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Insomnia: More Chemical Causes

By Ronald D. Whitmont, M.D. Created: July 20, 2011 Last Updated: July 20, 2011
Related articles: Health » Western Medicine
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AMBIEN: This sleeping pill requires increasing doses to maintain the same effect and is difficult to discontinue. (Tim Boyle/Getty Images)

AMBIEN: This sleeping pill requires increasing doses to maintain the same effect and is difficult to discontinue. (Tim Boyle/Getty Images)

The use of medications, herbs, and supplements to promote sleep frequently backfires and leads to greater disruptions. Some of the common sleep medications include benzodiazepines, zolpidem (Ambien), eszopiclone (Lunesta), ramelteon (Rozerem), and antihistamines like diphenhydramine (Benadryl).

Benzodiazepines. These attach to specific gamma-aminobutyric acid (GABA) receptors, and induce non-REM sleep. They block the transition to deeper levels of stage 4 REM sleep.

Even when these agents are helpful in inducing sleep, they prevent the progression to the deepest levels of regenerative sleep. They pose very serious risks of physical and psychological addiction and dependence.

Zolpidem (Ambien). This is a short-acting hypnotic that potentiates GABA, an inhibitory neurotransmitter, by binding to GABA receptors at the same location as benzodiazepines.

Zolpidem helps initiate sleep but does not maintain it. It can be particularly difficult to discontinue this medicine since it typically requires increasing dosages to combat worsening insomnia and leads to rebound insomnia when discontinued.

Frequent side effects include memory loss, amnesia, asthenia, ataxia, confusion, euphoria, headache, insomnia, vertigo, dyspepsia, hiccup, nausea, arthralgia, myalgia, upper respiratory infection, double vision, and urinary tract infections.

Eszopiclone (Lunesta). This drug tends to worsen sleep problems once it is discontinued. Frequent side effects include chest pain, migraine, peripheral edema, and depression. So far, the only clinical trials of eszopiclone published were funded by the drug’s manufacturer.

Ramelteon (Rozerem). The drug binds to melatonin receptors and as a result, it interferes with other hormonal systems. Ramelteon increases prolactin levels and has been associated with an increased incidence of cancer in laboratory animals.

Side effects include nausea, diarrhea, myalgia, and arthralgia, exacerbated insomnia, headache, fatigue, depression, hallucinations, and upper respiratory tract infections.

Antihistamines. Typically associated with prolonged morning drowsiness, antihistamines like diphenhydramine (Benadryl) often require the use of stimulants like caffeine to counteract them. Users run the risk of ping-pong cycles, utilizing daytime stimulants to stay wake and nighttime sedatives to fall back to sleep. This behavior has been associated with increased risk of adverse cardiovascular events.

Many sleep agents contribute to psychological as well as physical dependence. Discontinuation can be extremely difficult since withdrawal symptoms typically lead to rebound insomnia that is worse than the original condition.

Drugs and herbs used to promote sleep should never be considered first-line approaches for acute insomnia unless circumstances warrant no other options. These chemicals should be reserved for use only when hygienic and behavioral methods have failed.

Environmental Contamination. The overflow of many pharmaceutical products into the environment and the water supply poses another concern. Many medications pass through the body intact before they are secreted in feces or urine. As more of the population uses medications, these chemical residues have built up in the water table.

Exposure to these drugs is more common today than ever before via contaminated food and water. As a result of this contamination, a cornucopia of pharmaceutical and chemical wastes are consumed regularly, unknowingly, unwittingly, and in increasing amounts by more of the population than ever before.

The effects of this long-term pollution have not been extensively studied and are only vaguely understood. Unnecessary use of pharmaceuticals to promote sleep or to treat other conditions must be curtailed both individually and globally since this reckless practice endangers everyone.

This is the fifth of a 10-part series.

Dr. Whitmont is a classical homeopathic physician and internist who practices in New York. He is a clinical assistant professor of family and community medicine at New York Medical College. His website is HomeopathicMD.com

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