Circumventing Gabapentin's saturation levels at LAT1 & LAT2???

[ongos]

from what someone had mentioned to me, Sabril, another anti epilepsy is actually better, pharmacologically, in working for OCD and as an overall gabaergic for OCD. If anyone know why this is, chime in!

This is an interesting topic, as I have been trying to get behind the science of these interesting acute effects of pregabalin & gabapentin that seem to be somewhat independent of the anti epileptic activity that comes with chronic use (look here). I've read about phenytoin having some interesting mentally-calming anti-obsessive effects before but I did not continue the research on it and did not try it for myself as it seemed to have too strong adverse effects.

 

[chrisincville]

First, I have zero interest in sticking gabapentin in my ass for a better high, lnao..but to each their own.

Now

:Strange that pregabalin is a schedule 5 drug...and gabapentin isn't.

Not really..pregablin has a potency approx 4x stronger than gabapentin. I guess the FDA wasn't having any of that uncontrolled...

 

[Pharmosis]

And depression is being looked into as more of a dopamine/norepinephrine problem rather than the traditional serotonin "hypothesis" of depression.

Your assertion here is slightly inaccurate. There are several different classifications of major depression. There exists a strong scientific consensus that serotonin depletion is the cause of common major depressions. For more severe major depressions, such as melancholic depression and psychotic depression, the monoamine neurotransmitter systems are thought to be strongly involved (i.e., serotonin, norepinephrine and dopamine). This is certainly not a new theory; perhaps look into the "monoamine hypothesis" of depression. Moreover, you might be unaware of the fact that sertraline (Zoloft), in addition to being a potent SSRI, is also a moderately potent dopamine reuptake inhibitor, which is probably one of the reasons why it is so effective for more severe major depressions (including melancholic depression and psychotic depression).

 

[AlphaOdure]

^^Given the myriad of questions which weren't really related to this topic.. I slightly over-glossed/over-simplified that part of my statement. I simply meant that the monoamine hypothesis is the most commonly accepted view towards treating depression. & to combine Pharmosis & nopos posts for the sake of length on this side topic: I'm aware of all the other studies going on w/ depression alternatives, the most fascinating one in my book is using several-days-a-week NMDA antagonist dosages. Ketamine in paritucular to treat AD-resistant people (i.e., ME!!) Here's the WebMD article

and major/minor/psychotic depressions make no difference here in the US w/ most doctors. They'll just up your dose, change from a serotonergic to norepinephrinergic or to the new dopaminergics or create their own cocktail of such.. etc. Then... perhaps throw in some powerful (but useless) antipsychotic that'll zap your energy, turn you into a couch potato, & make you gain 40lbs. So, to the alternative, so what if it's fucking addictive (i.e., amphetamines)- SSRIs are "dependent" inducing, no difference between the two except "addictive" means (OH FOR HEAVEN'S SAKE NO!!) it may cause some acute euphoria?

If the depression patient is among those 30-40% who doesn't respond to that traditional CRAP (me!!) w/ major depression, suicide attempt histories, etc.. why not try these methods more broadly is my view? I was put on depakote (& yes sodium valproate is the same as depakote ONGOS) along w/ abilify- when i finally got rid of that a bitch of a doctor- my new PCP looked at me like i was crazy that i was depakote for depression (had did a self taper some 6mo prior & felt no different, no worse no better- just lost 30lbs lol). Depakote he went on to is not approved for this use, nor even Rx'd off label for for depression (yet my old doc said "we're at the end of the line of meds here, next step is lithium" ...dumb bitch). Depakote is more for manic episodes, which i never even said i'd ever had (haven't talked to him about depression yet, just saw once for my referral to my pain doc for my debilitating neuropathic & traditional back pain- GREAT pain doc btw! listened.. answered questions.. gave me time.. didn't rush.. not intimidated about my knowledge of pharmaceuticals & pharmacology relative to the avg layman- plus very cute too )

& glanced over your link about phenytoin.. and as i mentioned earlier, its of no surprise to me that a lot of different antiepileptics could have different functions as they all operate through so many different pathways to help manage epilepsy & seizures. But use caution w/ certain sorts of "experimentations" as phenytoin made my uncle go blind over period of decades of use- despite this not even being listed as a rare side effect.

how is gabapentin prescribed, for what condition so that way my insurance covers it? Is it for pain? For epilepsy? I doubt it would be prescribed to me for OCD

Started out as an antiepileptic, which was how/why it was originally approved by the FDA. But i've seen neurologists in the past for seizures i got from an accidental overdose of 3-meo-pcp & asked about GBP.. & he said "its potency is so low that newer drugs are now used"- i'd say now its mostly used off label for anxiety quite often.. that & neuropathic pain- which it is quite helpful for (in both areas). I've heard of it as a "mood stabilizer"- but i don't feel qualified enough to label it as such myself, but i'm inclined to say it has potential there.

Its certainly helping stabilize my mood, but so too is daily clonazolam and/or flubromazolam. However, i take these benzos on regime- only 2-3x at night. no morning doses; & still get same anti-anxiety effects: i.e., no dysphoria around people, no physical illness/dissociation/"brain freeze" when directly interacting w/ a person. No more hiding in my basement till 4pm afraid to job search b/c of anxiety/depression issues. And furthermore, i'm SO much more active on here & other forums I had basically just dropped as of the last year or so.

 

[AlphaOdure]

First, I have zero interest in sticking gabapentin in my ass for a better high, lnao..but to each their own.

Lol.. another plugger hater.. I used to be the same way. "nothings going up there".. but when my recent IV binge brought me down so hard so fast.. i resorted to trying an alternative method of ROA, particularly for sub strips which i was given for a month rather than my typical subutex pills. & plugging them actually has a slightly higher BOA than intranasal (never did really IV bupe that much unless in combo w/ a decent amount of a benzo.. then BAM.. felt like a full agonist for an hour, but then i'd start fiending for more bupe, so limited that ROA.. as by itself caused no diff in effects except quicker come up & quicker come down).

Plugging MXP is preferable too! Along w/ GBP (as far as i'm concerned) according to my anecdotal experience & some of the great helpful evidence Kittycat5 is digging into!

One day my friend... you'll realize an attractive, young, 30 yer old heterosexual male can stick shit (no pun intended) up their butt w/o being gay lol

 

[AlphaOdure]

Ive been reading a bit and there are other transporters involved but have nothing concrete yet about which ones and where they are expressed.

And LAT1 may be saturable at the BBB despite what I said there. Reading up on that too. I will post more info when I find it.

I wasnt doubting your experience alphaodure. Just think LAT1 has little to do with it.

Oh didn't mean to come off as if you were doubting me. just wanted to reaffirm how strong this experience was compared to my previous attempts at concurrent (daily) GBP use.

Well keep up the looking in your free time hun! & feel free to post any links, even if the info is sparse. I will do my research too, but i've been pretty busy here lately. All i know is i got the same (if not greater) effects on the 3rd day of concurrent use; which was the only day i'd use one 300mg cap orally & 1 300mg cap rectally (every hour- used same method on two previous days, but w/ just 1 300mg cap orally. Same total dose all 3 days 300 x 10=3000mg).

Was smashed. Somethings going on here.. it was NOT placebo.. b/c thought i lost the "magic" for good from GBP a while ago from too often use/abuse. Now it seemed i recaptured it w/ the plug ROA? Maybe should try JUST a plug experiment next time? But gotta give it a good week or so for tolerance to go down.

 

[Kittycat5]

I couldnt find anything specifically about other transporters yet but found a small study that did administer gabapentin rectally with poor results. It is only 2 patients, they are children vs adults, the formulation may have been bad and there was some absorption so not a great reference.

http://www.ncbi.nlm.nih.gov/pubmed/9579927

Definitely try the plugging solo and let us know. I will keep reading and see what I find.

 

[atara]

as i don't tend on abusing it

If you're trying to circumvent the body's natural uptake mechanisms, you're way past "normally" using. Abuse doesn't mean that you lost your job and your house, it means the drug plays a much larger role in your life than it should.

The best way to "circumvent" your tolerance is to take a break. The next best way might be piperine.

 

[ongos]

so prega is just a concentrated form of gabapentin or what? Is the molecule entirely different but different enough to be called something else but is it in the same class of drugs then?

So all these people are saying the high is like a benzo? Is it a downer then?

First, I have zero interest in sticking gabapentin in my ass for a better high, lnao..but to each their own.

Now


Not really..pregablin has a potency approx 4x stronger than gabapentin. I guess the FDA wasn't having any of that uncontrolled...

 

[ongos]

hello?

is gabapentin a good pain killer? Does it have any action on the opioid receptor or just gaba?

 

[ongos]

Has anyone here tried Pregabalin (Lyrica)? I see different doses of 75, 100, and 300 mg. This is a schedule 5 drug in the U.S.

How is this even addicting? Is this a concentrated form of Gabapentin?

 

[aced126]

Gabapentin and pregabalin have different structures; you can go look at them on Wikipedia. I don't believe either of them have non negligible opioid action.

 

[ongos]

Seems as if prega has some close relation to GHB, which is supposedly a great antidepressant. Also, it's closely related to phenibut and baclofen. Phenibut is unscheduled and OTC.

 

[ongos]

for obsession, you guys ever tried Dilantin?

 

[ongos]

γ-Amino-β-hydroxybutyric acid (GABOB) (brand names Gamibetal, Gabomade, Aminoxan, Bogil, Diastal, Gabimex, Gaboril, Kolpo), or β-hydroxy-γ-aminobutyric acid (β-hydroxy-GABA), is an anticonvulsant which is used for the treatment of epilepsy in Europe, Japan, and Mexico.[1][2] It is also an endogenous active metabolite and analogue of the neurotransmitter γ-aminobutyric acid (GABA), and for this reason, may function as a neurotransmitter itself.[2][3][4][5] Relative to GABA, GABOB has more potent inhibitory effects on the central nervous system, perhaps due to its greater capacity to cross the blood-brain-barrier.[5][6] However, GABOB is of relatively low potency as an anticonvulsant when used by itself, and is more useful as an adjuvant treatment used alongside another anticonvulsant.[7][8] GABOB has two stereoisomers, with the (3S) isomer d-GABOB being around twice as potent an anticonvulsant as the (3R) isomer l-GABOB.[9]

GABOB (β-hydroxy-GABA) is a close structural analogue of GABA (see GABA analogue), as well as of γ-hydroxybutyric acid (GHB), phenibut (β-phenyl-GABA), baclofen (β-(4-chlorophenyl)-GABA),[10] and pregabalin (β-isobutyl-GABA).

https://en.wikipedia.org/wiki/Gamma-Amino-beta-hydroxybutyric_acid

Anyone tried this? Similar to GHB? More potent than Pregabalin yet unscheduled? Who has it?