• N&PD Moderators: Skorpio | thegreenhand

Maximizing Gabapentin bioavailability.

Do you guys really think gabapentin is good for opiate withdrawal? I found that it didn't give very much relief. I guess it's better than nothing. In mild withdrawal it does help you sleep.

I don't take gabapentin very much now. I would usually pop 300mg every half hour 2 45 minutes. 1200mg would have me feeling really heavy, whole body felt weak, especially legs , kind of hard to keep eyes open. I sometimes get a mood lift from gaba but rarely.
 
hi im a new member to bluelight, though i have read and re-read this thread many times. when i first started taking gabapentin it was my wife's who only kept filling scripts for me, since i was a bad opiate addict at the time. i would always dose 1800 to 3600 mgs at a time for 3 or 4 days before the script was gone, at which time i would go looking to score something else. anyway, she now gets waaay more (4500 mg a day!) we now only get the script cause im totally off the opiates and everything else for that matter. that afore mentioned dose doesn't do anything for me 3 1/2 weeks later, so for someone with an apparently high tolerance need to dose for an at least mellow affect? any advice would be greatly appreciated!
 
The problem is the amino acid transporter gets saturated so no more can be transported. I don't know what the exact time at which it ceases to be saturated by the drug, but I'm guessing it's around 45 minutes to an hour. The bioavailability is also slightly enhanced with food.

Gabapentin is weird in that the bioavailability goes down almost linearly with increasing dose -- so whether you're taking 150mg (about when it starts to decline) or 600mg, nearly the same amount of the drug is absorbed. This is because of the above mentioned transporter saturation. The rest gets excreted. Hence, the staggering method and lower doses.

I think you mean that bioavailability is almost inversely proportional to dose. This is VERY different than a linear relationship.
 
It's a linear relationship with a negative slope. I intended "goes down almost linearly with increasing dose" to be synonymous with "inversely proportional".
 
It's a linear relationship with a negative slope. I intended "goes down almost linearly with increasing dose" to be synonymous with "inversely proportional".

But they are not synonymous at all. A linear relationship with a negative slope would mean there exists some sufficiently large dose, where literally zero gabapentin would be absorbed. This is obviously not true.
 
Whooo boy.

I don't know even know what to say about that.
 
I'd say "whooo boy" is about adequate...(took the words right outta my mouth...)
 
But they are not synonymous at all. A linear relationship with a negative slope would mean there exists some sufficiently large dose, where literally zero gabapentin would be absorbed. This is obviously not true.

literally it may not be true but there comes a point where not enough of a drug is absorbed to have any noticable effect and thats the cut off

bodies dont have absolutes
 
literally it may not be true but there comes a point where not enough of a drug is absorbed to have any noticable effect and thats the cut off

bodies dont have absolutes

Sure the bioavailability may approach zero as the dose increases, but what I meant is that, given a linear relationship with negative slope between bioavailability and dose, there is a point where zero of the drug (zero in absolute quantity, not bioavailability) get absorbed.

I don't think anyone would argue that there is some large dose of gabapentin that has ess of an overall effect (again, talking about absolute quantity of drug absorbed) than a smaller dose. This is different than saying that the increase in dose has no noticeable effect, which is likely true.

With a high enough dose, the amino acid transporters will be saturated and the gabapentin should theoretically absorb at a constant rate independent of dosage. How could it be possible, then, that further increasing the dose beyond this would decrease the absorption rate (absorption rate, NOT bioavailability)?

Say you double the dose beyond the minimum dose needed to saturate the transporters. The transporters will still be saturated, then, the absorption rate should be roughly the same, and the excess gabapentin from the larger dose will be excreted. The increase in dose may have no noticeable effect, but the larger dose will still have roughly the same effect as the smaller dose. This describes an inversely proportional bioavailability-dose relationship.

The only possible mechanism I can think of that would decrease absolute quantity of absorbed gabapentin with a sufficiently high dose is that somehow, too much gabapentin would literally destroy your amino acid transporters, in which case you would probably die anyways. I doubt this happens within a few orders of magnitude of a typical medical or recreational dose, considering gabapentin's safety record, however. If this effect happened at typical doses and was responsible for the negative correlation between bioavailability and dose, then you would expect gabapentin to be very toxic in medical doses.

On another note, saying `I intend linear to be synonymous to inversely proportional' makes about as much sense as "I intend orange to be synonymous with apple".
 
So I just got a few of these to try, and 900mg and 1200mg combined with a benzo was amazing. Like the first time I took the benzo (phenaz for the 900 and etiz for the 1200). I was floating around in a warm blanket - the only difference was it was less sedating and lasted much longer.

To those who are prescribed gabapentin, try combining with a benzo if grams of it aren't doing anything anymore :)
 
^ And how, exactly, do benzos increase Gabapentin bioavailability, as this is percisely and entirely the reason for this particular thread's existence?
 
^ They don't. They just synergize nicely. To me, it's like, okay, I don't really feel this gabapentin (or I'm not getting what I wanted out of it), so I'll take this other drug to add to the effects. Then I'm not really sure what's what, or what I'm feeling from this or that. Sure, benzos feel great with gabapentin, but they don't increase bioavailability in any way.

I'm still waiting to find out how to increase the bioavailability in a way that's more effective than what we already know. To you use your words exactly, Jammy, it's "horrible and fluctuating" bioavailability can lead to different therapeutic effects on a daily basis, and I take the same amount every day (3,600mg + 450mg pregabalin). BTW, gabapentin and pregabalin seem to compliment each others' effects quite well. Especially considering the more "consistent" effect that pregabalin has on a person.
 
And that was my point exactly (with my previous post).

Kakti and everyone else: please don't make these kinds of posts in ADD. There are other places where they may fit better like OD or TR (if written well).
 
It's been some time since I visited this thread so I figure it's due for a personal update.

I find the absolute best way to take my gabapentin is by using a pill cutter for portioning doses. I'm prescribed 800 QID and I'll take 200 mg (roughly 1/4 of a pill) every half hour until I've made the 2 hour mark.

Then I'll wait a few hours and do this again.

I find this to be the only financially/tolerantly prudent way to take this medicine.


I still find it unreliable at times, but It's an odd relationship we share with one another.

I was prescribed this for anxiety but find the only thing it treats is uni/bi-polar depression. Quite adequately at that, but it tends to make me manic depending on the dose. I'm not taking anything other than pristiq 100 QD.

Once I find a new doctor and get the meds I really need, I'll revisit and share my experiences.
 
I doubt this has anything to do with bioavailability, but I've always noticed that caffeinated soda seems to 'bring on' the effects of gabapentin, especially with staggered doses. I usually dose 900mg with a soda, another 900mg twenty five minutes later, and finally a 1200mg dose with more soda an hour and fifteen minutes after the first dose.

It's not the caffeine, it's the acid in the soda ;) I'm surprised nobody has mentioned this yet, but an acidic stomach increases bioavailibility! I can't remember why, but a quick search on google should help. i usually take it with lemon juice.
 
It's not the caffeine, it's the acid in the soda ;) I'm surprised nobody has mentioned this yet, but an acidic stomach increases bioavailibility! I can't remember why, but a quick search on google should help. i usually take it with lemon juice.

Gabapentin is 2-[1-(aminomethyl)cyclohexyl]acetic acid; how would adding acid to an already acidic stomach increase bioavailibility?

Can you cite a reference for this?


carbonic acid, such as found in soda becomes a base when the co2 is released--making this a base in your stomach if I am correct.
In addition, taking gbp with food also supposed to help--the effect of this being a buffer for stomach acid...

I'm not the authority on this, just raising an eyebrow at your claims based on my amateur understanding of acid/base chemistry

edit: people do advise taking a base (baking soda, tums, etc.) with either opiates or amphetamines to potentiate--both of which are base salts...idk
 
I have been on gabapentin 1500 mgs (at once) a day for about 3 months. I have tried the staggering method today, 300mgs half hour intervals for a total of 1500 mgs over 2 and half hours. I can say this did not seem to increase the effects at all and actually seemed to have less of an effect then just taking it all at once.
 
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.
 
Top