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A few questions about pregabalin

swilow

swilow

Sr. Moderator: AADD, CE&P, TD
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So, I've been prescribed pregabalin for sciatic nerve pain and a few other similar nerve issues; basically, the entire right side of my body is fucked. I've had issues with neuralgia and I get migraines, all of which are thought to have some connection. The major issue is sciatica though, and I have been prescribed 150mg twice a day for this. It seems to be helping but I have some concerns.

Going on ten years ago, I got addicted to benzos for PTSD/anxiety and was addicted for 3-4 years, and the withdrawal I went through was insane. Literally, I was psychotic, blacking-out, having seizures, from regular partial/absent seizures to more grand mal type, hallucinating, mania/depression. Please don't read any of my posts from that period, I take no responsibility for them. I tapered from high doses of diazepam and the taper was gentle and gradual. The theory behind why my withdrawal was so intense is likely due to kindling of the CNS; I have mild epilepsy that was a lot more severe when I was a young child, and so I was given multiple different anticonvulsants including GABAergic ones at this stage in my life. I basically stopped having large seizures when I was 11 but continued (and continue) to have absent seizures. These become minimal until I went through benzo w/d in my lateish 20's. It seems my CNS was probably primed to cease GABA production or whatever it is that happens during benzo use. Any dose reduction saw me in outer space. I've not read of many people experiencing withdrawal on such a scale. Lucky me. :|

I'm clean of benzo's though I'd use occasionally. I've come to realise I cannot really even do that; I was gifted some diazepam and etizolam about 18 months ago and stayed on it for 1.5 weeks and experiencing a return of my withdrawal, though significantly less. This has continued every time I take benzos for more than 2 days- I need to do a basic brief taper to reduce the chance of kindling based w/d but I still get rebound weirdness. Basically, I've stopped taking benzo's. Good move right. :\ The second last time I took temazepam, I had a progressive 'twitch' moving from my big toe up my leg. It stopped twitching. :)

My major question with pregabalin is whether using it consistently will cause a kindling effect.

I've reason to believe it will. I've been taking it for about 2 weeks; I tried a few high doses and got that drunk, weird feeling which I don't especially like so do not plan to continue doing that, and will use it at therepeutic levels. Anyway, its making me nervous, so I decided to stop for 2 days and see what happened. At the end of the first day I experienced some very odd symptoms that I did not anticipate; racing thoughts, cramping muscles, a feeling of trippiness, body pains, some anxiety. This increased until I took 150mg. The symptoms seemed to subside, but then I was getting very concerned and had to work so I took 20mg of temazepam after which I felt pretty much fine. I have continued to take prescribed doses of pregabalin and do not not plan to take any further high doses. Well, maybe every now and then. ;)

Is pregabalin GABAergic? Is it cross-tolerant with benzo's? Will withdrawal from pregabalin cause kindling of the CNS due to my past addiction/s?

Basically, I'm think this medication is not for me, but my doctor claims it is non-addictive. And yet, the packaging of the medication tells me not to cease use abruptly. He's a shitty doctor.

There is a huge chance I am being paranoid and anxious.

Clearly, I am not an advanced drug neuroscientist but I am really curious about any information you guys will have re my situation.

My last question would be whether Gabapentin is a safer option for me. I simply cannot go through this experience again, it totally derailed my life.

Thanks in advance.
 
Pregabalin is not directly GABAergic nor is it cross tolerant with BZDs. It's abusable, mind you, and can definitely produce a dependence syndrome similar to benzos, although generally speaking it has much less trouble with long-term usage.

The prevailing attitude is that it produces its action through actions at voltage gated calcium receptors.
 
I think there is some anecdotal evidence that suggests that people previously dependent upon benzos will have a tougher time withdrawing from gabapentinoids.
 
One thing I got from a place on the web 'It does apparently affect GABA synthesis by modulating the action of GAD the enzyme that catalyzes glutamate into GABA.' but I don't have a proper source.
 
From what I've read, Gabapentinoids are kind of mislabeled as GABAergic drugs, because they actually exert their effects through calcium channels. I actually have a personal experience that kind of demonstrates this fact. I'm an avid user of these drugs. I use them for withdrawal and just because they help me get motivated and get work done. Well, I decided I was gonna cop Fluvoaxamine (Luvox) from my prescriber under the guise of OCD in order to potentiate my Methadone that I occasionally get off the street. Well, Fluvoxamine, in addition to being an SSRI, exerts action upon the Sigma-1 receptor, which, among other things, regulates calcium channels.

After about a week of Fluvoxamine, I noticed my Gabapentin was being severely stunted in its effects. It's just an anecdote, but that should say something.
 
Sort of weird that drugs are prescribed and we don't know what they truly do. :\

Pregabalin does not appear to cause anxyiolysis in a benzo manner, the high dose seems edgy to me. At normal doses, it does not appear to potentiate either temazapam or Ghb. I have not nor will not try high doses with eithr.

I'm keen to continue pregabalin as I can finally sit down- I can even lie down- without shooting pains. I am also keen to avoid tolerance and don't think I really want to go above the projected 300mg per day.

Is it likely to exhibit cross tolerance with GHB?.I use G 3-4 times a week but will happily cease if it ensures pregabalin retains efficacy.

Lastly, is gabapentin as useful? Its certainly cheaper. :\
 
Gabapentin and pregabalin have very similar pharmacological effects, the difference seems to be one of potency per mg mostly.

I would not expect too much cross tolerance with GHB, as GHB is a GABA-B agonist/GHBR agonist. Not a significant LVCC binder, I don't think.
 
GHB might be a bad idea itself actually. In addition to low GABA levels being proconvulsant, excessive glutamate levels, the primary excitatory CNS neurotransmitter are also convulsant, and excitotoxic. GHB has a much MUCH higher affinity for the GHB receptor than it does for GABAb. GABAb agonists reduce glutamate release, but on the other hand, GHBr agonists induce glutamate release, resulting in a biphasic action of GHB. It takes a lot more GHB to activate GABAb to a sufficient level for recreational effects when combined with its GHBr agonistic action than it does to activate GHBr which in doses insufficient to activate significantly GABAbRs is neurotoxic (excitotoxicity, and IMO, the GHB receptor agonism-mediated glutamate releaser effects of GHB are probably responsible for the fact that despite being a sedative-hypnotic, in overdose GHB is a convulsant.


I avoid the stuff like the plague now, did fuck up big time a couple of times in the past on GBL/GHB and the results after what going up inevitably coming crashing down were nasty as fuck.

As for gabapentin, its similar to pregabalin, an agonist at alpha2delta subunit-containing voltage-gated calcium channels, rather than a direct agonist or allosteric modulator at GABA receptors themselves, although this does not preclude action mediated by GAD being modified. I have taken both pregabalin and gabapentin, if on pregabalin, or gabapentin they can have quite a nasty set of teeth. They don't always bare their fangs, and are a lot more forgiving than benzos and barbs, but they can definitely cause seizure on too fast or abrupt withdrawal if severely physically habituated to them, and tapering is a good idea.
 
I can tell you for fact that high doses of Gabapentinoids do little to treat symptoms of Alcohol withdrawal in my personal experience. Whereas, with Opioids, Gabapentinoids can eliminate nearly all symptoms of withdrawal. As far as the comparison goes, it's been stated in the past that Gabapentin and Pregabalin exert similar effects. Gabapentin is also stated to be a suitable substitute pharmacoligically and also, economically. Pregabalin is generally quite expensive.

The main advantage of Pregabalin, in my opinion, is that its bioavailability doesn't seem to fluctuate or depend upon physiological or gastric environment to exert effect. When I take Gabapentin, there is a ritual surrounding it that is pretty annoying. I have to eat a high fat meal and then split the dose up 6 times over a 3 hour period. Pregabalin, you can just swallow and enjoy.
 
Thanks for the replies.

I stopped taking pregabalin last Thursday just to test the waters. I must say, I've felt pretty shitty but nothing too difficult to manage. Moody and anxious but okay. Its made me very wary of this stuff though, I was on it for 2 weeks.

Unfortunately, the back pain is still very present and is sightly worse, but for now, I will continue treating with codeine and will take lyrica during bad patches.
 
I'm currently taking gabapentin and I too have made the decision to go to my prescriber to ask for fluvoxamine. I guess if I feel the effects of gabapentin are diminished, I should take more gabapentin?
 
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