About: Ramelteon     Goto   Sponge   NotDistinct   Permalink

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http://linked.open...gbank/description
  • Ramelteon is the first in a new class of sleep agents that selectively binds to the melatonin receptors in the suprachiasmatic nucleus (SCN). It is used for insomnia, particularly delayed sleep onset. Ramelteon has not been shown to produce dependence and has shown no potential for abuse. (en)
http://linked.open...y/drugbank/dosage
http://linked.open...generalReferences
  • # Karim A, Tolbert D, Cao C: Disposition kinetics and tolerance of escalating single doses of ramelteon, a high-affinity MT1 and MT2 melatonin receptor agonist indicated for treatment of insomnia. J Clin Pharmacol. 2006 Feb;46(2):140-8. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16432265 # Miyamoto M: Pharmacology of ramelteon, a selective MT1/MT2 receptor agonist: a novel therapeutic drug for sleep disorders. CNS Neurosci Ther. 2009 Winter;15(1):32-51. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/19228178 # Pandi-Perumal SR, Srinivasan V, Spence DW, Moscovitch A, Hardeland R, Brown GM, Cardinali DP: Ramelteon: a review of its therapeutic potential in sleep disorders. Adv Ther. 2009 Jun;26(6):613-26. Epub 2009 Jun 30. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/19568703 # Borja NL, Daniel KL: Ramelteon for the treatment of insomnia. Clin Ther. 2006 Oct;28(10):1540-55. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17157111 # Roth T, Stubbs C, Walsh JK: Ramelteon (TAK-375), a selective MT1/MT2-receptor agonist, reduces latency to persistent sleep in a model of transient insomnia related to a novel sleep environment. Sleep. 2005 Mar 1;28(3):303-7. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16173650 # Simpson D, Curran MP: Ramelteon: a review of its use in insomnia. Drugs. 2008;68(13):1901-19. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/18729542 (en)
http://linked.open...gy/drugbank/group
  • approved (en)
  • investigational (en)
http://linked.open...drugbank/halfLife
  • ~1-2.6 hours (en)
http://linked.open...ugbank/indication
  • For the treatment of insomnia characterized by difficulty with sleep onset. (en)
http://linked.open...bank/manufacturer
sameAs
Title
  • Ramelteon (en)
adms:identifier
http://linked.open...mechanismOfAction
  • Ramelteon is a melatonin receptor agonist with both high affinity for melatonin MT<sub>1</sub> and MT<sub>2</sub> receptors, and lower selectivity for the MT<sub>3</sub> receptor. Melatonin production is concurrent with nocturnal sleep, meaning that an increase in melatonin levels is related to the onset of self-reported sleepiness and an increase in sleep propensity. MT<sub>1</sub> receptors are believed to be responsible for regulation of sleepiness and facilitation of sleep onset, and MT<sub>2</sub> receptors are believed to mediate phase-shifting effects of melatonin on the circadian rhythm. While MT<sub>1</sub> and MT<sub>2</sub> receptors are associated with the sleep-wake cycle, MT<sub>3</sub> has a completely different profile, and therefore is not likely to be involved in the sleep-wake cycle. Remelteon has no appreciable affinity for the gamma-aminobutyric acid (GABA) receptor complex or receptors that bind neuropeptides, cytokines, serotonin, dopamine, norepinephrine, acetylcholine, or opiates. (en)
http://linked.open...drugbank/packager
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http://linked.open...outeOfElimination
  • Following oral administration of radiolabeled ramelteon, 84% of total radioactivity was excreted in urine and approximately 4% in feces, resulting in a mean recovery of 88%. Less than 0.1% of the dose was excreted in urine and feces as the parent compound. (en)
http://linked.open.../drugbank/synonym
  • Rozerem (en)
http://linked.open...umeOfDistribution
  • * 73.6 L (en)
http://linked.open...k/foodInteraction
  • Avoid alcohol. (en)
  • Do not take with or immediately after a high-fat meal. (en)
http://linked.open...nk/proteinBinding
  • ~82% (in human serum) (en)
http://linked.open...ynthesisReference
  • Vinod Kumar Kansal, Dhirenkumar N. Mistry, Sanjay L. Vasoya, "Intermediates and processes for the synthesis of Ramelteon." U.S. Patent US20080242877, issued October 02, 2008. (en)
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http://linked.open...ugbank/absorption
  • Rapid, total absorption is at least 84%. (en)
http://linked.open.../affectedOrganism
  • Humans and other mammals (en)
http://linked.open...casRegistryNumber
  • 196597-26-9 (en)
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