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

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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	Positive Allosteric Modulator	101.0 nM [IC50]
Cytochrome P450 3A4	Substrate
Cytochrome P450 2C19	Substrate
Cytochrome P450 2C9	Substrate

Conditions

Condition	Modality	Targets	Highest Phase	Product
Insomnia	Primary		Approved	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

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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...

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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	substrate

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP2B6 CYP2C8 CYP2E1	CYP2C19

Drug as perpetrator

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Target	Modality	Activity	Clinical evidence
CYP2B6	inhibitor	likely	likely (co-administration study)
CYP2C8	inhibitor	no
CYP2E1	inhibitor	no

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Drug as victim

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Target	Modality	Activity	Clinical evidence
CYP3A4	substrate	major	no (co-administration study)
CYP2C19	substrate	minor
CYP2C9	substrate	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

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PubMed

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Title	Date	PubMed
Interaction study between fluvoxamine and quazepam.	2003 Dec	14615476
Effects of foods on the pharmacokinetics and clinical efficacy of quazepam.	2003 Oct	14653226
Insomnia in the elderly.	2007 Oct 1	19450355
Interactions between herbal medicines and prescribed drugs: an updated systematic review.	2009	19719333
Algorithms for the assessment and management of insomnia in primary care.	2009 Nov 3	19936140