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cefapirin 🐶 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 | 575 | 21593-23-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Cephalosporin antibiotic, partly plasma-bound, that is effective against gram-negative and gram-positive organisms.
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 |
| EoM (Fraction excreted unchanged in urine) | 48 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 236.14 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) | 0.13 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 2.70 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.55 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 1.20 hours | Lombardo F, Berellini G, Obach RS |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,ACVRL1,ALK,AURKA,AURKB,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GRK3,GSK3B,IGF1R,IKBKB,ITK,JAK1,JAK2,JAK3,KDR,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 | 65 | |||
| kinase-selectivity-class | AXL,BRAF,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,GSK3B,JAK2,MAP2K6,MAP3K14,MAPK7,MARK4,PRKDC,SIK2,STK33,SYK,TEK,TGFBR1,TTK | 22 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| March 12, 1974 | FDA | APOTHECON |
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 | J01DB08 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE OTHER BETA-LACTAM ANTIBACTERIALS First-generation cephalosporins |
| CHEBI has role | CHEBI:36047 | antibacterial drug |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D000900 | Anti-Bacterial Agents |
| CHEBI has role | CHEBI:33282 | antibacterial agent |
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 |
|---|---|---|---|
| Septicemia due to Escherichia coli | indication | 9323009 | |
| Bacterial septicemia | indication | 10001005 | DOID:0040085 |
| Infection of skin AND/OR subcutaneous tissue | indication | 19824006 | |
| Staphylococcal pneumonia | indication | 22754005 | |
| Streptococcal septicemia | indication | 29577008 | |
| Pneumonia due to Streptococcus | indication | 34020007 | |
| Lower respiratory tract infection | indication | 50417007 | |
| Klebsiella cystitis | indication | 60867007 | |
| Urinary tract infectious disease | indication | 68566005 | |
| Haemophilus influenzae pneumonia | indication | 70036007 | |
| Infection due to Escherichia coli | indication | 71057007 | |
| Rhinoscleroma | indication | 72409005 | DOID:11336 |
| Staphylococcal endocarditis | indication | 73028002 | |
| Infection of bone | indication | 111253001 | |
| Staphylococcal septicemia | indication | 111821004 | |
| Bacterial infection due to Klebsiella pneumoniae | indication | 186435004 | |
| Pneumonia | indication | 233604007 | DOID:552 |
| Escherichia coli urinary tract infection | indication | 301011002 | |
| Proteus urinary tract infection | indication | 301012009 | |
| Bacterial endocarditis | indication | 301183007 | |
| Streptococcus pyogenes infection | indication | 302809008 | |
| Infectious disorder of joint | indication | 363162000 | |
| Infection due to Staphylococcus aureus | indication | 406602003 | |
| Osteomyelitis due to Staphylococcus aureus | indication | 428783003 | |
| Skin and Skin Structure Proteus Infection | indication | ||
| Streptococcus Osteomyelitis | indication | ||
| Staphylococcus Epidermidis Skin and Skin Structure Infection | indication | ||
| Streptococcal Endocarditis | indication | ||
| Proteus Mirabilis Osteomyelitis | indication | ||
| Prevention of Perioperative Infection | indication | ||
| Staphylococcus Aureus Urinary Tract Infection | indication | ||
| Klebsiella Pneumoniae Osteomyelitis | indication |
🐶 Veterinary Drug Use
| Species | Use | Relation |
|---|---|---|
| Cattle | Mastitis caused by Streptococcus dysgalactiae | Indication |
| Cattle | Mastitis caused by Staphylococcus aureus | Indication |
🐶 Veterinary products
| Product | Applicant | Ingredients |
|---|---|---|
| ToDAY | Boehringer lngelheim Animal Health USA Inc. | 1 |
| ToMORROW | Boehringer lngelheim Animal Health USA Inc. | 1 |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 2.39 | acidic |
| pKa2 | 5.58 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Mu-type opioid receptor | GPCR | IC50 | 5.34 | WOMBAT-PK | |||||
| D(2) dopamine receptor | GPCR | IC50 | 4.66 | WOMBAT-PK | |||||
| Sigma non-opioid intracellular receptor 1 | Membrane receptor | IC50 | 6.21 | WOMBAT-PK | |||||
| Cytochrome P450 3A4 | Enzyme | IC50 | 5.31 | WOMBAT-PK | |||||
| 5-hydroxytryptamine receptor 1A | GPCR | IC50 | 5.48 | WOMBAT-PK | |||||
| 5-hydroxytryptamine receptor 2B | GPCR | IC50 | 4.82 | WOMBAT-PK | |||||
| D(3) dopamine receptor | GPCR | IC50 | 4.59 | WOMBAT-PK | |||||
| Histamine H2 receptor | GPCR | IC50 | 5.24 | WOMBAT-PK | |||||
| Alpha-2C adrenergic receptor | GPCR | IC50 | 4.68 | WOMBAT-PK | |||||
| Cannabinoid receptor 1 | GPCR | IC50 | 4.07 | WOMBAT-PK | |||||
| D(4) dopamine receptor | GPCR | IC50 | 5.01 | WOMBAT-PK | |||||
| Kappa-type opioid receptor | GPCR | IC50 | 5.29 | WOMBAT-PK | |||||
| Delta-type opioid receptor | GPCR | IC50 | 5.06 | WOMBAT-PK | |||||
| Substance-P receptor | GPCR | IC50 | 4.89 | WOMBAT-PK | |||||
| Nischarin | Membrane receptor | IC50 | 4.85 | WOMBAT-PK | |||||
| Interstitial collagenase | Enzyme | IC50 | 4.43 | WOMBAT-PK | |||||
| Substance-K receptor | GPCR | IC50 | 4.85 | WOMBAT-PK | |||||
| Cytochrome P450 3A5 | Enzyme | IC50 | 5.11 | WOMBAT-PK | |||||
| Somatostatin receptor type 4 | GPCR | IC50 | 5.17 | WOMBAT-PK | |||||
| Cytochrome P450 2D6 | Enzyme | IC50 | 4.84 | WOMBAT-PK | |||||
| Bacterial penicillin-binding protein | Enzyme | INHIBITOR | CHEMBL | CHEMBL | |||||
| Penicillin-binding protein 1A | Enzyme | WOMBAT-PK |
External reference:
| ID | Source |
|---|---|
| 4018153 | VUID |
| N0000179299 | NUI |
| D00908 | KEGG_DRUG |
| 1294563 | RXNORM |
| C0007737 | UMLSCUI |
| CHEBI:554446 | CHEBI |
| CHEMBL1599 | ChEMBL_ID |
| CHEMBL1201043 | ChEMBL_ID |
| DB01139 | DRUGBANK_ID |
| 12191 | IUPHAR_LIGAND_ID |
| 24356-60-3 | SECONDARY_CAS_RN |
| 30699 | PUBCHEM_CID |
| 4396 | MMSL |
| d00187 | MMSL |
| 002721 | NDDF |
| 004842 | NDDF |
| 370337008 | SNOMEDCT_US |
| 6873003 | SNOMEDCT_US |
| 87303007 | SNOMEDCT_US |
| 96043002 | SNOMEDCT_US |
| D002514 | MESH_DESCRIPTOR_UI |
| CHEMBL3989837 | ChEMBL_ID |
| 97468-37-6 | SECONDARY_CAS_RN |
| 2871 | INN_ID |
| 4018153 | VANDF |
| 4019670 | VANDF |
| 89B59H32VN | UNII |
Pharmaceutical products:
None