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Details

Stereochemistry RACEMIC
Molecular Formula C16H11ClN2O3
Molecular Weight 314.723
Optical Activity ( + / - )
Defined Stereocenters 0 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of CLORAZEPIC ACID

SMILES

OC(=O)C1N=C(C2=CC=CC=C2)C3=CC(Cl)=CC=C3NC1=O

InChI

InChIKey=XDDJGVMJFWAHJX-UHFFFAOYSA-N
InChI=1S/C16H11ClN2O3/c17-10-6-7-12-11(8-10)13(9-4-2-1-3-5-9)19-14(16(21)22)15(20)18-12/h1-8,14H,(H,18,20)(H,21,22)

HIDE SMILES / InChI

Molecular Formula C16H11ClN2O3
Molecular Weight 314.723
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry RACEMIC
Additional Stereochemistry No
Defined Stereocenters 0 / 1
E/Z Centers 0
Optical Activity ( + / - )

Description

Clorazepate is a water-soluble benzodiazepine derivative effective in the treatment of anxiety. It has also muscle relaxant and anticonvulsant actions. Studies in healthy men have shown that clorazepate dipotassium has depressant effects on the central nervous system. clorazepate is a prodrug since orally administered it is rapidly decarboxylated to form nordiazepam, there is essentially no circulating parent drug. Nordiazepam positively modulates GABAA receptors to produce anxiolytic and anticonvulsant effects.

CNS Activity

Approval Year

Targets

Primary TargetPharmacologyConditionPotency

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
TRANXENE
Palliative
TRANXENE

Cmax

ValueDoseCo-administeredAnalytePopulation
413 μg/L
20 mg single, oral
NORDAZEPAM plasma
Homo sapiens
245 μg/L
20 mg single, oral
NORDAZEPAM plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
54.7 h
20 mg single, oral
NORDAZEPAM plasma
Homo sapiens
29.8 h
20 mg single, oral
NORDAZEPAM plasma
Homo sapiens
2.42 h
20 mg single, intravenous
CLORAZEPIC ACID plasma
Homo sapiens
46 h
20 mg single, intravenous
NORDAZEPAM plasma
Homo sapiens
2.291 h
20 mg single, intramuscular
CLORAZEPIC ACID plasma
Homo sapiens
45.1 h
20 mg single, intramuscular
NORDAZEPAM plasma
Homo sapiens

Doses

Overview

CYP3A4CYP2C9CYP2D6hERG

OverviewOther

Other InhibitorOther SubstrateOther Inducer

Drug as victim

Sourcing

PubMed

Patents

Sample Use Guides

In Vivo Use Guide
For the symptomatic relief of anxiety: TRANXENE T-TAB tablets are administered orally in divided doses. The usual daily dose is 30 mg. The dose should be adjusted gradually within the range of 15 to 60 mg daily in accordance with the response of the patient. In elderly or debilitated patients it is advisable to initiate treatment at a daily dose of 7.5 to 15 mg. TRANXENE tablets may also be administered in a single dose daily at bedtime; the recommended initial dose is 15 mg. After the initial dose, the response of the patient may require adjustment of subsequent dosage. Lower doses may be indicated in the elderly patient. Drowsiness may occur at the initiation of treatment and with dosage increment. As an Adjunct to Antiepileptic Drugs: In order to minimize drowsiness, the recommended initial dosages and dosage increments should not be exceeded. Adults: The maximum recommended initial dose in patients over 12 years old is 7.5 mg three times a day. Dosage should be increased by no more than 7.5 mg every week and should not exceed 90 mg/day. Children (9-12 years): The maximum recommended initial dose is 7.5 mg two times a day. Dosage should be increased by no more than 7.5 mg every week and should not exceed 60 mg/day
Route of Administration: Oral
In Vitro Use Guide
Unknown
Substance Class Chemical
Record UNII
D51WO0G0L4
Record Status Validated (UNII)
Record Version