Maximizing Gabapentin bioavailability.

thouart_that said:

Epsilon Alpha -

You are now my new favorite bler of the week for not only bumping this, one of my very favorite threads, but casting this king-bitch of a knowledge gem into the myalgia pool!

I just started lyrica again 75mg TID for Anxiety, Fibromyalgia, and arthritis, and was planning on adding neurontin into the mix again.

From the years 2009-2010 I used neurontin exclusively for anxiety and depression, although I'd consider it more of a euphoriant than anything else. After discovering this thread I started cutting my 800mg tablets 4 ways, taking 200mg every half hour for two hours. I would do this an additional four times a day. It sounds like more of a pain in the ass than it actually was. The timing was always approximate because I didn't use the reminder feature on my phone as I have a pretty good memory when it comes to taking medicine.

I have an appointment Tuesday to try and get another script for neurontin strictly for pain, but from a GP. The lyrica I have prescribed to me is for anxiety by a psychiatrist, but helps muscle and nerve pain as well (as well as the 2mg klonopin on top of that).

I'll be adding capsaicin to the mix and I'll respond with the results once achieved.

Lastly, and this is for AE, how would one upregulate your L-type Amino Acid Transporters? I'm curious.

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I'll try and find some of his papers on the topic but the capsaicin thing looks promising in vitro, not sure if orally or topically applied would work depending on your situation. I do know that capsaicin patches are given out for postherpeic neuralgia, so it might be worth a shot if your pain is more towards the surface of the body. But, for those of you who don't know what capsaicin is its the active ingredient in hot sauce so it may burn like a motherfucker if you dose it wrong (wish I could help more on that front).

I remember megadoses of essential amino acid's upregulated L-type Amino Acid Transporters in muscle, but I have no clue on what would be the effects on nerves.

Dr. Smith seemed fairly personable at the conference, so it might be worth emailing him to see if there are any human trials going on right now on this approach.

Fuck. I'm allergic to capsaicin.

TheTwighlight said:

Fuck. I'm allergic to capsaicin.

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Burning and redness is the rule rather than the exception with this stuff, though I might be missing something here.
Mind sharing some details?

Makes me stop breathing.

TheTwighlight said:

Makes me stop breathing.

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Mr Burns: Smithers? What's the meaning of this slacking off?
Smithers: Uh... there's a bee in my eye sir.
Mr Burns: And...
Smithers: Uh.. I'm allergic to bee stings. They cause me to uh... die.
Mr Burns: But we're running out of forward momentum!
Smithers: Um.. perhaps you could pedal for just a little while sir?
Mr Burns: Quite impossible. I could try to bat him off if you like.
Smithers: Uh... really that's no... (bat). aaaaaaaaaugh.

Thanks for that. Not sure it makes me feel any better about my allergy, though. As long as I stay the fuck away from the shit I'm fine, so it's all good! Thank goodness I'm not allergic to stingy things!

@Thou: Perhaps it would be best for me to PM you, but I'm also curious for any answer from anyone with experience regarding my question:
You mentioned fibromyalgia, and that is where my experience with gabapentin (Neurontin) and pregabalin (Lyrica) come in. I was diagnosed with the condition about a year ago; I have recently lost my insurance but am working on reinstating it...anyway, before running out of my last supply, I was taking 1 100mg tablet of Lyrica in the mornings, with 2 100mg tablets of Lyrica + 2 10mg caps of Nortriptyline + 1 10mg tab of Zolpidem Tartrate each evening. When I get my health insurance problems sorted out, I plan on continuing the Lyrica at the very least...

My question to everyone is this - do those who suffer from fibromyalgia find that a large dose of Lyrica (1200mg or so) every couple of days is more effective in pain regulation than much smaller (~300mg) daily dose? I'm in a lot of pain right now, the last of my Lyrica finally leaving my body after going without for about two weeks now...so I'm looking for the best way to effectively regulate my pain. While my doctor is willing to work with me, it is painfully obvious that she is rather inexperienced with this condition. I am admittedly hesitant to have to rely on a cocktail of pills just to get by day-to-day, as I'm only 23, but I also wish I could function like a normal human being... any advice?

PHEW. I read this post and it started with people takign 150-300 mgs and I was pretty worried because I got perscribed gabapentin and I would take like 5-6 300 mgs to get my favorite high. I love gabapentin. I was worried that I was damaging my body because there have been a couple times when I would take 10-12 300mg which is a shit ton but i only did that like twice. I take about 4 to get a nice buzz now.

SinisterMuffin - I'm only 27, and I didn't really want to HAVE to take a cocktail of pills for the rest of my life (although it wasn't a problem when I was hooked lol). But then I found out about my really bad blood pressure problem. So now I'm taking 2 BP meds, Lamictal, Lyrica, tramadol, and Neurontin. Oh, well...so much for that pill thing. It's not so bad, so long as you remember to take them! I have fibromyalgia, so I know the pain you feel. It sucks. In my personal, extensive experience, I would say that lower doses every day are better than one big one ever day or 2.
My reasoning as far as the whole Lyrica-dosing debate is that when we as FMS sufferers begin to feel pain, it can be quite bad and we may want immediate relief because it's just too much. Taken every day, you might still be able to feel the spark-ups, but it's NEVER as bad, not by a long shot. You've just got a tolerance, but it's doing what it's supposed to be doing, trust me. Quit taking it and in 2 days you'll realize BIGTIME what it was doing for you.
If I'm in bigtime pain (due to FMS), and I want it to go away, take a big dose of Lyrica and it'll be gone. Complete and total pain relief. That may psychologically just SEEM like a better fix, since every time you take it you not only get the pain relief, you can also FEEL it working. I'm not even talking about necessarily being high from it. I just mean "feeling" the drug working. When I take Lyrica every day, I can't ever "feel it" or tell that it's doing it's job, other than the fact that the FMS pain is gone. Which is a pretty big plus, and in my personal opinion the drug just works better this way. It's a good "mood lifter:, as well!

Ridethecircuswheel - I guess I don't know how the "average" gabapentin user feels on reasonable doses of the stuff...I'm prescribed 3200mg per day; 800mg 4x/day. I can't get a buzz at all, period, anymore. I have taken up to 20 grams. It works fucking great as a medication, so I guess it doesn't matter. It used to be one of my favorite "high" pills, but now I use it as a legit med, and it's amazing. I've been taking itfor the past 8, almost 9 years...ever since the first time I tried it. Damn, this drug is versatile! Sorry...got sidetracked. Anyways, have fun!

@TheTwighlight - I've certainly been without any Lyrica for a couple of weeks now. It's been getting worse, the longer I go without it, of course. But since I'll pretty much be starting from scratch when I do manage to restore my health insurance and get my prescription again, I was just looking to see if perhaps there were a better way to dose to keep the pain at bay. I've never used pregabalin or gabapentin recreationally; I don't know that I necessarily will, despite my curiosity, considering how vital they are to providing me with pain-free days.

It's a damn nice high, especially from pregabalin, but if you always use it medically, good for you! I enjoy the occasional buzz from it. Get back on the shit. Or in the meantime, get a script of gabapentin (very easy btw). Take it to a mom/pop pharmacy and typically it will be cheap-ish to fill. Works almost as well at the right dose, no lie. I guess that's why pregabalin is a "gabapentoid".

I have been taking gabapentin for over 2 years constant, from 1 gram a day to 8, staggering, 200 and 400mgs between half an hour and an hour. I have tried it all and have basically come to one conclusion: staggering works but this medicine has to have another medication to set it off. right now, I nearly always take 6X400mg doses 45min apart and start feeling it after the 3rd 400mg. on the other days I tend to take 1-2mg of clonazepam. so 1 day is gaba/lyrica day and one day is clonazepam day (or 60-120mg of temazepam when I have it. tends to run out fast as well). I have been doing this for about a year, controls my anxiety and I have yet to have another seizure. so as for maximizing bioavailability, it just seems to come to an end, no matter how you do it.


my question is: how does anyone feel valerian goes with gabapentin, at least pharmacologically? It has always seemed to decrease the effects for me.. but why? can anyone here answer that?

I've prescribed to it and used to take 600mx x3 a day, after down to 300 x3 a day in the last month, still 20 minute staggering with 300mg pills and a little snack doesn't really change much. I still feel very very little, also I have a high tollerance to benzos but that's not supposed to interfere since gabapentin isn0t actually a GABA agonist so i still don't get why many grams in interval doses still dont work for me. Could it be just tollerance due to my medical doses?

I couldn't help but comment on this topic. I too am an experienced Gabapentin user (and all other GABA drugs for that matter). I agree with what everyone has said here. I get prescribed 800 mg 3X/daily. Since I have pretty much an endless supply, how much do you think I could possibly stuff on that transporter? 800 like every 45 min?

... and now... on to what I really wanted to say. One word. Gabatril. If you haven't tried it, try it! In my experience Gabatril (Tiagabine) works great with both Neurontin and Lyrica. I believe it's a GABA reuptake inhibitor. I've played around with those combos and could capture the feeling everyone's describing endlessly, everyday with no tolerance built at all. It's expensive as hell though. I can't wait until I get back on insurance and then I'm going to get some Gabatril. I like to use 16 mg at a time. Thoughts???

Also... I'm hearing 2 days, as far as resetting tolerance. Is that the general consensus (for Gabapentin only)?

I don't think there's any consensus on how long it takes to "reset" gabapentin tolerance, as it doesn't act on GABA-A/B like you'd expect, instead through soe unknown, possibly calcium-channel mediated effect.

It's probably variant between people, just like any other drug tolerance.

sekio said:

I don't think there's any consensus on how long it takes to "reset" gabapentin tolerance, as it doesn't act on GABA-A/B like you'd expect, instead through soe unknown, possibly calcium-channel mediated effect.

It's probably variant between people, just like any other drug tolerance.

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Yes I'm aware of the variance between subjects. I was just trying to get a ball-park figure. I have nothing to go on...

theirs not much out their that interacts with your calcium channels like gaba and lyrica? i really think a pregablin analog could be a euphoric RC.

FPU4eva said:

theirs not much out their that interacts with your calcium channels like gaba and lyrica? i really think a pregablin analog could be a euphoric RC.

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Tons of stuff modulates alpha2 delta1 calcium channels, granted they tend to be dirty drugs and/or neurotoxins...
But, there's a lot more going on than selective alpha2delta1 modulation with them.

But, this paper hints that caffeine might counteract some of the positive effects of gabapenitinoids via general stimulant properties and increasing cAMP signalling. http://www.ncbi.nlm.nih.gov/pmc/articles/PMC514605/

This paper suggest taking pregabalin, but not gabapentin, with salt (a sodium souce) and on a empty stomach may moderately boost uptake.
http://www.springerlink.com/content/r34v268235818680/

This paper suggests that a high protein intake can increase gabapentin uptake
http://www.springerlink.com/content/8p7w262tq223r516/

This in vitro paper shows that LAT1 (L-type amino acid transporter 1, a major player in gabapentin uptake) is induced in uterine cells by progesterone, granted the uterus isn't a nerve cell so I have no clue if these results carry over at any relevance.
http://jcem.endojournals.org/content/94/11/4533.full.pdf

And some random links detailing LAT1's regulation:
http://www.ncbi.nlm.nih.gov/pubmed/22444698
http://www.ncbi.nlm.nih.gov/pubmed/22185814
http://molpharm.aspetjournals.org/content/61/4/729.short

So in short: a high protein diet, taking it on a empty stomach with a small amount of sodium (gatoraid?), and perhaps the pill seem like probable ways to increase its uptake.

If anyone has started taking the pill while taking gabapentin it might be interesting to hear if there were any noticeable differences.

Best,
EA

Thanks for all the info guys, it's been so helpful for me. I've been having a blast this week. So far my tolerance if fine I've had no problems using the stagger method daily.