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Calcium α2δ Binding Drugs

^ See, the problem with us who take Gabapentin/Pregabalin medicinally is that we also tend not to be organic chemists. I am very sure you can produce tens of gabapentin analogues in a round-bottom flask (or in a round-top human head). But as far as we are concerned, these are not relevant.

Thus my hopeless search for things that already exist on the market, or are plant-derived.

Yet, somehow the conspicuous absence of α2δ calcium-blocking substances, and the fact that they seem to have a lot in common with NMDA-antagonists, leads me to think that these two have something in common. Do we have information on Ketamne's effect on these receptors, or on calcium channels in general?
 
I can tell you from experience and from a few other people's anecdotes is that they (gabapentin and pregabalin) potentiate Ketamine.

And for me, low doses of Ketamine work even better than these two for my depression/pain.

Have you tried taking tiny (and I mean TINY, ie. <10mg) doses of Ketamine with your gabapentin and see what happens? I assume if you're in Mexico, Ketamine shouldn't be difficult to find...
 
No I haven't actually, and yeah sure I can get some, I'll have to do some and get back to you with the report.
What about opioids? (Haven't tried those either)

Mixing it with benzos (I do 3~4 mgs of Clonazepam) works very well, also taking beforehand a couple of aleves (Naproxene, or any other common NSAID) seems to potentiate it.
Then potentiate the benzos with the classical well-known techniques (grapefruit juice, metronidazole, etc). Pregabalin is excreted 98% unchanged through the urine, so reducing your fluids intake (or if you are up to, even drink your urine, not recommended).

That should give you a great buzz all day long, for me, it keeps anxiety away very well all day.
 
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As for not having other T-type Ca-channel blockers (alpha2beta sub)... you need only look the the very old absence seizure drugs (ethosuxamide, and even older is trimethadione). As for their specificity, don't get too excited...

And as for Jamshyd's inevitable 'What about ketamine' question... I can think of few things that look more like an absence (or mayyyybe a complex partial) seizure than ketamine, heh... just think about Matt drooling and unable to blink back at the Spadina house.
 
Weird drugs indeed. Tolerance developes very rapidly but if you take a break you can actually get to the point where your tolerance is same as before you started.

Twice a week 600mg of pregabalin doesnt seem to increase my tolerance at all. Been on this "regiment" for half a year now, very effective. Any more than that and i can feel the tolerance build up :X
 
leungkachong said:
And as for Jamshyd's inevitable 'What about ketamine' question... I can think of few things that look more like an absence (or mayyyybe a complex partial) seizure than ketamine, heh... just think about Matt drooling and unable to blink back at the Spadina house.
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By all that's holy you DO exist, contrary to all the reports of your abduction by space cowboys from saturn! I miss you <3

And OMG @ memory of Matt. That said, let's be fair. He was injecting several vials a day. I am talking here about micro-doses.
 
kken said:
Weird drugs indeed. Tolerance developes very rapidly but if you take a break you can actually get to the point where your tolerance is same as before you started.

Twice a week 600mg of pregabalin doesnt seem to increase my tolerance at all. Been on this "regiment" for half a year now, very effective. Any more than that and i can feel the tolerance build up :X
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How long can you feel the effects, after a break and everything
?
 
after 3 days of continued use you start to notice the dimished effect from same dosage. Ive abused it in incremental doses up to a week topping at 1200 mgs per day 8o but still after such heavy use only 1 full week of abstinence and you are pretty much back to no tolerance / base line. great stuff
 
kken said:
after 3 days of continued use you start to notice the dimished effect from same dosage. Ive abused it in incremental doses up to a week topping at 1200 mgs per day 8o but still after such heavy use only 1 full week of abstinence and you are pretty much back to no tolerance / base line. great stuff
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Yeah thats my experience. Some docs say there is no tolerance to pregabalin but thats probably because here in the UK they don't seem to give out more than 600mg per day.

Well that's what I was told, maybe some get more?
 
I was taking 1200 mg and 4 mg of clonazepam for about 6 months, with an amazing tolerance to benzos (been taking them for 5 years). I took breaks during the weekends and holidays. Today I only take 600 ot 900 mgs, depending on how I feel in the afternoon, and 2mg of Clonazepam.
I've had GAD all my life, and those were the happiest six months of it, now I'm at a more normal dose and feel great, though not that nice buzz.
I gotta tell you, I never felt anything from Gabapentin, and the Lyrica rush never lasted until the other day, plus there were amazing days, and "just ok" days.
Anxiety was always gone though, just came back like once a month during that period of time.

grimmo said:
Yeah thats my experience. Some docs say there is no tolerance to pregabalin but thats probably because here in the UK they don't seem to give out more than 600mg per day.

Well that's what I was told, maybe some get more?
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I never got more, I found Lyrica myself, bought my first box (not a controlled substance in Mexico), showed it to my dads (both doctors), to my pdoc, everyone agreed and then I just started at 1 capsule (300 mg the ones I bought), and started incrementing the dosage, 300 mg every day: after 1200 mg I felt nothing so went back to 1200mg and there I held for 6 amazing months.
 
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Maybe you guys would know, because I've not boned-up on my chemistry for a while.... but whenever I get my Lyrica, at a dosage of about 600mg/day, why would it be that I don't need to take any opiates and feel no withdrawals? At one point I went almost 2wks on nothing but pregabalin & buproprion, with no opiate usage or w/ds. When I ran out of Lyrica I didn't experience a crash of opiate w/ds.
??
 
Same happens to me, but with the benzo withdrawals.
In my case I find it very simple as they both affect the GABA, in very different ways, but still.
If you don't have any GABA tolerance I can only infere Lyrica sedates you, plus Lyrica boosts opiates.
 
Pfizers marketing text says pregabalin potentiates opioids

large doses with no tolerance seem to stimulate me more than sedate, a nice body high + no sleep for next 20hrs or so but need atleast 1g to reach that in a single serving
 
Don't know if it's been mentioned, but the OP should be aware that a carbamate of gabapentin may be widely marketed soon. It'll either be called gabapentin enacarbil or Solzira or Horizant or Chrissy Lee or something. The net effect is somewhat akin to hiring a coyote to smuggle busloads of undocumented gabapentins into the central nervous system. Should be interesting.
 
seep said:
Don't know if it's been mentioned, but the OP should be aware that a carbamate of gabapentin may be widely marketed soon. It'll either be called gabapentin enacarbil or Solzira or Horizant or Chrissy Lee or something. The net effect is somewhat akin to hiring a coyote to smuggle busloads of undocumented gabapentins into the central nervous system. Should be interesting.
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hmm sounds suspiciously like a quick varient on gabapentin to license all those unlicensed NOW found out indications for gabapentin.

I.e past entries:
Depokate (semisodium valproate) + Valproate
escitalopram + citalopram
armodafinil + modafinil

Not doubting it's potential benefits but these new patents last another 15-20 years or so which can translate as lots of money. Typical LOW risk HIGH gain scenario. I wouldn't get too excited about it personally.
 
Amazing! I just can wait to get my hands on it! I'd love to feel the commented effects of gabapentin, because it never did anything for me.
Is it gonna be available any time soon in the US?
 
Charles Ferdinand said:
Is it gonna be available any time soon in the US?
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That's up to the FDA. I'd like to know too so I can buy shares of XNPT (the drug's developer). FDA announces the approval of a small-cap's Investigational Product and kapow! the stockholders double, triple or quadruple their money instantaneously. It's better than slangin rocks.
 
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