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- What is zaleplon, and how does it work (mechanism of action)?
- What brand names are available for zaleplon?
- Is zaleplon available as a generic drug?
- Do I need a prescription for zaleplon?
- What are the uses for zaleplon?
- What are the side effects of zaleplon?
- What is the dosage for zaleplon?
- Which drugs or supplements interact with zaleplon?
- Is zaleplon safe to take if I'm pregnant or breastfeeding?
- What else should I know about zaleplon?
What is zaleplon, and how does it work (mechanism of action)?
Zaleplon is a hypnotic (a medication that induces sleep) that is used for treating insomnia. It is chemically unrelated to the benzodiazepine class of medications for sleep, for example, lorazepam (Ativan), oxazepam (Serax), flurazepam (Dalmane), triazolam (Halcion), and temazepam (Restoril), but it has similar effects because it attaches to the same receptors on nerve cells as these well-known medications. It was approved by the FDA in 1999.
What are the uses for zaleplon?
Zaleplon is used for the short-term treatment of insomnia. It decreases the time to the onset of sleep and was used for up to 5-weeks in clinical trials. It does not increase total sleep time or decrease the number of awakenings.
What are the side effects of zaleplon?
The most common side effects associated with zaleplon are:
Studies have shown that zaleplon has a potential for abuse similar to benzodiazepines. Patients may experience rebound insomnia on the first night after stopping zaleplon. Zaleplon can cause abnormal behavior or thinking or "complex sleep-related behaviors," which may include sleep-driving (driving with no memory of having done so). If these side effects occur, zaleplon should be discontinued.
PREPARATIONS: Capsules: 5 and 10 mg
What is the dosage for zaleplon?
The recommended dose is 5 to 20 mg at bedtime for assistance in falling asleep. Because of its short duration of activity, it is not effective for persons who wake up during the night. Zaleplon should be taken immediately before bedtime or after going to bed and experiencing difficulty falling asleep. Taking zaleplon with a high-fat meal slows its absorption and may also slow its onset of action.
Which drugs or supplements interact with zaleplon?
Rifampin reduces the amount of zaleplon in the blood by more than 80%. This could lead to a decrease in zaleplon's activity. Cimetidine (Tagamet) can increase the amount of zaleplon in the blood by 85% by reducing the breakdown of zaleplon in the liver. If cimetidine must be used, lower doses of zaleplon are suggested. Ketoconazole (Nizoral, Extina, Xolegel, Kuric), erythromycin and similar drugs that reduce breakdown of drugs in the liver also increase blood concentrations of zaleplon. The drowsiness that can occur with zaleplon is accentuated by alcohol, and, therefore, patients taking zaleplon should not drink alcoholic beverages. Imipramine (Tofranil, Tofranil-PM) and thioridazine also increase drowsiness when combined with zaleplon.
Is zaleplon safe to take if I'm pregnant or breastfeeding?
There are no studies of zaleplon in pregnant women. In studies in rats, damage to fetuses were reported. Therefore, zaleplon is not recommended for pregnant women unless the physician feels the benefits outweigh the potential risks.
A small amount of zaleplon is excreted in breast milk. Because the effects of zaleplon on nursing infants are unknown, it is recommended that nursing mothers not take zaleplon.
What else should I know about zaleplon?
How should I keep zaleplon stored?
Capsules should be stored at room temperature, between 20 C - 25 C (68 F - 77 F).
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Drug InteractionsDrug interactions occur frequently. Get facts about the types of drug interactions, what substances or other things that may interact with drugs such as OTC drug and prescription drugs, vitamins, food(s) (grapefruit), and laboratory tests. Find out how to protect yourself from potential drug interactions.
Drugs: What You Should Know About Your DrugsImportant information about your drugs should be reviewed prior to taking any prescription drug. Side effects, drug interactions, warnings and precauctions, dosage, what the drug is used for, what to do if you miss a dose, how the drug is to be stored, and generic vs. brand names.
Hypnotics Drug Class Side Effects
Hypnotics are sleep medications used to treat different types of insomnia. There are a variety of hypnotic drugs, and they are grouped into five types. Benzodiazepines, nonbenzodiazepines, selective melatonin agonists (these three drug types are classified as sedatives), antidepressants, and an orexin receptor agonist. Some hypnotics can be addictive and may cause withdrawal symptoms if discontinued abruptly.
The side effects of hypnotics depend upon the drug used, but they may include:
- Dry mouth
- Rebound insomnia
Other side effects may include:
- Hair loss
- Dry skin
- Upset stomach
- Abnormal dreams
Hypnotics may have serious side effects and adverse effects, for example:
- Abnormal thinking
- Suicidal thinking
- Sleep paralysis
- Sleep driving and other complex behavior
- Exfoliate dermatitis
Hypnotic drugs available over-the-counter (OTC) include diphenhydramine (Benadryl) and doxylamine (Unisom). Natural herbal supplements used for insomnia are melatonin and Valerian.
Do not drink alcohol while taking hypnotic drugs. Stimulants like caffeine or amphetamines reduce the effect of insomnia medications.
Your doctor or other health care professional will recommend the type of hypnotic drug for you depending upon the type of sleep problem you have, your current lifestyle habits, other medications you are taking, and any other medical problems you may have.
FDA. "Sleep Disorder (Sedative-Hypnotic) Drug Information." Updated: Jun 13, 2017.
Chawala, J, MD. "Insomnia Medication." Medscape. Updated: Aug 01, 2016.
InsomniaInsomnia is the perception or complaint of inadequate or poor-quality sleep because of difficulty falling asleep; waking up frequently during the night with difficulty returning to sleep; waking up too early in the morning; or unrefreshing sleep. Secondary insomnia is the most common type of insomnia. Treatment for insomnia include lifestyle changes, cognitive behavioral therapy, and medication.
A number of vital tasks carried out during sleep help maintain good health and enable people to function at their best. Sleep needs vary from individual to individual and change throughout your life. The National Institutes of Health recommend about 7-9 hours of sleep each night for older, school-aged children, teens, and most average adults; 10-12 for preschool-aged children; and 16-18 hours for newborns. There are two stages of sleep; 1) REM sleep (rapid-eye movement), and 2) NREM sleep (non-rapid-eye movement). The side effects of lack of sleep or insomnia include:
- Feeling sleepy during the day
- Concentration or memory problems
Lack of sleep and insomnia can be caused by medical conditions or diseases, medications, stress, or pain. The treatment for lack of sleep and insomnia depends upon the cause.
Sleep Aids And StimulantsInsomnia is difficulty in falling or staying asleep, the absence of restful sleep, or poor quality of sleep. Insomnia is a symptom and not a disease. The most common causes of insomnia are medications, psychological conditions, environmental changes and stressful events. Treatments may include non-drug treatments, over-the-counter medicines, and/or prescription medications.
Take the Sleep QuizTake our Sleeping Quiz to learn which sleep disorders, causes, and symptoms rule the night. Trouble falling or staying asleep? Find out which medical treatments fight sleep deprivation, apnea, insomnia, and more!