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Chemical Compound Review

Dormalin     9-chloro-6-(2-fluorophenyl)- 2-(2,2,2...

Synonyms: Prosedar, Quazapam, quazepam, Cetrane, Quazium, ...
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Disease relevance of Quazepamum

  • All 20 reported daytime somnolence (drowsiness, lethargy, or sleepiness), and one quazepam-treated patient also had hypokinesia [1].
  • Eleven patients, six receiving quazepam and five receiving the placebo, had adverse experiences, including ataxia, which was observed in two quazepam-treated and one place-bo-treated patient [2].
  • 7-Chloro-5-(2-fluorophenyl)-1,3-dihydro-1-(2,2,2-trifluoroethyl)-2H-1,4- benzodiazepine-2-thione (quazepam, Sch 16134, Dormalin) was evaluated for evidence of systemic toxicity, carcinogenicity and reproductive toxicity in several laboratory animal species including the hamster [3].

Psychiatry related information on Quazepamum


High impact information on Quazepamum

  • Comparison of short and long half-life benzodiazepine hypnotics: triazolam and quazepam [4].
  • The kinetics of quazepam and 2-oxoquazepam can be best described by a two-compartment open model with first-order absorption/formation kinetics [9].
  • Maximum concentration and AUC of quazepam and 2-oxoquazepam and AUC of N-desalkyl-2-oxoquazepam were somewhat higher after nighttime dosing, most likely a result of decreased apparent volume of distribution of the central compartment after the nighttime dose (5.0 l/kg for nighttime dosing and 8.6 l/kg for morning dosing) [10].
  • Triazolam, zolpidem, quazepam, and placebo were administered orally in a double-blind, crossover design [11].
  • Binding of [3H]GABA was studied in frozen-thawed and repeatedly washed cortical membranes incubated in 20 mM KH2PO4 plus 50 mM KCl, pH 7.4, at 4 degrees C in the absence and presence of quazepam or its metabolites [12].

Chemical compound and disease context of Quazepamum


Biological context of Quazepamum


Anatomical context of Quazepamum

  • These results suggest that quazepam may act through facilitation of the EEG-synchronizing mechanisms localized in the lower brain stem which are involved in physiological EEG-synchronizing and sleep-inducing processes [16].
  • Excretion of quazepam into human breast milk [17].
  • It was found that quazepam and two of its metabolites have a higher affinity for benzodiazepine receptors in cerebellum than for those in hippocampus, indicating a preferential interaction of these compounds with BZ1-receptors [18].
  • Diazepam, quazepam and the beta-carboline, ZK 93423, enhanced the specific binding of [3H]GABA in a concentration-dependent manner (10(-7)-10(-5) M) in the cerebral cortex and hippocampus but not in the spinal cord and cerebellum [19].
  • Itraconazole inhibited the formation of OQ from quazepam, HOQ from OQ and DOQ from OQ in human liver microsomes with Ki values of 8.40, 0.08 and 0.39 microM, respectively [20].

Associations of Quazepamum with other chemical compounds


Gene context of Quazepamum

  • CYP3A4 is the enzyme predominantly responsible for all the metabolic pathways of quazepam [20].
  • In addition, CYP2C9 and CYP2C19 inhibitors failed to inhibit OQ formation from quazepam [20].
  • The present study thus suggests that CYP 3A4 is partly involved in the metabolism of quazepam [21].
  • Single oral dose pharmacokinetics of quazepam is influenced by CYP2C19 activity [26].
  • Blood samplings and evaluation of psychomotor function by the Digit Symbol Substitution Test and Stanford Sleepiness Scale were conducted up to 240 h after quazepam dosing [21].

Analytical, diagnostic and therapeutic context of Quazepamum

  • In a randomized two-way crossover design, each subject received one 15-mg quazepam tablet either at night just before sleep or in the morning after a night's sleep [10].
  • In the cerveau isolé, quazepam did not influence the typical synchronized EEG pattern [16].
  • Sleep laboratory studies on human volunteers have shown quazepam 15 mg to be an effective hypnotic dose, with the 30-mg dose being optimal [27].
  • In 18-day pregnant mice, concentrations of quazepam and its metabolites were measured either by gas-liquid chromatography or thin layer radiochromatography [28].
  • Plasma concentrations of quazepam and its active metabolite 2-oxoquazepam (OQ) were measured by HPLC [26].


  1. Quazepam in the short-term treatment of insomnia in outpatients. Aden, G.C., Thatcher, C. The Journal of clinical psychiatry. (1983) [Pubmed]
  2. Short-term treatment with quazepam of insomnia in geriatric patients. Martinez, H.T., Serna, C.T. Clinical therapeutics. (1982) [Pubmed]
  3. Preclinical safety evaluation of the benzodiazepine quazepam. Black, H.E., Szot, R.J., Arthaud, L.E., Massa, T., Mylecraine, L., Klein, M., Lake, R., Fabry, A., Kaminska, G.Z., Sinha, D.P. Arzneimittel-Forschung. (1987) [Pubmed]
  4. Comparison of short and long half-life benzodiazepine hypnotics: triazolam and quazepam. Kales, A., Bixler, E.O., Vela-Bueno, A., Soldatos, C.R., Niklaus, D.E., Manfredi, R.L. Clin. Pharmacol. Ther. (1986) [Pubmed]
  5. Drug interaction between St John's Wort and quazepam. Kawaguchi, A., Ohmori, M., Tsuruoka, S., Nishiki, K., Harada, K., Miyamori, I., Yano, R., Nakamura, T., Masada, M., Fujimura, A. British journal of clinical pharmacology. (2004) [Pubmed]
  6. Nocturnal traffic noise, sleep, and quality of awakening: neurophysiologic, psychometric, and receptor activity changes after quazepam. Saletu, B., Grünberger, J., Sieghart, W. Clinical neuropharmacology. (1985) [Pubmed]
  7. The effects of alprazolam, quazepam and diazepam on saccadic eye movements, parameters of psychomotor function and the EEG. Blom, M.W., Bartel, P.R., de Sommers, K., Van der Meyden, C.H., Becker, P.J. Fundamental & clinical pharmacology. (1990) [Pubmed]
  8. Relationships of brain and plasma levels of quazepam, flurazepam, and their metabolites with pharmacological activity in mice. Hilbert, J.M., Iorio, L., Moritzen, V., Barnett, A., Symchowicz, S., Zampaglione, N. Life Sci. (1986) [Pubmed]
  9. Multiple-dose quazepam kinetics. Chung, M., Hilbert, J.M., Gural, R.P., Radwanski, E., Symchowicz, S., Zampaglione, N. Clin. Pharmacol. Ther. (1984) [Pubmed]
  10. Effect of sleep on quazepam kinetics. Hilbert, J.M., Chung, M., Maier, G., Gural, R., Symchowicz, S., Zampaglione, N. Clin. Pharmacol. Ther. (1984) [Pubmed]
  11. Benzodiazepine-receptor ligands in humans: acute performance-impairing, subject-rated and observer-rated effects. Rush, C.R., Armstrong, D.L., Ali, J.A., Pazzaglia, P.J. Journal of clinical psychopharmacology. (1998) [Pubmed]
  12. Enhancement of gamma-aminobutyric acid binding by quazepam, a benzodiazepine derivative with preferential affinity for type I benzodiazepine receptors. Corda, M.G., Sanna, E., Concas, A., Giorgi, O., Ongini, E., Nurchi, V., Pintori, T., Crisponi, G., Biggio, G. J. Neurochem. (1986) [Pubmed]
  13. Hypnotic effects of low doses of quazepam in older insomniacs. Roth, T.G., Roehrs, T.A., Koshorek, G.L., Greenblatt, D.J., Rosenthal, L.D. Journal of clinical psychopharmacology. (1997) [Pubmed]
  14. Benzodiazepine receptors and their relationship to the treatment of epilepsy. Meldrum, B.S., Chapman, A.G. Epilepsia (1986) [Pubmed]
  15. Effect of dietary fat content in meals on pharmacokinetics of quazepam. Yasui-Furukori, N., Kondo, T., Takahata, T., Mihara, K., Ono, S., Kaneko, S., Tateishi, T. Journal of clinical pharmacology. (2002) [Pubmed]
  16. Effects of a new benzodiazepine hypnotic (quazepam--SCH 16134) on EEG synchronization and sleep-inducing mechanisms in cats. Ongini, E., Mariotti, M., Mancia, M. Neuropharmacology (1982) [Pubmed]
  17. Excretion of quazepam into human breast milk. Hilbert, J.M., Gural, R.P., Symchowicz, S., Zampaglione, N. Journal of clinical pharmacology. (1984) [Pubmed]
  18. Several new benzodiazepines selectively interact with a benzodiazepine receptor subtype. Sieghart, W. Neurosci. Lett. (1983) [Pubmed]
  19. Functional coupling of GABAA receptors and benzodiazepine recognition site subtypes in the spinal cord of the rat. Corda, M.G., Giorgi, O., Longoni, B., Ongini, E., Pesce, G., Cruciani, R., Biggio, G. Eur. J. Pharmacol. (1989) [Pubmed]
  20. In vitro metabolism of quazepam in human liver and intestine and assessment of drug interactions. Miura, M., Ohkubo, T. Xenobiotica (2004) [Pubmed]
  21. Effects of itraconazole on the plasma kinetics of quazepam and its two active metabolites after a single oral dose of the drug. Kato, K., Yasui-Furukori, N., Fukasawa, T., Aoshima, T., Suzuki, A., Kanno, M., Otani, K. Therapeutic drug monitoring. (2003) [Pubmed]
  22. Interaction study between fluvoxamine and quazepam. Kanda, H., Yasui-Furukori, N., Fukasawa, T., Aoshima, T., Suzuki, A., Otani, K. Journal of clinical pharmacology. (2003) [Pubmed]
  23. Differences in pharmacological profiles of a new generation of benzodiazepine and non-benzodiazepine hypnotics. Perrault, G., Morel, E., Sanger, D.J., Zivkovic, B. Eur. J. Pharmacol. (1990) [Pubmed]
  24. Differentiating the effects of three benzodiazepines on non-REM sleep EEG spectra. A neural-network pattern classification analysis. Gevins, A.S., Stone, R.K., Ragsdale, S.D. Neuropsychobiology (1988) [Pubmed]
  25. Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Wamsley, J.K., Golden, J.S., Yamamura, H.I., Barnett, A. Pharmacol. Biochem. Behav. (1985) [Pubmed]
  26. Single oral dose pharmacokinetics of quazepam is influenced by CYP2C19 activity. Fukasawa, T., Yasui-Furukori, N., Aoshima, T., Suzuki, A., Tateishi, T., Otani, K. Therapeutic drug monitoring. (2004) [Pubmed]
  27. Respiratory effects of quazepam and pentobarbital. Murray, A., Bellville, J.W., Comer, W., Danielson, L. Journal of clinical pharmacology. (1987) [Pubmed]
  28. Placental transfer of quazepam in mice. Hilbert, J.M., Ning, J., Symchowicz, S., Zampaglione, N. Drug Metab. Dispos. (1986) [Pubmed]
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