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

Stem definitionDrug idCAS RN
antibacterials, nalidixic acid derivatives 2412 101363-10-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • rufloxacin hydrochloride
  • rufloxacin hydrobromide
  • MF-934
  • rufloxacin
  • Molecular weight: 363.41
  • Formula: C17H18FN3O3S
  • CLOGP: -0.03
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 1
  • TPSA: 64.09
  • ALOGS: -2.58
  • ROTB: 2

Drug dosage:

DoseUnitRoute
0.20 g O

ADMET properties:

PropertyValueReference
BA (Bioavailability) 70 %

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 -0.315 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 2.630 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 10.814 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 2.388 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 78.050 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 72.870 % High 1
herg hERG pIC50 4.556 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 1.069 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 3.090 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 68.930 % High 1
kinase-safety-class ACVR2B,CAMK2D,CDK5,EIF2AK3,GRK2,ITK,MAPK7,PDK1,PDK2,PDK4,PRKDC 11
kinase-selectivity-class ACVR2B,AXL,BRAF,CAMK2D,CDK9,DYRK1B,EIF2AK3,EPHB4,GRK2,MAPK7,PDK4,PRKDC,SIK2,STK33,TEK,TTK 16
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 10.257 High 1
mh-clint Mouse hepatocyte intrinsic clearance 3.499 High 1
mppb Mouse plasma protein binding (% unbound) 71.710 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 17.061 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 77.780 % High 1
rh-clint Rat hepatocyte intrinsic clearance 1.393 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 86.590 % High 1
rppb Rat plasma protein binding (% unbound) 50.750 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 790.679 uM High 1

Approvals:

None

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
Neuroglycopenia 122.47 70.12 20 1301 1095 90626031
Peripheral circulatory failure 115.21 70.12 20 1301 1584 90625542
Blood cholesterol decreased 98.44 70.12 18 1303 1913 90625213
Stupor 96.25 70.12 21 1300 5461 90621665
Gastric polyps 93.87 70.12 20 1301 4652 90622474
Atrioventricular block first degree 87.05 70.12 21 1300 8490 90618636
Bradykinesia 86.43 70.12 20 1301 6768 90620358
Muscle rigidity 76.23 70.12 21 1300 14288 90612838
Initial insomnia 75.16 70.12 19 1302 9291 90617835
Multiple drug therapy 70.16 70.12 17 1304 6992 90620134

FDA Adverse Event Reporting System (Male)

None

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
Neuroglycopenia 126.26 67.74 20 1301 1106 110586872
Peripheral circulatory failure 116.67 67.74 20 1301 1799 110586179
Blood cholesterol decreased 95.89 67.74 18 1303 2698 110585280
Gastric polyps 94.50 67.74 20 1301 5503 110582475
Stupor 91.82 67.74 21 1300 8244 110579734
Bradykinesia 81.17 67.74 20 1301 10768 110577210
Atrioventricular block first degree 80.49 67.74 21 1300 14204 110573774
Initial insomnia 76.85 67.74 19 1302 10370 110577608
Multiple drug therapy 71.26 67.74 17 1304 7997 110579981
Muscle rigidity 69.60 67.74 21 1300 24010 110563968

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC J01MA10 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIBACTERIALS FOR SYSTEMIC USE
QUINOLONE ANTIBACTERIALS
Fluoroquinolones
MeSH PA D000970 Antineoplastic Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D059003 Topoisomerase Inhibitors
MeSH PA D059005 Topoisomerase II Inhibitors
CHEBI has role CHEBI:33282 antibacterial agent

Related Drugs by ATC class:

J01MA Fluoroquinolones 22 drugs
ciprofloxacindelafloxacinenoxacinfleroxacingarenoxacingatifloxacingemifloxacingrepafloxacinlascufloxacinlevofloxacinlomefloxacinmoxifloxacin show all 22 →

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

None




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 5.53 acidic
pKa2 8.29 Basic
pKa3 1.12 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

None

External reference:

IDSource
D02474 KEGG_DRUG
106017-08-7 SECONDARY_CAS_RN
C0073704 UMLSCUI
CHEBI:8909 CHEBI
CHEMBL295619 ChEMBL_ID
DB13772 DRUGBANK_ID
C060328 MESH_SUPPLEMENTAL_RECORD_UI
58258 PUBCHEM_CID
12473 IUPHAR_LIGAND_ID
6080 INN_ID
Y521XM2900 UNII
008179 NDDF
008180 NDDF
717102009 SNOMEDCT_US
717103004 SNOMEDCT_US

Pharmaceutical products:

None