Comparative pharmacokinetics and pharmacodynamics of short-acting hypnosedatives: Zaleplon, zolpidem and zopiclone

Clinical Pharmacokinetics

Volumn 43, Issue 4, 2004, Pages 227-238

  Drover, David R ^a  

^a STANFORD UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

4 AMINOBUTYRIC ACID RECEPTOR; BENZODIAZEPINE; CIMETIDINE; CYTOCHROME P450 3A4; DIGOXIN; ERYTHROMYCIN; FLUCONAZOLE; IBUPROFEN; ITRACONAZOLE; KETOCONAZOLE; RECEPTOR SUBUNIT; RIFAMPICIN; SERTRALINE; SHORT ACTING DRUG; THIORIDAZINE; ZALEPLON; ZOLPIDEM; ZOPICLONE;

AMNESIA; AMNESIC ACTIVITY; ANTIEPILEPTIC ACTIVITY; AREA UNDER THE CURVE; DRUG ACTIVITY; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG EFFECT; DRUG ELIMINATION; DRUG HALF LIFE; DRUG INHIBITION; DRUG MECHANISM; DRUG METABOLISM; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG STRUCTURE; FATIGUE; HUMAN; INSOMNIA; MAINTENANCE THERAPY; MEMORY DISORDER; PHARMACODYNAMICS; PHARMACOKINETICS; PRIORITY JOURNAL; PSYCHOMOTOR ACTIVITY; RECEPTOR AFFINITY; REVIEW; SEDATION; SIDE EFFECT; SLEEP STAGE; TASTE DISORDER; TRANQUILIZING ACTIVITY; TREATMENT INDICATION; VISUAL DISORDER; XEROSTOMIA;

ACETAMIDES; AGED; HUMANS; HYPNOTICS AND SEDATIVES; KIDNEY FAILURE; LIVER FAILURE; PIPERAZINES; PYRIDINES; PYRIMIDINES;

EID: 1842609539     PISSN: 03125963     EISSN: None     Source Type: Journal    
DOI: 10.2165/00003088-200443040-00002     Document Type: Review

References (113)

1. Mendelson WB, Jain B. An assessment of short-acting hypnotics. Drug Saf 1995; 13 (4): 257-70
2. George CF. Pyrazolopyrimidines. Lancet 2001; 358 (9293): 1623-6
3. A receptor subtypes. Curr Top Med Chem 2002; 2 (8): 795-816
4. A receptors. Neurochem Int 1999; 34 (5): 379-85
5. A receptor subtypes. Pharmacol Rev 1995; 47 (2): 181-234
6. Terzano MG, Rossi M, Palomba V, et al. New drugs for insomnia: comparative tolerability of zopiclone, zolpidem and zaleplon. Drug Saf 2003; 26 (4): 261-82
7. Wagner J, Wagner ML. Non-benzodiazepines for the treatment of insomnia. Sleep Med Rev 2000; 4 (6): 551-81
8. Weitzel KW, Wickman JM, Augustin SG, et al. Zaleplon: a pyrazolopyrimidine sedative-hypnotic agent for the treatment of insomnia. Clin Ther 2000; 22 (11): 1254-67
9. Dooley M, Plosker GL. Zaleplon: a review of its use in the treatment of insomnia. Drugs 2000; 60 (2): 413-45
10. Hoehns JD, Perry PJ. Zolpidem: a nonbenzodiazepine hypnotic for treatment of insomnia. Clin Pharm 1993; 12 (11): 814-28
11. Langtry HD, Benfield P. Zolpidem: a review of its pharmacodynamic and pharmacokinetic properties and therapeutic potential. Drugs 1990; 40 (2): 291-313
12. Holm KJ, Goa KL. Zolpidem: an update of its pharmacology, therapeutic efficacy and tolerability in the treatment of insomnia. Drugs 2000; 59 (4): 865-89
13. Goa KL, Heel RC. Zopiclone: a review of its pharmacodynamic and pharmacokinetic properties and therapeutic efficacy as an hypnotic. Drugs 1986; 32 (1): 48-65
14. Noble S, Langtry HD, Lamb HM. Zopiclone: an update of its pharmacology, clinical efficacy and tolerability in the treatment of insomnia. Drugs 1998; 55 (2): 277-302
15. Kales A, Manfredi RL, Vgontzas AN, et al. Rebound insomnia after only brief and intermittent use of rapidly eliminated benzodiazepines. Clin Pharmacol Ther 1991; 49 (4): 468-76
16. Kales A, Soldatos CR, Bixler EO, et al. Midazolam: dose-response studies of effectiveness and rebound insomnia. Pharmacology 1983; 26 (3): 138-49
17. A receptors different from zolpidem, zopiclone and benzodiazepines. Neurosci Res Commun 1999; 25 (3): 139-48
18. Sanger DJ, Zivkovic B. Further behavioural evidence for the selective sedative action of zolpidem. Neuropharmacology 1988; 27 (11): 1125-30
19. Vanover KE, Barrett JE. Evaluation of the discriminative stimulus effects of the novel sedative-hypnotic CL 284,846. Psychopharmacology (Berl) 1994; 115 (3): 289-96
20. Day IP, Clody DE, Monaghan MM, et al. Pharmacology of CL 284,846 a non-benzodiazepine sedative with reduced amnestic liability [abstract]. Soc Neurosci 1992; 18: 725
21. ω receptor subtypes. Psychopharmacology (Berl) 1999; 146 (2): 205-13
22. Noguchi H, Kitazumi K, Mori M, et al. Binding and neuropharmacological profile of zaleplon, a novel nonbenzodiazepine sedative/hypnotic. Eur J Pharmacol 2002; 434 (1-2): 21-8
23. Drover D, Lemmens H, Naidu S, et al. Pharmacokinetics, pharmacodynamics, and relative pharmacokinetic/pharmacodynamic profiles of zaleplon and zolpidem. Clin Ther 2000; 22 (12): 1443-61
24. 1 receptor-selective ligands in rhesus monkeys. J Pharmacol Exp Ther 2002; 300 (2): 505-12
25. Sanger DJ. The effects of new hypnotic drugs in rats trained to discriminate ethanol. Behav Pharmacol 1997; 8 (4): 287-92
26. Sanger DJ. Behavioural effects of novel benzodiazepine (omega) receptor agonists and partial agonists: increases in punished responding and antagonism of the pentylenetetrazole cue. Behav Pharmacol 1995; 6 (2): 116-26
27. Davies M, Newell JG, Derry JM, et al. Characterization of the interaction of zopiclone with γ-aminobutyric acid type A receptors. Mol Pharmacol 2000; 58 (4): 756-62
28. Blanchard JC, Zundel JL, Julou L. Differences between cyclopyrrolones (suriclone and zopiclone) and benzodiazepine binding to rat hippocampus photolabelled membranes. Biochem Pharmacol 1983; 32 (23): 3651-3
29. Blanchard JC, Boireau A, Julou L. Brain receptors and zopiclone. Pharmacology 1983; 27 Suppl. 2: 59-69
30. Blanchard JC, Boireau A, Garret C, et al. In vitro and in vivo inhibition by zopiclone of benzodiazepine binding to rodent brain receptors. Life Sci 1979; 24 (26): 2417-20
31. A receptor subtype selectivity in vivo. J Pharmacol Exp Ther 2003; 304 (3): 1251-7
32. A receptor modulators: in vitro-in vivo correlations. J Pharmacol Exp Ther 2003; 304 (1): 88-101
33. A receptor gene expression induced by withdrawal of, but not by long-term exposure to, zaleplon or zolpidem. Neuropharmacology 2002; 42 (2): 191-8
34. Danjou P, Paty I, Fruncillo R, et al. A comparison of the residual effects of zaleplon and zolpidem following administration 5 to 2h before awakening. Br J Clin Pharmacol 1999; 48 (3): 367-74
35. Walsh JK, Pollak CP, Scharf MB, et al. Lack of residual sedation following middle-of-the-night zaleplon administration in sleep maintenance insomnia. Clin Neuropharmacol 2000; 23 (1): 17-21
36. Vermeeren A, Riedel WJ, van Boxtel MP, et al. Differential residual effects of zaleplon and zopiclone on actual driving: a comparison with a low dose of alcohol. Sleep 2002; 25 (2): 224-31
37. Hedner J, Yaeche R, Emilien G, et al. Zaleplon shortens subjective sleep latency and improves subjective sleep quality in elderly patients with insomnia. The Zaleplon Clinical Investigator Study Group. Int J Geriatr Psychiatry 2000; 15 (8): 704-12
38. Elie R, Ruther E, Farr I, et al. Sleep latency is shortened during 4 weeks of treatment with zaleplon, a novel nonbenzodiazepine hypnotic: Zaleplon Clinical Study Group. J Clin Psychiatry 1999; 60 (8): 536-44
39. Uchiumi M, Isawa S, Suzuki M, et al. The effects of zolpidem and zopiclone on daytime sleepiness and psychomotor performance. Nihon Shinkei Seishin Yakurigaku Zasshi 2000; 20 (3): 123-30
40. Dietrich B, Emilien G, Salinas E. Zaleplon does not produce residual sedation in a phase-advance model of transient insomnia [abstract]. J Sleep Res 1998; 7 Suppl. 2: 67
41. Hemmeter U, Muller M, Bischof R, et al. Effect of zopiclone and temazepam on sleep EEG parameters, psychomotor and memory functions in healthy elderly volunteers. Psychopharmacology (Berl) 2000; 147 (4): 384-96
42. Nakajima T, Sasaki T, Nakagome K, et al. Comparison of the effects of zolpidem and zopiclone on nocturnal sleep and sleep latency in the morning: a cross-over study in healthy young volunteers. Life Sci 2000; 67 (1): 81-90
43. Hajak G. A comparative assessment of the risks and benefits of zopiclone: a review of 15 years clinical experience. Drug Saf 1999; 21 (6): 457-69
44. Hajak G, Clarenbach P, Fischer W, et al. Zopiclone improves sleep quality and daytime well-being in insomniac patients: comparison with triazolam, flunitrazepam and placebo. Int Clin Psychopharmacol 1994; 9 (4): 251-61
45. Voderholzer U, Riemann D, Hornyak M, et al. A double-blind, randomized and placebo-controlled study on the polysomnographic withdrawal effects of zopiclone, zolpidem and triazolam in healthy subjects. Eur Arch Psychiatry Clin Neurosci 2001; 251 (3): 117-23
46. Sanger DJ, Morel E, Perrault G. Comparison of the pharmacological profiles of the hypnotic drugs, zaleplon and zolpidem. Eur J Pharmacol 1996; 313 (1-2): 35-42
47. Gaudreault J, Varin F, Pollack GM. Pharmacokinetics and anticonvulsant effect of a new hypnotic, CL 284,846, in rats. Pharm Res 1995; 12 (11): 1592-7
48. Julou L, Bardone MC, Blanchard JC, et al. Pharmacological studies on zopiclone. Pharmacology 1983; 27 Suppl. 2: 46-58
49. Griebel G, Perrault G, Sanger DJ. Differences in anxiolytic-like profile of two novel nonbenzodiazepine BZ (omega) receptor agonists on defensive behaviors of mice. Pharmacol Biochem Behav 1999; 62 (4): 689-94
50. Lobarinas E, Falk JL. Comparison of benzodiazepines and the non-benzodiazepine agents zolpidem and zaleplon with respect to anxiolytic action as measured by increases in hypertonic NaCl-solution drinking in rats. Psychopharmacology (Berl) 2000; 149 (2): 176-80
51. Depoortere H, Zivkovic B, Lloyd KG, et al. Zolpidem, a novel nonbenzodiazepine hypnotic: I. neuropharmacological and behavioral effects. J Pharmacol Exp Ther 1986; 237 (2): 649-58
52. Berson A, Descatoire V, Sutton A, et al. Toxicity of alpidem, a peripheral benzodiazepine receptor ligand, but not zolpidem, in rat hepatocytes: role of mitochondrial permeability transition and metabolic activation. J Pharmacol Exp Ther 2001; 299 (2): 793-800
53. Griebel G, Perrault G, Sanger DJ. Limited anxiolytic-like effects of non-benzodiazepine hypnotics in rodents. J Psychopharmacol 1998; 12 (4): 356-65
54. Carlson JN, Haskew R, Wacker J, et al. Sedative and anxiolytic effects of zopiclone's enantiomers and metabolite. Eur J Pharmacol 2001; 415 (2-3): 181-9
55. Georgiev V. (S)-Zopiclone (Sepracor). Curr Opin Investig Drugs 2001; 2 (2): 271-3
56. Ghoneim MM, Mewaldt SP, Berie JL, et al. Memory and performance effects of single and 3-week administration of diazepam. Psychopharmacology 1981; 73 (2): 147-51
57. Curran HV. Tranquillising memories: a review of the effects of benzodiazepines on human memory. Biol Psychol 1986; 23 (2): 179-213
58. Troy SM, Lucki I, Unruh MA, et al. Comparison of the effects of zaleplon, zolpidem, and triazolam on memory, learning, and psychomotor performance. J Clin Psychopharmacol 2000; 20 (3): 328-37
59. File SE, Lister RG. Do lorazepam-induced deficits in learning result from impaired rehearsal, reduced motivation or increased sedation? Br J Clin Pharmacol 1982; 14 (4): 545-50
60. Beer B, Ieni JR, Wu WH, et al. A placebo-controlled evaluation of single, escalating doses of CL 284,846, a non-benzodiazepine hypnotic. J Clin Pharmacol 1994; 34 (4): 335-44
61. Rush CR, Frey JM, Griffiths RR. Zaleplon and triazolam in humans: acute behavioral effects and abuse potential. Psychopharmacology (Berl) 1999; 145 (1): 39-51
62. Isawa S, Suzuki M, Uchiumi M, et al. The effect of zolpidem and zopiclone on memory. Nihon Shinkei Seishin Yakurigaku Zasshi 2000; 20 (2): 61-9
63. Dingemanse J, Bury M, Hussain Y, et al. Comparative tolerability, pharmacodynamics, and pharmacokinetics of a metabolite of a quinolizinone hypnotic and zolpidem in healthy subjects. Drug Metab Dispos 2000; 28 (12): 1411-6
64. Dingemanse J, Bury M, Bock J, et al. Comparative pharmacodynamics of Ro 41-3696, a new hypnotic, and zolpidem after night-time administration to healthy subjects. Psychopharmacology (Berl) 1995; 122 (2): 169-74
65. Greenblatt DJ, Harmatz JS, von Moltke LL, et al. Comparative kinetics and response to the benzodiazepine agonists triazolam and zolpidem: evaluation of sex-dependent differences. J Pharmacol Exp Ther 2000; 293 (2): 435-43
66. Subhan Z, Hindmarch I. Effects of zopiclone and benzodiazepine hypnotics on search in short-term memory. Neuropsychobiology 1984; 12 (4): 244-8
67. Fossen A, Godlibsen OB, Loyning Y, et al. Effects of hypnotics on memory. Pharmacology 1983; 27 Suppl. 2: 116-26
68. Morton S, Lader M. Studies with alpidem in normal volunteers and anxious patients. Pharmacopsychiatry 1990; 23 Suppl. 3: 120-3
69. Morton S, Lader M. Alpidem and lorazepam in the treatment of patients with anxiety disorders: comparison of physiological and psychological effects. Pharmacopsychiatry 1992; 25 (4): 177-81
70. Vidailhet P, Kazes M, Danion JM, et al. Effects of lorazepam and diazepam on conscious and automatic memory processes. Psychopharmacology (Berl) 1996; 127 (1): 63-72
71. Greenblatt DJ, Harmatz JS, von Moltke LL, et al. Comparative kinetics and dynamics of zaleplon, zolpidem, and placebo. Clin Pharmacol Ther 1998; 64 (5): 553-61
72. Allen D, Curran HV, Lader M. The effects of single doses of CL284,846, lorazepam, and placebo on psychomotor and memory function in normal male volunteers. Eur J Clin Pharmacol 1993; 45 (4): 313-20
73. Bhatia SC, Arora M, Bhatia SK. Perceptual disturbances with zaleplon. Psychiatr Serv 2001; 52 (1): 109-10
74. Musch B, Maillard F. Zopiclone, the third generation hypnotic: a clinical overview. Int Clin Psychopharmacol 1990; 5 Suppl. 2: 147-58
75. Delahaye C, Ferrand B, Pieddeloup C, et al. Post marketing surveillance of zopiclone: interim analysis on the first 10,000 cases in a clinical study in general practice. Int Clin Psychopharmacol 1990; 5 Suppl. 2: 131-8
76. Bianchetti G, Dubruc C, Thiercelin JF, et al. Clinical pharmacokinetic of zolpidem in various physiological and pathological conditions. In: Sauvanet JP, Langer SZ, Morelli PL, editors. Imidazopyridines in sleep disorders. 2E New York: Raven Press, 1988: 155-63
77. Gaillot J, Le Roux Y, Houghton GW, et al. Critical factors for pharmacokinetics of zopiclone in the elderly and in patients with liver and renal insufficiency. Sleep 1987; 10 Suppl. 1: 7-21
78. Greenblatt DJ, Harmatz JS, Shader RI. Clinical pharmacokinetics of anxiolytics and hypnotics in the elderly: therapeutic considerations (Part II). Clin Pharmacokinet 1991; 21 (4): 262-73
79. Greenblatt DJ, Harmatz JS, Shader RI. Clinical pharmacokinetics of anxiolytics and hypnotics in the elderly: therapeutic considerations (Part I). Clin Pharmacokinet 1991; 21 (3): 165-77
80. Rosen AS, Fournie P, Darwish M, et al. Zaleplon pharmacokinetics and absolute bioavailability. Biopharm Drug Dispos 1999; 20 (3): 171-5
81. Durand A, Thenot JP, Bianchetti G, et al. Comparative pharmacokinetic profile of two imidazopyridine drugs: zolpidem and alpidem. Drug Metab Rev 1992; 24 (2): 239-66
82. Thenot JP, Herman P, Durand A, et al. Pharmacokinetics and metabolism of zolpidem in various animal species and in humans. In: Sauvanet JP, Langer SZ, Morelli PL, editors. Imidazopyridines in sleep disorders. New York: Raven Press, 1988: 139-53
83. Patat A, Trocherie S, Thebault JJ, et al. EEG profile of intravenous zolpidem in healthy volunteers. Psychopharmacology (Berl) 1994; 114(1): 138-46
84. Gaillot J, Heusse D, Hougton GW, et al. Pharmacokinetics and metabolism of zopiclone. Pharmacology 1983; 27 Suppl. 2: 76-91
85. Fernandez C, Martin C, Gimenez F, et al. Clinical pharmacokinetics of zopiclone. Clin Pharmacokinet 1995; 29 (6): 431-41
86. Renwick AB, Mistry H, Ball SE, et al. Metabolism of zaleplon by human hepatic microsomal cytochrome P450 isoforms. Xenobiotica 1998; 28 (4): 337-48
87. Houghton GW, Dennis MJ, Templeton R, et al. A repeated dose pharmacokinetic study of a new hypnotic agent, zopiclone (Imovane). Int J Clin Pharmacol Ther Toxicol 1985; 23 (2): 97-100
88. Fernandez C, Maradeix V, Gimenez F, et al. Pharmacokinetics of zopiclone and its enantiomers in Caucasian young healthy volunteers. Drug Metab Dispos 1993; 21 (6): 1125-8
89. Wickland C, Patat A. The safety and pharmacokinetics of zaleplon in hepatically impaired patients [abstract]. Sleep Res Online 1999; 2 Suppl. 1: 171
90. Parker G, Roberts CJ. Plasma concentrations and central nervous system effects of the new hypnotic agent zopiclone in patients with chronic liver disease. Br J Clin Pharmacol 1983; 16 (3): 259-65
91. Wickland C, Patat A. The pharmacokinetics and safety of zaleplon in patients with renal impairment [abstract]. Sleep Res Online 1999; 2 Suppl. 1: 172
92. Fillastre JP, Geffroy-Josse S, Etienne I, et al. Pharmacokinetics and pharmacodynamics of zolpidem following repeated doses in hemodialyzed uraemic patients. Fundam Clin Pharmacol 1993; 7 (1): 1-9
93. Pacifici GM, Viani A, Rizzo G, et al. Plasma protein binding of zolpidem in liver and renal insufficiency. Int J Clin Pharmacol Ther Toxicol 1988; 26 (9): 439-43
94. Viron B, De Meyer M, Le Liboux A, et al. Steady state pharmacokinetics of zopiclone during multiple oral dosing (7.5mg nocte) in patients with severe chronic renal failure. Int Clin Psychopharmacol 1990; 5 Suppl. 2: 95-104
95. Dresser GK, Spence JD, Bailey DG. Pharmacokinetic-pharmacodynamic consequences and clinical relevance of cytochrome P450 3A4 inhibition. Clin Pharmacokinet 2000; 38 (1): 41-57
96. Hetta J, Broman JE, Darwish M, et al. Psychomotor effects of zaleplon and thioridazine coadministration. Eur J Clin Pharmacol 2000; 56 (3): 211-7
97. Sanchez Garcia P, Paty I, Leister CA, et al. Effect of zaleplon on digoxin pharmacokinetics and pharmacodynamics. Am J Health Syst Pharm 2000; 57 (24): 2267-70
98. Sanchez Garcia P, Carcas A, Zapater P, et al. Absence of an interaction between ibuprofen and zaleplon. Am J Health Syst Pharm 2000; 57 (12): 1137-41
99. Allard S, Sainati SM, Roth-Schechter BF. Coadministration of short-term zolpidem with sertraline in healthy women. J Clin Pharmacol 1999; 39 (2): 184-91
100. Greenblatt DJ, von Moltke LL, Harmatz JS, et al. Kinetic and dynamic interaction study of zolpidem with ketoconazole, itraconazole, and fluconazole. Clin Pharmacol Ther 1998; 64 (6): 661-71
101. Villikka K, Kivisto KT, Luurila H, et al. Rifampin reduces plasma concentrations and effects of zolpidem. Clin Pharmacol Ther 1997; 62 (6): 629-34
102. Hulhoven R, Desager JP, Harvengt C, et al. Lack of interaction between zolpidem and H2 antagonists, cimetidine and ranitidine. Int J Clin Pharmacol Res 1988; 8 (6): 471-6
103. Villikka K, Kivisto KT, Lamberg TS, et al. Concentrations and effects of zopiclone are greatly reduced by rifampicin. Br J Clin Pharmacol 1997; 43 (5): 471-4
104. Jalava KM, Olkkola KT, Neuvonen PJ. Effect of itraconazole on the pharmacokinetics and pharmacodynamics of zopiclone. Eur J Clin Pharmacol 1996; 51 (3-4): 331-4
105. Aranko K, Luurila H, Backman JT, et al. The effect of erythromycin on the pharmacokinetics and pharmacodynamics of zopiclone. Br J Clin Pharmacol 1994; 38 (4): 363-7
106. Alderman CP, Gebauer MG, Gilbert AL, et al. Possible interaction of zopiclone and nefazodone. Ann Pharmacother 2001; 35 (11): 1378-80
107. Beal S, Sheiner L. NONMEM user guide. San Francisco (CA): University of California, San Francisco, 1998
108. Patat A, Paty I, Hindmarch I. Pharmacodynamic profile of zaleplon, a new non-benzodiazepine hypnotic agent. Hum Psychopharmacol 2001; 16 (5): 369-92
109. Sanger DJ, Benavides J, Perrault G, et al. Recent developments in the behavioral pharmacology of benzodiazepine (omega) receptors: evidence for the functional significance of receptor subtypes. Neurosci Biobehav Rev 1994; 18 (3): 355-72
110. A receptor subtypes. Eur J Pharmacol 2002; 451 (2): 103-10
111. Stanski DR, Ham J, Miller RD, et al. Pharmacokinetics and pharmacodynamics of d-tubocurarine during nitrous oxide-narcotic and halothane anesthesia in man. Anesthesiology 1979; 51 (3): 235-41
112. Sheiner LB, Stanski DR, Vozeh S, et al. Simultaneous modeling of pharmacokinetics and pharmacodynamics: application to d-tubocurarine. Clin Pharmacol Ther 1979; 25 (3): 358-71
113. Wada DR, Drover DR, Lemmens HJ. Determination of the distribution volume that can be used to calculate the intravenous loading dose. Clin Pharmacokinet 1998; 35 (1): 1-7