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Jamshyd
02-11-2009, 20:24
As many here know, Gabapentin is a very uneconomical drug. Even as generic, it costs a shit-load of money, and as most of you know it has horrible and fluctuating oral bioavailability.

From what I gather, it has absolutely no use taken rectally because it is a Zwitteron, or something like that. I have no idea but both I and pubmed can confirm the fact that gabapentin cannot be taken rectally.

I assume the zwitteron thingy applies to nasal absorption.

Short of injection (which I'd do if I had less talc anc cellulose to deal with), I'd like to collect as much info as possible about increasing oral bioavailability.

Literature search was not very helpful. The only thing I gathered is that frequent divided dosing is better than taking it all at once.

---

Does anyone know which is better, an acidic or an alkaline gut pH for the absorption of gabapentin?

What foods should one avoid, what foods should one eat, is it better before, after, or between meals? (literature seems to suggest that during meals is the best).

Are there any supplements one can take to improve its absorption?

Thanks a lot in advance...

nuke
02-11-2009, 22:28
I've done a crazy amount of experimenting and I've found the following is best:
Take 150mg at a time. Stagger the doses by 45 minute interval. Take with a snack each time.

That usually would get me just plastered on 600mg, but I would need to have no tolerance and it takes about 2 hours after the first one to feel anything. My experience has been that the effects are variable among individuals and that tolerance occurs incredibly fast.

Jamshyd
03-11-2009, 10:35
Oh for sure, I have an ungodly tolerance to it because I use it medicinally. My doses are in the grams.

I will follow your method in 300mg increments (that's basically 1 cap), and see what happens).

MurphyClox
03-11-2009, 17:55
Yo Jamshyd, your question was already researched. Take for example these 2 abstracts:

"Inter- and intra-subject variability in gabapentin absorption and absolute bioavailability."
Epilepsy Research 2000, 40(2-3), pp.123-127

Abstract
Gabapentin (GBP) is a non-metabolized, non-plasma protein bound, renally excreted antiepileptic drug that is actively absorbed via the system L amino acid transporter. Previous studies have demonstrated that gabapentin displays dose-dependent absorption.
Objectives: These studies were conducted to det. inter- and intra-subject variability of gabapentin absorption. Two prospective clin. studies in healthy adult volunteers were conducted. Coeff. of variation (CV) was used to express variability of gabapentin absorption.
Methods: Study A: 400-mg single dose, randomized, cross-over study to assess bioavailability of four different gabapentin formulations (9 males, 11 females; mean age and wt. 41 yr, 75.1 kg). Plasma was serially collected up to 48 h and bioavailability (F) calcd. post-dose to det. concn.-time curves (AUC). All four formulations were bioequiv., thus repeated measures anal. was performed to assess inter-and intra-subject variability. Study B: 600-mg single dose study (15 males, 35 females; mean age and wt. 31.1 yr, 72.7 kg) was conducted to det. inter-subject variability in gabapentin F. Urine was collected over 48 h and bioavailability (F) calcd. Urine and plasma gabapentin concns. were measured by HPLC-UV.
Results: Study A: Overall mean (CV) of GBP AUC values was 34.124 .mu.g/h per mL. Inter-subject CV for AUC was 22.5% and intra-subject CV was 12.1%. Study B: Overall mean (SD) GBP F was 49.313.6%. Inter-subject CV of F was 27.6%.
Discussion: The inter-subject variability in gabapentin absorption is substantially less than that of the inter-subject variability. This indicates that one would expect a wide range in gabapentin absorption between subjects; however, a much smaller variability within a subject. The within subject variability of gabapentin is small enough that plasma drug monitoring may be used to assess gabapentin absorption for a given subject and the benefit of dose individualization.


"Gabapentin bioavailability: effect of dose and frequency of administration in adult patients with epilepsy."
Epilepsy Research 1998, 31(2), pp.91-99

Abstract
Gabapentin (GBP) is a non-metabolized antiepileptic drug that is eliminated by renal excretion and displays saturable, dose dependent absorption. The recommended dosing schedule for GBP is t.i.d. At large daily doses, oral bioavailability (F) may be improved by giving the daily dose more frequently. The objective is to evaluate whether switching GBP dosage regimen from t.i.d. to q.i.d. results in increased oral bioavailability. This study consisted of 2 parts; a computer simulated pharmacokinetic model and a clin. pharmacokinetic study in 9 adult epileptic patients receiving 3600 mg/day and 11 receiving 4800 mg/day. All patients were evaluated during both t.i.d. and q.i.d. regimens. F were detd. by calcn. of percent of dose excreted unchanged using steady-state 24-h urine collections and were compared using a paired t-test. At 3600 mg/day, mean F following t.i.d. and q.i.d. dosing were 38.7 and 40.0%, resp. At 4800 mg/day, mean F following t.i.d. and q.i.d. dosing were 29.2 and 35.6%, resp. Good agreement was obsd. between values from this study and predicted values based on the pharmacokinetic model. Improved GBP F at doses of 3600 mg/day was not achieved with more frequent drug administration, and thus is not warranted. At 4800 mg/day, a 22% increase in F was obsd. with more frequent drug dosing. GBP F may be significantly increased by q.i.d. vs. t.i.d. dosing, depending upon dose level. This increase in F however must be balanced against the inconvenience of more frequent dosing. Therapeutic drug level monitoring may aid in the evaluation of such pharmacokinetic maneuvers.
(full articles available upon PM-request)

________________________________


Apart from this, you might be interested to read about XP13512 ("gabapentin enacarbil"). It's a gabapentin-prodrug that gets actively (!) transported by intestinal transporters.
http://img692.imageshack.us/img692/4182/xp13512.gif (http://img692.imageshack.us/i/xp13512.gif/)

Selected bibliography:

"XP13512 [()-1-([(α-isobutanoyloxyethoxy)carbonyl]aminomethyl)-1-cyclohexaneacetic acid], a novel gabapentin prodrug: I. Design, synthesis, enzymatic conversion to gabapentin, and transport by intestinal solute transporters."
Journal of Pharmacology and Experimental Therapeutics 2004, 311(1), pp.315-323

"XP13512 [()-1-([(α-isobutanoyloxyethoxy)carbonyl]aminomethyl)-1-cyclohexaneacetic acid], a novel gabapentin prodrug: II. Improved oral bioavailability, dose proportionality, and colonic absorption compared with gabapentin in rats and monkeys."
Journal of Pharmacology and Experimental Therapeutics 2004, 311(1), pp.324-333

"Clinical pharmacokinetics of XP13512, a novel transported prodrug of gabapentin."
Journal of Clinical Pharmacology 2008, 48(12), pp.1378-1388

(other publications are available, including numerous patents)

Cheers, Mr. Murphy

Thou
05-01-2010, 20:37
First off that you for that information Murphy I've been scanning the web for the last few days looking. I just now encountered this thread.


Oh for sure, I have an ungodly tolerance to it because I use it medicinally. My doses are in the grams.

I will follow your method in 300mg increments (that's basically 1 cap), and see what happens).

If you don't mind my asking, what is your daily dose Jam?

I've just started taking gabapentin again in increments of 400 mg three times per day and already I'm noticing the therapeutic values I had experienced the first week waning considerably.

I'd personally like to go up to 2400 mg daily although instead of 800 T.I.D. I wanted to try 400 6 times a day or a similar dosing schedule to that effect.

I too am interested whether stomach PH plays a role in absorption so if anyone has the answer I'd be delighted to hear it.

Thanks

MurphyClox
06-01-2010, 17:14
First off that you for that information Murphy I've been scanning the web for the last few days looking. I just now encountered this thread.

At least somebody noticed my last post :\

RedLeader
24-01-2010, 11:53
I've done a crazy amount of experimenting and I've found the following is best:
Take 150mg at a time. Stagger the doses by 45 minute interval. Take with a snack each time.

That usually would get me just plastered on 600mg

I have been taking gabapentin for 6 months now, but I have always dosed all at once. I have tried some large doses (2400mg usually) and it was nice, but not great.

I just now have started with the staggering method, and I very much agree with it. It's great!

I've been doing 300mg every 30 minutes for about 3 hours to get to a really nice place.

Again, I repeat, stagger gabapentin!!!

I might try 150mg every 20 minutes over 4-5 hours in a week or so and see how that compares. But doing what I described above knocked my socks off, and showed me a completely different side of this compound.

nuke
24-01-2010, 18:37
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.

RedLeader
25-01-2010, 05:36
^ Understood.

With that said, I'm going to instead try :45 increments tonight.

Thank you for your elaboration.

RedLeader
26-01-2010, 12:31
Okay, given the known similarities between gabapentin and pregabalin, would the staggering approach also work for pregabalin? Thoughts?

barry351
26-01-2010, 13:50
My thoughts on gabbapentin brand name neurontin,I have been a user of this for more than a year.I doubt many know this and it needs to get out there,and before I tell all I need to say to the one that said gabbapentin has no uses I dont agree at all it can for some be great for some types of nerve pain.I take it just because it puts me on a better level hard to explain.What I really would like to let people know is if one is in serious opiate withdrawal you must take way more than the maximum recommended dose which is 800 milligrams,I am supposed to take 800 mills 3 times a day thats the max dose.I was in opiate withdrawal and took 4 of my 800 milligram gabbapentin and thought wow relief. I was totally amazed,I thought man people need to know this,and then I thougt maybe its just me so when a friend came over asking for one of my 8 milligram buprenorphine and was to low to give one I said hey try these out,he took 4 800-s and was also amazed. This drug is easy to get from most doctors for they most I feel know little about it. I asked my psyciatrist for it told her I had tried it and it made me feel better so no problem, a friend also had no problem.Some doctors may ask you to start out on a low dose so give it time and just move up.I just told her I had taken the 800 mill rite off but she still gave me 300 then 600 then to 800 in about a month or 2 so I say give it a try especially if you are in and out of opiate withdrawal lots, which can get very old you already know if and opiate addict. Just one problem the drug is expensive as said above,I am on dshs and get many of my drugs paid for.dshs is very picky about what they pay for I had to get approved by whats called the pharmacy appl. board to be on neurontin it took a week and got it, they dont pay for my buprenorphine or my soma (carisoprodal) I am on klonipin 2 milligrams 4 times a day they pay for that. I was lucky to find a doctor to give me the klonipin and soma it may not last for long for he is 81. Hope this helps someone.Just in case some think oh he gets soma and klonipin thats what helped well I am an addict and take more than supposed to I was out of both my klonopin and soma and buprenorphine when I took the gabbapentin for withdrawal,later b351.

nuke
26-01-2010, 19:21
Okay, given the known similarities between gabapentin and pregabalin, would the staggering approach also work for pregabalin? Thoughts?

The pharmacokinetics for pregabalin are pretty regular if I remember right, it's just straight absorbed without metabolism and then excreted unchanged. So you can probably eat as much as you want whenever you want.


Absorption and Distribution

Following oral administration of LYRICA capsules under fasting conditions, peak plasma concentrations occur within 1.5 hours. Pregabalin oral bioavailability is ≥90% and is independent of dose. Following single- (25 to 300 mg) and multiple-dose (75 to 900 mg/day) administration, maximum plasma concentrations (Cmax) and area under the plasma concentration-time curve (AUC) values increase linearly. Following repeated administration, steady state is achieved within 24 to 48 hours. Multiple-dose pharmacokinetics can be predicted from single-dose data.

The rate of pregabalin absorption is decreased when given with food, resulting in a decrease in Cmax of approximately 25% to 30% and an increase in Tmax to approximately 3 hours. However, administration of pregabalin with food has no clinically relevant effect on the total absorption of pregabalin. Therefore, pregabalin can be taken with or without food.

Pregabalin does not bind to plasma proteins. The apparent volume of distribution of pregabalin following oral administration is approximately 0.5 L/kg. Pregabalin is a substrate for system L transporter which is responsible for the transport of large amino acids across the blood brain barrier. Although there are no data in humans, pregabalin has been shown to cross the blood brain barrier in mice, rats, and monkeys. In addition, pregabalin has been shown to cross the placenta in rats and is present in the milk of lactating rats.
https://www.pfizerpro.com/product_info/lyrica_pi_clinical_pharmacology.jsp

barry351
26-01-2010, 20:21
I have just awoken this mourning and thought I would re-read this thread on gabbapentin and on doing so I realized that before posting I should read more carefully the posts by others before spewing my thoughts here.what I would like to add to my above last night 4 am to tired to be giving others info post is that jamshyd and nuke are very correct in that gabbapentin is way to expensive and does build tolerance very fast,in one week I dont get anywhere near the same affect as I did with the first dose,also I noticed that jamshyd said his doses are in the grams,this also made me realize that when I said the max dose was 800 milligrams 3 times a day that,that was the max dose here in the usa,other countries I should have known may have much different doseing amounts.I should also add that I read (sorry cant give exact site I read it on but it was a true study) gabbapentin when taken with a certain amount of morphine became 44% more available to you and this I believe from experience for I have done a gram of (we have shitty tar H here) heroin and the affect was not worth the price I paid,and a day later with same H and same amount but with having taken say 2 hours before 3 800 milligram gabbapentin tabs I awoke on the floor to my mom pissed off thinking I took klonipin and H again when in fact it was gabbbapentin and H. I was totally out of klonopin,so as with klonopin mixed with an opiate gabbapentin and an opiate must also have a synergistic effect,to those that dont know what a synertistic affect is it is like say 2+2 =6 . The methadone clinic which is 50 miles away (or I would be on it) wont even allow one to be takeing a benzodiazapine which the family of these drugs is to long to list but here are a few klonopin generic clonazapam,valium generic diazapam,xanex generic alprazolam,and many more lams and pams. So be very carefull when mixiing other drugs especially opiates and other downers,I have lost a few friends over this exact mixing of opiates and any other downers.

RedLeader
27-01-2010, 14:35
https://www.pfizerpro.com/product_info/lyrica_pi_clinical_pharmacology.jsp

Based on their "3 hours," I'd venture to say that it should be staggered a bit faster. A mat of mine will be trying this soon and I'll report back with results.

Edit: Putting my faith in pfizer's words = lol

jeah
04-03-2010, 18:58
so would me taking 1800mg earlier affect the stagger results if I did 600mg every hour from now on? usually I tak 1800, 1800 2 hour later and 1800 3-4 hours after that. would be nice to take 600mg at a time every hour.

just wondering about flooding receptors...

what is anyone's daily dose? mine is 2400mg so 4X600 tabs. i usually take twice that (4,800mg) every other day. it works for my sleep and restless leg syndrome very well. in helps my fiancee's pregnancy pains but she is only on 600X2 daily. very early in pregnancy. she got off klonopin and adderall.

It nevery really makes me drowsy it seems to be a cure all. and I probably only take that dose twice a week. it has strange effects at all dose levels but I have been on it for 6 months. I have also had a grand mal coming off of klonopin so I made the switch from klonopin to neurontin. after a month long klonopin withdrawl (4mg for 5 years), anyway, off all things been prescribed many great things all the time neurontin is what I could not live witohut. I can't say enough about this drug it reallt woroks for me. I also have severe ADHD and hypomania but anyway, best medicine, psychoactive occasionally wonder drug that helps even everything out without any unintended side effects.. at least in normal 600-2400 q.i.d doses.

The Ghost of Omar
08-04-2010, 08:25
Just breaking my message cherry... Just moved up to 600mg 2x day but not sure what I'm supposed to notice.... Just like with all these frickin' antidepressant/non-benzo anti-anxiety meds they can be quite subtle - and for those of us (not moi naturally) who have trained the brain for the more instant relief chemicals it's fucking hard to be patient with "regular" meds.

Nexius
19-05-2010, 16:21
Bringing back the past....

I'm practicing the stagger method right now, I always take lyrica but it's so unglodly expensive.

Thus, I went and got myself a script for gaba 180 x300mg

I took a single dose of 4.8grams knowing it wasnt going to do much...

I'm trying this stagger method right now, 600mg a hour (300mg x30 minutes)

I'll report back tonight


Takin the kids to the park for the whole dayyyyyyyyyyyyyyyyyyyyyyyy

Get some sunshine

Day 2 of opiate cold turkey

And I'm feelin grrrrrreeeeeaaaatttttttttttt http://4pack.files.wordpress.com/2008/10/tony-the-tiger-frosties.jpg



EDIT:

Yeah i really don't feel that great, but I feel better than one normally does during detox
Taking massive doses of protein, amino acids and vitamins are really working... I slept like a baby, with the aid of jwh
I woke up feeling refreshed
It's going to be a good day


I think I may be on to something here http://www.chumpysclipart.com/images/illustrations/thumbnail/3250_picture_of_a_man_dressed_as_sherlock_holmes_l ooking_through_a_magnifying_glass.jpg

fryingsquirrel
20-05-2010, 08:54
My usual recreational dose is 3600 mgs. My wifes is 12000 (OMFG). We'll definately try staggering doses. Naproxen (aleve) increases absorbtion 12-15%. Whether this is true at recreational dose levels is likely unresearched.

drunken_etard
20-05-2010, 17:35
I am prescribed it at 900mgs a day. I have taken doses up to 2100-2400mgs and did acheive any sort of high. Maybe a bit of fuzzyness in the head and a little bit off balance...But no real high.

But I find it can potentiate some drugs.

SizzleSword
22-06-2010, 23:24
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. I'm usually feeling all the effects at +02:30 (sociability, reduced anxiety, shiny surfaces, slight floating sensation, very slight closed-eye imagery) and they usually last for the rest of the day more or less.

When I first started using gabapentin, I would dose around 3000mg at once but I found out that it was a big waste after I started trying the staggered doses. Tolerance builds strong and fast, and at one point I was having diminished effects even up to two weeks after my last dose, but that was still taking one large dose (3000mg or more) at once. Nowadays I'm usually taking gabapentin two to three times a week at up to 6000mg (1800mg, 1800mg twenty five minutes later, 2400mg an hour and fifteen minutes after first dose) using staggered doses and I'm not noticing the diminished effects at all unless I attempt dosing two days in a row.

So, yeah.. If anyone's getting upset about the tolerance issue, I'd definitely try staggered dosing because I can tell you from experience that works a heck of a lot better than taking one massive dose at once. Try some soda, too. Gabapentin's a lot better when you're able to take it when you want to, not just when you -think- it'll work. Peace.

love2party
22-06-2010, 23:57
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.

thatguyinthecorner
15-04-2011, 19:17
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!

isobob
19-04-2011, 15:50
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.

nuke
19-04-2011, 18:06
It's a linear relationship with a negative slope. I intended "goes down almost linearly with increasing dose" to be synonymous with "inversely proportional".

isobob
20-04-2011, 03:59
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.

nuke
20-04-2011, 04:07
Whooo boy.

I don't know even know what to say about that.

amanitadine
20-04-2011, 04:56
I'd say "whooo boy" is about adequate...(took the words right outta my mouth...)

pofacedhoe
20-04-2011, 16:42
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

isobob
20-04-2011, 19:05
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".

kakti
26-04-2011, 05:30
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 :)

Jamshyd
27-04-2011, 18:09
^ And how, exactly, do benzos increase Gabapentin bioavailability, as this is percisely and entirely the reason for this particular thread's existence?

TheTwighlight
27-04-2011, 21:40
^ 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.

Jamshyd
28-04-2011, 20:49
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).

Thou
29-04-2011, 02:14
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.

Justin Sane 53
13-07-2011, 22:48
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.

Fixed5217
05-10-2011, 01:39
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

ABakedAlien
17-12-2011, 07:52
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
17-12-2011, 17:54
I met this guy at a conference in BC, he's fucking awesome. But, capsaicin has a lot of promise for increasing gabapentin and pregabalin uptake into nerve cells. Also, you could always try to upregulate your L-type Amino Acid Transporters to increase its uptake.

http://www.pva.org/site/c.ajIRK9NJLcJ2E/b.6768681/k.1168/2011_Research_Foundation_Grant_Recipient_Smith.htm

Hope this helps out some chronic pain sufferers.

Thou
17-12-2011, 18:13
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.

laCster
17-12-2011, 19:06
stack, stack, stack em' up!

Epsilon Alpha
17-12-2011, 20:39
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.

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.

TheTwighlight
17-12-2011, 21:26
Fuck. I'm allergic to capsaicin.

Epsilon Alpha
17-12-2011, 21:43
Fuck. I'm allergic to capsaicin.

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

TheTwighlight
18-12-2011, 20:49
Makes me stop breathing.

Thou
19-12-2011, 18:00
Makes me stop breathing.


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.


http://27.media.tumblr.com/tumblr_ks1zcxJSUh1qztjn5o1_500.png

TheTwighlight
19-12-2011, 22:39
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!

SinisterMuffin
19-01-2012, 08:12
@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?

Ridethecircuswheel
19-01-2012, 12:08
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.

TheTwighlight
20-01-2012, 00:35
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!

SinisterMuffin
20-01-2012, 01:47
@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.