colistin 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
Drug resistance 137.46 28.23 44 1923 17324 46666771
Multiple organ dysfunction syndrome 112.60 28.23 51 1916 51659 46632436
Infective pulmonary exacerbation of cystic fibrosis 109.07 28.23 33 1934 10774 46673321
Klebsiella infection 92.19 28.23 26 1941 6636 46677459
Pseudomonas infection 66.09 28.23 22 1945 9736 46674359
Acute kidney injury 60.30 28.23 61 1906 235794 46448301
Acinetobacter infection 57.04 28.23 13 1954 1409 46682686
Pathogen resistance 54.70 28.23 17 1950 6043 46678052
Osteomyelitis bacterial 47.54 28.23 8 1959 176 46683919
Morganella infection 46.11 28.23 9 1958 461 46683634
Haemostasis 45.22 28.23 8 1959 238 46683857
Haemodynamic instability 42.84 28.23 15 1952 7710 46676385
Septic shock 40.51 28.23 27 1940 57866 46626229
Klebsiella bacteraemia 37.89 28.23 9 1958 1167 46682928
Respiratory failure 36.70 28.23 31 1936 94785 46589310
Geotrichum infection 34.08 28.23 7 1960 465 46683630
Wound haemorrhage 32.60 28.23 9 1958 2118 46681977
Central nervous system fungal infection 30.41 28.23 5 1962 95 46684000

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
Drug resistance 159.04 33.38 62 2655 20071 29929690
Choroiditis 155.70 33.38 31 2686 804 29948957
Endophthalmitis 120.95 33.38 33 2684 3447 29946314
Septic shock 116.32 33.38 72 2645 63535 29886226
Pathogen resistance 111.53 33.38 38 2679 8372 29941389
Infective pulmonary exacerbation of cystic fibrosis 103.07 33.38 36 2681 8536 29941225
Intraocular pressure increased 99.87 33.38 31 2686 5089 29944672
Uveitis 97.81 33.38 31 2686 5446 29944315
Drug ineffective 97.08 33.38 135 2582 340252 29609509
Geotrichum infection 84.54 33.38 17 2700 463 29949298
Multiple organ dysfunction syndrome 82.23 33.38 58 2659 63429 29886332
Eye pain 81.43 33.38 33 2684 11756 29938005
Condition aggravated 67.20 33.38 72 2645 137794 29811967
Visual acuity reduced 65.81 33.38 31 2686 15815 29933946
Klebsiella infection 64.29 33.38 24 2693 6863 29942898
Candida infection 57.54 33.38 28 2689 15334 29934427
Acute kidney injury 52.81 33.38 91 2626 273751 29676010
Pseudomonas infection 48.15 33.38 22 2695 10460 29939301
Acinetobacter infection 46.62 33.38 12 2705 998 29948763
Sepsis 44.17 33.38 60 2657 146335 29803426
Gallstone ileus 40.61 33.38 6 2711 22 29949739
Multiple-drug resistance 37.82 33.38 13 2704 2928 29946833

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 (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

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 6.77 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
CHEMBL507048 ChEMBL_ID
CHEMBL2221249 ChEMBL_ID
CHEMBL499783 ChEMBL_ID
CHEMBL2218908 ChEMBL_ID
CHEMBL407135 ChEMBL_ID
CHEMBL1275798 ChEMBL_ID
DB00803 DRUGBANK_ID
D003091 MESH_DESCRIPTOR_UI
5311054 PUBCHEM_CID
10794 IUPHAR_LIGAND_ID
916 INN_ID
Z67X93HJG1 UNII
2709 RXNORM
11126 MMSL
4496 MMSL
002804 NDDF
004903 NDDF
23375008 SNOMEDCT_US
387412007 SNOMEDCT_US
73074003 SNOMEDCT_US

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