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

Stem definitionDrug idCAS RN
quinoline derivatives 1457 83-73-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • iodoquinol
  • diiodohydroxyquinoline
  • diiodohydroxyquin
  • diiodoquin
  • diiodoquinol
One of the halogenated 8-quinolinols widely used as an intestinal antiseptic, especially as an antiamebic agent. It is also used topically in other infections and may cause CNS and eye damage. It is known by very many similar trade names world-wide.
  • Molecular weight: 396.95
  • Formula: C9H5I2NO
  • CLOGP: 4.14
  • LIPINSKI: 0
  • HAC: 2
  • HDO: 1
  • TPSA: 33.12
  • ALOGS: -3.69
  • ROTB: 0

Drug dosage:

DoseUnitRoute
0.20 g V

ADMET properties:

PropertyValueReference
BA (Bioavailability) 8 %

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 4.107 Moderate 0.71
caco2-efflux Caco-2 efflux ratio (BA/AB) 0.303 Moderate 0.71
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 14.689 10^-6 cm/s Moderate 0.71
dh-clint Dog hepatocyte intrinsic clearance 148.936 uL/min/10^6 cells Moderate 0.71
dppb Dog plasma protein binding (% unbound) 0.170 % Moderate 0.71
fcs-ppb Fetal calf serum protein binding (% unbound) 0.240 % Moderate 0.71
herg hERG pIC50 4.702 pIC50 Moderate 0.71
hh-clint Human hepatocyte intrinsic clearance 100.462 uL/min/10^6 cells Moderate 0.71
hlm-clint Human liver microsomal intrinsic clearance 34.995 uL/min/mg protein Moderate 0.71
hppb Human plasma protein binding (% unbound) 0.380 % Moderate 0.71
kinase-safety-class ACVR2A,ACVR2B,ACVRL1,AKT2,AKT3,ALK,AURKA,AURKB,AURKC,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK1,CDK2,CDK4,CDK5,CDK7,CDK9,CHEK1,CLK4,CSF1R,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GSK3A,GSK3B,IKBKB,IRAK1,ITK,JAK1,JAK2,JAK3,KDR,KIT,MAP2K1,MAP2K6,MAP3K1,MAP3K10,MAP3K11,MAP3K14,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAPK1,MAPK10,MAPK12,MAPK7,MAPK8,MAPK9,MAPKAPK2,MARK4,MELK,MET,MTOR,NTRK2,PAK4,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PIM1,PIM2,PIM3,PLK1,PRKAA1,PRKCD,PRKDC,SGK1,SIK2,SIK3,STK10,STK33,SYK,TEK,TGFBR1,TTK,UHMK1,ULK1,ULK2,ZAP70 92
kinase-selectivity-class ACVR2B,AURKA,AXL,BRAF,CAMK2D,CDK4,CDK9,DDR1,DYRK1B,EIF2AK3,GRK2,GSK3B,MAP2K1,MAP2K3,MAP2K6,MAPK1,MAPK12,MAPK7,MARK4,PIK3CB,PRKDC,SIK2,STK33,SYK,TEK,TTK,ULK1 27
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 0.242 Moderate 0.71
mh-clint Mouse hepatocyte intrinsic clearance 483.059 Moderate 0.71
mppb Mouse plasma protein binding (% unbound) 0.370 Moderate 0.71
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 0.072 Moderate 0.71
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 0.200 % Moderate 0.71
rh-clint Rat hepatocyte intrinsic clearance 338.065 uL/min/10^6 cells Moderate 0.71
rh-fuinc Rat hepatocyte fraction unbound in incubation 4.440 % Moderate 0.71
rppb Rat plasma protein binding (% unbound) 0.120 % Moderate 0.71
solubility-dd Solubility at pH 7.4 in DMSO 1.156 uM Moderate 0.71

Approvals:

DateAgencyCompanyOrphan
None FDA

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC G01AC01 GENITO URINARY SYSTEM AND SEX HORMONES
GYNECOLOGICAL ANTIINFECTIVES AND ANTISEPTICS
ANTIINFECTIVES AND ANTISEPTICS, EXCL. COMBINATIONS WITH CORTICOSTEROIDS
Quinoline derivatives
MeSH PA D000563 Amebicides
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000977 Antiparasitic Agents
MeSH PA D000981 Antiprotozoal Agents
CHEBI has role CHEBI:33282 antibacterial agent
CHEBI has role CHEBI:35820 antiprotozoal drug
CHEBI has role CHEBI:48218 antiseptic drug
CHEBI has role CHEBI:171664 antiamoebic agent

Related Drugs by ATC class:

G01AC Quinoline derivatives 5 drugs

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

DiseaseRelationSNOMED_IDDOID
Amebic infection indication 111910009 DOID:9181
Atopic dermatitis off-label use 24079001 DOID:3310
Contact dermatitis off-label use 40275004 DOID:2773
Lichen simplex chronicus off-label use 53891004
Pruritus ani off-label use 90446007
Pruritus of genital organs off-label use 267802000
Eruption of skin off-label use 271807003 DOID:0050486
Optic neuritis contraindication 66760008 DOID:1210
Disease of liver contraindication 235856003 DOID:409
Telangiectasia disorder contraindication 247479008
Peripheral nerve disease contraindication 302226006
Adrenal cortical hypofunction contraindication 386584007 DOID:10493
Atrophoderma contraindication 399979006
Peripheral vascular disease contraindication 400047006




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 7.61 acidic
pKa2 2.03 Basic

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
Adenosine receptor A3 GPCR Ki 6.28 DRUG MATRIX
Epidermal growth factor receptor Kinase IC50 5.72 DRUG MATRIX
Tyrosine-protein kinase Lck Kinase IC50 5.61 DRUG MATRIX
Tyrosine-protein kinase Fyn Kinase IC50 5.80 DRUG MATRIX
Receptor tyrosine-protein kinase erbB-2 Kinase IC50 5.07 DRUG MATRIX
Mitogen-activated protein kinase 3 Kinase IC50 5.28 DRUG MATRIX
Mitogen-activated protein kinase 14 Kinase IC50 6.44 DRUG MATRIX
Mitogen-activated protein kinase 1 Kinase IC50 6.53 DRUG MATRIX
Angiotensin-converting enzyme Enzyme IC50 6.04 DRUG MATRIX
Catechol O-methyltransferase Enzyme IC50 5.25 CHEMBL
Beta-lactamase NDM-1 Enzyme IC50 5.60 CHEMBL

External reference:

IDSource
4018600 VUID
N0000146916 NUI
D00581 KEGG_DRUG
4018600 VANDF
C0012341 UMLSCUI
CHEBI:5950 CHEBI
CHEMBL86754 ChEMBL_ID
DB09115 DRUGBANK_ID
3728 PUBCHEM_CID
3435 RXNORM
2439 MMSL
4903 MMSL
d01105 MMSL
002952 NDDF
387355005 SNOMEDCT_US
64851009 SNOMEDCT_US
D004103 MESH_DESCRIPTOR_UI
1613 INN_ID
63W7IE88K8 UNII

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Vytone HUMAN PRESCRIPTION DRUG LABEL 2 44118-704 CREAM 10 mg TOPICAL unapproved drug other 9 sections
HYDROCORTISONE, IODOQUINOL HUMAN PRESCRIPTION DRUG LABEL 2 52187-532 CREAM 10 mg TOPICAL unapproved drug other 11 sections
Hydrocortisone Acetate, Iodoquinol HUMAN PRESCRIPTION DRUG LABEL 2 52187-551 CREAM 10 mg TOPICAL unapproved drug other 9 sections
Alcortin HUMAN PRESCRIPTION DRUG LABEL 2 68040-702 GEL 1 g TOPICAL unapproved drug other 2 sections
Alcortin A HUMAN PRESCRIPTION DRUG LABEL 3 68040-705 GEL 10 mg TOPICAL UNAPPROVED OTHER 17 sections
Aloquin HUMAN PRESCRIPTION DRUG LABEL 2 68040-706 GEL 12.50 mg TOPICAL Unapproved other 15 sections
IODOQUINOL HYDROCORTISONE ACETATE ALOE POLYSACCHARIDES HUMAN PRESCRIPTION DRUG LABEL 3 72056-020 GEL 10 mg TOPICAL UNAPPROVED DRUG OTHER 17 sections
HYDROCORTISONE IODOQUINOL HUMAN PRESCRIPTION DRUG LABEL 2 72056-040 CREAM 10 mg TOPICAL Unapproved drug other 17 sections
HYDROCORTISONE 2.5% / IODOQUINOL 1% / KETOCONAZOLE 2% HUMAN PRESCRIPTION DRUG LABEL 3 72934-2111 CREAM 1 g TOPICAL unapproved drug other 4 sections