Ramelteon: profile of a new sleep-promoting medication

Abstract

To date the mainstay of the pharmacological treatment of insomnia has involved the modulation of the gabaminergic system via benzodiazepines or the Z-drugs, zolpidem, zopiclone or zaleplon. A new approach has explored the melatoninergic system, namely activation of MT1 and MT2 receptors in the suprachiasmatic nucleus of the hypothalamus. Ramelteon (TAK-375) is a novel sleep-promoting agent that acts as an agonist at these receptors; its preclinical pharmacology, mode of action, pharmacokinetics, drug interactions, clinical efficacy, and safety and tolerability are reviewed here.