Ramelteon
Hypnotic medication / From Wikipedia, the free encyclopedia
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Ramelteon, sold under the brand name Rozerem among others, is a melatonin agonist medication which is used in the treatment of insomnia.[3][5] It is indicated specifically for the treatment of insomnia characterized by difficulties with sleep onset.[3] It reduces the time taken to fall asleep, but the degree of clinical benefit is small.[6] The medication is approved for long-term use.[3] Ramelteon is taken by mouth.[3]
Clinical data | |
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Trade names | Rozerem, others |
Other names | TAK-375 |
AHFS/Drugs.com | Monograph |
MedlinePlus | a605038 |
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Dependence liability | Low[1] |
Routes of administration | By mouth |
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Pharmacokinetic data | |
Bioavailability | 1.8%[3] |
Protein binding | 82% (mainly albumin)[3] |
Metabolism | Liver (CYP1A2 major, CYP2C and CYP3A4 minor)[3] |
Metabolites | M-II (active metabolite)[3] |
Elimination half-life | Ramelteon: 1–2.6 hours[3] M-II: 2–5 hours[3][4] |
Excretion | Kidney: 84%[3] Feces: 4%[3] |
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ECHA InfoCard | 100.215.666 |
Chemical and physical data | |
Formula | C16H21NO2 |
Molar mass | 259.349 g·mol−1 |
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Side effects of ramelteon include somnolence, dizziness, fatigue, nausea, exacerbated insomnia, and changes in hormone levels.[3] Ramelteon is an analogue of melatonin and is a selective agonist of the melatonin MT1 and MT2 receptors.[3] The half-life and duration of ramelteon are much longer than those of melatonin.[7] Ramelteon is not a benzodiazepine or Z-drug and does not interact with GABA receptors, instead having a distinct mechanism of action.[3][8]
Ramelteon was first described in 2002[9] and was approved for medical use in 2005.[10] Unlike certain other sleep medications, ramelteon is not a controlled substance[contradictory] and has no known potential for misuse.[3]