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

Stem definition	Drug id	CAS RN
antibacterials, nalidixic acid derivatives	2466	110871-86-8

Description:

Molecule

Description

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:

Dose	Unit	Route
0.20	g	O

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Bocci G, Oprea TI, Benet LZ
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 µM/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:

Date	Agency	Company	Orphan
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:

Source	Code	Description
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
MeSH PA	D059003	Topoisomerase Inhibitors

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

Disease	Relation	SNOMED_ID	DOID
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

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		Ki	4.41		DRUG MATRIX
Topoisomerase IV	Enzyme		PARC_ECOLI PARE_ECOLI	INHIBITOR				CHEMBL	CHEMBL
DNA gyrase	Enzyme		GYRA_ECOLI GYRB_ECOLI	INHIBITOR				CHEMBL	CHEMBL

External reference:

ID	Source
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