5-HTP
chipdouglas 12 Sep 2007
Now, I used mainly 5-HTP to control my anxiety and it's worked very well, at least so far. I'm conservative as far as dosing, and do not think megadosing in anything is a good thing. So I've used nothing in excess of 50 mg/day. 5-HTP is known to be about 10 times more potent than L-Tryptophan, so that is one of the reasons why I kept it low. Normally, I even do 25 mg a day to good result--Placebo effect ? Surely to some extent.
Years ago I stumbled across a post made by Steeven Harris, M.D. raising a red flag about the use of 5HTP as being hazardous and which could potentially cause heart valves damage in a manner similar to the former drug Fenfluramine.
Here's the post by Steeven Harris : http://72.14.205.104...lnk&cd=18&gl=ca
I think L-tryptophan would still be safer, given that it doesn't bypass the rate limiting factor for serotonin production. Also there's still *some* concern over peak-X contamination in either 5HTP or L-Tryptophan, although this doesn't appear to be a significant concern when bought from a reliable manufacturer who is willing to provide C of A for the substance.
Be that as it may, I'd like to hear what those most documented here thing about my using low does of 5-HTP or whether I should either stop, find a replacement or switch to L-Tryptophan ?
Thanks
ajnast4r 12 Sep 2007
NOW brand 5-htp, is >99% pure and certfieid peak X free... and its cheap.
krillin 12 Sep 2007
Try a Sirius Light and Sound machine for anxiety control.
chipdouglas 12 Sep 2007
200 mg nearly killed Meatwad with a stomach lesion. (Hmm. He hasn't posted for over a month. I hope he's OK.) Do you feel lucky?
Try a Sirius Light and Sound machine for anxiety control.
Initially when I tought of posting on the subject of 5-HTP I had what you or someone else has posted about Meatwad, although I failed to mention this bit of info in my initial post above.
I own a CES device prescribed by Dr. Eric Braverman--This works well for anxiety issues. This is the one I have : http://www.cesultra.com/
I'll Google the sirius light---sound machines, I'm acquainted with, but not the sirius light though....sounds interesting.
ajnast4r 13 Sep 2007
chip is already taking it, with no problems. 50mg/day is nothing... if it makes you feel better.. TAKE IT
jagged 14 Sep 2007
Try a Sirius Light and Sound machine for anxiety control.
Any recommendations for a sound machine? I have an old sharper image 'white noise' only machine, but its getting very old and i'm thinking about replacing it.
luv2increase 14 Sep 2007
Try a Sirius Light and Sound machine for anxiety control.
Any recommendations for a sound machine? I have an old sharper image 'white noise' only machine, but its getting very old and i'm thinking about replacing it.
I have a proteus L & S machine. I used to use it a lot but not anymore. I would hook it up to my computer using Neuro-Programmer 2 from transparentcorp.com. I would customize my own sessions. It is very interesting and psychedelic! I think using it too much will F up your brain though [mellow] IMO
chipdouglas 14 Sep 2007
Quercetin acts as a natural catechol-O-methyl transferase (COMT) inhibitor that improves L-DOPA's conversion into Dopamine in the brain and helps prevent Dopamine breakdown.
Found this here : http://www.uniquenut....asp?itemid=455
whitenoise 17 Sep 2007
A few things to keep in mind:
-Vitamin B6 catalyzes the reaction from 5-HTP to 5-HT. Wait a while after taking 5-HTP to take any B6. I say this because B6 is common in energy drinks and is a common supplement used for alertness. 5-HT can't cross the BBB and is generally bad outside the CNS, so co-supplementing with B6 wastes 5-HTP and increases plasma levels, although honestly the waste of good supplements is probably the bigger problem.
-Don't combine 5-HTP with MAOIs. The risk of serotonin syndrome is not particularly large, but better safe than sorry.
~Whitenoise
chipdouglas 17 Sep 2007
luv2increase 17 Sep 2007
-Don't combine 5-HTP with MAOIs. The risk of serotonin syndrome is not particularly large, but better safe than sorry.
At least not maois that inhibit mao-a. MAOIs that inhibit mao-b wouldn't be a problem. Also, taking 5-HTP with fruit juice will help it cross the blood brain barrier.
stayin_alive 17 Sep 2007
sometimes in the morning and when having trouble sleeping.
A few years ago, I'd take it and wait some small period of time and drink strong coffee - maybe even esspresso and for a very small period - like a fraction of second, I'd get a bump of "feel good" like having an orgasm. And then, if i laid down ..anytime in the next few hours I would drift off, just like as if I had an orgasm [mellow]
shifter 17 Sep 2007
I didn't notice anything like that when taking it though.
Evolutionary 17 Sep 2007
krillin 17 Sep 2007
-Vitamin B6 catalyzes the reaction from 5-HTP to 5-HT. Wait a while after taking 5-HTP to take any B6. I say this because B6 is common in energy drinks and is a common supplement used for alertness. 5-HT can't cross the BBB and is generally bad outside the CNS, so co-supplementing with B6 wastes 5-HTP and increases plasma levels, although honestly the waste of good supplements is probably the bigger problem.
B6 body half-life is about 25 days, so you'd have to wait a long while.
chipdouglas 17 Sep 2007
krillin 17 Sep 2007
Yikes, I had no idea it was that long. But aren't B6 water soluble, and therefore flushed through urine within a day ?
B6 gets phosphorylated to PLP, which is bound to proteins in tissues. The body's a lot better at hanging on to B-vitamins than many vitamin companies would have you believe.
whitenoise 18 Sep 2007
B6 body half-life is about 25 days, so you'd have to wait a long while.
Curious, live and learn I suppose. Do you know if the phosphorylated form still catalyzes/catalyzes as well as the standard form of B6? I wonder because I found that taking them simultaneously or taking B6 prior to 5-HTP significantly weakened the effect of the 5-HTP. However, taking the 5-HTP first and giving it some time, then taking the B6 seemed to have a stronger effect. My theoretical explaination was that taking the 5-HTP first gave it time to build up in the brain and CNS before catalyzing the reaction.
Since complex molecules' catalytic properties are structure-dependent, the phosphorylated and protein-bound form may not necessary work with 5-HTP. I may also be completely off and my experiances may have been dependent on other factors that I have not taken into consideration.
Thoughts? I'm curious about the biochemistry behind this.
krillin 18 Sep 2007
Curious, live and learn I suppose. Do you know if the phosphorylated form still catalyzes/catalyzes as well as the standard form of B6? I wonder because I found that taking them simultaneously or taking B6 prior to 5-HTP significantly weakened the effect of the 5-HTP. However, taking the 5-HTP first and giving it some time, then taking the B6 seemed to have a stronger effect. My theoretical explaination was that taking the 5-HTP first gave it time to build up in the brain and CNS before catalyzing the reaction.
Since complex molecules' catalytic properties are structure-dependent, the phosphorylated and protein-bound form may not necessary work with 5-HTP. I may also be completely off and my experiances may have been dependent on other factors that I have not taken into consideration.
Thoughts? I'm curious about the biochemistry behind this.
B6 doesn't work at all unless it gets phosphorylated. I believe I read in Murray's supplement book that you can only convert about 50 mg of pyridoxine to pyridoxal-5-phosphate at a time, but I've never been able to track down a primary reference. If you take gobs of pyridoxine, the unconverted portion could act as a B6 receptor blocker, since the toxicity symptoms are similar to deficiency symptoms.
whitenoise 18 Sep 2007
krillin 19 Sep 2007
Thanks Krillin, appreciate the information. Maybe when I get some time I'll poke around the University science library.
A good place to start is to read the National Academies Press dietary reference intake books. Just google "nap [insert nutrient here]".
chipdouglas 19 Sep 2007
19 Sep 2007
A few things to keep in mind:
-Vitamin B6 catalyzes the reaction from 5-HTP to 5-HT. Wait a while after taking 5-HTP to take any B6. I say this because B6 is common in energy drinks and is a common supplement used for alertness. 5-HT can't cross the BBB and is generally bad outside the CNS, so co-supplementing with B6 wastes 5-HTP and increases plasma levels, although honestly the waste of good supplements is probably the bigger problem.
-Don't combine 5-HTP with MAOIs. The risk of serotonin syndrome is not particularly large, but better safe than sorry.
~Whitenoise
What form of b6 are you referring to the pyridoxine form or the p-5-p form that wastes 5-htp?
whitenoise 19 Sep 2007
20 Sep 2007
Pyridoxine, but according to krillin it's metabolized into p-5-p form shortly afterwards.
Yeah, thanks, I saw that.
That might be true for some people (that you can only convert about 50 mg of pyridoxine to pyridoxal-5-phosphate at a time) but not for me. I take two doses of 1,000 mg. of pyridoxine every day because of by B6 dependency. The only problem I ever had was increasing the amount of p-5-p I also take with it. I have read and have had the experience myself that at some point the pyrdoxine form by itself stops working and you have to also use the p-5-p form. That is why I usually recommend to people that they just take both forms because long term supplementing with just the pyridoxine form will stop working at some point. I don't exactly understand why that is though, but thought it was something about how the liver converts it into the active form.
We may be referring to the same issue. I see it as a problem with the liver just doesn't process the pyridoxine form alone at some point (and needs the more active form of p-5-p for some reason to utilize the pyridoxine form) while krillin sees it as the amount of the pyridoxine dose as the problem. It seems like these two may be the same issue just slightly different interpretaions.
whitenoise 20 Sep 2007
krillin 20 Sep 2007
http://www.ajcn.org/...t/full/75/4/616
3 mg pyridoxine/day will get you 60 nM P5P.
25 mg/day will get you 200 nM.
http://www.pubmedcen...ageindex=3#page
100 mg/day will get you about 430 nM.
Higher doses are hit and miss. For one group, there was no real difference between 100, 200, 300, and 400 mg/day, with the range being 340.6-478.8. For the other group, there was no real difference between 100, 200, and 300 mg/day (range 303.3-458.0), but it spiked to 689.6 at 400 mg/day.
So it looks more like diminishing returns than a threshold.
20 Sep 2007
The Warning claims that without a PDI most or all of the 5-HTP will be converted to serotonin in the bloodstream outside the brain; and since serotonin does not cross the blood-brain barrier, this would nullify any hoped-for brain benefit from 5-HTP. Yet successful studies (only some of many published) using 5-HTP without a PDI (1,2,4,6,11) clearly refute this contention. Furthermore, studies infusing tryptophan or 5-HTP directly into the bloodstream of human subjects have been performed, and these studies have not found any increase in blood serotonin caused by increased blood 5-HTP. Thus, one report states: Six healthy male subjects received ... 5-hydroxy-L-tryptophan (5-HTP) ... on two occasions in a randomized cross-over study. There were marked increases in urinary 5-HTP and 5-HT [serotonin] excretion after infusion of [5-HTP] ... .
http://jamessouth.or...id=101&Itemid=9
Further down on that site it mentions B6's possible role.
The Warning also claims that Americans use of vitamin B-6 supplements further worsens 5-HTPs (alleged) danger, since B-6 activates the enzyme that could convert 5-HTP to serotonin in the bloodstream. Yet experiments with monkeys (18) and rats (19) fed even moderate excess amounts of B-6, increased brain serotonin production up to 60%--an impossible finding if B-6 would cause the bulk of ingested 5-HTP to be prematurely converted to serotonin outside the brain. And College Pharmacy of Colorado, one of Americas premier mail-order compounding pharmacies, has been selling (by prescription) a 100 mg 5-HTP with 12.5 mg B-6 (and no PDI) since 1990 with no problems.
The site has some interesting warnings about 5htp though.
bgwowk 20 Sep 2007
http://yarchive.net/med/5-htp.html
Even if it is now known that 5-HTP does successfully make into the brain and become serotonin there, surely *some* of it is being converted to serotonin in the liver, and one has to wonder about the long-term effects on heart valves.
Comment: Yes, and in fact 5-HTP needs only one more step to
become serotonin-- a decarboxylation. The sequence is:
Tryptophan --> 5-HTP --> Serotonin.
An exactly analogous sequence is:
Tyrosine --> L-DOPA --> Dopamine
In both cases the end product neurotransmitter does not get
across the blood brain barrier very well, but all of the
precursor molecules above are transported by the brain's large
neutral amino acid pump, and they get into the brain fine. Thus,
if you are a Parkinson's patient who wants to raise dopamine
levels, you must take L-DOPA, not dopamine. Similarly, it would
do you no good to take serotonin-- you must take tryptophan or
5-hydroxytryptophan (5-HTP).
Now for the complications. (Aren't there always complications
in life?) The final reaction to the neurotransmitter in both the
case of dopamine and serotonin, is decarboxylation, and the same
enzyme (the aromatic L-amino acid decarboxylase) is involved in
both conversions. This decarboxylase enzyme is present in the
liver, and it acts in the case of L-DOPA to convert the compound
to dopamine before it can make it into the brain (and if this
happens, the L-DOPA is wasted). The decarboxylase enzyme uses B6
as a cofactor for this reaction, and for this reason a
Parkinson's disease patient taking L-DOPA cannot take more than
the RDA of B6, because doing so would act to neutralize
oral L-DOPA too quickly. These days, almost all Parkinson's
patients on L-DOPA take the drug in a combination with an
artificial decarboxylase inhibitor, called Carbidopa (the
combination is called Sinemet). But even with Carbidopa,
Parkinson's patients are advised not to exceed a daily dose of B6
of 25 mg, since more will overwhelm the Carbidopa effect, and
cause pharmacologic L-DOPA to be destroyed in the liver before it
can get into the brain.
Now, Carbidopa, because it acts on the same metabolizing
enzyme in the liver, performs exactly the same preservative
service for 5-HTP as for L-DOPA. For this reason, neurologists
have experimented with giving Carbidopa to people who needed to
take 5-HTP to raise brain serotonin (this in the days before
selective serotonin re-uptake inhibitor antidepressants like
Prozac were available). The problem today with 5-HTP-selling
companies bypassing doctors and going to laymen, is that a lot of
health enthusiasts with problems who are enthusiastically taking
5-HTP are NOT taking Carbidopa, but they ARE taking a lot of B6
in one form or another. Yet without Carbidopa, more than a few
milligrams of extra B6 per day would be expected to insure that
most dietary 5-HTP gets turned into serotonin before it can get
into the brain.
Alas, one company I know packages their 5-HTP in 50 mg
capsules with 10 mg of B6. They do this ostensibly so that 5-HTP
can be converted to serotonin in the brain. Duh. This insures
that any 5-HTP will get converted to serotonin in the liver
instead, and thus never make it to the brain. Vitamin B6 is the
*LAST* thing you want in an 5-HTP product.
At the very best, people who take B-vitamins with 5-HTP, or
who take 5-HTP products with B6, waste their money. All this
would be merely humorous (caveat emptor) were it not for some
other facts. At worst, ignorant people fooling with 5-HTP
actually risk their health, since serotonin in the peripheral
blood is not benign. 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 in their right hearts, which can cause heart failure.
This fibrosis is caused by the serotonin. This 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 mash (matuki), which poisons them
with its serotonin content. No, I'm not making this up. The
hydroxylation of tryptophan is a rate-limiting step in the
peripheral production of serotonin, and one bypasses it at one's
peril.
How much does it take? Several hundred milligrams of 5-HTP
taken per day, if converted to serotonin, would result in a
urinary excretion of the serotonin metabolite 5-hydroxyindoleac-
etic acid (5-HIAA) of several hundred milligrams also-- an amount
well within the urinary excretion range of the average person
with a serotonin producing carcinoid. Such a dose of 5-HTP
certainly would result in a serotonin blood load comparable to
that of green-banana-diet eating people who have
serotonin-induced heart valve disease. Normally, people do not
excrete breakdown products of more than 10 mg of serotonin
metabolites per day. If you take one capsule per day of 50 mg
5-HTP with 10 mg B6, however, you would be expected to go to at
least 50 mg per day of 5-HIAA in the urine. Less metabolism in
the liver (less B6) would result in less 5-HIAA in the urine. If
you are going to take 5-HTP, therefore, you probably need 5-HIAA
urine monitoring, to figure out just how big a dose of systemic
serotonin you're actually getting (and incidentally, how much
5-HTP you're wasting). See a doctor!
For all the reasons outlined above, I am presenting those
vitamin companies who sell 5-HTP with B6, or who sell it alone
but don't warn their customers about 5-HIAA monitoring or B6
intake, a special award: the Green Banana Award. This honor is
for those supplement-sellers who monkey around with people's
health before consulting with some really good nutrition and
medical specialists to make sure they don't f*&% up and hurt
somebody. Hopefully, companies which receive the Green Banana
Award will contemplate its message, and will thereby change their
behavior in order to avoid some of the less-coveted awards which
otherwise await them in the future: the Civil Damage Award, for
instance, or even the All-Expense-Paid Guest of the Federal
Government Award.
Steven B. Harris, M.D.