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Sublingual Deprenyl


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#1 Guest_da_sense_*

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Posted 31 July 2005 - 02:36 PM


Since i'm taking 5mg tablets of deprenyl daily i thought why not try it sublingualy? I let it dissolved under my tongue, and now i almost can't feel my tongue, it's like anesthetic!
Ok it's back to normal now, but for few mins it felt like i got a anesthetic shot at my tongue ;)

Does anyone knows if taking deprenyl tablets sublingual increases bioavailability? (I know that taking it with food does)

Edited by da_sense, 01 August 2005 - 04:22 PM.


#2 vastman

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Posted 01 August 2005 - 08:15 AM

da sense...

switch to the liquid form... it lasts longer and it is the "sublingual" form you are searching for. You use a dropper and drop drops (ha ha) under the tounge which is absorbed directly into the bloodstream.

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#3 Guest_da_sense_*

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Posted 01 August 2005 - 04:21 PM

I still have some selepryl left, saving it for dark days ;) Liquid has 300mg versus 250mg in a box of tablets, but still price for tablet is much lower than liquid, plus i haven't noticed any difference between tablet and liquid in terms of effects.

#4 vastman

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Posted 02 August 2005 - 06:57 AM

I don't know if it's been discussed, but I generally prefer the sublingual/muscual formulations as they go directly into the bloodstream, thus reaching their target without the normal losses associated with digestion. I presume that this is true with Deprenyl also but don't know for sure.... if so, not only is it easier to titrate your dose but more gets to where it needs to go.... Thus, while on the surface the tabs are a bit cheaper, I presume the cost per unit actually delivered is more...

Hopefully someone much wiser than me knows if this is true.... LifeMirage?

#5 poser

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Posted 05 September 2006 - 09:05 AM

I have tried to crush the pill to get better absorption (orally they haven't really worked for me...). I don't know if it's placebo but now that I held it in my mouth for 60 minutes (that may be overkill I admit), I am sure there was a difference between having it in your mouth for 10-15 minutes. Like really big difference. There was at 60 minutes no more acid in my mouth, which I take for an indicator as well.

I will try the citrate form anyway but would like to hear if you have find out what works with the pills.

#6 Guest_aidanpryde_*

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Posted 19 September 2006 - 10:54 AM

It has nothing to do with a placebo, studies done with "Zydis Selegiline" a fast dissolving form of SelegilineHCL for buccal absorption, show that this form enabled a higher absorption, higher then the usual with selegeline tablets. (1)
You also don`t have to let it for a such long time in your mouth, it seems to get pretty fast absorbed.
But you should not forget, that by partially bypassing the first pass metabolism you also reduce the amount of the selegiline metabolites, especially one of them (l-amphetamine) is probably important for the cognitive enhancement effect of selegiline. Look at the measurements of the metabolite plasma concentration, there is a significant difference.
So by changing the administration route you change the metabolic one and so the effect of this drug.
Perhaps this method would be interesting for a higher dosage and so a nonselective inhibition of MAO, for the treatment of depression, but avoiding problems accuring with tyramine by avoiding the first pass, it would be similar to the patch administrated selegiline.

(1)
Clarke A, Brewer F, Johnson ES, Mallard N, Hartig F, Taylor S, Corn TH.
A new formulation of selegiline: improved bioavailability and selectivity for MAO-B inhibition.
J Neural Transm. 2003 Nov;110(11):1241-55.

or

A new formulation of selegiline: improved bioavailability and selectivity for MAO-B inhibition.

    * Clarke A,
    * Brewer F,
    * Johnson ES,
    * Mallard N,
    * Hartig F,
    * Taylor S,
    * Corn TH.

Scherer DDS, Swindon, United Kingdom. aclarke@cephalon.com

Seven randomised comparative studies were conducted in healthy volunteers to compare the pharmacokinetic and pharmacodynamic profiles of selegiline hydrochloride in a new formulation designed for buccal absorption "Zydis Selegiline" (1.25-10 mg) with conventional selegiline hydrochloride tablets "conventional selegiline tablets" (10 mg). A total of 156 healthy volunteers participated in these studies. Plasma concentrations of selegiline and its primary metabolites, N-desmethylselegiline (DMS), l-amphetamine (AMT), and l-methamphetamine (MET) were measured using Gas Chromatography Mass Spectrometry (GCMS) and gas liquid chromatography (GLC) assays. Inhibition of monoamine-oxidase type B (MAO-B) and monoamine oxidase type A (MAO-A) activity was determined by measurement of as beta-phenylethylamine (PEA) by GCMS and 5-hydroxyindoleacetic acid (5-HIAA) by High Performance Liquid Chromatography (HPLC) assays. Almost a third (2.96 mg) of a 10 mg selegiline dose in Zydis Selegiline was absorbed pre-gastrically (predominantly buccally) within 1 minute. Mean [SD] area-under-the curve (AUC(0- infinity)) values following Zydis Selegiline 10 mg (5.85 [7.31] ng.h/mL) were approximately five times higher than those following conventional selegiline tablets 10 mg (1.16 [1.05] ng.h/mL). In contrast, plasma concentrations of metabolites were significantly ( p<0.001) lower following Zydis Selegiline 10 mg than following conventional selegiline tablets 10 mg. Plasma concentrations of selegiline and its metabolites increased in a dose-dependent manner over the dose-range Zydis Selegiline 1.25-5 mg. Bioavailability was determined using AUC and peak plasma concentrations (C(max)). The C(max) of selegiline was similar following administration of Zydis Selegiline 1.25 mg (1.52 ng/mL) or conventional selegiline tablets 10 mg (1.14 mg/mL). The range of values for AUC(0- infinity) and C(max) following Zydis Selegiline 1.25 mg were entirely contained within the range following conventional selegiline tablets 10 mg, with a much higher variability of plasma selegiline concentrations occurring after conventional selegiline tablets than after Zydis Selegiline. As expected, peak plasma concentrations for DMS, AMT and MET were consistently lower after Zydis Selegiline 1.25 mg (1.19, 0.34, 0.93 ng/ml, respectively) than after conventional selegiline tablets 10 mg (18.37, 3.60, 12.92 ng/ml, respectively). A significant (r=0.0001) correlation between daily PEA excretion (a measure of brain MAO-B inhibition) and the log-transformed AUC((0-t)) for selegiline was demonstrated. Mean daily PEA excretion was similar following Zydis Selegiline 1.25 mg and conventional selegiline tablets 10 mg (13.0 microg versus 17.6 microg). In contrast, there was no correlation between PEA excretion and selegiline metabolites, indicating that selegiline metabolites do not significantly inhibit MAO-B. Urinary excretion of 5-HIAA (used as a marker for MAO-A inhibition) was unrelated to plasma concentrations of selegiline or DMS following single or repeat dosing of Zydis Selegiline 1.25 mg or conventional selegiline tablets 10 mg. However, comparison of treatment groups revealed a significantly lower excretion of 5-HIAA in the conventional selegiline tablets 10 mg group than in the Zydis Selegiline 1.25 mg group after repeated administration over 13 days. In summary, by reducing the opportunity for first-pass metabolism, the absorption of selegiline from Zydis Selegiline was more efficient and less variable than from conventional selegiline tablets. Compared with conventional selegiline tablets 10 mg, Zydis Selegiline 1.25 mg yielded similar plasma concentrations of selegiline and degree of MAO-B inhibition, but markedly reduced concentrations of the principal metabolites. Thus, the lower but equally MAO-B inhibitory dose of selegiline in Zydis Selegiline 1.25 mg, which is associated with lower concentrations of potentially harmful metabolites, could offer a safer and more predictable treatment in the management of patients with Parkinson's disease.



#7 poser

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Posted 24 September 2006 - 07:38 PM

I don't know about l-amphetamine but d-methylselegiline is the metabolite that there's about 10 times more than the others and that has been said to be of benefit for ADHD, somewhere.

On the other hand, what was peculiar about that study was that the 10 mg Zydis swallowed produced 3 times as much b-PEA, which is a marker for MAO-B inhibition and production of dopamine, than 10 mg of oral Eldepryl. I don't know how that is possible, unless there was something different in the content of the pill - but there isn't. So I think that's some kind of error. If it was true, that would that mean MAO-A inhibition would begin at or over 30 mgs. 20-30 mg is more likely though some may have other offsets.

I am testing a transdermal gel I have made myself. It lacks several components but I would say it already beats the sublingual in both effects and bioavailability.

The sublingual has a clear high after which the effects wane too much. TD 'grows on you' and lasts a lot longer and overall packs more punch.

#8 Guest_aidanpryde_*

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Posted 27 September 2006 - 10:36 PM

Just for information:
One should not make the mistake and mix up the l-amphetamines derived from selegiline with the usual d-amphetamines, used by peoples in order to dance the whole night.
As you said, the desmethylselegiline (DMS) ist the most occuring metabolite, but as you can also see here, METH is the second one and the concentration it occurs in, is not really far away from the DMS. As you can see in the following study dealing with selegiline and L-amphetamine, both substances were equal in in cognitive enhancement.

Chronic L-deprenyl or L-amphetamine: equal cognitive enhancement, unequal MAO inhibition.

    * Gelowitz DL,
    * Richardson JS,
    * Wishart TB,
    * Yu PH,
    * Lai CT.

Department of Psychology, University of Saskatchewan, Saskatoon, Canada.

The effect of chronic (4 month), subcutaneous injections of saline, L-deprenyl (0.25 mg/kg), or L-amphetamine (0.25 mg/kg) on the acquisition of a learned spatial habit in a modified Morris Water Maze was investigated in middle aged rats. Injections, given three times weekly starting at 6 months of age, were continued during behavioral testing, which occurred at 10 months of age. The cognitive performance of the middle aged rats was compared to that of 2-month-old control rats. Twenty-four hours after the last behavioral test, the rats were sacrificed and their brains were removed, dissected, and frozen in liquid nitrogen. The activities of MAO-A and MAO-B in the lateral cortex were determined. Results indicate that rats in the L-deprenyl group, the L-amphetamine group, and the young control group all learned the water maze task equally rapidly and significantly faster than rats in the saline group. MAO-A did not differ among the saline, amphetamine, and young control rats, but MAO-B was significantly higher in the middle aged saline and L-amphetamine rats than in the young controls. Both MAO-A and MAO-B activities were significantly lower in the L-deprenyl group than in the other three groups. This indicates that low-dose L-deprenyl can also inhibit MAO-A following chronic SC administration. Moreover, the improved cognitive performance produced by L-deprenyl may not be due to its ability to inhibit MAO-B, but rather to some other effect such as the activation of growth factors.


The Zydis selegiline may be interesting for clear MAO-B inhibiting purposes and nothing else, the bioavailibilty seems to raise extremly when the selegiline has not to pass the gut and liver. Very nice how in this case the pharmacokinetics mix with the pharmacodynamics and perhaps it is not suprising to see such huge differences in the effect one can reach with this different application forms. Look at the EMSAM patch, it delivers not more than (6mg,9mg )12mg/24h and reaches a non-selective MAO inhibition.
Very nice to read: http://www.bms.com/c...SEQ=112&key=PPI
But the question remains if the buccal, sublingual application is also effective for use as a nootropic.
For which purpose do you use selegiline and your self created patch?

I don`t know if selegiline is really enhancing my cognition, I have used 5mg daily for about 3 months and have a break now. There was a clear difference in using it sublingual/buccal or just swallowing the tab. Here in Germany we are not really so far with the whole nootropic stuff, much more sceptic and the people are very cautious in experiments with medicals. Mostly students are interested in this issue, in order to pass exams and so on. As I was screening the most boards, studies and so on, selegiline seemed to be that "magic pill" although it is usually not called nootropic. Something I can`t understand is the attitude in the community to call any drug nootropic, just because one or two studies say it would be neuroprotective, would raise the content of some neurotransmitter and so on. Also I can`t really understand the logics behind some of the unbelieveable NTcombinations I have read here and on other boards. So I question myself is there a scientific background for using them or just "Ooh let me see this drug sounds nice, and this one also, I will throw everything in the bowl and let it cook." Do you have any effects with selegiline which you could describe as an improvement in your cognition?

Now I am looking further for something else. Perhaps some natural alternatives, like celastrus paniculatus and so on although I am not really a friend of using extracts with unknown compounds and their quantity in the extract. Sorry for my bad english, haven`t wrote for a whole while. :)

Edited by aidanpryde, 28 September 2006 - 06:21 AM.


#9 Mixter

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Posted 30 September 2006 - 10:33 AM

Btw, there are many things you shouldn't chew, take sublingually or keep in
mouth that are otherwise no problem. Most common criteria is a very low or high pH.

Every dentist knows that chewing aspirin half a dozen times might irrevocably
damage your teeth, doing it regularly would definitely do that... take care...
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#10 poser

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Posted 01 October 2006 - 01:21 PM

I hope tol get back to the pharma chat soon but this first.

Selegiline HCL is a weak base.

With citric acid, it may have a lower PH but maybe not.

Nothing that a dose of xylitol couldn't tackle, no?

Also, now I don't recommend keeping it longer in your mouth than 1-5 minutes (WITHOUT SWALLOWING). I just spit out the remainder, microwave it for 100 seconds and put it back in - repeat until nothing remains.

A bit gross, but probably saves me money.

edit: I stopped doing it - can't be bothered. Now trying to add an effervescent mix to increase the absorption and then swallow.

Edited by poser, 03 October 2006 - 11:29 PM.


#11 poser

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Posted 03 October 2006 - 11:26 PM

As you said, the desmethylselegiline (DMS) ist the most occuring metabolite, but as you can also see here, METH is the second one and the concentration it occurs in, is not really far away from the DMS. As you can see in the following study dealing with selegiline and L-amphetamine, both substances were equal in in cognitive enhancement.

Very interesting abstract. I get lost though; why is the conclusion that the cognitive enhancement of deprenyl is not from MAO-B inhibition? I see no data that would warrant that.

But the question remains if the buccal, sublingual application is also effective for use as a nootropic.
For which purpose do you use selegiline and your self created patch?

Quantifying nootropic properties is beyond me, too subtle (and I do too many other things to attribute effects to one drug); I was looking for something to get me going (for depression). It does that. Though I admit methylphenidate complemented it nicely.

Something I can`t understand is the attitude in the community to call any drug nootropic, just because one or two studies say it would be neuroprotective, would raise the content of some neurotransmitter and so on.[ Also I can`t really understand the logics behind some of the unbelieveable NTcombinations I have read here and on other boards. So I question myself is there a scientific background for using them or just "Ooh let me see this drug sounds nice, and this one also, I will throw everything in the bowl and let it cook." Do you have any effects with selegiline which you could describe as an improvement in your cognition?

It's like a kid in a candy store. But people often 'grow up' after putting a lot of money in them and cut down.

Now I am looking further for something else. Perhaps some natural alternatives, like celastrus paniculatus and so on although I am not really a friend of using extracts with unknown compounds and their quantity in the extract. Sorry for my bad english, haven`t wrote for a whole while. :)

Personally, when I see the word 'Ayurvedic', I tend to put extra-strong filters on. But who knows, maybe the magic herb can be found...

#12 Guest_aidanpryde_*

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Posted 17 October 2006 - 10:23 PM

Sorry had no time for posting because of the university (starting med. biotech) took up a lot of my time, although I read from time to time some of the new threads here.
I have some selegiline here but I have stopped taking it, the nootropic effect was dimnished after a while, I often feeled really buzzed out and upside down. If I should try it ever once again, I would stick much more to an another dosing schedule, perhaps just some mgs every second or third day.

Very interesting abstract. I get lost though; why is the conclusion that the cognitive enhancement of deprenyl is not from MAO-B inhibition? I see no data that would warrant that.


Me too, I guess the complete study contains much more data which could affirm they hypothesis. Or perhaps they thought simple in the following way:

selegiline is converted to L-amphetamine - L-amphetamine alone produces a similar effect in relation to the cognitive enhancement like selegiline, but it does not lower MAO - the cognitive enh. does not need lowered MAO - selegiline could do this through his amphetamine metabolite or other factors

I have to go to bed soon, so I can`t look for some more studies, but I also do believe that this effects of selegiline are much more caused through other factors than through MAO inhibition alone.

Personally, when I see the word 'Ayurvedic', I tend to put extra-strong filters on. But who knows, maybe the magic herb can be found...


I share your opinion, I am also very sceptic with this kind of medicine. The problem with natural products, is of course that you have often a wide spectrum of different active agents inside such a herb. So you have to take all of them, although perhaps just some of them are really interesting and some other might be also contraproductive. Then there is the issue with the purity, respective the percental of the active agents in the extract you use.

I have used celastrus paniculatus, but this is a little bit to strong for me, just some drops of the seedoil produce a strong effect.
It`s not easy to describe, it goes as first in the euphoric direction, awakened mind, not caffeinelike but in this direction, strong energyboost.
It clearly does manipulate some neurotransmitter.

Effects of Celastrus paniculatus on passive avoidance performance and biogenic amine turnover in albino rats.

Nalini K, Karanth KS, Rao A, Aroor AR.

Department of Clinical Biochemistry and Nutrition, Kasturba Medical College, Karnataka, India.

The effects of an indigenous drug, Celastrus oil, extracted from the seeds of Celastrus paniculatus on learning and memory in a two compartment passive avoidance task was studied in albino rats. The effects on the contents of norepinephrine (NE), dopamine (DA) and serotonin (5-HT) in the brain and on the levels of their metabolites both in the brain and urine were also assessed. Significant improvement was observed in the retention ability of the drug treated rats compared with the saline administered controls. The contents of NE, DA and 5-HT and their metabolites in the brain were significantly decreased in the drug treated group. The urinary metabolite levels were also significantly decreased except for total 3-methoxy-4-hydroxyphenyl glycol. These data indicate that Celastrus oil causes an overall decrease in the turnover of all the three central monoamines and implicate the involvement of these aminergic systems in the learning and memory process.


Now I have sticked to rhodiola rosea and it is simply great, exactly that I was searching for.
As I said I read some of the new threads here and I would not say that rhodiola is just a hype. Now I am using it together with L-carnitine, piracetam and some lecithine.
It works great for me, so if I should try something new it would only be huperzine A.
I tried the piracetam much more for the reason to demonstrate myself that it is totaly worthless, so I could mark it as non effective and try other products. But I must confess, that I will try it a little bit longer now, yes I am surprized. ;)
Now this is going to be offtopic, so I stop now and will take part in other discussions later.

#13 rsnuk

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Posted 13 September 2007 - 10:17 PM

Lolol, i've just realised, all you life extensionalist got lead astray by pharmaceutical influence.

You thought that the fake selegeline they created could extend life or have positve effects, even though it metabolises into amphetamines, methamphetamine,

Also you don't seem to realise amphetamines and psychiatric drugs are majoritively neurotoxic and will shorten you life spans.

Selegeline citrate developed by Dr. Kimbal in the early 90's will extend your life span and improve your conitive function more effectively than methamphetamine or amphetamines, but big pharma and the FDA surpressed it.

So now if you really want to improve your mental ability and lifespan, you need selegeline citrate, that's the compound the life extensialist movement wents nuts for in the 90's not the toxic crap the drug companies are making today...

Lol.
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#14 luv2increase

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Posted 14 September 2007 - 01:59 AM

Lolol, i've just realised, all you life extensionalist got lead astray by pharmaceutical influence.

You thought that the fake selegeline they created could extend life or have positve effects, even though it metabolises into amphetamines, methamphetamine,

Also you don't seem to realise amphetamines and psychiatric drugs are majoritively neurotoxic and will shorten you life spans.

Selegeline citrate developed by Dr. Kimbal in the early 90's will extend your life span and improve your conitive function more effectively than methamphetamine or amphetamines, but big pharma and the FDA surpressed it.

So now if you really want to improve your mental ability and lifespan, you need selegeline citrate, that's the compound the life extensialist movement wents nuts for in the 90's not the toxic crap the drug companies are making today...

Lol.



rsnuk, I kinda felt a little sorry for you at first, but I'm having second thoughts now.


You do realize that there is a difference between L-amphetamine and D-amphetamine right? It is apparent that you don't. Also, the metabolites that deprenyl turn into is such a small small amount that it is harmless, even if it were D-amphetamine. Let's see. 1-2.5mg of deprenyl everday (good if you are under 40---MAYBE) would turn into, who knows, like .005mg of L-amphetamine??? This is what, 1/1000 a dose of 10mg (not doing the math---typing quit) of adderall pill. Plus, it is the weaker L-amphetamine and not the D-amphetamine like the adderall.

Concluding from this, you need to shut your trap sonny. You don't know what you are talking about.
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#15 shamus

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Posted 14 September 2007 - 07:32 AM

Haha.

While I agree with you luv2increase, isn't levo-amphetamine more neurotoxic than dextro-amphetamine?


+ shouldn't we be referring to 'the metabolite' as levo-methamphetamine as that's what it is? Even more neurotoxic again?

#16 rsnuk

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Posted 14 September 2007 - 10:27 AM

Did you even read what i said?

There are two kinds of selegeline:

1 is pharma poisonous amphetamine

2 is an extract from the ephedra plant

Number one will shorten your live span like all amphetamines

Number two has potensial to porlong it, along with mental function

Did you not understand what i said in other thread, about Dr. Kimballs discoverey and imprisonment?
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#17 toza

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Posted 10 November 2008 - 11:41 PM

Hello,

this site(http://www.liquid-deprenyl.com) claims that Cyto Pharma's Cyprenil and Selepryl:

are the exact same liquid Selegiline Hydrochloride product, highly contaminated with amphetamine and methamphetamine, more so than any other Deprenyl on the market. Cyto Pharma calls their products "Deprenyl Liquid, Selegiline Citrate," scrambling the words "Liquid Deprenyl Citrate" and "Selegiline Citrate." It is beyond fraudulent for a company to deceive consumers and make them believe they are selling another company's brand name product. It is also fraudulent for Cyto Pharma to call their products "Selegiline Citrate", as their product has a TOTALLY different structure then the chemical entity Selegiline Citrate.


Is it true? Should I be worried about ordering Cyto Pharma's Cyprenil or Selepryl or are the information on that site false?

thanks...

#18 luv2increase

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Posted 15 November 2008 - 06:48 PM

Hmmm... cytopharma is an actual pharmaceutical company, and this site looks like they are selling some tintured herbal extract. They post no sources or chemical analysis for their horrible, unbased claims. It is simply one company trying to smear another company. I along with others have taken cytopharma's cyprenil with great results. Don't listen to everything you hear. I would bet that this company may be getting sued sometime soon too.

BTW, this company must be brand-new because I've never heard of them before, and I've been looking and researching this stuff prenty intensively for the last 2-3 years.


cyprenil for the win!

Edited by luv2increase, 15 November 2008 - 06:49 PM.


#19 SvenKr01

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Posted 23 November 2008 - 11:58 PM

Hmmm... cytopharma is an actual pharmaceutical company, and this site looks like they are selling some tintured herbal extract. They post no sources or chemical analysis for their horrible, unbased claims. It is simply one company trying to smear another company. I along with others have taken cytopharma's cyprenil with great results. Don't listen to everything you hear. I would bet that this company may be getting sued sometime soon too.

BTW, this company must be brand-new because I've never heard of them before, and I've been looking and researching this stuff prenty intensively for the last 2-3 years.


cyprenil for the win!


No, this company seems not to be brand new (they existed before 2000, if one can trust the web..).
There are several references to them on the web, also by some doctors, saying that they had better results
with Discovery´s product than with other companies product (cant find the link now).
However, the web site from IAS has some more information on this: http://www.antiaging...mballletter.htm
Also some google searches with "liquid deprenyl" or "liquid deprenyl FDA" gives interesting results.
I am also interested in trying deprenyl and searched the web a lot about it (and found beside other things, DEDI and the strange remarks
about the other companies producing it ... and this post here)
CytoPharma seems to be localized in Mexiko and NatuPharma in Brazil.

I am now quite unsure about what to think about all this information.

#20 owtsgmi

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Posted 26 October 2010 - 04:53 AM

No replies?

Where do you order your liquid deprenyl from? Are there diiferent forms of 'liquid deprenyl' on the market?



I was researching this recently and came across these articles:

http://www.antiaging...73/deprenyl.htm
http://www.antiaging...yl-selepryl.htm
http://www.liquid-deprenyl.com/

From the second link:
"Liquid Deprenyl Citrate works by naturally restoring balance to at least 4 vital neurotransmitters, most notably dopamine"

"Selegiline and Selegiline Hcl. are 2 different chemical entities. When you search "Selegiline", the information you pull up is not for Selegiline, it's for Selegiline Hydrochloride"

My take is this:
What is on the market now selling as "Selegiline" (e.g., Jumex) is actually Selegiline HCL.

The "old" Selegiline (Selegiline Citrate, also called Liquid Deprenyl Citrate) is claimed to be an amazing anti-aging supplement and dopamine agonist. The "new" Selegiline (Selegiline HCL) has limited value.

Selegiline Citrate is not sold anymore because the FDA banned it. The makers of the HCL version seemed to have co-opted the great reputation of the Citrate version.

There seem to be a lot of conspiracy theories related to the whole subject. Personally, I would try Selegiline Citrate if it were still available, but I wouldn't try Selegiline HCL.

#21 chrono

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Posted 26 October 2010 - 06:37 AM

The "new" Selegiline (Selegiline HCL) has limited value.

The makers of the HCL version seemed to have co-opted the great reputation of the Citrate version.

Deprenyl was around commercially for about 10 years before Jay Kimball started marketing the citrate version. Essentially the entire body of literature refers to either the freebase or HCl versions, while the citrate is only supported by the claims of the manufacturer.

The claims made by the LDC companies on those websites are frankly ridiculous: "Selegiline Hcl. has a completely different chemical structure and totally different properties. It is indisputable, as any knowledgeable scientist is aware, that Selegiline and Selegiline Hcl. are 2 completely different chemical entities, regardless of their names." 'Completely different' is an absolutely incorrect thing to say here. The only difference is that the selegiline molecule either has an HCl group stuck on it, or it doesn't. And it's not a conspiracy that the name is used interchangeably with the HCl salt; how often do you use the name of the salt when buying a drug at the pharmacy? The citrate salt is probably more like the HCl salt (which they demonize) than the freebase. They say that the pharmaceutical HCl salt is "impure selegiline fused with hydrochloric acid," while their LDC product is "stabilized" with citrate (it's precisely the same salting process). Hilarious, and transparent.

The citrate may have better pharmacokinetics if it can be absorbed sublingually—but there's a hydrochloride version designed for buccal absorption, as well. However, I would be very surprised if the salt form makes any kind of difference by the time it gets to the brain. And the preponderance of evidence is certainly not in favor of the citrate, as you suggest; searching for deprenyl/selegiline citrate on pubmed returns 0 results, against the 2900 for the normal version (either the freebase or HCl). And I'm pretty sure that the unnamed studies they refer to which show benefits of deprenyl (esp. lifespan) employed either the freebase or the HCl. There is nothing special about a citrate salt that privileges it to inherit the qualities of the freebase molecule, that would not hold equally true for a hydrochloride.

If anything, Jay Kimball "co-opted" the body of thousands of research papers making the drug what it was, and made unsubstantiated claims about the complete superiority of a slightly different version that he could bring to market. It's sad that he got screwed over by the FDA. But speaking for myself, I would never buy from a company that throws up such a smokescreen of misinformation to try to create a market for itself, and I'd suggest a little more skepticism when reading unreferenced claims made by drug marketeers.

Edited by chrono, 11 October 2011 - 12:49 PM.

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#22 chrono

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Posted 26 October 2010 - 09:30 AM

A little more relevant info, from an old CERI newsletter:

It is equally unwarranted to assume, as the Discovery brochure implies, that only the hydrochloride form of selegiline is somehow responsible for this increased mortality. Their specious assertion that “selegiline” and “selegiline hydrochloride” are “different chemical entities” hardly justifies their implication that the increased mortality in the PDRG study is only attributable to the selegiline hydrochloride and not selegiline (or selegiline citrate). The possibility that the hydrochloric acid salt of selegiline has special toxicity is unsupported by any evidence, real or theoretical. It’s a good thing; the natural hydrochloric acid in the human stomach converts selegiline and selegiline citrate into selegiline hydrochloride. Furthermore, selegiline hydrochloride tablets are now being compounded with citric acid, which converts some selegiline hydrochloride into selegiline citrate in the GI tract.

As the Discovery brochure correctly states, the real issues about deprenyl are about “efficacy, purity and side effects.” There are genuine differences in efficacy between the high-purity Discovery-brand liquid deprenyl citrate and standard pharmaceutical deprenyl hydrochloride products. These differences are real, and they are not explained by the specific ion — chloride or citrate — which happens to accompany the selegiline molecule. It’s my considered opinion that it will turn out to be a toxic impurity in the commercial deprenyl products that is not present in the Discovery liquid deprenyl due to 1) superior quality control in their manufacturing process, or 2) some degree of chemical instability of deprenyl in its crystalline solid form. We may never know for sure.


Note that CERI was recommending the LDC product at the time, and still considered the product description "specious." I'm curious about the source of the assertion about "genuine differences in efficacy." Regarding the speculation (and DEDI's flat-out assertion) of impurities in pharmaceutical DPR, keep in mind that this was written 12 years ago. A higher degree of purity might be a good reason to buy a certain product...assuming there's a good reason for believing it's true.

Edited by chrono, 27 October 2010 - 07:08 AM.

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#23 longevitynow

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Posted 27 October 2010 - 04:19 AM

I've only had good experiences with Selepryl and Cyprenil, and prefer them to selegiline hcl tabs, but maybe only because it is easy to take the liquid deprenyl sublingually and doesn't taste as bad as the tabs sublingually. Anyone ordered and received liquid selegiline lately? If so, where?

#24 owtsgmi

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Posted 28 October 2010 - 04:39 AM

I admit I am not an expert, so it's great to get your take on this. I have read all the claims and controversy, Googled profusely and still could not come to a conclusion on this. And, online research is something I do in my job every day, so I am not a novice at it. In a way, I am somewhat relieved that the DEDI claims about selegiline citrate as a unique substance may be wrong or overblown, simply because it means that there is not a wonder dopaminergic drug out there that is being kept secret. I am not a scientist, so I will humbly agree to your assertion that the chloride vs. citrate argument is moot.
However, this part is intriguing:

As the Discovery brochure correctly states, the real issues about deprenyl are about “efficacy, purity and side effects.” There are genuine differences in efficacy between the high-purity Discovery-brand liquid deprenyl citrate and standard pharmaceutical deprenyl hydrochloride products. These differences are real, and they are not explained by the specific ion — chloride or citrate — which happens to accompany the selegiline molecule. It’s my considered opinion that it will turn out to be a toxic impurity in the commercial deprenyl products that is not present in the Discovery liquid deprenyl due to 1) superior quality control in their manufacturing process, or 2) some degree of chemical instability of deprenyl in its crystalline solid form. We may never know for sure.


This implies that the selegiline citrate version could be more effective, and thus could have completely different effects. But, you make a good point...

Regarding the speculation (and DEDI's flat-out assertion) of impurities in pharmaceutical DPR, keep in mind that this was written 12 years ago. A higher degree of purity might be a good reason to buy a certain product...assuming there's a good reason for believing it's true.


So bottom line, there is no reason to believe DEDI's marketing claims about selegiline citrate. And, there is no reason not to believe them.

#25 tjcbs

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Posted 28 October 2010 - 06:21 PM

Didn't Discovery extract their's from an herb? If so, then doesn't it seem plausible that theirs is in fact chemically distinct, regardless of the fact that they labeled it "segeline citrate"? Did anyone actually analyze this molecule?

#26 tham

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Posted 29 November 2010 - 10:46 AM

Annetta Freeman swears by Discovery's
liquid deprenyl citrate as the main force
behind her regimen in saving her from the
ravages of Parkinson's, after she found
Eldepryl tablets uselss.

http://www.ceri.com/annett4.htm


" Eldepryl, which is prescribed to persons
with Parkinson's disease, was found in
1990 to contain methamphetamine and a
publicly unidentified neurotoxin by the U.S.
Pharmocological Conference. The 1998
Physician's Desk Reference supports claims
made by Eldepryl users that use of the drug
causes side effects which include severe
body pains, nausea, vomiting, hallucinations,
anxiety, confusion and clinical depression.
Aside from no real evidence that Eldepryl
helps to reverse the ravages of Parkinson's
disease, Parkinson's advocate Annetta
Freeman believes that use of the drug as
prescribed has resulted in the death of
several victims of the degenerative disease. "

" To the contrary, the court and the FDA
have been flooded with hundreds of
people who have experienced a
reversal of their symptoms, without
adverse side effects, once they stopped
using Eldepryl and began using LDC. "

" Ranking FDA Criminal Invistigations
Division official Don Liggett, who has
been party to his agency's persecution
of DEDI since 1990, admitted that he is
not aware of even one reported adverse
reaction to LDC, nor was his agency's
$multi-million investigation of Kimball
prompted by a consumer complaint. "

" The Tampa Tribune's story "'Youth'
peddler receives 13 years," which was
published Oct. 20, ignored court
documents, clinical studies, science
and truth to fool the public into believing
government persecution of Kimball was
a justified conclusion to a decade-long
attempt to block public access to LDC. "

http://www.prolibert...er/20001104.htm

http://www.mail-arch...m/msg55051.html


" Annetta Freeman of Hollywood, California,
was a Parkinson's victim confined to a
wheelchair who was continuing to deteriorate
while using Eldepryl. She got off Eldepryl and
began taking Liquid Deprenyl Citrate (LDC),
a clean selegeline developed by Jay Kimball
of Discovery Experimental and Development,
Inc. (DEDI). Today Freeman, 64, is leading an
active and productive life as an advocate for
Parkinson's victims and LDC. Unfortunately,
the result of a 10-year conspiracy that involved
Somerset Pharmaceuticals, the FDA and the
U.S. Department of Justice (DOJ), LDC is
temporarily unavailable in the U.S. The FDA
has admitted that there has never been, after
thousands of applications, even one reported
incident of LDC harming people. The FDA has
admitted that there has never been one reported
consumer complaint about LDC. Thousands of
LDC users who have had quality of life restored
to them have been denied access to the natural
and comparatively inexpensive nutritive plant
product that controlled their Parkinson's
symptoms. "

http://www.pl.net/9.3health/fox.html


" According to FDA Office of Criminal
Investigations spokesman Don Liggett,
the FDA's 10-year, multi-million-dollar
persecution of Jay Kimball is purely
administrative
. Liggett admits that
the FDA has never received one complaint
over LDC, nor is the FDA aware of LDC
ever causing an adverse reaction. "

" The FDA can determine whether or not
it has the authority to regulate a product
based upon the intent of the user, not
the product itself
. In other words, if
you drink carrot juice because it tastes
good, it is not a drug. But, if you drink
carrot juice because you believe it cures
cancer, carrot juice, according to the logic
of the FDA, is a drug to be placed under its
regulatory authority. "

http://www.lafayette...20Treatment.htm


" DEDI customer Annetta Freeman, who
attributes her nearly complete recovery
from Parkinson's to LDC, received such
a letter dated February 17, 1995, from
Somerset Attorney Arthur J. Mahoney
from Gunster, Yoakley, Valdes-Fauli &
Stewart of Stuart, Florida, warning her to
immediately discontinue using LDC. "

http://www.raven1.net/jaykimbl.htm


" Somerset Lawyers Threaten
Liquid-Deprenyl Users. "

http://www.ceri.com/editoria.htm


" The liquid deprenyl does one other
thing that just bowls me over every
time I hear about it; it clears up senility
within days. I know an elderly actress
who had Parkinson's and was also
getting quite senile. Within 3 days of
starting liquid deprenyl citrate, her
senility totally lifted. "

" Then the FDA appended copies of letters
from Discovery asking for ID numbers so
that it appears like Discovery is the one
responsible for the contamination. "

http://www.ceri.com/annetta.htm

http://www.ceri.com/parkpage.htm

Edited by tham, 29 November 2010 - 10:53 AM.

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#27 longevitynow

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Posted 29 November 2010 - 12:19 PM

Missing my liquid deprenyl (Selepryl,selgiline, suppossedly citrate). I ran out of my liquid so now I am stuck with some tablets from both the US and India. I get an immediate brightening effect after holding the liquid under my tongue for 1 minute. Dissolving the tablets under my tongue (which takes longer and tastes terrible), doesn't have the same immediate effect. So whatever the claims for or against liquid deprenyl citrate, I feel a qualitative difference. A lot of the articles bashing conventional deprenyl (hcl) and promoting liquid deprenyl citrate are basically well-written advertisements for the liquid form. IME there is a difference in the two but many things that have been said in these articles ("ads"), are probably not correct or supported.

#28 jasonshadow

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Posted 16 June 2011 - 02:02 AM

Are there any studies indicating one method (sublingual or with food) is better than the other?

#29 jadamgo

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Posted 16 June 2011 - 04:47 AM

It depends on what you mean by "better," but in general, absorption that bypasses the digestive tract causes lower levels of l-amphetamine and l-methamphetamine in the body. This reduces side effects, and dramatically increases the bioavailability.
So sublingual absorption will deliver more selegiline and less amphetamine into the body per dose, which can save you money.

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#30 longevitynow

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Posted 20 June 2011 - 10:46 PM

I think selegiline has recently become available as a prescription sublingual, very expensive. Supposedly the effective dose is lower than with the pills. Whatever studies are or are not available, I much prefer taking my selegiline sublingually. But I get the pills and bite the bullet, taking them sublingually even if they are not designed for it. They don't taste very good but for me it is worth it for the enhanced effect. I previously got Selepryl and Cyprenil liquid, which I took under my tongue (and loved), but they seem to have disappeared from the market.




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