Introduction
In a world where sleep is often elusive, and the pressures of modern life keep us burning the midnight oil, the quest for a good night's rest has never been more critical. Amid this pursuit, one topic has sparked heated debates and divided opinions: Melatonin. Is it the magical elixir for sleep-deprived souls, or are we merely buying into an overhyped trend? Let's dive in to find out the truth.
What is Melatonin?
Melatonin is a hormone secreted by the Pineal gland, a small, pea-sized structure in the brain. This hormone regulates the sleep-wake cycle, also known as the circadian rhythm. This is a simplified pathway of production:
Tryptophan (amino acid) -> Serotonin -> Melatonin
Melatonin is typically released in response to the absence of light, signalling to your body that it's time to wind down and prepare for sleep.
How much Melatonin does the body Normally Produce?
The amount of melatonin the body produces typically can vary from person to person and is influenced by several factors, including age, genetics, and individual sleep patterns. In particular, melatonin production decreases as we age.
Under normal conditions:
- Melatonin has a baseline secretion level but ramps in the evening, peaking by 2-4 AM and returning to baseline by 6-8 AM.
- Night production is estimated at 10–80 µg (1)
- Overall, 24-hour production is estimated at less than 0.3 mg (300 µg) for most people. This is reduced in older adults.
Source: Wikimedia
What affects Melatonin production?
1) Age - In older adults, daily production reduces. This is why melatonin is often not recommended before the age of 55.
2) Light- Blue light exposure can delay the peak in melatonin. Red light exposure has no or minimal effect and can be viewed safely, especially useful as a bedside night light.
3) Caffeine - Coffee consumption too late in the day blocks adenosine receptors and has been shown to inhibit melatonin secretion. (3)
4) Overseas travel & shift work - When your circadian cycle is out of sync, you will likely be getting light or consuming caffeine when your body attempts to signal you to sleep via melatonin release.
What Melatonin Dose should I take and when?
There are some ridiculously high dosages (such as 10-60mg) of melatonin available online - consumption of these makes no physiological sense and will likely lead to next-day grogginess.
Timing:
Melatonin is best taken 1-2 hours before bed when you have a diagnosed circadian rhythm disorder or briefly need help adjusting to a new sleep schedule, e.g. change of time zones. Melatonin is not a sleeping pill.
Dosage:
- 0.3 mg for most adults.
- As we noted above, the average night-time secretion of melatonin is less than 0.1 mg. Taking standard-high commercial dosages of melatonin, such as 5-20mg, in the hopes that it will be an effective sleeping pill will likely lead to side effects.
- A study comparing melatonin levels in the blood after a 0.3 and 3 mg dose found that sleep efficiency was best at 0.3 mg. Melatonin plasma levels remained artificially elevated into the daylight hours after the 3 mg dose (4). Imagine what 60 mg would do!
Sleep efficiency in subjects with normal sleep (A) and age-related insomnia (B) following melatonin.
Source: J Clin Endocrinol Metab, Volume 86, Issue 10, 1 October 2001, Pages 4727–4730, https://doi.org/10.1210/jcem.86.10.7901.
What dose are you REALLY getting of Melatonin?
A study of 30 commercially available melatonin supplements found that the actual melatonin content ranged from -83% to +478%!! 26% of the supplements also contained serotonin, which should not be in a melatonin supplement (5).
The moral of the story here is that many supplements you buy online are unfortunately not produced to a sufficiently high standard. Especially when the dosage is critical, like with melatonin, do you want to roll the dice?
It is best to buy your supplements/medicines from a retailer producing listed medicines such as those on the Australian Register of Therapeutic Goods (ARTG) and with Good Manufacturing Practice (GMP) principles.
Please note that melatonin is only available over the counter in Australia (2023) if strict conditions are met.
What can you expect from Melatonin?
Melatonin is not a sleeping pill. It is a hormone released by the body, enhanced by certain conditions such as darkness.
Melatonin (immediate release) may improve sleep onset (by a modest 7 minutes, according to this meta-analysis (6)). Some people may find themselves then waking up in the night due to its short half-life (20-60 minutes) or conversely higher dosages may lead to elevated plasma levels for far too long. It is also essential to be used in groups more likely to benefit, such as those over 55 with circadian rhythm disorders.
Effects vary significantly from mild improvements to daytime drowsiness.
What about Tart Cherry for melatonin?
Tart Cherry is predominantly a natural source of melatonin, so it would be expected to work similarly (7). That being said, the dosage of melatonin you receive will be highly variable.
Side Effects of Melatonin
- Daytime Drowsiness: Taking too much melatonin or consuming too late can lead to excessive drowsiness during the day, impairing concentration and performance. Melatonin levels should drop to baseline by 6-8 am. High dose melatonin supplements can prevent this.
- Nausea: Some people may experience digestive issues, including nausea, stomach cramps, or mild gastrointestinal discomfort after taking melatonin.
- Headaches: Occasional headaches have been reported as a side effect of melatonin supplementation.
- Dizziness: Melatonin can cause dizziness in some individuals, mainly when used in high doses or combined with other medications or substances that affect blood pressure.
- Mood Changes: While uncommon, mood swings and changes have been reported in some people taking melatonin supplements.
- Interactions with Medications: Melatonin can interact with certain medications, including blood thinners, anticoagulants, and immunosuppressants.
- Allergic Reactions: While extremely rare, some individuals may experience allergic reactions to melatonin supplements, such as itching, swelling, or skin rash.
- Sleep Disruptions: Paradoxically, melatonin can disrupt sleep patterns in some individuals, leading to sleep disturbances or nightmares.
- Suppression of endogenous production: There is insufficient evidence to say if taking high dosages of melatonin regularly will ablate your body's melatonin production. However, it is plausible based on how other hormone systems work in the body. It is unlikely to occur at small dosages, but the very high dosages available online could be problematic.
Why does Melatonin make me tired in the morning?
This is a frequent side effect and relates to:
- Taking melatonin too late in the evening
- Taking a dose that is too high (almost all melatonin supplements available online)
- Variability in the listed dose versus the actual amount contained in the product
- Using melatonin without a specific indication to do so
When Melatonin doesn't work
For some people, especially those diagnosed with an applicable sleep disorder, melatonin may be helpful. For many people, however, melatonin does not get the job done as it is not a sleeping pill and is frequently misused.
Try the following:
1) Increase melatonin naturally to assist with sleeping
- Avoid excessive bright, blue light in the evening or near bed-time. This means phone screens, computers and TVs.
- Use a sleep-mask, especially if you're a shift worker or your room is not dark enough.
- Get sunlight in the morning after waking or use an artificial bright light.
- Avoid caffeine after 2 PM (or 6-8 hours before bed).
- Keep a regular sleep routine where possible.
- If travelling, try to take flights that allow you to stick to your existing circadian rhythm or adjust to a new timezone if staying for an extended time.
2) Have a wind-down routine
- Don't eat too close to bed-time
- Avoid working until late
- Calm the mind with meditation or music
- Read a book rather than scroll on your phone
- Take a warm bath
- Ensure your room is cool when ready to sleep
3) Try natural relaxing sleep aids
Suppose you have done all the above and still need help. In that case, various medicines with evidence-based mechanisms assist with mind relaxation and sleep. See below.
4) Serious insomnia
It is best to see your medical doctor.
Best Alternatives to Melatonin
1) Valerian root - effective for some but can cause paradoxical arousal, headaches or daytime drowsiness
2) Chamomile - mild relaxation support, can be consumed in a tea, avoid if you have an allergy to ragweeds
3) Lemon balm or passionflower - gentle relaxation via optimising GABA in your brain
4) Ziziphus - traditionally used in Chinese medicine as a sleep aid
5) Magnesium - needs to be taken in a suitable form for you at a higher dose than most supplements provide. It can also assist with muscle relaxation.
5) Combination supplements are often the most effective as they target multiple different synergistic mechanisms of action. It is essential to look for proper therapeutic dosages and a high level of transparency and regulation. Check out Unwind+ by We Know Health. It contains therapeutic dosages of magnolia bark, lemon balm, passionflower, ziziphus and taurine. You can also read about the research behind the ingredients.
Conclusion
Taking melatonin is not as simple as popping a pill and falling asleep, waking refreshed in the morning. It is not a sleeping pill but a hormone that is tightly regulated by your body.
There are many issues in selecting the right people who may benefit, the correct dosage, the right timing and the right product (melatonin content can vary wildly despite label claims).
There are many alternatives to melatonin. We recommend starting with optimising your night-time release of melatonin and practising a wind-down routine, followed by trialling different natural, evidence-based medicines.
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