nordazepam 🐶 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 µM/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 961.38 103.49 326 1482 246924 63240290
Asphyxia 233.33 103.49 50 1758 6131 63481083
Drug abuse 205.28 103.49 77 1731 72441 63414773
Poisoning 155.39 103.49 42 1766 13658 63473556
Completed suicide 130.31 103.49 69 1739 145604 63341610
Victim of sexual abuse 125.78 103.49 21 1787 663 63486551
Coma 121.13 103.49 51 1757 64313 63422901
Substance abuse 105.50 103.49 25 1783 4782 63482432
Accidental overdose 104.77 103.49 35 1773 23274 63463940
Drug interaction 103.76 103.49 70 1738 229061 63258153

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 2021.44 122.63 800 3824 199562 34752745
Drug abuse 900.04 122.63 372 4252 98724 34853583
Aggression 277.08 122.63 124 4500 38840 34913467
Depressed level of consciousness 199.49 122.63 102 4522 42739 34909568
Respiratory depression 197.74 122.63 76 4548 16169 34936138
Logorrhoea 192.94 122.63 48 4576 2378 34949929
Dysarthria 189.02 122.63 92 4532 34690 34917617
Drug dependence 184.51 122.63 81 4543 24136 34928171
Pulmonary oedema 183.91 122.63 100 4524 47429 34904878
Bradyphrenia 182.46 122.63 53 4571 4745 34947562
Substance abuse 158.16 122.63 53 4571 7588 34944719
Brain oedema 141.22 122.63 57 4567 13764 34938543
Poisoning 133.85 122.63 53 4571 12173 34940134
Drug interaction 123.45 122.63 150 4474 225796 34726511

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 2777.99 100.35 1077 5303 420463 79317545
Drug abuse 1118.80 100.35 435 5945 162256 79575752
Aggression 353.52 100.35 138 6242 50820 79687188
Asphyxia 322.34 100.35 90 6290 11630 79726378
Poisoning 288.98 100.35 99 6281 25173 79712835
Substance abuse 276.54 100.35 78 6302 10448 79727560
Respiratory depression 250.14 100.35 91 6289 27539 79710469
Accidental overdose 245.69 100.35 99 6281 39482 79698526
Drug dependence 219.12 100.35 92 6288 40677 79697331
Bradyphrenia 209.32 100.35 63 6317 10577 79727431
Logorrhoea 208.73 100.35 52 6328 4313 79733695
Drug interaction 203.65 100.35 205 6175 414978 79323030
Dysarthria 200.74 100.35 101 6279 67521 79670487
Pulmonary oedema 194.44 100.35 108 6272 88146 79649862
Overdose 179.89 100.35 135 6245 184071 79553937
Depressed level of consciousness 177.37 100.35 105 6275 96547 79641461
Coma 153.08 100.35 97 6283 100552 79637456
Brain oedema 132.26 100.35 56 6324 25207 79712801
Miosis 131.69 100.35 49 6331 15740 79722268
Abnormal behaviour 121.64 100.35 59 6321 36362 79701646
Completed suicide 115.69 100.35 119 6261 245648 79492360
Intentional overdose 112.99 100.35 82 6298 105878 79632130
Bradykinesia 105.60 100.35 35 6345 8008 79730000
Victim of crime 104.85 100.35 20 6360 468 79737540
Victim of sexual abuse 103.12 100.35 20 6360 512 79737496

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 | 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 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