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cefoperazone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antibiotics, cefalosporanic acid derivatives | 543 | 62893-19-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Semisynthetic broad-spectrum cephalosporin with a tetrazolyl moiety that is resistant to beta-lactamase. It may be used to treat Pseudomonas infections.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 4 | g | P |
| 4 | g | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 309.75 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 3 | Hosey CM, Chan R, Benet LZ |
| EoM (Fraction excreted unchanged in urine) | 29 % | Hosey CM, Chan R, Benet LZ |
| BA (Bioavailability) | 10 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 0.17 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 1.30 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.07 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 1.80 hours | Lombardo F, Berellini G, Obach RS |
| S (Water solubility) | 50 mg/mL | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | -2.096 | Moderate | 0.76 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.662 | Moderate | 0.76 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 0.646 | 10^-6 cm/s | Moderate | 0.76 |
| dh-clint | Dog hepatocyte intrinsic clearance | 1.400 | uL/min/10^6 cells | Moderate | 0.76 |
| dppb | Dog plasma protein binding (% unbound) | 76.930 | % | Moderate | 0.76 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 60.930 | % | Moderate | 0.76 |
| herg | hERG pIC50 | 4.411 | pIC50 | Moderate | 0.76 |
| hh-clint | Human hepatocyte intrinsic clearance | 1.159 | uL/min/10^6 cells | Moderate | 0.76 |
| hlm-clint | Human liver microsomal intrinsic clearance | 3.404 | uL/min/mg protein | Moderate | 0.76 |
| hppb | Human plasma protein binding (% unbound) | 57.030 | % | Moderate | 0.76 |
| kinase-safety-class | ACVR2B,AURKA,AXL,BRAF,BTK,CAMK2D,CDK5,CDK9,DYRK1B,EIF2AK3,ERBB2,GRK2,ITK,MAPK10,MAPK7,MAPKAPK2,NTRK2,PDK1,PDK2,PIK3CB,PRKDC,STK33,SYK,TEK | 24 | |||
| kinase-selectivity-class | AXL,BRAF,CDK9,DYRK1B,EIF2AK3,GRK2,MAPK7,STK33,TEK | 9 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.809 | Moderate | 0.76 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 1.442 | Moderate | 0.76 | |
| mppb | Mouse plasma protein binding (% unbound) | 75.040 | Moderate | 0.76 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 1.309 | Moderate | 0.76 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 57.540 | % | Moderate | 0.76 |
| rh-clint | Rat hepatocyte intrinsic clearance | 1.035 | uL/min/10^6 cells | Moderate | 0.76 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 90.040 | % | Moderate | 0.76 |
| rppb | Rat plasma protein binding (% unbound) | 54.990 | % | Moderate | 0.76 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 946.237 | uM | Moderate | 0.76 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Nov. 18, 1982 | FDA |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Multiple organ dysfunction syndrome | 42.89 | 39.01 | 21 | 757 | 151689 | 110436832 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | J01DD12 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE OTHER BETA-LACTAM ANTIBACTERIALS Third-generation cephalosporins |
| ATC | J01DD62 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE OTHER BETA-LACTAM ANTIBACTERIALS Third-generation cephalosporins |
| FDA CS | M0003827 | Cephalosporins |
| FDA EPC | N0000175488 | Cephalosporin Antibacterial |
| CHEBI has role | CHEBI:36047 | antibacterial drug |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D000900 | Anti-Bacterial Agents |
Related Drugs by ATC class:
J01DD Third-generation cephalosporins 17 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Alcohol intoxication | contraindication | 25702006 | |
| Vitamin K deficiency | contraindication | 52675005 | DOID:11249 |
| Disorder of digestive system | contraindication | 53619000 | DOID:77 |
| Blood coagulation disorder | contraindication | 64779008 | DOID:1247 |
| Factor II deficiency | contraindication | 73975000 | |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Pseudomembranous enterocolitis | contraindication | 397683000 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 2.63 | acidic |
| pKa2 | 8.03 | acidic |
| pKa3 | 12.64 | acidic |
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 |
|---|---|---|---|---|---|---|---|---|---|
| Bacterial penicillin-binding protein | Enzyme | INHIBITOR | CHEMBL | CHEMBL | |||||
| Penicillin-binding protein 1A | Enzyme | WOMBAT-PK |
External reference:
| ID | Source |
|---|---|
| 4019662 | VUID |
| N0000147754 | NUI |
| D00918 | KEGG_DRUG |
| 62893-20-3 | SECONDARY_CAS_RN |
| 2184 | RXNORM |
| C0007552 | UMLSCUI |
| CHEBI:3493 | CHEBI |
| CHEMBL507674 | ChEMBL_ID |
| CHEMBL1200482 | ChEMBL_ID |
| D002438 | MESH_DESCRIPTOR_UI |
| DB01329 | DRUGBANK_ID |
| 12025 | IUPHAR_LIGAND_ID |
| 4742 | INN_ID |
| 113826-44-1 | SECONDARY_CAS_RN |
| 7U75I1278D | UNII |
| 44187 | PUBCHEM_CID |
| 4377 | MMSL |
| 998 | MMSL |
| d00074 | MMSL |
| 3136005 | SNOMEDCT_US |
| 372743004 | SNOMEDCT_US |
| 44938006 | SNOMEDCT_US |
| CHEMBL1697715 | ChEMBL_ID |
| 4018506 | VANDF |
| 4019662 | VANDF |
| 002728 | NDDF |
| 004846 | NDDF |
Pharmaceutical products:
None