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Details

Stereochemistry ACHIRAL
Molecular Formula C16H15ClN2OS
Molecular Weight 318.821
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of CLOTIAZEPAM

SMILES

CCC1=CC2=C(S1)N(C)C(=O)CN=C2C3=CC=CC=C3Cl

InChI

InChIKey=CHBRHODLKOZEPZ-UHFFFAOYSA-N
InChI=1S/C16H15ClN2OS/c1-3-10-8-12-15(11-6-4-5-7-13(11)17)18-9-14(20)19(2)16(12)21-10/h4-8H,3,9H2,1-2H3

HIDE SMILES / InChI

Description

Clotiazepam is a compound of the benzodiazepine class. The drug was developed in Japan and approved for the treatment of insomnia, anxiety and before anesthesia. Clotiazepam was marketed worlwide under different names, however, currently it is available only in South America under the name Neuroval and presumably in Japan. Clotiazepam exerts its action by binding and activating GABA-A receptors.

CNS Activity

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
184.0 nM [EC50]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
DISTENSAN
Primary
NEUROVAL
Preventing
DISTENSAN

Cmax

ValueDoseCo-administeredAnalytePopulation
178.8 ng/mL
5 mg single, oral
CLOTIAZEPAM plasma
Homo sapiens
383 ng/mL
10 mg single, oral
CLOTIAZEPAM plasma
Homo sapiens
162 ng/mL
5 mg single, oral
CLOTIAZEPAM plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
528.2 ng × h/mL
5 mg single, oral
CLOTIAZEPAM plasma
Homo sapiens
1798 ng × h/mL
10 mg single, oral
CLOTIAZEPAM plasma
Homo sapiens
494 ng × h/mL
5 mg single, oral
CLOTIAZEPAM plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
4.62 h
5 mg single, oral
CLOTIAZEPAM plasma
Homo sapiens
5.3 h
10 mg single, oral
CLOTIAZEPAM plasma
Homo sapiens
5.4 h
5 mg single, oral
CLOTIAZEPAM plasma
Homo sapiens

Funbound

ValueDoseCo-administeredAnalytePopulation
1%
CLOTIAZEPAM plasma
Homo sapiens

Doses

AEs

PubMed

Patents

Sample Use Guides

In Vivo Use Guide
Treatment of anxiety: the usual dose in adults is 1 tablet (10 mg) 1 to 3 times a day for 8-12 weeks. Treatment of insomnia: the usual adult dose is 1 tablet (10 mg) to 2 tablets (20 mg) administered at night, before bedtime. The duration of treatment is usually 2-4 weeks.
Route of Administration: Oral
In Vitro Use Guide
Unknown