The Latest News on The Use of Melatonin: It Preps Your Metabolism and Circadian Rhythm
Sixty years after
melatonin was isolated and with more than 23,000 published studies showing the
many functions of this hormone secreted by the pineal gland, it’s time for us
to talk about the safest guidelines for us.
In an article
published in the journal Endocrine Reviews, Dec 2018, Cipolla Neto,
the principal investigator for a project supported by São Paulo Research
Foundation — FAPESP on the role of melatonin in energy metabolism regulation.
According to the research team, melatonin not only adapts us to rest at night but
also prepares us metabolically for the next day, when it will need to be
sufficiently sensitive to absorb food.
“If the nocturnal
production of melatonin is blocked by light during the night, especially by the
blue light from smartphones, this can contribute to diseases, such as sleep
disorders and hypertension, and metabolic disturbances, including obesity and
diabetes. This potentially pathogenic situation is due not only to insufficient
melatonin production but also to one of its more immediate consequences, which
is a condition known as chronodisruption,
a temporal disorganization of the circadian rhythm of biological functions.
The use of melatonin
has been studied greatly over time. For example, between 1996 and July 2017, over
195 systematic reviews were published on the effects of the clinical use of
melatonin, among which 96 addressed the use of melatonin to treat psychiatric
diseases and neurological disturbances, including sleep disorders, while 43
focused on the association between melatonin and cancer.
relating to therapeutic uses of melatonin and analogs filed worldwide between
2012 and September 2014 focused predominantly on the central nervous system —
including sleep disorders, the disruption of the circadian cycle and
neuroprotection — as well as cancer and immunological issues.
New Benefits of
Melatonin — which
derives from tryptophan, an essential amino acid found in proteins — is highly
efficient at eliminating free radicals and has remarkable antioxidant
properties. It interacts directly with free radicals and stimulates antioxidant
enzymes in different tissues.
In recent years,
researchers have discovered that owing to its special properties, it is an
exceptionally important molecule that acts through several mechanisms at almost
all physiological levels, including components of the cardiovascular,
reproductive, immune, respiratory and endocrine systems as well as energy
our temporal order, meaning a property relating to time. chronological
sequence and chronological succession, both daily and on the
seasonal time scale. Its effects depend not just on the route of administration
and concentration but also on the time of administration, among other factors.
Onset of melatonin
production vary from person to person. Early birds (people who wake early)
start their daily melatonin production before night owls (people who stay up
late), and people who sleep for longer periods of time produce melatonin over a
longer time than those who sleep for shorter periods.
A given dose of
melatonin may result in different plasma levels in different patients owing to
individual differences in absorbing, distributing, metabolizing and eliminating
melatonin. These differences are associated with age, clinical condition, the
existence of pathologies, and the functional integrity of physiological systems
such as the gastrointestinal tract, liver and kidneys. A proper chronic
melatonin hormonal replacement therapy is only achieved when dosage and
formulation are carefully chosen and individually tailored and controlled to
accomplish the desired clinical effect.
A more practical
approach is to take the time at which the patient usually goes to sleep at
night as a reference for the timing of melatonin administration. An oral
lozenge formula like Clear
ZZZ’sshould be taken 45 to 60 minutes before bedtime to be
bioavailable. Also, given that melatonin is a powerful timer of the organism’s
physiology, it should be taken strictly at the same time every day. I explain to patients that feeling groggy
in the morning means you have taken the melatonin at too high of a dose or too
Dose is another key
point to be discussed. There is no consensus in the literature on this matter.
On average, plasma levels in young people who take 0.1-0.3 milligrams will
reach 100-200 picograms per milliliter (pg/ml), equivalent to the expected
normal physiological range, while 1 gram will probably result in plasma levels
of 500-600 pg/ml, which is much higher than the physiological range. I usually recommend
1 to 3 lozenges of theClear
strength, pharmaceutical grade melatonin.
José Cipolla-Neto, Fernanda Gaspar do
Amaral. MELATONIN AS A HORMONE: NEW PHYSIOLOGICAL AND CLINICAL INSIGHTS. Endocrine
Reviews, 2018; DOI: 10.1210/er.2018-00084