delorazepam Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
diazepam derivatives 800 2894-67-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • delorazepam
  • chlordemethyldiazepam
  • chlordesmethyldiazepam
  • chlorodesmethyldiazepam
  • Molecular weight: 305.16
  • Formula: C15H10Cl2N2O
  • CLOGP: 3.08
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 1
  • TPSA: 41.46
  • ALOGS: -4.68
  • ROTB: 1

Drug dosage:

None

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.28 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
Vd (Volume of distribution) 2.20 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 0.17 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.05 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 200 hours Lombardo F, Berellini G, Obach RS

Approvals:

None

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Drug abuse 1137.81 236.85 185 121 11841 2345938
Sopor 878.46 236.85 130 176 3865 2353914
Intentional self-injury 708.69 236.85 109 197 4018 2353761

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Sopor 502.37 113.67 74 123 1927 1744657
Drug abuse 354.10 113.67 73 124 13616 1732968
Intentional self-injury 272.98 113.67 46 151 2627 1743957

Pharmacologic Action:

SourceCodeDescription
MeSH PA D000927 Anticonvulsants
MeSH PA D002491 Central Nervous System Agents

Drug Use (View source of the data)

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 11.52 acidic
pKa2 2.23 Basic

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
GABA-A receptor alpha-1/beta-2/gamma-2 Ion channel IC50 8.75 WOMBAT-PK
GABA-A receptor; anion channel Ion channel IC50 8.55 CHEMBL

External reference:

IDSource
D07784 KEGG_DRUG
CHEBI:135295 CHEBI
CHEMBL268254 ChEMBL_ID
C013434 MESH_SUPPLEMENTAL_RECORD_UI
O91W32476G UNII
4510 INN_ID
DB01511 DRUGBANK_ID
17925 PUBCHEM_CID

Pharmaceutical products:

None