The Food and Drug Administration of the United States approved Zaleplon in 1999 to treat short-term sleep problems. Zaleplon is thought to act by mimicking a chemical in the brain that helps to facilitate sleep. It is different from other sleeping pills in that it begins to work almost immediately and its effects are rather short-lived (a few hours). These properties make it beneficial both for people who have troubling falling asleep at bedtime and for people who awaken in the middle of the night and have trouble falling back to sleep. Zaleplon may be taken in the middle of the night so long as the person can sleep at least four more hours before having to awaken.

Zaleplon is available as capsules. The drug is broken down by the liver. It is a controlled substance and can be habit-forming.

Recommended dosage

The usual dose of zaleplon for adults is 5-20 mg. For healthy adults, 10 mg is a common dosage. However, people over age 65, small adults with low body weight, and people with serious health problems (especially liver disease) should take a dose at the low end of this range (usually 5 mg). Zaleplon is taken immediately before bedtime. It usually takes only about 30 minutes for the sleep-inducing actions of zaleplon to be felt, and sleep-facilitating effects appear to last only a few hours. If zaleplon is taken with a meal, it will take longer to work. For the fastest sleep onset, it should be taken on an empty stomach. The maximum dose for one day is 20 mg. Under no circumstances should a person take more than 20 mg in one day.

Precautions

Zaleplon can be habit-forming and should be taken exactly as directed by a physician. A person who forgets a dose of zaleplon should skip the dose and take the next dose at the regularly scheduled time.

Because zaleplon is used to help people fall asleep, it should not be used with other drugs (over-the-counter or prescription) that also cause drowsiness. Zaleplon should be used only with close physician supervision in people with liver disease and in the elderly, because these individuals are especially sensitive to the sedative properties of zaleplon. Zaleplon should not be used before driving, operating machinery, or performing activities that require mental alertness. People with a history of drug abuse, psychiatric disorders, or depression should be carefully monitored when using zaleplon since zaleplon may worsen symptoms of some psychiatric disorders and can become a drug of abuse.

If zaleplon is needed for more than seven to ten days, patients should be reevaluated by a physician to determine if another disorder is causing their difficulty sleeping. When zaleplon or other sleeping pills are used every night for more than a few weeks, they begin to lose their effectiveness and/or people may become dependent upon them to fall asleep. Zaleplon can be addictive. People using zaleplon should not stop taking the drug suddenly because withdrawal symptoms, including sleep disturbances, may occur even if zaleplon has been used only for a short time.

Side effects

Some sleeping pills such as zaleplon can cause aggressiveness, agitation, hallucinations, and amnesia

KEY TERMS

Amnesia —A general medical term for loss of memory that is not due to ordinary forgetfulness. Amnesia can be caused by head injuries, brain disease, or epilepsy as well as by dissociation.

Antidepressant —A medication used to treat the symptoms of depression.

Antihistamine —A medication used to alleviate allergy or cold symptoms such as runny nose, itching, hives, watering eyes, or sneezing.

Antipsychotic —A medication used to treat psychotic symptoms of schizophrenia such as hallucinations, delusions, and delirium. May be used to treat symptoms in other disorders as well.

Hypnotic —A type of medication that induces sleep.

Milligram (mg) —One-thousandth of a gram. A gram is the metric measure that equals approximately 0.035 ounces.

Tuberculosis —An infection caused by the bacteria Mycobacterium tuberculosis that usually affects the lungs. Individuals with tuberculosis may have nighttime sweating, fever, weight loss, cough, and may spit up blood and mucus.

(memory problems). A patient experiencing these side effects should call a physician immediately. A physician should also be called immediately if a person taking zaleplon develops a fast or irregular heartbeat, chest pains, skin rash, or itching.

The most common side effects of zaleplon are less serious and include dizziness, drowsiness, impaired coordination, upset stomach, nausea, headache, dry mouth, and muscle aches. Other side effects that may occur include: fever, amnesia, tremor, or eye pain. Many side effects appear worse at higher doses, so it is important to use the lowest dose that will induce sleep.

Interactions

Any drug that causes drowsiness may lead to substantially decreased mental alertness and impaired motor skills when taken with zaleplon. Some examples include alcohol, antidepressants such as imipramine or paroxetine, antipsychotics like thioridazine, and some antihistamines.

Because zaleplon is broken down by the liver, it may interact with other drugs also broken down by the liver. For example, the drug rifampin, which is used to treat tuberculosis, may cause zaleplon to be less effective. Alternatively, cimetidine (Tagamet), a drug commonly used to treat heartburn, may cause people to be more sensitive to zaleplon.

Resources

BOOKS

Facts and Comparisons Staff. Drug Facts and Comparisons, 6th ed. St. Louis: A Wolter Kluwer Company, 2002.

Preston, John D., John H. O’Neal, and Mary C. Talaga. Handbook of Clinical Psychopharmacology for Therapists, 4th ed. Oakland, CA: New Harbinger Publications, 2004.

PERIODICALS

Bain, Kevin T. “Management of Chronic Insomnia in Elderly Persons.” American Journal of Geriatric Pharmacotherapy 4.2 (June 2006): 168–92.

Conn, David K. and Robert Madan. “Use of Sleep-Promoting Medications in Nursing Home Residents: Risks versus Benefits.” Drugs and Aging 23.4 (2006): 271–87.

Glass, Jennifer, and others. “Sedative Hypnotics in Older People with Insomnia: Meta-Analysis of Risks and Benefits.” British Medical Journal 331.7526 (Nov. 2005): 1–7.

McCall, W. “Diagnosis and Management of Insomnia in Older People.” Journal of the American Geriatrics Society 53.7 (July 2005): S272–S277.

Rosenberg, Russell P. “Sleep Maintenance Insomnia: Strengths and Weaknesses of Current Pharmacologic Therapies.” Annals of Clinical Psychiatry 18.1 (Jan.–Mar. 2006): 49–56.

Kelly Karpa, R.Ph., PhD

Ruth A. Wienclaw, PhD

The Gale Encyclopedia of Mental Health