cefalotin ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
antibiotics, cefalosporanic acid derivatives 574 153-61-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • cefalotin sodium
  • cephalothin sodium
  • cephalothin
  • cefalotin
  • cephalotin
  • cephalothin sodium salt
A cephalosporin antibiotic.
  • Molecular weight: 396.43
  • Formula: C16H16N2O6S2
  • CLOGP: 0.04
  • LIPINSKI: 0
  • HAC: 8
  • HDO: 2
  • TPSA: 113.01
  • ALOGS: -3.88
  • ROTB: 7

  • Status: OFM

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
4 g P

ADMET properties:

PropertyValueReference
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 ยตM/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

Approvals:

DateAgencyCompanyOrphan
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:

SourceCodeDescription
ATC J01DB03 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIBACTERIALS FOR SYSTEMIC USE
OTHER BETA-LACTAM ANTIBACTERIALS
First-generation cephalosporins
MeSH PA D000900 Anti-Bacterial Agents
MeSH PA D000890 Anti-Infective Agents
CHEBI has role CHEBI:33281 antibiotics
CHEBI has role CHEBI:36047 antibacterial drugs

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
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




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 2.39 acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Solute carrier family 22 member 8 Transporter INHIBITOR IC50 7.59 IUPHAR
Matrix metalloproteinase-9 Enzyme IC50 4.66 WOMBAT-PK
Prostaglandin G/H synthase 2 Enzyme IC50 4.70 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:

IDSource
4017538 VUID
N0000178975 NUI
D00907 KEGG_DRUG
58-71-9 SECONDARY_CAS_RN
2236 RXNORM
C0007735 UMLSCUI
CHEBI:124991 CHEBI
CLS PDB_CHEM_ID
CHEMBL1632 ChEMBL_ID
CHEMBL617 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

Pharmaceutical products:

None