QUAZEPAM

Details

Stereochemistry	ACHIRAL
Molecular Formula	C17H11ClF4N2S
Molecular Weight	386.794
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

FC1=C(C=CC=C1)C2=NCC(=S)N(CC(F)(F)F)C3=C2C=C(Cl)C=C3

InChI

InChIKey=IKMPWMZBZSAONZ-UHFFFAOYSA-N

InChI=1S/C17H11ClF4N2S/c18-10-5-6-14-12(7-10)16(11-3-1-2-4-13(11)19)23-8-15(25)24(14)9-17(20,21)22/h1-7H,8-9H2

HIDE SMILES / InChI

Molecular Formula	C17H11ClF4N2S
Molecular Weight	386.794
Charge	0
Count	MOL RATIO 1 MOL RATIO (average)

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description

Quazepam is indicated for the treatment of insomnia characterized by difficulty in falling asleep, frequent nocturnal awakenings, and/or early morning awakenings. Quazepam interact preferentially with the benzodiazepine-1 (BZ1) receptors. Most common adverse reactions (>1%): drowsiness, headache, fatigue, dizziness, dry mouth, dyspepsia. Downward of CAN depressant dose adjustment may be necessary due to additive effects.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
GABA-A receptor; anion channel 202	Positive Allosteric Modulator 179	101.0 nM [IC50]
Cytochrome P450 3A4 127	Substrate 661
Cytochrome P450 2C19 51	Substrate 661
Cytochrome P450 2C9 50	Substrate 661

Conditions

Condition	Modality	Targets	Highest Phase	Product
Insomnia 108	Primary		Approved 8,429	DORAL

C_max

Value	Dose	Co-administered	Analyte	Population
28 ng/mL	20 mg single, oral		QUAZEPAM plasma	Homo sapiens
81.2 ng/mL	20 mg single, oral		QUAZEPAM plasma	Homo sapiens

AUC

Value	Dose	Co-administered	Analyte	Population
291 ng × h/mL	20 mg single, oral		QUAZEPAM plasma	Homo sapiens
468 ng × h/mL	20 mg single, oral		QUAZEPAM plasma	Homo sapiens

T_1/2

Value	Dose	Co-administered	Analyte	Population
14.3 h	20 mg single, oral		QUAZEPAM plasma	Homo sapiens
15.5 h	20 mg single, oral		QUAZEPAM plasma	Homo sapiens

F_unbound

Value	Dose	Co-administered	Analyte	Population
5%			QUAZEPAM plasma	Homo sapiens

Doses

Show entries

Dose	Population	Adverse events
15 mg 1 times / day steady, oral Recommended	healthy, 19 - 39 years
30 mg 1 times / day steady, oral Highest studied dose	unhealthy, 22 -58 years
20 mg single, oral	healthy, 30.6 years
15 mg 1 times / day steady, oral Recommended	unhealthy, adult	Other AEs: Drowsiness, Headache...

Showing 1 to 4 of 4 entries

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AEs

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AE	Significance	Dose	Population
Dyspepsia	1%	15 mg 1 times / day steady, oral Recommended	unhealthy, adult
Drowsiness	12%	15 mg 1 times / day steady, oral Recommended	unhealthy, adult
Dizziness	2%	15 mg 1 times / day steady, oral Recommended	unhealthy, adult
Dry mouth	2%	15 mg 1 times / day steady, oral Recommended	unhealthy, adult
Fatigue	2%	15 mg 1 times / day steady, oral Recommended	unhealthy, adult

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Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1,737	substrate 1,037

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP2B6 810 CYP2C8 911 CYP2E1 882	CYP2C19 991

Drug as perpetrator

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Target	Modality	Activity	Clinical evidence
CYP2B6 1,001	inhibitor 3,277	likely	likely (co-administration study)
CYP2C8 965	inhibitor 3,277	no
CYP2E1 970	inhibitor 3,277	no

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Drug as victim

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Target	Modality	Activity	Clinical evidence
CYP3A4 1,737	substrate 3,367	major	no (co-administration study)
CYP2C19 991	substrate 3,367	minor
CYP2C9 1,037	substrate 3,367	minor

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Sourcing

Sourcing

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Vendor/Aggregator	ID	URL
ABI Chem	AC1L1JE0
Alfa Chemistry	36735-22-5	https://www.alfa-chemistry.com/quazepam-civ-200-mg-cas-36735-22-5-item-291703.htm
Ambinter	Amb13889656	http://www.ambinter.com/reference/13889656
Chemieliva Pharmaceutical Co., Ltd	PBCM0529451
ChemTik	CTK6H1725

Showing 1 to 5 of 18 entries

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PubMed

Show entries

Title	Date	PubMed
Feasibility of an every-other-night regimen in insomniac patients: subjective hypnotic effectiveness of quazepam, triazolam, and placebo.	1993 Jan	8428895
[Cytochrome P450 3A4 and Benzodiazepines].	2003	12875231
Safety and tolerability of oral antifungal agents in the treatment of fungal nail disease: a proven reality.	2005 Dec	18360572
Simultaneous determination of benzodiazepines and their metabolites in human serum by liquid chromatography-tandem mass spectrometry using a high-resolution octadecyl silica column compatible with aqueous compounds.	2009 Apr	18937304
Drugs associated with more suicidal ideations are also associated with more suicide attempts.	2009 Oct 2	19798416