loprazolam 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
diazepam derivatives 1602 61197-73-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • loprazolam mesylate
  • loprazolam
  • loprazolam mesilate
  • Molecular weight: 464.91
  • Formula: C23H21ClN6O3
  • CLOGP: 0.43
  • LIPINSKI: 0
  • HAC: 9
  • HDO: 0
  • TPSA: 97.33
  • ALOGS: -3.71
  • ROTB: 3

Drug dosage:

DoseUnitRoute
1 mg O

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1983 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
Coma 167.10 48.62 48 518 64316 63424140
Pyramidal tract syndrome 78.56 48.62 11 555 352 63488104
Hepatocellular injury 68.71 48.62 20 546 27361 63461095
Bundle branch block right 55.32 48.62 12 554 4986 63483470
Bradypnoea 53.50 48.62 11 555 3539 63484917
Somnolence 51.59 48.62 27 539 178658 63309798
Miosis 50.71 48.62 12 554 7341 63481115

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
Rhabdomyolysis 58.54 50.76 24 396 68139 34888372

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
Coma 191.33 37.21 65 985 100584 79642754
Miosis 90.45 37.21 24 1026 15765 79727573
Somnolence 78.71 37.21 45 1005 238936 79504402
Pyramidal tract syndrome 61.54 37.21 10 1040 587 79742751
Bradypnoea 58.53 37.21 14 1036 6038 79737300
Hepatocellular injury 53.58 37.21 21 1029 47572 79695766
Toxicity to various agents 53.36 37.21 44 1006 421496 79321842
Rhabdomyolysis 49.45 37.21 25 1025 103106 79640232

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N05CD11 NERVOUS SYSTEM
PSYCHOLEPTICS
HYPNOTICS AND SEDATIVES
Benzodiazepine derivatives

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

DiseaseRelationSNOMED_IDDOID
Insomnia indication 193462001




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.28 Basic
pKa2 4.28 Basic
pKa3 2.6 Basic
pKa4 1.98 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-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
GABA-A receptor alpha-1/beta-3/gamma-2 Ion channel WOMBAT-PK

External reference:

IDSource
D07326 KEGG_DRUG
C0077013 UMLSCUI
CHEBI:135754 CHEBI
CHEMBL2107448 ChEMBL_ID
DB13643 DRUGBANK_ID
4884 INN_ID
70111-54-5 SECONDARY_CAS_RN
759N8462G8 UNII
3033860 PUBCHEM_CID
235846 RXNORM
004097 NDDF
004098 NDDF
321119005 SNOMEDCT_US
395774003 SNOMEDCT_US
442011001 SNOMEDCT_US

Pharmaceutical products:

None