Ramelteon
| Clinical data | |
|---|---|
| Trade names | Rozerem, others |
| Other names | TAK-375 |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a605038 |
| License data | |
| 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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| CompTox Dashboard (EPA) | |
| ECHA InfoCard | 100.215.666 |
| Chemical and physical data | |
| Formula | C16H21NO2 |
| Molar mass | 259.349 g·mol−1 |
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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]
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 in nearly every country and has no known potential for misuse.[3]
- ^ Kim HK, Yang KI (December 2022). "Melatonin and melatonergic drugs in sleep disorders". Translational and Clinical Pharmacology. 30 (4): 163–171. doi:10.12793/tcp.2022.30.e21. PMC 9810491. PMID 36632077.
- ^ Anvisa (31 March 2023). "RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial" [Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control] (in Brazilian Portuguese). Diário Oficial da União (published 4 April 2023). Archived from the original on 3 August 2023. Retrieved 16 August 2023.
- ^ a b c d e f g h i j k l m n o p q Cite error: The named reference
Rozerem FDA labelwas invoked but never defined (see the help page). - ^ Karim A, Tolbert D, Cao C (February 2006). "Disposition kinetics and tolerance of escalating single doses of ramelteon, a high-affinity MT1 and MT2 melatonin receptor agonist indicated for treatment of insomnia". Journal of Clinical Pharmacology. 46 (2): 140–148. doi:10.1177/0091270005283461. PMID 16432265. S2CID 38171735.
- ^ Neubauer DN (February 2008). "A review of ramelteon in the treatment of sleep disorders". Neuropsychiatric Disease and Treatment. 4 (1): 69–79. doi:10.2147/ndt.s483. PMC 2515902. PMID 18728808.
- ^ Cite error: The named reference
pmid24656909was invoked but never defined (see the help page). - ^ Cite error: The named reference
pmid18368944was invoked but never defined (see the help page). - ^ Atkin T, Comai S, Gobbi G (April 2018). "Drugs for Insomnia beyond Benzodiazepines: Pharmacology, Clinical Applications, and Discovery". Pharmacological Reviews. 70 (2): 197–245. doi:10.1124/pr.117.014381. PMID 29487083. S2CID 3578916.
- ^ Cite error: The named reference
pmid12213063was invoked but never defined (see the help page). - ^ Cite error: The named reference
FDA2005was invoked but never defined (see the help page).