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  • BDD Moderators: Keif’ Richards | negrogesic

Pregabalin VS Gabapentin (bioavailabilty, duration etc)

Toz

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Oct 2, 2012
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tl:dr version: does pregabalin share the same side effects as gabapentin, same bioavailabilty problems and the same short duration or is it longer? are they interchangeable?

So I've been trying to get off gabapentin over a year. The withdrawal is still going strong and I can no longer take it. 17:th june last year I took my last gabapentin pill. I was at 3600mg daily.

I just quit because I had been using them long and couldn't for the life of me imagine they would bring such horrible withdrawal symptoms. Well, I was dead wrong. Since it's been so long and the symptoms are still so far from gone I've come to the realization that I've just been a complete idiot and this whole trying to get off the meds has been a huge waste of time.

Not wanting to start gabapentin again because it put me in withdrawals during the day due to what seems to be completely random bioavailabilty + I also woke up with just as bad withdrawals as when I was doing heroin has just put me off from ever taking one off these pills again.

So I'm looking at pregabalin instead. I know it's more addictive. I also don't care seeing as I'll have to take these pills for the rest of my life due to withdrawals that just won't go away. What I want to know is if they have the same problem with absorption that gabapentin does and also if they have the same short and shitty duration of effects. I'd very much like to hear they don't.

Also, will this all really have been a waste of time or should I at least be able to start up at a lower dosage and try to taper from there, if it's possible? I just know one thing, this shit can't continue or I'll commit suicide real soon...

Reinstating either gabapentin or pregabalin should clear up any withdrawal symptoms in a matter of hours, right?

(got a doctors appointment for other complications tomorrow but I intend to ask him for a lyrica prescription if it doesn't share gabapentin's problems)
 
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They're of the same class. Gabapentin has a bioavailability of 30-65% and Pregabalin is around 90%. Pregabalin also has a linear plasma concentration with increased dosing, unlike Gabapentin. Gabapentin concentrations will peak around 3-4 hours after dosing whereas Pregabalin peaks 1 hour after dosing. Pregabalin is also around 2.5x more potent than Gabapentin.

Taking one will help the others withdrawals. They are cross-tolerant. Benzodiazepines will also help withdrawals. They are all GABA analogues.

All in all, Pregabalin is more potent and effective. IIRC it is also more effective at crossing the blood-brain barrier.

Hope this clears everything up.
 
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Thanks, but you are wrong with the benzodiazepines, they do nothing at all for withdrawals from gabapentin/pregabalin except ease anxiety a bit. I've tried and the relief was so minimal it was not worth it. They did not even alleviate the muscle cramps.
 
Thanks, but you are wrong with the benzodiazepines, they do nothing at all for withdrawals from gabapentin/pregabalin except ease anxiety a bit. I've tried and the relief was so minimal it was not worth it. They did not even alleviate the muscle cramps.

I'm not wrong. Benzodiazepines will alleviate Gabapentin or Pregabalin withdrawals. Just like Gabapentin will alleviate Benzodiazepine withdrawals. They work on the same receptor, GABA. Any analogue will helps withdrawals. Hell, even Valerian Root will help with the withdrawals.
 
No, they do not. I tried taking 10mg clonazepam to alleviate withdrawal from 3600mg gabapentin, it did almost nothing at all. Horrible burning pain and anxiety + muscle cramps still. Taking more benzos seemed pointless as I was not addicted to benzos. Likewise when trying to get off benzos I tried gabapentin, it helped a bit more than benzos for gabapentin withdrawal but still not much at all.

Well, it helps, but not much at all. It won't relieve withdrawals.

It's not that strange as gabapentin has zero affinity for GABA A. it does not even work on GABA receptors at all from my understanding.
 
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They may work via different mechanisms of action but the end results is essentially the same, they increase the concentration of GABA in the brain. They may not "cure" withdrawals, but they will, as I said, help with them. The exact mechanism of action for Gabapentin is actually still not fully understood. It's been shown to have affinity for GABA-B in some studies and some studies suggest it has no effect on the receptor but some of its activity may involve interaction with voltage-gated calcium channels.

Either way, they increase the concentration/enhance GABA responses in the brain.
 
No, they do not. I tried taking 10mg clonazepam to alleviate withdrawal from 3600mg gabapentin, it did almost nothing at all. Horrible burning pain and anxiety + muscle cramps still. Taking more benzos seemed pointless as I was not addicted to benzos. Likewise when trying to get off benzos I tried gabapentin, it helped a bit more than benzos for gabapentin withdrawal but still not much at all.

Well, it helps, but not much at all. It won't relieve withdrawals.

It's not that strange as gabapentin has zero affinity for GABA A. it does not even work on GABA receptors at all from my understanding.

You're contradicting yourself with the bold stuff. The italic stuff is incorrect.

It won't rid you of withdrawals, but it will most definitely help. It should help quite a bit actually.
 
Yea it helps, but not to any significant degree in my oppinion, that was what I meant. It's definitely not worth it at least considering how addictive benzos are. The main problem I experience from gabapentin withdrawal is burning pain, which benzos do not help at all with.

I actually found opiates to be much more effective, since they reduced the pain. However that's not a viable option either and considering how long this has been going on the only option I have left is to reinstate the meds, whether I want to or not, it doesn't really matter by now :(
 
Well Toz,
the thing i can't get, is that, are you sure that this "burning pain" you feel, is from the gabapentin W/D? IDK, but one year is waaayy too long, are you sure that you're not effecting some kind of maybe neuropathetic pain, which is not from the gbpn W/D, but it's coming from somewhere else?...Well, of course i don't wanna fuckin say that i'm a Dr or smth but IDK, one year, burning pain, 10mg clonazepam doesn't help much, all these doesn't make sense , you know what i mean..but anyway, as for pregabalin, the good thing is that (if you take a good dose in the morning), it works for all the day...


MarinFn
 
I've been thinking that too so I completely understand where you are coming from. But I never experienced pain in all my life untill I quit the gabapentin. I don't really know what went wrong to be honest, it could be some kind of damage caused by cold turkey high dose anticonvulsants as the symptoms did not appear immediately after stopping the meds, the pain appeared after being unable to sleep for 10 days and then collapsing and waking up on the floor. Since then I have terrible vision problems / problems with memory/learning and this fucking pain that never ends. I just don't want to believe it's permanent damage, as it does get better over time but it does so extremely slowly unfortunately.

It's at least worth trying reinstating the meds. If it doesn't work, then I simply don't want to live anymore. I've already tried everything else from fentanyl to lower doses of ketamine/pcp and nothing cures the pain. All I feel is a reduction in intensity. High dose NMDA antagonists can block it but will also render me unable to function.

It isn't constant either, one day I will have horrible pain and the next day can be almost ok which seems strange if it actually was some nerve damage. Everytime I go to bed I fear that the next day the pain will be worse, I hate it and it just feels painful having to know I have to wake up the next morning by now.
 
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I'm not wrong. Benzodiazepines will alleviate Gabapentin or Pregabalin withdrawals. Just like Gabapentin will alleviate Benzodiazepine withdrawals. They work on the same receptor, GABA. Any analogue will helps withdrawals. Hell, even Valerian Root will help with the withdrawals.

Sorry bud, but neither gabapentin nor pregabalin exert their effects through GABA activity, though this is what was believed when gabapentin was originally released and marketed. These drugs bind to volatage gated calcium ion channels thus inhibiting excitatory neurotransmitters like glutamate, norepinephrine and substance P. As GABA inhibits excitatory neurotransmitters and excitatory neurotransmitters inhibit GABA, the overall amount of available GABA may be increased indirectly by these compounds but they are NOT considered GABAergic.

By all accounts I have read (quite a few as I've researched these compounds extensively) gabapentin and pregabalin are often miraculously effective at alleviating benzo and opiate withdrawals, but neither benzos or opiates will alleviate gabapentin or pregabalin withdrawals, though they may make them a bit easier to endure for the same reasons they make any uncomfortable experience more bearable.

OP, Pregabalin is 6x more potent than gabapentin and it completely lacks the bioavailability issues of gabapentin. In fact pregabalin has an oral bioavailability perhaps as high as 96%. It also comes in significantly wider range of doses. I believe (but could be wrong and don't feel like checking at the moment) that Lyrica comes in seven doses ranging from 25mg to 300mg. For these reasons Lyrica is a far better maintenance medication than Neurontin and is also significantly better for tapering. Actually, Pregabalin is just a stellar compound all around (I myself take 150mg 3x daily). Gabapentin is kind of shitty IME.
 
By all accounts I have read (quite a few as I've researched these compounds extensively) gabapentin and pregabalin are often miraculously effective at alleviating benzo and opiate withdrawals, but neither benzos or opiates will alleviate gabapentin or pregabalin withdrawals, though they may make them a bit easier to endure for the same reasons they make any uncomfortable experience more bearable.

OP, Pregabalin is 6x more potent than gabapentin and it completely lacks the bioavailability issues of gabapentin. In fact pregabalin has an oral bioavailability perhaps as high as 96%. It also comes in significantly wider range of doses. I believe (but could be wrong and don't feel like checking at the moment) that Lyrica comes in seven doses ranging from 25mg to 300mg. For these reasons Lyrica is a far better maintenance medication than Neurontin and is also significantly better for tapering. Actually, Pregabalin is just a stellar compound all around (I myself take 150mg 3x daily). Gabapentin is kind of shitty IME.

Yea thanks this was exactly what I meant, benzodiazepines will work for gabapentin withdrawals in the same way they work for anything that's terrible, but the mechanism of action seems to be quite far off from gabapentin/pregabalin.

It seems like pregabalin is a good choice then, unfortunately, insurance will not pay for it I found out. It is really expensive also :/ Fuck this really. I wish I never took these pills, I regret it more than I do injecting heroin.
 
Lyrica samples are falling off the shelves at physicians offices everywhere. You could potentially get large amounts for FREE.
 
Hey Toz,
hope you're doing fine (or maybe as fine as it gets..). You said that you tried everything, from fentanyl to low doses of ketamine or pcp, but nothing did cure the pain, just reduce it's intensity...you didn't make it clear, if you've try the lyrica, and give it a 2-4 weeks time, it needs to see if it works. Believe me, i can totally understand you when you say that living in such a pain doesn't worth it...yeah, so fuckin fucked difficult..

If you don't mind, of course, i would like to know why you initially started taking the gabapentin, (and i don't know, maybe some other anticonsulvants, or whatever oher meds, too..).
I wish I never took these pills, I regret it more than I do injecting heroin.

Well, this is..WOW!! Being a junkie, with on-off for more than 20 years, with all the shits that come together, i find it hard to believe that a person who has gone through these shits, puts smth else first in his list of "things i regret for"..what, a fuckin neurontin..well, maybe you think that i'm ironic, but believe me, i'm not, not at all..I know how hard is to be allmost constantly in pain, a pain that from the way you describe it (burning pain..), it sounds like fuckin neuropathetic pain..

From this regret you wrote, i could guess the intensity of your pain..But hold on, my friend, don't give it fuckin up (i'm sure you wouldn't, you doesn't seem to be this way of man..;)). Try to ask a lot of (good) Drs, make your own research, cause IDK but it seems a rather rare case, (just IMO, of course..). Anyway, i wish you good luck, i'm sure that soon or late, (soon better..:)), you'll find the solution..Be safe and have strength, my friend..and patience, it's a key-feeling in pain conditions...%)




MartinFn
 
its very complicated, gabapentin NOR lyrica even though they al act on GABA receptors, they're are different gaba receptors. just like if ur in xanax withdrawl, u can drink alcohol and expect xanax withdrawl to go away, it actually exaggerates withdrawl symptoms...

if ur in benzo withdrawl, u need benzos (xanax, klonopin valium ativan, etc) to avoid physical dangers, poppin neutonin or lyrica wont solve this problem
 
I'm done with benzo withdrawal, that's not a problem. I am starting lyrica tomorrow I think, doctor wrote a prescription for 300 pills and said he will write increasing doses untill the pain goes away, if it does.

And I am diagnosed with neuropathic pain / allodynia, doctor told me it can't possibly be the neurontin that caused it but I don't believe a word of it. The pain appeared after stopping the pills, if the pain goes away by taking the same pills it is safe to say the pills was the cause from the beginning, at least in my oppinion.

But it doesn't really matter, as long as this fucking pain goes away, I could care less.

@MartinFn, I'd chose the pain from heroin withdrawal any day of the week instead of the horrid burning pain I experienced a year ago after quitting the neurontin. It is better now than it was then fortunately, though the pain still sucks. It burns with an extreme sense of cold that makes the burning cold feeling from heroin withdrawal seem like something desirable.

edit: I wonder how lyrica combines with my favourite drugs, dissociatives/weed. Will it synergize or reduce the effects? I'm guessing it will reduce them being an anxiolytic medicine.
 
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So far so good Toz, i'm sure you'll be better with the lyrica, don't forget it has a wide range of therapeutic doses, that's why i think it comes in capsules from 25mg till 300mg..i've a feeling that you'll be fine.
As about the interactions with other drugs, it works very nice with benzos, and it potentiates the opiates (even in it's leaflet it says that it potentiates oxycodone..%)), so that's good news i think..When i take it with opiates, it gives a more energy kind of feeling, but it also increases the nod, when you close your eyes, for example..yeah, when i was started takin it, i didn't gave it much of attention, but latter, i tried it in higher doses, and i can say that now is one of my better potentiators..Anyway, i wish you find the relief you need and deserve, finally, you've been through a lot of fuckin pain, and as i'm a chronic pain patient, i fuckin know how awful and fuckin unbearable it can be..
All my wishes for better days coming, bro..


MartinFn
 
Ive been on gabapentin for a very long time and have recently switched to lyrica. Ive been taking between 300-1200mgs of lyrica a day for close to a month. Prior to that I was taking around 3 grams give or take staggered neurontin. I cant afford the money to buy anymore lyrica. I just took my last 600mg tonight. Can I resume taking neurontin to avoid lyrica withdrawal?
Is it cross tolerant?
And can gabapentin be taken with lyrica in a way that it would be just like taking more lyrica (a synergy)
 
I have been prescribed pregabalin 300 ml + hydromorphone 2 ml and codine 180 ml i have found that with the pregabalin , i built up a fast resistance to it , taking 2x the amount the next day, I have found that it gives me a stoned feeling mixed with a drunk feeling, as for the pain it works moderately i guess,
 
back prescribed to both neurontin 600mg qid and lyrica 300mg bid. I'd say the lyrica is more habit forming. you get a tolerance and want the effects and chase them sort of ordeal. neurontin is the same as always. a very sturdy drug I love you have. if I had to lose one of the two scripts I'd probably keep the neurontin
 
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