The circadian nature of melatonin secretion, coupled with the localization of melatonin receptors to the suprachiasmatic nucleus, has led to numerous studies of the role of melatonin in modulation of the sleep-wake cycle and circadian rhythms in humans. Although much more needs to be understood about the various functions exerted by melatonin and its mechanisms of action, three therapeutic agents (ramelteon, prolonged-release melatonin, and agomelatine) are already in use, and melatonin receptor agonists are now appearing as new promising treatment options for sleep and circadian-rhythm related disorders.
Recently, Spadoni et al reviewed the medicinal chemistry strategies leading to MLT receptor agonists, and the evidence supporting therapeutic efficacy of compounds undergoing clinical evaluation.
A wide range of clinical trials demonstrated that ramelteon, prolonged-release melatonin and tasimelteon have sleep-promoting effects, providing an important treatment option for insomnia and transient insomnia, even if the improvements of sleep maintenance appear moderate.
Despite a large number of high affinity nonselective melatonin receptor agonists, only limited data on MT(1) or MT(2) subtype-selective compounds are available up to now. Administration of the MT(2)-selective agonist IIK7 to rats has proved to decrease NREM sleep onset latency, suggesting that MT(2) receptor subtype is involved in the acute sleep-promoting action of melatonin; rigorous clinical studies are needed to demonstrate this hypothesis. Further clinical candidates based on selective activation of MT(1) or MT(2) receptors are expected in coming years.
5/16/2011
5/12/2011
Overview of cognitive behavioral therapy for insomnia
A recent study found that Cognitive Behavioral Therapy for Insomnia (CBT-I) is more effective than hypnotic medications in controlling insomnia.
In Cognitive Behavioral Therapy, patients are taught improved sleep habits and relieved of counter-productive assumptions about sleep. Common misconceptions and expectations that can be modified include:
1. Unrealistic sleep expectations (e.g., I need to have 8 hours of sleep each night).
2. Misconceptions about insomnia causes (e.g., I have a chemical imbalance causing my insomnia).
3. Amplifying the consequences of insomnia (e.g., I cannot do anything after a bad night's sleep).
4. Performance anxiety after trying for so long to have a good night's sleep by controlling the sleep process.
Numerous studies have reported positive outcomes of combining cognitive behavioral therapy for insomnia treatment with treatments such as stimulus control and the relaxation therapies. Hypnotic medications are equally effective in the short-term treatment of insomnia but their effects wear off over time due to tolerance. The effects of CBT-I have sustained and lasting effects on treating insomnia long after therapy has been discontinued. The addition of hypnotic medications with CBT-I adds no benefit in insomnia. The long lasting benefits of a course of CBT-I shows superiority over pharmacological hypnotic drugs. Even in the short term when compared to short-term hypnotic medication such as zolpidem (Ambien), CBT-I still shows significant superiority. Thus CBT-I is recommended as a first line treatment for insomnia.
In Cognitive Behavioral Therapy, patients are taught improved sleep habits and relieved of counter-productive assumptions about sleep. Common misconceptions and expectations that can be modified include:
1. Unrealistic sleep expectations (e.g., I need to have 8 hours of sleep each night).
2. Misconceptions about insomnia causes (e.g., I have a chemical imbalance causing my insomnia).
3. Amplifying the consequences of insomnia (e.g., I cannot do anything after a bad night's sleep).
4. Performance anxiety after trying for so long to have a good night's sleep by controlling the sleep process.
Numerous studies have reported positive outcomes of combining cognitive behavioral therapy for insomnia treatment with treatments such as stimulus control and the relaxation therapies. Hypnotic medications are equally effective in the short-term treatment of insomnia but their effects wear off over time due to tolerance. The effects of CBT-I have sustained and lasting effects on treating insomnia long after therapy has been discontinued. The addition of hypnotic medications with CBT-I adds no benefit in insomnia. The long lasting benefits of a course of CBT-I shows superiority over pharmacological hypnotic drugs. Even in the short term when compared to short-term hypnotic medication such as zolpidem (Ambien), CBT-I still shows significant superiority. Thus CBT-I is recommended as a first line treatment for insomnia.
5/11/2011
Sleep Restriction for insomniac
Sleep restriction is a component of stimulus control therapy. It aims to match the time spent in bed with actual time spent asleep. It involves maintaining a strict sleep-wake schedule, sleeping only at certain times of the day and for specific amounts of time to induce mild sleep deprivation.
It is achieved by averaging the time in bed that the patient spends only sleeping. Rigid bedtime and rise time are set, and the patient is forced to get up at the rising time even if they feel sleepy. This may help the patient sleep better the next night because of the sleep deprivation from the previous night.
Complete treatment usually lasts up to 3 weeks. At the begining, make oneself sleep for only a minimum amount of time that they are actually capable of on average, and then, if capable (i.e. when sleep efficiency improves), slowly increasing this amount (~15 min) by going to bed earlier as the body attempts to reset its internal sleep clock.
Sleep restriction has been helpful in some cases.
It is achieved by averaging the time in bed that the patient spends only sleeping. Rigid bedtime and rise time are set, and the patient is forced to get up at the rising time even if they feel sleepy. This may help the patient sleep better the next night because of the sleep deprivation from the previous night.
Complete treatment usually lasts up to 3 weeks. At the begining, make oneself sleep for only a minimum amount of time that they are actually capable of on average, and then, if capable (i.e. when sleep efficiency improves), slowly increasing this amount (~15 min) by going to bed earlier as the body attempts to reset its internal sleep clock.
Sleep restriction has been helpful in some cases.
5/08/2011
Stimulus control therapy for insomnia
Stimulus control therapy is a treatment for patients who have conditioned themselves to associate the bed, or sleep in general, with a negative response. As stimulus control therapy involves taking steps to control the sleep environment, it is sometimes referred interchangeably with the concept of sleep hygiene.
Examples of stimulus control therapy include:
1. Go to bed when you feel sleepy and when there is a high likelihood that sleep will occur.
2. Do not watch TV, read, eat, or worry in bed. Your bed should be used only for sleep and sexual activity.
3. If you do not fall asleep 30 minutes after going to bed, get up and go to another room and resume your relaxation techniques.
4. Reduce the subjective effort and energy expended trying to fall asleep.
5. Set your alarm clock to get up at a certain time each morning, even on weekends. Do not oversleep.
6. Avoid exposure to bright light during nighttime hours.
7. Avoid taking naps in the daytime.
Examples of stimulus control therapy include:
1. Go to bed when you feel sleepy and when there is a high likelihood that sleep will occur.
2. Do not watch TV, read, eat, or worry in bed. Your bed should be used only for sleep and sexual activity.
3. If you do not fall asleep 30 minutes after going to bed, get up and go to another room and resume your relaxation techniques.
4. Reduce the subjective effort and energy expended trying to fall asleep.
5. Set your alarm clock to get up at a certain time each morning, even on weekends. Do not oversleep.
6. Avoid exposure to bright light during nighttime hours.
7. Avoid taking naps in the daytime.
5/06/2011
Sleep hygiene for insomniac
Sleep hygiene is a variety of different practices that are necessary to have normal, quality nighttime sleep and full daytime alertness.
Good sleep hygiene practices include:
1. Sleep and wake pattern
The most important sleep hygiene measure is to maintain a regular sleep and wake pattern seven days a week. It is also important to spend an appropriate amount of time in bed, not too little, or too excessive. This may vary by individual; for example, if someone has a problem with daytime sleepiness, they should spend a minimum of eight hours in bed, if they have difficulty sleeping at night, they should limit themselves to 7 hours in bed in order to keep the sleep pattern consolidated.
2. Regular relaxing bedtime routine
Try to avoid emotionally upsetting conversations and activities before trying to go to sleep. Don't dwell on, or bring your problems to bed.
3. Associate your bed with sleep
It's not a good idea to use your bed to watch TV, listen to the radio, or read.
4. Good sleep environment
Make sure that the sleep environment is pleasant and relaxing. The bed should be comfortable, the room should not be too hot or cold, or too bright.
5. Exercise
Exercise can promote good sleep. Vigorous exercise should be taken in the morning or late afternoon. A relaxing exercise, like yoga, can be done before bed to help initiate a restful night's sleep.
6. Light
Ensure adequate exposure to natural light. This is particularly important for older people who may not venture outside as frequently as children and adults. Light exposure helps maintain a healthy sleep-wake cycle.
6. No napping
Avoid napping during the day; it can disturb the normal pattern of sleep and wakefulness.
7. No stimulants
Avoid stimulants such as caffeine, nicotine, and alcohol too close to bedtime. While alcohol is well known to speed the onset of sleep, it disrupts sleep in the second half as the body begins to metabolize the alcohol, causing arousal.
8. No food before sleep
Food can be disruptive right before sleep; stay away from large meals close to bedtime. Also dietary changes can cause sleep problems, if someone is struggling with a sleep problem, it's not a good time to start experimenting with spicy dishes. And, remember, chocolate has caffeine.
Good sleep hygiene practices include:
1. Sleep and wake pattern
The most important sleep hygiene measure is to maintain a regular sleep and wake pattern seven days a week. It is also important to spend an appropriate amount of time in bed, not too little, or too excessive. This may vary by individual; for example, if someone has a problem with daytime sleepiness, they should spend a minimum of eight hours in bed, if they have difficulty sleeping at night, they should limit themselves to 7 hours in bed in order to keep the sleep pattern consolidated.
![]() |
| Do not disturb your biological clock |
2. Regular relaxing bedtime routine
Try to avoid emotionally upsetting conversations and activities before trying to go to sleep. Don't dwell on, or bring your problems to bed.
![]() |
| Do not think when going to bed. Sleep like a baby. |
3. Associate your bed with sleep
It's not a good idea to use your bed to watch TV, listen to the radio, or read.
![]() |
| Make you bed comfortable |
4. Good sleep environment
Make sure that the sleep environment is pleasant and relaxing. The bed should be comfortable, the room should not be too hot or cold, or too bright.
5. Exercise
Exercise can promote good sleep. Vigorous exercise should be taken in the morning or late afternoon. A relaxing exercise, like yoga, can be done before bed to help initiate a restful night's sleep.
![]() |
| Yoga is good for your sleep |
6. Light
Ensure adequate exposure to natural light. This is particularly important for older people who may not venture outside as frequently as children and adults. Light exposure helps maintain a healthy sleep-wake cycle.
![]() |
| Light is good. |
6. No napping
Avoid napping during the day; it can disturb the normal pattern of sleep and wakefulness.
![]() |
| No nap for insomniac |
7. No stimulants
Avoid stimulants such as caffeine, nicotine, and alcohol too close to bedtime. While alcohol is well known to speed the onset of sleep, it disrupts sleep in the second half as the body begins to metabolize the alcohol, causing arousal.
![]() |
| Smoking is bad for your sleep |
8. No food before sleep
Food can be disruptive right before sleep; stay away from large meals close to bedtime. Also dietary changes can cause sleep problems, if someone is struggling with a sleep problem, it's not a good time to start experimenting with spicy dishes. And, remember, chocolate has caffeine.
![]() |
| Do not eat spicy food |
5/05/2011
Treatment of Insomnia
It is important to identify or rule out medical and psychological causes before deciding on the treatment for insomnia. The treatment of insomnia is including:
1. Non-pharmacological strategies:
Non-pharmacological strategies are superior to hypnotic medication for insomnia because tolerance develops to the hypnotic effects. In addition, dependence can develop with rebound withdrawal effects developing upon discontinuation. Hypnotic medication is therefore only recommended for short-term use, especially in acute or chronic insomnia. Non pharmacological strategies however, have long lasting improvements to insomnia and are recommended as a first line and long term strategy of managing insomnia.
Non pharmacological strategies include:
(1). Sleep hygiene
(2). Stimulus control
(3). Behavioral interventions
(4). Sleep-restriction therapy
(5). Paradoxical intention
(6). Patient education
(7). Relaxation therapy
(8). Cognitive behavioral therapy for insomnia
2. Medications
Many insomniacs rely on sleeping tablets and other sedatives to get rest, with research showing that medications are prescribed to over 95% of insomniac cases.
The medications for insomnia include:
(1). Benzodiazepines
(2). Non-benzodiazepines
(3). Opioids
(4). Antidepressants
(5). Melatonin and melatonin agonists
(6). Antihistamines
(7). Atypical antipsychotics
(8). Other substances, for example, Some insomniacs use herbs such as valerian, chamomile, lavender, hops, and passion-flower.
1. Non-pharmacological strategies:
Non-pharmacological strategies are superior to hypnotic medication for insomnia because tolerance develops to the hypnotic effects. In addition, dependence can develop with rebound withdrawal effects developing upon discontinuation. Hypnotic medication is therefore only recommended for short-term use, especially in acute or chronic insomnia. Non pharmacological strategies however, have long lasting improvements to insomnia and are recommended as a first line and long term strategy of managing insomnia.
Non pharmacological strategies include:
(1). Sleep hygiene
(2). Stimulus control
(3). Behavioral interventions
(4). Sleep-restriction therapy
(5). Paradoxical intention
(6). Patient education
(7). Relaxation therapy
(8). Cognitive behavioral therapy for insomnia
2. Medications
Many insomniacs rely on sleeping tablets and other sedatives to get rest, with research showing that medications are prescribed to over 95% of insomniac cases.
The medications for insomnia include:
(1). Benzodiazepines
(2). Non-benzodiazepines
(3). Opioids
(4). Antidepressants
(5). Melatonin and melatonin agonists
(6). Antihistamines
(7). Atypical antipsychotics
(8). Other substances, for example, Some insomniacs use herbs such as valerian, chamomile, lavender, hops, and passion-flower.
Causes of Insomnia
Symptoms of insomnia can be caused by:
1. Environmental factors, e.g., noise
2. Disturbances of the circadian rhythm, such as shift work and jet lag, can cause an inability to sleep at some times of the day and excessive sleepiness at other times of the day. Chronic circadian rhythm disorders are characterized by similar symptoms.
3. Life events, such as fear, stress, anxiety, emotional or mental tension, work problems, financial stress, birth of a child and bereavement.
4. Hormone shift, such as those that precede menstruation and those during menopause.
5. Diseases:
(1). Restless legs syndrome, which can cause sleep onset insomnia due to discomforting sensations felt and the need to move the legs or other body parts to relieve these sensations.
(2). Periodic limb movement disorder, which occurs during sleep and can cause arousals that the sleeper is unaware of.
(3). Pain. An injury or condition that causes pain can preclude an individual from finding a comfortable position in which to fall asleep, and can in addition cause awakening.
(4). Parasomnias, which include such disruptive sleep events as nightmares, sleepwalking, night terrors, violent behavior while sleeping, and REM behavior disorder, in which the physical body moves in response to events within dreams.
(5). Medical disorders, such as hyperthroidism and rheumatoid arthritis.
(6). Neurological disorders, like brain lession, or a history of traumatic brain injury.
(7). Mental disorders, such as bipolar disorder, clinical depression, generalized anxiety disorder, post traumatic stress disorder, schizophrenia, obsessive complusive disorder, Dementia or excessive alcohol intake.
6. Drugs:
(1). Certain psychoactive drugs or stimulants, including certain medications, herbs, caffeine, cocaine, amphetamines, methylphenidate, MDMA and modafinil.
(2). Fluoroquinolone antibiotic drugs
(3). Abuse of over-the counter or prescription sleep aids can produce rebound insomnia.
7. A rare genetic condition can cause a prion-based, permanent and eventually fetal form of insomnia called fetal familial insomnia.
1. Environmental factors, e.g., noise
2. Disturbances of the circadian rhythm, such as shift work and jet lag, can cause an inability to sleep at some times of the day and excessive sleepiness at other times of the day. Chronic circadian rhythm disorders are characterized by similar symptoms.
3. Life events, such as fear, stress, anxiety, emotional or mental tension, work problems, financial stress, birth of a child and bereavement.
4. Hormone shift, such as those that precede menstruation and those during menopause.
5. Diseases:
(1). Restless legs syndrome, which can cause sleep onset insomnia due to discomforting sensations felt and the need to move the legs or other body parts to relieve these sensations.
(2). Periodic limb movement disorder, which occurs during sleep and can cause arousals that the sleeper is unaware of.
(3). Pain. An injury or condition that causes pain can preclude an individual from finding a comfortable position in which to fall asleep, and can in addition cause awakening.
(4). Parasomnias, which include such disruptive sleep events as nightmares, sleepwalking, night terrors, violent behavior while sleeping, and REM behavior disorder, in which the physical body moves in response to events within dreams.
(5). Medical disorders, such as hyperthroidism and rheumatoid arthritis.
(6). Neurological disorders, like brain lession, or a history of traumatic brain injury.
(7). Mental disorders, such as bipolar disorder, clinical depression, generalized anxiety disorder, post traumatic stress disorder, schizophrenia, obsessive complusive disorder, Dementia or excessive alcohol intake.
6. Drugs:
(1). Certain psychoactive drugs or stimulants, including certain medications, herbs, caffeine, cocaine, amphetamines, methylphenidate, MDMA and modafinil.
(2). Fluoroquinolone antibiotic drugs
(3). Abuse of over-the counter or prescription sleep aids can produce rebound insomnia.
7. A rare genetic condition can cause a prion-based, permanent and eventually fetal form of insomnia called fetal familial insomnia.
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