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Understanding Insomnia Medications (cont.)

What are nonbenzodiazepine hypnotics?

Nonbenzodiazepine hypnotic drugs include

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).

TThe 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.

Uses: 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 medications also can 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. Proper dosing is important to minimize the likelihood of side effects and differs between men and women. Patients should allow for a full 8 hours after taking the medication before driving or operating equipment.

Pregnancy and breastfeeding safety: 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.

What are orexin receptor antagonists?

This is a newer class of medications to treat insomnia that also does not fall into the benzodiazepine category. Currently, the only US Food and Drug Administration (FDA)-approved medication in this category is uvorexant (Belsomra).

How does the orexin receptor antagonist drug work?

The drug works by decreasing activity in the wake center of the brain and therefore promoting sleep. This particular type of insomnia medication works on orexin receptors in the lateral hypothalamus in the brain. It acts by decreasing activity in the wake centers of the brain and helping patients transition to sleep. This is in contrast to traditional insomnia medications, which attempt to increase activity in the sleep centers of the brain. The mechanism action of suvorexant (Belsomra) is completely unrelated to both the benzodiazepine and non-benzodiazepine sedative-hypnotic drugs.

Who should not use these medications?

People with the following conditions should not use orexin receptor antagonists:

  • Allergy to orexin antagonists or components of the drug
  • A history of narcolepsy or sudden falling asleep during the day
  • Pregnancy
  • Severe liver impairment

Uses: Take the prescribed dose 30 minutes before bedtime.

Drug or food interactions: Other drugs that depress the brain's functioning, such as alcohol or barbiturates, may increase the likelihood of abnormal behaviors during sleep, drowsiness, and cause an increased risk of side effects.

Side effects: The most significant side effect noted in studies was increased daytime sleepiness. Caution is advised and it should be reported to your doctor if there is any incident of increased abnormal night-time activity such as activity out of bed while not fully awake, "sleep driving" increased symptoms of depression or suicidal thoughts, change in breathing function, sleep paralysis, or hallucinations.

Pregnancy and breastfeeding safety: The drug is classified as Pregnancy Class C since there are no established studies in humans. The drug should be avoided during pregnancy unless the benefits significantly outweigh the risks. Based on animal data, the drug may cause fetal harm when administered to a pregnant woman. Because many drugs are excreted in human milk, caution should be exercised when administered to a woman breastfeeding, as the effect on a nursing infant is not known.

Medically Reviewed by a Doctor on 8/26/2016

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