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

Stem definitionDrug idCAS RN
diazepam derivatives 816 1088-11-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • desmethyldiazepam
  • demethyldiazepam
  • demoxazepam
  • desalkylprazepam
  • N-Demethyldiazepam
  • nordazepam
  • nordiazepam
  • norprazepam
  • praxadium
An intermediate in the metabolism of DIAZEPAM to OXAZEPAM. It may have actions similar to those of diazepam.
  • Molecular weight: 270.72
  • Formula: C15H11ClN2O
  • CLOGP: 3.02
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 1
  • TPSA: 41.46
  • ALOGS: -4.09
  • ROTB: 1

Drug dosage:

DoseUnitRoute
15 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.06 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 0.50 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.79 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
Vd (Volume of distribution) 0.45 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 0.12 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.03 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 46 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1961 YEAR INTRODUCED

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
Toxicity to various agents 844.31 89.87 292 1303 212207 50391322
Asphyxia 173.39 89.87 39 1556 5388 50598141
Drug abuse 171.83 89.87 66 1529 59780 50543749
Completed suicide 121.86 89.87 66 1529 131823 50471706
Accidental overdose 107.40 89.87 35 1560 19498 50584031
Victim of sexual abuse 101.13 89.87 17 1578 504 50603025
Poisoning 92.17 89.87 28 1567 12401 50591128
Drug interaction 91.81 89.87 64 1531 199557 50403972

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
Toxicity to various agents 1788.81 143.07 710 3332 172951 29397534
Drug abuse 602.53 143.07 266 3776 79617 29490868
Aggression 261.68 143.07 117 3925 35424 29535061
Logorrhoea 194.21 143.07 48 3994 2240 29568245
Dysarthria 193.53 143.07 91 3951 30820 29539665
Bradyphrenia 187.59 143.07 53 3989 4161 29566324
Respiratory depression 175.94 143.07 67 3975 13456 29557029
Pulmonary oedema 160.12 143.07 89 3953 42646 29527839

FDA Adverse Event Reporting System (Geriatric)

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
Toxicity to various agents 2383.87 98.11 943 4586 362570 64130633
Drug abuse 775.53 98.11 322 5207 132052 64361151
Aggression 332.69 98.11 131 5398 46101 64447102
Respiratory depression 228.44 98.11 83 5446 23360 64469843
Accidental overdose 226.92 98.11 91 5438 33466 64459737
Bradyphrenia 212.74 98.11 63 5466 9343 64483860
Substance abuse 209.12 98.11 62 5467 9230 64483973
Logorrhoea 208.95 98.11 52 5477 4007 64489196
Dysarthria 203.65 98.11 100 5429 59306 64433897
Asphyxia 198.70 98.11 60 5469 9506 64483697
Pulmonary oedema 163.75 98.11 95 5434 78579 64414624
Drug interaction 153.64 98.11 171 5358 361912 64131291
Overdose 150.95 98.11 118 5411 159448 64333755
Drug dependence 144.48 98.11 66 5463 33246 64459957
Poisoning 139.76 98.11 57 5472 21822 64471381
Coma 126.86 98.11 84 5445 87531 64405672
Depressed level of consciousness 122.57 98.11 80 5449 81356 64411847
Abnormal behaviour 122.29 98.11 59 5470 33563 64459640
Completed suicide 112.51 98.11 116 5413 224298 64268905
Bradykinesia 110.26 98.11 35 5494 6525 64486678
Patient uncooperative 100.48 98.11 20 5509 547 64492656

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N05BA16 NERVOUS SYSTEM
PSYCHOLEPTICS
ANXIOLYTICS
Benzodiazepine derivatives
MeSH PA D014151 Anti-Anxiety Agents
MeSH PA D002491 Central Nervous System Agents
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D018682 GABA Agents
MeSH PA D018757 GABA Modulators
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D011619 Psychotropic Drugs
MeSH PA D014149 Tranquilizing Agents
CHEBI has role CHEBI:35474 anti-anxiety agents
CHEBI has role CHEBI:35623 anticonvulsants
CHEBI has role CHEBI:35717 hypnotics
CHEBI has role CHEBI:50268 GABA modulators
CHEBI has role CHEBI:77746 Homo sapiens metabolite

Drug Use (View source of the data)

None




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 11.98 acidic
pKa2 3.43 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
Gamma-aminobutyric acid type B receptor subunit 2 GPCR IC50 8.03 WOMBAT-PK
Gamma-aminobutyric acid receptor subunit rho-2 Ion channel WOMBAT-PK
GABA-A receptor alpha-1/beta-2/gamma-2 Ion channel IC50 6.28 WOMBAT-PK
GABA-A receptor; anion channel Ion channel Ki 4.14 CHEMBL

External reference:

IDSource
N0000166921 NUI
D08283 KEGG_DRUG
3155 RXNORM
C0011279 UMLSCUI
CHEBI:111762 CHEBI
CHEMBL523 ChEMBL_ID
D003708 MESH_DESCRIPTOR_UI
DB14028 DRUGBANK_ID
4400 INN_ID
67220MCM01 UNII
2997 PUBCHEM_CID
005387 NDDF
96232003 SNOMEDCT_US

Pharmaceutical products:

None