fludiazepam 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
diazepam derivatives 1190 3900-31-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • fludiazepam
  • erispan
  • fludiazepan
  • Molecular weight: 302.73
  • Formula: C16H12ClFN2O
  • CLOGP: 2.75
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 0
  • TPSA: 32.67
  • ALOGS: -4.32
  • ROTB: 1

Drug dosage:

DoseUnitRoute
0.75 mg O

ADMET properties:

PropertyValueReference
BA (Bioavailability) 50 %

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 2.724 Moderate 0.78
caco2-efflux Caco-2 efflux ratio (BA/AB) 0.493 Moderate 0.78
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 74.989 10^-6 cm/s Moderate 0.78
dh-clint Dog hepatocyte intrinsic clearance 65.313 uL/min/10^6 cells Moderate 0.78
dppb Dog plasma protein binding (% unbound) 7.840 % Moderate 0.78
fcs-ppb Fetal calf serum protein binding (% unbound) 22.670 % Moderate 0.78
herg hERG pIC50 4.456 pIC50 Moderate 0.78
hh-clint Human hepatocyte intrinsic clearance 3.614 uL/min/10^6 cells Moderate 0.78
hlm-clint Human liver microsomal intrinsic clearance 10.544 uL/min/mg protein Moderate 0.78
hppb Human plasma protein binding (% unbound) 7.610 % Moderate 0.78
kinase-safety-class EIF2AK3,GRK2,PDK1,PDK2,PDK4 5
kinase-selectivity-class AXL,GRK2 2
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 0.426 Moderate 0.73
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 0.307 Moderate 0.78
mh-clint Mouse hepatocyte intrinsic clearance 147.231 Moderate 0.78
mppb Mouse plasma protein binding (% unbound) 12.150 Moderate 0.78
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 0.515 Moderate 0.78
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 12.810 % Moderate 0.78
rat-kpuu-brain Rat brain Kpuu 1.303 % Moderate 0.73
rh-clint Rat hepatocyte intrinsic clearance 105.925 uL/min/10^6 cells Moderate 0.78
rh-fuinc Rat hepatocyte fraction unbound in incubation 71.150 % Moderate 0.78
rppb Rat plasma protein binding (% unbound) 10.050 % Moderate 0.78
solubility-dd Solubility at pH 7.4 in DMSO 483.059 uM Moderate 0.78

Approvals:

None

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 N05BA17 NERVOUS SYSTEM
PSYCHOLEPTICS
ANXIOLYTICS
Benzodiazepine derivatives
MeSH PA D000927 Anticonvulsants
MeSH PA D002491 Central Nervous System Agents
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D009125 Muscle Relaxants, Central
MeSH PA D009465 Neuromuscular Agents
MeSH PA D011619 Psychotropic Drugs
MeSH PA D014149 Tranquilizing Agents
MeSH PA D014151 Anti-Anxiety Agents
MeSH PA D018373 Peripheral Nervous System Agents
CHEBI has role CHEBI:35474 anxiolytic drug

Related Drugs by ATC class:

N05BA Benzodiazepine derivatives 23 drugs
adinazolamalprazolambentazepambromazepamcamazepamchlordiazepoxideclobazamclorazepateclotiazepamcloxazolamdiazepamethyl loflazepate show all 23 →

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

None




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 2.47 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

None

External reference:

IDSource
D01354 KEGG_DRUG
C0060485 UMLSCUI
CHEBI:31618 CHEBI
CHEMBL13291 ChEMBL_ID
DB01567 DRUGBANK_ID
C006107 MESH_SUPPLEMENTAL_RECORD_UI
3369 PUBCHEM_CID
4089 INN_ID
7F64A2K16Z UNII

Pharmaceutical products:

None