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Sleep–Wake Disorders
Published in Philip B. Gorelick, Fernando D. Testai, Graeme J. Hankey, Joanna M. Wardlaw, Hankey's Clinical Neurology, 2020
Margaret Kay-Stacey, Eunice Torres-Rivera, Phyllis C. Zee
Treatment is aimed to entrain the circadian rhythm to a 24-hour cycle. For both blind and sighted persons, a multimodal approach using timed structured nonphotic cues, such as social and physical activity, meal timing, and melatonin agonists can strengthen circadian entrainment. Studies with melatonin have used 0.5 mg up to 10 mg at a fixed time at desired sleep onset can entrain circadian rhythms, with low doses possibly being more effective than higher doses. Tasimelteon is a melatonin receptor agonist and the only FDA-approved medication for the treatment of N24SWD. When administered 1 hour prior to the desired bedtime, tasimelteon demonstrated entrainment after 1 month of taking the medication, and 90% were able to maintain entrainment.89 For sighted individuals with N24SWD, there have been a handful of case reports that demonstrated the efficacy of timed light exposure in the morning shortly after awakening, timed melatonin, or combination therapy.90
Sedative and Hypnotic Drugs
Published in Sahab Uddin, Rashid Mamunur, Advances in Neuropharmacology, 2020
Arup Kumar Misra, Pramod Kumar Sharma
Tasimelteon is also melatonin receptors agonist approved recently for the treatment of non-24-h sleep–wake disorder. It is specially indicated in totally blind patients. Tasimelteon is used to improve the onset to fall asleep, thus improving the sleep timing but on discontinuation, the patient will continue with his/her previous sleep pattern within a month (Bonacci et al., 2015). It has affinity for MT2 receptor which gets reflected as it maintains the circadian rhythm of sleep. Inability to maintain mental alertness is an undesirable side effect which may affect the daily activities of the patients. Tasimelteon is given in the dose of 20 mg which is given before sleep. It reached its peak of action at 0.5–3 h after drug administration. The drug is metabolized in the liver by CYP1A2 and CYP3A4 (Vachharajani and Yeleswaram, 2003).
Medication effects on sleep
Published in S.R. Pandi-Perumal, Meera Narasimhan, Milton Kramer, Sleep and Psychosomatic Medicine, 2017
Melatonin is a neural hormone that is effective at resetting circadian rhythms of sleep and body core temperature through its actions on the suprachiasmatic nucleus. For individuals with insomnia secondary to disruptions in circadian rhythms, melatonin can act as a hypnotic and is a useful adjunct to treatment that often includes cognitive therapies, light exposure, and other hypnotics. Ramelteon (Rozerem) is a melatonin receptor agonist that is indicated for the treatment of transient and chronic sleep-onset insomnia. Tasimelteon is a new agent that is designed to treat 24-hour sleep–wake disorder in the blind.
Circadian rhythms in diabetic retinopathy: an overview of pathogenesis and investigational drugs
Published in Expert Opinion on Investigational Drugs, 2020
Ashay D. Bhatwadekar, Varun Rameswara
Tasimelteon is a dual melatonin receptor agonist with high specificity and affinity for both melatonin receptors MT1 and MT2 [91]. Tasimelteon is currently approved by the FDA for the treatment of non-24-hour sleep-wake disorder (Non-24) [92]. The Non-24 is a rare circadian rhythms disorder affecting blind individuals; the major symptoms of Non-24 include delays in sleep onset and wake timings. Other symptoms include cyclic changes in alertness, mood levels, and difficulties in maintaining schoolwork and social schedules [93]. The prevalence of Non-24 is 40–76% among blind people. While tasimelteon is currently prescribed to patients where blindness is secondary to PDR, it is enticing that tasimelteon may be beneficial for treating DR considering the melatonin agonistic effect and potential benefit to circadian rhythms and glycemic control; however, there are no preclinical or clinical studies supporting the above hypothesis.
Tasimelteon for treating non-24-h sleep-wake rhythm disorder
Published in Expert Opinion on Pharmacotherapy, 2019
Shohei Nishimon, Mari Nishimon, Seiji Nishino
Non-24, a serious disorder with periodic nighttime insomnia and daytime sleepiness, is related to the secretion of melatonin during daytime hours due to altered circadian rhythms. Tasimelteon is a dual melatonin receptor agonist, and it can entrain circadian rhythms and improve the sleep-wake functions of patients with non-24.