Ramelteon: a review of its use in insomnia

Drugs. 2008;68(13):1901-19. doi: 10.2165/00003495-200868130-00011.


Ramelteon (Rozerem) is the first melatonin receptor agonist to be approved for the treatment of insomnia; it is not classified as a controlled substance. In patients with chronic insomnia, objectively assessed latency to persistent sleep (LPS) at week 1 was improved with oral ramelteon 8 mg administered 30 minutes before bedtime, compared with placebo, and this effect was maintained throughout the duration of 5-week and 6-month clinical studies. Subjectively assessed sleep latency (sSL) improved in some, but not all, studies. When a statistically significant improvement in sSL occurred at week 1, the effect was maintained throughout the duration of the 5-week studies, but not at all timepoints throughout a 6-month study. Improvements in objectively assessed total sleep time (TST) and sleep efficiency (SE) were only reported during the first week of treatment. Improvements in other objective or subjective measures of sleep were not consistent. Ramelteon was generally well tolerated, did not impair next-day cognitive or motor performance and was not associated with withdrawal symptoms, rebound insomnia or abuse potential. Thus, ramelteon provides a well tolerated option for the treatment of patients with insomnia characterized by difficulty in sleep onset.

Publication types

  • Review

MeSH terms

  • Administration, Oral
  • Area Under Curve
  • Clinical Trials as Topic
  • Half-Life
  • Humans
  • Indenes / administration & dosage
  • Indenes / pharmacokinetics
  • Indenes / therapeutic use*
  • Receptor, Melatonin, MT1 / agonists
  • Receptor, Melatonin, MT2 / agonists
  • Sleep Initiation and Maintenance Disorders / drug therapy*
  • Sleep Initiation and Maintenance Disorders / metabolism
  • Treatment Outcome


  • Indenes
  • Receptor, Melatonin, MT1
  • Receptor, Melatonin, MT2
  • ramelteon