II. Class

  1. Long acting Benzodiazepine

III. Indications

  1. Insomnia
    1. Short-term use only

IV. Dose

  1. Insomnia
    1. Start 7.5 orally at bedtime
    2. Maximum: 15 mg orally at bedtime (7.5 mg in the elderly)

V. Safety

  1. Pregnancy Category X (esp. first trimester)
  2. Avoid in Lactation
  3. Schedule IV Controlled Substance

VI. Pharmacokinetics

  1. Half-Life: 39 hours

VII. Metabolism

  1. Primarily metabolized by CYP3A4 to active metabolites
  2. Also metabolized by CYP2C9 and CYP2C19 to active metabolites

IX. References

  1. (2019) Med Lett Drugs Ther 61(1578): 121-6
  2. (2020) Presc Lett, Resource #361206, Appropriate Use of Benzodiazepines
  3. Olson (2020) Clinical Pharmacology, Medmaster Miami, p. 55
  4. Hamilton (2020) Tarascon Pocket Pharmacopoeia

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Ontology: quazepam (C0072828)

Definition (NCI) 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.
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C025130
SnomedCT 108391004, 371372004
LNC LP17870-4, MTHU024725
English 7-chloro-5-(2-fluorophenyl)-1,3-dihydro-1-(2,2,2-trifluoroethyl)-2H-1,4-benzodiazepine-2-thione, quazepam, 2H-1,4-Benzodiazepine-2-thione, 7-chloro-5-(2-fluorophenyl)-1,3-dihydro-1-(2,2,2-trifluoroethyl)-, quazepam (medication), quazepam [Chemical/Ingredient], QUAZEPAM, Quazepam (substance), Quazepam product (product), Quazepam product, Quazepam
Spanish quazepam, producto (producto), quazepam (producto), quazepam, quazepam, producto, quazepam (sustancia), cuacepam (sustancia), cuazepam, cuacepam

Ontology: Doral (C0720023)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C025130
English Doral, doral, Wallace brand of quazepam