Pharmacology of Ramelteon, a Selective MT1/MT2 Receptor Agonist: A Novel Therapeutic Drug for Sleep Disorders
Open Access
- 13 February 2009
- journal article
- review article
- Published by Wiley in CNS Neuroscience & Therapeutics
- Vol. 15 (1), 32-51
- https://doi.org/10.1111/j.1755-5949.2008.00066.x
Abstract
An estimated one-third of the general population is affected by insomnia, and this number is increasing due to more stressful working conditions and the progressive aging of society. However, current treatment of insomnia with hypnotics, gamma-aminobutyric acid A (GABAA) receptor modulators, induces various side effects, including cognitive impairment, motor disturbance, dependence, tolerance, hangover, and rebound insomnia. Ramelteon (Rozerem; Takeda Pharmaceutical Company Limited, Osaka, Japan) is an orally active, highly selective melatonin MT1/MT2 receptor agonist. Unlike the sedative hypnotics that target GABAA receptor complexes, ramelteon is a chronohypnotic that acts on the melatonin MT1 and MT2 receptors, which are primarily located in the suprachiasmatic nucleus, the body's “master clock.” As such, ramelteon possesses the first new therapeutic mechanism of action for a prescription insomnia medication in over three decades. Ramelteon has demonstrated sleep-promoting effects in clinical trials, and coupled with its favorable safety profile and lack of abuse potential or dependence, this chronohypnotic provides an important treatment option for insomnia.Keywords
This publication has 106 references indexed in Scilit:
- The Efficacy and Safety of Drug Treatments for Chronic Insomnia in Adults: A Meta-analysis of RCTsJournal of General Internal Medicine, 2007
- A 2-night, 3-period, crossover study of ramelteon's efficacy and safety in older adults with chronic insomniaCurrent Medical Research and Opinion, 2007
- Effects of ramelteon on patient-reported sleep latency in older adults with chronic insomniaSleep Medicine, 2006
- Ramelteon (TAK-375) Accelerates Reentrainment of Circadian Rhythm after a Phase Advance of the Light-Dark Cycle in RatsJournal of Biological Rhythms, 2005
- Melatonin Treatment of Day-Night Rhythm Disturbances and Sundowning in Alzheimer DiseaseJournal of Clinical Psychopharmacology, 2004
- New Drugs for InsomniaDrug Safety, 2003
- Mammalian melatonin receptors: molecular biology and signal transductionCell and tissue research, 2002
- Improvement of sleep quality by controlled-release melatonin in benzodiazepine-treated elderly insomniacsArchives of Gerontology and Geriatrics, 1997
- Circadian rhythm abnormalities in totally blind people: incidence and clinical significanceJournal of Clinical Endocrinology & Metabolism, 1992
- ISOLATION OF MELATONIN, THE PINEAL GLAND FACTOR THAT LIGHTENS MELANOCYTES1Journal of the American Chemical Society, 1958