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Sleeping Pills. Sedative Hypnotics Overview.
Insomnia is an experience of inadequate or poor quality sleep as characterized by one or more of the following sleep complaints:
Insomnia is not a serious medical condition but it can greatly affect the person’s work and social life. Sleep (sedative-hypnotic) medications are medicines that have been shown to reduce the length of time it takes to fall asleep or increase sleep duration. These medicines are usually taken at bedtime to relieve the symptoms of insomnia, although some newer medications may be appropriate for use on an "as needed" basis, whenever symptoms occur. There are different classes of sedative-hypnotic medications. However, most of these medicines fall into a class of drugs known as benzodiazepines, or into a newer class of drugs known as "non-benzodiazepine, benzodiazepine receptor agonists." Prescription medications that promote sleep are called hypnotics. These are the most effective sleep aids available. Sleep medications may be taken when:
Treatment with medications should:
Disadvantages of sleep medications
Advantages of sleep medications
Benzodiazepines, also referred to as benzodiazepine receptor agonists, were once the most commonly prescribed sedative hypnotics. These drugs were originally developed in the 1960s to treat anxiety. They have since proven effective and safe. The main difference among benzodiazepines is length of effectiveness, or half life, in the body. Longer-acting benzodiazepines cause a lot of carry-over morning sedation, and shorter-acting benzodiazepines cause a higher incidence of rebound insomnia after discontinuation. There is a risk for developing drug dependency with long-term use. Long acting benzodiazepines include: flurazepam (Dalmane), clonazepam (Klonopin), quazepam (Doral). Medium- to short-acting benzodiazepines include triazolam (Halcion), lorazepam (Ativan), alprazolam (Xanax), temazepam (Restoril), oxazepam (Serax), prazepam (Centrax), estazolam (ProSom), and flunitrazepam (Rohypnol). Short-acting benzodiazepines are particularly useful for air travelers who want to reduce the effects of jet lag. Benzodiazepines are potentially dangerous when used in combination with alcohol, and some medications, like the ulcer medication cimetidine, can slow the metabolism of the benzodiazepine. Rebound insomnia, which often occurs after withdrawal, typically includes one to two nights of sleep disturbance, daytime sleepiness, and anxiety. In some cases patients may experience the return of original severe insomnia. The chances for rebound are higher with the short-acting benzodiazepines than with the longer-acting ones. Non-Benzodiazepines - Short-acting sedative-hypnotics In the late 1980s a newer class of medications, known as non-benzodiazepine, benzodiazepine receptor agonists were introduced for the treatment of insomnia. The drugs in this class are as effective as the benzodiazepines in promoting sleep. Both benzodiazepine and non-benzodiazepine sedative hypnotics act on GABA-A receptor sites in the brain. However, they are believed to be associated with a very low risk of abuse or dependence and fewer adverse effects than the benzodiazepines. From an efficacy standpoint, there are no clinical trials that show that non-BZDs are more effective than the BZDs. These drugs can be particularly helpful for preventing jet lag (but zolpidem should not be used on flights less than 7 - 8 hours). They also may be helpful for people who also have accompanying mood disorders, such as depression or post-traumatic stress disorder. Because they are short-acting, zaleplon and zolpidem may pose fewer risks for falls and memory loss in elderly patients. The risk for rebound insomnia, dependence, and tolerance is lower with non-benzodiazepine hypnotics than with benzodiazepine drugs. However, these drugs are still subject to abuse. As non-benzodiazepines have relatively short half life these medications do not cause “hangover” the following day. As with any hypnotics, alcohol increases the sedative affects of these drugs. These hypnotics also interact with other drugs, including rifampin, ketoconazole, erythromycin, and cimetidine. They may also interfere or be interfered by other drugs. Patients should report all medications to their doctors. Ramelteon (Rozerem) was approved by the FDA in July 2005. Rozerem is a novel non-benzodiazepine hypnotic. Rozerem is the first insomnia medication in a new drug class known as the melatonin receptor agonists. Unlike other prescription sleep medications, Rozerem works by mimicking the actions of melatonin in the body. Melatonin is a hormone released by the brain that is believed to be important in the sleep-wake cycle. Rozerem also differs from other sleep medications because in clinical studies, it has demonstrated no abuse potential, no withdrawal syndrome and no rebound insomnia. These findings led to Rozerem’s market approval without a controlled designation. All other prescription sleep aids have a Schedule IV designation, indicating a low, yet recognizable risk of abuse/addiction. Rozerem may be particularly helpful in adolescents - who don’t usually do well on typical sleep medications. It may also be helpful for insomnia in the elderly who have reduced melatonin (that usually peaks in the late afternoon or evening). Rozerem probably won’t be helpful for severe insomnia or insomnia associated with anxiety or mood disorders. Development of tolerance hasn’t been seen but there are no very long studies. It may be helpful if added on to other sleeping pills when they are not fully effective. Rozerem has the following advantages over the other benzodiazepines and non-benzodiazepines:
Because of its different mechanism of action, Rozerem may not be the best medication for someone who needs sleep immediately because it takes time for the drug to begin working. Zolpidem (Ambien) is one of the most commonly prescribed drugs for insomnia. A 2002 study suggested that the drug might be used on an as-needed basis, with up to 5 tablets taken a week. After 3 weeks, two-thirds of the patients taking zolpidem this way were able to reduce their tablet intake by more than 25% without losing improvements in sleep. Ambien has a medium half-life. It has a rapid onset of action and a half-life of only 1.5- 2.5 hours. This means that Ambien may be taken later in the night when having trouble falling asleep without worrying about residual cognitive impairment the next morning. Ambien decreases sleep latency and increases total sleep time. Unlike nonselective -benzodiazepines, Ambien does not decrease REM or sleep. Ambien could be less helpful if you tend to wake up a lot in the middle of the night. Zaleplon (Sonata) is the shortest-acting hypnotic available. Its half-life is just one hour. That means you can try to fall asleep on your own. Then, if you're still staring at the clock at 2 a.m., you can take it without feeling drowsy in the morning. The drug takes effect within 30 minutes and may be taken at bedtime or later as long as you can sleep for at least 4 hours. However, if you tend to wake during the night, this might not be the best choice for you. Sonata appears to have a better safety record than other hypnotics and may be particularly useful for patients in the younger and older age groups. Eszopiclone (Lunesta) is a new, non-benzodiazepine hypnotic approved by the FDA in December 2004. It may help improve both sleep maintenance and daytime alertness. Eszopiclone is related to zopiclone (Imovane), which has been used for many years in Europe. Unlike other sleep medications, Lunesta can be taken on a long-term basis. In clinical trials, patients used Lunesta for up to 6 months. Of all the new sleeping pills approved so far, Lunesta has the longest half-life - about 6 hours. The FDA has approved Lunesta for patients who have difficulty falling asleep as well as those who are unable to sleep through the night. benzodiazepine Comparison of Non-Benzodiazepines
Sedating antidepressants are prescription medications that have been developed for the treatment of depression, but that are known to have sedative side effects. These medications have been used for many years to promote sleep. The sedating antidepressant medications most commonly used include trazodone (Desyrel), nefazodone (Serzone), amitriptyline (Elavil), nortriptyline (Pamelor), and doxepin (Sinequan). Benefits of these antidepressants include:
The last few years have seen a remarkable rise in the off-label use of trazodone for inducing sleep in non-depressed patients, to a degree that it is prescribed for this purpose as commonly as the leading hypnotics. Trazodone also decreases the insomnia caused by selective serotonin reuptake inhibitors and is a good choice for depressed patients with difficulty sleeping. Trazodone does not disturb sleep architecture and is not associated with tolerance or dependence. Trazodone does not affect sleep latency but does decrease REM sleep and may be associated with significant rebound insomnia. It has an advantage over benzodiazepines in that it does not cause respiratory depression and anticholinergic effects. Priapism is a potentially serious side effect of trazodone and may limit its use in men. Trazodone has more serious potential side effects for induction of arrhythmias, primarily in patients with histories of cardiac disease. Interesting Facts
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