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

Stem definition	Drug id	CAS RN
diazepam derivatives	2336	36735-22-5

Description:

Molecule

Description

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:

Dose	Unit	Route
15	mg	O

ADMET properties:

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

Approvals:

Date	Agency	Company	Orphan
Dec. 27, 1985	FDA	SCIECURE PHARMA INC

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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:

Source	Code	Description
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)

Disease	Relation	SNOMED_ID	DOID
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 level	Dissociation constant	Type (acidic/basic)
pKa1	1.65	Basic

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent 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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
GABA A receptor alpha-1/beta-1/gamma-2	Ion channel	P14867 P18505 P18507	GBRA1_HUMAN GBRB1_HUMAN GBRG2_HUMAN	POSITIVE ALLOSTERIC MODULATOR	Ki	7.71		WOMBAT-PK	CHEMBL
GABA A receptor alpha-3/beta-1/gamma-2	Ion channel	P18505 P18507 P34903	GBRB1_HUMAN GBRG2_HUMAN GBRA3_HUMAN	POSITIVE ALLOSTERIC MODULATOR	Ki	6.63		WOMBAT-PK	CHEMBL
GABA A receptor alpha-2/beta-1/gamma-2	Ion channel	P18505 P18507 P47869	GBRB1_HUMAN GBRG2_HUMAN GBRA2_HUMAN	POSITIVE ALLOSTERIC MODULATOR	Ki	6.69		WOMBAT-PK	CHEMBL

External reference:

ID	Source
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:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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