Behavioral Pharmacology of Zolpidem Relative to Benzodiazepines A Review

Rush, Craig R.

doi:10.1016/s0091-3057(98)00102-6

Cited by 258 publications

(83 citation statements)

References 106 publications

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“…These ®ndings are concordant with several previous studies that examined the performance-impairing effects of zolpidem and triazolam on a Digit-Enterand-Recall task (e.g., Mintzer et al, 1997; for a review also see Rush, 1998). Worth noting, however, is that most of these previous studies failed to ®nd signi®cant differences between the dose-related effects of zolpidem and triazolam.…”

Section: Discussionsupporting

confidence: 89%

“…Thus, the doses tested in the present study were 75, 150 and 225% of the recommended hypnotic doses. We chose these doses because the effects of therapeutic and subtherapeutic doses of zolpidem and triazolam are variable and sometimes not signi®cant (for a review, see Rush, 1998). Thus, we wanted to test two supratherapeutic doses.…”

Section: Drug Administrationmentioning

confidence: 99%

“…A recent review of the experimental literature summarized the results of 13 published studies that directly compared the acute performance-impairing effects of zolpidem and a benzodiazepine in humans (Rush, 1998). The results of these studies were rather consistent despite the use of different methods, performance tasks, subject populations, and comparison drugs.…”

Section: Introductionmentioning

confidence: 99%

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Zolpidem and triazolam interact differentially with a delay interval on a digit‐enter‐and‐recall task

Rush

Baker

2001

Human Psychopharmacology

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Zolpidem (AMBIEN((R))), an imidazopyridine, is now the most commonly prescribed hypnotic in the United States. Zolpidem is neuropharmacologically distinct from benzodiazepine hypnotics in that it binds with low affinity to alpha(5)-containing GABA(A)-receptor subtypes. Despite its unique benzodiazepine-receptor binding profile, the results of most of the published studies conducted with humans suggest that the absolute magnitude of impairment produced by zolpidem is comparable to that observed with benzodiazepine hypnotics like triazolam. The present study compared the acute effects of zolpidem (0, 7.5, 15 and 22.5 mg) and triazolam (0, 0.1875, 0.375 and 0.5625 mg) in 10 non-drug-abusing humans using a Digit-Enter-and-Recall task with varying delay intervals (0, 10 and 20 s). To more fully characterize the behavioral effects of zolpidem and triazolam, several other performance tasks and subject-rated drug-effect questionnaires were included. Zolpidem and triazolam impaired performance on the Digit-Enter-and-Recall task as a function of dose under all delay intervals. However, the dose-related effects of the drugs interacted differentially with the delay interval such that zolpidem produced significantly less impairment than triazolam following the longest delay (i.e., 20 s). Zolpidem and triazolam produced comparable dose-related impairment on the digit symbol substitution test (DSST), circular lights task, and picture recall/recognition task. Zolpidem and triazolam generally produced qualitatively and quantitatively similar subject-rated drug effects, although some between-drug differences were observed. Consistent with the pharmacokinetics of these drugs, the effects of zolpidem peaked sooner and were shorter in duration than those observed with triazolam. The results of this experiment suggest that zolpidem may have less potential than triazolam to impair recall, which may be due to differences between these compounds in terms of their benzodiazepine-receptor binding profile. The results of the present study are also concordant with previous studies that found that drugs that act at the GABA(A)-receptor complex can be differentiated based on their interaction with the delay interval on a Digit-Enter-and-Recall task. Copyright 2001 John Wiley & Sons, Ltd.

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Section: Discussionsupporting

confidence: 89%

Section: Drug Administrationmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Zolpidem and triazolam interact differentially with a delay interval on a digit‐enter‐and‐recall task

Rush

Baker

2001

Human Psychopharmacology

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“…Although zolpidem binds within the BZD binding site and induces many of the same behavioral effects as other positive modulators of the BZD site, it differs from classic BZDs in both chemical structure ( Fig. 1) and neuropharmacological profile (Rush, 1998). Zolpidem binds with high affinity to GABARs containing the ␣1 subunit isoform and with low affinity for GABARs containing the ␣2 or ␣3 subunits, whereas receptors containing the ␣5 subunit are virtually zolpidem-insensitive (Pritchett and Seeburg, 1990).…”

mentioning

confidence: 99%

Structural Determinants for High-Affinity Zolpidem Binding to GABA-A receptors

Sancar

Ericksen²,

Kucken³

et al. 2007

Molecular Pharmacology

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“…Possivelmente, por ser o primeiro agonista seletivo do receptor GABA-A para a subunidade α1, foi apontado como o hipnótico mais prescrito no mundo 6 . Apresenta uma meia vida de 2,4 horas e não tem metabólitos ativos.…”

Section: Hipnóticos De 2ª Geraçãounclassified

Novos sedativos hipnóticos

Sukys-Claudino

Moraes

Tufik

et al. 2010

Rev. Bras. Psiquiatr.

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ResumoNas últimas décadas houve um esforço para o desenvolvimento de hipnóticos mais seguros e eficazes. Zolpidem, zaleplona, zopiclona, eszopiclona (drogas-z) e indiplona são moduladores do receptor GABA-A, os quais agem de forma seletiva na subunidade α1, exibindo, desta forma, mecanismos similares de ação, embora evidências recentes sugiram que a eszopiclona não seja tão seletiva para a subunidade α1 quanto o zolpidem. Ramelteon e tasimelteon são novos agentes crono-hipnóticos seletivos para os receptores de melatonina MT1 e MT2. Por outro lado, nos últimos anos, o consumo de drogas antidepressivas sedativas tem aumentado significativamente no tratamento da insônia. Como droga experimental, a eplivanserina tem sido testada como um potente agonista inverso do subtipo 5-HT 2A da serotonina, com um uso potencial na dificuldade da manutenção do sono. Outro agente farmacológico para o tratamento da insônia é o almorexant, o qual apresenta um novo mecanismo de ação envolvendo antagonismo do sistema hipocretinérgico, desta forma levando à indução do sono. Finalmente, também discutiremos o potencial papel de outras drogas gabaérgicas no tratamento da insônia.Descritores: Hipnóticos e sedativos; Efeitos fisiológicos de drogas; Receptores de melatonina; Antidepressivos; Distúrbios do início e da manutenção do sono AbstractThere has been a search for more effective and safe hypnotic drugs in the last decades. Zolpidem, zaleplon, zopiclone, eszopiclone (the z-drugs) and indiplon are GABA-A modulators which bind selectively α1 subunits, thus, exhibiting similar mechanisms of action, although recent evidence suggests that eszopiclone is not as selective for α1 subunit as zolpidem is. Ramelteon and tasimelteon are new chrono-hypnotic agents, selective for melatonin MT1 and MT2 receptors. On the other hand, the consumption of sedative antidepressant drugs is significantly increasing for the treatment of insomnia, in the last years. As an experimental drug, eplivanserin is being tested as a potent antagonist of serotonin 2-A receptors (ASTAR) with a potential use in sleep maintenance difficulty. Another recent pharmacological agent for insomnia is almorexant, which new mechanism of action involves antagonism of hypocretinergic system, thus inducing sleep. Finally we also discuss the potential role of other gabaergic drugs for insomnia. Descriptors: Hypnotics and sedatives; Physiological effects of drugs; Receptors, melatonin; Antidepressive agents; Sleep initiation and maintenance disordersIntrodução A insônia é, sem dúvida, na atualidade, o distúrbio do sono mais comum, afetando de 10 a 50% da população 1,2 . As conclusões de um consenso do National Institutes of Health (NHI) indicam que quando utilizamos como critério diagnóstico a necessidade de comprometimento ou impacto nas atividades diurnas, a prevalência da insônia cai para cerca de 10% 3 . Estima-se que cerca de 40% dos indivíduos insones apresentem comorbidade psiquiátrica 4 .Desde a década de 50, a psicofarmacologia vem evoluindo no tratamento da insônia em busca ...

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Behavioral Pharmacology of Zolpidem Relative to Benzodiazepines A Review

Cited by 258 publications

References 106 publications

Zolpidem and triazolam interact differentially with a delay interval on a digit‐enter‐and‐recall task

Zolpidem and triazolam interact differentially with a delay interval on a digit‐enter‐and‐recall task

Structural Determinants for High-Affinity Zolpidem Binding to GABA-A receptors

Novos sedativos hipnóticos

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