Sleep Medications
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Medicines and Their Commonly Used Names

There are several types of prescription and nonprescription medicines that can be used to treat insomnia.

Prescription Drugs
Benzodiazepine-receptor agonists —These medicines attach to special sites in the brain, causing relaxation. This class includes drugs in the benzodiazepine family and newer non-benzodiazepine drugs with similar effects. These drugs can be short-, intermediate-, or long-acting.

MedicationBrand namesBenzodiazepinesAlprazolamXanaxChlordiazepoxideLibriumClonazepamKlonopinClorazepateTranxene, GenXeneDiazepamValiumEstazolamTasedanFlurazepamDalmaneLorazepamAtivanOxazepamSeraxTemazepamRestorilTriazolamHalcionNon-benzodiazepineZaleplonSonataZolpidemAmbienEszopicloneLunesta
Melatonin-receptor agonist (e.g., ramelteon [Rozerem])—This medicine is used to treat insomnia characterized by difficulty with falling asleep. It shortens the time it takes to fall asleep in people with transient insomnia.

Antidepressants —For long-term treatment of insomnia or when insomnia is accompanied by depression and/or caused by depression, antidepressants may be prescribed.

Nonprescription Drugs
Nonprescription sleeping aids can leave people feeling drowsy the next day and may not always be effective at providing restful sleep. However, they are often used as the first line of treatment for short-term insomnia because they are not addictive and a fatal overdose is extremely rare. These include the following:

Antihistamines —There are many antihistamines available over-the-counter. Diphenhydramine is a commonly used antihistamine for insomnia. Not all antihistamines are effective for this purpose, especially the newer, nondrowsy antihistamines.

Melatonin —This is a hormone produced by the brain. Melatonin may be helpful for jet lag.

Pain relievers —These drugs are useful when insomnia is caused by minor pain.

The information below relates to hypnotics (sleep medicines), unless stated otherwise.

What These Medicines Are Prescribed For
To promote sleep in someone who has insomnia, especially in these cases:

  • Sleep difficulties cause problems in accomplishing daily activities
  • Behavioral approaches have proven ineffective
  • Insomnia associated with:
    • Psychological condition (eg, anxiety )
    • Temporary changes in circadian rhythms (internal clock), such as those due to jet lag or shift work
Hypnotics can help to do the following:

  • Shorten the time it takes to fall asleep
  • Increase total sleep time
  • Decrease the number of wakings during sleep
How These Medicines Work
Benzodiazepine-receptor agonists work by enhancing the effect of a brain chemical responsible for reducing neuron excitability. Antidepressants may cause immediate drowsiness as well as alter brain chemistry in such a way as to improve sleep. Some antihistamines cause immediate drowsiness.

Precautions While Using These Medicines
Avoid overuse and dependence —Benzodiazepines and other sleep medicines may become less effective over time, requiring higher doses to produce effects. This can lead to dependence. Antidepressants and antihistamines present a lower risk for dependency.

Do not stop suddenly —When you are discontinuing regular use of a prescription sleep aid, your doctor may gradually lower your dose. Stopping abruptly can cause withdrawal.

Mild withdrawal of benzodiazepines is common. The usual symptom is several nights of poor sleep. More serious withdrawal may occur with higher doses of benzodiazepines and may include the following symptoms:

  • Anxiety
  • Irritability
  • Depression
  • Insomnia
  • Sweating
  • Vomiting
  • Diarrhea
  • Blurred vision
  • Impaired memory and concentration
  • Tremor
  • Muscle and abdominal cramps
  • Decreased appetite
  • Hallucinations or seizures (in severe cases)
Do not combine with certain substances —Be sure to tell your doctor about all of the medicines, both prescription and nonprescription and any herbal supplements you take. Hypnotics can have potentially dangerous interactions when combined with certain other substances, such as the following:

  • Alcohol
  • Anesthetics, including dental anesthetics
  • Anticonvulsants (barbiturates, other benzodiazepines, hydantoins, succinimide, and others)
  • Antidepressants (MAO inhibitors, tricyclics, fluoxetine [Prozac], fluvoxamine [Luvox], paroxetine [Paxil], sertraline [Zoloft], trazodone, venlafaxine [Effexor], Nefazodone [Serzone])
  • Lithium
  • Narcotic analgesics for pain relief for surgery and obstetrics
  • Sedatives
  • Antipsychotic tranquilizing agents (phenothiazine, clozapine, haloperidol, loxapine, molindone, pimozide, risperidone, thioxanthenes)
  • Cimetidine (Tagamet)
  • Fluconazole (Diflucan)
  • Itraconazole (Sporanox)
  • Ketoconazole (Nizoral)
Practice good sleep habits —Due to the risks of overuse and withdrawal, sleep medicines should not be considered a long-term or first solution to insomnia. While using these medicines, it is essential to adopt good sleep habits in order to establish normal sleeping patterns that can be maintained without the use of drugs. These habits include the following:

  • Exercising regularly, at least six hours before you want to sleep
  • Avoiding naps
  • Going to sleep and waking up at the same time every day
  • Saving your worries for daytime (Schedule time during the day to write down concerns.)
  • Practicing a relaxing bedtime ritual, like a hot bath or listening to calming music
  • Using your bed only for sleeping and sex
Proper Usage
Your doctor will determine the appropriate dose and usage schedule for you.

Possible Side Effects
Elderly people are more susceptible to side effects and therefore hypnotics are not recommended for them.

Possible side effects of hypnotics include the following:

  • Clumsiness or unsteadiness
  • Dizziness or lightheadedness
  • Drowsiness (more common with long-acting than short-acting drugs)
  • Weakness
  • Slurred speech
  • Agitation
  • Headache
  • Depression
  • Memory loss
Rare side effects include the following:

  • Sleepwalking
  • Odd moods and behavior
  • Hallucinations
  • Lack of usual inhibitions
  • Confusion
Possible side effects of antihistamines include the following:

  • Dizziness or lightheadedness
  • Drunken movements
  • Blurred vision
  • Dry mouth and throat
  • Urinary retention
  • Constipation
With every medicine, there are important precautions to consider. These include allergies, interactions with other drugs and medical conditions, and safety during pregnancy, lactation, and other stages of life.




RESOURCES:
National Center on Sleep Disorders Research

National Sleep Foundation

CANADIAN RESOURCES
Better Sleep Council Canada

The Canadian Sleep Society

References:
Benzodiazepine withdrawal. EBSCO DynaMed website. Available at: http://www.ebscohost.com/dynamed/what.php. Updated February 1, 2012. Accessed December 28, 2012.

Benzodiazepine withdrawal syndrome. Benzodiazepines Cooperation Not Confrontation website. Available at: http://www.bcnc.org.uk/symptoms.html. Accessed December 28, 2012.

Healthy Sleep Tips. National Sleep Foundation website. Available at: http://www.sleepfoundation.org/article/sleep-topics/healthy-sleep-tips. Accessed December 28, 2012.

Insomnia. EBSCO DynaMed website. Available at: http://www.ebscohost.com/dynamed/what.php. Updated December 25, 2012. Accessed December 28, 2012.

Proctor A, Bianchi MT. Clinical Pharmacology in Sleep Medicine. ISRN Pharmacol . 2012 epub ahead of print.

Ramelteon. EBSCO DynaMed website. Available at: http://www.ebscohost.com/dynamed/what.php. Updated December 14, 2011. Accessed JDecember 28, 2012.

Sack RL, Auckley D, Auger RR, et al. Circadian rhythm sleep disorders: Part I, basic principles, shift work and jet lag disorders. Sleep. 2007;30:1460-1483.

Sleep Aids and Insomnia. National Sleep Foundation website. Available at: http://www.sleepfoundation.org/article/sleep-related-problems/sleep-aids-and-insomnia. Accessed December 28, 2012.

Last Reviewed December 2012



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