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

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

CLICK HERE for subscription information about this journal.

Nat Clin Pract Neurol. 2007;3(4):221-228. © 2007 Nature Publishing Group

Cite this: Drug Insight: The Use of Melatonergic Agonists for the Treatment of Insomnia -- Focus on Ramelteon - Medscape - Apr 01, 2007.