Bootlegger
Bluelighter
- Joined
- Dec 9, 2000
- Messages
- 222
Make of it what you will
WARNING About 5-hydroxytryptophan
Many members of Life Extension Foundation have called us to ask that we offer 5-hydroxytryptophan (5-HT). 5-HT is approved as drug in Europe for the treatment of depression and it would be logical to assume that Americans should also be able to benefit from this amino acid analog.
In reviewing the published literature, however, we've found some potentially serious adverse side effects that Americans might encounter when using 5-HT. Interestingly, most Europeans would be far less likely to encounter these side effects.
--------------------------------------------------------------------------------
The reasons for the potential risks of 5-HT, were brought to our attention by Steven B. Harris, M.D. Dr. Harris explained that:
5-hydroxytryptophan 5-HT is one step closer to serotonin than tryptophan. The sequence is as follows:
Tryptophan
5-hydroxytryptophan
Serotonin
Based on the above metabolic sequence, it would appear desirable to use 5-HT instead of tryptophan since 5-HT more readily,converts to serotonin.
Serotonin is a neurotransmitter that is often deficient in the brains of depressed people. Boosting serotonin can alleviate depression in some people and reduce carbohydrate cravings in others, thus including weight loss.
Here's why 5-HT will not work for most Americans and could be lethal to some people: The blood-brain barrier does not allow significant absorption of serotonin from the blood. The brain does have a large neutral amino acid pump that freely allows tryptophan and 5-HT into the brain for conversion into serotonin
The process by which 5-HT is converted into serotonin is called decarboxylation. If decarboxylation occurs before 5-HT absorbed by the brain, then blood levels of serotonin will elevate significantly, but very little serotonin will enter the brain.
When Europeans take 5-HT, they are often prescribed the dopa decarboxylase inhibitor carbidopa that prevents 5-HT from being converted into serotonin until it reaches the brain. Americans do not take carbidopa with 5-HT and the result is possible serotonin overload in the blood, with virtually no serotonin reaching the brain. We will describe later the dangers of overloading the blood with serotonin.
Americans taking 5-HT are more vulnerable to blood serotonin overload because, unlike most Europeans are who are vitamin deficient, Americans who use 5-HT usually take large doses of vitamin B6 as well. Vitamin B6 rapidly converts 5-HT into serotonin before it reaches the brain. Even when combined with carbidopa, high levels of vitamin B6 will break through the carbidopa barrier and insure that 5-HT converts into serotonin in the blood before the it can reach the brain.
The multiple health benefits of vitamin B6 are too important, we believe, to recommend that people avoid taking vitamin B6 just to enable them to try using 5-HT to boost brain serotonin levels. This may be difficult anyway without also taking carbidopa, which is only available in the U.S. as a prescription drug.
At the very best, those who take vitamin B6 with 5-HT are probably wasting their money. Unfortunately, high serotonin in the blood is not benign. Anyone suffering from heart disease should avoid 5-HT because the elevation in blood serotonin could cause coronary artery spasm and/or abnormal platelet aggregation, which are risk factors for sudden death heart attack.
Here is the real frightening aspect of serotonin overload, as described by Dr. Harris: "Serotonin causes not only harmless flushing and diarrhea, but people with serotonin secreting tumors (hindgut carcinoids) also have problems with fibrosis of the endocardium and valves of their right hearts, which can cause heart failure The effect can also be seen with dietary intake of only modest amounts of serotonin, and there has actually been described in the medical literature, a tribe of South Sea islanders with right heart fibrosis as a result of eating green banana mush, which poisons them with its serotonin content."
Dr. Harris goes on to state that people who ingest several hundred milligrams a day of 5-HT with B6 and without a decarboxylase inhibitor would expect to see urinary excretion of a serotonin metabolite in the same range as a person with a serotonin secreting tumor.
Based upon Dr. Harris' report, the Foundation had its analysts conduct an extensive review of the medical literature and have come to the following preliminary conclusions:
For 5-HT to boost serotonin levels in the brain it is necessary to:
a) Take 50 mg of carbidopa before each 5-HT dose. Carbidopa is a prescription drug.
b) Limit vitamin B6 supplementation to a small dose taken at least before or after 5-HT/carbidopa dosing.
c) Have a urinary test to metabolite of serotonin called 5-hydroxy indoleacetic acid (5-HIAA) regular basis. As long as 5HIAA levels are normal, than 5-HT intake would be safe.
Those with existing cardiovascular disease, including arterial fibrillation, coronary artery disease, congestive heart failure, cardiomyopathy, valvular disease or pulmonary hypertension want to avoid 5-HT completely. One Foundation analyst felt that 81 mg of aspirin and 500 mg a day of magnesium would reduce the risk of 5-HT inducing a heart attack.
The effects of 5-HT by itself elevating blood serotonin are extremely individualistic. Some people may not experience any blood serotonin increase, while others could suffer from lethal serotonin peripheral overload.
Despite the potential dangers of 5-HT, most FDA-approved drugs to treat depression and obesity appear to be more toxic.
At the time of this printing, we have not been able to verify whether 5-HT serotonin overload would cause fibrosis of the aortic valve and destruction of the heart muscle.
Based on the potential health risks of ingesting 5-HT, the Foundation has decided not to offer it to members at this time. We encourage anyone seeking to use 5-HT to follow strictly the above protocol for safe 5-HT supplementation. We'll be reporting further evidence regarding 5-HTP as soon as it becomes available.
This warning applies only to 5-hydroxy tryptophan (5-HT), not tryptophan itself. Published studies show that tryptophan does not readily convert into serotonin blood, but that 5-HT does, since 5-HT convert directly into serotonin tryptophan has to go through one additional metabolic step which protects against serotonin overload.
From http://www.lef.org/magazine/hotlines3.html
------------------
And the Mission is the Mouse...
And then this...
From: UnclJunior ( [email protected] )
Subject: Re: LEF and 5-HTP
Newsgroups: sci.life-extension
Date: 2000/08/15
I received this letter from Will Block of Life Enhancement regarding
Life
extentions 5-HTP attack:
The basis for all their accusations are non-existant. Steve Harris,
MD, was
the original source for their criticism in an online missive that
never
provided any references. And he was largely wrong, as the widespread
studies -- and loads of empirical and clinical evidence -- done over
the
years have shown.
For one, and LEF continues to ingnore this, quite a few studies have
been
done with 5-HTP in humans in which the 5-HTP was given with nothing
else
(Zmilacher, 1988). 5-HTP works as well (if not better) when used
without
peripheral decarboxylase inhibitors. Moreover, side effects have been
found
to be greater with peripheral decarboxylase inhibitors than without. A
review of the scientific literature found that 5-HTP given alone had
better
results (249/389 subjects were found improved) than when 5-HTP was
used with
a peripheral decarboxylase inhibitor (93/176 subjects). This
represents a
significant superiority of 21% (64% vs 52.9%) for 5-HTP alone over
5-HTP
with a peripheral decarboxylase inhibitor.
Regarding the use of vitamin B6, its presences does not cause 5-HTP to
rapidly convert into serotonin before it even reaches the brain. In
one
notable study on rats, vitamin B6 deficiency was deliberately induced.
It
was discovered that very little serotonin was produced in the rat
brain when
deficient in B6 (Dakshinamurti, 1976). In other experiments with
monkeys and
rats, the presence of ample amounts of B6 - even to the point of
"moderate
excess" - increased production of serotonin (in the brain) from 5-HTP
by up
to 60%.(Dakshinamurti, 1976; Hartvig, 1995). Once again, it is clear
that
5-HTP raises brain serotonin levels - with or without carbidopa or
benserazide, and with or without vitamin B6. But the evidence
indicates that
it's better to take 5-HTP without carbidopa or benserazide and with
vitamin
B6 (Siow, 1985).
So what can I say? I used to write for LEF and they were much better
then,
citing references so an inquisitive person could find out the basis
for any
statement, and be closer to the truth. There are undoubtedly good
things
published by Bill and Saul -- I applaud their attitude about
regulation and
the goals of life extension -- but, they do their members and the
public a
disservice when they don't reference their articles and the source of
their
positions.
By the way, the sigle most responsible person for the introduction of
the
concept of Life Extension is a user of 5-HTP, as are friends of mine
who
still work for LEF.
All the best,
WB
[This message has been edited by Bootlegger (edited 08 August 2001).]
WARNING About 5-hydroxytryptophan
Many members of Life Extension Foundation have called us to ask that we offer 5-hydroxytryptophan (5-HT). 5-HT is approved as drug in Europe for the treatment of depression and it would be logical to assume that Americans should also be able to benefit from this amino acid analog.
In reviewing the published literature, however, we've found some potentially serious adverse side effects that Americans might encounter when using 5-HT. Interestingly, most Europeans would be far less likely to encounter these side effects.
--------------------------------------------------------------------------------
The reasons for the potential risks of 5-HT, were brought to our attention by Steven B. Harris, M.D. Dr. Harris explained that:
5-hydroxytryptophan 5-HT is one step closer to serotonin than tryptophan. The sequence is as follows:
Tryptophan
5-hydroxytryptophan
Serotonin
Based on the above metabolic sequence, it would appear desirable to use 5-HT instead of tryptophan since 5-HT more readily,converts to serotonin.
Serotonin is a neurotransmitter that is often deficient in the brains of depressed people. Boosting serotonin can alleviate depression in some people and reduce carbohydrate cravings in others, thus including weight loss.
Here's why 5-HT will not work for most Americans and could be lethal to some people: The blood-brain barrier does not allow significant absorption of serotonin from the blood. The brain does have a large neutral amino acid pump that freely allows tryptophan and 5-HT into the brain for conversion into serotonin
The process by which 5-HT is converted into serotonin is called decarboxylation. If decarboxylation occurs before 5-HT absorbed by the brain, then blood levels of serotonin will elevate significantly, but very little serotonin will enter the brain.
When Europeans take 5-HT, they are often prescribed the dopa decarboxylase inhibitor carbidopa that prevents 5-HT from being converted into serotonin until it reaches the brain. Americans do not take carbidopa with 5-HT and the result is possible serotonin overload in the blood, with virtually no serotonin reaching the brain. We will describe later the dangers of overloading the blood with serotonin.
Americans taking 5-HT are more vulnerable to blood serotonin overload because, unlike most Europeans are who are vitamin deficient, Americans who use 5-HT usually take large doses of vitamin B6 as well. Vitamin B6 rapidly converts 5-HT into serotonin before it reaches the brain. Even when combined with carbidopa, high levels of vitamin B6 will break through the carbidopa barrier and insure that 5-HT converts into serotonin in the blood before the it can reach the brain.
The multiple health benefits of vitamin B6 are too important, we believe, to recommend that people avoid taking vitamin B6 just to enable them to try using 5-HT to boost brain serotonin levels. This may be difficult anyway without also taking carbidopa, which is only available in the U.S. as a prescription drug.
At the very best, those who take vitamin B6 with 5-HT are probably wasting their money. Unfortunately, high serotonin in the blood is not benign. Anyone suffering from heart disease should avoid 5-HT because the elevation in blood serotonin could cause coronary artery spasm and/or abnormal platelet aggregation, which are risk factors for sudden death heart attack.
Here is the real frightening aspect of serotonin overload, as described by Dr. Harris: "Serotonin causes not only harmless flushing and diarrhea, but people with serotonin secreting tumors (hindgut carcinoids) also have problems with fibrosis of the endocardium and valves of their right hearts, which can cause heart failure The effect can also be seen with dietary intake of only modest amounts of serotonin, and there has actually been described in the medical literature, a tribe of South Sea islanders with right heart fibrosis as a result of eating green banana mush, which poisons them with its serotonin content."
Dr. Harris goes on to state that people who ingest several hundred milligrams a day of 5-HT with B6 and without a decarboxylase inhibitor would expect to see urinary excretion of a serotonin metabolite in the same range as a person with a serotonin secreting tumor.
Based upon Dr. Harris' report, the Foundation had its analysts conduct an extensive review of the medical literature and have come to the following preliminary conclusions:
For 5-HT to boost serotonin levels in the brain it is necessary to:
a) Take 50 mg of carbidopa before each 5-HT dose. Carbidopa is a prescription drug.
b) Limit vitamin B6 supplementation to a small dose taken at least before or after 5-HT/carbidopa dosing.
c) Have a urinary test to metabolite of serotonin called 5-hydroxy indoleacetic acid (5-HIAA) regular basis. As long as 5HIAA levels are normal, than 5-HT intake would be safe.
Those with existing cardiovascular disease, including arterial fibrillation, coronary artery disease, congestive heart failure, cardiomyopathy, valvular disease or pulmonary hypertension want to avoid 5-HT completely. One Foundation analyst felt that 81 mg of aspirin and 500 mg a day of magnesium would reduce the risk of 5-HT inducing a heart attack.
The effects of 5-HT by itself elevating blood serotonin are extremely individualistic. Some people may not experience any blood serotonin increase, while others could suffer from lethal serotonin peripheral overload.
Despite the potential dangers of 5-HT, most FDA-approved drugs to treat depression and obesity appear to be more toxic.
At the time of this printing, we have not been able to verify whether 5-HT serotonin overload would cause fibrosis of the aortic valve and destruction of the heart muscle.
Based on the potential health risks of ingesting 5-HT, the Foundation has decided not to offer it to members at this time. We encourage anyone seeking to use 5-HT to follow strictly the above protocol for safe 5-HT supplementation. We'll be reporting further evidence regarding 5-HTP as soon as it becomes available.
This warning applies only to 5-hydroxy tryptophan (5-HT), not tryptophan itself. Published studies show that tryptophan does not readily convert into serotonin blood, but that 5-HT does, since 5-HT convert directly into serotonin tryptophan has to go through one additional metabolic step which protects against serotonin overload.
From http://www.lef.org/magazine/hotlines3.html
------------------
And the Mission is the Mouse...
And then this...
From: UnclJunior ( [email protected] )
Subject: Re: LEF and 5-HTP
Newsgroups: sci.life-extension
Date: 2000/08/15
I received this letter from Will Block of Life Enhancement regarding
Life
extentions 5-HTP attack:
The basis for all their accusations are non-existant. Steve Harris,
MD, was
the original source for their criticism in an online missive that
never
provided any references. And he was largely wrong, as the widespread
studies -- and loads of empirical and clinical evidence -- done over
the
years have shown.
For one, and LEF continues to ingnore this, quite a few studies have
been
done with 5-HTP in humans in which the 5-HTP was given with nothing
else
(Zmilacher, 1988). 5-HTP works as well (if not better) when used
without
peripheral decarboxylase inhibitors. Moreover, side effects have been
found
to be greater with peripheral decarboxylase inhibitors than without. A
review of the scientific literature found that 5-HTP given alone had
better
results (249/389 subjects were found improved) than when 5-HTP was
used with
a peripheral decarboxylase inhibitor (93/176 subjects). This
represents a
significant superiority of 21% (64% vs 52.9%) for 5-HTP alone over
5-HTP
with a peripheral decarboxylase inhibitor.
Regarding the use of vitamin B6, its presences does not cause 5-HTP to
rapidly convert into serotonin before it even reaches the brain. In
one
notable study on rats, vitamin B6 deficiency was deliberately induced.
It
was discovered that very little serotonin was produced in the rat
brain when
deficient in B6 (Dakshinamurti, 1976). In other experiments with
monkeys and
rats, the presence of ample amounts of B6 - even to the point of
"moderate
excess" - increased production of serotonin (in the brain) from 5-HTP
by up
to 60%.(Dakshinamurti, 1976; Hartvig, 1995). Once again, it is clear
that
5-HTP raises brain serotonin levels - with or without carbidopa or
benserazide, and with or without vitamin B6. But the evidence
indicates that
it's better to take 5-HTP without carbidopa or benserazide and with
vitamin
B6 (Siow, 1985).
So what can I say? I used to write for LEF and they were much better
then,
citing references so an inquisitive person could find out the basis
for any
statement, and be closer to the truth. There are undoubtedly good
things
published by Bill and Saul -- I applaud their attitude about
regulation and
the goals of life extension -- but, they do their members and the
public a
disservice when they don't reference their articles and the source of
their
positions.
By the way, the sigle most responsible person for the introduction of
the
concept of Life Extension is a user of 5-HTP, as are friends of mine
who
still work for LEF.
All the best,
WB
[This message has been edited by Bootlegger (edited 08 August 2001).]
