sparfloxacin ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
antibacterials, nalidixic acid derivatives 2466 110871-86-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • sparfloxacin
  • sparcin
  • PD 131501
  • AT-4140
  • CI-978
  • Molecular weight: 392.41
  • Formula: C19H22F2N4O3
  • CLOGP: -0.35
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 3
  • TPSA: 98.90
  • ALOGS: -3.54
  • ROTB: 3

  • Status: OFM

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.20 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 1.10 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 10 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 8.49 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 92 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 3.90 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 2.70 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.55 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 20 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Dec. 19, 1996 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 J01MA09 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIBACTERIALS FOR SYSTEMIC USE
QUINOLONE ANTIBACTERIALS
Fluoroquinolones
MeSH PA D000900 Anti-Bacterial Agents
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000970 Antineoplastic Agents
MeSH PA D000995 Antitubercular Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D059005 Topoisomerase II Inhibitors

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

DiseaseRelationSNOMED_IDDOID
Pneumonia due to Streptococcus indication 34020007
Pneumonia due to Mycoplasma pneumoniae indication 46970008
Haemophilus influenzae pneumonia indication 70036007
Bacterial infection due to Klebsiella pneumoniae indication 186435004
Acute Moraxella catarrhalis bronchitis indication 195722003
Acute bacterial bronchitis indication 233598009
Pneumonia indication 233604007 DOID:552
Chlamydial pneumonia indication 233609002
Haemophilus Parainfluenzae Bronchitis indication
Enterobacter Cloacae Bronchitis indication
Haemophilus Parainfluenzae Pneumonia indication
Moraxella Catarrhalis Pneumonia indication
Staphylococcus Aureus Bronchitis indication
Haemophilus Influenzae Bronchitis indication
Chlamydia Pneumoniae Bronchitis indication
Streptococcus Pneumoniae Bronchitis indication




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 5.98 acidic
pKa2 8.3 Basic
pKa3 2.83 Basic
pKa4 0.4 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
Potassium voltage-gated channel subfamily H member 2 Ion channel Ki 4.41 DRUG MATRIX
Topoisomerase IV Enzyme INHIBITOR CHEMBL CHEMBL
DNA gyrase Enzyme INHIBITOR CHEMBL CHEMBL

External reference:

IDSource
4020985 VUID
N0000148455 NUI
D00590 KEGG_DRUG
4020985 VANDF
C0034428 UMLSCUI
CHEBI:9212 CHEBI
CHEMBL850 ChEMBL_ID
DB01208 DRUGBANK_ID
C061363 MESH_SUPPLEMENTAL_RECORD_UI
60464 PUBCHEM_CID
10860 IUPHAR_LIGAND_ID
6612 INN_ID
Q90AGA787L UNII
18469 RXNORM
5504 MMSL
d04108 MMSL
005789 NDDF
387554008 SNOMEDCT_US
96090000 SNOMEDCT_US

Pharmaceutical products:

None