The Secret of Great Health Care

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Medications for Insomnia

Medications

When all of the above interventions have failed medications can be considered

 

 

 

There are many medications used to treat insomnia. They range from over the counter to controlled substances.

Sometimes treatment of insomnia starts with medications, but it should not. Medications are not without risk and starting with many of the lifestyle interventions is a better first line option than drugs.

Medications are an easy fix for Americans. It is much easier to pop a pill than take the time and effort to implement lifestyle changes. Twenty-four million prescriptions are written for sleeping pills each year (1).

Advertising executives do not help. Lunesta and Ambien CR spend almost 500 million dollars on direct to consumer advertising a year (1).






Drugs are often taken much longer than they are supposed to be. Most drugs are indicated for short-term use, but many people take them for years on end. This misuse of sleeping aids can lead to many problems including dependency, memory problems sleepwalking, hallucinations and daytime drowsiness.

In addition to approved sleeping pills, there are many drugs indicated for other purposes, used for insomnia. This includes anti-anxiety drugs such as alprazolam (Xanax), antidepressants such as trazodone and pain medications such as Vicodin or Darvocet.

The most common over the counter medication is some form of antihistamine. They often contain diphenhydramine (Benadryl) or doxylamine succinate. Many people do not realize that they are taking an antihistamine to sleep. They assume it is a specific sleeping pill. Popular over the counter products includes Tylenol PM, Sominex, Simply Sleep and Unisom.

Antihistamines are used to treat allergies, they are not sleep aids. They do have the side effect of drowsiness and therefore can help promote sleep. They are also associated with other side effects such as dry mouth, constipation, confusion and difficulty urinating. Side effects are more common in the older population. One problematic side effect in the older population is confusion. These drugs can lead to significant confusion in the hospitalized older adult.

According to Consumer Reports (1) over the counter drugs and supplements help over 50% of the people that took them. This survey found sound machines to be more effective than over the counter sleeping pills.





Over the counter medications are popular because they are cheap and convenient. The problem is that there are many problems with these medications.

They have not been proven effective in inducing sleep on a consistent basis. For healthy people they are quite effective and safe to use for one to two nights. If used for longer than a couple nights tolerance may develop. Tolerance is when the body gets used to the drug and it is no longer effective.

These drugs are not encouraged for long-term use because they are not proven effective in the long-term, reduce the quality of sleep and are associated with many side effects.

Sedating anti-depressants

The effectiveness of the sedating anti-depressants has not been shown to be effective in patients who are not depressed. They are not approved for use in sleep, but are often prescribed. Sometimes they are prescribed as agents solely for sleep, but more often they are prescribed to the depressed individual who need help sleeping. Common drugs in this class are included on the table below.

 

 

 

 

Medication

Side effects

Trazodone

Dry mouth, constipation, daytime sleepiness

Doxepine

Dry mouth, drowsiness, constipation, GI upset, photosensitivity

Amitriptyline

Dry mouth, constipation, daytime sleepiness

Mirtazapine

Drowsiness, weight gain, sore throat, neutropenia

Hypnotics

Hypnotics are agents meant to induce sleep. Most of these should not be used if there is a history of drug abuse, untreated sleep apnea, alcohol abuse or pregnancy – particularly the benzodiazepine class. Those who have used these drugs for an extended period of time need to be tapered off slowly and not abruptly discontinued.

Hypnotics include:

  • Benzodiazepines
  • Nonbenzodiazepines
  • Melatonin receptor agonists

The first two classes work on a receptor in the brain called the gamma-aminobutyric acid (GABA) receptor. The benzodiazepines are the older class of drugs and generally have a longer half-life. This means that the drug stays in the system much longer. Sedation often carries over to the next day. The most commonly used benzodiazepine for sleep problems is Temazepam (Restoril). Its half-life is about 9-12 hours.

Benzodiazepines are often used in the treatment of anxiety. Drugs such as alprazolam (Xanax) and lorazepam (Ativan), are indicted for anxiety, but due to their sedating properties are often used for sleep. When used in this way it is an off label use.

Other medications in the benzodiazepines class are older drugs and are not used as often today. They include: flurazepam (Dalmane) and Triazolam (Halcion).

Dependency is a major risk with this class; this is especially problematic in those who use them for more than a few weeks. Withdrawal from these medications can be bad and lead to anxiety, nausea, rebound insomnia, depression, nightmares and memory problems. Gradual reduction in dose is needed when these drugs are used.

The nonbenzodiazepines were more recent additions to the insomnia armamentarium. These medications work differently and do not affect the sleep stages and do not cause REM sleep rebound. This class is associated with fewer side effects than the benzodiazepines.

There are three drugs in this class: Zolpidem (Ambien), Zaleplon (Sonata) and Eszopiclone (Lunesta).

Eszopiclone (Lunesta) works though unknown mechanisms but is thought to interact with the GABA receptor. Its half-life is about 6 hours. It is most effective in higher doses for sleep maintenance and lower doses are more effective in sleep initiation.

Zolpidem (Ambien) is most helpful in the initiation of sleep. Half-life is about 2.5 hours. The extended release product (Ambien CR) helps with sleep initiation and/or maintaining sleep.

Zaleplon (Sonata) is useful in helping those fall asleep with a half-life of about .5 to 1 hour.

Benzodiazepines and nonbenzodiazepines should be used with extreme caution in older adults and those with lung disease. It can lead to confusion, restlessness or excitement. Some sleeping agents (Ambien) are associated with bizarre nighttime behavior such as sleep walking or doing things at night in which there is no memory of in the morning.

Many of the drugs need to be tapered as some can lead to rebound insomnia and in some severe cases, seizures, tremor or anxiety.

Melatonin receptor agonists

There is one drug in this class – Ramelteon (Rozerem). It speeds up the time it takes to fall asleep and increases the length of time one sleeps. The melatonin receptor agonist is a unique drug that is not associated with abuse. It is taken within 30 minutes of bedtime and is contraindicated in those with severe hepatic impairment. It is not recommended in those with severe chronic obstructive pulmonary disease or sleep apnea. Side effects include daytime sleepiness, fatigue, nausea, headache and dizziness.

 

 

 

 

Drug

Note

Temazepam (Restoril)

Benzodiazepine – Half-life 9-12 hours. Less effective for sleep onset, may lead to daytime sleepiness.

Eszopiclone (Lunesta)

Longest half-life of the nonbenzodiazepine class and is useful for sleep onset and the maintainable of sleep. Higher doses are more effective for sleep onset and maintenance, lower doses are effective for sleep onset.

Zolpidem ER (Ambien CR)

Used for sleep onset and sleep maintenance insomnia. There is no tolerance when used 3-7 nights a week for 6 months.

Zolpidem

Used for sleep onset insomnia NOT sleep maintenance, can lead to rebound insomnia. Side effects are more problematic when doses are greater than 20 mg a day.

Zaleplon (Sonata)

Very short half-life. Useful for sleep onset insomnia or when waking up in the middle of the night as long as there is four or more hours of sleep remaining. Least commonly associated with daytime drowsiness.

Ramelteon (Rozerem)

Melatonin receptor agonist. No abuse risk. Likely safe to use long-term.

Adding medications together has not been shown to be effective. The combination of CBT and benzodiazepines is better than the drug alone.

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