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Understanding Insomnia Medications (cont.)

Nonbenzodiazepine Hypnotics

Nonbenzodiazepine hypnotic drugs include eszopiclone (Lunesta), zaleplon (Sonata), and zolpidem (Ambien, Ambien CR), zolpidem tartrate (Intermezzo sublingual).

How do sedative hypnotic drugs work?

Although these drugs are not chemically like benzodiazepines, they bind to a specific benzodiazepine receptor in the brain called omega-1, thereby inducing sleep. They may be less likely than benzodiazepine medications to disrupt natural sleep rhythm patterns (called the rapid eye movement [REM] ratio). Disruption of REM sleep may make sleep less restful. How Lunesta works is not fully understood. Lunesta is thought to promote sedation and to affect brain receptor sites that are close to gamma-aminobutyric acid (GABA).

The extended-release product (Ambien CR) consists of a coated 2-layer tablet and is useful for insomnia characterized by difficulties with sleep onset and/or sleep maintenance. The first layer releases drug content immediately to induce sleep, whereas the second layer gradually releases additional drug to provide continuous sleep.

Who should not use these medications?

People with an allergy to sedative hypnotics should not take them.

Use: Take the prescribed dose 30 minutes before bedtime. Elderly individuals are prescribed smaller doses. If taking an extended-release product, such as Ambien CR, it must be swallowed whole (do not divide, chew, or crush). If taking Intermezzo sublingual tablet, it must be placed under the tongue and allow it to break apart completely, then swallow. It also must be taken only if you have at least 4 hours of sleep time left.

Drug or food interactions: Other drugs that depress the brain's functioning, such as alcohol or barbiturates may increase drowsiness and cause an increased risk of toxicity. Cimetidine (Tagamet) increases Sonata levels, thereby increasing the risk of toxicity. Antidepressant medication can also interact with sedative hypnotic medications by causing additive affects and dose adjustment of concomitant CNS depressants may be necessary. Ketoconazole (Nizoral), itraconazole (Sporanox), clarithromycin (Biaxin), nefazodone (Serzone), ritonavir (Norvir, Kaletra), and nelfinavir (Viracept) may increase blood levels of Lunesta, therefore increasing the risk for side effects. Zolpidem's effect may be delayed if taken with food or shortly after a meal.

Side effects: Common side effects include drowsiness and dizziness, possibly impairing coordination, balance, and/or mental alertness. These drugs must be used with caution in individuals with a history of drug abuse or dependence. Ambien, Lunesta, and Sonata work very quickly and should only be taken just before going to bed.

Pregnancy: Nonbenzodiazepine hypnotics are Pregnancy Category C. This means there are no adequate and well-controlled studies in pregnant women for non-benzodiazepines. Consult a physician to determine if the potential benefit justifies the potential risk to the fetus. Because many drugs are excreted in human milk, caution should be exercised when administered to a nursing woman as the effect of on a nursing infant is not known.

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Insomnia »

Insomnia is defined as repeated difficulty with the initiation, duration, maintenance, or quality of sleep that occurs despite adequate time and opportunity for sleep that results in some form of daytime impairment.

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