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

Stem definitionDrug idCAS RN
antibacterials, nalidixic acid derivatives 2071 70458-92-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • pefloxacin
  • peflacine
  • pefloxacine
A synthetic broad-spectrum fluoroquinolone antibacterial agent active against most gram-negative and gram-positive bacteria.
  • Molecular weight: 333.36
  • Formula: C17H20FN3O3
  • CLOGP: -0.07
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 1
  • TPSA: 64.09
  • ALOGS: -2.43
  • ROTB: 3

Drug dosage:

DoseUnitRoute
0.80 g O
0.80 g P

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 11.40 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 12 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 34.28 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 90 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 1.50 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 2 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.75 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 11 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1985 YEAR INTRODUCED

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 J01MA03 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIBACTERIALS FOR SYSTEMIC USE
QUINOLONE ANTIBACTERIALS
Fluoroquinolones
CHEBI has role CHEBI:35441 antiinfective agents
CHEBI has role CHEBI:36047 antibacterial drugs
CHEBI has role CHEBI:59517 DNA synthesis inhibitors
MeSH PA D000900 Anti-Bacterial Agents
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000970 Antineoplastic Agents
MeSH PA D065609 Cytochrome P-450 CYP1A2 Inhibitors
MeSH PA D065607 Cytochrome P-450 Enzyme Inhibitors
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D065606 Metabolic Side Effects of Drugs and Substances
MeSH PA D059005 Topoisomerase II Inhibitors
MeSH PA D059003 Topoisomerase Inhibitors

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

None




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 8.23 Basic
pKa3 1.06 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
Cytochrome P450 1A2 Enzyme Ki 4.10 WOMBAT-PK
DNA gyrase subunit A Enzyme IC50 6.79 WOMBAT-PK
DNA gyrase subunit B Enzyme IC50 6.79 WOMBAT-PK

External reference:

IDSource
N0000166915 NUI
D02306 KEGG_DRUG
C0030771 UMLSCUI
CHEBI:50199 CHEBI
CHEMBL267648 ChEMBL_ID
DB00487 DRUGBANK_ID
D015366 MESH_DESCRIPTOR_UI
51081 PUBCHEM_CID
12411 IUPHAR_LIGAND_ID
5006 INN_ID
2H52Z9F2Q5 UNII
7960 RXNORM
005283 NDDF
443149005 SNOMEDCT_US
96089009 SNOMEDCT_US

Pharmaceutical products:

None