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Melatonin

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What is melatonin?

Melatonin in the brain

Melatonin is a hormone produced by the pineal gland within the brain. It's function is to regulate sleep by inducing tiredness in accordance with the daily light cycle. A deficiency of melatonin consequentially results in insomnia. A supplement of melatonin is therefore a safe treatment to prevent insomnia.

Other than regulating sleep, it's also a very effective anti-oxidant which efficiently protects the brain. Melatonin is a very special anti-oxidant in that it has no adverse effects when too much of it is consumed, contrary to all other anti-oxidants, because it is self-regulating.

Besides its anti-oxidant and sleep regulating properties, melatonin also has a positive effect on the genital glands, it is an anti-inflammatory and it stimulates the immune system. In short, even people that don't suffer from insomnia can benefit from taking melatonin as a supplement.

History

Back in the days when people with a darker skin colour were still considered by some to be inferior to those with lighter skins, people were looking for a substance that could bleach the skin. During his literature study in 1953, researcher Aaron Lemer stumbled across an article about frogs whose skin would turn lighter after they were emerged in a crate of pineal-gland extract of cows.

This piqued his interest and after extensive research he found the substance responsible for the change in colour. He called this substance melatonin. “Mela” is derived from the word “melanin” which is a substance in the body responsible for the production of pigmentation; the word “tonin” was used because melatonin is a derivative of serotonin. However, soon it became clear that melatonin could do much more than just changing the skin tone.

Because of the discovery of melatonin, another important purpose of the pineal gland was uncovered. For a long time it was thought to be a rudimentary organ; that is was expendable much like the appendix. Fortunately, due to the discovery of melatonin this perspective has changed, for the pineal gland is an extremely special organ, also referred to as the third eye. Researcher Rick Strassmann even speculates that the pineal gland produces DMT, which is a highly hallucinogenic substance which, according to Strassmann, induces high amounts of DMT the moment a person dies, or has a near death experience. The discovery of melatonin thus resulted in a deeper understanding of the purpose of the pineal gland.

Chemistry

Melatonin is chemically known as N-Acetyl-5-methoxytryotamine. The moment less light enters the cornea, a signal is sent from the eye to the pineal gland, which converts serotonin into melatonin through the process of methylation. If one produces a low amount of serotonin, he or she will also produce low amount of melatonin. This explains why people suffering from depression (which is a consequence serotonin deficiency), also encounter sleeping difficulties.

melatonin chemical structure

Melatonin supplements always contain the synthetic variant. Theoretically it would be possible to extract the hormone out of the pineal gland of animals, but it's an expensive procedure. However, synthetic melatonin is just as effective as the natural extraction.

Effects of Melatonin

Melatonin belongs to, as the chemical name suggests, the tryptamine group. Melatonin thus has a consciousness altering effect, in that it makes dreams very lively, although these dreams often contain seemingly unrelated absurdities. However, if you are interested in lucid dreaming, it could be interesting to experiment with melatonin.

Medicinal application

Melatonin can also come in handy when facing jet lag. After all, your body has not evolved to withstand flying across the globe within mere hours. This can seriously effect your bodily rhythm, but melatonin can help you restore the balance rapidly. In this same way it can help people who work night shifts.

As was discussed in the introduction, melatonin is often used as a remedy for insomnia. However, you must realize that not all problems can be solved with melatonin. Only when a person experiences trouble falling asleep it could be a good solution, because melatonin does not keep you asleep. Notwithstanding that it's always worth a shot, due to the lack of risk and it not being addictive, in contrast to many pharmaceutical sedatives.

Alzheimer-, Lyme-, Parkinson-, MS- en ME patients usually produce too little melatonin, resulting in difficulties with sleeping. It also appears that a disorder such as autism, depression or psychosis often results in a low production of melatonin. Taking supplements may be an effective treatment, but one has to be careful, because if a person experiences a disorder within the autoimmune system, such as in the case of arthritis and MS, it could also have adverse effects. Melatonin is quite powerful in stimulating the immune system, which means that diseases related to the autoimmune system could develop further. The opinions are divided on whether or not to adopt melatonin as a treatment for these diseases.

insomnia

In addition, when women experience hypertension (high blood pressure) as a result of hormonal fluctuation caused by menopause, melatonin stabilizes these swings, which in turn lowers the blood pressure. For men, nightly blood pressure swings can be stabilized as well. Because melatonin also protects the brain it can be advised to take supplements after someone has had a heart attack. After a heart attack the oxidative stress rises, which negatively effects the brain tissue. Taking melatonin stops this from occurring.

It also appears that the use of melatonin is promising in reducing severe forms of headaches such as migraine and cluster headaches. This is due to the following properties of melatonin: the anti-inflammatory property, melatonin removes free radicals, it inhibits the activity of nitric oxide synthase, it reduces the sensitivity of pro-inflammatory cytokine, it inhibits dopamine secretion, it creates membrane stabilization and neurovascular regulation. Furthermore, it stimulates the production of GABA and endorphins, thus relieving pain. All of these effects may contribute to diminishing the uncomfortable episodes experienced by people suffering from these attacks.

Melatonin and cannabis

Smoking cannabis drastically increases the uptake of melatonin. After smoking a joint, the level of melatonin can be up to 40 times higher than normal, which explains why cannabis can make you so drowsy. It also explains why people who quit smoking cannabis experience problems falling to sleep. When smoking daily, it results in an extremely high melatonin uptake, so when you quit this habit, the body is going to have to produce melatonin all by itself again. It usually takes a few days up to a few weeks before the melatonin production in the brain is restored. By taking melatonin supplements on the first day you quit, you can counteract the sleeplessness and help secure your resolution. The melatonin can then gradually be phased out.

After a night of partying it can also be difficult to fall asleep and melatonin can also be of help in this scenario. Melatonin is produced by the body in small amounts all throughout the day. With the nightfall, however, it increases steadily peaking at about 3:00 in the morning, after which it's rapidly reduced again. This explains why people working night shifts have expressed 4:00 am to be the most difficult time to stay awake. It also explains why people with insomnia usually lay awake till 4:00 in the morning.

Moreover, it serves as an explanation for why party people are not able to sleep in the morning. On the one hand, certain stimulating substances could have been ingested which increase adrenaline, which inhibits the bodily production of melatonin. On the other hand the body produces very little melatonin in the morning. The phrase “I'm past sleeping” seems all the more appropriate now. Melatonin can offer a solution for this, moreover, after the use of substances and/or alcohol it is all the more vital for the body to get some rest.

Dosing

The dosing lies somewhere between 0.1 mg to 5 mg a day. If you're experiencing trouble with sleeping and wish to experiment with melatonin, it's important to realize not everybody is as quick in breaking down melatonin, which makes the right dose difficult to determine. If your body breaks it down slowly you should take less, otherwise it could lead to unpleasant results.

In severe cases it's advised to visit a sleeping centre, where the level of melatonin is carefully measured. Based on these results you can determine how much your personal dose is and when it should be taken.

melatonin capsules

The adverse effects of too much melatonin include waking up every hour and a half and having very intense dreams. You will be able to remember all of these dreams because you're waking up so frequently; not exactly contributing to a restful night. This is why it is important to take the right amount of melatonin. If you do not have the time or money to consult experts, you can experiment yourself by taking different doses on different moments. If afterwards you're restless in your sleep you've taken too much.

If you are using melatonin to create a more intense dreaming experience a dose of 3 mg is a good starting point. However, you shouldn't have too many things planned for the coming day because you might well experience a restless night. We advise everyone to dose carefully.

Side effects

As discussed, a high dose can have adverse effects. It can contribute to feeling tired during the day, it can make your joints feel painful and it could cause headaches and stomach aches. This makes it important to handle this supplement with care and to use the right dose which provides the desired effect.

It's important to realize that melatonin lowers the blood pressure. If you have hypertension it could possibly be dangerous to take melatonin. It's also been determined that some diabetes-1 patients developed an elevated blood sugar level. In short, melatonin is not without side effects and caution is advised.

Combinations

In order to address sleeping problems, there are a large number of supplements that melatonin may compliment such as: glycine, L-theanine, GABA, calcium, 5-HTP, taurine, vitamin B-6, and zinc. Furthermore, there are herbs with calming properties, such as Valerian, lime-tree blossom, Lebanon cedar, wild lettuce and California poppy. If you are using melatonin as a remedy for insomnia, you can safely and simultaneously experiment with these herbs and supplements. Obviously you should not use them all at once, but try combining two substances to determine the effect it has on you. If you have failed in reaching the desired effect, you can try something else.

lucid dreaming

If you wish to use melatonin in order to promote lucid dreaming it might be nice to experiment with a combination of melatonin and a dream-enhancing herb, such as Uvuma-omhlope, African Dream Root or Calea Zacatechichi. All of these herbs and more can be ordered at Azarius.

Contraindications

Leukaemia and cervical cancer patients are not advised to use melatonin. There is still too little is known of the effects of melatonin on these diseases. Also, pregnant or breastfeeding women should certainly not use melatonin, because during the first year a baby produces no melatonin of its own.

Melatonin reaches the baby through the uterus or through breast-feeding. Additional levels of this hormone could disrupt the natural balance of the child.

When using steroids such as dexamethasone and cortisol, it is not recommended to use melatonin. This will negate the effect of these medicines. If a woman wishes to conceive, it is unwise to use melatonin, because any dose over 10 mg can prevent ovulation. Psychiatric patients should also treat lightly when it comes to taking melatonin, because an increased level of melatonin can worsen certain symptoms. People with severe allergies or autoimmune diseases such as rheumatoid arthritis, should be very careful when it comes to melatonin because, as stated before, melatonin stimulates the immune system which can worsen an allergic or autoimmune reaction.

Links/ References

This article is based on the following sources:

Farmacotherapeutisch Kompas

• Buscemi N, Vandermeer B, Hooton N, et al. Efficacy and safety of exogenous melatonin for secondary sleep disorders and sleep disorders accompanying sleep restriction: meta-analysis. (2006) BMJ 332:385-393. PMID 16473858. Complete article.

• WEISS MD, WASDELL MB, BOMBEN MM, REA KJ, FREEMAN RD Sleep hygiene and melatonin treatment for children and adolescents with ADHD and initial insomnia. J Am Acad Child Adolesc Psychiatry. 2006 May;45(5):512–9. DOI: 10.1097/01.chi.0000205706.78818.ef. PMID 16670647 Abstract.

• Lissoni, P., Resentini, M., and Fraschini, F. "Effects of Tetrahydrocannabinol on Melatonin Secretion in Man." Hormone and Metabolic Research 1986; 77-78. At baseline, the mean value of their melatonin levels was 21.3 pg/ml. Two hours later, it was 904 pg/ml.

• Grinspoon, L., and Bakaler, J.B. "Marihuana as Medicine." Journal of the American Medical Association 1995; 237(23): 1875-76.

• DeVries, Marten W. M.D.1; Peeters, Frenk P.M.L. M.D. Melatonin as a Therapeutic Agent in the Treatment of Sleep Disturbance in Depression, Journal of Nervous & Mental Disease: March 1997 - Volume 185 - Issue 3 - pp 201,202.

• Miller E1, Walczak A, Majsterek I, Kedziora J. Melatonin reduces oxidative stress in the erythrocytes of multiple sclerosis patients with secondary progressive clinical course. J Neuroimmunol. 2013 Apr 15;257(1-2):97-101. doi: 10.1016/j.jneuroim.2013.02.012. Epub 2013 Mar 19. Abstract.


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