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

Stem definitionDrug idCAS RN
diazepam derivatives 1102 40054-69-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • Y 7131
  • etizolam
  • depas
  • AHR-3219
  • Y-7131
  • Molecular weight: 342.85
  • Formula: C17H15ClN4S
  • CLOGP: 3.02
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 0
  • TPSA: 43.07
  • ALOGS: -3.91
  • ROTB: 2

Drug dosage:

None

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 0.30 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.17 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1984 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 115.97 23.12 115 4570 247135 63237202
Hepatic function abnormal 89.52 23.12 47 4638 37095 63447242
Altered state of consciousness 78.61 23.12 38 4647 25192 63459145
Drug abuse 76.43 23.12 54 4631 72464 63411873
Intentional overdose 70.79 23.12 52 4633 74100 63410237
Distributive shock 65.01 23.12 16 4669 1367 63482970
Spinal compression fracture 61.69 23.12 27 4658 14256 63470081
Neutrophil count decreased 50.32 23.12 38 4647 56368 63427969
Cardiac failure 48.27 23.12 45 4640 89097 63395240
Suicide attempt 47.73 23.12 38 4647 60880 63423457
Platelet count decreased 46.95 23.12 50 4635 116072 63368265
Fatigue 39.01 23.12 9 4676 888019 62596318
Pemphigoid 38.73 23.12 16 4669 7328 63477009
Drug ineffective 37.96 23.12 15 4670 1044750 62439587
Anaemia 37.66 23.12 73 4612 293357 63190980
Haemorrhage subcutaneous 36.22 23.12 12 4673 2971 63481366
Renal impairment 35.61 23.12 38 4647 88317 63396020
Interstitial lung disease 33.00 23.12 31 4654 61877 63422460
Hypokalaemia 32.24 23.12 39 4646 103765 63380572
Overdose 32.16 23.12 41 4644 115037 63369300
Cerebral infarction 30.37 23.12 20 4665 23873 63460464
Needle track marks 28.04 23.12 4 4681 14 63484323
Disseminated intravascular coagulation 26.81 23.12 17 4668 19034 63465303
Counterfeit product administered 25.39 23.12 4 4681 31 63484306
Vasoplegia syndrome 25.38 23.12 8 4677 1691 63482646
Osteonecrosis of jaw 23.49 23.12 20 4665 35103 63449234
Accidental poisoning 23.23 23.12 6 4679 622 63483715

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 627.25 21.86 342 3553 200020 34753016
Respiratory depression 244.90 21.86 85 3810 16160 34936876
Drug abuse 223.67 21.86 138 3757 98958 34854078
Pulmonary oedema 140.50 21.86 79 3816 47450 34905586
Pulmonary congestion 69.93 21.86 33 3862 13732 34939304
Alcohol interaction 66.95 21.86 21 3874 2892 34950144
Drug interaction 66.65 21.86 102 3793 225844 34727192
Brain oedema 57.77 21.86 29 3866 13792 34939244
Counterfeit product administered 52.43 21.86 10 3885 165 34952871
Interstitial lung disease 42.64 21.86 44 3851 65238 34887798
Hepatic function abnormal 40.55 21.86 36 3859 44327 34908709
Pneumonia aspiration 26.90 21.86 28 3867 41875 34911161
Left ventricular enlargement 24.54 21.86 7 3888 695 34952341
Product counterfeit 23.14 21.86 5 3890 157 34952879
Fatigue 22.03 21.86 7 3888 370646 34582390

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 605.66 19.71 442 8425 421098 79314423
Drug abuse 269.50 19.71 187 8680 162504 79573017
Respiratory depression 210.71 19.71 88 8779 27542 79707979
Hepatic function abnormal 113.65 19.71 81 8786 73026 79662495
Pulmonary oedema 95.86 19.71 79 8788 88175 79647346
Altered state of consciousness 80.90 19.71 54 8813 43768 79691753
Alcohol interaction 79.11 19.71 27 8840 4847 79730674
Interstitial lung disease 68.43 19.71 73 8794 112527 79622994
Intentional overdose 64.93 19.71 69 8798 105891 79629630
Spinal compression fracture 60.54 19.71 32 8835 16926 79718595
Fatigue 57.96 19.71 16 8851 929711 78805810
Drug interaction 54.32 19.71 133 8734 415050 79320471
Suicide attempt 52.56 19.71 55 8812 82877 79652644
Pulmonary congestion 51.46 19.71 34 8833 27066 79708455
Cardiac failure 51.30 19.71 74 8793 154768 79580753
Counterfeit product administered 48.59 19.71 9 8858 126 79735395
Distributive shock 48.00 19.71 16 8851 2671 79732850
Pneumonia aspiration 45.29 19.71 46 8821 66921 79668600
Brain oedema 43.90 19.71 30 8837 25233 79710288
Neutrophil count decreased 43.62 19.71 53 8814 93906 79641615
Platelet count decreased 42.53 19.71 77 8790 194587 79540934
Drug ineffective 42.42 19.71 35 8832 1080878 78654643
Cerebral infarction 35.77 19.71 34 8833 45642 79689879
Pemphigoid 30.99 19.71 20 8847 15295 79720226
Renal impairment 30.20 19.71 59 8808 157724 79577797
Accidental poisoning 30.13 19.71 10 8857 1647 79733874
Haemorrhage subcutaneous 29.03 19.71 13 8854 4796 79730725
White blood cell count decreased 28.56 19.71 64 8803 188224 79547297
Pain 28.52 19.71 22 8845 703780 79031741
Delusion 28.00 19.71 21 8846 20402 79715119
Arthralgia 25.63 19.71 16 8851 571787 79163734
Restlessness 24.50 19.71 28 8839 46464 79689057
Left ventricular enlargement 24.13 19.71 7 8860 739 79734782
Blood creatine phosphokinase increased 23.95 19.71 33 8834 66057 79669464
Decreased appetite 23.94 19.71 88 8779 342330 79393191
Erythema multiforme 23.87 19.71 18 8849 17633 79717888
Drug hypersensitivity 23.07 19.71 3 8864 298913 79436608
Overdose 22.93 19.71 58 8809 184148 79551373
Malignant neoplasm progression 22.63 19.71 48 8819 135942 79599579
Enterocolitis 22.33 19.71 16 8851 14496 79721025
Anaemia 22.16 19.71 103 8764 444912 79290609
Hypokalaemia 21.87 19.71 49 8818 143991 79591530
Pyelonephritis 21.58 19.71 18 8849 20370 79715151
Upper respiratory tract inflammation 21.49 19.71 10 8857 4025 79731496
Rhabdomyolysis 21.49 19.71 40 8827 103091 79632430
Drug withdrawal maintenance therapy 21.46 19.71 4 8863 58 79735463
Disseminated intravascular coagulation 21.32 19.71 23 8844 35819 79699702
Heat illness 21.30 19.71 6 8861 571 79734950
White blood cell count increased 20.89 19.71 33 8834 74600 79660921
Drug dependence 20.55 19.71 24 8843 40745 79694776
Urinary retention 20.10 19.71 28 8839 56602 79678919

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N05BA19 NERVOUS SYSTEM
PSYCHOLEPTICS
ANXIOLYTICS
Benzodiazepine derivatives
MeSH PA D002491 Central Nervous System Agents
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D011619 Psychotropic Drugs
MeSH PA D014149 Tranquilizing Agents

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

DiseaseRelationSNOMED_IDDOID
Anxiety indication 48694002




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 6.64 Basic
pKa2 4.89 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 EC50 8.10 WOMBAT-PK
GABA-A receptor alpha-2/beta-3/gamma-2 Ion channel WOMBAT-PK
GABA-A receptor alpha-3/beta-3/gamma-2 Ion channel WOMBAT-PK
GABA-A receptor alpha-5/beta-3/gamma-2 Ion channel WOMBAT-PK

External reference:

IDSource
D01514 KEGG_DRUG
C0059862 UMLSCUI
CHEBI:31583 CHEBI
CHEMBL1289779 ChEMBL_ID
DB09166 DRUGBANK_ID
C044610 MESH_SUPPLEMENTAL_RECORD_UI
3307 PUBCHEM_CID
4563 INN_ID
A76XI0HL37 UNII
008161 NDDF
1163197005 SNOMEDCT_US
1173020002 SNOMEDCT_US
H4C PDB_CHEM_ID

Pharmaceutical products:

None