Sceletium Pro (formulation)
Balance - Attain Emotional Wellness
The Significance of Sceletium tortuosum
In its 4th century of recorded use!
Sceletium tortuosum is a rare succulent from the Mesembryanthemaceae
family and is distributed in certain semi-desert areas of Southern Africa.
It was (and still is) highly regarded and sought after by both the Khoikhoi
and the San (bushmen) people who have used this plant as a mood enhancer
since prehistoric times.
The earliest written record of the use of the plant
dates back to 1662 when Sceletium was an item of barter during the early
settler culture in South Africa and it was considered then the “…greatest
clearer of spirits, and the noblest Restorative in the world…”.
Sceletium elevates mood and decreases anxiety, stress
and tension, and functions as a model anxiolytic, as well as being a
very effective anti-depressant. Sceletium is also known to reduce addictive
cravings particularly with regard to nicotine and also lessens the withdrawal
effects of alcohol. Due to its ability to stimulate feelings of empathy
it has also been used with success in couple therapy.
In large doses Sceletium can cause euphoria, but without
any associated come-down. Long-term use followed by abstinence
has not been reported to result in any withdrawal state. The plant is
not hallucinogenic, and no severe adverse effects have been documented.
Sceletium is a truly effective plant with which to
treat the stress, anxiety and lack of balance often attributed to our
busy western lifestyle. Sceletium has a unique ability to bring about
emotional balance and, simultaneously cause both relaxation and stimulation
of a positive mood. More profoundly it also engenders a sense of connectedness
and meaning, making it an ideal supplement for anyone living in the
modern world.
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Sceletium
formulation including co-factors
2 Size "0" Vegetarian Capsules (a daily dose) supply:
| Sceletium tortuosum* |
50 |
mg |
| L-Tyrosine (free-base) |
120 |
mg |
| Trimethylglycine |
125 |
mg |
| Nira Brahmi (Bacopa mannieri) 8:1 extract |
150 |
mg |
| Folate (from Folic acid) |
200 |
µg |
| Vitamin B12 (as Methylcobalamin) |
150 |
µg |
* The question may be asked as to why this product is called Sceletium
given the formulation, where 3 of the other co-factors are present in
greater volume? The relative potency of the Sceletium tortuosum employed
is such that, even though it is in the minority by volume relative to
L-Tyrosine, Trimethylglycine and Nira Brahmi, it nonetheless dominates
the resulting performance of the formulation.
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Chemistry
and Pharmacology
Sceletium
The active constituents of the plant are alkaloids, including
mesembrine, mesembrenone, mesembrenol and tortuosamine. Mesembrine is
the major alkaloid present in Sceletium, and has been determined in,
as yet, unpublished laboratory studies, to be a very potent and effective
serotonin re-uptake inhibitor.
This receptor-specific activity, as well as receptor
activities also found on nicotinic, dopamine and norepinephrine sites
validate the traditional mood-elevating uses, and suggest additional
therapeutic and wellness potential.
Mesembrine alkaloids also appear to have a harmonizing
and balancing effect on other neurotransmitters such dopamine and norepinephrine
and epinephrine.
L-Tyrosine (free-base)
Tyrosine is the nutrient pre-cursor of dopamine, norepinephrine
and epinehrine and is intimately involved with these important mood-affecting
brain neuro-transmitters.
Environmental stress is associated with reduced levels
of norepinephrine. Tyrosine prevents reduction of norepinephrine levels
that are associated with this stress. Many clinical studies, along with
a large body of anecdotal evidence, indicate that Tyrosine is a vital
substance in alleviating depression, as well as the symptoms of premenstrual
syndrome.
L-Tyrosine is also a direct precursor to Thyroxin (Triiodo
Tyrosine), which is a primary Thyroid hormone. Thyroxine deficiency
results in a series of conditions including excess weight gain, cold
hands and feet and decreased basal metabolism. L-Tyrosine supplementation
works to counteract this.
It has also been found that Tyrosine lowers blood pressure
by increasing norepinephrine metabolites.
One of L-Tyrosine's primary metabolic pathways is:
L-Tyrosine -> L-Dopa -> Dopamine -> Norepinephrine (nor-adrenalin)
-> Epinephrine (adrenalin).
Increased levels of L-Dopa are associated with improved
mood and greater capacity for pleasure in the body-mind, while norepinephrine
controls our level "mental" energy". It is included for
these reasons and also to balance the relaxation effect that is induced
by the Sceletium.
Nira Brahmi (Bacopa monnieria)
Bacopa monnieria, or Brahmi, is a famous Ayurvedic herbal remedy
for mental revitalizing and enhancement. It is effective for all body
types. Bacopa is highly recommended in the Asian medical literature
and has been prescribed by Oriental physicians as one of the very best
mental revitalizing herbs for thousands of years. Contemporary phytochemical
research has revealed evidence that Bacopa is an antioxidant. Antioxidants
have been linked to improved brain and nervous system function. Another
study found that Bacopa use increases the I.Q. scores of students.
Bacopa monnieria is used traditionally for memory, insomnia, epilepsy,
insanity and other related conditions, mental acuity, and mental clarity,
as a nervine, for learning disabilities, attention span deficiencies,
speech impediments, and headache.
In addition, Bacopa contains several glycosides that
have demonstrated significant anxiolytic, relaxing and anti-stress effects
in pharmacological studies.
Studies revealed that bacosides, which are the major
phyto constituents in Bacopa monnieria, help to repair damaged neurons
by enhancing proteins involved in the regeneration of neural-cell synapses.
[The Bacopa used in our formulation is an 8:1 extract standardized to
16% bacosides.]
Thus Bacopa monnieria can be viewed as nourishment
for neural processes that, restores depleted synaptic activity and leads
to enhanced memory function, clarity and mental balance.
Trimethylglycine
Trimethylglycine (TMG), which is also called glycine betaine,
is a methylation agent (or methyl donor) that lowers homocysteine levels
(a contributory factor in heart disease) and, by contributing one of
its methyl groups to DNA, potentially reduces DNA aging and errant DNA
replication processes.
Methyl donors (like TMG) are directly involved in the
formation of numerous brain chemicals, which accounts for their positive
cognitive effects.
TMG functions specifically as a biological stable precursor
of the very unstable
S-adenosyl-methionine (SAMe). SAMe is a critical factor in biochemical
reactions and a proven anti-depressant.
SAMe has been used in clinical studies to treat depression,
schizophrenia, demyelination diseases, dementia, peripheral neuropthy
and other conditions. Several studies have confirmed that SAMe is up
to15% more effective in the treatment of depression than traditional
pharmaceutical anti-depressants.
Methyl donors are:
- Required for the growth of new cells.
- Essential for the manufacture of DNA bases.
- Able to prevent DNA mutations and strand breaks.
- Able to prevent the expression of disease causing genes.
- Able to reduce the risk of genetically induced cancers.
- Able to protect against alcohol induced liver injury.
- Used to neutralize a wide range of toxins.
- Required to support the function of many antioxidants.
- Able to promote the production of serotonin, melatonin and other
neurotransmitters.
- Required to detoxify histamine to relieve allergic symptoms.
- Vital in the final steps of protein manufacture.
- Able to help repair and regenerate vital proteins.
- Able to slow and even reverse aging.
Folate (from Folic acid)
Folate is a B Vitamin that plays many critical roles in the
body especially with regard to emotional state and mental acuity. It
is crucial for DNA and RNA synthesis and is used by the body to produce
S-adenosyl methionine (SAMe), which has been established as having a
strong effect on mood. SAMe is also essential for over 100 identified
essential methylation reactions, such as the methylation of nucleic
acids (DNA and RNA), phospholipids (myelin), polysaccharides, and catecholamines,
and many other molecules.
The effects of adequate Folic acid supplementation
for the treatment of depression, anxiety and other forms of mental /
emotional impairment are well documented. Studies have shown that a
high proportion of the American population is deficient in folate, and
folic acid deficiencies have been linked to depression in clinical studies.
Folic acid deficiency also causes serotonin levels in the brain to decrease,
which is another cause of depressed mood and impaired mental function.
Vitamin B12 (as Methylcobalamin)
Although the most commonly used form of Vitamin B12 is cyanocobalamin,
vitamin B12 is biologically active in only two forms, methylcobalamin
(which is used in this formulation) and adenosylcobalamin. While methylcobalamin
is active immediately upon absorption, cyanocobalamin must be converted
to either methylcobalamin or adenosylcobalamin by the body before use.
Methylcobalamin is the superior form of Vitamin B12
to use, especially in a formulation that is designed to impact on mood.
Methylcobalamin is the only form of vitamin B12 found in the brain and
it supports a healthy brain, spinal cord and nervous system, which together
are necessary foundation optimum mental and emotional health.
Methylcobalamin is essential for the metabolism of
nerve tissue and it stimulates the utilization of proteins, fats, and
carbohydrates. It is important for the synthesis of DNA and RNA, as
well as for production of choline and methionine, a key SAMe component.
Methylcobalamin has been used for many other symptoms
including fatigue, nervousness and irritability, insomnia, memory problems,
depression, and poor balance.
Adequate methylcobalamin supplementation:
- Regulates sleeping patterns and improves daytime alertness
- Treats physical and mental fatigue (both a cause and effect of depression)
- Ensures optimum cognitive functioning
- Balance's mood
- Stimulates neuronal regeneration in the brain
- Relieves depression, nervousness and irritability
Co-factors Formulation Rationale
Nira Brahmi (Bacopa mannieri) 8:1 extract
Bacopa, in addition to being an axiolytic (and thus supporting
Sceletium's anxiolytic effect), is also a cognitive stimulant, which
Sceletium is not. Sceletium is the superior product for balancing
ones emotional state and is both anxiolytic and anti-depressive to
a significant degree. Bacopa is included for it's profound effect
on balancing mental processes rather than exclusively emotional ones.
L-Tyrosine (free-base)
L-Tyrosine is included as a key nutritional neurotransmitter
precursor. As well as having an excellent stimulating effect on mood
by increasing available brain dopamine, it also causes very mild mental
and physical stimulation via the "downstream" metabolites
of dopamine, being norepinephrine (noradrenalin) and epinephrine (adrenalin).
This will counter any tendency towards "drowsiness" which
could be induced in some cases by the strong relaxation effect of
the Sceletium.
Trimethylglycine
Trimethylglycine is another key nutritional factor that functions
specifically as a biological stable precursor of (the very unstable)
S-adenosyl-methionine (SAMe). SAMe is currently a highly regarded
natural anti-depressant due to its efficacy. In addition, TMG, as
a methyl donor, is involved in countless neurochemical processes and
it specifically harmonizes and enhances the production of key neurotransmitters
such as serotonin (intimately concerned with mood) and melatonin (which
positively affects our waking and sleeping cycles). TMG, in a similar
fashion to our other included co-factors, can be seen as promoting
a "fertile environment" (in terms of brain chemistry) for
supporting the more specific actions of Sceletium, Bacopa and L-Tyrosine.
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Clinical
and Supplement Uses
Sceletium is being used successfully by a number of
psychiatrists, psychologists and doctors with excellent results for
anxiety states and mild to moderate depression, and it can also be used
by the lay public as a food supplement to elevate mood and for relief
from stress and tension.
In addition to Sceletium's common use to mitigate the
stress and mental fatigue of modern day living, Sceletium has been used
as a natural food supplement in treating:
- Low mood, including gray weather syndrome
- Anxiety states, including social phobia
- Irritability in menopause
- Improvement in libido, when lack of libido is from anxiety or low
mood
- Post-traumatic stress disorder, as part of a support program
- Bereavement
- Any anxiety and/or tension producing state, such as examinations
In addition to these better-known clinical uses, there
is some preliminary evidence that Sceletium may be of value as a supplement
in drug addiction rehabilitation and alcohol rehabilitation support,
as part of a formal program. Research is currently underway to evaluate
it’s potential in cognitive enhancement, and the management of
Parkinson’s Disease and Alzheimer’s Disease.
Our supplement formulation, based on Sceletium, is
designed to build upon and enhance the primary effects of Sceletium
and offer benefits in all areas related to mental and emotional balance
and enhancement.
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Dosage
Sceletium may also be used in conjunction with Sutherlandia
Pro, or taken alone.
The recommended consumption is 2 capsules per day,
together or divided, usually taken later in the day. Under a practitioner’s
guidance this can be increased to 4 capsules spread throughout the day.
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Side
Effects
Very few people experience side effects. The reported
side effects are considered mild and include rare occurrence of:
- Mild headache
- Slight nausea, no vomiting
- Soft stool or loose stool with no cramping
- Transient increase in anxiety or irritability, which resolves itself
after an hour or so
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Contraindications
Although there have been no confirmed reports of drug
interactions, because of the neuro-receptor activities of Sceletium
there are theoretical interactions with other psychiatric medications
and cardiac drugs. People taking any psychiatric drug (including all
anti-anxiety drugs, sedatives, hypnotics, anti-depressants and anti-psychotics
and so-called designer or recreational drugs) or any cardiac medications,
are advised not to take Sceletium-containing products.
As with most supplements and modern drugs, safety in
pregnancy has not been established and Sceletium should not be taken
without prior consultation with one's physician.
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Raw
Materials
Stocks of wild Sceletium plants have dwindled from
over-harvesting over centuries. Therefore no wild-harvested plant material
should be used in commercial supplements, and manufacturers should always
insist on certificates of origin for Sceletium raw material.
Sceletium is also a very sensitive plant and has thus
far been notoriously difficult to grow on a large commercial scale and
so supply has generally lagged behind commercial demand.
Our group has pioneered an association of local growers,
and is significantly invested in developing the means to cultivate Sceletium
on a sustainable commercial basis to meet the anticipated increasing
demand.
Currently, because Sceletium is grown on a small scale
by a number of tightly-knit groups in South Africa that include local
indigenous communities, limited quantities of top-grade raw material
are available, and only seasonally. The Sceletium being tendered is
only sourced in this manner and is certified organically cultivated
and non wild-harvested.
Brahmi extract is sourced from one of the top Ayurvedic
plant extracts company in India.
Natural Stress Relief with Sceletium Tortuosum Sceletium Tortuosum has been used by hunter-gatherers and shepherds as a mood-enhancing substance for hundreds of years and is far more effective and rapidly acting than the well-known St John's Wort. It lessens anxiety, stress and tension, raises spirits and enhances the sense of connection. If you take a very large dose you may even feel euphoric, then taken over by a sense of drowsiness. It does not cause hallucinations.
Your mood and mental performance depend on a variety of nutrients that feed the brain, nervous system and neurotransmitters. These include vitamins B3, B6, folic acid (folate), B12 and C, zinc, magnesium, essential fatty acids, and the amino acids, tryptophan and tyrosine.
Research has found that a lot of people with psychiatric disorders, including depression, were deficient in the B vitamin folate. Some government dietary surveys also show that a large portion of the population don't even receive the bare minimum recommended amount of these vitamins and minerals, in their daily diet. That is why depression is on the increase.
A link between depression, insomnia, anxiety, suicide, migraines, PMS, obsessive/compulsive behaviour, stress, obesity, and addiction is a low level of serotonin.
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What is Serotonin and How does it work?
Serotonin is a chemical neurotransmitter, a chemical in the nervous system that helps transmit messages along the nervous system. Serotonin is considered the 'mood neurotransmitter', which keeps us emotionally, and socially stable. Our body naturally produces serotonin from the essential amino acid tryptophan, which is found in protein-containing foods.
Researchers have found that when they take recovered depressed patients and deprive them of tryptophan, their depression returns. In general, giving tryptophan to depressed people has been beneficial. Some types of depression are called Serotonin Depression because people affected by imbalances in serotonin levels. Serotonin depression symptoms can affect depressive disorders, bipolar disorders, anxiety and eating disorders. Women seem to have more problems than men in maintaining their serotonin levels. Women who are low in serotonin are likelier to express their anger inwardly, with depression and even suicidal behaviour. Men who are low in serotonin are often violent and can even engage in dangerous criminal acts. Alcohol and drug abusers also turn out to be low in serotonin. The good news is that you can successfully correct these imbalances with supplements that raise serotonin.
Supplementing an amino acid called 5-hydroxytryptophan (5-htp), which is one step closer than trytophan to serotonin, has been shown to produce even better mood-enhancing results.
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How does Sceletium Work?
The mood-elevating action of Sceletium is caused by a number of alkaloids including mesembrine, mesembrenol and tortuosamine which interact with the brain's dopamine and serotonin receptors. Sceletium also contains many nutrients, including minerals and amino acids. According to laboratory studies sponsored by the National Institute of Mental Health near Washington DC, its major alkaloid, mesembrine, promotes serotonin levels. It also appears to have a harmonising and balancing effect on the other feel-good neurotransmitters, dopamine and noradrenalin, as well as on adrenalin. An effective dose is 50mg a day, although some doctors report needing to use 100 to 200mg a day for those with chronic depression or anxiety.
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