Rozerem: a novel hypnotic: a melatonin receptor agonist
Question:
Medscape: Another topic that we have discussed in this newsletter is insomnia associated with psychiatric and medical disorders. Are there particular considerations that you take into account when diagnosing those types of patients as well as treating them? Dr. Buysse: *The previous assumption was that if insomnia is associated with another condition, one would be best off just treating that other condition, and then the insomnia should get better*. While there is clearly some evidence that treating comorbid conditions does lead to some improvement in insomnia, in many individuals insomnia may persist, even when the other disorder is adequately or optimally treated. In those cases, it may be *useful to think of insomnia as a comorbid condition rather than as, strictly speaking, a symptom of that other disorder*. *If you think of insomnia as a comorbid condition, then in many cases it’s appropriate to direct treatment at the insomnia itself*. Insomnia is quite pervasive in psychiatric disorders. Eighty percent of outpatients[29] and 90% of inpatients[30] with depression report disturbed sleep. **Oddly enough, this disturbance does not seem to result from depression, as insomnia precedes depressive symptoms in nearly half of patients with first-time MDD**, is concurrent with it 20% of the time, and follows depression 30% of the time.[31] Moreover, in recurrent MDD, insomnia appears before depressed symptoms 56% of the time.[31] This pattern is also seen in the elderly.[13] Ramelteon (Rozerem) is a newly developed *melatonin receptor agonist* that was recently approved by the US Food and Drug Administration (FDA). This agent was studied in a group of older patients with chronic insomnia for 5 weeks.[19] In this study, patients reportedly fell asleep more quickly at 1 week and 5 weeks, slept longer at 1 week, and had no rebound or withdrawal symptoms or increased adverse events. Given the mechanism of action and the likelihood that this agent will produce decreased side effects it may be appropriate for longer-term use. Although more research is needed, this agent may be a promising new development in the pharmacologic treatment of insomnia. — The charter is available at: http://readystump.algebra.com/~asapm
Response:
– Hide quoted text — Show quoted text – Medscape: Another topic that we have discussed in this newsletter is insomnia associated with psychiatric and medical disorders. Are there particular considerations that you take into account when diagnosing those types of patients as well as treating them? Dr. Buysse: *The previous assumption was that if insomnia is associated with another condition, one would be best off just treating that other condition, and then the insomnia should get better*. While there is clearly some evidence that treating comorbid conditions does lead to some improvement in insomnia, in many individuals insomnia may persist, even when the other disorder is adequately or optimally treated. In those cases, it may be *useful to think of insomnia as a comorbid condition rather than as, strictly speaking, a symptom of that other disorder*. *If you think of insomnia as a comorbid condition, then in many cases it’s appropriate to direct treatment at the insomnia itself*. Insomnia is quite pervasive in psychiatric disorders. Eighty percent of outpatients[29] and 90% of inpatients[30] with depression report disturbed sleep. **Oddly enough, this disturbance does not seem to result from depression, as insomnia precedes depressive symptoms in nearly half of patients with first-time MDD**, is concurrent with it 20% of the time, and follows depression 30% of the time.[31] Moreover, in recurrent MDD, insomnia appears before depressed symptoms 56% of the time.[31] This pattern is also seen in the elderly.[13] Ramelteon (Rozerem) is a newly developed *melatonin receptor agonist* that was recently approved by the US Food and Drug Administration (FDA). This agent was studied in a group of older patients with chronic insomnia for 5 weeks.[19] In this study, patients reportedly fell asleep more quickly at 1 week and 5 weeks, slept longer at 1 week, and had no rebound or withdrawal symptoms or increased adverse events. Given the mechanism of action and the likelihood that this agent will produce decreased side effects it may be appropriate for longer-term use. Although more research is needed, this agent may be a promising new development in the pharmacologic treatment of insomnia.
— The charter is available at: http://readystump.algebra.com/~asapm
Response:
I’ve been told that daily doses of sunshine will work miracles with depression, anxiety, and my general well-being. It doesn’t seem to matter that I detest sitting in the sun. It’s a little more tolerable if I have dark sunglasses on and a steady cool breeze. My eyes have always been too sensitive to sunlight, and I hate sweating. But apparently the dark sunglasses cancel out most of the psychological benefits. I looked into light boxes but they are hugely expensive. It’s easier and cheaper to sit in a dimly lit apartment. It’s also more depressing. There’s always a price. — The charter is available at: http://readystump.algebra.com/~asapm
Response:
http://www.rozerem.com/ Rozerem binds to MT1 and MT2 (melatonin) receptors, and thus promotes sleep. The Sleep-Wake Cycle The sleep-wake cycle can best be understood as an alternating period of activity and rest as it relates to the 24-hour cycle of daylight and darkness, or circadian rhythm. The circadian rhythm influences a wide range of biologic functions, but the influence on the sleep-wake cycle is the most familiar.[1] Suprachiasmatic nucleus Circadian rhythms are generated by the expression of "clock" genes in the human body’s internal master clock located in the suprachiasmatic nucleus (SCN). Composed of a small cluster of neurons located in the hypothalamus, the SCN is thought to play an important role in the timing and consolidation of sleep by producing an alerting signal. As with most systems in the body, the sleep-wake cycle is in a state of homeostasis with the alerting signal opposing the sleep load (the need for sleep that increases the longer a person stays awake).[1-5] During the day, the SCN emits an alerting signal that helps maintain wakefulness.[4] Ventrolateral preoptic nucleus If the SCN is the wake-promoting system, then the ventrolateral preoptic nucleus (VLPO) is the sleep-promoting system. The VLPO is situated close to the SCN, but controls a descending group of inhibitory neurons known as sleep pathways. It has a critical role in both sleep initiation and the maintenance of sleep. During the night, sleep load simultaneously stimulates sleep pathways in the brain while inhibiting the SCN’s alerting signal. During the day, the opposite occurs.[6] At night, the alerting signal is attenuated, facilitating the onset of sleep.[3] Sleep switch **The melatonin receptors MT1 and MT2 are heavily concentrated in the SCN**. These are known to be important to the natural promotion and timing of sleep. With the onset of darkness, the pineal gland releases melatonin. Melatonin binds to MT1 and MT2 receptors to attenuate the wake-promoting signal of the SCN, allowing the homeostatic sleep load to promote sleep. Waning levels of melatonin and decreasing sleep load tip the balance again in favor of waking.[3,7] — The charter is available at: http://readystump.algebra.com/~asapm
Response:
http://www.rozerem.com/ Rozerem binds to MT1 and MT2 (melatonin) receptors, and thus promotes
sleep. Some facts about melatonin: 1) it’s secreted by the pineal gland (which is located about in the middle of the brain) 2) it’s a derivative (metabolite) of serotonin 3) the eyes (retinas) are connected to the pineal gland (and thus secretion or non secretion of melatonin) by a series of nerve tracts 4) melatonin is secreted at night between about 9 PM and 4 AM and is thought to help maintain sleep 5) OTC melatonin is made of ground up hog pineal glands and is popular for inducing and maintaining sleep 6) since sleep disorders are often connected with depression and anxiety, melatonin may play some role in both disorders — The charter is available at: http://readystump.algebra.com/~asapm
Response:
Well, that explains why my pdocs always tell me to get some sunshine every day. I sit in a dim room for hours at a time, but semi-darkness is comfortable to me. Perhaps that’s just because it’s easy. Thanks for posting this. Deirdre — The charter is available at: http://readystump.algebra.com/~asapm
Response:
Well, that explains why my pdocs always tell me to get some sunshine every day. I sit in a dim room for hours at a time, but semi-darkness is comfortable to me. Perhaps that’s just because it’s easy.
Why do they tell you to get sunshine? So you’ll sleep better at night? For seasonal affective disorder (SAD)? Chip — The charter is available at: http://readystump.algebra.com/~asapm
