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Chemical Compound Review

zolpidem     N,N-dimethyl-2-[3-methyl-8- (4...

Synonyms: Sanval, Zolpidemum, Lorex, CHEMBL911, Zolpidem (INN), ...
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Disease relevance of zolpidem


Psychiatry related information on zolpidem


High impact information on zolpidem


Chemical compound and disease context of zolpidem


Biological context of zolpidem

  • In this study, the effects of rifampin on the pharmacokinetics and pharmacodynamics of zolpidem were studied [18].
  • RESULTS: Kinetics of zaleplon and zolpidem were not significantly related to dose [19].
  • All granule cell GABAR currents were uniformly sensitive to Zn2+ (IC50 = 29 microM), diazepam (EC50 = 158 nM), zolpidem (EC50 = 75 nM), and dimethoxyl-4-ethyl-beta-carboline-3-carboxylate (IC50 = 60 nM) [20].
  • Hence, alpha 5 beta 3 gamma 3 recpetors are not a major fraction of the native zolpidem-insensitive receptors, even though their genes are colocalized on mouse chromosome 7 and on human chromosome 15 [21].
  • Short- and long-term memory (paired words associate and pictures test), psychomotor performances (critical flicker fusion frequency, choice reaction time, digit symbol substitution test), and postural sway were evaluated before and 1.5, 4, 6, and 8 h after the administration of a single dose of zolpidem (10 mg), triazolam (0.25 mg), and placebo [9].

Anatomical context of zolpidem


Associations of zolpidem with other chemical compounds

  • However, zaleplon had more rapid elimination (apparent elimination half-life [t1/2] of 1 hour) and higher apparent oral clearance (approximately 4300 mL/min) than zolpidem (t1/2, 2.0 to 2.2 hours; apparent oral clearance, 340 to 380 mL/min) [19].
  • The imidazopyridine zolpidem (Ambien) is one of the most commonly prescribed sleep aids in the United States (Rush, 1998) [13].
  • In our pursuit to identify selective ligands for Bz/GABA(A) receptor subtypes, a novel pyrazolo[1,5-a]pyrimidine derivative (4), the azaisostere of zolpidem, was synthesized and evaluated in vitro on bovine brain homogenate and on recombinant benzodiazepine receptors (alphaxbeta2/3gamma2, x = 1-3, 5) expressed in HEK293 cells [25].
  • Expression of specific GABAA, receptor subunit assemblies in Xenopus oocytes was utilized to evaluate functionally both the efficacy and potency of the positive modulation of GABA-evoked Cl- currents by 7f and 7m in comparison with Zolpidem [26].
  • Placebo, zolpidem (5, 10, and 20 mg/70 kg), triazolam (0.125, 0.25, and 0.50 mg/70 kg), and temazepam (15, 30, and 60 mg/70 kg) were administered orally in a randomized, double-blind, cross-over design [27].

Gene context of zolpidem

  • We conclude that the formation of alcohol derivatives of zolpidem is rate-limiting and principally mediated by CYP3A4 [28].
  • CONCLUSIONS: The incomplete dependence of zolpidem clearance on CYP3A activity has clinical implications for susceptibility to metabolic inhibition [29].
  • Microsomes containing human cytochromes CYP1A2, 2C9, 2C19, 2D6, and 3 A4 expressed by cDNA-transfected human lymphoblastoid cells mediated zolpidem metabolism in vitro [29].
  • The distinct affinities of recombinant receptors for CI 218,872 suggested that the alpha 5 beta 3 gamma 2 receptor is the dominant zolpidem-insensitive GABAA receptor in the brain [21].
  • Here, we have tested the effects of zolpidem on the hippocampus of gamma2 subunit (gamma2F77I) point mutant mice [30].

Analytical, diagnostic and therapeutic context of zolpidem


  1. Zolpidem in progressive supranuclear palsy. Daniele, A., Moro, E., Bentivoglio, A.R. N. Engl. J. Med. (1999) [Pubmed]
  2. Zolpidem in Parkinson's disease. Lavoisy, J., Marsac, J. Lancet (1997) [Pubmed]
  3. Zolpidem-induced macropsia in anorexic woman. Iruela, L., Ibañez-Rojo, V., Baca, E. Lancet (1993) [Pubmed]
  4. Effect of zolpidem on the efficacy of continuous positive airway pressure as treatment for obstructive sleep apnea. Berry, R.B., Patel, P.B. Sleep. (2006) [Pubmed]
  5. Benzodiazepines and zolpidem for chronic insomnia: a meta-analysis of treatment efficacy. Nowell, P.D., Mazumdar, S., Buysse, D.J., Dew, M.A., Reynolds, C.F., Kupfer, D.J. JAMA (1997) [Pubmed]
  6. Test for catatonia with zolpidem. Thomas, P., Rascle, C., Mastain, B., Maron, M., Vaiva, G. Lancet (1997) [Pubmed]
  7. Imidazenil and diazepam increase locomotor activity in mice exposed to protracted social isolation. Pinna, G., Agis-Balboa, R.C., Zhubi, A., Matsumoto, K., Grayson, D.R., Costa, E., Guidotti, A. Proc. Natl. Acad. Sci. U.S.A. (2006) [Pubmed]
  8. Effect of zolpidem on sleep and ventilatory patterns at simulated altitude of 4,000 meters. Beaumont, M., Goldenberg, F., Lejeune, D., Marotte, H., Harf, A., Lofaso, F. Am. J. Respir. Crit. Care Med. (1996) [Pubmed]
  9. Comparison of the effects of zolpidem and triazolam on memory functions, psychomotor performances, and postural sway in healthy subjects. Berlin, I., Warot, D., Hergueta, T., Molinier, P., Bagot, C., Puech, A.J. Journal of clinical psychopharmacology. (1993) [Pubmed]
  10. Altered kinetics and benzodiazepine sensitivity of a GABAA receptor subunit mutation [gamma 2(R43Q)] found in human epilepsy. Bowser, D.N., Wagner, D.A., Czajkowski, C., Cromer, B.A., Parker, M.W., Wallace, R.H., Harkin, L.A., Mulley, J.C., Marini, C., Berkovic, S.F., Williams, D.A., Jones, M.V., Petrou, S. Proc. Natl. Acad. Sci. U.S.A. (2002) [Pubmed]
  11. A point mutation in the gamma2 subunit of gamma-aminobutyric acid type A receptors results in altered benzodiazepine binding site specificity. Buhr, A., Sigel, E. Proc. Natl. Acad. Sci. U.S.A. (1997) [Pubmed]
  12. Hemoglobin metabolites mimic benzodiazepines and are possible mediators of hepatic encephalopathy. Ruscito, B.J., Harrison, N.L. Blood (2003) [Pubmed]
  13. Structural Determinants for High-Affinity Zolpidem Binding to GABA-A receptors. Sancar, F., Ericksen, S.S., Kucken, A.M., Teiss??re, J.A., Czajkowski, C. Mol. Pharmacol. (2007) [Pubmed]
  14. A case of parenteral zolpidem dependence with opioid-like withdrawal symptoms. Kao, C.L., Huang, S.C., Yang, Y.J., Tsai, S.J. The Journal of clinical psychiatry. (2004) [Pubmed]
  15. Zolpidem, triazolam, and diazepam decrease distress vocalizations in mouse pups: differential antagonism by flumazenil and beta-Carboline-3-carboxylate-t-butyl ester (beta-CCt). Rowlett, J.K., Tornatzky, W., Cook, J.M., Ma, C., Miczek, K.A. J. Pharmacol. Exp. Ther. (2001) [Pubmed]
  16. Next-day residual effects of hypnotics in DSM-IV primary insomnia: a driving simulator study with simultaneous electroencephalogram monitoring. Staner, L., Ertlé, S., Boeijinga, P., Rinaudo, G., Arnal, M.A., Muzet, A., Luthringer, R. Psychopharmacology (Berl.) (2005) [Pubmed]
  17. Daytime wakefulness following a bedtime oral dose of zolpidem 20 mg, flunitrazepam 2 mg and placebo. Bensimon, G., Foret, J., Warot, D., Lacomblez, L., Thiercelin, J.F., Simon, P. British journal of clinical pharmacology. (1990) [Pubmed]
  18. Rifampin reduces plasma concentrations and effects of zolpidem. Villikka, K., Kivistö, K.T., Luurila, H., Neuvonen, P.J. Clin. Pharmacol. Ther. (1997) [Pubmed]
  19. Comparative kinetics and dynamics of zaleplon, zolpidem, and placebo. Greenblatt, D.J., Harmatz, J.S., von Moltke, L.L., Ehrenberg, B.L., Harrel, L., Corbett, K., Counihan, M., Graf, J.A., Darwish, M., Mertzanis, P., Martin, P.T., Cevallos, W.H., Shader, R.I. Clin. Pharmacol. Ther. (1998) [Pubmed]
  20. Pharmacological properties of gamma-aminobutyric acidA receptors from acutely dissociated rat dentate granule cells. Kapur, J., Macdonald, R.L. Mol. Pharmacol. (1996) [Pubmed]
  21. Impact of beta and gamma variants on ligand-binding properties of gamma-aminobutyric acid type A receptors. Lüddens, H., Seeburg, P.H., Korpi, E.R. Mol. Pharmacol. (1994) [Pubmed]
  22. Prevalence between different alpha subunits performing the benzodiazepine binding sites in native heterologous GABA(A) receptors containing the alpha2 subunit. del Río, J.C., Araujo, F., Ramos, B., Ruano, D., Vitorica, J. J. Neurochem. (2001) [Pubmed]
  23. Heterogeneity in the allosteric interaction between the gamma-aminobutyric acid (GABA) binding site and three different benzodiazepine binding sites of the GABAA/benzodiazepine receptor complex in the rat nervous system. Ruano, D., Vizuete, M., Cano, J., Machado, A., Vitorica, J. J. Neurochem. (1992) [Pubmed]
  24. Maternal behavior regulates benzodiazepine/GABAA receptor subunit expression in brain regions associated with fear in BALB/c and C57BL/6 mice. Caldji, C., Diorio, J., Anisman, H., Meaney, M.J. Neuropsychopharmacology (2004) [Pubmed]
  25. A novel selective GABA(A) alpha1 receptor agonist displaying sedative and anxiolytic-like properties in rodents. Selleri, S., Bruni, F., Costagli, C., Costanzo, A., Guerrini, G., Ciciani, G., Gratteri, P., Besnard, F., Costa, B., Montali, M., Martini, C., Fohlin, J., De Siena, G., Aiello, P.M. J. Med. Chem. (2005) [Pubmed]
  26. Synthesis and binding affinity of 2-phenylimidazo[1,2-alpha]pyridine derivatives for both central and peripheral benzodiazepine receptors. A new series of high-affinity and selective ligands for the peripheral type. Trapani, G., Franco, M., Ricciardi, L., Latrofa, A., Genchi, G., Sanna, E., Tuveri, F., Cagetti, E., Biggio, G., Liso, G. J. Med. Chem. (1997) [Pubmed]
  27. Zolpidem, triazolam, and temazepam: behavioral and subject-rated effects in normal volunteers. Rush, C.R., Griffiths, R.R. Journal of clinical psychopharmacology. (1996) [Pubmed]
  28. Oxidative metabolism of zolpidem by human liver cytochrome P450S. Pichard, L., Gillet, G., Bonfils, C., Domergue, J., Thénot, J.P., Maurel, P. Drug Metab. Dispos. (1995) [Pubmed]
  29. Zolpidem metabolism in vitro: responsible cytochromes, chemical inhibitors, and in vivo correlations. Von Moltke, L.L., Greenblatt, D.J., Granda, B.W., Duan, S.X., Grassi, J.M., Venkatakrishnan, K., Harmatz, J.S., Shader, R.I. British journal of clinical pharmacology. (1999) [Pubmed]
  30. Loss of zolpidem efficacy in the hippocampus of mice with the GABAA receptor gamma2 F77I point mutation. Cope, D.W., Halbsguth, C., Karayannis, T., Wulff, P., Ferraguti, F., Hoeger, H., Leppä, E., Linden, A.M., Oberto, A., Ogris, W., Korpi, E.R., Sieghart, W., Somogyi, P., Wisden, W., Capogna, M. Eur. J. Neurosci. (2005) [Pubmed]
  31. Evaluation of EEG cyclic alternating pattern during sleep in insomniacs and controls under placebo and acute treatment with zolpidem. Terzano, M.G., Parrino, L. Sleep. (1992) [Pubmed]
  32. Nonselective and selective benzodiazepine receptor agonists--where are we today? Mitler, M.M. Sleep. (2000) [Pubmed]
  33. Zolpidem displays heterogeneity in its binding to the nonhuman primate benzodiazepine receptor in vivo. Schmid, L., Bottlaender, M., Fuseau, C., Fournier, D., Brouillet, E., Mazière, M. J. Neurochem. (1995) [Pubmed]
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