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Current treatment of insomnia with hypnotics, GABA(A) receptor modulators, induces various side effects, including cognitive impairment, motor disturbance, dependence, tolerance, hang-over, and rebound insomnia. Ramelteon (Rozerem) is an orally active, highly selective melatonin MT1/MT2 receptor agonist. Unlike the sedative hypnotics that target GABA(A) receptor complexes, ramelteon is a chronohypnotic that acts on the melatonin MT1 and MT2 receptors, which are primarily located in the suprachiasmatic nucleus. Ramelteon has demonstrated sleep-promoting effects in clinical trials, and coupled with its favorable safety profile and lack of abuse potential or dependence, this chronohypnotic provides an important treatment option for insomnia.

Citation

Masaomi Miyamoto. A novel therapeutic drug: ramelteon]. Nihon rinsho. Japanese journal of clinical medicine. 2009 Aug;67(8):1595-600

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PMID: 19768947

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