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pefloxacin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antibacterials, nalidixic acid derivatives | 2071 | 70458-92-3 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A synthetic broad-spectrum fluoroquinolone antibacterial agent active against most gram-negative and gram-positive bacteria.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.80 | g | O |
| 0.80 | g | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| 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 µM/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 |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 0.131 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 1.138 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 25.468 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 5.508 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 78.950 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 82.520 | % | High | 1 |
| herg | hERG pIC50 | 4.414 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 1.130 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 3.819 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 68.330 | % | High | 1 |
| kinase-safety-class | ACVR2B,CDK5,EIF2AK3,GRK2,MAPK7,PDK1,PDK2,PDK4,PRKDC | 9 | |||
| kinase-selectivity-class | ACVR2B,AXL,CAMK2D,CDK9,DYRK1B,EIF2AK3,EPHB4,GRK2,MAP3K14,MAPK7,MARK4,PDK4,PIK3CB,PRKDC,SIK2,STK33,SYK,TEK,TTK | 19 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 1.644 | High | 1 | |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 8.091 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 5.957 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 73.500 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 12.388 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 75.760 | % | High | 1 |
| rat-kpuu-brain | Rat brain Kpuu | 0.153 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 3.412 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 89.310 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 57.990 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 874.984 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| 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:
| Source | Code | Description |
|---|---|---|
| ATC | J01MA03 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE QUINOLONE ANTIBACTERIALS Fluoroquinolones |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D000900 | Anti-Bacterial Agents |
| MeSH PA | D000970 | Antineoplastic Agents |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D059005 | Topoisomerase II Inhibitors |
| MeSH PA | D065607 | Cytochrome P-450 Enzyme Inhibitors |
| MeSH PA | D065609 | Cytochrome P-450 CYP1A2 Inhibitors |
| CHEBI has role | CHEBI:33282 | antibacterial agent |
| CHEBI has role | CHEBI:35441 | antiinfective agent |
| CHEBI has role | CHEBI:36047 | antibacterial drug |
| CHEBI has role | CHEBI:59517 | DNA synthesis inhibitor |
Related Drugs by ATC class:
J01MA Fluoroquinolones 22 drugs
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 level | Dissociation constant | Type (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:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA 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:
| ID | Source |
|---|---|
| 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