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Primary Insomnia (cont.)

Medications

Pharmacologic treatment usually provides rapid symptomatic relief.

Hypnotics (agents that promote sleep) and benzodiazepines (compounds with antianxiety, hypnotic, anticonvulsant, and muscle relaxant properties) are the mainstays of short-term treatment of primary insomnia.

Hypnotics

Basic principles for the treatment of insomnia include the following:

Use the lowest effective dose.

Use intermittent dosing (2-3 nights per week).

Use for short term (2-3 weeks at a time).

Discontinue after slow taper if the person has been taking it regularly.

Use drugs with short and/or intermediate half-life to minimize daytime sedation.

Table 1. Commonly Used Hypnotics

Agent	Dose	Peak action
Long acting
Flurazepam (Dalmane)	15-30 mg	0.5-1 h
Quazepam (Doral)	7.5-15 mg	2 h
Intermediate acting
Eszopiclone (Lunesta)	Nonelderly: 2-3 mg Elderly: 1-2 mg	1 h
Estazolam (ProSom)	1-2 mg	2 h
Temazepam (Restoril)	7.5-30 mg	1.2-1.6 h
Lorazepam (Ativan)	0.5-2 g	2-4 h
Oxazepam (Serax)	10-15 mg	3 h
Short acting
Triazolam (Halcion)	0.125-0.5 mg	1-2 h
Zolpidem* (Ambien)	5-10 mg	1.6 h
Zaleplon* (Sonata)	5-10 mg	0.9-1.5 h

*Zolpidem and Zaleplon are not structurally related to benzodiazepines.

Common side effects of hypnotics are as follows:

Amnesia (total or partial inability to recall past experiences) and withdrawal effects may occur, especially with short-acting benzodiazepines (not with zolpidem and zaleplon).

Residual daytime sedation with intermediate-acting and long-acting drugs may occur, depending on dosage.

Rebound insomnia may occur with short-acting and intermediate-acting benzodiazepine after discontinuation.

Short-acting agents are recommended for persons with difficulty falling asleep, while intermediate-acting drugs are indicated for problems with sleep maintenance.

Avoid long-acting agents, especially in older people, because they cause daytime sedation, impair cognition, and, thereby, increase the risk of falls.

Contraindications of hypnotics are as follows:

Pregnancy

Untreated obstructive sleep apnea

History of substance abuse

Caution and close monitoring is needed in older people and in persons with hepatic, renal, or pulmonary disease.

Antidepressants

Antidepressants are indicated for use in persons with insomnia associated with psychiatric disorders or persons who have a previous history of substance abuse. Sedating (sleep inducing) antidepressants, such as trazodone and nefazodone, are sometimes used at bedtime in small doses (50 mg). They are not associated with tolerance or withdrawal.

Melatonin stimulants

Ramelteon (Rozerem) is a prescription drug that stimulates melatonin receptors. Melatonin is a hormone produced by the pineal gland (located in the brain) during the dark hours of the day-night cycle (circadian rhythm). Melatonin levels in the body are low during daylight hours. The pineal gland responds to darkness by increasing melatonin levels in the body. This process is thought to be integral to maintaining circadian rhythm. Ramelteon promotes the onset of sleep and helps normalize circadian rhythm disorders. Ramelteon is approved by the FDA for insomnia characterized by difficulty falling asleep.

Over-the-counter drugs

The active agent in many of the over-the-counter medications is one of the sedating antihistamines (drugs used for the treatment of allergy). They are generally safe but have side effects such as dry mouth, blurred vision, urinary retention, and confusion in older persons. They are also minimally effective in inducing sleep and may reduce sleep quality. Therefore, these drugs should not be used on a routine basis.

Herbal preparations (eg, herbal tea) and so-called nutritional substances should not be used because of the lack of evidence of efficacy.

Melatonin is a hormone that is thought to induce sleep. Studies have shown that melatonin may be useful for short-term adaptation to jet lag or other circadian rhythm sleep disorders. This hormone is produced by the pineal gland (located in the brain) in response to darkness, and it may be an important part of an individual’s “biologic clock.” Melatonin may be particularly useful for individuals with conditions that do not produce sufficient melatonin in response to darkness, such as blindness. The effectiveness of melatonin for long-term sleeplessness is less clear. Melatonin is sold over the counter and, therefore, is not controlled by the FDA. The optimal dose and its long-term adverse effects are also not known.

For more information, see Understanding Insomnia Medications.