Eszopiclone for Insomnia

Melton, Sarah T.; Wood, Jill M.; Kirkwood, Cynthia K.

doi:10.1345/aph.1g179

Cited by 28 publications

(5 citation statements)

References 6 publications

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“…The nonbenzodiazepine compound zolpidem first became available in the 1990s and now is the most widely prescribed hypnotic worldwide 46–48 . Although zolpidem and eszopiclone do not have benzodiazepine structures, their clinical action is nonetheless explained by interaction with the GABA‐benzodiazepine receptor complex 49–52 …”

Section: Discussionmentioning

confidence: 99%

Age and Gender Effects on the Pharmacokinetics and Pharmacodynamics of Ramelteon, a Hypnotic Agent Acting via Melatonin Receptors MT₁ and MT₂

Greenblatt¹,

Harmatz²,

Karim³

2007

The Journal of Clinical Pharma

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Effects of age and gender on the pharmacokinetics and pharmacodynamics of ramelteon, a hypnotic acting via binding to melatonin MT(1) and MT(2) receptors, were evaluated in healthy young (18-34 years) and elderly (63-79 years) volunteers. Part 1 evaluated the pharmacokinetics of open-label oral ramelteon, 16 mg. Part 2 was a double-blind, randomized, 2-trial crossover pharmacodynamic study of 16-mg ramelteon and matching placebo. Ramelteon clearance was significantly reduced in elderly vs young volunteers (384 vs 883 mL/min/kg, P<.01) and half-life significantly increased (1.9 vs 1.3 h, P<.001). Gender did not significantly influence clearance or half-life. Ramelteon was extensively transformed to its hydroxylated M-II metabolite, with serum AUC values averaging about 30 times those of the parent drug. Compared to placebo, ramelteon increased self- and observer-rated sedation, but age and gender did not influence the magnitude of the ramelteon-placebo difference. Ramelteon did not significantly impair digit-symbol substitution test performance or impair information acquisition and recall. Thus, the reduced clearance and higher serum levels of ramelteon in elderly subjects were not associated with enhanced pharmacodynamic effects. The usually recommended clinical dose of ramelteon (8 mg) does not require modification based on age or gender.

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Section: Discussionmentioning

confidence: 99%

Age and Gender Effects on the Pharmacokinetics and Pharmacodynamics of Ramelteon, a Hypnotic Agent Acting via Melatonin Receptors MT₁ and MT₂

Greenblatt¹,

Harmatz²,

Karim³

2007

The Journal of Clinical Pharma

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“…Eszopiclone (Box 1), the S-enantiomer of racemic zopiclone, became available as a prescription hypnotic drug in the United States in December 2004 [1][2][3][4][5][6]. The extent of use has been relatively constant over the last 5 years, with retail prescriptions in the range of 5 to 6 million per year, and total retail costs reaching nearly US$1 billion ( Figure 1) [7,8].…”

Section: Introductionmentioning

confidence: 99%

Pharmacokinetic evaluation of eszopiclone: clinical and therapeutic implications

Greenblatt

Zammit

2012

Expert Opinion on Drug Metabolism & Toxicology

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Eszopiclone is metabolized mainly by Cytochrome P450-3A (CYP3A) isoforms. The mean half-life in healthy nonelderly individuals (6.1 h) is prolonged in the elderly, in patients with hepatic insufficiency, and by coadministration of CYP3A inhibitors. In clinical trials, eszopiclone consistently improves sleep maintenance relative to placebo, based on measures of shortened wake time after sleep onset, and prolonged total sleep time. However eszopiclone may also produce residual sedation and impairment of driving performance in the initial morning waking hours. A bitter or metallic taste is a common though non-serious adverse effect of eszopiclone. Overall, eszopiclone provides a therapeutic option for patients with sleep maintenance problems, though with accompanying potential for residual morning sedation, as well as a relatively high dollar cost of treatment.

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“…As shown by animal studies, the (S)-enantiomer of racemic zopiclone is the one of two stereoisomers that mainly mediates its hypnotic e ects (Melton 2005;Hair 2008). Accordingly, recommended clinical dosages are about 50% lower for eszopiclone compared to racemic zopiclone (Greenblatt 2012).…”

Section: Cochrane Database Of Systematic Reviewsmentioning

confidence: 99%

Eszopiclone for insomnia

Rösner

Englbrecht

Wehrle³

et al. 2018

Cochrane Database of Systematic Reviews

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BackgroundInsomnia is a major public health issue a ecting between 6% to 10% of the adult population in Western countries. Eszopiclone is a hypnotic drug belonging to a newer group of hypnotic agents, known as new generation hypnotics, which was marketed as being just as e ective as benzodiazepines for this condition, while being safer and having a lower risk for abuse and dependence. It is the aim of the review to integrate evidence from randomised controlled trials and to draw conclusions on eszopiclone's e icacy and safety profile, while taking methodological features and bias risks into consideration. ObjectivesTo assess the e icacy and safety of eszopiclone for the treatment of insomnia compared to placebo or active control. Search methodsWe searched the Cochrane Central Register of Controlled trials (CENTRAL), MEDLINE, Embase, PsycINFO, PSYNDEX and registry databases (WHO trials portal, ClinicalTrials.gov) with results incorporated from searches to 10 February 2016. To identify trials not registered in electronic databases, we contacted key informants and searched reference lists of identified studies. We ran an update search (21 February 2018) and have placed studies of interest in awaiting classification/ongoing studies. These will be incorporated into the next version of the review, as appropriate. Selection criteriaParallel group randomised controlled trials (RCTs) comparing eszopiclone with either placebo or active control were included in the review. Participants were adults with insomnia, as diagnosed with a standardised diagnostic system, including primary insomnia and comorbid insomnia. Data collection and analysisTwo authors independently extracted outcome data; one reviewer assessed trial quality and the second author cross-checked it. Main resultsA total of 14 RCTs, with 4732 participants, were included in this review covering short-term (≤ 4 weeks; 6 studies), medium-term (> 4 weeks ≤ 6 months; 6 studies) and long-term treatment (> 6 months; 2 studies) with eszopiclone. Most RCTs included in the review included participants aged between 18 and 64 years, three RCTs only included elderly participants (64 to 85 years) and one RCT included participants with a broader age range (35 to 85 years). Seven studies considered primary insomnia; the remaining studies considered secondary insomnia comorbid with depression (2), generalised anxiety (1), back pain (1), Parkinson's disease (1), rheumatoid arthritis (1) and menopausal transition (1).

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Eszopiclone for Insomnia

Cited by 28 publications

References 6 publications

Age and Gender Effects on the Pharmacokinetics and Pharmacodynamics of Ramelteon, a Hypnotic Agent Acting via Melatonin Receptors MT₁ and MT₂

Age and Gender Effects on the Pharmacokinetics and Pharmacodynamics of Ramelteon, a Hypnotic Agent Acting via Melatonin Receptors MT₁ and MT₂

Pharmacokinetic evaluation of eszopiclone: clinical and therapeutic implications

Eszopiclone for insomnia

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Eszopiclone for Insomnia

Cited by 28 publications

References 6 publications

Age and Gender Effects on the Pharmacokinetics and Pharmacodynamics of Ramelteon, a Hypnotic Agent Acting via Melatonin Receptors MT1 and MT2

Age and Gender Effects on the Pharmacokinetics and Pharmacodynamics of Ramelteon, a Hypnotic Agent Acting via Melatonin Receptors MT1 and MT2

Pharmacokinetic evaluation of eszopiclone: clinical and therapeutic implications

Eszopiclone for insomnia

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Product

Resources

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Age and Gender Effects on the Pharmacokinetics and Pharmacodynamics of Ramelteon, a Hypnotic Agent Acting via Melatonin Receptors MT₁ and MT₂

Age and Gender Effects on the Pharmacokinetics and Pharmacodynamics of Ramelteon, a Hypnotic Agent Acting via Melatonin Receptors MT₁ and MT₂