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SLEEP MEDICATIONS

In the past, the most commonly prescribed medications for sleeping problems included two classes of sedative-hypnotic drugs: the benzodiazepines and the “non-benzodiazepine, benzodiazepine receptor agonists”. In addition to these categories, a new medication (Ramelteon, under the brand name Rozerem) became more widely available in 2006 that aids sleep with a unique mechanism of action.

BENZODIAZEPHINE SLEEP AIDS
Although all of the benzodiazepines are used for the treatment of insomnia, the first 5 in the list are used most commonly for sleep disorders.

  • Dalmane (Flurazepam)
  • Doral (Quazepam)
  • Halcion (Triazolam)
  • ProSom (Estazolam)
  • Restoril (Temazepam)
  • Klonopin (Clonazepam)
  • Ativan (Lorazepam)
  • Xanax (Alprazolam)

The benzodiazepines have been the most commonly used medications in the treatment of insomnia and are certainly safer than some of the older sleeping medications such as the barbiturates (Amytal, Nembutoal, Seconal). However, there have been concerns regarding inappropriate use and abuse of these medications. These medications are generally recommended only to be used on a short term basis since physical tolerance and dependence can develop. In addition, these medications can often produce a “hangover” effect the following day. These medications should not be used with opioid pain medications whenever possible.  If both types of medications are used concurrently, please speak to your treating physician to determine if better alternatives are available and understand the risks associated with both medications.

NON-BENZODIAZEPHINE MEDICATIONS
In recent years, a newer class of medications has been developed often termed the “non-benzodiazepine, benzodiazepine receptor agonists”. These newer medications appear to have better safety profiles and less adverse effects. These medications are associated with a lower risk of abuse and dependence than the benzodiazepines. Examples of medications in this class include:

  • Ambien (Zolpidem)
  • Sonata (Zaleplon)
  • Lunesta (Eszopiclone, formerly known as Estorra)
  • Belsomra

These medications are known to reduce the time it takes to fall asleep and, thus, their effects are quite similar to those in the benzodiazepine class. These medicines appear to have different characteristics and may be used in different ways. Again, although these medications are safer than the benzodiazepines, it is not recommended that they be used on a long term basis (except Lunesta which will be discussed subsequently).

Ambien. This sleeping pill has effects that persist later into the night and may help the individual stay asleep longer. Thus, it must be taken at bedtime and may be used when the individual has trouble falling asleep and/or staying asleep.

Sonata. This sleep aid is generally used for those individuals having trouble falling asleep. Therefore, it is often taken at bedtime or later such as when awakening during the night as long as there are at least four or more hours left to sleep.

Lunesta. This sleep aid was approved by the FDA in December of 2004 as a new, longer lasting sleeping pill. Clinical trials have demonstrated that Lunesta helps people get to sleep faster, similar to Ambien and Sonata. However, it appears that it also helps the individual stay asleep through the night. The FDA has approved Lunesta for patients who have difficulty falling asleep as well as those who are unable to sleep through the night. Lunesta has about a six hour half life, so it is more likely to maintain sleep. Due to its long half life, Lunesta must be taken immediately before bedtime and the individual should make sure that he or she has a full eight hours devoted to sleeping before taking it. As with the other medications, side effects can occur, including daytime drowsiness, dry mouth, and dizziness. Unlike the other medications in this class which are recommended only for use on a temporary basis, Lunesta is approved for longer term use.

Advantages:

  • A relatively short half life so one does not wake up with a “hangover” the following day.
  • Having little effect on sleep staging, allowing the individual to obtain approximately the same amount of time in each stage of sleep as one would without the medications.
  • Less likely to cause addiction, withdrawal, or tolerance relative to older sleeping medications.

However, it should be kept in mind that these medications will not address any underlying medical problems causing the insomnia, such as sleep-related breathing disorders (sleep apnea), restless legs syndrome, and of course, chronic pain. Therefore, they should only be used in conjunction with other treatments that are focusing on the primary medical problem.

Melatonin receptor agonists for falling sleep 

Rozerem (ramelteon) is a prescription insomnia medication that was approved by the FDA in July 2005 and began to be marketed to consumers in 2006. Rozerem has a unique mechanism of action-melatonin receptor agonist-that selectively targets specific receptors in the brain that are responsible for controlling the body’s sleep-wake cycle. It works by mimicking melatonin, a naturally occurring hormone that is produced during the sleep period.

Rozerem may have an advantage over the other benzodiazepine and non-benzodiazepine classes for the following reasons:

  • It specifically targets brain structures responsible for the sleep-wake cycle.
  • It is the first and only prescription sleep medication that has shown no evidence of abuse, dependence or withdrawal (as such it has not been designated as a controlled substance by the U.S. DEA).
  • Rozerem is approved by the FDA to be prescribed for long-term use in adults.
  • Rozerem has been shown to be safe in older adults, as well as those with mild-to-moderate chronic obstructive pulmonary disease (COPD) and mild-to-moderate sleep apnea.

Some of the primary warnings, side-effects, and contraindications for the use of Rozerem include the following (there are many others but these are the most significant):

  • It is not recommend for use in patient with severe COPD or sleep apnea.
  • It should not be used in patients with severe hepatic impairment or sensitivity to the medication.
  • It is not recommended to used in conjunction with alcohol consumption.
  • More common side-effects include daytime sleepiness, dizziness and fatigue.
  • In primarily depressed patients, the medication may cause worsening of depression or suicidal ideation (this issue has not been directly studied with Rozerem but is seen with other sleeping medications).

Some of the issues that should be taken into account when using Rozerem for insomnia associated with chronic pain include the following:

  • As with the other sleeping medications (aside from the antidepressants), the use of Rozerem has not been directly studied in a chronic pain patient population.
  • Rozerem has no analgesic (pain relieving) properties as has been shown with some of the antidepressants medications when used for sleep.
  • Most chronic pain patients have difficulty initiating and maintaining sleep. While Rozerem has been shown to improve sleep-onset, its effects on sleep-maintenance are unknown.

As with the other sleeping medications, Rozerem will not address any underlying medical problems causing the insomnia. It should be used in conjunction with other treatments that are focused on the primary medical problem (e. g. chronic pain).

ANTIDEPRESSANTS AS SLEEP AIDS
Depression is a common occurrence in a chronic pain condition, and insomnia is quite common in depression. If the individual with chronic pain is also experiencing clinical depression, treating the depression with psychological treatment and an appropriate antidepressants (antidepressant medication), if indicated, may also help with the sleep disruption as well as other symptoms of depression.

Even in chronic back pain patients who are not experiencing significant or clinical depression, sedating antidepressants are often used in low doses to help with insomnia as well as providing some analgesic (pain relieving) benefit. The sedating antidepressants most commonly used to help with sleep include Trazodone(Desyrel), Amitriptyline (Elavil), and Doxepin (Sinequan). It should be noted that when these medications are used for sleeping and pain relieving properties, it is in much lower doses than when used in the treatment of depression. Benefits of these antidepressants include:

  • They are non-addictive.
  • Added benefit of providing some analgesic benefit as compared to the hypnotic class of medications discussed previously (which have no pain relieving properties).
  • Do not produce physical dependence or tolerance.
  • Generally have a low incidence of side effects, especially when used in low doses.

Some individuals do experience adverse side effects, including such things as dry mouth, blurred vision, a “hangover” in the morning, constipation, urinary retention, and nausea.

Contact Us

13710 Olive Boulevard (Primary Office)
Chesterfield, MO 63017
Telephone: 314-469-PAIN (7246)

Fax: 314-469-7251
Exchange: 314-441-6965 (for after-hour Emergencies Only)

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