Many Americans use some form of sleep aid pill, including prescription or over-the-counter drugs. Over-the-counter (nonprescription) medications make use of the drowsiness caused by some common medications. Prescription drugs used specifically for improving sleeping are called sedative hypnotics. These drugs include benzodiazepines and non-benzodiazepines.
Sedative hypnotics carry risks for dependence, tolerance, and rebound insomnia:
Dependence means relying on a drug for falling asleep and having difficulty falling asleep or achieving restful sleep without it.
Tolerance is being unable to fall asleep using the original dose and needing to take progressively higher doses of medication.
Rebound insomnia can occur after a patient stops taking the drug. It typically causes 1 - 2 nights of sleep disturbance, daytime sleepiness, and anxiety. In some cases, patients may experience a temporary worsening of long-term insomnia.
Common Non-Prescription Sleep Medications
Brands with Antihistamines. Many over-the-counter sleeping medications use antihistamines, which cause drowsiness. Diphenhydramine (Benadryl, generic) is the most common antihistamine used in non-prescription sleep aids.
Some drugs marketed as sleep aids contain diphenhydramine alone, while others contain combinations of diphenhydramine with pain relievers (such as Tylenol PM and its generic forms). Doxylamine (Unison, generic) is another antihistamine used in sleep medications. Certain antihistamines indicated only for allergies, such as chlorpheniramine (Chlor-Trimeton, generic) or hydroxyzine (Atarax, Vistaril, generic) may also be used as mild sleep-inducers.
Unfortunately, most of these drugs leave patients feeling drowsy the next day and may not be very effective in providing restful sleep. Side effects include:
- Daytime sleepiness
- Cognitive impairment
- Drunken movements
- Blurred vision
- Dry mouth and throat
In general, people with angina, heart arrhythmias, glaucoma, or problems urinating should avoid these drugs. They should not be used at the same time as medications that prevent nausea or motion sickness. Patients with chronic lung disease should also avoid some non-prescription sleeping aids, such as those containing doxylamine.
Common Pain Relievers. When sleeplessness is caused by minor pain, simply taking acetaminophen (Tylenol, generic) or a non-steroidal anti-inflammatory drug (NSAID) such as ibuprofen (Advil, Motrin, generic), can be very helpful without causing any daytime sleepiness. The extra "P.M." antihistamine found in combination products is simply an extra, needless chemical in these situations.
Non-benzodiazepines (also called “Z” drugs) are the preferred sedative hypnotic drugs for the treatment of insomnia. In general, non-benzodiazepine hypnotics are recommended for short-term use (7 - 10 days), and treatment should not exceed 4 weeks.
Brands. Non-benzodiazepine hypnotics currently approved in the United States are:
- Zolpidem (Ambien, Ambien CR, generic) is the most commonly prescribed drugs for insomnia. Because it is long-lasting, patients should not take it unless they plan on getting at least 7 - 8 hours of sleep. A lower-dose, sublingual (under-the-tongue) formulation of zolpidem (Intermezzo) is approved for patients who wake up abruptly in the middle of the night and have trouble falling back asleep. Patients take it as needed when they awaken in the night but must be able to get at least 4 hours of sleep after taking.
- Zaleplon (Sonata, generic) is the shortest-acting hypnotic available. Because it is rapidly eliminated from the body it may be best for people who have difficulty falling asleep, not those who wake up often throughout the night. The drug takes effect within 30 minutes and may be taken at bedtime or later as long as the patient can sleep for at least 4 hours.
- Eszopiclone (Lunesta) is related to zopiclone (Imovane), which has been used for many years in Europe. Unlike other sleep medications, eszopiclone was the first sleep medication approved to be taken on a long-term basis.
- Ramelteon (Rozerem) is the newest type of sedative hypnotic. Unlike other prescription sleep drugs, which target GABA receptors, ramelteon works by targeting melatonin receptors. Ramelteon is not habit forming and is the first sleep drug not designated as a controlled substance.
Dosage. In 2013, the FDA made changes to the recommended dosage for zolpidem products:
- All zolpidem products now have lower recommended bedtime dosages.
- Women have lower recommended dosages than men (women metabolize zolpidem more slowly than men and are more susceptible to its effects on next-day mental impairment)
- Use of higher doses increases the risk for next-day impairment of driving. In addition, the FDA warns people to refrain from next-day driving or activities involving mental alertness if they take the extended-release form of zolpidem (Ambien CR, generic).
Side Effects. Non-benzodiazepines tend to have fewer side effects than other sleep medications. However, these drugs can still cause residual morning sedation even if you are feeling fully awake. When patients first start taking any of these drugs, they should use caution during morning activities until they are sure how the drug affects them.
General side effects may include:
- Diarrhea or constipation
All non-benzodiazepine drugs carry labels warning that that these drugs can cause strange sleep-related behavior, including driving, making phone calls, and preparing and eating food while asleep. Most cases of sleepwalking and sleep driving likely occur when patients use the drug along with alcohol or other drugs or take more than the recommended dose. .
Anyone who receives a prescription for these medicines will get a patient medication guide explaining the risks of the drugs and the precautions to take. Talk to your doctor if you have any questions concerning these drugs or their potential side effects.
Patients should carefully read the information labels for all drugs and follow the directions. Some sleeping pills take 30 - 60 minutes to take effect, while others (such as zolpidem) act quickly. For zolpidem, patients should:
- Take zolpidem immediately before going to sleep
- Take zolpidem only when able to get a full night’s sleep (7 - 8 hours)
- Not drink alcohol the same evening
- Not take more than the prescribed dose
- Use caution in the morning when getting out of bed, driving, or operating heavy machinery
Interactions. As with any hypnotics, alcohol increases the sedative effects of these drugs. These hypnotics also interact with other drugs, including rifampin, ketoconazole, erythromycin, and cimetidine. They may also interfere with or be interfered by other drugs. Patients should report all medications to their doctors.
Rebound Insomnia, Dependence, and Tolerance. The risk for rebound insomnia, dependence, and tolerance is lower with non-benzodiazepine hypnotics than with benzodiazepine drugs. These drugs are still subject to abuse. In any case, no hypnotic should be taken for more than 7 - 10 days in a row or at higher than the recommended dose without a doctor's approval.
Benzodiazepines used to be the most commonly prescribed sedative hypnotics. These drugs were originally developed in the 1960s to treat anxiety.
Brands. Commonly prescribed benzodiazepines are:
- Long-acting benzodiazepines include flurazepam (Dalmane, generic), clonazepam (Klonopin, generic), and quazepam (Doral).
- Medium- to short-acting benzodiazepines include triazolam (Halcion), lorazepam (Ativan), alprazolam (Xanax), temazepam (Restoril), oxazepam (Serax), and estazolam (ProSom), which are all available as generics. Short-acting benzodiazepines may be useful for air travelers who want to reduce the effects of jet lag.
Side Effects. Elderly people are more susceptible to side effects and should usually start at half the dose prescribed for younger people. They should not take long-acting forms.
Side effects may differ depending on whether the benzodiazepine is long or shorting acting. They include:
- Respiratory problems may occur with overuse or in people with pre-existing respiratory illness.
- The drugs may increase depression, a common co-condition in many people with insomnia.
- Residual daytime drowsiness is common with benzodiazepines. Long-acting benzodiazepines may increase the risk for automobile accidents and falls in the elderly, particularly in the first week after taking them. Shorter-acting benzodiazepines do not appear to pose as high a risk.
- Memory loss, sleepwalking, sleep driving, eating while asleep, and other odd mood states may occur. These effects are enhanced by alcohol.
- Urinary incontinence may occur, particularly in older patients and when taking long-acting formulations.
- Because these drugs cross the placenta and enter breast milk, pregnant women or nursing mothers should not use them. Benzodiazepine use in the first trimester of pregnancy may be associated with the development of cleft lip in newborns.
- In rare cases, overdoses can be fatal.
Interactions. Benzodiazepines are potentially dangerous when combined with alcohol. Some medications, like the ulcer medication cimetidine, can slow the metabolism of the benzodiazepine.
Withdrawal Symptoms. Withdrawal symptoms usually occur after prolonged use and indicate dependence. They can last 1 - 3 weeks after stopping the drug and may include:
- Gastrointestinal distress
- Disturbed heart rhythm
- Rebound insomnia (the risk is higher with short-acting benzodiazepines than long-acting ones)
- In severe cases, hallucinations or seizures
Antidepressants are sometimes used to treat insomnia that may be caused by depression (secondary insomnia). In addition, certain types of antidepressants with sedating properties are prescribed for the treatment of primary insomnia, generally in lower doses than used to treat depression.
For example, the antidepressant trazodone (Desyrel, generic) is prescribed in low doses as a hypnotic to help induce sleep. A very low dose formulation of the tricyclic antidepressant doxepin (Silenor) is approved for treatment of insomnia. Other antidepressants used for insomnia include the tricyclics trimipramine (Surmontil, generic) and amitriptyline (Elavil, generic) and the tetracyclic antidepressant mirtazapine (Remeron, generic).
Precautions should be taken in the use of trazodone and other sedating antidepressants in elderly patients, due to the risk for side effects (daytime sleepiness, dizziness, priapism, and increased risk of falls) and drug interactions.