of Rings	2	ChemAxon
Bioavailability	0	ChemAxon
Rule of Five	No	ChemAxon
Ghose Filter	No	ChemAxon
Veber's Rule	No	ChemAxon
MDDR-like Rule	No	ChemAxon

Predicted ADMET Features

Not Available

Spectra

Mass Spec (NIST): Not Available
Spectra: Not Available

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 . [PubMed:18447592]
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

Details1. Solute carrier family 15 member 2

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

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 April 07, 2021 04:45

Polymyxin B

Identification

Structure for Polymyxin B (DB00781)

Pharmacology

Interactions

Products

Categories

Chemical Identifiers

References

Clinical Trials

Pharmacoeconomics

Properties

Spectra

Targets

References

Transporters

References