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cefmetazole 🐶 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 | 539 | 56796-20-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A semisynthetic cephamycin antibiotic with a broad spectrum of activity against both gram-positive and gram-negative microorganisms. It has a high rate of efficacy in many types of infection and to date no severe side effects have been noted.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 4 | g | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 4 | Bocci G, Oprea TI, Benet LZ |
| S (Water solubility) | 0.09 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 80 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 212.07 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| Vd (Volume of distribution) | 0.13 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 1.50 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.15 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 1.50 hours | Lombardo F, Berellini G, Obach RS |
| BA (Bioavailability) | 80 % |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | -2.214 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 2.679 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 0.750 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 1.687 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 84.420 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 68.930 | % | High | 1 |
| herg | hERG pIC50 | 4.055 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 0.993 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 3.864 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 46.950 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,GRK2,GRK3,GSK3B,IGF1R,ITK,JAK2,MAP2K6,MAP3K21,MAP3K7,MAPK10,MAPK7,MAPK9,MAPKAPK2,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PIK3CD,PIM2,PRKDC,SIK2,STK33,SYK,TEK,TTK | 42 | |||
| kinase-selectivity-class | AXL,BRAF,CDK9,DYRK1B,EIF2AK3,GRK2,MAP2K6,MAPK7,PRKDC,STK33,TEK | 11 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 0.560 | Moderate | 0.68 | |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 1.452 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 1.824 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 75.590 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 1.062 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 53.160 | % | High | 1 |
| rat-kpuu-brain | Rat brain Kpuu | 0.008 | % | Moderate | 0.68 |
| rh-clint | Rat hepatocyte intrinsic clearance | 1.321 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 94.720 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 48.270 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 1039.920 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Dec. 11, 1989 | FDA |
FDA Adverse Event Reporting System (Female)
| 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 |
|---|---|---|---|---|---|---|
| Intrauterine infection | 56.88 | 42.15 | 7 | 490 | 133 | 90627817 |
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 |
|---|---|---|---|---|---|---|
| Intrauterine infection | 47.13 | 32.45 | 6 | 1210 | 72 | 110588011 |
| Hepatic function abnormal | 44.47 | 32.45 | 21 | 1195 | 89274 | 110498809 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | J01DC09 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE OTHER BETA-LACTAM ANTIBACTERIALS Second-generation cephalosporins |
| CHEBI has role | CHEBI:33282 | antibacterial agent |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
| CHEBI has role | CHEBI:36047 | antibacterial drug |
| CHEBI has role | CHEBI:33281 | antimicrobial agent |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D000900 | Anti-Bacterial Agents |
Related Drugs by ATC class:
J01DC Second-generation cephalosporins 13 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Infection of skin AND/OR subcutaneous tissue | indication | 19824006 | |
| Staphylococcal pneumonia | indication | 22754005 | |
| Pneumonia due to Streptococcus | indication | 34020007 | |
| Lower respiratory tract infection | indication | 50417007 | |
| Pneumonia due to Escherichia coli | indication | 51530003 | |
| Urinary tract infectious disease | indication | 68566005 | |
| Haemophilus influenzae pneumonia | indication | 70036007 | |
| Infectious disease of abdomen | indication | 128070006 | |
| Pneumonia | indication | 233604007 | DOID:552 |
| Prevention of Perioperative Infection | 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 | 2.85 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Insulin-degrading enzyme | Enzyme | IC50 | 5.16 | CHEMBL | |||||
| Bacterial penicillin-binding protein | Enzyme | INHIBITOR | CHEMBL | CHEMBL | |||||
| Penicillin-binding protein 1A | Enzyme | WOMBAT-PK |
External reference:
| ID | Source |
|---|---|
| 4019509 | VUID |
| N0000179604 | NUI |
| D00910 | KEGG_DRUG |
| 56796-39-5 | SECONDARY_CAS_RN |
| 203140 | RXNORM |
| C0007550 | UMLSCUI |
| CHEBI:3489 | CHEBI |
| 4KO | PDB_CHEM_ID |
| CHEMBL1201195 | ChEMBL_ID |
| CHEMBL1201118 | ChEMBL_ID |
| D015311 | MESH_DESCRIPTOR_UI |
| DB00274 | DRUGBANK_ID |
| 12215 | IUPHAR_LIGAND_ID |
| 4423 | INN_ID |
| 3J962UJT8H | UNII |
| 42008 | PUBCHEM_CID |
| 4375 | MMSL |
| d00093 | MMSL |
| 370344004 | SNOMEDCT_US |
| 397422004 | SNOMEDCT_US |
| 96059002 | SNOMEDCT_US |
| 4019509 | VANDF |
| 4019660 | VANDF |
| 003540 | NDDF |
| 004851 | NDDF |
Pharmaceutical products:
None