More than 30 million adults in the U.S. rely on Xanax®, Valium®, Ativan®, or other prescription benzodiazepine drugs to cope with sleep disorders.^1-3

These drugs come with side effects, and long-term use can lead to addiction.

Benzodiazepines cause another issue. Their use is associated with reduced melatonin levels.^4-6

In one study, a single dose of a benzodiazepine derivative (which is metabolized into active benzodiazepines) before bedtime significantly suppressed the production of melatonin.⁴

Melatonin helps regulate our sleep cycles. This means that benzodiazepines interfere with the body’s natural ability to initiate healthy sleep.

Clinical trials show that melatonin intake can improve sleep quality in many people and appears to help reduce dependence on benzodiazepine drugs.

Dangers of Benzodiazepines

More than 50 million U.S. adults suffer from a sleep disorder like insomnia or sleep apnea.^7,8

Poor sleep has been linked with health problems, including type II diabetes, obesity, and injuries. In the elderly, sleep problems are associated with increased risk of falls, frailty, and death. ^9-14

Many people turn to benzodiazepine drugs for help. ¹⁵ These drugs enhance sleep onset, reduce the number of times waking at night, and improve total sleep time and sleep quality with short-term use.¹⁶ Too often, these drugs are taken longer than needed, increasing their addictive potential.

Well-known downsides to regular benzodiazepine use:^17-19

• They are heavily sedating, impairing the ability to think clearly and increasing risk for accidents.
• They can lead to tolerance, which means users need to take higher and higher doses to get the same effect.
• They can lead to dependence or addiction.
• They come with common side effects including dizziness, weakness, depression, and confusion.

What’s less well-known is that benzodiazepines interfere with how the brain naturally promotes healthy sleep.

Benzodiazepines Deplete Melatonin

Melatonin is a hormone secreted by the brain’s pineal gland. Often called the "sleep hormone," it is central to regulating the body’s natural sleep-wake cycle.²⁰

Benzodiazepines interfere with the body’s natural melatonin production.⁴

As early as 1986, scientists found that even a single dose of a benzodiazepine derivative (which is metabolized into active benzodiazepines) before bedtime significantlysuppresses the production of melatonin. ⁴ When scientists administered a drug that blocked the action of benzodiazepines, melatonin was restored to normal levels.

Larger studies have confirmed this finding. For example, after a single nighttime dose of alprazolam (Xanax®), peak levels of melatonin in the bloodstream are roughly half what they would be normally.^5,6

By trying to improve sleep quality with benzodiazepines, people are impeding their body’s natural ability to regulate sleep.

How Oral Melatonin Improves Sleep

A meta-analysis of 19 studies found that melatonin improves sleep in multiple ways, including:²¹

• Reducing the time it takes to fall asleep,
• Improving sleep quality, and
• Extending the duration of sleep.

Melatonin promotes relaxation and sleep, without side effects or the risk of dependence associated with benzodiazepines.

For example, an observational study of patients undergoing kidney dialysis—which is often associated with sleep disturbances—found that taking 3 mg of melatonin before bedtime was more effective than Xanax® in improving sleep quality as shown in multiple subjective sleep assessment scales.²²

Regrettably, not all sleep-deprived sufferers find complete relief using melatonin alone.

Reduce Dependence on Drugs

Melatonin is safer than benzodiazepines and has side benefits that include potential to reduce risks of certain cancers.²³

It is not addictive or sedating, and melatonin supports the brain’s natural ability to promote sleep instead of interfering with it.

In elderly insomniacs who use benzodiazepines to be able to sleep, adding melatonin significantly improved sleep quality and time.²⁴ In a follow-up study, scientists evaluated whether taking melatonin could help people stop using benzodiazepines.²⁵

They randomized elderly insomniacs on benzo-diazepines to receive either 2 mg of controlled-release melatonin before bed or a placebo. During the six weeks of the study, participants were encouraged to try to wean themselves off benzodiazepines.

By the end of the study, 79% of those taking melatonin were able to completely discontinue benzodiazepine use. In the placebo group, only 25% were able to stop using benzodiazepines.

Life Extension advises not to discontinue any medication without prior approval from your treating physician.

What you need to know

Melatonin Compared to Prescription Sleep Medications

• Many people turn to benzodiazepine drugs to help promote sleep. But benzodiazepines cause sedation and are often addictive.
• Research has revealed that even a single dose of a benzodiazepine significantly lowers levels of melatonin, the sleep hormone that is integral to sleep control in the body.
• Trials show that oral melatonin promotes sleep without side effects or the risk for dependence associated withbenzodiazepines.

Summary

The use of benzodiazepines to promote sleep comes with potential side effects and may lead to dependence.

Clinical trials show that melatonin improves sleep quality, helps people fall asleep faster, helps them stay asleep longer, and can help benzodiazepine users discontinue their use of these drugs.

The dilemma is that melatonin does not work for everyone and better methods to improve sleep quality, especially in older individuals, is urgently needed.

Please consult with your treating physician before discontinuing use of any medication.

If you have any questions on the scientific content of this article, please call a Life Extension Wellness Specialist at 1-866-864-3027.

Common Benzodiazepines

The benzodiazepines, often referred to as "benzos," are a group of drugs that induce sedation and sleep.

Below is a list of the most commonly used benzodiazepines:²⁶

Alprazolam (Xanax®)
Diazepam (Valium®)
Lorazepam (Ativan®)
Clonazepam (Klonopin®)
Chlordiazepoxide (Librium®)
Temazepam (Restoril®)
Clorazepate (Tranxene®)
Halazepam (Paxipam®)
Estazolam (ProSom®)
Flurazepam (Dalmane®)
Triazolam (Halcion®)
Oxazepam (Serax®)
Prazepam (Centrax®)
Quazepam (Doral®)

References

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