Page last updated: 2024-11-04

sch 16134

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

quazepam: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID4999
CHEMBL ID1200472
CHEBI ID8694
SCHEMBL ID29504
MeSH IDM0084145

Synonyms (63)

Synonym
nsc-309702
sch 16134
7-chloro-5-(o-fluorophenyl)-1,2,2-trifluoroethyl)-2h-1,4-benzodiazepine-2-thione
2h-1, 7-chloro-5-(2-fluorophenyl)-1,3-dihydro-1-(2,2,2-trifluoroethyl)-
nsc309702
dormalin
prosedar
cetrane
sch-16134
sch-161
quazium
oniria
selepam
doral
2h-1,4-benzodiazepine-2-thione, 7-chloro-5-(2-fluorophenyl)-1,3-dihydro-1-(2,2,2-trifluoroethyl)-
einecs 253-179-4
nsc 309702
quazepamum
quazepamum [inn-latin]
7-chloro-5-(o-fluorophenyl)-1,3-dihydro-1-(2,2,2-trifluoroethyl)-2h-1,4-benzodiazepine-2-thione
brn 0901084
dea no. 2881
quazapam
C07336
quazepam
36735-22-5
DB01589
quazepam (jan/usp/inn)
D00457
doral (tn)
chebi:8694 ,
quazepam civ
CHEMBL1200472
7-chloro-5-(2-fluorophenyl)-1-(2,2,2-trifluoroethyl)-3h-1,4-benzodiazepine-2-thione
quazepam [usan:usp:inn:ban]
unii-jf8v0828zi
5-24-04-00356 (beilstein handbook reference)
doral [sedative]
jf8v0828zi ,
quazepam [who-dd]
quazepam [mart.]
quazepam civ [usp-rs]
quazepam [mi]
quazepam [jan]
quazepam [usan]
quazepam [inn]
quazepam [usp monograph]
quazepam [vandf]
quazepam [orange book]
7-chloro-5-(2-fluorophenyl)-1-(2,2,2-trifluoroethyl)-2,3-dihydro-1h-1,4-benzodiazepine-2-thione
gtpl7288
SCHEMBL29504
DTXSID60190193 ,
quazepam civ(200 mg)
Q3927403
doral (sedative)
n05cd10
dtxcid70112684
quazepam (usp monograph)
quazepam (usan:usp:inn:ban)
quazepam (mart.)
quazepamum (inn-latin)
quazepam civ (usp-rs)

Research Excerpts

Toxicity

ExcerptReferenceRelevance
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
0.32
" Yet, these agents can produce adverse effects such as tolerance to the hypnotic effect, rebound insomnia, next-day residual drowsiness, as well as amnesia and complex behaviours such as sleep-walking, sleep-eating and sleep-driving."( Reintroduction of quazepam: an update on comparative hypnotic and adverse effects.
Moniri, NH, 2019
)
0.51

Pharmacokinetics

ExcerptReferenceRelevance
"Quazepam and flurazepam share pharmacokinetic properties that result in prevention of early-morning insomnia, daytime rebound anxiety, and withdrawal rebound insomnia."( Quazepam and flurazepam: differential pharmacokinetic and pharmacodynamic characteristics.
Battista, D; Hilbert, JM, 1991
)
0.28
" Important differences exist among the drugs in the physicochemical properties of lipid solubility and protein binding and in pharmacokinetic properties of absorption, distribution, elimination, and clearance."( Benzodiazepine hypnotics: sorting the pharmacokinetic facts.
Greenblatt, DJ, 1991
)
0.28
"To assess pharmacodynamic and pharmacokinetic properties of acute, subchronic and withdrawn quazepam, a single-blind, longitudinal study was run in eight male, healthy young volunteers."( Longitudinal study on pharmacodynamics and pharmacokinetics of acute, steady-state and withdrawn quazepam.
Kauert, G; Klausnitzer, W; Schaffler, K; Wauschkuhn, CH, 1989
)
0.28
" The method was applied to sublingual pharmacokinetic studies of quazepam in healthy volunteers."( Liquid chromatographic assay and pharmacokinetics of quazepam and its metabolites following sublingual administration of quazepam.
Ellinwood, EH; Gupta, SK, 1988
)
0.27
" Therefore, the authors measured and compared pharmacokinetic parameters of quazepam taken in a fasted state and taken 30 minutes after consuming meals containing different amounts of dietary fat."( Effect of dietary fat content in meals on pharmacokinetics of quazepam.
Kaneko, S; Kondo, T; Mihara, K; Ono, S; Takahata, T; Tateishi, T; Yasui-Furukori, N, 2002
)
0.31
" In addition, differences were observed neither in other pharmacokinetic parameters or blood metabolite concentration under all of the study conditions, nor in clinical evaluation of subjective symptoms, complete blood count, or biochemical analyses between administrations 2 and 11 hrs after a meal."( Effects of foods on the pharmacokinetics and clinical efficacy of quazepam.
Danno, T; Igarashi, J; Ishida, E; Kajimoto, T; Kim, Y; Kishimoto, T; Kou, M; Morikawa, M; Nakamura, Y; Nakata, M; Ohsawa, H; Tokuyama, A; Yokoyama, T, 2003
)
0.32
" The pharmacokinetic parameters of OQ and pharmacodynamic parameters were not different between the 2 groups."( Single oral dose pharmacokinetics of quazepam is influenced by CYP2C19 activity.
Aoshima, T; Fukasawa, T; Otani, K; Suzuki, A; Tateishi, T; Yasui-Furukori, N, 2004
)
0.32

Bioavailability

ExcerptReferenceRelevance
" The methods were shown to be suitable for investigating the bioavailability and pharmacokinetics of quazepam at therapeutic doses."( Gas chromatographic determination of quazepam and two major metabolites in human plasma.
Hilbert, JM; Jimenez, A; Murphy, G; Ning, JM; Zampaglione, N, 1984
)
0.27
"Light food increased the bioavailability of quazepam and affected psychomotor performance."( Different effects of light food on pharmacokinetics and pharmacodynamics of three benzodiazepines, quazepam, nitrazepam and diazepam.
Fujita, T; Hasunuma, T; Kumagai, Y; Maeda, M; Majima, M; Otani, Y; Yamazaki, A; Yokota, S, 2007
)
0.34

Dosage Studied

ExcerptRelevanceReference
" Abrupt withdrawal of quazepam or diazepam after 52 weeks of dosing was associated at all dose levels with excitability, hyperactivity and convulsions."( Preclinical safety evaluation of the benzodiazepine quazepam.
Arthaud, LE; Black, HE; Fabry, A; Kaminska, GZ; Klein, M; Lake, R; Massa, T; Mylecraine, L; Sinha, DP; Szot, RJ, 1987
)
0.27
" In contrast, triazolam dosing did not significantly improve any of the major sleep efficiency parameters, and there was a rapid development of tolerance for the drug's slight initial effectiveness."( Comparison of short and long half-life benzodiazepine hypnotics: triazolam and quazepam.
Bixler, EO; Kales, A; Manfredi, RL; Niklaus, DE; Soldatos, CR; Vela-Bueno, A, 1986
)
0.27
" The resuls confirm that quazepam in a dosage of 15 mg/night is safe and that it is more effective than placebo in treating insomnia in older patients."( Short-term treatment with quazepam of insomnia in geriatric patients.
Martinez, HT; Serna, CT, 1982
)
0.26
" In hamsters, 66-77% of the radioactivity was excreted within 48 hr, and 97% within 7 days of dosing (57% found in urine and 40% in feces after iv; 54% in urine and 43% in feces after po dosing)."( The disposition and metabolism of a hypnotic benzodiazepine, quazepam, in the hamster and mouse.
Hilbert, J; Pramanik, B; Symchowicz, S; Zampaglione, N,
)
0.13
"Previous metabolic studies have established that two major metabolites, 2-oxoquazepam and N-desalkyl-2-oxoquazepam, are present in plasma after dosing with quazepam, a new benzodiazepine hypnotic."( Excretion of quazepam into human breast milk.
Gural, RP; Hilbert, JM; Symchowicz, S; Zampaglione, N, 1984
)
0.27
" The dosing of quazepam after a long period of ordinary fasting might reduce its efficacy because a 3 h interval between the timing of the evening meal and bedtime administration of hypnotics is regarded as normal in daily life."( Time effects of food intake on the pharmacokinetics and pharmacodynamics of quazepam.
Kaneko, S; Kondo, T; Mihara, K; Takahata, T; Tateishi, T; Yasui-Furukori, N, 2003
)
0.32
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
benzodiazepineA group of heterocyclic compounds with a core structure containing a benzene ring fused to a diazepine ring.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Bioassays (28)

Assay IDTitleYearJournalArticle
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID539464Solubility of the compound in 0.1 M phosphate buffer at 600 uM at pH 7.4 after 24 hrs by LC/MS/MS analysis2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Experimental solubility profiling of marketed CNS drugs, exploring solubility limit of CNS discovery candidate.
AID588214FDA HLAED, liver enzyme composite activity2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID588215FDA HLAED, alkaline phosphatase increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (106)

TimeframeStudies, This Drug (%)All Drugs %
pre-199062 (58.49)18.7374
1990's24 (22.64)18.2507
2000's14 (13.21)29.6817
2010's6 (5.66)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 9.05

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index9.05 (24.57)
Research Supply Index5.04 (2.92)
Research Growth Index4.10 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (9.05)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials41 (36.28%)5.53%
Reviews13 (11.50%)6.00%
Case Studies1 (0.88%)4.05%
Observational0 (0.00%)0.25%
Other58 (51.33%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]