Another class of drugs used to treat insomnia are melatonin receptor agonists. They work at the MT1 and MT2 receptor sites. They promote sleepiness and regulate the circadian rhythm to coordinate the sleep wake cycle. Examples of melatonin receptor agonists are ramelteon and tasimelteon. A warning associated with ramelteon is complex sleep behavior. Sides effects of melatonin receptor agonists include somnolence, and dizziness. They are not a controlled substance. They are to not to be taken with fatty food or fluvoxamine (a strong CYP 1A2 inhibitor that increases the serum concentration of ramelteon and tasimelteon. Tricyclic antidepressants are another class of drugs that can be used to treat insomnia. They work by inhibiting norepinephrine and serotonin reuptake. They also block acetylcholine and histamine receptors, which contributes to side effects. Doxepin is a tricyclic antidepressant that is approved by the FDA for the treatment of insomnia. Doxepin can cause seizures and are not to be used within 2 weeks of a MAO inhibitor. Benzodiazepines like temazepam, estazolam, quazepam, flurazepam, and triazolam can be used to treat insomnia. Benzodiazepine work by enhancing GABA which leading to CNS depression. Warnings associated with benzodiazepines are that use of opioids with benzodiazepines should be avoided because it can lead to sedation, respirator depression and death. There is also a risk of abuse, misuses, and addiction with benzodiazepines. They are considered as C-IV medications. Lorazepam, oxazepam, and temazepam (LOT) are the benzodiazepines recommended for use in older patients as they have a reduced risk of adverse effects. Lastly antihistamines can be used to treat insomnia. They work by blocking the H1 receptor. Side effects of antihistamines are sedation, confusion, memory loss, and peripheral anticholinergic side effects like urinary retention. Its use is also avoided in patients with BPH and glaucoma. Another sleep disorder is restless leg syndrome. This is when there is an urge to move the lower legs and gets worse at night. RLS is believed to be related to a dysfunction of dopamine. Restless leg syndrome is treat with dopamine agonists and gabapentin. The IR formulations of pramipexole and ropinirole are taken 1-3 hours before bedtime. Rotigotine is a dopamine agonist patch that is applied once daily. “Gabapentin enacarbril (Horizant) is an extended release form of gabapentin approved for RLS. It is taken at 5:00PM daily.” (UWorld RxPrep) Another sleep disorder is narcolepsy. This is when there is excessive daytime sleepiness with cataplexy (sudden loss of muscle tone), and sleep paralysis. Patients with narcolepsy experience sleep attacks which can affect them throughout the day at school, work, or in the middle of conversations. It can be diagnosed with “two specialized tests, which can be performed in a sleep disorders clinic, are required to establish a diagnosis of narcolepsy: a polysomnogram (PSG or sleep study)—This overnight test records brain activity, muscle movements, breathing, and eye movements during sleep. It helps determine if REM sleep happens too early in the sleep cycle and checks for other conditions like sleep apnea and multiple sleep latency test (MSLT)—This test measures how quickly a person falls asleep and whether they enter REM sleep. Sometimes, measuring the level of hypocretin in the fluid surrounding the brain and spinal cord can help with diagnosis. To perform this test, a doctor will take a sample of the cerebrospinal fluid using a lumbar puncture (also called a spinal tap) and measure the level of hypocretin-1” (NIH). Narcolepsy is treated with stimulants like modafinil, armodafinil, or sodium oxybate. Other medications that can be used for narcolepsy are pitolisant and solriamfetol.
Sleep Disorders Part 2
Another class of drugs used to treat insomnia are melatonin receptor agonists. They work at the MT1 and MT2 receptor sites. They promote sleepiness and regulate the circadian rhythm to coordinate the sleep wake cycle. Examples of melatonin receptor agonists are ramelteon and tasimelteon. A warning associated with ramelteon is complex sleep behavior. Sides effects of melatonin receptor agonists include somnolence, and dizziness. They are not a controlled substance. They are to not to be taken with fatty food or fluvoxamine (a strong CYP 1A2 inhibitor that increases the serum concentration of ramelteon and tasimelteon. Tricyclic antidepressants are another class of drugs that can be used to treat insomnia. They work by inhibiting norepinephrine and serotonin reuptake. They also block acetylcholine and histamine receptors, which contributes to side effects. Doxepin is a tricyclic antidepressant that is approved by the FDA for the treatment of insomnia. Doxepin can cause seizures and are not to be used within 2 weeks of a MAO inhibitor. Benzodiazepines like temazepam, estazolam, quazepam, flurazepam, and triazolam can be used to treat insomnia. Benzodiazepine work by enhancing GABA which leading to CNS depression. Warnings associated with benzodiazepines are that use of opioids with benzodiazepines should be avoided because it can lead to sedation, respirator depression and death. There is also a risk of abuse, misuses, and addiction with benzodiazepines. They are considered as C-IV medications. Lorazepam, oxazepam, and temazepam (LOT) are the benzodiazepines recommended for use in older patients as they have a reduced risk of adverse effects. Lastly antihistamines can be used to treat insomnia. They work by blocking the H1 receptor. Side effects of antihistamines are sedation, confusion, memory loss, and peripheral anticholinergic side effects like urinary retention. Its use is also avoided in patients with BPH and glaucoma. Another sleep disorder is restless leg syndrome. This is when there is an urge to move the lower legs and gets worse at night. RLS is believed to be related to a dysfunction of dopamine. Restless leg syndrome is treat with dopamine agonists and gabapentin. The IR formulations of pramipexole and ropinirole are taken 1-3 hours before bedtime. Rotigotine is a dopamine agonist patch that is applied once daily. “Gabapentin enacarbril (Horizant) is an extended release form of gabapentin approved for RLS. It is taken at 5:00PM daily.” (UWorld RxPrep) Another sleep disorder is narcolepsy. This is when there is excessive daytime sleepiness with cataplexy (sudden loss of muscle tone), and sleep paralysis. Patients with narcolepsy experience sleep attacks which can affect them throughout the day at school, work, or in the middle of conversations. It can be diagnosed with “two specialized tests, which can be performed in a sleep disorders clinic, are required to establish a diagnosis of narcolepsy: a polysomnogram (PSG or sleep study)—This overnight test records brain activity, muscle movements, breathing, and eye movements during sleep. It helps determine if REM sleep happens too early in the sleep cycle and checks for other conditions like sleep apnea and multiple sleep latency test (MSLT)—This test measures how quickly a person falls asleep and whether they enter REM sleep. Sometimes, measuring the level of hypocretin in the fluid surrounding the brain and spinal cord can help with diagnosis. To perform this test, a doctor will take a sample of the cerebrospinal fluid using a lumbar puncture (also called a spinal tap) and measure the level of hypocretin-1” (NIH). Narcolepsy is treated with stimulants like modafinil, armodafinil, or sodium oxybate. Other medications that can be used for narcolepsy are pitolisant and solriamfetol.
https://www.ninds.nih.gov/health-information/disorders/narcolepsy#:~:text=Narcolepsy%20is%20a%20chronic%20neurological,throughout%20much%20of%20the%20day.
UWorld RxPrep NAPLEX Review 2025 Chapter 67 Sleep Disorders Page 830