colistin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | 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

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 165.73 30.48 64 2001 56688 63430269
Drug resistance 157.38 30.48 49 2016 22884 63464073
Infective pulmonary exacerbation of cystic fibrosis 119.41 30.48 32 2033 8785 63478172
Septic shock 88.05 30.48 43 2022 66586 63420371
Geotrichum infection 81.42 30.48 14 2051 460 63486497
Pathogen resistance 80.86 30.48 22 2043 6376 63480581
Pseudomonas infection 76.98 30.48 24 2041 11189 63475768
Morganella infection 51.32 30.48 10 2055 661 63486296
Osteomyelitis bacterial 48.59 30.48 8 2057 201 63486756
Acinetobacter infection 48.09 30.48 11 2054 1572 63485385
Haemodynamic instability 48.04 30.48 16 2049 9174 63477783
Haemostasis 47.16 30.48 8 2057 242 63486715
Klebsiella infection 45.12 30.48 15 2050 8551 63478406
Drug ineffective 39.71 30.48 97 1968 1044668 62442289
Fungaemia 38.62 30.48 10 2055 2393 63484564
Acute kidney injury 38.53 30.48 45 2020 263370 63223587
Enterococcal infection 38.39 30.48 13 2052 7835 63479122
Wound haemorrhage 38.16 30.48 10 2055 2506 63484451
Klebsiella bacteraemia 37.02 30.48 9 2056 1669 63485288
Neutropenic colitis 36.11 30.48 10 2055 3085 63483872

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 284.61 39.62 54 2917 1161 34952799
Endophthalmitis 238.01 39.62 56 2915 3452 34950508
Drug resistance 217.85 39.62 82 2889 25845 34928115
Intraocular pressure increased 185.57 39.62 50 2921 5333 34948627
Uveitis 168.94 39.62 50 2921 7485 34946475
Eye pain 159.63 39.62 55 2916 13407 34940553
Drug ineffective 149.63 39.62 187 2784 456564 34497396
Visual acuity reduced 131.54 39.62 50 2921 16099 34937861
Pathogen resistance 121.18 39.62 41 2930 9441 34944519
Septic shock 107.55 39.62 70 2901 71764 34882196
Infective pulmonary exacerbation of cystic fibrosis 105.30 39.62 34 2937 6767 34947193
Condition aggravated 104.29 39.62 103 2868 192093 34761867
Geotrichum infection 72.96 39.62 15 2956 489 34953471
Klebsiella infection 71.51 39.62 27 2944 8504 34945456
Multiple organ dysfunction syndrome 69.30 39.62 55 2916 76511 34877449
Candida infection 61.40 39.62 30 2941 17685 34936275
Product use issue 47.91 39.62 41 2930 63175 34890785
Sepsis 42.63 39.62 61 2910 166500 34787460
Multiple-drug resistance 41.79 39.62 16 2955 5223 34948737
Gallstone ileus 41.00 39.62 6 2965 22 34953938

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 378.11 31.87 129 4813 42084 79697362
Choroiditis 281.65 31.87 52 4890 1329 79738117
Endophthalmitis 211.80 31.87 54 4888 6374 79733072
Multiple organ dysfunction syndrome 197.36 31.87 111 4831 120135 79619311
Septic shock 192.49 31.87 110 4832 122691 79616755
Pathogen resistance 185.56 31.87 58 4884 14284 79725162
Infective pulmonary exacerbation of cystic fibrosis 183.27 31.87 56 4886 12795 79726651
Drug ineffective 173.34 31.87 267 4675 1080646 78658800
Intraocular pressure increased 170.01 31.87 49 4893 9156 79730290
Uveitis 140.91 31.87 49 4893 16781 79722665
Geotrichum infection 137.73 31.87 27 4915 954 79738492
Eye pain 115.21 31.87 53 4889 37525 79701921
Visual acuity reduced 114.24 31.87 49 4893 29420 79710026
Klebsiella infection 113.46 31.87 41 4901 15679 79723767
Pseudomonas infection 85.11 31.87 36 4906 20867 79718579
Condition aggravated 81.03 31.87 125 4817 500999 79238447
Acute kidney injury 80.43 31.87 127 4815 519277 79220169
Sepsis 62.45 31.87 80 4862 269348 79470098
Enterococcal infection 60.52 31.87 26 4916 15634 79723812
Klebsiella bacteraemia 59.93 31.87 17 4925 2993 79736453
Acinetobacter infection 56.71 31.87 16 4926 2761 79736685
Candida infection 56.40 31.87 33 4909 38181 79701265
Multiple-drug resistance 56.24 31.87 21 4921 8787 79730659
Haemodynamic instability 45.49 31.87 22 4920 17360 79722086
Fungaemia 44.78 31.87 15 4927 4576 79734870
Eosinophilia 43.92 31.87 30 4912 45315 79694131
Respiratory failure 40.72 31.87 53 4889 180858 79558588
Morganella infection 39.72 31.87 10 4932 1117 79738329
Systemic candida 39.23 31.87 15 4927 6691 79732755
Haemostasis 38.21 31.87 8 4934 394 79739052
Osteomyelitis bacterial 36.76 31.87 8 4934 474 79738972
Flavobacterium infection 35.09 31.87 6 4936 97 79739349
Burkholderia cepacia complex infection 34.13 31.87 7 4935 311 79739135
Fatigue 34.07 31.87 8 4934 929719 78809727

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 D000900 Anti-Bacterial Agents
MeSH PA D000890 Anti-Infective Agents
CHEBI has role CHEBI:50909 agente nefrotoxico

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
CHEMBL2221249 ChEMBL_ID
CHEMBL499783 ChEMBL_ID
CHEMBL507048 ChEMBL_ID
CHEMBL407135 ChEMBL_ID
CHEMBL1275798 ChEMBL_ID
CHEMBL2218908 ChEMBL_ID
DB00803 DRUGBANK_ID
10794 IUPHAR_LIGAND_ID
916 INN_ID
Z67X93HJG1 UNII
44144393 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