Although safe, this dosage has not been approved by the FDA for the treatment of insomnia. 18, 37 Doxepin is also available in a much less expensive generic formulation in 10-mg capsules. 36 The adverse effect profile of both doses is favorable in older adults and similar to placebo, even when used long term. Compared with placebo, doxepin at doses of 3 and 6 mg improves sleep efficiency and total sleep time, and a 6-mg dose improves sleep latency. The mechanism of action is not known but is likely related to antagonism of the histamine H 1 receptor. Because of their abuse potential, eszopiclone, zaleplon, and zolpidem are classified as schedule IV drugs.Īlthough antidepressants have been widely used for their sedative effects, only the tricyclic antidepressant doxepin (Silenor) has been FDA approved for the treatment of insomnia characterized by difficulties with sleep maintenance. These agents should be used during pregnancy only if the benefits outweigh the risks. Each of the z-drugs has a slightly different pharmacologic profile, indications, effectiveness, and adverse effect profile ( Tables 1 13 and 2 32 ). Zaleplon, a pyrazolopyrimidine drug, has an extremely short half-life and is indicated for improving sleep latency but not sleep maintenance. 31 One unique adverse effect of eszopiclone is unpleasant taste that affects nearly one-third of patients at the maximum recommended dosage. 28 – 30 Eszopiclone is a cyclopyrrolone drug that has been used to improve sleep latency, and it is particularly well suited for sleep maintenance given its long half-life. 18 In addition to treating insomnia related to difficulty with sleep latency and sleep maintenance, zolpidem, an imidazopyridine agent, has been used to treat circadian rhythm misalignment and high-altitude insomnia. The z-drugs have been used to treat a broad array of sleep problems without sacrificing sleep efficiency. 24 – 26 The prescriber must be aware of the abuse potential of the z-drugs because they may cause stimulation, euphoria, and anxiolysis in some patients, particularly at high dosages. Uncommonly, complex sleep-related behaviors (e.g., sleep driving, sleep eating) have been reported in patients taking high doses of z-drugs this risk should be discussed with patients when these medications are initially prescribed. 23 Like benzodiazepines, the z-drugs have several adverse effects, particularly in higher dosages, including memory loss, dizziness, disinhibition, gastrointestinal upset, and hallucinations. However, unlike benzodiazepines, the z-drugs bind more selectively to certain subunits of the GABA A receptor, primarily targeting the sedative effect of the receptor rather than the anxiolytic effect. 22 Like benzodiazepines, the z-drugs bind to the GABA A receptor, causing hyperpolarization of the cell.

21 Numerous trials have demonstrated the effectiveness of these drugs, including a recent meta-analysis that showed that they decreased sleep latency by an average of 42 minutes vs. The most commonly prescribed class of medication for insomnia is the so-called z-drugs, zaleplon (Sonata), zolpidem (Ambien), and eszopiclone (Lunesta). Persons with sleep apnea or chronic lung disease with nocturnal hypoxia should be evaluated by a sleep specialist before sedating medications are prescribed. Sedating antihistamines, antiepileptics, and atypical antipsychotics are not recommended unless they are used primarily to treat another condition. Although the orexin receptor antagonist suvorexant appears to be relatively effective, it is no more effective than the z-drugs and much more expensive. Benzodiazepines are not recommended because of their high abuse potential and the availability of better alternatives. For those who have difficulty staying asleep, low-dose doxepin and the z-drugs should be considered. For the general population with difficulty falling asleep, controlled-release melatonin and the z-drugs can be considered. Controlled-release melatonin and doxepin are recommended as first-line agents in older adults the so-called z-drugs (zolpidem, eszopiclone, and zaleplon) should be reserved for use if the first-line agents are ineffective. Understanding the risks and benefits of insomnia medications is critical. Although behavioral interventions are the mainstay of treatment, pharmacologic therapy may be necessary for some patients. Insomnia accounts for more than 5.5 million visits to family physicians each year.

Trazodone for insomnia elderly