quazepam Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
diazepam derivatives 2336 36735-22-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • Sch-16134
  • Sch 16134
  • quazepam
  • quazium
  • prosedar
  • Molecular weight: 386.79
  • Formula: C17H11ClF4N2S
  • CLOGP: 3.70
  • LIPINSKI: 0
  • HAC: 2
  • HDO: 0
  • TPSA: 15.60
  • ALOGS: -5.22
  • ROTB: 3

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
15 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.55 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 32 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

DateAgencyCompanyOrphan
Dec. 27, 1985 FDA SCIECURE PHARMA INC

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
Suicide attempt 68.63 35.01 26 630 58142 53290268
Altered state of consciousness 47.84 35.01 16 640 24820 53323590
Intentional overdose 38.51 35.01 18 638 67187 53281223

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
Altered state of consciousness 49.54 35.41 20 933 21977 32490596
Blood creatine phosphokinase increased 38.44 35.41 21 932 45455 32467118

Pharmacologic Action:

SourceCodeDescription
ATC N05CD10 NERVOUS SYSTEM
PSYCHOLEPTICS
HYPNOTICS AND SEDATIVES
Benzodiazepine derivatives
FDA CS M0002356 Benzodiazepines
MeSH PA D002491 Central Nervous System Agents
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D006993 Hypnotics and Sedatives
FDA EPC N0000175694 Benzodiazepine

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Insomnia indication 193462001
Suicidal thoughts contraindication 6471006
Disorder of lung contraindication 19829001 DOID:850
Alcohol intoxication contraindication 25702006
Shock contraindication 27942005
Depressive disorder contraindication 35489007
Substance abuse contraindication 66214007
Sleep apnea contraindication 73430006 DOID:0050847
Decreased respiratory function contraindication 80954004
Kidney disease contraindication 90708001 DOID:557
Hypoalbuminemia contraindication 119247004
Disease of liver contraindication 235856003 DOID:409
Sleep automatism contraindication 247962006
Pregnancy, function contraindication 289908002
Severe chronic obstructive pulmonary disease contraindication 313299006
Coma contraindication 371632003
Breastfeeding (mother) contraindication 413712001
Porphyria contraindication 418470004

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 1.65 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
15MG DORAL GALT PHARMS N018708 Dec. 27, 1985 RX TABLET ORAL 7608616 June 3, 2028 METHOD FOR TREATING INSOMNIA WHILE REDUCING THE RISK OF AN ADVERSE DRUG INTERACTION
7.5MG DORAL GALT PHARMS N018708 Feb. 26, 1987 DISCN TABLET ORAL 7608616 June 3, 2028 METHOD FOR TREATING INSOMNIA WHILE REDUCING THE RISK OF AN ADVERSE DRUG INTERACTION

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-1/gamma-2 Ion channel POSITIVE ALLOSTERIC MODULATOR Ki 7.71 WOMBAT-PK CHEMBL
GABA A receptor alpha-3/beta-1/gamma-2 Ion channel POSITIVE ALLOSTERIC MODULATOR Ki 6.63 WOMBAT-PK CHEMBL
GABA A receptor alpha-2/beta-1/gamma-2 Ion channel POSITIVE ALLOSTERIC MODULATOR Ki 6.69 WOMBAT-PK CHEMBL

External reference:

IDSource
4019522 VUID
N0000147639 NUI
D00457 KEGG_DRUG
4019522 VANDF
C0072828 UMLSCUI
CHEBI:8694 CHEBI
CHEMBL1200472 ChEMBL_ID
DB01589 DRUGBANK_ID
C025130 MESH_SUPPLEMENTAL_RECORD_UI
4999 PUBCHEM_CID
7288 IUPHAR_LIGAND_ID
4018 INN_ID
JF8V0828ZI UNII
35185 RXNORM
273189 MMSL
5398 MMSL
d00917 MMSL
001469 NDDF
108391004 SNOMEDCT_US
371372004 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
DORAL HUMAN PRESCRIPTION DRUG LABEL 1 61825-165 TABLET 15 mg ORAL NDA 29 sections
Quazepam HUMAN PRESCRIPTION DRUG LABEL 1 71993-265 TABLET 15 mg ORAL NDA 29 sections