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

Stem definitionDrug idCAS RN
antibiotics, 6-aminopenicillanic acid derivatives 277 37091-66-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • azlocillin
  • azlocillin sodium
  • azlocillin sodium salt
A semisynthetic ampicillin-derived acylureido penicillin.
  • Molecular weight: 461.49
  • Formula: C20H23N5O6S
  • CLOGP: 1.56
  • LIPINSKI: 1
  • HAC: 11
  • HDO: 4
  • TPSA: 148.15
  • ALOGS: -3.30
  • ROTB: 5

  • Status: OFM

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

Drug dosage:

DoseUnitRoute
12 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) 65 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 650.05 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) 0.26 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 2.50 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.65 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 1.20 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Sept. 3, 1982 FDA BAYER PHARMACEUTICALS CORP

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 J01CA09 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIBACTERIALS FOR SYSTEMIC USE
BETA-LACTAM ANTIBACTERIALS, PENICILLINS
Penicillins with extended spectrum
CHEBI has role CHEBI:36047 antibacterial drugs
MeSH PA D000900 Anti-Bacterial Agents
MeSH PA D000890 Anti-Infective Agents

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 Pseudomonas indication 41381004
Pneumonia due to Escherichia coli indication 51530003
Urinary tract infectious disease indication 68566005
Haemophilus influenzae pneumonia indication 70036007
Bacterial infection due to Serratia indication 71120004
Infection of bone indication 111253001
Bacterial infection due to Klebsiella pneumoniae indication 186435004
Infectious disorder of joint indication 363162000
Aspiration pneumonia indication 422588002 DOID:3240
Enterobacter Pneumonia indication
Cholangitis off-label use 82403002 DOID:9446
Infectious disease of abdomen off-label use 128070006
Abscess of brain off-label use 441806004
Pseudomonas Aeruginosa Meningitis off-label use
Kidney disease contraindication 90708001 DOID:557
Infectious mononucleosis contraindication 271558008 DOID:8568
Pseudomembranous enterocolitis contraindication 397683000




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 2.79 acidic
pKa2 12.4 acidic
pKa3 12.92 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
Penicillin-binding protein Enzyme INHIBITOR CHEMBL CHEMBL

External reference:

IDSource
4019621 VUID
N0000147715 NUI
D02339 KEGG_DRUG
1266 RXNORM
C0004499 UMLSCUI
CHEBI:2956 CHEBI
CHEMBL1537 ChEMBL_ID
D001390 MESH_DESCRIPTOR_UI
DB01061 DRUGBANK_ID
12260 IUPHAR_LIGAND_ID
4011 INN_ID
37091-65-9 SECONDARY_CAS_RN
HUM6H389W0 UNII
6479523 PUBCHEM_CID
10730008 SNOMEDCT_US
387308000 SNOMEDCT_US
55432002 SNOMEDCT_US
CHEMBL1201041 ChEMBL_ID
4018389 VANDF
4019621 VANDF
002697 NDDF
004836 NDDF

Pharmaceutical products:

None