colistin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
4425 1066-17-7

Description:

MoleculeDescription

Synonyms:

  • colistin
  • colimycin
  • Polymyxin E
  • colistin sulfate
  • colistins sulfate
Cyclic polypeptide antibiotic from Bacillus colistinus. It is composed of Polymyxins E1 and E2 (or Colistins A, B, and C) which act as detergents on cell membranes. Colistin is less toxic than Polymyxin B, but otherwise similar; the methanesulfonate is used orally.
  • Molecular weight: 2324.94
  • Formula: C105H198N32O26
  • CLOGP:
  • LIPINSKI: None
  • HAC: None
  • HDO: None
  • TPSA: 490.66
  • ALOGS:
  • ROTB: None

Drug dosage:

DoseUnitRoute
9 MU O
3 MU Inhal.powder
3 MU Inhal.solution
9 MU P

ADMET properties:

PropertyValueReference
BA (Bioavailability) 0 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Predicted pharmacokinetic/toxicological properties (PK-AZ):

None

Approvals:

DateAgencyCompanyOrphan
May 17, 1962 FDA PAR STERILE PRODUCTS

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Multiple organ dysfunction syndrome 192.25 33.30 73 2591 68263 90557520
Drug resistance 160.62 33.30 52 2612 30397 90595386
Infective pulmonary exacerbation of cystic fibrosis 131.86 33.30 35 2629 10244 90615539
Pathogen resistance 120.30 33.30 31 2633 8084 90617699
Septic shock 97.21 33.30 48 2616 84112 90541671
Pseudomonas infection 93.25 33.30 29 2635 14836 90610947
Geotrichum infection 85.85 33.30 15 2649 601 90625182
Drug ineffective 83.36 33.30 146 2518 1384152 89241631
Haemodynamic instability 57.57 33.30 19 2645 11720 90614063
Acinetobacter infection 51.86 33.30 12 2652 1996 90623787
Tonsillitis bacterial 50.68 33.30 8 2656 170 90625613
Morganella infection 50.37 33.30 10 2654 806 90624977
Renal failure 48.51 33.30 36 2628 130971 90494812
Osteomyelitis bacterial 47.93 33.30 8 2656 243 90625540
Klebsiella infection 47.83 33.30 16 2648 10281 90615502
Acute kidney injury 46.61 33.30 52 2612 320335 90305448
Haemostasis 44.53 33.30 8 2656 376 90625407
Fungaemia 41.00 33.30 11 2653 3339 90622444
Nephropathy toxic 40.83 33.30 15 2649 12673 90613110
Neutropenia 40.65 33.30 41 2623 224863 90400920
Sepsis 40.48 33.30 37 2627 179777 90446006
Klebsiella bacteraemia 38.87 33.30 10 2654 2582 90623201
Wound haemorrhage 37.87 33.30 10 2654 2857 90622926
Enterococcal infection 36.60 33.30 13 2651 9978 90615805
Respiratory failure 36.08 33.30 29 2635 118389 90507394
Neutropenic colitis 34.22 33.30 10 2654 4133 90621650

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Choroiditis 286.16 38.22 56 3835 1319 42616125
Drug resistance 268.45 38.22 105 3786 34143 42583301
Endophthalmitis 230.81 38.22 58 3833 4375 42613069
Drug ineffective 204.59 38.22 266 3625 629931 41987513
Pathogen resistance 184.50 38.22 60 3831 11390 42606054
Intraocular pressure increased 182.07 38.22 52 3839 6381 42611063
Uveitis 163.39 38.22 52 3839 9206 42608238
Septic shock 160.03 38.22 101 3790 91571 42525873
Eye pain 150.25 38.22 57 3834 16973 42600471
Visual acuity reduced 130.88 38.22 52 3839 17498 42599946
Infective pulmonary exacerbation of cystic fibrosis 102.11 38.22 35 3856 7783 42609661
Candida infection 94.81 38.22 44 3847 21566 42595878
Condition aggravated 92.62 38.22 116 3775 260638 42356806
Multiple organ dysfunction syndrome 84.04 38.22 70 3821 96965 42520479
Klebsiella infection 75.55 38.22 31 3860 11301 42606143
Geotrichum infection 69.86 38.22 15 3876 562 42616882
Sepsis 54.18 38.22 78 3813 199256 42418188
Gingivitis ulcerative 51.10 38.22 10 3881 234 42617210
Product use issue 44.03 38.22 44 3847 76707 42540737
Pseudomonas infection 42.03 38.22 23 3868 15900 42601544
Multiple-drug resistance 41.98 38.22 18 3873 7304 42610140
Gallstone ileus 40.57 38.22 6 3885 22 42617422
Systemic candida 40.44 38.22 16 3875 5303 42612141
Off label use 38.33 38.22 136 3755 638199 41979245

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Drug resistance 440.32 29.82 153 6266 56221 110526659
Pathogen resistance 292.04 29.82 85 6334 17587 110565293
Choroiditis 289.56 29.82 54 6365 1561 110581319
Drug ineffective 278.95 29.82 386 6033 1520154 109062726
Septic shock 263.55 29.82 144 6275 157384 110425496
Multiple organ dysfunction syndrome 238.10 29.82 133 6286 151577 110431303
Endophthalmitis 211.80 29.82 56 6363 8131 110574749
Infective pulmonary exacerbation of cystic fibrosis 191.78 29.82 59 6360 14712 110568168
Intraocular pressure increased 173.81 29.82 51 6368 10825 110572055
Geotrichum infection 145.76 29.82 29 6390 1183 110581697
Uveitis 139.19 29.82 51 6368 21659 110561221
Klebsiella infection 120.88 29.82 45 6374 19964 110562916
Visual acuity reduced 119.73 29.82 51 6368 32122 110550758
Eye pain 109.81 29.82 55 6364 50044 110532836
Pseudomonas infection 106.45 29.82 45 6374 27808 110555072
Sepsis 95.81 29.82 106 6313 327240 110255640
Candida infection 91.57 29.82 48 6371 47961 110534919
Acute kidney injury 88.55 29.82 143 6276 635287 109947593
Condition aggravated 71.01 29.82 141 6278 734695 109848185
Enterococcal infection 68.26 29.82 30 6389 20336 110562544
Multiple-drug resistance 62.88 29.82 25 6394 13210 110569670
Klebsiella bacteraemia 61.26 29.82 19 6400 4850 110578030
Haemodynamic instability 58.73 29.82 28 6391 22860 110560020
Acinetobacter infection 58.14 29.82 17 6402 3556 110579324
Venoocclusive liver disease 52.91 29.82 23 6396 15184 110567696
Eosinophilia 52.79 29.82 36 6383 57900 110524980
Respiratory failure 49.98 29.82 62 6357 215270 110367610
Fungaemia 49.23 29.82 17 6402 6069 110576811
Gingivitis ulcerative 48.07 29.82 10 6409 510 110582370
Systemic candida 47.94 29.82 19 6400 9955 110572925
Fatigue 43.34 29.82 9 6410 1215949 109366931
Leukocytosis 43.32 29.82 31 6388 53797 110529083
Tonsillitis bacterial 42.61 29.82 8 6411 239 110582641
Pain 41.12 29.82 4 6415 954951 109627929
Nephropathy toxic 40.01 29.82 23 6396 27455 110555425
Renal failure 39.89 29.82 57 6362 226517 110356363
Morganella infection 38.37 29.82 10 6409 1369 110581511
Drug reaction with eosinophilia and systemic symptoms 37.64 29.82 34 6385 82061 110500819
Burkholderia cepacia complex infection 37.16 29.82 8 6411 481 110582399
Haemostasis 36.14 29.82 8 6411 548 110582332
Osteomyelitis bacterial 35.90 29.82 8 6411 565 110582315
Drug interaction 35.59 29.82 85 6334 500098 110082782
Off label use 34.84 29.82 175 6244 1500010 109082870
Flavobacterium infection 33.81 29.82 6 6413 130 110582750
Thrombocytopenia 33.59 29.82 67 6352 348818 110234062
Acute respiratory distress syndrome 30.41 29.82 25 6394 53173 110529707

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC A07AA10 ALIMENTARY TRACT AND METABOLISM
ANTIDIARRHEALS, INTESTINAL ANTIINFLAMMATORY/ANTIINFECTIVE AGENTS
INTESTINAL ANTIINFECTIVES
Antibiotics
ATC J01XB01 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIBACTERIALS FOR SYSTEMIC USE
OTHER ANTIBACTERIALS
Polymyxins
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000900 Anti-Bacterial Agents
CHEBI has role CHEBI:33281 antimicrobial agent
CHEBI has role CHEBI:33282 antibacterial agent
CHEBI has role CHEBI:35441 antiinfective agent
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:50909 nephrotoxic agent

Related Drugs by ATC class:

A07AA Antibiotics 12 drugs
amphotericin BfidaxomicinkanamycinnatamycinneomycinnystatinparomomycinPolymyxin Brifamycinrifaximinstreptomycinvancomycin
J01XB Polymyxins 1 drug
Polymyxin B

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Otitis externa indication 3135009
Infection due to Escherichia coli indication 71057007
Enterobacter Infection indication
Pseudomonas Aeruginosa Infections indication
Mastoidectomy Cavity Infections indication
Klebsiella Infections indication
Chronic purulent otitis media off-label use 38394007 DOID:14247
Pseudomonas Respiratory Tract Infection in Cystic Fibrosis off-label use
Herpes zoster auricularis contraindication 21954000 DOID:9210
Bullous myringitis contraindication 33528003 DOID:13791
Neuromuscular block, function contraindication 55394004
Perforation of tympanic membrane contraindication 60442001
Herpes simplex contraindication 88594005 DOID:8566
Kidney disease contraindication 90708001 DOID:557
Myasthenia gravis contraindication 91637004 DOID:437
Tuberculosis of ear contraindication 186269001
Viral ear infection contraindication 312137007
Fungal ear infection contraindication 312148000
Pseudomembranous enterocolitis contraindication 397683000




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Epidermal growth factor receptor Kinase IC50 5.82 DRUG MATRIX
Tyrosine-protein kinase Fyn Kinase IC50 6.02 DRUG MATRIX
Receptor tyrosine-protein kinase erbB-2 Kinase IC50 5.65 DRUG MATRIX
Melanocortin receptor 4 GPCR Ki 6.09 DRUG MATRIX
Melanocortin receptor 5 GPCR Ki 6.60 DRUG MATRIX
Melanocortin receptor 3 GPCR Ki 6.78 DRUG MATRIX

External reference:

IDSource
D02138 KEGG_DRUG
4019695 VUID
N0000147787 NUI
1264-72-8 SECONDARY_CAS_RN
4018640 VANDF
4019695 VANDF
C0009316 UMLSCUI
CHEBI:37943 CHEBI
CHEMBL6067481 ChEMBL_ID
CHEMBL1201441 ChEMBL_ID
CHEMBL6067482 ChEMBL_ID
DB00803 DRUGBANK_ID
10794 IUPHAR_LIGAND_ID
916 INN_ID
Z67X93HJG1 UNII
5311054 PUBCHEM_CID
2709 RXNORM
11126 MMSL
4496 MMSL
002804 NDDF
004903 NDDF
23375008 SNOMEDCT_US
387412007 SNOMEDCT_US
73074003 SNOMEDCT_US
D003091 MESH_DESCRIPTOR_UI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Cortisporin-TC HUMAN PRESCRIPTION DRUG LABEL 4 54868-0564 SUSPENSION 3 mg AURICULAR (OTIC) NDA 22 sections
Cortisporin TC HUMAN PRESCRIPTION DRUG LABEL 4 63481-529 SUSPENSION 3 mg AURICULAR (OTIC) NDA 22 sections