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Sleep supplements are a hugely popular contributor to the globally growing sleep market; with a global spend in excess of $81.19 Billion each year on sleep medications since 2020.

Sleep diagnostics such as Tracking Wearable Devices (FitBit, Oura), Smart Bedding (Withings), Sleep Lab Services and Sleep Apnea Devices have all contributed significantly to the popularity of sleep tracking and improving the quality of sleep.  

But what if I told you sleep and its complexities of falling asleep and remaining asleep – are not that complex at all.

The answers actually lie in simple biochemistry reliant on the Biopterin pathway of the body.

Biopterin, also known as tetrahydrobiopterin or BH4 is a cofactor of the three aromatic amino acid hydroxylase enzymes, used in the degradation of amino acid phenylalanine and in the biosynthesis of the neurotransmitters serotonin (5-hydroxytryptamine, 5-HT), melatonin, dopamine, norepinephrine (noradrenaline), epinephrine (adrenaline). It is also a cofactor for the production of nitric oxide (NO) by the nitric oxide syntheses (PMID 393083).

 

The Biopterin pathways of the body shows us two distinct biochemical situations the body requires for sleep:

  1. Elevated Serotonin and Reduced Dopamine.
  2. Conversion of Serotonin to Melatonin during Sleep.


We can then look for nutritional deficiencies which could be leading to:

  1. Reduced Serotonin or Tryptophan deficiency.
    Supplement with tryptophan or direct precursor 5-HTP.
  2. Reduced melatonin production (daytime exposure to sunlight isn’t enough).
    Main root cause for waking up in middle of the night and not falling back asleep.

    Your body converts Serotonin to Melatonin using a circadian clock enzyme called AANAT. This is why Melatonin as a supplement just doesn’t work; the half-life is too short and when you have eliminated it from your body, the lack of endogenous Melatonin wakes you up.

    The two main nutritional deficiencies contributing to reduced Melatonin:

    Vitamin B6 (Pyridoxal-5-Phosphate) deficiency causing poor conversion of 5-HTP to Serotonin

    or

    B5 (Pantothenic acid) deficiency which could be causing poor Serotonin conversion to Melatonin.

    Let’s also not forget about the impact blue and UV-light can have on the pineal gland secretion of melatonin at nighttime to signal its dark and to prepare for sleep onset.

 

  1. Magnesium deficiency.
    Main cofactor for Catechol-O-Methyltransferase (COMT) which clears Catecholamines – Dopamine, Epinephrine and Ephedrine in the body.

    Too much Dopamine/ Epinephrine etc being produced in your brain at bedtime and you will be “wired” at bedtime.

    The glycinate version (Magnesium Bisglycinate) is a bioavailable form which provides 2 of the amino acid Glycine which helps feed into GABA cycle.

    GABA (Gamma Aminobutyric acid) is an amino acid that acts on GABA receptors in the brain, which seek to inhibit brain activity, calming the brain down.

    GABA as a supplement is a poor way of eliciting GABA activity as if you don’t efficiently clear GABA, it will convert to Glutamate which is neuro-stimulatory leaving you feeling wired and tired also.

 

  1. Too much Tyrosine.
    Avoiding too much tyrosine close to bed time as this will feed into Dopamine cycle.

    Serotonin also acts as an inhibitor of COMT so if you are increasing the levels of Serotonin though 5-HTP supplementation, we must ensure there is no further stimulation in the production of Dopamine or other catecholamines in the body.

    Why there is a trend to include Tyrosine (which is also the precursor to thyroid hormone) in a sleep supplement today is beyond any reasonable point of sleep biochemistry but I digress.

 

  1. Possible SAM (methylation) issue
    S-Adenosyl-Methionine (SAMe) is also a cofactor of COMT, as it provides the methyl donor (CH3) group for methylation (the process which turns our genes on or off).

    Supplementing with SAMe so close to sleep can go very wrong if you are a poor methylator; as the increase in SAMe will just lead to insomnia.

    Niacin acts as a methyl donor acceptor, so it can readily clear SAMe; and a strategy often implemented by those who utilize Niacin as a health supplement.  

 

 

From all this complex science and sleep biochemistry, I designed the Sleep Stack to utilize 6 simple ingredients to help you fall asleep, and to then keep you asleep.

  1. 5-HTP to raise Serotonin neurotransmitter levels to aid with sleep onset.

  2. Pyridoxal-5-Phosphate to improve the function of tryptophan hydroxylase (TPH) and Aromatic Aminoacid Decarboxylase (AADC) which converts 5-HTP to Serotonin.

  3. Pantothenic acid (Vitamin B5) to support the function of the arylalkylamine-N-acetyltransferase (AANAT) which converts Serotonin to N-Acetylserotonin which undergoes methyltransferase activity to Melatonin.

  4. Zinc Monomethionine as a bioavailable source of Zinc which contributes positively to Central Nervous System (CNS) recovery and also provides a source of methionine which is important in the production of SAMe (S-Adenosyl-Methionine).

  5. Magnesium Bisglycinate to supply Magnesium to COMT to work efficiently to clear Dopamine to calm the brain down and Glycine to aid with GABA receptor activity.

  6. L-Theanine (gamma-glutamylethylamide), an amino acid which influences Serotonin and GABA levels in the brain.


With the ever-increasing trend and focus on sleep, its important that we don’t just address insomnia with medications which fail to induce slow wave brain patterns of sleep. Benzodiazepines etc. effectively just take a sledgehammer to your brain to induce a state of unconsciousness without allowing the brain to progress through the various cycles of sleep.

 

Next time, I’ll cover what we can do from a sleep hygiene perspective and why you might consider stacking the PM Priming Stack alongside Sleep Stack and our blue light blocking glasses for the perfect evening setup for restorative sleep.

 

Dr Dean St. Mart PhD; Product Manager and Formulator for Supplement Needs 

 

TLDR - Summary:

What promotes the perfect biochemical environment for deep sleep?

  1. High Serotonin to promote alpha wave production and sleep onset (falling asleep)
  2. Conversion of Serotonin to Melatonin (staying asleep).
  3. Low Cortisol (low stress)
  4. Low Epiniephine/Norepinephrine
  5. Low Dopamine.

 

What contributes to poor sleep onset (falling asleep)?

COMT overload and not clearing catecholamines efficiently

This could be from:
1. Too many androgens (PED users)
2. Too much estrogen / not eliminating estrogen at the liver (poor COMT activity)
3. Lack of magnesium
4. Lack of SAM and methylation
5. Too much Dopamine (stimulation at bedtime).
6. Lack of Progesterone (can tie in with time of month for females)


References
Peuhkuri K, Sihvola N, Korpela R. Dietary factors and fluctuating levels of melatonin. Food Nutr Res. 2012;56:10.3402/fnr.v56i0.17252. 
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3402070/