DIAZEPAM HYDROCHLORIDE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C16H13ClN2O.ClH
Molecular Weight	321.201
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

Cl.CN1C2=CC=C(Cl)C=C2C(=NCC1=O)C3=CC=CC=C3

InChI

InChIKey=BPYZIOINRAWEQL-UHFFFAOYSA-N

InChI=1S/C16H13ClN2O.ClH/c1-19-14-8-7-12(17)9-13(14)16(18-10-15(19)20)11-5-3-2-4-6-11;/h2-9H,10H2,1H3;1H

HIDE SMILES / InChI

Description
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/013263s092lbl.pdf
Curator's Comment: description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/24552479

Diazepam is a benzodiazepine first discovered at Hoﬀman-La Roche in the late 1950s. Diazepam was approved by FDA for the treatment of anxiety disorders as well as for such conditions as skeletal muscle spasm, alcohol withdrawal syndrom and convulsions (under the most known brand Valium). The drug acts by binding to GABA-A receptors and potentiating GABA evoked current. Chronic diazepam use is associated with tolerance, dependence, and withdrawal.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
GABA-A receptor; benzodiazepine site 38 Target ID: CHEMBL2109243 Sources: http://www.hamiltonhealthsciences.ca/workfiles/basehospital/diazepam.pdf	Agonist 2678		8.6 nM [Ki]

Conditions

Condition	Modality	Highest Phase	Product
Anxiety 267 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/013263s092lbl.pdf	Primary	Approved 8429	VALIUM Approved Use Valium is indicated for the management of anxiety disorders or for the shortterm relief of the symptoms of anxiety. In acute alcohol withdrawal, Valium may be useful in the symptomatic relief of acute agitation, tremor, impending or acute delirium tremens and hallucinosis. Valium is a useful adjunct for the relief of skeletal muscle spasm due to reflex spasm to local pathology (such as inflammation of the muscles or joints, or secondary to trauma), spasticity caused by upper motor neuron disorders (such as cerebral palsy and paraplegia), athetosis, and stiff-man syndrome. Oral Valium may be used adjunctively in convulsive disorders, although it has not proved useful as the sole therapy. Launch Date 1963
Acute alcohol withdrawal 2 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/013263s092lbl.pdf	Palliative	Approved 8429	VALIUM Approved Use Valium is indicated for the management of anxiety disorders or for the shortterm relief of the symptoms of anxiety. In acute alcohol withdrawal, Valium may be useful in the symptomatic relief of acute agitation, tremor, impending or acute delirium tremens and hallucinosis. Valium is a useful adjunct for the relief of skeletal muscle spasm due to reflex spasm to local pathology (such as inflammation of the muscles or joints, or secondary to trauma), spasticity caused by upper motor neuron disorders (such as cerebral palsy and paraplegia), athetosis, and stiff-man syndrome. Oral Valium may be used adjunctively in convulsive disorders, although it has not proved useful as the sole therapy. Launch Date 1963
Muscle spasm 40 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/013263s092lbl.pdf	Palliative	Approved 8429	VALIUM Approved Use Valium is indicated for the management of anxiety disorders or for the shortterm relief of the symptoms of anxiety. In acute alcohol withdrawal, Valium may be useful in the symptomatic relief of acute agitation, tremor, impending or acute delirium tremens and hallucinosis. Valium is a useful adjunct for the relief of skeletal muscle spasm due to reflex spasm to local pathology (such as inflammation of the muscles or joints, or secondary to trauma), spasticity caused by upper motor neuron disorders (such as cerebral palsy and paraplegia), athetosis, and stiff-man syndrome. Oral Valium may be used adjunctively in convulsive disorders, although it has not proved useful as the sole therapy. Launch Date 1963
Convulsive disorders 2 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/013263s092lbl.pdf	Palliative	Approved 8429	VALIUM Approved Use Valium is indicated for the management of anxiety disorders or for the shortterm relief of the symptoms of anxiety. In acute alcohol withdrawal, Valium may be useful in the symptomatic relief of acute agitation, tremor, impending or acute delirium tremens and hallucinosis. Valium is a useful adjunct for the relief of skeletal muscle spasm due to reflex spasm to local pathology (such as inflammation of the muscles or joints, or secondary to trauma), spasticity caused by upper motor neuron disorders (such as cerebral palsy and paraplegia), athetosis, and stiff-man syndrome. Oral Valium may be used adjunctively in convulsive disorders, although it has not proved useful as the sole therapy. Launch Date 1963

C_max

Value	Dose	Analyte	Population
317 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1505149	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	DIAZEPAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
75 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1505149	2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered:	DIAZEPAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
172 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1505149	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	DIAZEPAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
208 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01417078	20 mg single, intranasal dose: 20 mg route of administration: intranasal experiment type: single co-administered:	DIAZEPAM plasma	Homo sapiens population: unhealthy age: sex: food status:

AUC

Value	Dose	Analyte	Population
1530 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1505149	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	DIAZEPAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
330 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1505149	2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered:	DIAZEPAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
779 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1505149	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	DIAZEPAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1227 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01417078	20 mg single, intranasal dose: 20 mg route of administration: intranasal experiment type: single co-administered:	DIAZEPAM plasma	Homo sapiens population: unhealthy age: sex: food status:

T_1/2

Value	Dose	Co-administered	Analyte	Population
48 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/013263s094lbl.pdf	unknown, oral		DIAZEPAM plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
2% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/013263s094lbl.pdf	unknown, oral		DIAZEPAM plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
2000 mg single, oral Overdose Dose: 2000 mg Route: oral Route: single Dose: 2000 mg Sources: https://pubmed.ncbi.nlm.nih.gov/357765	healthy, 28 years Health Status: healthy Age Group: 28 years Sex: M Sources: https://pubmed.ncbi.nlm.nih.gov/357765	Sources: https://pubmed.ncbi.nlm.nih.gov/357765
500 mg single, oral Overdose Dose: 500 mg Route: oral Route: single Dose: 500 mg Sources: https://pubmed.ncbi.nlm.nih.gov/357765	unhealthy, 61 years Health Status: unhealthy Age Group: 61 years Sex: F Sources: https://pubmed.ncbi.nlm.nih.gov/357765	Sources: https://pubmed.ncbi.nlm.nih.gov/357765
0.2 mg/kg 2 times / day multiple, rectal Recommended Dose: 0.2 mg/kg, 2 times / day Route: rectal Route: multiple Dose: 0.2 mg/kg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf	unhealthy, > 12 years Health Status: unhealthy Condition: seizure activity Age Group: > 12 years Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf	Other AEs: Respiratory depression, Abuse... Other AEs: Respiratory depression (serious\|grade 5) Abuse (serious\|grade 5) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf
0.2 mg/kg 2 times / day multiple, rectal Recommended Dose: 0.2 mg/kg, 2 times / day Route: rectal Route: multiple Dose: 0.2 mg/kg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf	unhealthy, > 12 years n = 573 Health Status: unhealthy Condition: seizure activity Age Group: > 12 years Population Size: 573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf	Disc. AE: Somnolence, Hypoventilation... AEs leading to discontinuation/dose reduction: Somnolence (3 patients) Hypoventilation (2 patients) Rash (2 patients) Asthenia (1 patient) Hyperkinesia (1 patient) Incoordination (1 patient) Vasodilatation (1 patient) Urticaria (1 patient) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf
10 mg 2 times / day multiple, intranasal Recommended Dose: 10 mg, 2 times / day Route: intranasal Route: multiple Dose: 10 mg, 2 times / day Co-administed with:: benzodiazepines Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211635s000lbl.pdf	unhealthy, adult Health Status: unhealthy Age Group: adult Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211635s000lbl.pdf	Other AEs: Respiratory depression... Other AEs: Respiratory depression (serious\|grade 5) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211635s000lbl.pdf
10 mg 4 times / day multiple, intramuscular Recommended Dose: 10 mg, 4 times / day Route: intramuscular Route: multiple Dose: 10 mg, 4 times / day Co-administed with:: benzodiazepines Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020124s033lbl.pdf	unhealthy, adult Health Status: unhealthy Condition: anxiety disorders Age Group: adult Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020124s033lbl.pdf	Other AEs: Respiratory depression, Abuse... Other AEs: Respiratory depression (serious\|grade 5) Abuse (serious\|grade 5) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020124s033lbl.pdf
10 mg 4 times / day multiple, oral Recommended Dose: 10 mg, 4 times / day Route: oral Route: multiple Dose: 10 mg, 4 times / day Co-administed with:: OPIOIDS Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/013263s094lbl.pdf	unhealthy, adult Health Status: unhealthy Condition: Anxiety Disorders Age Group: adult Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/013263s094lbl.pdf	Other AEs: Respiratory depression... Other AEs: Respiratory depression (serious\|grade 5) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/013263s094lbl.pdf

AEs

AE	Significance	Dose	Population
Abuse	serious\|grade 5	0.2 mg/kg 2 times / day multiple, rectal Recommended Dose: 0.2 mg/kg, 2 times / day Route: rectal Route: multiple Dose: 0.2 mg/kg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf	unhealthy, > 12 years Health Status: unhealthy Condition: seizure activity Age Group: > 12 years Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf
Respiratory depression	serious\|grade 5	0.2 mg/kg 2 times / day multiple, rectal Recommended Dose: 0.2 mg/kg, 2 times / day Route: rectal Route: multiple Dose: 0.2 mg/kg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf	unhealthy, > 12 years Health Status: unhealthy Condition: seizure activity Age Group: > 12 years Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf
Asthenia	1 patient Disc. AE	0.2 mg/kg 2 times / day multiple, rectal Recommended Dose: 0.2 mg/kg, 2 times / day Route: rectal Route: multiple Dose: 0.2 mg/kg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf	unhealthy, > 12 years n = 573 Health Status: unhealthy Condition: seizure activity Age Group: > 12 years Population Size: 573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf
Hyperkinesia	1 patient Disc. AE	0.2 mg/kg 2 times / day multiple, rectal Recommended Dose: 0.2 mg/kg, 2 times / day Route: rectal Route: multiple Dose: 0.2 mg/kg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf	unhealthy, > 12 years n = 573 Health Status: unhealthy Condition: seizure activity Age Group: > 12 years Population Size: 573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf
Incoordination	1 patient Disc. AE	0.2 mg/kg 2 times / day multiple, rectal Recommended Dose: 0.2 mg/kg, 2 times / day Route: rectal Route: multiple Dose: 0.2 mg/kg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf	unhealthy, > 12 years n = 573 Health Status: unhealthy Condition: seizure activity Age Group: > 12 years Population Size: 573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf
Urticaria	1 patient Disc. AE	0.2 mg/kg 2 times / day multiple, rectal Recommended Dose: 0.2 mg/kg, 2 times / day Route: rectal Route: multiple Dose: 0.2 mg/kg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf	unhealthy, > 12 years n = 573 Health Status: unhealthy Condition: seizure activity Age Group: > 12 years Population Size: 573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf
Vasodilatation	1 patient Disc. AE	0.2 mg/kg 2 times / day multiple, rectal Recommended Dose: 0.2 mg/kg, 2 times / day Route: rectal Route: multiple Dose: 0.2 mg/kg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf	unhealthy, > 12 years n = 573 Health Status: unhealthy Condition: seizure activity Age Group: > 12 years Population Size: 573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf
Hypoventilation	2 patients Disc. AE	0.2 mg/kg 2 times / day multiple, rectal Recommended Dose: 0.2 mg/kg, 2 times / day Route: rectal Route: multiple Dose: 0.2 mg/kg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf	unhealthy, > 12 years n = 573 Health Status: unhealthy Condition: seizure activity Age Group: > 12 years Population Size: 573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf
Rash	2 patients Disc. AE	0.2 mg/kg 2 times / day multiple, rectal Recommended Dose: 0.2 mg/kg, 2 times / day Route: rectal Route: multiple Dose: 0.2 mg/kg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf	unhealthy, > 12 years n = 573 Health Status: unhealthy Condition: seizure activity Age Group: > 12 years Population Size: 573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf
Somnolence	3 patients Disc. AE	0.2 mg/kg 2 times / day multiple, rectal Recommended Dose: 0.2 mg/kg, 2 times / day Route: rectal Route: multiple Dose: 0.2 mg/kg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf	unhealthy, > 12 years n = 573 Health Status: unhealthy Condition: seizure activity Age Group: > 12 years Population Size: 573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020648s022lbl.pdf
Respiratory depression	serious\|grade 5	10 mg 2 times / day multiple, intranasal Recommended Dose: 10 mg, 2 times / day Route: intranasal Route: multiple Dose: 10 mg, 2 times / day Co-administed with:: benzodiazepines Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211635s000lbl.pdf	unhealthy, adult Health Status: unhealthy Age Group: adult Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211635s000lbl.pdf
Abuse	serious\|grade 5	10 mg 4 times / day multiple, intramuscular Recommended Dose: 10 mg, 4 times / day Route: intramuscular Route: multiple Dose: 10 mg, 4 times / day Co-administed with:: benzodiazepines Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020124s033lbl.pdf	unhealthy, adult Health Status: unhealthy Condition: anxiety disorders Age Group: adult Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020124s033lbl.pdf
Respiratory depression	serious\|grade 5	10 mg 4 times / day multiple, intramuscular Recommended Dose: 10 mg, 4 times / day Route: intramuscular Route: multiple Dose: 10 mg, 4 times / day Co-administed with:: benzodiazepines Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020124s033lbl.pdf	unhealthy, adult Health Status: unhealthy Condition: anxiety disorders Age Group: adult Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020124s033lbl.pdf
Respiratory depression	serious\|grade 5	10 mg 4 times / day multiple, oral Recommended Dose: 10 mg, 4 times / day Route: oral Route: multiple Dose: 10 mg, 4 times / day Co-administed with:: OPIOIDS Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/013263s094lbl.pdf	unhealthy, adult Health Status: unhealthy Condition: Anxiety Disorders Age Group: adult Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/013263s094lbl.pdf

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1737	inhibitor 1767 substrate 1037	inhibitor 1852 substrate 1217	inhibitor 1612

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP2A6 707 Cav1.2 45 Nav1.5 97 OCT3 150	CYP2C19 991 CYP1A2 1054 CYP2A6 543 CYP2B6 664 CYP2C8 693 CYP2E1 667 CYP3A5 395

Drug as perpetrator

Target	Modality	Activity
CYP2A6 739	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/020648_S002_DIASTAT_AP.pdf#page=8 Page: 8.0	no
CYP2C9 1819	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/020648_S002_DIASTAT_AP.pdf#page=8 Page: 8.0	no
CYP2D6 1891	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/020648_S002_DIASTAT_AP.pdf#page=8 Page: 8.0	no
OCT3 150	inhibitor 3277 Sources: https://link.springer.com/article/10.1007/s00424-013-1335-8 Page: 1.0	strong [IC50 2 uM]

Drug as victim

Target	Modality	Activity
CYP2B6 664	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/8948091/ Page: 1.0	major
CYP2C19 991	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/020648_S002_DIASTAT_AP.pdf#page=8 Page: 8.0	major
CYP3A4 1737	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/020648_S002_DIASTAT_AP.pdf#page=8 Page: 8.0	major
CYP3A5 395	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/8948091/ Page: 1.0	major
CYP1A2 1054	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/8948091/ Page: 1.0	yes
CYP2A6 543	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/8948091/ Page: 1.0	yes
CYP2C8 693	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/8948091/ Page: 1.0	yes
CYP2C9 1037	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/8948091/ Page: 1.0	yes
CYP2D6 1217	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/8948091/ Page: 1.0	yes
CYP2E1 667	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/8948091/ Page: 1.0	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
Cav1.2 49	inhibitor 1626 Sources: https://static-content.springer.com/esm/art%3A10.1038%2Fsrep02100/MediaObjects/41598_2013_BFsrep02100_MOESM1_ESM.pdf#page=3 Page: 3.0
Nav1.5 100	inhibitor 1626 Sources: https://static-content.springer.com/esm/art%3A10.1038%2Fsrep02100/MediaObjects/41598_2013_BFsrep02100_MOESM1_ESM.pdf#page=3 Page: 3.0
hERG 1647	inhibitor 1626 Sources: https://static-content.springer.com/esm/art%3A10.1038%2Fsrep02100/MediaObjects/41598_2013_BFsrep02100_MOESM1_ESM.pdf#page=3 Page: 3.0

Sourcing

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:49575	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:49575
ZINC	ZINC000000006427	http://zinc15.docking.org/substances/ZINC000000006427
eMolecules	536763	https://www.emolecules.com/cgi-bin/more?vid=536763

PubMed

Title	Date	PubMed
The effect of cold and diazepam on the toxicity of fenfluramine in mice.	1975 Mar 15	1116545
A comparative study of etomidate and methohexital as induction agents for analgesic anesthesia.	1976	1015219
[Provocation of tonic seizures during intravenous faustan administration].	1978 Nov	104080
Influence of adenosine agonists and antiepileptic drugs on theophylline-induced seizures in rats.	1998 Oct	10874349
[A case of cardiac arrest after torsades de pointes due to prolonged QT interval syndrome possibly associated with subarachnoid hemorrhage].	1999 Jun	10402818
A fugue-like state associated with diazepam use.	1999 Jun	10377715
Involvement of nitric oxide and nitric oxide synthase activity in anticonvulsive action.	1999 Mar 1	10357070
Anticonvulsants for soman-induced seizure activity.	1999 Mar-Apr	10087439
Effects of L-arginine on picrotoxin-induced increase in brain ammonia concentrations and convulsions in rats.	1999 Oct	10776465
Syndrome of inappropriate secretion of antidiuretic hormone complicating neonatal diazepam withdrawal.	2000 Apr	10830465
Acute adverse reaction to fentanyl in a 55 year old man.	2000 Aug	10960295
Effects of anticonvulsants on local anaesthetic-induced neurotoxicity in rats.	2000 Feb	10728915
Manic episode in an ifosfamide-treated patient.	2000 Jan-Feb	10766557
Mice lacking the long splice variant of the gamma 2 subunit of the GABA(A) receptor are more sensitive to benzodiazepines.	2000 Jun	10880692
[Prevention of postoperative nausea and vomiting in gynecologic surgery with 3 fixed doses of metoclopramide, droperidol or placebo].	2001 Feb	11257953
Extracellular serotonin is enhanced in the striatum, but not in the dorsal hippocampus or prefrontal cortex, in rats subjected to an operant conflict procedure.	2001 Feb	11256436
Diazepam in the treatment of GHB dependence.	2001 Feb	11157447
[Premedication in ambulatory surgery].	2001 Feb 12	11228790
Alterations in cerebral diazepam binding inhibitor expression in drug dependence: a possible biochemical alteration common to drug dependence.	2001 Feb 2	11233989
[Premedication for endoscopy].	2001 Feb 2	11225389
Chronic benzodiazepine administration facilitates the subsequent development of ethanol dependence.	2001 Feb 9	11164828
[Anesthesia for a patient with cardiac sarcoidosis].	2001 Jan	11211755
Development of differential tolerance to the sedative and anti-stress effects of benzodiazepines.	2001 Jan	11211563
Effect of diazepam and midazolam on the antinociceptive effect of morphine, metamizol and indomethacin in mice.	2001 Jan	11210678
Sedative properties of the decoction of the rhizome of Cyperus articulatus.	2001 Jan	11163936
Treatment of nonfebrile status epilepticus in Rochester, Minn, from 1965 through 1984.	2001 Jan	11155411
Diazepam increases the number of punished responses in a conflict-operant paradigm during late proestrus and estrus in the Wistar rat.	2001 Jan	11150896
Effects of antiepileptic drugs on rat platelet aggregation: ex vivo and in vitro study.	2001 Jan	11137387
Effects of melatonin, morphine and diazepam on formalin-induced nociception in mice.	2001 Jan 12	11213364
Intranasal midazolam for treating febrile seizures in children. Buccal midazolam for childhood seizures at home preferred to rectal diazepam.	2001 Jan 13	11203721
Simple and sensitive high-performance liquid chromatographic method for the determination of 1,5-benzodiazepine clobazam and its active metabolite N-desmethylclobazam in human serum and urine with application to 1,4-benzodiazepines analysis.	2001 Jan 5	11204222
Topical anesthesia for cataract surgery: a population-based perspective.	2001 Mar	11255059
Anxiogenic-like effects limit rewarding effects of cocaine in balb/cbyj mice.	2001 Mar	11166520
Modulation of GABA(A) receptors by benzodiazepines and barbiturates is autonomous of PKC activation.	2001 Mar	11166325
Evidence for a common binding cavity for three general anesthetics within the GABAA receptor.	2001 Mar 15	11245705
Systemic EMD 68843 injections reduce anxiety in the shock-probe, but not the plus-maze test.	2001 Mar 2	11239925

Patents

Sample Use Guides

In Vivo Use Guide

Tale 2-10 mg, 2 to 4 times daily.

Route of Administration: Oral

In Vitro Use Guide

Rat brain membranes were treated with diazepam (1-1000 nM) and the drug was shown to enhance the effects of iontophoretically applied GABA.

Name

Type

Language

DIAZEPAM HYDROCHLORIDE

Common Name

English

7-CHLORO-1,3-DIHYDRO-1-METHYL-5-PHENYL-2H-1,4-BENZODIAZEPIN-2-ONE HYDROCHLORIDE

Systematic Name

English

Classification Tree Code System Code

NCI_THESAURUS

C1012