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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.
Sedative and Hypnotic Drugs
Published in Sahab Uddin, Rashid Mamunur, Advances in Neuropharmacology, 2020
Arup Kumar Misra, Pramod Kumar Sharma
Zolpidem, eszopiclone, and zaleplon are collectively known as “Z-drugs” though they have the same mechanism of action as benzodiazepines but they are structurally unrelated (Gregory, 2016). Ramelteon and tasimelteon are the melatonin receptor agonists which are approved by US FDA as newer hypnotics indicated for non-24-h sleep–wake disorders (Laudon, 2014). An orexin receptor antagonist, suvorexant was introduced in the market in August 2014 and is indicated to improve sleep duration. Buspirone is a slow-onset anxiolytic agent differing from the conventional sedative–hypnotics in their mechanism of action (Mendelson, 1990).
Medication effects on sleep
Published in S.R. Pandi-Perumal, Meera Narasimhan, Milton Kramer, Sleep and Psychosomatic Medicine, 2017
A number of sleep disorders are linked to abnormally timed sleep–wake cycles. These include delayed and advance sleep phase syndromes in which the sleep period is markedly later or earlier than what is socially accepted, jet lag, shift work, and certain sleep abnormalities associated with aging. Low doses of melatonin—the photoneuroendocrine transducer that conveys information controlling sleep–wake cycles and circadian rhythms in the central nervous system—may be useful in treating these disorders. Because it is marketed as a dietary supplement, there is minimal data on safety, side effects, and drug interactions for this compound.46 Jet lag and shift work disorders can also be effectively treated with bright light therapy and the repetitive shortterm use of sedative/hypnotics.47 Ramelteon and tasimelteon are melatonin receptor agonists with high affinity for melatonin MT1 and MT2 receptors in the suprachiasmatic nucleus. Ramelteon reduces sleep latency in most patients and is not a controlled substance since there is no potential for abuse. The most frequent adverse events leading to discontinuation were somnolence, dizziness, nausea, fatigue, headache, and insomnia.19
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).
Pharmacological management of post-stroke depression
Published in Expert Review of Neurotherapeutics, 2020
Luis Castilla-Guerra, Maria del Carmen Fernandez Moreno, Guadalupe Esparrago-Llorca, Miguel Angel Colmenero-Camacho
The introduction of tricyclic antidepressants (TCAs) and monoamine oxidase inhibitors in the 1950s revolutionized the treatment of depression. Since then, the search for more selective and possibly better tolerated antidepressants has continued. This movement of rational drug development gave birth to selective serotonin reuptake inhibitors (SSRIs). The ensuing years have witnessed SSRIs becoming the first-line drugs for the treatment of depression among several other indications [22]. Following the marketing success of SSRIs, many newer generation antidepressants have gained approval as treatments for depression, including but not limited to serotonin and noradrenaline reuptake inhibitors (SNRIs) (e.g. venlafaxine, desvenlafaxine, and duloxetine), bupropion (a noradrenaline and dopamine reuptake Inhibitor), mirtazapine (noradrenaline and selective serotonin antagonist) and trazodone (serotonin antagonist and reuptake inhibitor). With the exception of agomelatine (melatonin receptor agonist with 5-HT2C receptor antagonist properties), all other agents primarily act through the modulation of monoaminergic neurotransmission. More recently, new additional antidepressants, namely vilazodone, levomilnacipran, and vortioxetine have been commercialized [22,23].
Tasimelteon for treating non-24-h sleep-wake rhythm disorder
Published in Expert Opinion on Pharmacotherapy, 2019
Shohei Nishimon, Mari Nishimon, Seiji Nishino
Currently, several melatonin receptor agonists are available for the treatment of insomnia, major depression disorder, or non-24 [68,69]. However, their availability depends on the country. For example, ramelteon is approved in the US and Japan for the treatment of insomnia [70], agomelatine is approved in Europe and Canada for the treatment of major depression disorder, tasimelteon is approved in the US and Europe for the treatment of non-24. In addition, immediate-release melatonin is available over the counter in the US, whereas prolonged-release melatonin is approved in Europe and Australia for the treatment of insomnia in individuals aged ≥55 [71]. They have significant pharmacodynamic and pharmacokinetic differences in the regulation of the melatonin system [68,72].