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Thread: Vyvanse (lisdexamphetamine) conversion

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    Vyvanse (lisdexamphetamine) conversion 
    #1
    Bluelighter lenses's Avatar
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    Does anyone know of a simple and reliable way to convert lisdexamphetamine to dexamphetamine , mainly to be used in IR administration?

    I don't want to do an acid/base extraction, i was thinking more along the enzymatic route. Would dissolving vyvanse in a protease or tryspin solution and letting it sit for a bit work? I imagine it would... I'll experiment on this later when I can get a hold of either...
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    #2
    Acid seems like a decent enough method, but I dunno how much you're gonna ruin the amphetamine, though.

    What about this tryptsin method?
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    #3
    Bluelighter lenses's Avatar
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    Well first off, THE TRYPSIN METHOD WORKS! Yay!

    Second off I don't really think of this as synthesis... It's refining something thats already present, not making something new.

    So mods, if that argument sways you, tell me and I will post more detailed info.
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    #4
    As far as I actually don't KNOW if this works, it's only speculation. I guess that should be allowed according to the forum rules. And btw: It's the actual route that the drugs takes in the natural metabolism...just biochemistry, so to say.

    So let's see. Trypsin cleaves an amide bond if it is placed after an lysine residue (or arginine or cystein but these are not relevant in this case). That means that in a chain of aminoacids (e.g. in a peptide) the NH2-end is defined as the start, the free COOH-group as the end. As Lisdexamphetamine is just amphetamin amide-bonded to lysin in the mentioned fashion, it can be readyly considered as (inactive!) prodrug. I would therefor agree to the "It's no synth but just refining"-proposal from Lenses.

    Trypsin in water (or better in a suitable buffer) must be perfect for the aforementioned method. I would recommend for native trypsin 36-40 C reaction temperature, but there may be temperature-modified variants out there. The final "product" should be obtainable by A/B-Extraction. No sidereactions are expected, yields should be (with an optimized protocol) quantitative.

    Quite a "modern" way of working. And it works indeed, yeah? Nice...
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    #5
    It's not true that this is 'just refining' the product. It's more like turning AMT into 5-MEO-AMT.

    amphetamine =/= lisdexamphetamine. It's not a mixture.
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    #6
    No no no, it is NOT a mixture. In plain pharmaceutical terms: "Lis" is just the inactive prodrug.

    Hmmm... so the phrase "something thats already present" from Lenses' statement isn't correct though. On the other hand I still agree with him. Modification in the mentioned manner is just a way of releasing the active compound from the time-delayed form... In my opinion it's in this case more philosophical if this already counts as "synthesis" or still as simple "refinement".
    Last edited by MurphyClox; 27-03-2008 at 16:36.
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    #7
    Bluelighter lenses's Avatar
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    I also found tyypsin is useful to abort a vyvanse run, somedays i'll want to sleep, so if you pop 1 trypsin you feel the effects like you would dexamp IR (the quick and hard comeup and comedown). But it runs its course in 2-4 hours, versus vyvanse.
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    #8
    So you mean, Vyvanse & Trypsin together make it a shorter trip while Vyvanse alone creates a prolonged high? Makes sense to me, as you actually experience just a "normal" Dexamphetamin-Trip. What I would like to know is, if you could transform the Vyvanse succesfully (and quantitavely!) already outside the body, in a beaker or whatever. I think less about extraction of Amphe afterwards but more about preparing an oral Amphe-Trip by the means of Vyvanse.

    Asked just out of curiosity: What "kind" of Trypsin do you use (no source requested, just the brand resp. the label)?

    Peace! Murphy
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    #9
    ^ Lol. I don't think s/he buys it from Walgreens. It's probably more of a university/research siphoning-type acquisition.
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    #10
    Has someone got a link to the patent of this stuff. I would love to know WHAT amides work. It would certainly give the MoDA a run for it's money, I can tell you!
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    #11
    @Johanneschimpo: Depending on the country where you live you can actually buy Trypsin; not only for R/D-reasons!

    @haribo1: This is the link for the International Patent: http://v3.espacenet.com/textdoc?DB=E...2005000334&F=0
    and that one for the US patent: http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&Sect2=HITOFF&d=PG01&p=1&u=/netahtml/PTO/srchnum.html&r=1&f=G&l=50&s1='20050054561'.PGNR.&O SN/20050054561&RSN/20050054561

    (damn....some letters are changed into smileys...you have to change them into = and D, written together)

    Btw, what is a MoDA?

    Murphy
    Last edited by MurphyClox; 03-04-2008 at 17:47.
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    #12
    Bluelighter RockWell's Avatar
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    I been on Adderall XR for a year now and I told my DR it was not working like it once did. She gave me Vyvanse to try. I took it, I really don't feel any different. However, I now am wondering if this stuff is even good or better then then Adderall.

    Any thoughts would be helpfull


    Thanks,

    Rock
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    #13
    It's practically the same like Adderall, just the prodrug of enantiopure D-Amphe. Better or worse is therefore only a question of how fast/delayed you need your daily amphetamine dose. This can onyl be found out be TRYING (IMHO).
    That it felt the same like Adderall is completely OK. Maybe a comparison that helps: Amphetamine and Methamphetamine are pratically the same considering the effects. Meth works just faster, more intense in the beginning and lasts longer. But they are the "same". Same comparison with Adderall/Vyvanse.
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    #14
    Seems to me that you could do this in the test tube w/ a light solution of Ca2+ and Mg2+, in pH 8.0 buffer.
    Produced d-amphetamine could then be removed via A/B extraction, which should also inactivate trypsin enzyme left in the solution.
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    #15
    Quote Originally Posted by MurphyClox
    Btw, what is a MoDA?
    Misuse of Drugs Act
    Its a UK thing; apparently better than the equivalent we have here in the US...
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    #16
    ^ Well, it doesn't have an arbritary analogue law. Great success!
    I wish NZ had kept the same MoDA as the UK for this reason . Damn them and their substantially similar clause...
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    #17
    Hoffman reaction. Calcium Hypochlorous (bleach) will change an amide to an amine.
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    #18
    Ex-Bluelighter Gaian Planes's Avatar
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    well I had a brilliant time on this stuff! 70mg +1 gram piracetam +some DMAE had me ROLLING for a little while. Seriously, nystagmus, my tongue was going crazy in my mouth. my body was vibrating.

    the full works.
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    #19
    Quote Originally Posted by oldkaw
    Hoffman reaction. Calcium Hypochlorous (bleach) will change an amide to an amine.
    Nope, Hofmann degradation is supposed to work only on primary (=unsubstituted) amides.
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    #20
    how about vyvensa and coke?
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    #21
    ^ Well, how do you feel about taking dextroamphetamine and coke together? Thats up to you.
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    #22
    Bluelighter lenses's Avatar
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    The enzymes were bought at a high quality "vitamin shop" *wink* *wink*

    Made by "Miller Pharmacal Group" , Proteolytic enzymes is the title on the bottle.

    They were not hard to find.

    An extraction would go something like add enzymes to lisdex,buffer ph to 8.0, then do an A/B to get the lisdex.

    Simple. Each bottle of 50mg vyvanse is equal to about 86 dexamp 10mg blue pills.Thats alot!

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    Vyvanse crash 
    #23
    I take 50mg in the morning and crash about 1pm in the afternoon. I've been keeping myself awake with blow.

    Does anyone have the same reaction or another tip on how to stay awake for the rest of the day?

    Can I just buy a bottle of Best Proteolytic Enzymes at the Vitamin Shop and take it with Vyvanse or do I have to perform all the chemistry described above?
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    #24
    Yes all that chemistry, lol. All that. It will take you 5 minutes dude, its not hard.
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    #25
    Well my doctor just added 20mg Adderall IR to avoid the crash in the pm which did not do much for me.
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