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  • AADD Moderators: swilow | Vagabond696

Possible danger associated with 5-HTP?

R

Runner

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Joined
Jul 11, 2002
Messages
325
The link below has come up before and has been brought up again by Pinkanga:
http://yarchive.net/med/5-htp.html
Basically, when injested, 5-HTP being an amino acid, undergoes decarboxylation inside the liver by a certain enzyme. By this process it is converted into 5-HT (serotonin). That is all good, but all this happens way before 5-HTP crosses the blood-brain barrier, and so it is wasted!!! Moreover, serotonin outside the brain causes other complications such as heart fibrosis etc.
All this should have been a common knowledge to all of us, if we did a bit more research! In fact, patients with Parkinson's desease (low levels of dopamine) have been treated using the same principle of using a dopamine precurser (L-DOPA) instead of using a serotonin precursor (5-HTP). EXCEPT, L-DOPA is never given by itself! Otherwise it would be decarboxylised in the liver the same way 5-HTP does! It is given with a decarboxylase inhibitor CarbiDOPA. This prevents L-DOPA being broken down in the liver, and lets it cross over into the brain, which is what we need. This also goes for 5-HTP!!!
Here is some info on Carbidopa (first decent page i've found so might not be the best one for facts/info):http://home.caregroup.org/clinical/altmed/interactions/Drugs/Carbidopa.htm
If anyone has any info on its availability, it would be great. All of this would explain why 5-HTP never really worked for me well, and if it did, it was probably a placebo effect.
[ 09 January 2003: Message edited by: Runner ]
[Edit: Changed title. BigTrancer]
[ 10 January 2003: Message edited by: BigTrancer ]
 
Very interesting article Runner, I would like to hear a second opinion... (this is your cue BT)
 
5-HTP by itself is actually bad for you... I do not think that this is a fair statement.
Firstly, were you taking 5-HTP as a HM measure? If your answer to that question is yes, then 5-HTP was not meant to work for you. There are thousands of stories showing its continuing success as an antidepressant, a cure for insomnia and a weight loss assistant. It has been approved for production & consumption for these uses. If what you're saying is true, then the thousands of 5-HTP users who have never even heard of "Carbidopa" must be feeling one hell of a placebo. Also, would the drug not have been withdrawn from the markets if it was actually harmful on its own (and this harm was as blatantly obvious as this article indicates?) And, why is no one marketing Carbidopa as a supplement to 5-HTP?
From the page you've linked to on Carbidopa -
• nutritional concerns: Until further research is conducted into the interactions of carbidopa and 5-HTP individuals taking carbidopa should refrain from taking 5-HTP as a supplement unless they have consulted with and are under the supervision of a physician trained in nutritional therapies. and
• research: Some studies have found that the combination of 5-HTP and carbidopa 5-HTP and carbidopa may have a beneficial effect in the treatment of intention myoclonus, a neuromuscular disorder. Other research has not been able to confirm these outcomes. and
used to treat: Management of symptoms of Parkinson's disease.
Would you take 5-HTP and Carbidopa in the interests of HM?
There's argument over the safety (namely dosages) of 5-HTP. 100mg a day appears to be a safe dose, however some claim stupidly large doses can be used without side effects. It is undisputed that excesses of serotonin in ones peripheral circulation can cause cardiovascular disease and other side effects. Too much 5-HTP in the diet could potentially result in too much serotonin in the peripheral circulation.
You have a point, but I can't see how you can justify
5-HTP by itself is actually bad for you... nor how you can justify much of an interest in Carbidopa.
There's a lot to be answered for in terms of 5-HTP and how it becomes serotonin. Personally, I'm too sceptical to take it at all.
[ 09 January 2003: Message edited by: apollo ]
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Firstly, the topic title was designed to attract attention, but after all that is what the article in question IS implying.
Secondly, I suggest the article I've linked is read thoroughly, as I have only summarised the general point.
Thirdly, the article states that 5-HTP WAS used in therapy before SSRIs like Prozac became popular. It was however used in combination with Carbidopa. When its limited use was discontinued, it was never approved by FDA, but it is still manufactured by some companies. The thing that strikes me mostly is that some companies combine Vitamin B6 with 5-HTP!!!
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.
In response to "Would I personally take Carbidopa together with 5-HTP", my answer is yes, id probably try in a small dose, but no I would not continue since I do not take 5-HTP at all (although I have in the past on a fair few occasions). I have experienced a bad case of serotonin syndrome possibly associated with 5-HTP consumption that scared me.
So, I do not mean to encourage people by any means to take Carbidopa with 5-HTP OR 5-HTP by itself for that matter. I lay down the facts, people make their own minds up. I personally know people that think 5-HTP is great, and I trust them, so like I said, the facts are before us to make whatever we can of them. Like I said, the article has changed a lot of things for me, primarily, if you think you know everything about something (5-HTP) and take it as common knowledge, more then likelly there is a lot more to be learned.
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To add to all that, perhaps some amount of the 5-HTP one takes does pass through the blood-brain barrier and does get converted into serotonin, but a common syndrome of slight nausea after taking 5-HTP is consistant with its premature decarboxylation.
One thing that should stand out without arguement is to avoid taking any dietary suppliments that contain vitamin B6 prior to taking 5-HTP if the desired effect is to be achieved. It does appear to be a fact that B6 contributes to 5-HTP premature breakdown.
I am writing this note because I just realised that phenylalanine (which ends up as L-DOPA -> dopamine) that I take every day without carbidopa works great for me, so obviously some of it gets to the brain. Similar must happen to 5-HTP.
[ 09 January 2003: Message edited by: Runner ]
 
As I understand it, those studies using carbidopa with 5HTP were very small - they are referred to on this page. There have been studies that have used dosages of up to 900mg and over per day of 5HTP, without using carbidopa. So I do not believe that "5HTP bt itself is actually bad for you".
What all this information demonstrates is the lack of solid evidence about the best way to use 5HTP. If 5HTP was invented tomorrow by a drug company and patented, we would have plenty of research about it. But of course it isn't, and we don't. Nonetheless, I am still happy to use it in moderate doses post MD**.
 
That article definitely took me aside and made me look at 5-HTP in new light. I sent the link over to nutritionist friend of mine who has worked with 5-HTP for many years to get his take on it(posted below). He doesnt think its quite as bad as the article makes out.. but i'll keep looking to find other evidence on the whole B6 issue.
"Most of the problems he discusses is called serotoninergic malignant syndrome and only applies to high doses of 5HTP ie 400 mg/day.
Concerning the B dosing this is basically conjecture. I have not seen any literature on this. I suspect that this would be a very individual response because the requirement for B6 can be very varied within any population."
 
Well, the fact that B6 plays a part in the activation of the decarboxylase enzyme in the liver is a FACT. Now, how significant this is may be up for a debate.
There is heated controversy over whether 5-HTP users should avoid taking vitamin B-6, or multi’s with B-6 in them, at the same time as 5-HTP (Sandyk R. 1992). Prudence suggests waiting at least 2 hours between doses and not exceed 5 mg of B6 near the time of 5-HTP use.
Taken from
http://www.lifelinknet.com/siteResources/ArchivePages/HTP-B6-Controversy.asp
and:
Vitamin B6 taken in doses of 5 milligrams or greater causes 5-HTP to be converted into serotonin before it passes into the brain. Since serotonin does not easily pass the blood-brain barrier as 5-HTP does, this effect is undesirable and can be detrimental.
taken from http://www.5-htp.net/Safety.asp
I guess that gives us a new basic thing to look out for if 5-HTP is to be used. So I guess I would now change the topic title to something like "Possible danger associated with 5-HTP" if I could.
[ 10 January 2003: Message edited by: Runner ]
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Nice work Runner.
This thread - 5-htp effectiveness is running along similar lines to this one, so avoid discussion fragmenting I've closed the other one... Here's the last two posts from it:
Originally posted by -Thoth:
My pharmacol freind on long drunken conversations is still sceptical about the entire concept of 5-HTP crossing the blood-brain barrier in the first place, although it must be conceeded there is much anecdotal evidence. He then went on to ramble about vitB6 in assisting with protien pumps and the like, at which point I realised I was somewhat out of my depth. He did, however leave me with the impression that vitb6 could play a role in more effectively allowing the serotonin precursor to cross the blood-brain barrier.
All of this however, has never been clearly demonstrated in clinical trials, and probably never will be. We make these decisions based upon logical reasoning, circumstantial evidence, and personal experience. The more you stray into specifics, the more this advice strays into the esoteric.
and...
Originally posted by BigTrancer:
Total guesswork...
Does the above imply that if you just take 5-HTP then your body can convert it safely to 5-HT using whatever B6 there is in your diet? If so, by postloading the 5-HTP with B6 by say 6-8 hours, perhaps that would replace any B6 that was depleted, but not before the 5-HTP was used up?
Not sure... I don't know nearly enough about the science.
BigTrancer :)
:)
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After reading a few new articles it does seem fairly apparent that b6 assists in the decarboxylisation process and healthy levels of vitamin b6 will lead to premature conversion to serotonin. This is going to go into the body for other functions instead of the brain where I want it.

The problem with this for me is that 5-HTP is fairly costly, so I am attempting to build up my Serotonin levels with Tryptophan as opposed to 5-HTP. High b6 levels will aid the tryptophan conversion, and are not dangerous as the additional metabolic step protects against blood serotonin overload. The problem comes when it comes time to use 5-HTP on the night to continue boosting...My incredibly unscientific hypothesis is this...if I boost my serotonin levels through tryptophan and b6, then drop my b6 levels right down (perhaps 2 days before hand) and continue on tryptophan anyway (why not...)till the day b4, THEN start dunking 5-HTP...my b6 levels will reduce in time to allow the 5-HTP to be absorbed directly to the brain as my decarboxylisation process will have slowed right down - maximum benefit from both levels.

This of course hinges on the speed at which I can reduce my b6 levels...If I have been boosting them with multivit's...how long b4 the big night am I required to stop to lower them right down again? AS an alternative to this, can I try boosting JUST my vitamin b3 levels (used to convert Tryptophan to 5-HTP) and leave the b6 levels low throughout? If my B6 levels are low on teh night...will this Significantly reduce any impact that taking 5-htp will have if i begin to come down (too slow to convert?)

Love any sugestions, thanx
 
This is taken form an old study done in mice.

The concentration of L-5-hydroxytryptophan (5-HTP) was measured in plasma and whole brain tissue from mice by use of high pressure liquid chromatography with fluorimetric detection after reaction with phthaldialdehyde. 5-HTP was injected intraperitoneally and the rise in plasma and brain 5-HTP concentrations was found directly related to the size of amino acid dose. Carbidopa, an extracerebral inhibitor of L-aromatic amino acid decarboxylation, increased dose dependently the brain bioavailability of systemically administered 5-HTP not only by peripheral enzyme inhibition, but also by inhibition of the decarboxylase activity within the blood-brain barrier as indicated by a rise in the calculated brain/plasma 5-HTP concentration ratio.

Magnussen I. Effects of carbidopa on the cerebral accumulation of exogenous L-5-hydroxytryptophan in mice. Acta Pharmacol Toxicol (Copenh). 1984 Sep;55(3):199-202

And this.

5-Hydroxytryptophan (5-HTP) is the intermediate metabolite of the essential amino acid L-tryptophan (LT) in the biosynthesis of serotonin. Intestinal absorption of 5-HTP does not require the presence of a transport molecule, and is not affected by the presence of other amino acids; therefore it may be taken with meals without reducing its effectiveness. Unlike LT, 5-HTP cannot be shunted into niacin or protein production. Therapeutic use of 5-HTP bypasses the conversion of LT into 5-HTP by the enzyme tryptophan hydroxylase, which is the rate-limiting step in the synthesis of serotonin. 5-HTP is well absorbed from an oral dose, with about 70 percent ending up in the bloodstream. It easily crosses the blood-brain barrier and effectively increases central nervous system (CNS) synthesis of serotonin. In the CNS, serotonin levels have been implicated in the regulation of sleep, depression, anxiety, aggression, appetite, temperature, sexual behaviour, and pain sensation. Therapeutic administration of 5-HTP has been shown to be effective in treating a wide variety of conditions, including depression, fibromyalgia, binge eating associated with obesity, chronic headaches, and insomnia.

Birdsall TC. 5-Hydroxytryptophan: a clinically-effective serotonin precursor. Altern Med Rev. 1998 Aug;3(4):271-80

You make up your mind but i'm sticking with the 5-HTP :D
 
My 5-htp has 20mg of vitamin B6 in it, I assure your, alot of it is going to my brain. I am one of those that can feel it. No its not a placebo either. I used to take double the amount of 5-htp without the b6, and id say, that the smaller 5-htp dose with b6, is just as effective as the larger 5-htp dose without the b6.
 
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