Drug Insight: The Use of Melatonergic Agonists for the Treatment of Insomnia -- Focus on Ramelteon

Seithikurippu R Pandi-Perumal; Venkataramanujan Srinivasan; Burkhard Poeggeler; Rüdiger Hardeland; Daniel P Cardinali


Nat Clin Pract Neurol. 2007;3(4):221-228. 

In This Article

Sidebar: Key Points

  • Ramelteon acts as an MT1 and MT2 melatonin receptor agonist, showing higher affinities for these receptors than does the natural ligand

  • Ramelteon induces sleep initiation and maintenance, as demonstrated in animal models and clinical trials

  • Ramelteon is efficient in treating chronic insomnia, without causing addiction, hangover or withdrawal effects

  • Ramelteon is assumed to promote sleep efficacy by influencing homeostatic as well as chronobiotic sleep regulation

  • A major metabolite of ramelteon, which accumulates to levels 10-fold higher than the parent drug, contributes to the drug's effects

  • Safety of ramelteon seems to be sufficient after short-term administration, but long-term treatment of elderly or unwell individuals requires further study

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