NDLI: Melatonin and melatonergic drugs on sleep: possible mechanisms of action.

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Melatonin and melatonergic drugs on sleep: possible mechanisms of action.

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Melatonin and melatonergic drugs on sleep: possible mechanisms of action.

Content Provider	World Health Organization (WHO)-Global Index Medicus
Author	Srinivasan, Venkataramanujan Pandi-Perumal, Seithikurippu R. Trahkt, Ilya Spence, D. Warren Poeggeler, Burkhard Hardeland, Ruediger Cardinali, Daniel P.
Description	Country affiliation: India Author Affiliation: Srinivasan V ( SRM Medical College Hospital and Research Centre, SRM University, Kattankulathoor, Kancheepuram District, India.)
Abstract	Pineal melatonin is synthesized and secreted in close association with the light/dark cycle. The temporal relationship between the nocturnal rise in melatonin secretion and the 'opening of the sleep gate' (i.e., the increase in sleep propensity at the beginning of the night), coupled with the sleep-promoting effects of exogenous melatonin, suggest that melatonin is involved in the regulation of sleep. The sleep-promoting and sleep/wake rhythm regulating effects of melatonin are attributed to its action on MT(1) and MT(2) melatonin receptors present in the suprachiasmatic nucleus (SCN) of the hypothalamus. Animal experiments carried out in rats, cats, and monkeys have revealed that melatonin has the ability to reduce sleep onset time and increase sleep duration. However, clinical studies reveal inconsistent findings, with some of them reporting beneficial effects of melatonin on sleep, whereas in others only marginal effects are documented. Recently a prolonged-release 2-mg melatonin preparation (Circadin(TM)) was approved by the European Medicines Agency as a monotherapy for the short-term treatment of primary insomnia in patients who are aged 55 or above. Several melatonin derivatives have been shown to increase nonrapid eye movement (NREM) in rats and are of potential pharmacological importance. So far only one of these melatonin derivatives, ramelteon, has received approval from the U.S. Food and Drug Administration to be used as a sleep promoter. Ramelteon is a novel MT(1) and MT(2) melatonergic agonist that has specific effects on melatonin receptors in the SCN and is effective in promoting sleep in experimental animals such as cats and monkeys. In clinical trials, ramelteon reduced sleep onset latency and promoted sleep in patients with chronic insomnia, including an older adult population. Both melatonin and ramelteon promote sleep by regulating the sleep/wake rhythm through their actions on melatonin receptors in the SCN, a unique mechanism of action not shared by any other hypnotics. Moreover, unlike benzodiazepines, ramelteon causes neither withdrawal effects nor dependence. Agomelatine, another novel melatonergic antidepressant in its final phase of approval for clinical use, has been shown to improve sleep in depressed patients and to have an antidepressant efficacy that is partially attributed to its effects on sleep-regulating mechanisms.
File Format	HTM / HTML
ISSN	00207454
Issue Number	6
Volume Number	119
e-ISSN	15435245
Journal	International Journal of Neuroscience
Language	English
Publisher	Taylor & Francis
Publisher Date	2009-01-01
Publisher Place	Great Britain (UK)
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	Discipline Neurology Acetamides Pharmacology Indenes Melatonin Sleep Drug Effects Aging Animals Antidepressive Agents Circadian Rhythm Depressive Disorder Drug Therapy Humans Hypnotics And Sedatives Biosynthesis Physiology Receptors, Melatonin Agonists Metabolism Signal Transduction Sleep Initiation And Maintenance Disorders Physiopathology Suprachiasmatic Nucleus Journal Article Review
Content Type	Text
Resource Type	Article
Subject	Neuroscience Medicine

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