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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. The most effective sleeping pills are benzodiazepines and a newer class of drugs known as non-benzodiazepine, benzodiazepine receptor agonists. 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 effect, which depends on drug half-life. Long-acting benzodiazepines cause a lot of next morning sedation. Short-acting benzodiazepines cause a higher rate of rebound insomnia after discontinuation. Short-acting benzodiazepines are particularly useful for travelers who want to reduce the effects of jet lag. Long-term use (sometimes even after a few weeks) is associated with dependence and withdrawal syndrome. 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). Benzodiazepines are potentially dangerous when used in combination with alcohol, and have potential to interact with other medications. Rebound insomnia, the most common withdrawal symptom, usually occurs on the first night and sometimes the second night after stoping benzodiazepine. In some cases people may experience the return of original severe insomnia. Rebound insomnia is less common with long-acting medications. 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 (BZD) and non-benzodiazepine (non-BZD) hypnotics act on GABA-A receptor sites in the brain. However, non-benzodiazepines are believed to have very low risk of abuse or dependence and fewer side effects. From an efficacy standpoint, there are no clinical trials that show non-BZDs are more effective than the BZDs. These drugs are very effective for preventing jet lag, however zolpidem (Ambien) should not be used on flights less than 7 - 8 hours. They also may be helpful for people with concomitant mood disorders, such as depression. The risk for dependence, tolerance, withdrawal symptoms, and rebound insomnia is lower with non-benzodiazepines than with benzodiazepine hypnotics. Also, non-benzodiazepines generally cause less disruption of sleep architecture than benzodiazepines. As with any hypnotics, alcohol increases the sedative effect of these drugs. These sleep medications also interact with other drugs, including rifampin, ketoconazole, erythromycin, and cimetidine. 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 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 sleep aids have a Schedule IV designation, indicating a low, yet recognizable risk of abuse/addiction. Rozerem may be particularly suitable for adolescents, who don't usually do well on benzodiazepines. It may be the medication of choice for elderly people who have reduced melatonin and trouble falling asleep. Rozerem is not the best choice for severe insomnia or insomnia associated with depression or anxiety. 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 specific mechanism of action, Rozerem may not be the best medication for persons who need sleep promptly because it takes time for the drug to begin working. Zolpidem (Ambien) is one of the most commonly prescribed drugs for insomnia. Large study demonstrated that the drug may be used on an as-needed basis, with up to 5 tablets taken a week1. 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. Zolpidem (Ambien) has a rapid onset of action and a half-life of only 1.5- 2.5 hours. This means that it 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 useful if you tend to wake up frequently in the middle of the night. Zaleplon (Sonata) is the shortest-acting non-benzodiazepine. 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 persons who have trouble falling asleep, wake frequently during the night, or wake up too early in the morning. 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) and is FDA approved for sleep maintenance. Comparison of Non-Benzodiazepines
Sedating antidepressants are 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 antidepressants most commonly used include trazodone (Desyrel), nefazodone (Serzone), amitriptyline (Elavil), nortriptyline (Pamelor), and doxepin (Sinequan). Benefits of these antidepressants include:
During last few years there have been a remarkable rise in the off-label use of trazodone for sleep problems in non-depressed patients, to a degree that it is prescribed for this purpose as commonly as the popular hypnotics. Trazodone also decreases the insomnia caused by selective serotonin reuptake inhibitors and is a good choice for depressed patients with difficulty sleeping. Trazodone 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 rare, but potentially serious side effect of trazodone and may limit its use in men. Trazodone may induce arrhythmias, primarily in persons with histories of cardiac disease. References
Last updated: March 2010 |
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