Ramelteon.

Abstract

Ramelteon, approved in the US for the treatment of insomnia characterised by difficulty with sleep onset, is a highly selective agonist for the melatonin MT1/MT2 receptors, which are believed to mediate the circadian rhythm in mammals. Ramelteon has negligible affinity for the MT3 binding sites and other receptors in the brain, including the opiate, dopamine, benzodiazepine and serotonin receptors, which may explain the lack of significant adverse events and lack of abuse or dependence potential observed with ramelteon. In three clinical trials in patients with chronic insomnia, ramelteon 8mg was effective in reducing sleep latency, without being associated with any significant or clinically relevant residual effects. It also generally increased total sleep time and, where assessed, sleep efficiency. In a first-night-effect model of transient insomnia, ramelteon 8mg was significantly more effective than placebo at reducing sleep latency and increasing total sleep time. Ramelteon was generally well tolerated; the most commonly reported adverse events occurring in more ramelteon than placebo recipients were somnolence (5% vs 3%), fatigue (4% vs 2%) and dizziness (5% vs 3%). Adverse events were mostly mild or moderate in nature. Ramelteon has been shown to have no potential for abuse or dependence.

• Authors: Adam McGechan, Keri Wellington
• Journal: CNS drugs (CNS Drugs) Vol. 19 Issue 12 Pg. 1057-65; discussion 1066-7 ( 2005) ISSN: 1172-7047 [Print] New Zealand
• PMID: 16332146 (Publication Type: Journal Article, Review)

Chemical References

• Indenes
• Receptors, Melatonin
• ramelteon

Topics

• Animals
• Biotransformation
• Clinical Trials as Topic
• Drug Interactions
• Humans
• Indenes (administration & dosage, adverse effects, pharmacokinetics, therapeutic use)
• Receptors, Melatonin (drug effects)
• Sleep (drug effects)
• Sleep Initiation and Maintenance Disorders (drug therapy)
• Tissue Distribution