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Behavioural pharmacology
Published in Adam Doble, Ian L Martin, David Nutt, Calming the Brain: Benzodiazepines and related drugs from laboratory to clinic, 2020
Adam Doble, Ian L Martin, David Nutt
Zaleplon is an ultra-short acting hypnotic drug, developed from the CL 218,872 series. Its receptor selectivity is essentially the same as that of zolpidem, apart from a higher affinity for recombinant receptors containing the γ3 subunit (Dämgen and Liiddens, 1999). There is little data published on the behavioural pharmacology of zaleplon, but what information does exist suggests that it is very similar to that of zolpidem (Sanger et al, 1996; Griebel et al, 1996, 1998; Paronis et al, 2001; Noguchi et al, 2002).
Fatigue and countermeasures
Published in Nicholas Green, Steven Gaydos, Hutchison Ewan, Edward Nicol, Handbook of Aviation and Space Medicine, 2019
Nicholas Green, Steven Gaydos, Hutchison Ewan, Edward Nicol
Sleep-promoting compounds: Helpful for minimising sleep loss and subsequent fatigue; half-life of each compound should be matched to length of available sleep opportunity in order to promote sleep and minimise hangover effects; national military policies vary but the following compounds have been used: Temazepam: Useful for maintaining relatively long periods of night-time sleep for day workers or daytime sleep for night workers.Zolpidem or zaleplon: Good choices for initiating sleep and/or for shorter sleep periods.Eszopiclone: Option for intermediate-length sleep opportunities.
Psychopharmacology EMIs
Published in Michael Reilly, Bangaru Raju, Extended Matching Items for the MRCPsych Part 1, 2018
Buspirone.Chloral hydrate.Diazepam.Lorazepam.Paraldehyde.Sodium amytal.Temazepam.Zaleplon.Zolpidem.Zopiclone.
Rapid oral transmucosal delivery of zaleplon–lavender oil utilizing self-nanoemulsifying lyophilized tablets technology: development, optimization and pharmacokinetic evaluation
Published in Drug Delivery, 2022
Sarah A. Ali, Nabil A. Alhakamy, Khaled M. Hosny, Eman Alfayez, Deena M. Bukhary, Awaji Y. Safhi, Moutaz Y. Badr, Rayan Y. Mushtaq, Majed Alharbi, Bader Huwaimel, Mohammed Alissa, Sameer Alshehri, Ali H. Alamri, Taha Alqahtani
Zaleplon (ZP) is a fast-acting hypnotic drug of the pyrazolopyrimidine class with a mild adverse-effect profile. It is primarily recommended for the short-term management of insomnia (Ebbens & Verster, 2010; Manda et al., 2018). Insomnia may be described as frustration with sleep quality or quantity, trouble starting or maintaining sleep, and repeated nighttime awakenings. It affects 15% to 30% of the population at some point in their lives and is associated with depression, psychiatric illnesses, several other diseases and has significant socioeconomic consequences and is associated with a diminished quality of life (Buysse et al., 2008; Foda & Bakhaidar, 2010; Hosny & Banjar, 2013; Qaseem et al., 2016; Sakhare, 2017). Neither rebound insomnia nor dependence was observed on discontinuing zaleplon. However, sustained hypnotic efficacy was often achieved (Popescu, 2015; Dudhipala, 2016; Vermeeren et al., 2017).
GABAA receptor subtype modulators in medicinal chemistry: an updated patent review (2014-present)
Published in Expert Opinion on Therapeutic Patents, 2020
Letizia Crocetti, Gabriella Guerrini
An important category of α1-GABAA receptor modulators is represented by the so-called ‘Z-drugs’ (Figure 1), zaleplon, zolpidem, zopiclone, eszopiclone (S-enantiomer of zopiclone), marketed as Sonata®, Ambien®, Imovane®, and Lunesta®, respectively, that are structurally not related to classical benzodiazepines showing a pyrazolopyrimidine, imidazopyridine, and pyrrolopyrazine scaffold. Due to their preferential selectivity and efficacy at α1-containing GABAAR, they exhibit sedative properties, thus becoming the drugs of first choice in the treatment of insomnia from the 1990 s [31]. In the pharmacological treatment of insomnia is generally required to reduce sleep latency, increase sleep maintenance, improve sleep quality without affecting the next-day working state of patients. Pharmacokinetic studies and clinical trial outcomes indicate, for example, that zaleplon could be used for those patients with difficult to fall asleep but not for patients with sleep maintenance difficulties. Zolpidem improves sleep duration and the use of these drugs is convenient for its short duration of action and reduced sedation upon waking. Racemic zopiclone reduces sleep latency and increases total sleep time but its utility is limited since it impairs next-day functioning. In addition to preferential modulation at α1-containing GABAAR, racemic zoplicone also significant binds other GABAAR subtypes; thus, further pharmacological effects, it could be expected. Eszopiclone, the (S)-enantiomer of zopiclone does not affect the next-day functioning and alertness and does not show tolerance, dependence, or rebound insomnia under long-term treatment [32].
Selecting a pharmacotherapy regimen for patients with chronic insomnia
Published in Expert Opinion on Pharmacotherapy, 2020
Amanda B. Hassinger, Nikolas Bletnisky, Rizwan Dudekula, Ali A. El-Solh
For patients who are experiencing both sleep-onset and sleep-maintenance insomnia, the choices are more diverse. The treatment selection can consist of a single agent or a combination of agents with the different onset of action. Eszopiclone is particularly well suited for this insomnia phenotype given its long half-life [41]. Higher doses (2 to 3 mg) are more effective for sleep maintenance, whereas lower doses (1 to 2 mg) are suitable for difficulty in falling asleep. Eszopiclone is among the few hypnotics that have been studied in double-blind, placebo-controlled, randomized trials of nightly administration for a period of 6 months [42] and is approved for the long-term treatment of sleep-onset and sleep-maintenance insomnia. One common adverse effect of eszopiclone is an unpleasant taste that affects nearly one-third of patients at the maximum recommended dosage [41]. Other agents that may be considered for chronic insomnia include zaleplon for sleep-onset insomnia and zolpidem CR for both sleep onset and sleep-maintenance insomnia. Both long-term trials of zaleplon and controlled-release (CR) zolpidem have shown a sustained response with no tolerance and dependence after 6 months of daily use [43,44]. The sedating profile of Zolpidem CR (6.25 and 12.5 mg dose) is attributed to its unique composite preparation which has a component that releases immediately and a component that is slowly released, allowing higher blood levels later in the sleep cycle. Notwithstanding the favorable safety profile of non-benzodiazepines compared to traditional benzodiazepines, a series of case reports have raised concerns about complex sleep-related behaviors (e.g. sleep walking, sleep driving) that have been linked to serious bodily injuries [45]. In response, the FDA has issued a black box warning recommending to avoid using these agents in patients who have previously experienced similar nocturnal episodes [46].