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Chemical Compound Review

Dalmadorm     9-chloro-2-(2- diethylaminoethyl)-6-(2...

Synonyms: Noctosom, Dalmane, Felison, Felmane, Insumin, ...
 
 
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Disease relevance of Dalmadorm

  • In five patients who had been on chronic maintenance haemodialysis for more than eight months a syndrome involving altered consciousness, asterixis, and abnormal electroencephalogram developed after they had been given flurazepam and diazepam [1].
  • Flurazepam was associated with significant increases in the number of sleep events (p = 0.01), episodes of apnea (p less than 0.01), and total duration of apnea (p less than 0.01) [2].
  • Effect of flurazepam on sleep-disordered breathing and nocturnal oxygen desaturation in asymptomatic subjects [2].
  • Toxicity of high-dose flurazepam in the elderly [3].
  • During hypoxic hypercapnia, the PCO2 at arousal from sleep was significantly lower than during hyperoxic hypercapnia, but the level of ventilation at arousal during hypercapnia was similar in the control condition and after flurazepam [4].
 

Psychiatry related information on Dalmadorm

 

High impact information on Dalmadorm

 

Chemical compound and disease context of Dalmadorm

 

Biological context of Dalmadorm

  • Furthermore, alpha1E122C, alpha1L127C, and alpha1R131C changed accessibility in response to flurazepam, providing structural evidence that residues in and near the GABA binding site move in response to benzodiazepine modulation [16].
  • Dose-related effects of triazolam and flurazepam on a circadian rhythm insomnia [17].
  • Kinetics and clinical effects of flurazepam in young and elderly noninsomniacs [18].
  • Flurazepam also produced a moderate decrease in REM sleep and marked decrease in eye movement density and stage 4 sleep with short- and intermediate-term use [19].
  • Analysis of heart rate (HR) data collected in sleep laboratory studies on the effects of 0.5 mg of triazolam (Halcion) and 30 mg of flurazepam (Dalmane) demonstrated that both benzodiazepine hypnotics produced a significant HR elevation that was present for up to 4 h during sleep [20].
 

Anatomical context of Dalmadorm

 

Associations of Dalmadorm with other chemical compounds

 

Gene context of Dalmadorm

 

Analytical, diagnostic and therapeutic context of Dalmadorm

  • In general, the distortions in sleep EEG produced by flurazepam qualitatively resemble, but are quantitatively greater than, those produced by barbiturates in equivalent hypnotic doses [31].
  • Triazolam, 0.4 and 0.8 mg, flurazepam, 15 and 30 mg, and placebo were compared in a double-blind, randomized 5-night crossover study in 25 inpatient insomniacs [32].
  • Thus, "first-pass" metabolism of flurazepam following oral administration occurs in the small bowel mucosa of man as well as in the liver [22].
  • On one phase of a cognitive task, the barbiturate and flurazepam groups made more errors than the control groups [33].
  • One hundred seven chronic insomniacs (41 men, 66 women; mean age, 37.9 years) with a history of use of benzodiazepines were recruited for a multicenter study testing the relative efficacy of flurazepam 15 mg or 30 mg, midazolam 15 mg, or placebo during a 14-day treatment period [34].

References

  1. Drug-induced encephalopathy in patients on maintenance haemodialysis. Taclob, L., Needle, M. Lancet (1976) [Pubmed]
  2. Effect of flurazepam on sleep-disordered breathing and nocturnal oxygen desaturation in asymptomatic subjects. Dolly, F.R., Block, A.J. Am. J. Med. (1982) [Pubmed]
  3. Toxicity of high-dose flurazepam in the elderly. Greenblatt, D.J., Allen, M.D., Shader, R.I. Clin. Pharmacol. Ther. (1977) [Pubmed]
  4. Effect of hypoxia on ventilatory and arousal responses to CO2 during NREM sleep with and without flurazepam in young adults. Gothe, B., Cherniack, N.S., Williams, L. Sleep. (1986) [Pubmed]
  5. Flurazepam effects on slow-wave sleep: stage 4 suppressed but number of delta waves constant. Feinberg, I., Fein, G., Walker, J.M., Price, L.J., Floyd, T.C., March, J.D. Science (1977) [Pubmed]
  6. Rebound insomnia. A potential hazard following withdrawal of certain benzodiazepines. Kales, A., Scharf, M.B., Kales, J.D., Soldatos, C.R. JAMA (1979) [Pubmed]
  7. Flurazepam hydrochloride, a benzodiazepine hypnotic. Greenblatt, D.J., Shader, R.I., Koch-Weser, J. Ann. Intern. Med. (1975) [Pubmed]
  8. Withdrawal symptoms after long-term treatment with flurazepam. Pearlman, T. The American journal of psychiatry. (1984) [Pubmed]
  9. Inosine may be an endogenous ligand for benzodiazepine receptors on cultured spinal neurons. MacDonald, J.F., Barker, J.L., Paul, S.M., Marangos, P.J., Skolnick, P. Science (1979) [Pubmed]
  10. Pharmacokinetic determinants of dynamic differences among three benzodiazepine hypnotics. Flurazepam, temazepam, and triazolam. Greenblatt, D.J., Harmatz, J.S., Engelhardt, N., Shader, R.I. Arch. Gen. Psychiatry (1989) [Pubmed]
  11. Silent GABAA synapses during flurazepam withdrawal are region-specific in the hippocampal formation. Poisbeau, P., Williams, S.R., Mody, I. J. Neurosci. (1997) [Pubmed]
  12. Nighttime and daytime efficacy of flurazepam and oxazepam in chronic insomnia. Bliwise, D., Seidel, W., Greenblatt, D.J., Dement, W. The American journal of psychiatry. (1984) [Pubmed]
  13. Quazepam. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in insomnia. Ankier, S.I., Goa, K.L. Drugs (1988) [Pubmed]
  14. Flunitrazepam: a review of its pharmacological properties and therapeutic use. Mattila, M.A., Larni, H.M. Drugs (1980) [Pubmed]
  15. Comparative hypnotic effects of flurazepam, triazolam, and placebo: a long-term simultaneous nighttime and daytime study. Mitler, M.M., Seidel, W.F., van den Hoed, J., Greenblatt, D.J., Dement, W.C. Journal of clinical psychopharmacology. (1984) [Pubmed]
  16. Agonist-, antagonist-, and benzodiazepine-induced structural changes in the alpha1 Met113-Leu132 region of the GABAA receptor. Kloda, J.H., Czajkowski, C. Mol. Pharmacol. (2007) [Pubmed]
  17. Dose-related effects of triazolam and flurazepam on a circadian rhythm insomnia. Seidel, W.F., Cohen, S.A., Bliwise, N.G., Roth, T., Dement, W.C. Clin. Pharmacol. Ther. (1986) [Pubmed]
  18. Kinetics and clinical effects of flurazepam in young and elderly noninsomniacs. Greenblatt, D.J., Divoll, M., Harmatz, J.S., MacLaughlin, D.S., Shader, R.I. Clin. Pharmacol. Ther. (1981) [Pubmed]
  19. Effectiveness of hypnotic drugs with prolonged use: flurazepam and pentobarbital. Kales, A., Kales, J.D., Bixler, E.O., Scharf, M.B. Clin. Pharmacol. Ther. (1975) [Pubmed]
  20. Benzodiazepine hypnotics increase heart rate during sleep. Muzet, A., Johnson, L.C., Spinweber, C.L. Sleep. (1982) [Pubmed]
  21. Reduced expression of gamma-aminobutyric acid type A/benzodiazepine receptor gamma 2 and alpha 5 subunit mRNAs in brain regions of flurazepam-treated rats. Zhao, T.J., Chiu, T.H., Rosenberg, H.C. Mol. Pharmacol. (1994) [Pubmed]
  22. Metabolism of flurazepam by the small intestine. Mahon, W.A., Inaba, T., Stone, R.M. Clin. Pharmacol. Ther. (1977) [Pubmed]
  23. Chronic benzodiazepine agonist treatment produces functional uncoupling of the gamma-aminobutyric acid-benzodiazepine receptor ionophore complex in cortical neurons. Hu, X.J., Ticku, M.K. Mol. Pharmacol. (1994) [Pubmed]
  24. Triazolam: a review of its pharmacological properties and therapeutic efficacy in patients with insomnia. Pakes, G.E., Brogden, R.N., Heel, R.C., Speight, T.M., Avery, G.S. Drugs (1981) [Pubmed]
  25. Objective measurements of daytime sleepiness and performance comparing quazepam with flurazepam in two adult populations using the Multiple Sleep Latency Test. Dement, W.C. The Journal of clinical psychiatry. (1991) [Pubmed]
  26. Loprazolam. A preliminary review of its pharmacodynamic and pharmacokinetic properties and therapeutic efficacy in insomnia. Clark, B.G., Jue, S.G., Dawson, G.W., Ward, A. Drugs (1986) [Pubmed]
  27. Modulation of delta activity by hypnotics in middle-aged subjects: studies with a benzodiazepine (flurazepam) and a cyclopyrrolone (zopiclone). Wright, N.A., Belyavin, A., Borland, R.G., Nicholson, A.N. Sleep. (1986) [Pubmed]
  28. Deletion of the alpha1 or beta2 subunit of GABAA receptors reduces actions of alcohol and other drugs. Blednov, Y.A., Jung, S., Alva, H., Wallace, D., Rosahl, T., Whiting, P.J., Harris, R.A. J. Pharmacol. Exp. Ther. (2003) [Pubmed]
  29. Benzodiazepine/cholecystokinin interactions at functional CCK receptors in rat brain. Boden, P.R., Woodruff, G.N. Br. J. Pharmacol. (1994) [Pubmed]
  30. Chronic benzodiazepine administration alters hippocampal CA1 neuron excitability: NMDA receptor function and expression(1). Van Sickle, B.J., Cox, A.S., Schak, K., Greenfield, L.J., Tietz, E.I. Neuropharmacology (2002) [Pubmed]
  31. Flurazepam effects on sleep EEG. Visual, computer, and cycle analysis. Feinberg, I., Fein, G., Walker, J.M., Price, L.J., Floyd, T.C., March, J.D. Arch. Gen. Psychiatry (1979) [Pubmed]
  32. Comparison of the hypnotic activity of triazolam, flurazepam hydrochloride, and placebo. Sunshine, A. Clin. Pharmacol. Ther. (1975) [Pubmed]
  33. Residual effects of temazepam and other hypnotic compounds on cognitive function. Pishkin, V., Lovallo, W.R., Fishkin, S.M., Shurley, J.T. The Journal of clinical psychiatry. (1980) [Pubmed]
  34. Characteristics of chronic insomniacs examined in a multicenter 14-day study of flurazepam and midazolam. Roth, T., Roehrs, T., Linnoila, M., Judd, L.L. Journal of clinical psychopharmacology. (1990) [Pubmed]
 
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