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Sedative and Hypnotic Drugs
Published in Sahab Uddin, Rashid Mamunur, Advances in Neuropharmacology, 2020
Arup Kumar Misra, Pramod Kumar Sharma
Eszopiclone, an S(+) enantiomer of zopiclone acts by enhancing the benzodiazepine binding site of GABAA receptor to promote its positive effects on sleep (Benjamin, 2006). It is usually used for long-term management of insomnia (nearly 12 months), thus differs its pharmacological actions from other Z compounds. It maintains sleep and also decreases the time to fall asleep. It has bioavailability of about 80%. Nearly 50–60% of its drug is bound to plasma proteins with a plasma half-life of nearly 6 h. Hepatic cytochromes CYP3A4 enzymes metabolized the drug to inactive metabolites, namely, N-oxide derivative and desmethyl eszopiclone, respectively (Benjamin, 2006). In elderly, the excretion of the drug is prolonged due to increase in elimination half-life. Eszopiclone administered with CYP3A4 inhibitors (e.g., ketoconazole, erythromycin, etc.) decrease its metabolism thus increasing its elimination half-life, whereas if coadministered with inducers of CYP3A4 (e.g., rifampin), the hepatic metabolism will increase leading to decrease in elimination half-life. The drug is available in the dosage of 1 mg, 2 mg, and 3 mg tablets. No tolerance or withdrawal syndrome is seen on discontinuation of the drug. Minor symptoms of withdrawal like abnormal dreams, anxiety, nausea, and upset stomach are seen in less than 2% of the patients taking the drug for management of sleep disorder (Atkin et al., 2018).
Olfaction in Palliative Care Patients
Published in Victor R. Preedy, Handbook of Nutrition and Diet in Palliative Care, 2019
Sagit Shushan, Arkadi Yakirevitch
Drugs in many major pharmacological categories (dopaminergic antagonists, gamma-aminobutyric acid [GABA]-ergic agonists, calcium channel blockers and some orally active local anaesthetic, antiarrhythmic drugs) can impair olfactory function (Henkin 1994) and do so more commonly than presently appreciated. Table 17.3 shows some medications that were reported to alter smell and/or taste. Impairment usually affects sensory function at a molecular level by drug inactivation of receptor function through inhibition of tastant/odorant receptor, causing two major perceptual modifications: decreased perception (i.e., hyposmia or anosmia) and/or perception distortion (i.e., dysosmia) (Table 17.1). Those modifications can impair appetite and food intake, trigger significant lifestyle changes and may even require discontinuation of drug administration. Some sleep-inducing agents are associated with taste and, in rare instances, smell disturbances as potential adverse effects. Zolpidem is listed in the Physicians’ Desk Reference as producing “taste perversion” and, more infrequently, “parosmia” (Physicians’ Desk Reference 2005). Eszopiclone, a nonbenzodiazepine pyrrolopyrazine derivative of the cyclopyrrolone class, is associated with complaints of “unpleasant taste” (Krystal et al. 2003).
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.
Pharmacological and non-pharmacological treatment options for sleep disturbances in Alzheimer’s disease
Published in Expert Review of Neurotherapeutics, 2023
Binish Javed, Amaan Javed, Chia Siang Kow, Syed Shahzad Hasan
Zopiclone and Zolpidem are Z-drugs frequently prescribed for insomnia in patients with late-onset Alzheimer’s disease. Louzada et al. [61], in a randomized triple-blind placebo-controlled trial, showed that zopiclone (81-minute decrease in main nocturnal sleep duration (MNSD); 26-minute drop in awake time after sleep onset (WASO)) and zolpidem (no significant difference in MNSD; 22-minute drop in WASO) had clinical benefit when used short-term even though there was a need for further evaluation of safety. In a prospective study by Huo et al. [62], eszopiclone improved sleep quality and cognition in elderly patients with dementia and insomnia. A usual daily oral dose of Zolpidem is 5–10 mg, and the usual daily maximum dose is 10 mg. The usual dosage of Zopiclone is 2–3 mg, with a usual daily maximum of 3 mg [5].
Insomnia and menopause: a narrative review on mechanisms and treatments
Published in Climacteric, 2020
P. Proserpio, S. Marra, C. Campana, E. C. Agostoni, L. Palagini, L. Nobili, R. E. Nappi
A short-term treatment (2–4 weeks) with short-acting benzodiazepines (triazolam, brotizolam) or Z-drugs (zolpidem, zoplicone, zaleplon) may be an efficacious approach11,62. In the general population, a buffered zolpidem sublingual formulation is approved to be taken in the middle of the night by patients with early awakening insomnia and at least 4 h of bedtime remaining. RCTs in menopause women are only available for Z-drugs. Zolpidem has been shown to increase reported total sleep time and decrease the wake time after sleep onset and number of awakenings in perimenopausal or postmenopausal women, without causing tolerance110. Similarly, eszopiclone resulted effective in the treatment of both insomnia and VMS in two RCTs111,112.
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].