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

Stem definition	Drug id	CAS RN
	4425	1066-17-7

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
9	MU	O
3	MU	Inhal.powder
3	MU	Inhal.solution
9	MU	P

ADMET properties:

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

Approvals:

Date	Agency	Company	Orphan
May 17, 1962	FDA	PAR STERILE PRODUCTS

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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:

Source	Code	Description
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|

Disease	Relation	SNOMED_ID	DOID
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:

Target	Class	Pharos	UniProt	Type	Activity value (-log[M])	Bioact source
Epidermal growth factor receptor	Kinase	P00533	EGFR_HUMAN	IC50	5.82	DRUG MATRIX
Tyrosine-protein kinase Fyn	Kinase	P06241	FYN_HUMAN	IC50	6.02	DRUG MATRIX
Receptor tyrosine-protein kinase erbB-2	Kinase	P04626	ERBB2_HUMAN	IC50	5.65	DRUG MATRIX
Melanocortin receptor 4	GPCR	P32245	MC4R_HUMAN	Ki	6.09	DRUG MATRIX
Melanocortin receptor 5	GPCR	P33032	MC5R_HUMAN	Ki	6.60	DRUG MATRIX
Melanocortin receptor 3	GPCR	P41968	MC3R_HUMAN	Ki	6.78	DRUG MATRIX

External reference:

ID	Source
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:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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