Insomnia

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The ideal hypnotic drug would be effective at reducing sleep latency and increasing total sleep time and would be free of unwanted side effects. Benzodiazepine receptor agonists, including traditional benzodiazepines, zolpidem, zaleplon, and eszo-piclone, are approved by the FDA for the treatment of insomnia and are first-line therapies..30,31 Not all products are available in all countries. Pharmacologic treatment of insomnia is recommended for transient and short-term insomnia. Long-term use of hypnotics is not contraindicated unless the patient has another contraindication to their use. Eszopiclone is the only sedative hypnotic approved by the FDA for chronic use

up to 6 months. Although not first-line agents for insomnia, sedating antidepressants are prescribed commonly, and the number of prescriptions for antidepressants for this

purpose has increased dramatically over the last 20 years. These and other therapies, detailed below, are used to treat insomnia.

Benzodiazepine Receptor Agonists

There are currently eight benzodiazepine receptor agonists (BZDRAs) approved for insomnia, and the pharmacokinetic differences between these agents help to guide selection depending on patient considerations and specific sleep complaints (Table 41-2). These agents occupy the benzodiazepine receptors on the gamma-aminobutyric acid (GABA) type A receptor complex, resulting in opening of chloride channels that facil itate GABA inhibition a nd promote sleepiness.34 BZDRAs have become the first-line agents for treating insomnia and sleep-maintenance problems because they are all efficacious, have wide therapeutic indices, and in clinical use have a low incidence of abuse.30,34

Patients should be instructed to take BZDRAs at bedtime and to avoid engaging in activities requiring alertness after ingestion. The BZDRAs come closer to the "ideal hypnotic" compared with other agents because they increase total sleep time (except for zaleplon) and reduce sleep latency with fewer adverse effects. Although BZDRAs generally are well-tolerated and have good safety profiles, mild to moderate side effects can occur, and precautions are warranted, especially in high-risk populations.

Precautions and Safety The most common side effects associated with BZDRAs include residual sedation (a prolongation of the sedative effects into the waking hours

after sleep), grogginess, and psychomotor impairment. Careful selection of a hypnotic agent with a duration of action matching the patient's budgeted sleep time can help minimize the risk of residual sedation. BZDRAs should be initiated at low doses, and agents with active metabolites (Table 41-2) should be avoided in elderly patients. BZDRAs may cause anterograde amnesia, defined as memory loss of activities and interactions after ingestion of the drug. All hypnotics can cause anterograde amnesia, and higher doses increase the extent of amnesia.36,37

On discontinuation of hypnotic BZDRAs, patients can experience rebound effects, specifically rebound insomnia that may last for one to two nights. Rebound insomnia occurs more frequently after discontinuation of shorter-duration BZDRAs (e.g., triazolam) compared with long-duration BZDRAs. Intermittent hypnotic therapy with the lowest dose possible reduces the likelihood of tolerance, dependence, and withdrawal when therapy is stopped. Patients should be counseled that rebound insomnia is not necessarily a return of their original symptoms, and it may take a few nights for rebound symptoms to subside.

Sedating Antidepressants

The increasing popularity of sedating antidepressants for the treatment of insomnia resulted in trazodone being the most prescribed drug in 2002.38 Other common an-tidepressants also prescribed for insomnia include amitriptyline, mirta-zapine, ne-fazadone, and doxepin. Antidepressants may be an appealing option for insomnia in patients with concomitant depression. However, at the doses frequently used for sleep, only mirtazapine exhibits significant antidepressant activity. Further, quality clinical studies demonstrating efficacy for treating insomnia are lacking. Side effects from an-tidepressants can be frequent and often are unpleasant, including carryover sedation, grogginess, anticholinergic effects, and weight gain. Tricyclic antidepressants (TCAs) should be used with caution in the elderly and patients with cardiovascular and hepatic impairment. Mirtazapine can cause daytime sedation, dizziness, and weight gain, a

side effect that may worsen concomitant OSA. Trazodone can cause hypotension and dizziness, and should be used with caution in patients with heart disease or hypertension and those taking cardiovascular agents.40, 1

What Receptors Cause Weight Gain

FIGURE 41-1. Primary assessment and initial treatment for complaint of excessive daytime sleepiness. (BZDRA, benzodiazepine receptor agonist; CPAP, continuous positive airway pressure; DA, dopamine agonist; MSLT, multiple sleep latency test; OSA, obstructive sleep apnea; RLS, restless legs syndrome; SNRI, serotonin and norepinephrine reuptake inhibitor; NPSG, nocturnal polysomnography; TCA, tricyclic antidepressant.)

FIGURE 41-1. Primary assessment and initial treatment for complaint of excessive daytime sleepiness. (BZDRA, benzodiazepine receptor agonist; CPAP, continuous positive airway pressure; DA, dopamine agonist; MSLT, multiple sleep latency test; OSA, obstructive sleep apnea; RLS, restless legs syndrome; SNRI, serotonin and norepinephrine reuptake inhibitor; NPSG, nocturnal polysomnography; TCA, tricyclic antidepressant.)

Over-the-Counter and Miscellaneous Agents

Over-the-counter antihistamines such as diphenhydramine are frequently used (usual doses 25 to 50 mg) for difficulty sleeping. Diphenhydramine is approved by the FDA for the treatment of insomnia and can be effective at reducing sleep latency and in-

creasing sleep time. However, diphenhydramine produces undesirable anticholinergic effects and carryover sedation that limit its use. As with TCAs and BZDRAs, diphenhydramine should be used with caution in the elderly. Valerian root is a herbal sleep remedy that has inconsistent effects on sleep but may reduce sleep latency and efficiency at commonly used doses of 400 to 900 mg valerian extract. Ramelteon, a new melatonin receptor agonist, is indicated for insomnia characterized by difficulty with sleep onset. The recommended dose is 8 mg at bedtime. Ramelteon is not a con trolled substance, and thus is a viable option for patients with a history of substance abuse.43

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