Zaleplon

Zaleplon is a relatively new, fast-acting sedative-hypnotic drug for treatment of insomnia. It was approved by the Food and Drug Administration (FDA) in August, 1999. King Pharmaceuticals first marketed the drug, which is sold under the names Sonata and Starnoc. Zaleplon is different from, and is an improvement over, the group of drugs called benzodiazepines, which are also used to treat insomnia. One advantage of zaleplon is that it appears safer and less likely to cause abuse and dependence. Even though they are structurally different, zaleplon and the benzodiazepines inhibit the same receptors in the brain, and they have similar effects.

Uses

Zaleplon is used to treat short-term difficulty in falling asleep. It has been shown to decrease the time to sleep onset for up to 30 minutes in clinical studies. It does not increase total sleep time or decrease the number of awakenings throughout the night.

How Zaleplon Is Taken

Zaleplon is available in 5-mg and 10-mg tablets. The usual starting dose is 5 mg taken immediately before bedtime or during the night if sleeping is difficult. The dose can be increased to 20 mg if needed. In general, medications used to bring on sleep are only used for between seven and ten days.

How Zaleplon Works

Zaleplon is classified as a sedative-hypnotic. It interacts with a protein in the brain called the gamma-aminobutyric acid (GABA) receptor. These receptors control the activity of neurons and, in turn, regulate alertness and sleep. The activity of nerves decreases, when zaleplon binds to the GABA receptors. Ultimately, the reduced brain activity causes sleepiness.

How The Body Affects Zaleplon

The liver contains an enzyme that changes the structure of zaleplon (a process called metabolism) to prepare it for excretion. The majority of zaleplon is excreted in the urine. Zaleplon is excreted very quickly. The half-life, or time needed for the concentration of the drug in the blood to be reduced by half, is about one hour. This short half-life allows zaleplon to be taken in the middle of the night with minimal risk of experiencing side effects in the morning.

Side Effects

Below are the most frequent side effects of zaleplon:

• headache
• edema (fluid collection in certain body parts)
• amnesia
• daytime somnolence (a condition much like sleepwalking)
• Sensitivity to light

Sometimes zaleplon causes "rebound insomnia" after discontinuation, meaning that falling asleep is more difficult than it was before taking the drug.

Risks and Precautions

Dependence and overuse of zaleplon may develop, which may occur with any sleep aid that works the same way as zaleplon.

The video explains a MedWatch Safety Alert from the Food and Drug Administration (FDA) about sedative/hypnotic drugs and the risk of severe allergic reactions and unusual behaviors (e.g., sleep driving) followed by amnesia.

Alternatives

Low- or no-cost treatments for insomnia include good sleep hygiene practices such as avoidance of caffeine, regular exercise, and a quiet, dark bedroom. These often work well, and the benefits of exercise (which are hard to overstate) include improvements in sleep that are comparable to drugs like zaleplon in some studies.^[1]

Other drugs used to treat insomnia include the following:

• Zopiclone (Imovane, Zimovane)
• Eszopiclone (Lunesta)
• Diphenhydramine (Benadryl)
• Estazolam (ProSom)
• Flurazepam (Dalmane)
• Hydroxyzine (Atarax, Vistaril)
• Ramelteon (Rozerem)
• Temazepam (Restoril)
• Triazolam (Halcion)
• Zolpidem (Ambien)

Research

Several clinical trials comparing benzodiazepines with the newer non-benzodiazepine sedative-hypnotics (zaleplon, zolpidem or zopiclone) were summarized in a meta-analysis published in 2004.^[2] The study found few clear and consistent differences between zaleplon and the benzodiazepines in terms of the time taken to fall asleep, total sleep duration, number of awakenings, quality of sleep, adverse events, tolerance, rebound insomnia, and daytime alertness.

Some studies have examined whether zaleplon is likely to cause side effects in the morning if the drug is taken in the middle of the night. In this regard, one study compared the residual effects of zaleplon and zolpidem in 36 healthy volunteers.^[3] Zaleplon had no residual effects when given two hours before rising in the morning, whereas zolpidem impaired memory and reaction times in the morning when given five hours before waking.

References

1. ↑ Ramakrishnan K, Scheid DC. Treatment options for insomnia. Am Fam Physician. 2007 Aug 15;76(4):517-26. Abstract
2. ↑ Dündar Y, Dodd S, Strobl J, Boland A, Dickson R, Walley T. Comparative efficacy of newer hypnotic drugs for the short-term management of insomnia: a systematic review and meta-analysis. Hum Psychopharmacol. 2004 Jul;19(5):305-22. Abstract
3. ↑ Danjou P, Paty I, Fruncillo R, et al. A comparison of the residual effects of zaleplon and zolpidem following administration two to five hours before awakening. Br J Clin Pharmacol. 1999 Sep;48(3):367-74. Abstract |Full Text | PDF

External Links

Sleep Health Centers: Practical Tips for Good Sleep Hygiene