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The vitamin B analogue--sulbutiamine


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#1 nootropi

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Posted 14 July 2004 - 02:11 PM


Well smi2le said he is getting this in really soon, so I thought I would post some data about this rather interesting substance:

[Treatment of chronic postinfectious fatigue: randomized double-blind study of two doses of sulbutiamine (400-600 mg/day) versus placebo]

[Article in French]

Tiev KP, Cabane J, Imbert JC.

Service de medecine interne, Hopital Saint-Antoine, Paris, France.

PURPOSE: Chronic fatigue remains a medical mystery and a therapeutic failure. The subgroup of chronic fatigue postinfectious fatigue (CPIF) is an interesting one since it is quite frequent in general practice. METHODS: We studied sulbutiamine (Su), isobutyryl-thiamine disulfide in this context. We included 326 general-practice patients suffering from CPIF: they received randomly either Su, 400 mg daily (n = 106), or Su, 600 mg daily (n = 111), or placebo (n = 109) for 28 days in a double-blind, parallel-group study. 315 patients completed the study. RESULTS: The evaluation of fatigue, by multiple means including mainly MFI, a validated multidimensional fatigue scale, showed overall no significant difference between the groups. On the 7th day, however, women receiving Su, 600 mg had less fatigue (P < 0.01), but the figures were quite diverse and no persistent effect was noted at the 28th day. CONCLUSION: Thus, we showed for the first time that a high level general-practice study of fatigue is feasible using specific tools. Whether the effect observed after 1 week in women represents a true finding needs additional research. Further studies are in progress in order to characterize better the potential usefulness of Su in chronic fatigue.


Chronic administration of sulbutiamine improves long term memory formation in mice: possible cholinergic mediation.

Micheau J, Durkin TP, Destrade C, Rolland Y, Jaffard R.

Thiamine deficiency in both man and animals is known to produce memory dysfunction and cognitive disorders which have been related to an impairment of cholinergic activity. The present experiment was aimed at testing whether, inversely, chronic administration of large doses of sulbutiamine would have a facilitative effect on memory and would induce changes in central cholinergic activity. Accordingly mice received 300 mg/kg of sulbutiamine daily for 10 days. They were then submitted to an appetitive operant level press conditioning test. When compared to control subjects, sulbutiamine treated mice learned the task at the same rate in a single session but showed greatly improved performance when tested 24 hr after partial acquisition of the same task. Parallel neurochemical investigations showed that the treatment induced a slight (, 10%) but significant increase in hippocampal sodium-dependent high affinity choline uptake. The present findings and previous results suggest that sulbutiamine improves memory formation and that this behavioral effect could be mediated by an increase in hippocampal cholinergic activity.

[Facilitation of a state of wakefulness by semi-chronic treatment with sulbutiamin (Arcalion) in Macaca mulatta]

[Article in French]

Balzamo E, Vuillon-Cacciuttolo G.

Cortical electroencephalographic (EEG) activities and nycthemeral states of vigilance organization were studied in 6 adult rhesus monkeys during subchronic administration (10 days) of Sulbutiamin, a synthesized derivative of thiamine (300 mg/kg/day). Sulbutiamin induced the following modifications: (1) In the EEG activities: increase in occurrence of fast rhythms (over 28 c/sec) during waking and also during slow sleep (SS) in which their amplitude doubled. SS spindles increased in number and amplitude. (2) In vigilance organization: waking was enhanced all along the 24 h recording and SS was reorganized (particularly at night), mostly light sleep: large decrease in stage 2 duration, increase in stage 1. REM sleep duration remained stable. These changes, occurring at around day 5 of the treatment, were more pronounced on day 10 and disappeared 2-5 days after withdrawal. This study demonstrated the clear action of Sulbutiamin upon the mechanisms regulating waking and light sleep.


Hmmm...I will try it, it sounds safe...lol

Edited by adamp2p, 15 July 2004 - 06:42 AM.


#2 nootropi

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Posted 14 July 2004 - 02:17 PM

also click here for a google translated page from french

market price for it

the brand name "SERDIA"

freedom pharmacy's price

SULBUTIAMINE (Arcalion)- Described as being like hydergine only better. Facilitates wakefullness, inproves long-term memory, speeds reaction time. decreases anxiety.

PRECAUTIONS- Do not exceed 3 x 200mg tablets at any time as may cause severe headaches. Other than this has no other adverse affects.

DOSE- 2 x 200mg. tablets for 20 days.

COST- 20 X 200 mg. tablets $11



Rizzer: let me know when you get this in...I want some!

Information from the manufacturer:

Sulbutamine Details

For more than 5 years, I have labored to bring this ingredient to the US supplement market place. Finally, after a torturous path I managed to find a manufacturing partner with the necessary technical skills and entrepreneurial mindset to help me make this product a reality. The end result is that we are currently introducing this powerful nutraceutical ingredient to a select group of companies and Avastar is at the top of the list!

I first used sulbutiamine as an athlete more than a decade ago. As a professional cyclist, sulbutiamine, or Arcalion as it is sold in Europe, was something of a secret weapon for many pros. Because it is a derivative of the B Vitamin, thiamin, it is legal for all drug-tested competition including the Olympics, and after seven hours on the bike it was something that could help bring you back from the dead before the finish line.

When I retired from cycling, I’d all but forgotten about the stuff, until I hooked up with Charles Poliquin who was working with me on putting some real muscle on my puny frame. One day in passing he mentioned that used to love this stuff called Arcalion and it got me thinking.

A quick trip to the research library gave me all the information I needed to send me on the long path to bringing sulbutiamine to the US. It turns out that sulbutiamine is considered a vitamin co-factor which means it squeaks by the FDA.

While I won’t bore you with the details of how I finally got the stuff made, I will tell you why I think sulbutiamine is amazing for both strength and power athletes (from bodybuilders to professional baseball players) and endurance athletes (like cyclists).
Sulbutiamine’s Effects

Sulbutiamine has been shown to have a number of profound effects upon physical and intellectual performance, it can help alleviate depression and the fatigue commonly associated with depression, will help normalize sleep wake cycles, improve motor performance, increase maximal strength and even help improve your visual acuity.

All in all, this is a pretty impressive list. Especially since these aren’t marketing claims but clinically documented effects. Remember, like vinpocetine, sulbutiamine has been used as a pharmaceutical agent in Europe for over twenty years.

From a scientific standpoint the way that sulbutiamine works has been fairly well defined. The compound, which is a linkage of two modified thiamin nuclei, is highly lipid-soluble, facilitating rapid gut absorption and crossing of the blood-brain barrier.

By injecting animals with radio active dye it has been determined that sulbutiamine levels are highest in the reticular activating system, the limbic system and the cerebellum. Interestingly, these regions of the brain are densely packed with cholinergic and serotonergic neurons. Incidentally, neurons are often grouped by virtue of their chief neurotransmitter. It is understood that by activation of these particular groups or neurons, sulbutiamine exerts its physical and psychological effects.
Sulbutiamine in the real world

Back when I was a professional cyclist my experience with sulbutiamine was that it helped bring me back around towards the end of long races. I noticed that my focus was sharper, that my legs didn’t feel quite so dead and that my reaction time improved.

As a bodybuilder I noticed that it made me stronger in the gym and helped get me “up” for workouts when I felt a little tired on my way into the gym. Research confirms that both animals and humans given sulbutiamine perform better on a variety of both physical and mental tests, including memory, resistance to fatigue and absolute strength.

Unlike caffeine or ephedra, however, sulbutiamine is subtle. You will not feel “jacked-up” and you certainly won’t get that shaky or jittery feeling that people sometimes experience when taking stimulants. If you expect that sort of sensation, you might think that sulbutiamine isn’t working, but if you are an experienced athlete and have some method of tracking your performance such as knowing your weight for sets and reps of specific exercises you should see a reasonably dramatic improvement in your capabilities with a single dose!

That’s right! Within 30 to 45 minutes you’re performance (along with your memory and cognitive ability) will be measurably improved. The other really cool thing about sulbutiamine is that it also helps normalize sleep wake cycles which can get you back on track if you’ve been having trouble sleeping and/or do lots of traveling and thus get jet lagged from time to time.

Right now, sulbutiamine is only available in a very few products, most importantly, in two of Avastar’s formulas; Ravive and Revyte. Both products are state-of-the art energy concentration and recovery products that can help sharpen you up, increase your concentration and energy levels, improve memory, mood and athletic performance, and in the case of Ravive, even help you feel more like yourself after a hard night on the town.

Final Thoughts

Sulbutiamine is one of those ingredients that you really have to try to believe. It can have a profound effect upon your training as well as other areas of your life. If you happen to be a student, an executive or anyone under stress you will quickly see just how valuable an addition sulbutiamine will be to your supplement regimen. I wouldn’t have spent more than half a decade trying to get sulbutiamine made if it wasn’t.


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#3 ejdavis1

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Posted 15 July 2004 - 05:55 AM

Smi2le has it on his order page as of tonight 7/14

#4 nootropi

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Posted 15 July 2004 - 06:12 AM

Smi2le has it on his order page as of tonight 7/14


I called him earlier tonight and placed an order. When I get it I will report if the effects are as dramatic as they sound.

I also got my order from QHI in the UK, and I am impressed, once again, by their excellent delivery time. I mean I just placed the order 13 days ago, and I already recieved it. Considering they are in the UK, that is very impressive. As I have been recently spoiled with 2 or 3 day delivery times from smi2le, I have become accustomed to waiting longer periods of time to recieve orders from Europe; but those particular nootropics are VERY important to my stack. Although smi2le has MUCH better pricing than QHI, and he has 90% of the elements of my stack, the importance of hydergine in my stack cannot be empahsized enough.

I got:

20 X 600mg pramiracteam "Pramistar"
60 X 4.5 mg FAS Hydergine
30 2.5 mg parlodel

I have been taking the Hydergine for over four months now, and finally have been seeing the results of it in my stack. I will let you guys know what I think of Pramistar as soon as I get to test it. The parodel is bromocriptine; I plan ONLY on adding 1.25 mg per day to my stack, as I already take 4.5 mg hydergine and 5 mg nicergoline, which are both ergot derivatives. I have had excellent results from the ergots, so I thought it would be "fun" to add another.

I just placed another order from QHI for deprenyl. I only plan on taking this once or twice a week; but the reports that I have read make it sound like good stuff...

Take care everybody...if you have some free time:




check out this thread of mine at avant labs and tell me what you think, or add to it. I particularly would like to hear from others with stacks as elaborate as mine.
;)

@ ejdavis: How is it going, my friend? Thanks again for the holosync recommendation! I have been using holosync for over a month now and have started to get really good results. I mean I can feel my brain "moving in waves" as it syncronizes with the Dive and Immersion--from the awakening. I really appreciate your thoughfulness to recommend it. Oh, and I just checked smi2le also has a couple other new things...but I am pretty much only interested in the ones that enhance cognition. Are you going to order any of the sulbutiamine? If you do, please share your results in this thread.



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Edited by adamp2p, 15 July 2004 - 06:31 AM.


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Posted 15 July 2004 - 07:43 AM

This is very interesting news (especially about Sub.), I'm in the process of recompiling my nootropic stack as I've mentioned before so I should eventually be making a big order.

#6 nootropi

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Posted 15 July 2004 - 02:09 PM

This is very interesting news (especially about Sub.), I'm in the process of recompiling my nootropic stack as I've mentioned before so I should eventually be making a big order.


Cosmos: have you been able to order Hydergine yet? If not, when do you plan on it? Personally, I think it is one of the most important nootoprics I have in my stack.

#7 zencatholic

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Posted 15 July 2004 - 04:23 PM

Adam-

I've been using Holosync for about 3 months now and I think it's great. Can't wait to start Awakening Level 1 in another 3 months. Finally I can "meditate deeper than a Zen monk" [lol]

Peace be with you,
AMDG

Zen Catholic

#8 ejdavis1

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Posted 15 July 2004 - 05:43 PM

Keep in mind that Holosync can push you a little uncomfortably at times. Don't blame the product if this happens - this is just the way that it works as your brain adapts and connects up more internal communications.

Centerpointe literature addresses all of this well - but it is worth mentioning again. In my case, side effects have been minor but definitely present at times. Occasional brain fog (but -racetams and choline seem to mitigate this a lot,) a tendency to drink a lot of coffee, and a few isolated episodes of anger. I go through periods of fantastic and / or disturbing dreams. It all passes and seems to get easier to recognize and deal with as you go along. I did call their 800 counseling line a number of times, but haven't called them for almost a year for counseling now.

I usually take about two weeks off from listening during exam time. There is no harm in this because you pick up at where you left off when you resume listening.

My current level (AL2) has been pushing me a lot, and I know that L-Theanine has been a great help.

Sulbutiamine is on a rush order. The 7 week summer semester seemed like a good way to get extra coursework done but it has turned out to be especially brutal.

Edited by ejdavis1, 16 July 2004 - 12:01 AM.


#9 nootropi

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Posted 15 July 2004 - 07:33 PM

Sulbutiamine is on a rush order.  The 7 week summer semester seemed like a good way to get extra coursework done but it has turned out to be especially brutal.


You can say that again...I am taking two 5 week "quarter" classes; a mulivariable calc course and an infinite series and differential equations class as well...I have found through experience that even though I get incredibly stressed before exams, I never have problems anymore integrating concepts VERY quickly, and I attribute it mostly to my stack...and I do quite well on exams. [lol]

#10 nootropi

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Posted 17 July 2004 - 12:15 AM

Well I got my order from Rizzer today (quite quick on the delivery, as usual)...and I ingested 200 mg of sulbutiamine: and I noticed immediately its effects. It has a head warming effect as well as a motivational effect as well. Potent. Does anybody else have any experiences to share?

;)

#11 nootropi

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Posted 17 July 2004 - 12:16 AM

Keep in mind that Holosync can push you a little uncomfortably at times.  Don't blame the product if this happens - this is just the way that it works as your brain adapts and connects up more internal communications. 


To be 100% honest with you, ej, I have never had an uncomfortable feeling since I started the program.

#12 lynx

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Posted 17 July 2004 - 05:45 PM

I will soon have some sulbutiamine experiences to relate.

#13 lynx

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Posted 18 July 2004 - 07:13 PM

This looks like the most relevant study relating to sulbutiamine that I could find.

They did use straight thiamine however considered in conjuction with animal studies showing sulbutiamine increases thiamine phosphate levels in the brain this provides evidence for sulbutiamine having a nootropic like effect in healthy subjects.



Ann Neurol. 1993 Nov;34(5):724-6.

Evidence for a central cholinergic effect of high-dose thiamine.

Meador KJ, Nichols ME, Franke P, Durkin MW, Oberzan RL, Moore EE, Loring DW.

Department of Neurology, Medical College of Georgia, Augusta 30912-3280.

In vitro animal studies have suggested that thiamine is involved in the presynaptic release of acetylcholine. Total thiamine content in cholinergic nerve terminals is comparable with that of acetylcholine, and the phosphorylation state of thiamine changes with release of acetylcholine. Thiamine binds to nicotinic receptors and may exhibit anticholinesterase activity. Based on these observations, we investigated the effects of pharmacological doses of thiamine on the cognitive deficits induced by the anticholinergic scopolamine in healthy young adults using a randomized, double-blind, placebo-controlled, double-crossover design. Drug effects were assessed by P3 event-related potential, quantitated electroencephalography, and free recall memory. Conditions included (1) baseline, (2) thiamine 5 gm p.o. and scopolamine 0.007 mg/kg IM, and (3) lactose PO and scopolamine 0.007 mg/kg IM. Thiamine significantly reduced adverse effects of scopolamine on P3 latency, spectral components of electroencephalography, and memory recall. The results are consistent with a cholinomimetic effect of thiamine in the central nervous system. Additional studies are needed to delineate the basic mechanisms and possible therapeutic efficacy of thiamine at pharmacological dosages.

Publication Types:
Clinical Trial
Randomized Controlled Trial

#14 ejdavis1

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Posted 20 July 2004 - 06:14 AM

My experience with sulbutiamine so far has been disappointing and actually counter-productive. I've been taking it for three days now at a dose of 200mg twice a day, with food. Dosage is measured on a MX-50 digital scale.

I feel very active about a half hour after taking it, and feel like talking or writing. Unfortunately, I also become scatter brained and lose a lot of my verbal / written fluency. This is not a good thing for a law student. I also experience a strong "let down" about 3-4 hours after a dose. The sensation is like I need to take a nap (which I did both days on the weekend - once in the library). I'm also ravenously hungry during the let-down period, which lasts for 2-4 hours. Coffee has no effect on this. After the let-down period, I do feel pretty vital and seem to have more strength physically than usual. Since I take 2-125mg doses of centrophenoxine and 2-25mg doses of CDP choline daily, I don't think acetylcholine depletion is the problem either. I took an extra 250mg of CDP choline the other night and all it did was give me a headache in addition to the depressed feeling.

Overall, these effects are disruptive enough that I am planning on discontinuining due to approaching summer exams. I have tried going without coffee for 12 hours because one reading indicated that an acid in coffee quickly neutralizes Thiamine. I also tried eating some candy tonight on the theory that the supplement metabolizes sugar so efficiently that it was lowering my blood sugar. Whatever the case, neither one of these tactics helped.

Also, during my "up" periods, I find myself thinking and acting more confrontational. Even when argument is justified, it is a miserable experience trying to engage in debate or intelligent discussion when you can't hold a train of thought or reason clearly.

Overall I give this substance two thumbs down so far. It might be just my system (I've been a low carb eater for years - maybe that has something to do with it,) or maybe I'll adjust to it soon. Further testing will have to wait until after summer finals are over.

Edited by ejdavis1, 20 July 2004 - 06:43 AM.


#15 nootropi

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Posted 20 July 2004 - 12:20 PM

My experience with sulbutiamine so far has been disappointing and actually counter-productive. I've been taking it for three days now at a dose of 200mg twice a day, with food. Dosage is measured on a MX-50 digital scale.

I feel very active about a half hour after taking it, and feel like talking or writing. Unfortunately, I also become scatter brained and lose a lot of my verbal / written fluency. This is not a good thing for a law student. I also experience a strong "let down" about 3-4 hours after a dose. The sensation is like I need to take a nap (which I did both days on the weekend - once in the library). I'm also ravenously hungry during the let-down period, which lasts for 2-4 hours. Coffee has no effect on this. After the let-down period, I do feel pretty vital and seem to have more strength physically than usual. Since I take 2-125mg doses of centrophenoxine and 2-25mg doses of CDP choline daily, I don't think acetylcholine depletion is the problem either. I took an extra 250mg of CDP choline the other night and all it did was give me a headache in addition to the depressed feeling.


That is kind of odd, because I have not experienced any of those symptoms; and you listed quite some detail about these symptoms. I think you should completely discontinue ingesting sulbutiamine until your finals are over. It is possible that there are other elements involved. Keep us updated.

Take care,

Adam

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#16 jvalentin

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Posted 20 July 2004 - 02:55 PM

Hi ejdavis1 and all,

According to french BIAM :
http://www.biam2.org/www/Sub1310.html
Classical secondary effect are headaches and speaking troubles. The reason seems to be because it increases glutamate activity :
http://www.informedi...fiche=oui&id=18
(read "Pr Michael SPEDDING (Intervenant)" (in french).
You may be overdosing. 200mg (or even lower) shared in 3 times over the day would probably be better. With that dosage you may increase memory on the long term but perhaps notice no mood effect. That doesn't mean it's useless.

Does anybody nows if sulbutiamine is a fat version of B1 like benfotiamine or a liquid form like classic B1 ? i take 150mg/ day benfotiamine and classic B1 too but it has no effect on mood.

I am french and post for the first time on this intersting forum.

Jacques




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