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Journal articles on the topic 'Tasimelteon'

Author: Grafiati

Published: 14 March 2023

Last updated: 19 July 2025

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1

Johnsa, Jessica D., and Michael W. Neville. "Tasimelteon." Annals of Pharmacotherapy 48, no. 12 (2014): 1636–41. http://dx.doi.org/10.1177/1060028014550476.

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2

Bonacci, Janene M., Jineane V. Venci, and Mona A. Gandhi. "Tasimelteon (Hetlioz™)." Journal of Pharmacy Practice 28, no. 5 (2014): 473–78. http://dx.doi.org/10.1177/0897190014544792.

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In January 2014, the US Food and Drug Administration approved tasimelteon (Hetlioz™), a melatonin-receptor agonist for the treatment of non-24-hour sleep–wake disorder. This article provides an overview of the mechanism of action, pharmacokinetic properties, as well as the clinical efficacy, safety, and tolerability of tasimelteon. Relevant information was identified through a comprehensive literature search of several databases using the key words tasimelteon, Non-24-hour Sleep–Wake disorder, Non-24, and melatonin. Further information was obtained from the tasimelteon package insert, fda.gov , clinicaltrials.gov , briefing materials provided by Vanda Pharmaceuticals, and posters from scientific meetings.

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3

Brooks, J., M. Gibson, K. Kite, et al. "1161 Tasimelteon Shows Persistence Of Efficacy In Improving Sleep Disturbances In Patients With Smith-Magenis Syndrome (SMS) In Open-Label Extension Study." Sleep 43, Supplement_1 (2020): A442—A444. http://dx.doi.org/10.1093/sleep/zsaa056.1155.

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Abstract Introduction Smith-Magenis Syndrome (SMS) is a rare (1/15,000 - 25,000 births) neurodevelopmental disorder resulting from an interstitial deletion of chromosome 17p11.2, or from a point mutation in the RAI1 gene. Severe sleep disorder is almost universal in patients with SMS and poses a significant challenge to patients and their families. Tasimelteon improved sleep symptoms in a randomized, double-blind, two-period, crossover study; and here we show that this effect persists for up to four years in an open-label extension. To our knowledge, this is the largest interventional study of SMS patients to date. Methods Following the 4-week crossover study, all eligible participants had the option to enroll in an open-label extension. 31/39 (79.4%) of all individuals who participated in the efficacy study have continued on tasimelteon treatment. Participants in the open-label extension provided daily diary sleep quality (DDSQ), and daily diary total sleep time (DDTST) measures via parental post sleep questionnaire and characterized behavior using the Aberrant Behavior Checklist (ABC). Results In the open-label extension, tasimelteon continued to show improvement in the primary endpoints of 50% worst sleep quality (mean = 0.7, SD = 0.94) and 50% worst total nighttime sleep duration (mean = 53.3, SD = 59.01) when compared to baseline. Tasimelteon also improved overall sleep quality (mean=0.7, SD=0.83) and overall total nighttime sleep duration (mean = 51.9, SD=53.03). ABC scores also improved with tasimelteon (mean= -16.3, SD = 15.82). Conclusion Tasimelteon continues to demonstrate persistence in efficacy (longest approximately 4 years) with similar magnitudes observed in the 4-week crossover study for sleep quality and total sleep time. Interestingly, daytime behavior also demonstrates long-term improvement in patients with SMS treated with tasimelteon. These results further confirm tasimelteon as a novel therapy for the treatment of sleep disorders in patients with SMS and may provide benefit for behavioral symptoms. Support This work was supported by Vanda Pharmaceuticals Inc.

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4

Lankford, D. Alan. "Tasimelteon for insomnia." Expert Opinion on Investigational Drugs 20, no. 7 (2011): 987–93. http://dx.doi.org/10.1517/13543784.2011.583235.

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5

&NA;. "Tasimelteon tackles chronic insomnia." Inpharma Weekly &NA;, no. 1645 (2008): 5. http://dx.doi.org/10.2165/00128413-200816450-00013.

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6

Torres, Rosarelis, Marlene A. Dressman, William G. Kramer, and Paolo Baroldi. "Absolute Bioavailability of Tasimelteon." American Journal of Therapeutics 22, no. 5 (2015): 355–60. http://dx.doi.org/10.1097/mjt.0000000000000195.

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7

Li, Xi-An, Lirong Yue, Jianrong Zhu, et al. "Total synthesis of Tasimelteon." Tetrahedron Letters 60, no. 30 (2019): 1986–88. http://dx.doi.org/10.1016/j.tetlet.2019.06.048.

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8

Dhillon, Sohita, and Madeleine Clarke. "Tasimelteon: First Global Approval." Drugs 74, no. 4 (2014): 505–11. http://dx.doi.org/10.1007/s40265-014-0200-1.

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9

&NA;. "Tasimelteon helps transient insomniacs nod off." Inpharma Weekly &NA;, no. 1667 (2008): 11. http://dx.doi.org/10.2165/00128413-200816670-00033.

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10

Adams, Katie S., and Ericka L. Breden Crouse. "Melatonin agonists in the management of sleep disorders: A focus on ramelteon and tasimelteon." Mental Health Clinician 4, no. 2 (2014): 59–64. http://dx.doi.org/10.9740/mhc.n190087.

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Melatonin agonists have become an area of interest in the treatment of sleep disorders. This article reviews the available data on this class of medications, with a focus on ramelteon and tasimelteon.

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11

Mi, Senyang, Xinzhe Sun, Chaogang Wu, and Xingxian Zhang. "A Facile and Practical Synthesis of (-)-tasimelteon." Journal of Chemical Research 40, no. 11 (2016): 667–69. http://dx.doi.org/10.3184/174751916x14758368248634.

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12

Stahl, Stephen M. "Mechanism of action of tasimelteon in non-24 sleep-wake syndrome: treatment for a circadian rhythm disorder in blind patients." CNS Spectrums 19, no. 6 (2014): 475–78. http://dx.doi.org/10.1017/s1092852914000637.

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ISSUE:Many individuals with total blindness can develop a circadian rhythm disorder—called non-24 sleep wake syndrome—because they cannot detect light to resynchronize their sleep–wake cycles. A new melatonin 1 and melatonin 2 agonist tasimelteon improves sleep in these patients, resetting their circadian sleep–wake clocks.

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13

Yuhas, Phillip T. "Non-24-Hour Sleep–Wake Disorder and Tasimelteon: A Review for Practitioners Who Work With Blind People." Journal of Visual Impairment & Blindness 116, no. 1 (2022): 70–84. http://dx.doi.org/10.1177/0145482x211072521.

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Introduction This narrative review summarizes the biology of human circadian rhythms; details the epidemiology, clinical manifestation, and diagnosis of non-24-hour sleep–wake disorder (N24SWD); and reviews the efficacy of possible treatments. Methods Searches of targeted phrases, such as “non-24-hour sleep–wake disorder” and “tasimelteon,” were conducted on PubMed between December 2016 and March 2020. Results As the world’s population ages, health practitioners frequently work with people who are blind. Damage to the retinal ganglion cells that signal environmental irradiance levels to the suprachiasmatic nucleus prevents many of these individuals from synchronizing their internal clocks to the 24-hour day. As a result, they experience a condition called N24SWD, where the body’s circadian rhythms fall in and out of phase with the solar cycle. The ability to fall asleep and remain asleep is a complex process that depends on many variables, including the release of the neurohormone melatonin. Melatonin is produced at night and is a key regulator of regular sleep cycles. Periods of interrupted sleep, increased sleep latency, and reduced total sleep time occur when melatonin production peaks during daytime. Thus, many persons with N24SWD have difficulty maintaining normal schedules due in part to the mistimed release of melatonin. Randomized clinical trials have shown that melatonin receptor agonist tasimelteon is an effective therapy for individuals with N24SWD. Other treatments have varying efficacy profiles. Conclusions Although rare, N24SWD is a serious condition that can impair quality of life for blind persons. Tasimelteon appears to be a safe and efficacious treatment option. Implications for Practitioners Practitioners can use this information to better understand why blind persons often report difficulties sleeping and to realize that therapeutic options are available to these individuals.

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14

Traynor, Kate. "Tasimelteon approved for circadian disorder in blind adults." American Journal of Health-System Pharmacy 71, no. 5 (2014): 350. http://dx.doi.org/10.2146/news140017.

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15

Lavedan, Christian, Mark Forsberg, and Anthony J. Gentile. "Tasimelteon: A selective and unique receptor binding profile." Neuropharmacology 91 (April 2015): 142–47. http://dx.doi.org/10.1016/j.neuropharm.2014.12.004.

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16

Wang, Wenbing, Xiangwei Meng, Jianrong Zhu, and Xingxian Zhang. "An efficient and practical asymmetric synthesis of (−)-tasimelteon." Synthetic Communications 49, no. 1 (2019): 129–35. http://dx.doi.org/10.1080/00397911.2018.1545031.

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17

Polymeropoulos, C., E. Czeisler, M. Fisher, et al. "Tasimelteon effective in treating JET lag during transatlantic travel." Sleep Medicine 64 (December 2019): S305. http://dx.doi.org/10.1016/j.sleep.2019.11.854.

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18

Liu, Kaihang, Xinbo Zhou, Zhejing Xu, et al. "Anhydrates and hemihydrate of tasimelteon: Synthesis, structure, and pharmacokinetic study." Journal of Pharmaceutical and Biomedical Analysis 151 (March 2018): 235–43. http://dx.doi.org/10.1016/j.jpba.2017.12.035.

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19

Polymeropoulos, Christos, Emily Czeisler, Michaela Fisher, et al. "0639 Tasimelteon Effective in Treating Jet Lag during Transatlantic Travel." Sleep 42, Supplement_1 (2019): A254—A255. http://dx.doi.org/10.1093/sleep/zsz067.637.

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20

Nishimon, Shohei, Mari Nishimon, and Seiji Nishino. "Tasimelteon for treating non-24-h sleep-wake rhythm disorder." Expert Opinion on Pharmacotherapy 20, no. 9 (2019): 1065–73. http://dx.doi.org/10.1080/14656566.2019.1603293.

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21

Neubauer, D. N. "Tasimelteon for the treatment of non-24-hour sleep-wake disorder." Drugs of Today 51, no. 1 (2015): 29. http://dx.doi.org/10.1358/dot.2015.51.1.2258364.

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Polymeropoulos, M. H., C. Xiao, and C. Polymeropoulos. "Tasimelteon improves symptoms of major depression in an African American population." Sleep Medicine 40 (December 2017): e266. http://dx.doi.org/10.1016/j.sleep.2017.11.779.

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23

Petrini, Agnese, Giovanni Ievoli, Francesca Migliorini, Maurizio Taddei, and Sofia Siciliano. "A Self-Immolative Linker for the pH-Responsive Release of Amides." Molecules 28, no. 6 (2023): 2445. http://dx.doi.org/10.3390/molecules28062445.

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The administration of therapeutics using bioconjugation has been mainly limited to drugs containing amine, alcohol, or thiol functional groups. Here, we report a general procedure for the preparation of benzylic N-acyl carbamates suitable for masking the amide group in important drugs such as Linezolid, Enzalutamide, or Tasimelteon in good to acceptable yields. These N-acyl carbamates appear to be stable in plasma, while a qualitative analysis of further drug uncage demonstrates that, at pH values of 5.5, a classical 1,6-benzyl elimination mechanism takes place, releasing more than 80% of the drug in 24 h.

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Polymeropoulos, M., C. Xiao, and C. Polymeropoulos. "0986 Tasimelteon Improves Symptoms of Major Depression in an African American Population." Sleep 41, suppl_1 (2018): A365—A366. http://dx.doi.org/10.1093/sleep/zsy061.985.

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25

de Klaver, P. A. G. "Melatonine agonist tasimelteon (VEC-162) bij voorbijgaande insomnia na nachtdienst: 2 gerandomiseerde onderzoeken." Medisch-Farmaceutische Mededelingen 47, no. 6 (2009): 93–94. http://dx.doi.org/10.1007/bf03079969.

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26

Dyrek, Nicola, Magdalena Balwierz, Marcin Łata, and Agnieszka Kosińska. "Melatonin receptor agonists in neurodegenerative diseases and psychiatric disorders." Quality in Sport 22 (September 22, 2024): 54717. http://dx.doi.org/10.12775/qs.2024.22.54717.

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Neurodegenerative and psychiatric diseases remain a therapeutic challenge. Mental illnesses such as depression and bipolar affective disorder lead to disruption of the diurnal rhythm of melatonin secretion and disruption of the sleep-wake axis. The use of new melatonergic drugs has received special attention in recent years. Selective melatoninergic M1 and M2 receptor agonists (tasimelteon, ramelteon) show a more favorable metabolic profile, better regulation of circadian rhythms, and effects on total sleep time and sleep quality compared to the already well-studied melatonin. In addition, these drugs show no addictive potential. Agomelatine, through its action on M1 and M2 receptors, as well as serotonergic 5-HT2C and 5-HT2B receptors, exhibits antidepressant, normothymic, and neuroprotective effects, providing primary therapy or adjunctive treatment.

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Polymeropoulos, C., E. Czeisler, M. Fisher, et al. "Tasimelteon demonstrates efficacy in improving sleep disturbances of individuals with smith-magenis syndrome (SMS)." Sleep Medicine 64 (December 2019): S423. http://dx.doi.org/10.1016/j.sleep.2019.11.1176.

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28

Keating, Gillian M. "Tasimelteon: A Review in Non-24-Hour Sleep-Wake Disorder in Totally Blind Individuals." CNS Drugs 30, no. 5 (2016): 461–68. http://dx.doi.org/10.1007/s40263-016-0330-y.

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29

Ogilvie, Brian W., Rosarelis Torres, Marlene A. Dressman, William G. Kramer, and Paolo Baroldi. "Clinical assessment of drug–drug interactions of tasimelteon, a novel dual melatonin receptor agonist." Journal of Clinical Pharmacology 55, no. 9 (2015): 1004–11. http://dx.doi.org/10.1002/jcph.507.

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30

Collins, Joseph, and Joseph Espiritu. "1187 Non-24-hour Sleep-Wake Disorder in Transgender Male Receiving Exogenous Testosterone." SLEEP 47, Supplement_1 (2024): A507. http://dx.doi.org/10.1093/sleep/zsae067.01187.

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Abstract Introduction Little is known about the effects of hormonal therapy for adolescents undergoing transgender care. We present a case of a biologic female being treated with exogenous testosterone for transgender care who develops non-24-hour circadian rhythm disorder (N24SWD), a rare sleep-wake disorder, most commonly seen in individuals who are totally blind. Report of case(s) A 19-year-old transgender man (female at birth) presented to our clinic with complaints of inconsistent sleep schedule and daytime sleepiness. They have a past medical history of anxiety, obsessive-compulsive disorder (OCD), and social phobia. As a younger teenager, the patient reported having a delayed sleep phase pattern. A year ago, the patient started exogenous testosterone injections every 2 weeks. Over the past year, the patient noticed a change in sleep pattern, described as going to bed and waking up 1-2 hours later, with each passing day. This was verified with 4 weeks of sleep diaries. The patient was diagnosed with N24SWD and was prescribed melatonin 0.5 mg 6 hours before bedtime without benefit. Other behavioral modifications with set wake times, bright light therapy, and morning exercises were not helpful. We prescribed tasimelteon, a melatonin receptor agonist, but it was denied by the health insurance. The current management plan is to optimize sleep behaviors and continue psychiatric follow-up for mood disorders while appealing the denial of tasimelteon. Conclusion Transgender individuals are particularly vulnerable to sleep disorders. Testosterone replacement therapy has been linked to sleep disordered breathing, insomnia, and sleep disruption. It has not been well established what role hormone therapy, and specifically testosterone in this case, plays on an individual’s circadian rhythm. Previous studies have demonstrated that melatonin production decreases more abruptly for women going through menopause and that delayed sleep phase in teenagers may be due to hormonal changes during puberty, although pathophysiology is not fully understood5. A similar case of a transgender male receiving exogenous testosterone was recently reported. More research is needed to elucidate the potential adverse effect of testosterone replacement on the circadian rhythm of the growing population of patients undergoing transgender care. Support (if any)

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Polymeropoulos, Christos, Emily Czeisler, Michaela Fisher, et al. "0641 Tasimelteon Demonstrates Efficacy in Improving Sleep Disturbances of Individuals with Smith-Magenis Syndrome (SMS)." Sleep 42, Supplement_1 (2019): A255. http://dx.doi.org/10.1093/sleep/zsz067.639.

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32

Torres, Rosarelis, William G. Kramer, and Paolo Baroldi. "Pharmacokinetics of the dual melatonin receptor agonist tasimelteon in subjects with hepatic or renal impairment." Journal of Clinical Pharmacology 55, no. 5 (2015): 525–33. http://dx.doi.org/10.1002/jcph.440.

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Satyanarayanan, Senthil Kumaran, Huanxing Su, Yi-Wen Lin, and Kuan-Pin Su. "Circadian Rhythm and Melatonin in the Treatment of Depression." Current Pharmaceutical Design 24, no. 22 (2018): 2549–55. http://dx.doi.org/10.2174/1381612824666180803112304.

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Background: Circadian rhythm disruption underlies the pathophysiology of psychiatric disorders, especially depression. Both pharmacological and non-pharmacological strategies affecting endogenous circadian rhythms have been developed with specificity to alter the circadian dysfunction. The current management strategy with antidepressants is far from being satisfactory in addressing this issue. In recent years, attempts at discovering new antidepressants focused on a melatonergic system which is known to be altered in depression have led to a potential option for treatment of depression. Methods: We reviewed all recently published relevant articles on melatonin and its analogues to look for their implication in the treatment of circadian rhythm disruption and depression. Results: Melatonin, a pleiotropic regulator molecule and its analogues (ramelteon, agomelatine, TIK-301, Neu- P11 and tasimelteon) have been observed to resynchronize the circadian rhythm and some were said to alleviate depressive symptoms in depressed subjects. Conclusion: This review focuses on substantial advances in the melatonin-based chronobiologic intervention and its responses in the treatment of depression.

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34

Erland, Lauren A. E., Christopher R. Dumigan, Jillian A. Forsyth, et al. "Mammalian Melatonin Agonist Pharmaceuticals Stimulate Rhomboid Proteins in Plants." Biomolecules 12, no. 7 (2022): 882. http://dx.doi.org/10.3390/biom12070882.

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Melatonin is a human neurotransmitter and plant signalling metabolite that perceives and directs plant metabolism. The mechanisms of melatonin action in plants remain undefined. We hypothesized that roots have a melatonin-specific receptor and/or transporter that can respond to melatonin-mediating pharmaceuticals. To test this hypothesis Arabidopsis seedlings were grown with melatonin pharmaceutical receptor agonists: ramelteon and tasimelteon, and/or antagonists: luzindole and 4-P-PDOT. Ramelteon was found both to mimic and competitively inhibit melatonin metabolism in plants. Due to the higher selectivity of ramelteon for the MT1 receptor type in humans, a sequence homology search for MT1 in Arabidopsis identified the rhomboid-like protein 7 (RBL7). In physiological studies, Arabidopsis rbl7 mutants were less responsive to ramelteon and melatonin. Quantum dot visualizations of the effects of ramelteon on melatonin binding to root cell membranes revealed a potential mechanism. We propose that RBL7 is a melatonin-interacting protein that directs root architecture and growth in a mechanism that is responsive to environmental factors.

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35

Edmonds, Chelsey, and Michael Swanoski. "A Review of Suvorexant, Doxepin, Ramelteon, and Tasimelteon for the Treatment of Insomnia in Geriatric Patients." Consultant Pharmacist 32, no. 3 (2017): 156–60. http://dx.doi.org/10.4140/tcp.n.2017.156.

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36

Ventimiglia, Giampiero, Sonja Bellomi, Giuseppe Barreca, Lorella Giovannelli, and Norberto Masciocchi. "Synthesis, Characterization, and Crystal Chemistry of Tasimelteon, a Melatonin Agonist, in Its Anhydrous and Hemihydrate Forms." Journal of Pharmaceutical Sciences 107, no. 2 (2018): 543–49. http://dx.doi.org/10.1016/j.xphs.2017.09.012.

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37

Xiao, C., C. Polymeropoulos, J. Brzezynski, et al. "Tasimelteon demonstrates efficacy to treat jet lag disorder in an 8 hour phase advance clinical study." Sleep Medicine 64 (December 2019): S423. http://dx.doi.org/10.1016/j.sleep.2019.11.1175.

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38

Leger, Damien, Maria-Antonia Quera-Salva, Marie-Françoise Vecchierini, Pascale Ogrizek, Christina A. Perry, and Marlene A. Dressman. "Safety profile of tasimelteon, a melatonin MT1and MT2receptor agonist: pooled safety analyses from six clinical studies." Expert Opinion on Drug Safety 14, no. 11 (2015): 1673–85. http://dx.doi.org/10.1517/14740338.2015.1093112.

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39

Rajaratnam, Shantha MW, Mihael H. Polymeropoulos, Dennis M. Fisher, et al. "Melatonin agonist tasimelteon (VEC-162) for transient insomnia after sleep-time shift: two randomised controlled multicentre trials." Lancet 373, no. 9662 (2009): 482–91. http://dx.doi.org/10.1016/s0140-6736(08)61812-7.

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40

Polymeropoulos, Vasilios, Jim Wang, Christos Polymeropoulos, Changfu Xiao, and Mihael Polymeropoulos. "0640 Tasimelteon Significantly Improves REM Sleep Accumulation During an 8-hour Phase Advance in the JET8 Study." Sleep 42, Supplement_1 (2019): A255. http://dx.doi.org/10.1093/sleep/zsz067.638.

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41

Rajaratnam, Shantha M. W., Mihael H. Polymeropoulos, Dennis M. Fisher, et al. "Melatonin Agonist Tasimelteon (VEC-162) for Transient Insomnia After Sleep-Time Shift: Two Randomized Controlled Multicentre Trials." Obstetrical & Gynecological Survey 64, no. 9 (2009): 604–5. http://dx.doi.org/10.1097/01.ogx.0000358014.55641.1c.

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42

Smieszek, S., A. Kaden, C. Johnson, et al. "Tasimelteon for the treatment of delayed sleep-wake phase disorder and optic nerve hypoplasia: a case study." Sleep Medicine 115 (February 2024): 66. http://dx.doi.org/10.1016/j.sleep.2023.11.215.

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43

Moschona, Fotini, Ioanna Savvopoulou, Maria Tsitopoulou, Despoina Tataraki, and Gerasimos Rassias. "Epoxide Syntheses and Ring-Opening Reactions in Drug Development." Catalysts 10, no. 10 (2020): 1117. http://dx.doi.org/10.3390/catal10101117.

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This review concentrates on success stories from the synthesis of approved medicines and drug candidates using epoxide chemistry in the development of robust and efficient syntheses at large scale. The focus is on those parts of each synthesis related to the substrate-controlled/diastereoselective and catalytic asymmetric synthesis of epoxide intermediates and their subsequent ring-opening reactions with various nucleophiles. These are described in the form of case studies of high profile pharmaceuticals spanning a diverse range of indications and molecular scaffolds such as heterocycles, terpenes, steroids, peptidomimetics, alkaloids and main stream small molecules. Representative examples include, but are not limited to the antihypertensive diltiazem, the antidepressant reboxetine, the HIV protease inhibitors atazanavir and indinavir, efinaconazole and related triazole antifungals, tasimelteon for sleep disorders, the anticancer agent carfilzomib, the anticoagulant rivaroxaban the antibiotic linezolid and the antiviral oseltamivir. Emphasis is given on aspects of catalytic asymmetric epoxidation employing metals with chiral ligands particularly with the Sharpless and Jacobsen–Katsuki methods as well as organocatalysts such as the chiral ketones of Shi and Yang, Pages’s chiral iminium salts and typical chiral phase transfer agents.

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Sukys-Claudino, Lucia, Walter André dos Santos Moraes, Sergio Tufik, and Dalva Poyares. "Novos sedativos hipnóticos." Revista Brasileira de Psiquiatria 32, no. 3 (2010): 288–93. http://dx.doi.org/10.1590/s1516-44462010000300014.

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Nas últimas décadas houve um esforço para o desenvolvimento de hipnóticos mais seguros e eficazes. Zolpidem, zaleplona, zopiclona, eszopiclona (drogas-z) e indiplona são moduladores do receptor GABA-A, os quais agem de forma seletiva na subunidade α1, exibindo, desta forma, mecanismos similares de ação, embora evidências recentes sugiram que a eszopiclona não seja tão seletiva para a subunidade α1 quanto o zolpidem. Ramelteon e tasimelteon são novos agentes crono-hipnóticos seletivos para os receptores de melatonina MT1 e MT2. Por outro lado, nos últimos anos, o consumo de drogas antidepressivas sedativas tem aumentado significativamente no tratamento da insônia. Como droga experimental, a eplivanserina tem sido testada como um potente agonista inverso do subtipo 5-HT2A da serotonina, com um uso potencial na dificuldade da manutenção do sono. Outro agente farmacológico para o tratamento da insônia é o almorexant, o qual apresenta um novo mecanismo de ação envolvendo antagonismo do sistema hipocretinérgico, desta forma levando à indução do sono. Finalmente, também discutiremos o potencial papel de outras drogas gabaérgicas no tratamento da insônia.

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45

Cocozza, Victoria, David Kim, Benjamin Long, and Shana Hansen. "0991 Dual Therapy to Treat Circadian Rhythm Disturbance in Unique Genetic Mutation of Smith-Magenis Syndrome." SLEEP 46, Supplement_1 (2023): A437. http://dx.doi.org/10.1093/sleep/zsad077.0991.

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Abstract Introduction Smith-Magenis syndrome (SMS) is a rare disorder associated with several genetic mutations. Patients with SMS experience circadian rhythm sleep-wake disorders, which may lead to significant behavioral concerns. A proposed etiology of sleep disturbances is diurnal melatonin secretion. Treatment approaches aim at blocking the abnormal morning secretion of melatonin and providing exogenous melatonin in the evening. Report of case(s) We present a patient with SMS having persistent sleep-wake disturbance despite dual therapy with beta-1 adrenergic antagonist in the morning and over-the-counter melatonin at night. Our patient switched to therapy with beta-1 adrenergic antagonist in the mornings and melatonin receptor agonist, tasimelteon, at night with significant improvement. In addition, our patient has mutations in JAKMIP1 and ZBTB18 genes. ZBTB18 mutation is a novel mutation in the setting of clinical features of SMS. Conclusion To the authors’ knowledge, this is the first case report of successful combination therapy to optimize treatment of sleep-wake disturbances in patients with SMS. Support (if any)

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Gomes, Abner do Amaral, and Bruna Marçal Guidoti Eleutério. "AÇÃO ANTIDEPRESSIVA DA MELATONINA E DO AGONISTA DO RECEPTOR DE MELATONINA: FISIOPATOLOGIA E TRATAMENTO." Revista Ibero-Americana de Humanidades, Ciências e Educação 9, no. 10 (2023): 3185–204. http://dx.doi.org/10.51891/rease.v9i10.11788.

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A depressão tornou-se um dos distúrbios neuropsiquiátricos mais comuns e prevalentes, e as principais características da depressão são distúrbios do sono e da secreção de melatonina, causados por alteração do ritmo circadiano. Alterações endógenas anormais da melatonina podem contribuir para a ocorrência e desenvolvimento da depressão. No entanto, os mecanismos moleculares subjacentes a essa anormalidade permanecem ambíguos. A presente revisão resume os mecanismos subjacentes aos efeitos antidepressivos da melatonina, que estão relacionados às suas funções na regulação do eixo hipotálamo-hipófise-adrenal, inibição da neuroinflamação, inibição do estresse oxidativo, alívio da autofagia e regulação positiva de neurotróficos, promoção de neuroplasticidade e regulação positiva dos níveis de neurotransmissores, etc. Além disso, agonistas do receptor de melatonina, como agomelatina, ramelteon, piromelatina, tasimelteon e GW117, receberam atenção crítica considerável e estão altamente implicados no tratamento de depressão e distúrbios comórbidos. Esta revisão enfoca a melatonina e alguns agonistas do receptor de melatonina na fisiopatologia e tratamento da depressão, com o objetivo de fornecer mais informações sobre a patogênese da depressão e explorar alvos potenciais para o desenvolvimento de novos agentes.

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Lockley, Steven, Marlene Dressman, Xiao Changfu, et al. "Le tasimelteon entraîne l’horloge circadienne et procure une amélioration significative aux personnes totalement aveugles, souffrant du libre-cours." Médecine du Sommeil 12, no. 1 (2015): 55–56. http://dx.doi.org/10.1016/j.msom.2015.01.099.

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Hull, J. T., C. Polymeropoulos, Y. Cho, C. Xiao, and M. H. Polymeropoulos. "Tasimelteon improves sleep quality and behavior in individuals with Smith-Magenis syndrome (SMS) in an open-label study." Sleep Medicine 40 (December 2017): e139. http://dx.doi.org/10.1016/j.sleep.2017.11.406.

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Polymeropoulos, V., C. Polymeropoulos, G. Birznieks, C. Xiao, and M. Polymeropoulos. "Tasimelteon significantly improves time to 30 minutes of REM (REM30) as compared to placebo in the JET8 study." Sleep Medicine 64 (December 2019): S305. http://dx.doi.org/10.1016/j.sleep.2019.11.855.

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Van Draanen, L., C. Xiao, and M. H. Polymeropoulos. "0649 Tasimelteon Improves Number of Sleep Free Days in Blind Patients with Non-24-Hour Sleep-Wake Disorder." Sleep 41, suppl_1 (2018): A241. http://dx.doi.org/10.1093/sleep/zsy061.648.

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