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Ramelteon

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Ramelteon Basic information
Ramelteon Chemical Properties
  • Melting point:113-1150C
  • alpha D20 -57.8° (c = 1.004 in chloroform)
  • Boiling point:455.3±24.0 °C(Predicted)
  • Density 1.119±0.06 g/cm3(Predicted)
  • Flash point:2℃
  • storage temp. -20°C Freezer
  • pka16.37±0.46(Predicted)
  • InChIKeyYLXDSYKOBKBWJQ-LBPRGKRZSA-N
  • CAS DataBase Reference196597-26-9(CAS DataBase Reference)
Safety Information
Ramelteon Usage And Synthesis
  • DescriptionUnlike most treatments of insomnia that target the GABA (g-aminobutyric acid) receptor complex, ramelteon is an agonist of the melatonin receptor. In particular, it has high selectivity for the MT1 and MT2 subtypes, which have been implicated in the maintenance of circadian rhythms, over the MT3 receptor responsible for other melatonin functions. Its lack of affinity for not only the GABA receptor complex but also neurotransmitter, dopaminerigic, opiate, and benzodiazepine receptors suggests an improved safety profile devoid of the abuse potential of the hypnotic drugs that target these receptors. As such, ramelteon is not a scheduled drug. Primary metabolites include hydroxylation and oxidation to carbonyl species with secondary metabolites resulting from glucuronidation. Since CYP1A2 is the major isozyme involved in the hepatic metabolism of ramelteon, it should not be taken in combination with strong CYP1A2 inhibitors, such as fluvoxamine. Co-administration with either ketoconazole (a CYP3A4 inhibitor) or fluconazole (a potent CYP2C9 inhibitor) resulted in significant increases in AUC and Cmax, but the extensive metabolism and highly variable plasma concentrations of ramelteon precluded the need for dose modification. The package insert, however, cautions patients about co-administration with potent CYP3A4 and CYP2C9 inhibitors. Based on the result of the clinical trials, the recommended dose of ramelteon is 8mg taken within 30 min of going to bed. In addition to the precaution of co-administration with CYP inhibitors, it should not be used in patients with severe hepatic impairment. The adverse events, observed in 5% of patients in clinical studies, were somnolence, dizziness, nausea, fatigue, headache, and insomnia.
  • Chemical PropertiesCrystalline Solid
  • OriginatorTakeda (Japan)
  • UsesMelatonin MT1/MT2 receptor agonist. Sedative, hypnotic
  • Usesmelatonin receptor agonist
  • brand nameRozerem (Takeda).
  • General DescriptionThe melatonin molecule wasmodified mainly by replacing the nitrogen of the indole ringwith a carbon to give an indane ring and by incorporating 5-methoxyl group in the indole ring into a more rigid furan ring.The selectivity of the resulting ramelteon for MT1 receptor iseight times more than that of MT2 receptor. Unlike melatonin,it is more effective in initiating sleep (MT1 activity)rather than to readjust the circadian rhythm (MT2 activity). Itappears to be distinctly more efficacious than melatonin butless efficacious than benzodiazepines as a hypnotic.Importantly, this drug has no addiction liability (it is not acontrolled substance). As a result, it has recently been approvedfor the treatment of insomnia.
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