From the Guidelines
Ramelteon, also known as Rozerem, is a melatonin receptor agonist that is used to treat sleep onset insomnia in adults.
Key Points
- The evidence for the effectiveness of ramelteon is weak, with marginal reduction in sleep latency and no significant improvement in sleep efficiency or sleep quality 1.
- Ramelteon is suggested for use in adults with sleep onset insomnia, based on trials of 8 mg doses 1.
- The medication has a low potential for adverse events, with no significant difference from placebo in terms of adverse effects 1.
- Commonly reported adverse events include headache, nausea, upper respiratory infection, and nasopharyngitis 1.
- There is no consistent evidence of next-day impairment associated with the use of ramelteon 1.
Dosage and Administration
- The recommended dose of ramelteon is 8 mg, taken orally before bedtime 1.
- The medication should be used with caution in older adults, as it may cause residual effects such as dizziness and somnolence 1.
Clinical Considerations
- Ramelteon may be considered for use in adults with sleep onset insomnia who have not responded to other treatments 1.
- The medication should be used in conjunction with good sleep hygiene practices, such as maintaining a consistent sleep schedule and creating a relaxing sleep environment 1.
From the FDA Drug Label
Ramelteon is a melatonin receptor agonist with both high affinity for melatonin MT1 and MT2 receptors and relative selectivity over the MT3 receptor
- Ramelteon is a melatonin receptor agonist that acts on MT1 and MT2 receptors, which are involved in the maintenance of the circadian rhythm underlying the normal sleep-wake cycle 2
- It has no appreciable affinity for other receptors, such as GABA, serotonin, dopamine, noradrenaline, acetylcholine, and opiates
- The major metabolite of ramelteon, M-II, is pharmacologically active and has a higher systemic exposure than the parent molecule
- Ramelteon is used for its sleep-promoting properties.
From the Research
Overview of Ramelteon
- Ramelteon, also known as Rozerem, is a melatonin receptor agonist approved for the treatment of insomnia characterized by difficulty falling asleep 3, 4, 5, 6, 7.
- It is a highly selective agonist for melatonin subtypes 1 and 2 receptors, which are believed to mediate the circadian rhythm in mammals 4, 5, 6.
Mechanism of Action
- Ramelteon acts specifically on MT(1) and MT(2) melatonin receptors, with negligible affinity for other receptors in the brain, including opiate, dopamine, benzodiazepine, and serotonin receptors 4, 5, 6.
- Its primary action in sleep promotion is not a generalized gamma-aminobutyric (GABA)-ergic central nervous system depression, but rather it acts as a melatonergic agonist in the suprachiasmatic nucleus (and at other central nervous system sites) 6.
Efficacy
- Ramelteon has been shown to be effective in reducing sleep latency and increasing total sleep time in patients with chronic insomnia 3, 4, 5, 6, 7.
- It has also been shown to improve sleep efficiency and reduce the number of nighttime awakenings in some studies 3, 4, 6.
Safety and Tolerability
- Ramelteon is generally well tolerated, with the most common adverse events being somnolence, dizziness, fatigue, and nausea 3, 4, 5, 6, 7.
- It is not associated with next morning hangover effects, reductions in alertness, or withdrawal symptoms 4, 6, 7.
- Ramelteon has been shown to have no potential for abuse or dependence 5, 6, 7.