History | Types of Medications Used in the Treatment of Insomnia | Frequently Asked Questions
Medications for Insomnia
There are many treatments for insomnia. Medication is among the most commonly used treatments, and is an important consideration for people who suffer from difficulty falling asleep, difficulty staying asleep, or poor quality ("non-restorative") sleep.
It is likely that humans have attempted to control states of sleep and wakefulness since the beginning of time. There are early reports of the use of herbal potions, alcohol, and laudanum to induce sleep. However, the first reports regarding a medication used to promote sleep were in the mid 19th century and related to the drug known as bromide. Bromide was initially developed for the treatment of epilepsy, but was soon found to be effective as a tranquilizer and sedative. This medication was prone to producing toxicity and serous adverse effects and was removed from the marketplace several years ago.
Following the introduction of bromide, other sedative-hypnotics were developed. These included drugs such as chloral hydrate, paraldehyde, urethane, and sulfonal. However, in the early 1900s a new class of drug was developed that represented an important advancement in sleep therapy. The drugs in this class are known as barbiturates (such as amobarbital, pentobarbital, secobarbital, and phenobarbital). They were known to be quite effective in promoting sleep and were used quite commonly until the 1960s when safety concerns and newer therapeutics resulted in a decline in prescriptions. Barbiturates were found to have a wide variety of effects on the body, were associated with multiple adverse effects, and were extremely dangerous, or lethal, when taken in overdose.
In the 1960s, the benzodiazepines were introduced for the treatment of insomnia. These medications were shown to be effective and safe medications. Most notably, they were much less likely to produce adverse effects, and much less likely to be fatal when taken in overdose than the barbiturates. Benzodiazepines are still in use today for the treatment of insomnia, anxiety, and seizures. They are less often prescribed now than in the past, however, because of concerns regarding abuse and dependence, impairment in memory and movement, and next day "hangover," or residual effects.
In the 1990s a newer class of medications, known as "non-benzodiazepine, benzodiazepine receptor agonists" were introduced for the treatment of insomnia. The drugs in this class are as effective as the benzodiazepines in promoting sleep. However, they are believed to be associated with a very low risk of abuse or dependence and fewer adverse effects than the benzodiazepines. Most users of these medications are satisfied with the outcome of therapy, and do not suffer from any unwanted or adverse effects.
Newer prescription medications for insomnia are currently in development. If we have learned the lessons of history, it is likely that manufacturers will identify medications that match or exceed the effectiveness of the existing drugs on the market, and are associated with better safety profiles.
Types of Medications Used in the Treatment of Insomnia
Sedative-Hypnotic Medications ("Sleep Medications") are medicines that have been shown to reduce the length of time it takes to fall asleep and/or increase sleep duration. These medicines are usually taken at bedtime to relieve the symptoms of insomnia, although some newer medications may be appropriate for use on an "as needed" basis, whenever symptoms occur. The sedative-hypnotic medicines that have been approved by the United States Food and Drug Agency (FDA) have undergone rigorous testing in clinical trials, and have been shown to be safe and effective.
There are different classes of sedative-hypnotic medications. However, most of these medicines fall into a class of drugs known as benzodiazepines, or into a newer class of drugs known as "non-benzodiazepine, benzodiazepine receptor agonists."
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The benzodiazepines approved for the treatment of insomnia include:
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The benzodiazepines were formerly the most commonly used treatment for insomnia. However, concerns regarding patterns of inappropriate use (abuse), dependence, adverse effects such as impairments in memory or movement, and next-day "hangover" led to caution in prescribing these medications. While many people continue to use these medications without problems, the benzodiazepines are no longer the "first line" treatment for insomnia.
Within recent years, physicians have been much more likely to prescribe treatment with newer drugs in the "non-benzodiazepine, benzodiazepine receptor agonist" class that seem to have better safety profiles.
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The "non-benzodiazepine, benzodiazepine receptor agonists" include:
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Zolpidem and zaleplon are known to reduce the time it takes to fall asleep, and in this regard their effects are probably quite similar. Zolpidem has effects that persist later into the night, and may help the sufferer stay asleep longer. The different characteristics of these medications mean that they may be used in different ways. Zolpidem must be taken at bedtime, and may be used when the sleeper has difficulty falling asleep and/or staying asleep. Zaleplon may be taken at bedtime or later (e.g., after getting into bed and having difficulty falling asleep or after a nighttime awakening), as long as there are four hours or more of time left to sleep.
The usual starting doses of zolpidem and zaleplon are 5 mg (elderly) and 10 mg (adult). Many elderly patients may use higher doses (e.g., 10 mg).
Over-the-Counter (OTC) Medications for the treatment of insomnia are those that can be purchased from a pharmacy without a prescription. These include medications such as Nytol, Sleep-Eze, Sominex, and others. Most of these products contain antihistamines, such as diphenhydramine (Benadryl), that act as sedatives.
The effects of antihistamines on sleep have been reported. Doses of 25 mg and 50 mg have been shown to promote sleep. However, people with insomnia who use these medications may not experience relief from their symptoms, and may experience adverse effects associated with their use. Some antihistamines produce effects such as dry mouth, dry eyes, urinary retention, confusion, and even delirium. Some users complain of vivid dreams and next day hangover effects when using an OTC product for sleep.
Sedating Antidepressants are prescription medications that have been developed for the treatment of depression, but that are known to have sedative side effects. These medications have been used for many years to promote sleep. The sedating antidepressant medications most commonly used include trazodone (Desyrel), amitriptyline (Elavil), and doxepin (Sinequan).
The value of the use of sedating antidepressants for the treatment of insomnia has been debated for some time. There is evidence that these medications are valuable in the treatment of insomnia when it occurs in the context of depression. However, there is conflicting evidence regarding the use of these medications in primary insomnia.
One concern regarding the use of sedating antidepressants is that these medications are associated with more troubling, adverse effects than prescription sedative-hypnotic medications. Therefore, many argue that the first line therapy for insomnia remains with the sedative-hypnotics.
"Natural," Herbal, and Other Home Remedies have been used for years. One of the most recent "natural" remedies for insomnia has been melatonin, which can be obtained at most health food stores. Melatonin is a hormone that is known to be involved in the regulation of sleep and wakefulness. It has been shown that the ingestion of melatonin prior to bedtime will help individuals fall asleep. However, scientific data have failed to confirm that melatonin is useful in maintaining sleep.
Herbal products such as valerian, chamomile, kava kava, and others have been promoted as natural remedies for insomnia. However, the effectiveness and safety of these products has not been documented.
It is important to note that products sold in health food stores have not been exposed to the rigorous testing that is required of all prescription products. Therefore, many of the claims that are made regarding these substances have not been adequately tested in a laboratory environment. The content of these products is also not regulated with the same scrutiny as prescription products, so consumers may not be certain of what they are getting. Finally, the safety profiles of these products are often not known. Several years ago many people used the substance tryptophan, an amino acid, to promote sleep. Dozens of users were then affected by a serious disorder called eosinophilia myalgia syndrome (EMS) due to a contaminant that entered the product during its manufacturing. Tryptophan has since been removed from the market in the United States.
Are sleep medications dangerous or addictive?
Modern
day sleep medications are not dangerous when used as prescribed.
The addictive potential of the newest classes of medication is believed
to be low.
When can sleep medications be used?
Sleep medications can be used on a periodic basis, when needed to combat insomnia. Many people experience insomnia only a few times per year or per month. It is appropriate to use the medication in this way, provided that your doctor has recommended it.
Sleep medications also may be used on a nightly basis. Current prescription guidelines indicate that sleep medications should be used on a continuous basis for a limited period of time (a few weeks). However, data show that some people use the medication for longer periods. These people may have chronic problems with insomnia that require chronic treatments.
Most sleep medications need to be taken just before bedtime or at bedtime. This is due to the persistence of their effects over the course of the night. Some sleep medications may be able to be taken after bedtime, in response to symptoms or awakenings. Those who use sleep medications should speak with their doctors regarding appropriate use.
Are sleep medications better than non-drug therapies for insomnia?
No single therapy is better than any other. Since insomnia often arises from a variety of causes, and different people have different desires and attitudes regarding medication, it is hard to say that "one size fits all" with regard to insomnia treatment. It is most important that patients talk to their doctors about their problems, what they hope for with treatment, and assess progress along the way.
How long can I use the pills?
Some people will use a sleeping pill for one night. Others may need long-term use of the medication on a nightly basis. If you use sleep medications over the long-term, it is important to maintain regular contact with your physician to determine the need for continued use and explore all of the options open to you. For example, in some cases a persistent problem with insomnia is a sign that other, underlying sleep problems exist. These need to be diagnosed and treated in order to find real relief.
Will I be able to stop taking pills after I start?
Yes. Newer sleep medications can be discontinued in a matter of a day or two, usually without withdrawal effects. Benzodiazepines may require a longer period of "tapering" before they actually can be discontinued. However, if managed properly, the discontinuation can be tolerated comfortably.
Always speak to your physician prior to discontinuing prescribed medication.