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The Dark Side Of Melatonin

sleep-melatonin

People should not self-medicate with melatonin.” – Dr. Richard Wurtmann, MIT neuroscientist who first discovered melatonin

– by Piyali Syam, Huffington Post

Twenty-one years ago, MIT neuroscientist Dr. Richard Wurtman introduced melatonin as a new solution to sleep problems. His lab patented supplements in hopes of curing insomnia in the older population, whose melatonin receptors calcify with age.

“Researchers say pills of the natural hormone…will bring on slumber quickly without the addictive effects of drugs,” the New York Times reported at the time. In the same article, Judith Vaitukaitis, then director of the National Center for Research Resource, said the hormone “offered hope for a natural, non-addictive agent that could improve sleep for millions of Americans.”

Wurtman himself wasn’t quite so cavalier. In that same article, he warned, “People should not self-medicate with melatonin.”

Despite Warnings And Lack Of Safety Trials, Melatonin Was Pushed Prematurely To The Shelves, Even Sold To Children

Nonetheless, melatonin was a hit. In the last two decades, the all-natural sleep aid has earned a spot in medicine cabinets across the country. Inexpensive, easily accessible, naturally occurring and considered safe, melatonin appeals to the those who’d rather avoid prescribed pills. Naturopaths, chronic insomniacs, shift-workers and frequent fliers pop milligrams of melatonin without thinking twice.

According to the National Center for Complementary and Integrative Health, nearly 1.3 million American adults reported taking melatonin in February, 2015. Parents are even handing it out to their kids — 419,000 as of February — believing melatonin to be a harmless, naturally produced hormone.

Melatonin is indeed naturally produced, but the hormone is one of the murkiest supplements on the market, unsubstantiated by incomplete and developing research.

Only in the U.S. is melatonin available over-the-counter as a dietary supplement, and long-term usage can alter natural hormone levels and even sabotage sleep. Given to children, its potential side effects are even more concerning.

Melatonin, secreted by the pineal gland, is the messenger that announces bedtime to our brains. Darkness stimulates its release into the bloodstream; light inhibits it. Once released, it binds to hormonal receptors located in the brain’s suprachiasmatic nuclei — a cluster of nerves that regulates the body’s internal clock and circadian rhythms — and travels into cerebrospinal fluid and the bloodstream.

“It won’t kill you, but it’ll make your life pretty miserable.”

Our bodies naturally produce “endogenous” melatonin (or, “growing or originating from within an organism”). What ends up on pharmacy shelves in synthesized “exogenous” melatonin — growing or originating from outside an organism. Its most common application is that of sleep aid; users are told to take their dose directly before bedtime, when endogenous levels are already on the rise. Frequent fliers swear by its effectiveness in recovering from jet lag recovery, saying the hormone helps reset their biological clock in a new time zone.

Studies also suggest melatonin can help prevent sleep disorders in children suffering from ADHD and autism (though its use in kids remains controversial).

The FDA classifies melatonin as a dietary supplement. Dr. Wurtman sees this as a marketing ploy to circumvent the bureaucratic web of research and patents that typically burden the process of bringing drugs and hormones to market.

And that’s where the problems arise.

Given the lack of apparent side effects, it may seem harmless to label melatonin as a dietary supplement. But the classification matters for consumers, because the FDA doesn’t require supplements to include warnings of overdose risks on their labels, as is mandatory for drugs and hormones.

Perhaps even riskier, the classification allows companies to sell melatonin in varying dosages.

In 2001, researchers at MIT concluded that the correct dosage for melatonin falls between .3 and 1 mg. Yet, walk down the pharmacy aisle and you’ll see stacks of sleep aids packing as 10 times that amount.

It’s easy to take too much, and most of melatonin’s side effects are the result of just that. While there’s no evidence that too much melatonin could be fatal, or even remotely life-threatening, exceeding the proper dosage can upset the body’s natural processes and rhythms.

“With some hormones, if you take too much you can really put your body in danger,” says Dr. Wurtman. “With melatonin, you’re not in danger, but you’re also not very comfortable. It won’t kill you, but it’ll make your life pretty miserable.”

And, despite common perception, melatonin can cause next-day drowsiness, according to Michael Grandner, a sleep researcher at the University of Pennsylvania.

More importantly, melatonin is a hormone. With children, according to Grander, it can affect puberty, disrupt menstrual cycles and impede normal hormonal development.

Excess melatonin can also induce hypothermia, as body temperatures reduce during melatonin release, and stimulate overproduction of the hormone prolactin, which can cause hormonal problems and even kidney and liver issues in men.

When used occasionally and at the correct time, melatonin is a fine means of encouraging sleep. But, ironically, with prolonged use, it can actually amplify insomnia. Having too much melatonin in the system, the theory goes, overwhelms the receptors, changing how a patient reacts to the hormone — whether it’s endogenous or exogenous.

According to Dr. Wurtman, melatonin supplements may work at first, but soon “you’ll stop responding because you desensitize the brain. And as a consequence, not only won’t you respond to the stuff you take…you won’t respond to the stuff you make, so it can actually promote insomnia after a period of time.”

Mauricio Farez, an Argentinian sleep researcher, has similar reservations. “I have some issues, in terms of the pharmacology, and…it’s really hard to have stable levels of the drug in our blood.”

“People should not self-medicate with melatonin.”

Grandner agrees. “Taking melatonin for an extended period of time your body may acclimate and re-adjust and produce less over time which will work against you.”

When it comes down to it, taking melatonin to fall asleep sooner doesn’t even work. “When it’s nighttime and melatonin levels are high,” says Dr. Wurtman “taking melatonin supplements is like putting a drop of water into an empty bucket; when it’s daytime, it’s like putting a drop of water into a full bucket.”

Farez wants to see more research on its immunologic potential, as his most recent study suggests melatonin could play a role in managing multiple sclerosis. It’s also widely used to fight certain types of cancer, as it combats tumor cells.

Allowing melatonin to sit on our shelves, unregulated and sold as freely as aspirin, is a problem waiting to happen.

Sleep Statistics By The Numbers:

  • Two-thirds of adults in developed nations fail to obtain the nightly eight hours of sleep recommended by the World Health Organisation.
  • An adult sleeping only 6.75 hours a night would be predicted to live only to their early 60s without medical intervention.
  •  A 2013 study reported that men who slept too little had a sperm count 29% lower than those who regularly get a full and restful night’s sleep.
  •  If you drive a car when you have had less than five hours’ sleep, you are 4.3 times more likely to be involved in a crash. If you drive having had four hours, you are 11.5 times more likely to be involved in an accident.
  •  A hot bath aids sleep not because it makes you warm, but because your dilated blood vessels radiate inner heat, and your core body temperature drops. To successfully initiate sleep, your core temperature needs to drop about 1C.
  •  The time taken to reach physical exhaustion by athletes who obtain anything less than eight hours of sleep, and especially less than six hours, drops by 10-30%.
  •  There are now more than 100 diagnosed sleep disorders, of which insomnia is the most common.
  •  Morning types, who prefer to awake at or around dawn, make up about 40% of the population. Evening types, who prefer to go to bed late and wake up late, account for about 30%. The remaining 30% lie somewhere in between.

Researchers Recommend Safer, More Effective Alternatives To Melatonin For Falling Asleep Faster and Staying Asleep Longer

According to the American Academy of Sleep Medicine 30-35% of adults experience regular symptoms of insomnia – whether it’s trouble falling asleep, trouble staying asleep, or lack of sound, fully-relaxing sleep quality – this is extremely troubling!

This statistic highlights the fact that our modern environment and stressful daily schedules will quickly lead to 1 in 3 people not living their daily life up to their full potential due to the low energy, drowsiness, and brain fog, and hormonal imbalance associated with lack of adequate sleep.

Common symptoms of insomnia include:

  • Fatigue
  • Inability to focus or concentrate
  • Poor memory
  • Mood disturbance
  • Daytime sleepiness
  • Low motivation or energy
  • Increased errors or accidents

If you’re not sleeping through the night, and not falling asleep within 10 minutes of laying down in bed, then you need to focus quickly on improving your body’s ability to achieve incredible, sound nightly rest and recovery.

One of the biggest issues associated with poor sleep quality is hormonal imbalance. Most people do not realize this, but their terrible sleep habits are actually killing their body’s ability to burn fat, due to a regular rise in excess cortisol (the stress hormone) over time, keeping your body in fight or flight mode constantly, which shuttles resources away from processes like fat metabolism over to more survival-oriented processes.

It’s time to take control over your sleep once again.

The following ingredients have been found in the scientific literature to help you safely fall asleep faster:

ASHWAGANDHA (300 mg) – Ashwagandha is an traditional ayurvedic herb that has been used for ages for healing and relaxation.  In fact, it’s technical name is “withania somnifera”, where “somnifera” literally means “sleep-inducer” in Latin.

Ashwagandha has powerful calming and sleep-inducing effects and has many other benefits for hormonal balance, stress reduction, and increased recovery, so we recommend 300 mg of this powerful herb.

LEMON BALM EXTRACT (400 mg) –  Lemon Balm Extract, technically called “Melissa officinalis”, is an herb with powerful relaxant properties. It has also been shown to reduce anxiety and restlessness, as it will help your body calm down and slow down for sleep.

As an added benefit, it also improves mood and increases cognition, helping you fall asleep with a smile on your face and the possibility of awesome dreams.

In terms of maximizing the recovery effect of your sleep, staying asleep longer and getting more benefit from your deep sleep, the following ingredients have been found to help:

L-GLYCINE (2,000 mg) –  L-Glycine is a conditionally essential amino acid that has been recently getting a lot of attention in the science world as an anti-stress, pro-metabolic nutrient.

It’s found in high concentrations in foods like bone broth and gelatin/collagen, which is why these foods are so good for reducing stress and increasing recovery.

It is incredibly protective for cell functioning, decreases inflammation, lowers oxidative stress, improves immune function, prevents muscle loss, protects against endotoxin, and improves mental function. The benefits of L-glycine are wide-reaching, and research shows that even though it’s not an essential amino acid, we don’t get enough in our diets for optimal health. More specifically, it’s been shown to improve sleep quality and duration, and even reduce the negative effects of sleep loss the day after a poor night’s sleep.

We recommend 2 grams of L-glycine, the highest amount we could include, so you can reap the maximum benefit from this important amino acid.

L-THEANINE (300 mg) – L-Theanine is another amino acid, similar to L-Glycine, that has been shown to have many calming and therapeutic properties for healing. It’s a common nutrient in many teas, which can help explain why certain teas can help improve sleep so well.

It helps to counteract sleep disturbances from caffeine and has been shown to generally counteract the effects of stress that commonly disrupt recuperative sleep.

Another interesting effect of L-theanine is its ability to slow your brainwaves, helping your brain more easily shift into deep sleep where the most physical recovery takes place.

We recommend 300 mg of L-theanine in order to deliver these benefits.

MAGNESIUM (200 mg) – Magnesium is one of the critical minerals in your body, and is specifically related to your cells’ ability to relax and move away from the stressed condition.

Magnesium is also one of the most common mineral deficiencies, which can lead to higher states of inflammation, stress, and degradation. Because of this, it’s no surprise that magnesium supplementation has been shown have relaxing properties and to improve sleep quality.

High doses of magnesium can cause gastric upset, so we recommend the perfect amount – 200 mg – to deliver the benefits without any side effects.

Also, due to the high typical consumption of caffeine for most people, it can be useful to be able to naturally clear this caffeine from your system so as to not disturb your sleep. The following ingredient is proven to help with this:

RUTAECARPINE (100 mg) – Rutaecarpine is a component of the evodia rutaecarpa fruit, and it has the ability to bind to caffeine and remove it from your bloodstream.(35-38) Since caffeine has a 6-hour half-life – possibly even longer depending on your metabolism and genetics – your sleep may be getting affected more than you realize.

With 100 mg of Rutaecarpine, you can be sure that you’re clearing your system of any caffeine before you hit the hay.

You might be wondering where you can find all of this…

Here at Kinobody we decided to help people safely, naturally fall asleep using these exact ingredients and dosages by developing the brand new Kino Sleep formula, which is now available here.

 

Greg O'Gallagher

Greg O'Gallagher is the founder of Kinobody, a site dedicated to helping men and women achieve the lean, muscular, and aesthetic "Hollywood" physique. His fitness programs have helped hundreds of thousands of people transform their bodies and change their lives in the process.