delorazepam ๐Ÿถ Veterinary Use | 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 ยตM/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 1550.99 56.39 417 3078 72101 63413426
Sopor 1433.22 56.39 312 3183 21852 63463675
Intentional self-injury 807.57 56.39 202 3293 25485 63460042
Intentional overdose 199.80 56.39 92 3403 74060 63411467
Suicide attempt 168.44 56.39 77 3418 60841 63424686
Bradyphrenia 151.09 56.39 41 3454 6939 63478588
Poisoning 131.87 56.39 43 3452 13657 63471870
Toxicity to various agents 106.13 56.39 96 3399 247154 63238373
Intentional product misuse 91.49 56.39 51 3444 60866 63424661
Substance abuse 89.06 56.39 25 3470 4782 63480745
Coma 75.73 56.39 46 3449 64318 63421209
Overdose 74.93 56.39 57 3438 115021 63370506
Bradykinesia 65.32 56.39 20 3475 5168 63480359
Confusional state 62.97 56.39 71 3424 236309 63249218
Tachycardia 62.90 56.39 52 3443 118104 63367423
Psychomotor hyperactivity 58.38 56.39 22 3473 10641 63474886
Sluggishness 56.64 56.39 18 3477 5251 63480276

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 901.45 58.64 191 1716 11945 34943079
Drug abuse 457.47 58.64 178 1729 98918 34856106
Intentional self-injury 300.58 58.64 81 1826 13690 34941334
Bradyphrenia 103.30 58.64 28 1879 4770 34950254
Toxicity to various agents 91.44 58.64 80 1827 200282 34754742
Respiratory depression 80.32 58.64 31 1876 16214 34938810
Bradykinesia 66.69 58.64 19 1888 3874 34951150
Drug interaction 66.56 58.64 71 1836 225875 34729149
Intentional overdose 61.72 58.64 35 1872 43639 34911385

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
Sopor 2221.48 54.89 498 4887 32512 79706491
Drug abuse 1750.51 54.89 577 4808 162114 79576889
Intentional self-injury 1092.74 54.89 281 5104 32138 79706865
Bradyphrenia 242.55 54.89 68 5317 10572 79728431
Intentional overdose 229.55 54.89 121 5264 105839 79633164
Suicide attempt 191.77 54.89 99 5286 82833 79656170
Toxicity to various agents 173.30 54.89 175 5210 421365 79317638
Bradykinesia 115.64 54.89 36 5349 8007 79730996
Psychomotor hyperactivity 103.67 54.89 40 5345 16809 79722194
Intentional product misuse 101.58 54.89 69 5316 95096 79643907
Overdose 95.18 54.89 87 5298 184119 79554884
Poisoning 94.39 54.89 42 5343 25230 79713773
Substance abuse 83.07 54.89 30 5355 10496 79728507
Confusional state 82.18 54.89 104 5281 317893 79421110
Coma 82.15 54.89 62 5323 100587 79638416
Sedation 81.31 54.89 48 5337 51847 79687156
Sluggishness 76.28 54.89 25 5360 6547 79732456
Drug interaction 71.82 54.89 112 5273 415071 79323932
Confabulation 64.49 54.89 13 5372 485 79738518
Somnolence 61.39 54.89 78 5307 238903 79500100
Respiratory depression 58.06 54.89 31 5354 27599 79711404
Tachycardia 57.06 54.89 65 5320 177703 79561300

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
MeSH PA D000927 Anticonvulsants
MeSH PA D002491 Central Nervous System 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




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 11.52 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
C0055353 UMLSCUI
CHEBI:135295 CHEBI
CHEMBL268254 ChEMBL_ID
DB01511 DRUGBANK_ID
17925 PUBCHEM_CID
C013434 MESH_SUPPLEMENTAL_RECORD_UI
4510 INN_ID
O91W32476G UNII

Pharmaceutical products:

None