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The story of modern tranquilliser drugs
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
Melatonin has been promoted as a useful treatment for certain sleep disorders, but again, hard evidence of efficacy is lacking. Melatonin is freely available from pharmacies in many countries and is widely used even though it has never been approved by regulatory agencies for such purposes. Several pharmaceutical companies are actively investigating melatonin receptor agonists for the treatment of sleep disorders.
Sleep Disorders in Older Adults
Published in K. Rao Poduri, Geriatric Rehabilitation, 2017
Armando Miciano, David Berbrayer
The benzodiazepines are psychoactive drugs with varying hypnotic, sedative, anxiolytic, anticonvulsant, muscle relaxant, and amnestic properties. Nonbenzodiazepines, also called benzodiazepine receptor agonists, are comparatively new drugs whose actions are similar to those of the benzodiazepines, although they are structurally unrelated. The one approved melatonin receptor agonist has a different mechanism of action. Melatonin receptors, acted upon by endogenous melatonin, are thought to be involved in the maintenance of the circadian rhythm underlying the normal sleep–wake cycle.
Depression, Anxiety, and Apathy
Published in Marc E. Agronin, Alzheimer's Disease and Other Dementias, 2014
It is generally wise to avoid use of both short-acting benzodiazepines such as triazolam and alprazolam due to their potential for paradoxical effects. Diphenhydramine should also be avoided in light of its problematic anticholinergic and anti-histaminic side effects, including excess sedation, dizziness, and confusion. A safer over-the-counter agent is melatonin, which has shown efficacy and minimal side effects in treating insomnia in elderly subjects (Wade, Ford, & Crawford, 2007). There is also the melatonin-receptor agonist ramelteon, which can take several weeks to have a full effect. Low dose doxepin is also being marketed as a sleeping pill, although there is a risk for anticholinergic effects since it is a TCA. Recommended dosing for all of these agents appears in Table 10.3.
Advances in the pharmacological management of non-24-h sleep-wake disorder
Published in Expert Opinion on Pharmacotherapy, 2021
Shohei Nishimon, Naoya Nishino, Seiji Nishino
With regards to pharmacological therapy, melatonin receptor agonists to resynchronize the circadian phase shift are recommended [52–54]. Melatonin can activate the MT1 and MT2 receptors in the SCN [25], and as previously mentioned, the MT1 and MT2 receptors are also expressed in other brain regions and peripheral tissues. Endogenous melatonin regulates various functions, including circadian rhythm and sleep-wake cycle, body temperature, endocrine function, vascular system, immunomodulation, anticancer activity, skin pigmentation, hair growth, and aging [31,55]. Exogenous melatonin, including melatonin receptor agonists, is available for the treatment of insomnia, mood disorder, and circadian rhythm sleep disorder, and is likely to be effective in treating non-24 [56–58]. Of note, tasimelteon is the only approved medication by the US Food and Drug Administration (FDA) and the European Medicines Agency (EMA) for the treatment of non-24 [53]. Available melatonin receptor agonists bind to the MT1 and MT2 receptors, and each agonist has a different binding affinity [59], thereby resulting in several significant pharmacodynamic and pharmacokinetic differences in the mediation of melatonin agonistic effects (Tables 2 and Tables 3).
Efficacy of agomelatine with cognitive behavioral therapy for delayed sleep-wake phase disorder in young adults: A randomized controlled study
Published in Behavioral Sleep Medicine, 2023
Ying Yu, Yan Chen, Long Ma, You-Yang Qu, Yu-Nong Li, Ying Peng, Yu-Lan Zhu, Jia He, Hai-Yan Gou, Yan-Mei Zhu
Current treatments for DSWPD include medication, chronotherapy, phototherapy, and cognitive behavior therapy (Feder & Baroni, 2021). However, clinical trials evaluating the therapeutic effects of DSWPD are rare. Melatonin treatment protocols for DSWPD vary in dose, formulation, and timing of melatonin, and they may lead to low compliance, thus limiting translation into clinical practice. Previous studies have reported that melatonin treatment is about 50% effective rate, and therefore half of the DSWPD patients resist melatonin treatment (Sletten et al., 2018). As light therapy requires patients to wake up early, but patients with severe DSWPD often fail to wake up in the morning, the actual effect of light therapy is minimal (Danielsson et al., 2018). There are no randomized controlled trials evaluating the efficacy of chronotherapy for DSWPD, and the evidence for this treatment is limited to case studies with unsatisfactory results (Alvarez et al., 1992; Czeisler et al., 1981; Ito et al., 1993). Nevertheless, the American Academy of Sleep Medicine (AASM) recommends that patients with DSWPD may be treated with strategic melatonin therapy (usually between 7 and 9 P.M.) rather than no treatment (Culnan et al., 2019). The French Medical and Research Sleep Society (SFRMS) decides that there are no standard dosages and recommend dosage be increased from 0.5 to 5 mg (Quera-Salva et al., 2021). Agomelatine is a novel melatonin receptor agonist that acts by resynchronizing circadian rhythms (Mairesse et al., 2013). Preliminary evidence indicates that agomelatine can advance phase and decrease latency to sleep onset in patients (Burgess & Emens, 2020).
Tasimelteon for treating non-24-h sleep-wake rhythm disorder
Published in Expert Opinion on Pharmacotherapy, 2019
Shohei Nishimon, Mari Nishimon, Seiji Nishino
Finally, we make a proposal about the future subject as an expert opinion. Although previous clinical trials have investigated on comparative trials on tasimelteon versus placebo for non-24, whether tasimelteon is superior or inferior to other melatonin receptor agonists as a treatment for non-24 has not been validated. A comparative clinical trial focusing on the efficacy and safety of tasimelteon versus other melatonin receptor agonists for non-24 should be conducted in the future.