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Overview of currently available benzodiazepine and nonbenzodiazepine hypnotics

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Clinical Pharmacology of Sleep

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References

  1. Webb WB (1971) Sleep behavior as a biorhythm. In: WP Colquehoun (ed): Biological rhythms and human performance. Academic Press, New York, 149–177

    Google Scholar 

  2. Monti JM (1981) Sleep laboratory and clinical studies of the effects of triazolam, flunitrazepam and flurazepam in insomniac patients. Meth Find Exptl Clin Pharmacol 3: 303–326

    CAS  Google Scholar 

  3. Hirshkowitz M (2004) Normal human sleep: an overview. Med Clin N Am 88: 551–565

    Article  PubMed  Google Scholar 

  4. Williams RL, Karacan I, Thornby JI, Salis PJ (1972) The electroencephalogram sleep patterns of middle-aged males. J Nerv Ment Dis 154: 22–30

    PubMed  CAS  Google Scholar 

  5. Gillin JC, Duncan WC, Murphy DL, Post RM, Wehr TA, Goodwin FK, Wyatt RJ, Bunney WE (1981) Age-related changes in sleep in depressed and normal subjects. Psychiatry Res 4: 73–78

    Article  PubMed  CAS  Google Scholar 

  6. Lauer CJ, Riemann D, Wiegand M, Berger M (1991) From early to late adulthood changes in EEG sleep of depressed patients and healthy volunteers. Biol Psychiatry 29: 979–993

    Article  PubMed  CAS  Google Scholar 

  7. Ohayon MM, Carskadon MA, Guilleminault C, Vitiello MV (2004) Meta-analysis of quantitative sleep parameters from childhood to old age in healthy individuals: Developing normative sleep values across the human lifespan. Sleep 27: 1255–1273

    PubMed  Google Scholar 

  8. National Sleep Foundation (2002) “2002 Sleep in America” Poll. Washington, D.C., 1–43

    Google Scholar 

  9. Foley DJ, Monjan AA, Brown SL, Simonsick EM, Wallace RB, Blazer DG (1995) Sleep complaints among elderly persons: an epidemiologic study of three communities. Sleep 18: 425–432

    PubMed  CAS  Google Scholar 

  10. Foley DJ, Monjan A, Izmirlian G, Hays JC, Blazer DG (1999) Incidence and remission of insomnia among elderly adults in a biracial cohort. Sleep (Suppl 2): S373–S378

    Google Scholar 

  11. American Sleep Disorders Association (1997) International classification of sleep disorders, revised: Diagnostic and coding manual. American Sleep Disorders Association, Rochester

    Google Scholar 

  12. Hohagen F, Kappler C, Schramm E, Riemann D, Weyerer S, Berger M (1994) Sleep onset insomnia, sleep maintaining insomnia and insomnia with early morning awakening — temporal stability of subtypes in a longitudinal study on general practice attenders. Sleep 17: 551–554

    PubMed  CAS  Google Scholar 

  13. American Psychiatric Association (1994) Diagnostic and Statistical Manual of Mental Disorders (DSM-IV). American Psychiatric Association, Washington, D.C.

    Google Scholar 

  14. Lichstein KL (2000) Secondary insomnia. In: KL Lichstein, CM Morin (eds): Treatment of late-life insomnia. Sage Publications, London, 297–319

    Google Scholar 

  15. McCrae CS, Lichstein KL (2001) Secondary insomnia: diagnostic challenges and intervention opportunities. Sleep Med Rev 5: 47–61

    Article  PubMed  Google Scholar 

  16. Paul SM (1995) GABA and glycine. In: FE Bloom, DJ Kupfer (eds): Psychopharmacology: The Fourth Generation of Progress. Raven Press, New York, 87–94

    Google Scholar 

  17. Graham D, Besnard F, Faure C, Langer SZ (1996) GABAA receptor subtype diversity: Implications for new generation hypnotic drug discovery. Sleep 19: S43–S45

    PubMed  CAS  Google Scholar 

  18. Teuber L, Watjen F, Jensen LH (1999) Ligands for the benzodiazepine binding side — a survey. Curr Pharm Design 5: 317–343

    CAS  Google Scholar 

  19. Ator NA, McCann UD (2005) New insights into the GABAA receptor. CNS Spectrums 10: 20

    Google Scholar 

  20. Charney DS, Mihic SJ, Harris RA (2001) Hypnotics and sedatives. In: JG Hardman, LE Limbird (eds): The Pharmacological Basis of Therapeutics. McGraw-Hill, New York, 399–427

    Google Scholar 

  21. Greenblatt DJ (1991) Benzodiazepine hypnotics: sorting the pharmacokinetic facts. J Clin Psychiatry 52(Suppl): 4–10

    PubMed  Google Scholar 

  22. Gaillot J, Heusse D, Houghton D, Aurele JM, Dreyfus J (1983) Pharmacokinetics and metabolism of zopiclone. Pharmacology 27(Suppl 2): 76–91

    PubMed  CAS  Google Scholar 

  23. Drover DR (2004) Comparative pharmacokinetics and pharmacodynamics of short-acting hypnosedatives. Clin Pharmacokinet 43: 227–238

    Article  PubMed  CAS  Google Scholar 

  24. Musch B, Maillard F (1990) Zopiclone, the third generation hypnotic: a clinical overview. Int Clin Psychopharmacol 5(Suppl 2): 147–158

    PubMed  Google Scholar 

  25. Carlson JN, Haskew R, Wacker J, Maisonneuve IM, Glick SD, Jerussi TP (2001) Sedative and anxiolytic effects of zopiclone’s enantionmers and metabolite. Eur J Pharmacol 415: 181–189

    Article  PubMed  CAS  Google Scholar 

  26. Fernández C, Alt P, Davrinche C, Adrien J, Thuillier A, Farinotti R, Gimenez F (2002) Stereoselective distribution and stereoconversion of zopiclone enantiomers in plasma and brain tissues in rats. J Pharm Pharmacol 54: 335–340

    Article  PubMed  Google Scholar 

  27. Thénot JP, Hermann P, Durand A, Burke JT, Allen J, Garrigou D, Vajta S, Albin H, Thébault JJ, Olive G et al (1988) Pharmacokinetics and metabolism of zolpidem in various animal species and in humans. In: JP Sauvanet, SZ Langer, PL Morselli (eds): Imidazopyridines in Sleep Disorders: A novel Experimental and Therapeutic Approach. Raven Press, New York, 139–163

    Google Scholar 

  28. Hurst M, Noble S (1999) Zaleplon. CNS Drugs 11: 387–392

    Article  CAS  Google Scholar 

  29. Rosen AS, Fournie P, Darwish M, Danjou P, Troy SM (1999) Zaleplon pharmacokinetics and absolute bioavailability. Biopharm Drug Dispos 20: 171–175

    Article  PubMed  CAS  Google Scholar 

  30. Kaplan SA, Jack ML (1983) Metabolism of benzodiazepines: Pharmacokinetic and pharmacodynamic Considerations. In: E Costa (ed): The Benzodiazepines: From Molecular Biology to Clinical Practice. Raven Press, New York, 173–199

    Google Scholar 

  31. Meyer BR (1982) Benzodiazepines in the elderly. Med Clin N Am 66: 1017–1035

    PubMed  CAS  Google Scholar 

  32. Wilkinson GR(1979) The effect of aging on the disposition of benzodiazepines in man. In: J Crooks, IH Stevenson (eds): Drugs and the Elderly: Perspectives in Geriatric Clinical Pharmacology. University Park Press, Baltimore, 103–116

    Google Scholar 

  33. Klotz U, Avant GR, Hoyumpa A, Schenker S, Wilkinson GR (1975) The effects of age and liver disease on the disposition and elimination of diazepam in adult man. J Clin Invest 55: 347–359

    Article  PubMed  CAS  Google Scholar 

  34. Noble S, Langtry HD, Lamb H M (1998) Zopiclone: An update of its pharmacology, clinical efficacy and tolerability in the treatment of insomnia. Drugs 55: 277–302

    Article  PubMed  CAS  Google Scholar 

  35. Fernandez C, Martin C, Gimenez F, Farinotti R (1995) Clinical pharmacokinetics of zopiclone. Clin Pharmacokinet 29: 431–441

    Article  PubMed  CAS  Google Scholar 

  36. Bianchetti G, Dubruc C, Thiercelin JF, Bercoff E, Bouchet JL, Emeriau JP, Galperine I, Lambert D, Vandel B, Thébault JJ (1988) Clinical pharmacokinetics of zolpidem in various physiological and pathological conditions. In: JP Sauvanet, SZ Langer, PL Morselli (eds): Imidazopyridines in Sleep Disorders: A Novel Experimental and Therapeutic Approach. Raven Press, New York, 155–163

    Google Scholar 

  37. Pacifici C, Viani A, Rizzo G, Carrai M, Ganansia J, Bianchetti G, Morselli PL (1988) Plasma protein binding of zolpidem in liver and renal insufficiency. Int J Clin Pharmacol Ther Toxicol 26: 439–443

    PubMed  CAS  Google Scholar 

  38. Darwish M (1999) The relationship between the pharmacokinetics and pharmacodynamics of zaleplon. Eur Neuropsychopharmacol 5(Suppl): S361

    Article  Google Scholar 

  39. Drover DR (2004) Comparative pharmacokinetics and pharmacodynamics of short-acting hypnosedatives. Clin Pharmacokinet 43: 227–238

    Article  PubMed  CAS  Google Scholar 

  40. Wickland C, Patat A (1999) The safety and pharmacokinetics of zaleplon in hepatically impaired patients. Sleep Res 2(Suppl 1): 171

    Google Scholar 

  41. Monti JM, Boussard M, Olivera S, Labraga P, Alvariño F (1993) The effect of midazolam on transient insomnia. Eur J Clin Pharmacol 44: 525–527

    PubMed  CAS  Google Scholar 

  42. Monti JM, Monti D, Estévez F, Giusti M (1996) Sleep in patients with chronic primary insomnia during long-term zolpidem administration and after its withdrawal. Int Clin Psychopharmacol 11: 255–263

    PubMed  CAS  Google Scholar 

  43. Asnis GM, Chakraburtty A, DuBoff EA, Krystal A, Londborg PD, Rosenberg R, Roth-Schechter B, Scharf MB, Walsh JK (1999) Zolpidem for persistent insomnia in SSRI-treated depressed patients. J Clin Psychiatry 60: 668–676

    PubMed  CAS  Google Scholar 

  44. Kales A, Kales JD (1984) Evaluation and Treatment of Insomnia. Oxford University Press, New York

    Google Scholar 

  45. Monti JM, Alterwain P, Debellis J, Altier H, Pellejero T, Monti D (1987) Short-term sleep laboratory evaluation of midazolam in chronic insomniacs. Arzneim-Forsch/Drug Res 37: 54–57

    CAS  Google Scholar 

  46. Bixler EO, Kales A, Soldatos CR, Scharf MB, Kales JD (1978) Effectivenes of temazepam with short-, intermediate-, and long-term use: sleep laboratory evaluation. J Clin Pharmacol 18: 110–118

    PubMed  CAS  Google Scholar 

  47. Kales A, Bixler EO, Soldatos CR, Vela-Bueno A, Jacoby J, Kales JD (1982) Quazepam and flurazepam: long-term use and extended withdrawal. Clin Pharmacol Ther 32: 781–788

    Article  PubMed  CAS  Google Scholar 

  48. Mamelak M, Csima A, Price V (1984) A comparative 25-night sleep laboratory study of the effects of quazepam and triazolam on chronic insomniacs. J Clin Pharmacol 24: 67–77

    Google Scholar 

  49. Mitler MM, Seidel BA, van den Hoed J, Greenblatt DJ, Dement WC (1984) Comparative hypnotic effects of flurazepam, triazolam, and placebo: a long-term simultaneous nighttime and daytime study. J Clin Psychopharmacol 4: 2–13

    PubMed  CAS  Google Scholar 

  50. Monti JM, Attali P, Monti D, Zipfel A, de la Giclais B, Morselli PL (1994) Zolpidem and rebound insomnia — a double-blind, controlled polysomnographic study in chronic insomniac patients. Pharmacopsychiatry 27: 166–175

    PubMed  CAS  Google Scholar 

  51. Kales A, Bixler EO, Soldatos CR, Vela-Bueno A, Jacoby JA, Kales JD (1986) Quazepam and temazepam: effects of short-and intermedaite-term use and withdrawal. Clin Pharmacol Ther 30: 345–352

    Article  Google Scholar 

  52. Vgontzas AN, Kales A, Bixler EO, Myers DC (1994) Temazepam 7.5 mg: effects on sleep in elderly insomniacs. Eur J Clin Pharmacol 46: 209–213

    Article  PubMed  CAS  Google Scholar 

  53. Soldatos CR, Dikeos DG, Whitehead A (1999) Tolerance and rebound insomnia with rapidly eliminated hypnotics: a meta-analysis of sleep laboratory studies. Int Clin Psychopharmacol 14: 287–303

    Article  PubMed  CAS  Google Scholar 

  54. Mamelak M, Csima A, Price V (1983) Effects of zopiclone on the sleep of chronic insomniacs. Pharmacology 27: 156–164

    PubMed  Google Scholar 

  55. Petre Quadens O, Hoffman G, Buytaert G (1983) Effects of zopiclone as compared to flurazepam on sleep in women over 40 years of age. Pharmacology 27(Suppl 2) 146–155

    Google Scholar 

  56. Pecknold J, Wilson R, Le Morvan P (1990) Long-term efficacy and withdrawal of zopiclone: a sleep laboratory study. Int Clin Psychopharmacol 5: 57–67

    Article  PubMed  Google Scholar 

  57. Tiberge M, Calvet U, Khayi N, Delahye C, Arbus L (1988) Comparison of the effects of zopiclone and triazolam on sleep in healthy subjects. Encephale 14: 319–324

    PubMed  CAS  Google Scholar 

  58. Billiard M, Besset A, De Lustrac C, Brissaud L, Cadilhac J (1989) Effect of zopiclone on sleep, daytime somnolence and nighttime performances in healthy volunteers. Neurophysiol Clin 19: 131–143

    PubMed  CAS  Google Scholar 

  59. Jovanovic UJ, Dreyfuss JF (1983) Polygraphical sleep recording in insomniac patients under zopiclone or nitrazepam. Pharmacology 27: 136–145

    PubMed  Google Scholar 

  60. Rosenberg R, Caron J, Roth T, Amato D (2005) An assessment of the efficacy and safety of eszopiclone in the treatment of transient insomnia in healthy adults. Sleep Med 6: 15–22

    Article  PubMed  Google Scholar 

  61. Zammit GK, McNabb LJ, Caron J, Amato DA, Roth T (2004) Efficacy and safety of eszopiclone across 6-weeks of treatment for primary insomnia. Curr Med Res Opin 20: 1979–1991

    Article  PubMed  CAS  Google Scholar 

  62. Krystal AD, Walsh JK, Laska E, Caron J, Amato DA, Wessel TC, Roth T (2003) Sustained efficacy of eszopiclone over 6 months of nightly treatment: Results of a randomized, double-blind, placebo-controlled study in adults with chronic insomnia. Sleep 26: 793–799

    PubMed  Google Scholar 

  63. Nicholson AN, Pascoe PA (1986) Hypnotic activity of an imidazopyridine (zolpidem). Brit J Clin Pharmacol 21: 205–211

    CAS  Google Scholar 

  64. Herrmann WM, Dubicki S, Wober W (1988) Zolpidem: a four week pilot polysomnographic study in patients with chronic sleep disturbances. In: JP Sauvanet, SZ Langer, PL Morselli (eds): Imidazopyridines in Sleep Disorders: a Novel Experimental and Therapeutic Approach. Raven Press, New York, 261–278

    Google Scholar 

  65. Monti JM(1989) Effects of zolpidem on sleep in insomniac patients. Eur J Clin Pharmacol 36: 461–466

    Google Scholar 

  66. Perlis ML, McCall WV, Krystal AD, Walsh JK (2004) Long-term, non-nightly administration of zolpidem in the treatment of patients with primary insomnia. J Clin Psychiatry 65: 1128–1137

    Article  PubMed  CAS  Google Scholar 

  67. Roger M, Dallot JY, Salmon O, Neveux E, Gitton JP, Gerson M, Brossel S, Sauvanet JP (1988) Hypnotic effect of zolpidem in geriatric patients: A dose-finding study. In: Sauvanet JP, Langer SZ, Morselli PL (eds): Imidazopyridines in Sleep Disorders: A Novel Experimental and Therapeutic Approach. Raven Press, New York, 279–287

    Google Scholar 

  68. Sauvanet JP, Maarek L, Roger M, Renaudin J, Louvel E, Orofiamma B (1988) Open long-term trials with zolpidem in insomnia. In: JP Sauvanet, SZ Langer, PL Morselli (eds): Imidazopyridines in Sleep Disorders: A Novel Experimental and Therapeutic Approach. Raven Press, New York, 339–349

    Google Scholar 

  69. Benoit O, Bouard G, Payan C, Prado J, Blanchet G (1994) Effect of a single dose (10 mg) of zolpidem on visual and spectral analysis of sleep in young poor sleepers. Psychopharmacology 116: 297–303

    Article  PubMed  CAS  Google Scholar 

  70. Monti JM, Alvariño F, Monti D (2000) Conventional and power spectrum analysis of the effects of zolpidem on sleep EEG in patients with chronic primary insomnia. Sleep 23: 1075–1084

    PubMed  CAS  Google Scholar 

  71. Heydorn WE(2000) Zaleplon — a review of a novel sedative hypnotic used in the treatment of insomnia. Exp Opin Invest Drugs 9: 841–858

    Google Scholar 

  72. Walsh JK, Vogel GW, Scharf M, Erman M, Erwin CW, Schweitzer PK, Mangano RM, Roth T (2000) A five week, polysomnographic assessment of zaleplon 10 mg for the treatment of primary insomnia. Sleep Med 1: 41–49

    Article  PubMed  Google Scholar 

  73. Elie R, Ruther E, Farr I, Emilien G, Salinas E (1999) Sleep latency is shortened during 4 weeks of treatment with zaleplon, a novel non-benzodiazepine hypnotic. J Clin Psychiatry 60: 536–544

    PubMed  CAS  Google Scholar 

  74. Bixler EO, Scharf MB, Soldatos CR, Mitsky DJ, Kales A (1979) Effects of hypnotic drugs on memory. Life Sci 25: 1379–1388

    Article  PubMed  CAS  Google Scholar 

  75. Bixler EO, Kales A, Manfredi RL, Vgontzas AN, Tyson KL, Kales JD (1991) Next-day memory impairment with triazolam use. Lancet 337: 827–831

    Article  PubMed  CAS  Google Scholar 

  76. Adam K, Oswald I (1989) Can a rapidly-eliminated hypnotic cause daytime anxiety? Pharmacopsychiatry 22: 115–119

    Article  PubMed  CAS  Google Scholar 

  77. Hindmarch I, Haller J, Sherwood N, Kerr JS (1990) Comparison of five anxiolytic benzodiazepines on measures of psychomotor performance and sleep. Neuropsychobiology 24: 84–89

    Article  PubMed  CAS  Google Scholar 

  78. Lader M (1994) Anxiety or depression during withdrawal of hypnotic treatments. J Psychosom Res 38(Suppl 1) 113–123

    Article  PubMed  Google Scholar 

  79. Trewin VF, Lawrence CJ, Veitch GB (1992) An investigation of the association of benzodiazepines and other hypnotics with the incidence of falls in the elderly. J Clin Pharm Ther 17: 129–133

    PubMed  CAS  Google Scholar 

  80. Allain H, Delahaye C, Le Coz F, Blin P, Decombe R, Martinet JP (1991) Postmarketing surveillance of zopiclone in insomnia: analysis of 20513 cases. Sleep 14: 408–413

    PubMed  CAS  Google Scholar 

  81. Kuitunen T, Mattila MJ, Seppala T (1990) Actions and interactions of hypnotics on human performance: single doses of zopiclone, triazolam and alcohol. Int Clin Psychopharmacol 5(Suppl 2) 115–130

    PubMed  Google Scholar 

  82. Holm KJ, Goa KL (2000) Zolpidem — An update of its pharmacology, therapeutic efficacy and tolerability in the treatment of insomnia. Drugs 59: 865–889

    Article  PubMed  CAS  Google Scholar 

  83. Monti JM (2004) Primary and secondary insomnia: Prevalence, causes and current therapeutics. Curr Med Chem — CNS Agents 4: 119–137

    CAS  Google Scholar 

  84. Zhdanova IV (2004) Advances in the management of insomnia. Expert Opin Pharmacother 5: 1573–1579

    Article  PubMed  CAS  Google Scholar 

  85. Sateia MJ, Pigeon WR (2004) Identification and management of insomnia. Med Clin N Am 88: 567–596

    Article  PubMed  Google Scholar 

  86. Cluydts R, Peeters K, de Bouyalski I, Lavoisy J (1998) Comparison of continuous versus intermittent administration of zolpidem in chronic insomniacs: a double-blind, randomized pilot study. J Int Med Res 26: 13–24

    PubMed  CAS  Google Scholar 

  87. Hajak G, Cluydts R, Allain H, Estivill E, Parrino L, Terzano MG, Walsh JK (2003) The challenge of chronic insomnia: is non-nightly hypnotic treatment a feasible alternative? Eur Psychiatry 18: 201–208

    Article  PubMed  CAS  Google Scholar 

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Authors and Affiliations

  1. Department of Pharmacology and Therapeutics, Clinics Hospital, 2833/602 Zudanez Street, Montevideo, 11300, Uruguay

    Jaime M. Monti

  2. Department of Psychiatry, Allegheny General Hospital, Pittsburgh, PA, 15212, USA

    Daniel Monti

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Editors and Affiliations

  1. Comprehensive Center for Sleep Medicine, Department of Pulmonary, Critical Care, and Sleep Medicine, Mount Sinai School of Medicine, 1176, 5th Avenue, New York, NY, 10029, USA

    S. R. Pandi-Perumal

  2. Pharmacology and Therapeutics, 2833/602 Zudanez Street, Montevideo, 11300, Uruguay

    Jaime M. Monti

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Monti, J.M., Monti, D. (2006). Overview of currently available benzodiazepine and nonbenzodiazepine hypnotics. In: Pandi-Perumal, S.R., Monti, J.M. (eds) Clinical Pharmacology of Sleep. Birkhäuser Basel. https://doi.org/10.1007/3-7643-7440-3_14

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