Details
Stereochemistry | ACHIRAL |
Molecular Formula | C14H10BrN3O |
Molecular Weight | 316.153 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
BrC1=CC=C2NC(=O)CN=C(C3=CC=CC=N3)C2=C1
InChI
InChIKey=VMIYHDSEFNYJSL-UHFFFAOYSA-N
InChI=1S/C14H10BrN3O/c15-9-4-5-11-10(7-9)14(17-8-13(19)18-11)12-3-1-2-6-16-12/h1-7H,8H2,(H,18,19)
DescriptionCurator's Comment: description was created based on several sources, including
https://www.drugbank.ca/drugs/DB01558 | https://www.ncbi.nlm.nih.gov/pubmed/639854 | https://www.ncbi.nlm.nih.gov/pubmed/6124947 | https://www.ncbi.nlm.nih.gov/pubmed/2570451 | https://www.ncbi.nlm.nih.gov/pubmed/24241181
Curator's Comment: description was created based on several sources, including
https://www.drugbank.ca/drugs/DB01558 | https://www.ncbi.nlm.nih.gov/pubmed/639854 | https://www.ncbi.nlm.nih.gov/pubmed/6124947 | https://www.ncbi.nlm.nih.gov/pubmed/2570451 | https://www.ncbi.nlm.nih.gov/pubmed/24241181
Bromazepam (marketed under several brand names, including Lectopam, Lexotan, Lexilium, Lexaurin, Brazepam, Rekotnil, and Lexotanil)[1] is a benzodiazepine derivative drug, patented by Roche in 1963 and developed clinically in the 1970s. It is mainly an anti-anxiety agent with similar side effects to diazepam (Valium). In addition to being used to treat anxiety or panic states, bromazepam may be used as a premedicant prior to minor surgery. Bromazepam typically comes in doses of 3 mg and 6 mg tablets.[5] Bromazepam is contraindicated and should be used with caution in women who are pregnant, the elderly, patients with a history of alcohol or other substance abuse disorders and children. Prolonged use of bromazepam causes tolerance and may lead to both physical and psychological dependence on the drug, and as a result, it is a medication which is controlled by international law. Bromazepam binds to the GABA receptor GABAA, causing a conformational change and increasing the inhibitory effects of GABA. Bromazepam is a long-acting benzodiazepine and is lipophilic and metabolized hepatically via oxidative pathways.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL1907607 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24241181 |
45.0 nM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | LECTOPAM Approved UseUnknown |
PubMed
Title | Date | PubMed |
---|---|---|
The antihypertensive effect of lexotan (bromazepam)- a new benzodiazepine derivative. | 1977 Jan |
|
[Prescriptions and consumption of hypnotic and anxiolytic drugs in the South University Hospital of Marseille]. | 2001 Jan-Feb |
|
Last performance with VIAGRA: post-mortem identification of sildenafil and its metabolites in biological specimens including hair sample. | 2002 Mar 28 |
|
[Pharmacokinetics of bromazepam in 57 patients with acute drug intoxication]. | 2003 Jan |
|
The effect of itraconazole on the pharmacokinetics and pharmacodynamics of bromazepam in healthy volunteers. | 2003 Nov |
|
Spectrophotometric and fluorimetric determination of diazepam, bromazepam and clonazepam in pharmaceutical and urine samples. | 2004 Mar |
|
Effects of etifoxine on stress-induced hyperthermia, freezing behavior and colonic motor activation in rats. | 2004 Oct 15 |
|
Comparison of capillary electrophoresis and reversed-phase liquid chromatography methodologies for determination of diazepam in pharmaceutical tablets. | 2005 Feb 23 |
|
Analysis of the influence of bromazepam on cognitive performance through the visual evoked potential (P300). | 2005 Jun |
|
[Electroencephalography measures in motor skill learning and effects of bromazepam]. | 2005 Jun |
|
Neuromodulatory effects of caffeine and bromazepam on visual event-related potential (P300): a comparative study. | 2005 Jun |
|
Screening method for benzodiazepines and hypnotics in hair at pg/mg level by liquid chromatography-mass spectrometry/mass spectrometry. | 2005 Oct 15 |
|
[Procedural learning and anxiolytic effects: electroencephalographic, motor and attentional measures]. | 2006 Jun |
|
Influence of bromazepam on cortical interhemispheric coherence. | 2007 Mar |
|
Thiodicarb and methomyl tissue distribution in a fatal multiple compounds poisoning. | 2008 Mar |
Patents
Sample Use Guides
Adults: Depending upon severity of symptoms- 6 mg to 18 mg, in equally divided doses. Treatment may be initiated at a lower dose.
Elderly: Maximum of 3 mg in equally divided doses. Dose can be increased gradually as needed and tolerated.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/639854
500mkl of this P2-suspension (corresponding to 10mg original brain tissue) was preincubated for 5 min with Bromazepam. 25 mkl of 3H-diazepam working solution (to give a final concentration of 1.9 X 10^-9 M or approximately 14,000 cpm) was then added and the incubation continued for an additional 15 min at 37°C. The samples were then cooled in an ice bath for 30 min. IC50 values, i.e. values for 50% inhibition of specific 3H-diazepam binding, were assessed with at least 3 and up to 7 concentrations of the Bromazepam in duplicate or triplicate.
Name | Type | Language | ||
---|---|---|---|---|
|
Official Name | English | ||
|
Code | English | ||
|
Code | English | ||
|
Common Name | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Systematic Name | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Brand Name | English | ||
|
Systematic Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Code | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English |
Classification Tree | Code System | Code | ||
---|---|---|---|---|
|
DEA NO. |
2748
Created by
admin on Fri Dec 15 15:11:58 GMT 2023 , Edited by admin on Fri Dec 15 15:11:58 GMT 2023
|
||
|
WHO-ATC |
N05BA08
Created by
admin on Fri Dec 15 15:11:58 GMT 2023 , Edited by admin on Fri Dec 15 15:11:58 GMT 2023
|
||
|
NCI_THESAURUS |
C1012
Created by
admin on Fri Dec 15 15:11:58 GMT 2023 , Edited by admin on Fri Dec 15 15:11:58 GMT 2023
|
||
|
WHO-VATC |
QN05BA08
Created by
admin on Fri Dec 15 15:11:58 GMT 2023 , Edited by admin on Fri Dec 15 15:11:58 GMT 2023
|
Code System | Code | Type | Description | ||
---|---|---|---|---|---|
|
X015L14V0O
Created by
admin on Fri Dec 15 15:11:58 GMT 2023 , Edited by admin on Fri Dec 15 15:11:58 GMT 2023
|
PRIMARY | |||
|
m2662
Created by
admin on Fri Dec 15 15:11:58 GMT 2023 , Edited by admin on Fri Dec 15 15:11:58 GMT 2023
|
PRIMARY | Merck Index | ||
|
SUB05907MIG
Created by
admin on Fri Dec 15 15:11:58 GMT 2023 , Edited by admin on Fri Dec 15 15:11:58 GMT 2023
|
PRIMARY | |||
|
1812-30-2
Created by
admin on Fri Dec 15 15:11:58 GMT 2023 , Edited by admin on Fri Dec 15 15:11:58 GMT 2023
|
PRIMARY | |||
|
2441
Created by
admin on Fri Dec 15 15:11:58 GMT 2023 , Edited by admin on Fri Dec 15 15:11:58 GMT 2023
|
PRIMARY | |||
|
399
Created by
admin on Fri Dec 15 15:11:58 GMT 2023 , Edited by admin on Fri Dec 15 15:11:58 GMT 2023
|
PRIMARY | |||
|
140669
Created by
admin on Fri Dec 15 15:11:58 GMT 2023 , Edited by admin on Fri Dec 15 15:11:58 GMT 2023
|
PRIMARY | |||
|
1749
Created by
admin on Fri Dec 15 15:11:58 GMT 2023 , Edited by admin on Fri Dec 15 15:11:58 GMT 2023
|
PRIMARY | RxNorm | ||
|
217-322-4
Created by
admin on Fri Dec 15 15:11:58 GMT 2023 , Edited by admin on Fri Dec 15 15:11:58 GMT 2023
|
PRIMARY | |||
|
1076465
Created by
admin on Fri Dec 15 15:11:58 GMT 2023 , Edited by admin on Fri Dec 15 15:11:58 GMT 2023
|
PRIMARY | |||
|
BROMAZEPAM
Created by
admin on Fri Dec 15 15:11:58 GMT 2023 , Edited by admin on Fri Dec 15 15:11:58 GMT 2023
|
PRIMARY | |||
|
DTXSID40171081
Created by
admin on Fri Dec 15 15:11:58 GMT 2023 , Edited by admin on Fri Dec 15 15:11:58 GMT 2023
|
PRIMARY | |||
|
100000092554
Created by
admin on Fri Dec 15 15:11:58 GMT 2023 , Edited by admin on Fri Dec 15 15:11:58 GMT 2023
|
PRIMARY | |||
|
C87454
Created by
admin on Fri Dec 15 15:11:58 GMT 2023 , Edited by admin on Fri Dec 15 15:11:58 GMT 2023
|
PRIMARY | |||
|
2692
Created by
admin on Fri Dec 15 15:11:58 GMT 2023 , Edited by admin on Fri Dec 15 15:11:58 GMT 2023
|
PRIMARY | |||
|
CHEMBL277062
Created by
admin on Fri Dec 15 15:11:58 GMT 2023 , Edited by admin on Fri Dec 15 15:11:58 GMT 2023
|
PRIMARY | |||
|
D001960
Created by
admin on Fri Dec 15 15:11:58 GMT 2023 , Edited by admin on Fri Dec 15 15:11:58 GMT 2023
|
PRIMARY | |||
|
DB01558
Created by
admin on Fri Dec 15 15:11:58 GMT 2023 , Edited by admin on Fri Dec 15 15:11:58 GMT 2023
|
PRIMARY |
ACTIVE MOIETY
METABOLITE (PARENT)