From the Guidelines
Ramelteon is a prescription sleep medication used to treat insomnia, specifically difficulty falling asleep, with a standard adult dose of 8 mg taken within 30 minutes before bedtime, as suggested by the American Academy of Sleep Medicine clinical practice guideline 1. The medication works by activating melatonin receptors in the brain, specifically the MT1 and MT2 receptors, which help regulate the body's natural sleep-wake cycle. This mechanism differs from benzodiazepines and other sedative-hypontics that work on GABA receptors. Some key points to consider when using ramelteon include:
- It should be taken on an empty stomach, as high-fat meals can reduce its effectiveness
- Common side effects include dizziness, fatigue, and somnolence
- It should be avoided in patients with severe liver disease and those taking fluvoxamine, which can increase ramelteon levels
- Unlike some sleep medications, ramelteon generally doesn't cause morning grogginess or rebound insomnia when discontinued
- For best results, it should be used alongside good sleep hygiene practices such as maintaining a regular sleep schedule and avoiding caffeine and electronics before bedtime, as recommended by the American College of Physicians guideline 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 The activity of ramelteon at the MT1 and MT2 receptors is believed to contribute to its sleep-promoting properties, as these receptors, acted upon by endogenous melatonin, are thought to be involved in the maintenance of the circadian rhythm underlying the normal sleep-wake cycle
The use of Ramelteon (Rozerem) is for its sleep-promoting properties, as it acts on the melatonin MT1 and MT2 receptors to help maintain the circadian rhythm underlying the normal sleep-wake cycle.
- Key points:
- Ramelteon is a melatonin receptor agonist
- It has high affinity for MT1 and MT2 receptors
- It helps maintain the circadian rhythm underlying the normal sleep-wake cycle
- It is used for its sleep-promoting properties 2
From the Research
Use of Ramelteon (Rozerem)
Ramelteon is a selective melatonin receptor (MT(1) and MT(2)) agonist that has been approved by the US Food and Drug Administration for the treatment of insomnia characterized by difficulty with sleep onset 3. The primary use of ramelteon is to enhance sleep through effects on sleep regulatory mechanisms within the suprachiasmatic nucleus, without having a direct sedating effect.
Key Benefits
- Ramelteon has been shown to reduce latency to persistent sleep (LPS) in patients with chronic insomnia 4, 5
- It is well tolerated and does not impair next-day cognitive or motor performance 4, 6
- Ramelteon is not associated with withdrawal symptoms, rebound insomnia, or abuse potential 3, 4, 6
- It is available as an 8 mg tablet, which should be taken approximately 30 minutes prior to bedtime 3
Efficacy in Specific Populations
- In elderly patients with primary insomnia, ramelteon has been shown to reduce subjective LPS and improve total sleep time (TST) 4, 7
- In older adults with severe sleep-onset difficulty, ramelteon 8 mg significantly reduced subjective sleep latency (sSL) at week 1, and this effect was sustained at weeks 3 and 5 7