![]() The activity of melatonin at the MT1, MT2 and MT3 receptors is believed to contribute to its sleep-promoting properties, as these receptors (mainly MT1 and MT2) are involved in the regulation of circadian rhythms and sleep regulation. ![]() Synthesis and secretion of endogenous melatonin are controlled by enzymes secreted by the hypothalamus which are activated by darkness and depressed by environmental light. Melatonin is an endogenous hormone secreted by the pineal gland that interacts with melatonin receptors. ![]() These medications block the binding of wake-promoting neuropeptides orexin A and orexin B to the OX1R and OX2R receptors, subsequently suppressing the wake drive. Suvorexant, lemborexant, and daridorexant exert their therapeutic effects through antagonism of orexin receptors. The MT1 and MT2 receptors are believed to be involved in the promotion of sleep and the maintenance of the normal circadian rhythm (shift between day and night), respectively, when acted upon by endogenous melatonin. The SCN functions as the internal clock of the body and regulates the 24-hour sleep-wake cycle. Ramelteon and tasimelteon selectively target the melatonin receptors MT1 and MT2, which are located in the suprachiasmatic nucleus (SCN) of the hypothalamus. Eszopiclone has a longer half-life (6 hours) than the other drugs in the class which contributes to improving sleep maintenance. The main site of modulatory drug action is located within the GABA-A receptor complex on the alpha-subunit, which is known as the benzodiazepine (BZ) or omega receptor. Zolpidem, eszopiclone, and zaleplon are thought to induce sleep by subunit modulation of the GABA-A receptor chloride channel macromolecular complex. Nonbenzodiazepine Benzodiazepine-Receptor Agonists ![]() Patients should be re-evaluated if insomnia does not improve within 7 to 10 days after starting pharmacological therapy regardless of the medication used.Äoxepin is a tricyclic antidepressant and is believed to exert sleep maintenance effects due to a strong binding affinity for histamine H1 receptors, which allows the use of the drug as a sedative at doses lower than those required for major depressive disorder.Although classified as a non-prescription herbal product in the U.S., melatonin is available by prescription in Europe under the brand name Circadin as a short-term monotherapy treatment for primary insomnia characterized by poor quality of sleep in patients who are 55 years or older.The use of non-prescription drugs, dietary supplements, or herbal products (e.g., melatonin, tryptophan, valerian) for the treatment of chronic insomnia in adults is not recommended by the AASM guidelines.The American Academy of Sleep Medicine (AASM) guidelines for the pharmacologic treatment of chronic insomnia in adults suggest the use of ramelteon or zaleplon for sleep-onset insomnia, eszopiclone or zolpidem for sleep-onset and sleep maintenance insomnia, and doxepin or suvorexant for sleep maintenance insomnia.When pharmacologic management is required, medication choice is based upon the individual characteristics and needs of the patient, including the type of sleep difficulty (e.g., sleep-onset insomnia, sleep maintenance insomnia, frequent awakenings, early morning awakenings, circadian rhythm disruption), treatment goals, prior treatment responses, comorbid conditions, other medications, and cost.Non-pharmacological therapy is effective and is the standard of care for the initial treatment of insomnia. ![]()
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