AI ASSISTANT
Ask DrugCentral
Explore drug information in your own words.
Type a question in the search bar above to get started. Each question is answered independently.
Try a sample question
Select a question to fill the search bar, then submit it or edit it first.
AI can make mistakes. Verify answers against the original sources before relying on them.
cefalotin 🐶 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 | 574 | 153-61-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A cephalosporin antibiotic.
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) | 3 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 50 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 52 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 252.24 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 0 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 0.07 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 1.80 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.22 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 0.95 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 | -1.477 | Moderate | 0.70 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 3.802 | Moderate | 0.70 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 0.303 | 10^-6 cm/s | Moderate | 0.70 |
| dh-clint | Dog hepatocyte intrinsic clearance | 4.932 | uL/min/10^6 cells | Moderate | 0.70 |
| dppb | Dog plasma protein binding (% unbound) | 57.600 | % | Moderate | 0.70 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 33.180 | % | Moderate | 0.70 |
| herg | hERG pIC50 | 4.170 | pIC50 | Moderate | 0.70 |
| hh-clint | Human hepatocyte intrinsic clearance | 8.710 | uL/min/10^6 cells | Moderate | 0.70 |
| hlm-clint | Human liver microsomal intrinsic clearance | 12.190 | uL/min/mg protein | Moderate | 0.70 |
| hppb | Human plasma protein binding (% unbound) | 21.790 | % | Moderate | 0.70 |
| kinase-safety-class | ACVR2A,ACVR2B,ACVRL1,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GRK3,GSK3B,ITK,JAK1,JAK2,JAK3,KIT,MAP2K6,MAP3K14,MAP3K21,MAP3K7,MAPK1,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MAPKAPK5,MARK4,MTOR,NTRK2,PDK1,PDK2,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PIM2,PLK1,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ULK1,ZAP70 | 61 | |||
| kinase-selectivity-class | AURKB,AXL,BRAF,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,JAK2,MAP2K6,MAP3K14,MAPK7,PRKDC,STK33,SYK,TEK,TGFBR1,TTK | 20 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 1.361 | Moderate | 0.70 | |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.809 | Moderate | 0.70 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 50.933 | Moderate | 0.70 | |
| mppb | Mouse plasma protein binding (% unbound) | 37.920 | Moderate | 0.70 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 1.288 | Moderate | 0.70 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 21.360 | % | Moderate | 0.70 |
| rat-kpuu-brain | Rat brain Kpuu | 0.009 | % | Moderate | 0.70 |
| rh-clint | Rat hepatocyte intrinsic clearance | 21.184 | uL/min/10^6 cells | Moderate | 0.70 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 89.660 | % | Moderate | 0.70 |
| rppb | Rat plasma protein binding (% unbound) | 24.790 | % | Moderate | 0.70 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 968.278 | uM | Moderate | 0.70 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Dec. 18, 1974 | FDA | LILLY |
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 | J01DB03 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE OTHER BETA-LACTAM ANTIBACTERIALS First-generation cephalosporins |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D000900 | Anti-Bacterial Agents |
| CHEBI has role | CHEBI:33281 | antimicrobial agent |
| CHEBI has role | CHEBI:36047 | antibacterial drug |
Related Drugs by ATC class:
J01DB First-generation cephalosporins 11 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Bacterial septicemia | indication | 10001005 | DOID:0040085 |
| Infection of skin AND/OR subcutaneous tissue | indication | 19824006 | |
| Pneumonia due to Streptococcus | indication | 34020007 | |
| Lower respiratory tract infection | indication | 50417007 | |
| Urinary tract infectious disease | indication | 68566005 | |
| Haemophilus influenzae pneumonia | indication | 70036007 | |
| Infection of bone | indication | 111253001 | |
| Female genital tract infection | indication | 125585007 | |
| Bacterial infection due to Klebsiella pneumoniae | indication | 186435004 | |
| Pneumonia | indication | 233604007 | DOID:552 |
| Infectious disorder of joint | indication | 363162000 | |
| Genitourinary Tract Infections | indication | ||
| 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 | 2.39 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Prostaglandin G/H synthase 2 | Enzyme | IC50 | 4.70 | WOMBAT-PK | |||||
| Solute carrier family 22 member 8 | Transporter | INHIBITOR | IC50 | 7.59 | IUPHAR | ||||
| Matrix metalloproteinase-9 | Enzyme | IC50 | 4.66 | WOMBAT-PK | |||||
| Somatostatin receptor type 4 | GPCR | IC50 | 4.40 | WOMBAT-PK | |||||
| Tyrosine-protein phosphatase non-receptor type 7 | Enzyme | IC50 | 6.04 | WOMBAT-PK | |||||
| Solute carrier family 22 member 11 | Transporter | INHIBITOR | Ki | 6.70 | IUPHAR | ||||
| Bacterial penicillin-binding protein | Enzyme | INHIBITOR | CHEMBL | CHEMBL | |||||
| Penicillin-binding protein 1A | Enzyme | WOMBAT-PK |
External reference:
| ID | Source |
|---|---|
| 4017538 | VUID |
| N0000178975 | NUI |
| D00907 | KEGG_DRUG |
| 58-71-9 | SECONDARY_CAS_RN |
| 2236 | RXNORM |
| C0007735 | UMLSCUI |
| CHEBI:124991 | CHEBI |
| CLS | PDB_CHEM_ID |
| CHEMBL617 | ChEMBL_ID |
| CHEMBL1632 | ChEMBL_ID |
| DB00456 | DRUGBANK_ID |
| 8798 | IUPHAR_LIGAND_ID |
| 6024 | PUBCHEM_CID |
| 3072 | MMSL |
| 4395 | MMSL |
| d00186 | MMSL |
| 002712 | NDDF |
| 004840 | NDDF |
| 373485007 | SNOMEDCT_US |
| 37628007 | SNOMEDCT_US |
| 59937009 | SNOMEDCT_US |
| D002512 | MESH_DESCRIPTOR_UI |
| 1477 | INN_ID |
| 4017538 | VANDF |
| 4019669 | VANDF |
| C22G6EYP8B | UNII |
| C22G6EYP8B | INXIGHT DRUGS |
Pharmaceutical products:
None