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    Quazepam

    ACTIVE PHARMA INGREDIENTS

    FINISHED DOSAGE FORMULATIONS

    RELATED EXCIPIENT COMPANIES

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    2D Structure
    Also known as: Doral, Prosedar, Quazium, Dormalin, Oniria, Selepam
    Molecular Formula
    C17H11ClF4N2S
    Molecular Weight
    386.8  g/mol
    InChI Key
    IKMPWMZBZSAONZ-UHFFFAOYSA-N
    FDA UNII
    JF8V0828ZI
    Quazepam is a synthetic benzodiazepine derivative with anxiolytic, sedative and hypnotic properties. Quazepam and its major metabolite 2-oxoquazepam potentiate gamma-aminobutyric acid (GABA) activity by binding to the benzodiazepine-1 recognition site (BZ-1) within the GABA-A receptor, located in the limbic, neocortical and mesencephalic reticular system. This increases the frequency of GABA-activated chloride channel opening events, allowing the flow of chloride ions into the neuron leading to membrane hyperpolarization and decreased neuronal excitability.
    Quazepam is a Benzodiazepine.
    1 2D Structure

    2D Structure

    2 Identification
    2.1 Computed Descriptors
    2.1.1 IUPAC Name
    7-chloro-5-(2-fluorophenyl)-1-(2,2,2-trifluoroethyl)-3H-1,4-benzodiazepine-2-thione
    2.1.2 InChI
    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
    2.1.3 InChI Key
    IKMPWMZBZSAONZ-UHFFFAOYSA-N
    2.1.4 Canonical SMILES
    C1C(=S)N(C2=C(C=C(C=C2)Cl)C(=N1)C3=CC=CC=C3F)CC(F)(F)F
    2.2 Other Identifiers
    2.2.1 UNII
    JF8V0828ZI
    2.3 Synonyms
    2.3.1 MeSH Synonyms

    1. Doral

    2. Quiedorm

    3. Sch 16134

    4. Sch-16134

    2.3.2 Depositor-Supplied Synonyms

    1. Doral

    2. Prosedar

    3. Quazium

    4. Dormalin

    5. Oniria

    6. Selepam

    7. 36735-22-5

    8. Sch 16134

    9. Quazepamum [inn-latin]

    10. Sch-16134

    11. Quazepam Civ

    12. 7-chloro-5-(2-fluorophenyl)-1-(2,2,2-trifluoroethyl)-3h-1,4-benzodiazepine-2-thione

    13. 7-chloro-5-(o-fluorophenyl)-1,3-dihydro-1-(2,2,2-trifluoroethyl)-2h-1,4-benzodiazepine-2-thione

    14. Nsc-309702

    15. Chebi:8694

    16. Jf8v0828zi

    17. 2h-1,4-benzodiazepine-2-thione, 7-chloro-5-(2-fluorophenyl)-1,3-dihydro-1-(2,2,2-trifluoroethyl)-

    18. Quazepamum

    19. Quazapam

    20. Cetrane

    21. Doral [sedative]

    22. 7-chloro-5-(2-fluorophenyl)-1-(2,2,2-trifluoroethyl)-2,3-dihydro-1h-1,4-benzodiazepine-2-thione

    23. Doral (tn)

    24. Einecs 253-179-4

    25. Nsc 309702

    26. Quazepam (jan/usp/inn)

    27. Sch-161

    28. Brn 0901084

    29. Unii-jf8v0828zi

    30. Dea No. 2881

    31. Quazepam [usan:usp:inn:ban]

    32. Quazepam [usan]

    33. Quazepam [inn]

    34. Quazepam [jan]

    35. Quazepam [mi]

    36. Quazepam [vandf]

    37. Quazepam Civ(200 Mg)

    38. Quazepam [mart.]

    39. Quazepam [who-dd]

    40. Schembl29504

    41. 5-24-04-00356 (beilstein Handbook Reference)

    42. Quazepam [orange Book]

    43. Quazepam Civ [usp-rs]

    44. Gtpl7288

    45. Chembl1200472

    46. Quazepam [usp Monograph]

    47. Dtxsid60190193

    48. Zinc538266

    49. Nsc309702

    50. Db01589

    51. C07336

    52. D00457

    53. 735q225

    54. Q3927403

    55. 2h-1, 7-chloro-5-(2-fluorophenyl)-1,3-dihydro-1-(2,2,2-trifluoroethyl)-

    56. 7-chloro-5-(o-fluorophenyl)-1,2,2-trifluoroethyl)-2h-1,4-benzodiazepine-2-thione

    2.4 Create Date
    2005-03-25
    3 Chemical and Physical Properties
    Molecular Weight 386.8 g/mol
    Molecular Formula C17H11ClF4N2S
    XLogP34
    Hydrogen Bond Donor Count0
    Hydrogen Bond Acceptor Count6
    Rotatable Bond Count2
    Exact Mass386.0267599 g/mol
    Monoisotopic Mass386.0267599 g/mol
    Topological Polar Surface Area47.7 Ų
    Heavy Atom Count25
    Formal Charge0
    Complexity539
    Isotope Atom Count0
    Defined Atom Stereocenter Count0
    Undefined Atom Stereocenter Count0
    Defined Bond Stereocenter Count0
    Undefined Bond Stereocenter Count0
    Covalently Bonded Unit Count1
    4 Drug and Medication Information
    4.1 Drug Information
    1 of 2  
    Drug NameDoral
    PubMed HealthQuazepam (By mouth)
    Drug ClassesHypnotic
    Drug LabelDORAL contains quazepam, a trifluoroethyl benzodiazepine hypnotic agent, having the chemical name 7-chloro-5- (o-fluoro-phenyl)-1,3-dihydro-1-(2,2,2-trifluoroethyl)-2H-1,4-benzodiazepine-2-thione and the following structural formula:Quazepam has the...
    Active IngredientQuazepam
    Dosage FormTablet
    RouteOral
    Strength15mg
    Market StatusPrescription
    CompanySciecure Pharma

    2 of 2  
    Drug NameDoral
    PubMed HealthQuazepam (By mouth)
    Drug ClassesHypnotic
    Drug LabelDORAL contains quazepam, a trifluoroethyl benzodiazepine hypnotic agent, having the chemical name 7-chloro-5- (o-fluoro-phenyl)-1,3-dihydro-1-(2,2,2-trifluoroethyl)-2H-1,4-benzodiazepine-2-thione and the following structural formula:Quazepam has the...
    Active IngredientQuazepam
    Dosage FormTablet
    RouteOral
    Strength15mg
    Market StatusPrescription
    CompanySciecure Pharma

    4.2 Drug Indication

    Used to treat insomnia.

    5 Pharmacology and Biochemistry
    5.1 Pharmacology

    Quazepam is a benzodiazepine derivative. The main pharmacological action of quazepam is the enhancement of the neurotransmitter GABA at the GABAA receptor.

    5.2 MeSH Pharmacological Classification

    Hypnotics and Sedatives

    Drugs used to induce drowsiness or sleep or to reduce psychological excitement or anxiety. (See all compounds classified as Hypnotics and Sedatives.)

    5.3 FDA Pharmacological Classification
    5.3.1 Active Moiety
    QUAZEPAM
    5.3.2 FDA UNII
    JF8V0828ZI
    5.3.3 Pharmacological Classes
    Benzodiazepines [CS]; Benzodiazepine [EPC]
    5.4 ATC Code

    N - Nervous system

    N05 - Psycholeptics

    N05C - Hypnotics and sedatives

    N05CD - Benzodiazepine derivatives

    N05CD10 - Quazepam

    5.5 Absorption, Distribution and Excretion

    Absorption

    Bioavailability is 29-35% following oral administration.

    5.6 Metabolism/Metabolites

    Hepatic.

    Quazepam has known human metabolites that include 2-oxoquazepam.

    S73 | METXBIODB | Metabolite Reaction Database from BioTransformer | DOI:10.5281/zenodo.4056560

    5.7 Biological Half-Life

    39 hours