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

Stem definition	Drug id	CAS RN
diazepam derivatives	800	2894-67-9

Description:

Molecule

Description

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:

Property	Value	Reference
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.28 µM/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 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
Drug abuse	1137.81	236.85	185	121	11841	2345938
Sopor	878.46	236.85	130	176	3865	2353914
Intentional self-injury	708.69	236.85	109	197	4018	2353761

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
Sopor	502.37	113.67	74	123	1927	1744657
Drug abuse	354.10	113.67	73	124	13616	1732968
Intentional self-injury	272.98	113.67	46	151	2627	1743957

Pharmacologic Action:

Source	Code	Description
MeSH PA	D000927	Anticonvulsants
MeSH PA	D002491	Central Nervous System Agents

Drug Use (View source of the data)

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
GABA-A receptor alpha-1/beta-2/gamma-2	Ion channel	P14867 P18507 P47870	GBRA1_HUMAN GBRB2_HUMAN GBRG2_HUMAN		IC50	8.75		WOMBAT-PK
GABA-A receptor; anion channel	Ion channel	O00591 O14764 P14867 P18505 P18507 P28472 P31644 P34903 P47869 P47870 P48169 P78334 Q16445 Q8N1C3 Q99928 Q9UN88	GBRA1_HUMAN GBRA2_HUMAN GBRA3_HUMAN GBRA4_HUMAN GBRA5_HUMAN GBRA6_HUMAN GBRB1_HUMAN GBRB2_HUMAN GBRB3_HUMAN GBRD_HUMAN GBRE_HUMAN GBRG1_HUMAN GBRG2_HUMAN GBRG3_HUMAN GBRP_HUMAN GBRT_HUMAN		IC50	8.55		CHEMBL

External reference:

ID	Source
D07784	KEGG_DRUG
CHEBI:135295	CHEBI
CHEMBL268254	ChEMBL_ID
C013434	MESH_SUPPLEMENTAL_RECORD_UI
O91W32476G	UNII
4510	INN_ID
DB01511	DRUGBANK_ID
17925	PUBCHEM_CID

Pharmaceutical products:

None