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Misc Insufflating combo Neurontin (Gabapentine) 600mg+Reboxetine (Edronax) 4mg. What to expect? Also combining with Klonopin 4mg and Valium 20mg. Same ROA.

Hyperfocus_Flow_Oddball

Hyperfocus_Flow_Oddball

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Well, the title sais it all...
I feel the Edronax 4mg is a bit too low a dose, though overall, tried this today for the 1st time, rather fine & synergetic effects up until now...

Anything I can do to get more adrenergic effect from the sNRI?

Thx&Grtz.
đź‘˝
 
Hey there. I'm not incredible familiar with it, but I understand that Edrononax (Reboxetine) is an antidepressant. It's not really the kind of drug that a person would use for recreational effects. Like most other antidepressants, I'm sure it affects the other drugs you're using to some extent. For what we're discussing here though, I don't think it's something that we can discuss easily. It's much easier for us to take a psychoactive substance like Gabapentin (Neurontin) and tell you how it might or might not affect you. Antidepressants are more subtle and their effects are often only realized following long-term treatment.

Gabapentin (Neurontin) is not something that needs to be insufflated. It is ultimately going to need to be processed in your gut to become active. There is a very specific "transporter" system that is found in your intestines that ultimately processes the Gabapentin. If you are feeling effects following insufflation, it's likely that this is just the substance dripping down your throat and then entering circulation in the normal way.

Benzodiazepines like you've mentioned here are going to sedate you. They will likely reduce feelings of tension and anxiety, while also contributing to an overall more lethargic feeling, especially at the doses listed here and in conjunction with Gabapentin.

Gabapentin and for that matter, Gabapentinoids in general are not "sedatives" per se, though when they are used in conjunction with other sedattives/depressants like Alcohol or Benzodiazepines, they seem to contribute to a greater level of intoxication. On the flip side, Gabapentin's effects are sometimes described as energizing. When in a cocktail with other depressants though, they more often just lead to a greater level of intoxication.
 
The reason I said that gabapentin may be worth insufflating is because there’s two research papers looking at nanoemulsion and nanoparticle aided nasal administration. Of course, snorting gabapentin powder is not the same as these nano delivery mechanisms, but the fact that they are working on these nasal methods and find them to be more effective than oral, is worth noting. Gabapentin does not need to be metabolised by the body to be active, so theoretically it could very well be stronger nasally. And gabapentin does not have great oral bioavailability to begin with. Plus, it’s water soluble.

I have not tried this myself, but I will.
 
Hey @fairnymph I hope you don't think I was challenging you on that. Everything that I've every learned about Gabapentin has told me that it must be absorbed by a certain protein transporter found within the intestines.


Gabapentin is absorbed from the intestines by an active transport process mediated via an amino acid transporter, presumably, LAT2.[93] As a result, the pharmacokinetics of gabapentin is dose-dependent, with diminished bioavailability and delayed peak levels at higher doses.

I've actually spent a lot of time learning about Gabapentin. I've always been curious about it due to its relatively odd pharmacology/pharmacokinetics. You mention the oral bioavailability being poor. The oral Bioavailability of Gabapentin is 80% at 100mg which is pretty decent for an orally administered drug. The bioavailability drops significantly as higher dosages are used. This is what has led to the common practice of "staggering doses". The specific amino acid transporter LAT2 becomes saturated easily. To counter this, doses are administered in a staggered manner, in the hopes that the transporter will not become overloaded and the drugs essentially wasted.

I understand that there are other forms of Gabapentin like Gabapentin Enacarbil that have different pharmacokinetics designed to counter this transporter saturation. It's possible that these different preparations you're mentioning, like the aforementioned Gabapentin Enacarbil, are engineered with a mechanism (like you've described) that would differentiate them from the pharmaceutical Gabapentin that we know and love. However, as we are talking about the commonly-available, standard Gabapentin, then it seems that it would need to be absorbed by that LAT2 transporter in the intestines.

Anyway, I'm unable to find anything that implies that Gabapentin itself can be absorbed through any means other than this transporter which is found in the intestines.

You are correct regarding Gabapentin not undergoing significant metabolism though. It's mostly excreted as unchanged drug if it's not absorbed.
 
As I understand it Gabapentin indeed metabolizes enzymatically - but like you said very specific targetting - in the liver. It definitely works sedating, since it binds to the Gaba-receptors in the brain.

However, by bypassing that specific metabolisation in the liver, it should enhance the insufflation of Erdonax, the uttermost controversial called an atypical "antidepressant", however trials have shown it has no actual antidepressive effects at all (115% placebo were more effective ratio-wise than Erdonax). Erdonax is used for ADHD as replacement for Amphetamines and those kind of derivates.

Erdonax is only very minimal selective and a purely Norepinephric and when used in higher doses or when insufflated not only an adrenergic but dopaminergic CNS stimulant as well. By insufflation the liver gets bypassed and on researchgate.net as wel as via pun -and chemnet I found studies stating the adregenergic CNS stimulation should be instant (of course I use instant here inversely in prĹŤportio to "kicking in" after some days of use.

It would have no affinity with 5-HT whatsoever...

Am I mistaken here?

I am a long time polyabuser who always thinks "nah. This will not do it" instead of "woohoow, let's get fucked up", and never before placebo effects had - as far as I am aware of this - any power over me: in fact au contraire to it!

Yet I swear, definitely after having insufflated a 2nd 4mg Erdonax, I for sure had - even rather intense for such small dosages - stimulating and mood-boosting effects...

So, what do you guys think about this...? That Neurontin is widely abused intranasally is a very well known fact actually, I mentioned the Gabapentine insufflation (as well as what benzo insufflation obviously does) only to ask about the drug interaction with insufflating Erdonax.

It is specifically Erdonax by insufflation as ROA I want to learn more about an sich then - interactions aside for a moment.

The bioavailability of Erdonax is high though via oral ROA, it would be >=97-98%... but the slow onset would greatly diminishes as well as negatively alter the recreational effects, right?

Thank you for your input so far all of you, friendly grtz.

đź‘˝
 
@Keif' Richards

Not at all, rather I wanted to clarify and discuss, so I appreciate your thoughtful replies.

LAT2 is found in not just the intestine but also the blood-brain barrier and the brain. See here. Gabapentin can cross the blood brain barrier via LAT1, too. See here.

Oral bioavailability isn’t bad at low doses, true, but as higher doses are usually needed, bioavailability drops substantially, even with staggered doses.

So given all that plus the research on nasal administration of gabapentin (even if it is with nanotechnology, that could be largely if not solely for patent purposes), I maintain that insufflation could be worthwhile. Hypothetically.

100mg snorted appears to have had no real effect, but I don’t believe I’ve ever done less than 400mg orally. I’m going to try another 100mg.
 
Hyperfocus_Flow_Oddball said:
As I understand it Gabapentin indeed metabolizes enzymatically - but like you said very specific targetting - in the liver. It definitely works sedating, since it binds to the Gaba-receptors in the brain.

However, by bypassing that specific metabolisation in the liver, it should enhance the insufflation of Erdonax, the uttermost controversial called an atypical "antidepressant", however trials have shown it has no actual antidepressive effects at all (115% placebo were more effective ratio-wise than Erdonax). Erdonax is used for ADHD as replacement for Amphetamines and those kind of derivates.

Erdonax is only very minimal selective and a purely Norepinephric and when used in higher doses or when insufflated not only an adrenergic but dopaminergic CNS stimulant as well. By insufflation the liver gets bypassed and on researchgate.net as wel as via pun -and chemnet I found studies stating the adregenergic CNS stimulation should be instant (of course I use instant here inversely in prĹŤportio to "kicking in" after some days of use.

It would have no affinity with 5-HT whatsoever...

Am I mistaken here?

I am a long time polyabuser who always thinks "nah. This will not do it" instead of "woohoow, let's get fucked up", and never before placebo effects had - as far as I am aware of this - any power over me: in fact au contraire to it!

Yet I swear, definitely after having insufflated a 2nd 4mg Erdonax, I for sure had - even rather intense for such small dosages - stimulating and mood-boosting effects...

So, what do you guys think about this...? That Neurontin is widely abused intranasally is a very well known fact actually, I mentioned the Gabapentine insufflation (as well as what benzo insufflation obviously does) only to ask about the drug interaction with insufflating Erdonax.

It is specifically Erdonax by insufflation as ROA I want to learn more about an sich then - interactions aside for a moment.

The bioavailability of Erdonax is high though via oral ROA, it would be >=97-98%... but the slow onset would greatly diminishes as well as negatively alter the recreational effects, right?

Thank you for your input so far all of you, friendly grtz.

đź‘˝
Click to expand...
The liver is not involved in gabapentin metabolism. Gabapentin does not need to undergo any metabolism to be active.

I highly doubt that reboxetine can be recreational, especially as someone who has taken it for therapeutic reasons without any significant effect. Norepinephrine alone just isn’t very fun, and if anything is likely to be un-fun. Even if insufflation did result in more rapid onset, I doubt there would be a point to it. But I haven’t tried snorting it.

When you snorted it before, it was on its own, not combined with any other drugs?
 
Snorted another 100mg, still nothing. Then eventually I took the last 200mg orally. It’s possible I didn’t hit the right threshold dosage until I took the last, oral dose, but so far I’m not convinced snorting had any benefit. I’ll try again sometime with a full 400mg all at once.
 
fairnymph said:
The liver is not involved in gabapentin metabolism. Gabapentin does not need to undergo any metabolism to be active.

I highly doubt that reboxetine can be recreational, especially as someone who has taken it for therapeutic reasons without any significant effect. Norepinephrine alone just isn’t very fun, and if anything is likely to be un-fun. Even if insufflation did result in more rapid onset, I doubt there would be a point to it. But I haven’t tried snorting it.

When you snorted it before, it was on its own, not combined with any other drugs?
Click to expand...
I insufflated 600mg Gabapentine. 4mg Klonopin. 10mg Valium (Diazepam). 4mg Reboxetine. All in 1 go.
 
Okay, so all research I did turnes out to be exactly as it is.

This morning at 8AM I took 2*Gabapentine=600mg via oral ROA+1*Reboxetine=4mg also via oral ROA and I simply fell asleep...

(I am a ND individual - not a singularity here I know - diagnosed with Aspergers syndrome, OCS, C-PTSD, Generalized anxiety&panic disorder and ADHD.

About 15min ago I insufflated 600mg Gabapentin+4mg Reboxetine+2mg Klonopin, and now I feel very euphoric and have all the desired synergetic effects and way more powerful.

I insufflated every drug with 15min intervals to check out each ones effects. I started with the 4mg Reboxetine and believe you me, it was a noradregenrgic+dopaminergic synergetic CNS stimulatory result with a significant moodlift.

Quod Erat Demonstrandum!

Grtz.

đź‘˝
 
Okay @fairnymph I think we are on the same page now. I read some of the references you threw out there. Based on what I read, it seems possible that the drug could be administered by the insufflation route. Maybe at some point we will see a drug like that on the market. For now though, my personal opinion is that the oral route is the most practical way of administering the drug.

Another odd thing about Gabapentin, is that it's bioavailability is increased when there is food in the stomach, preferably a fatty meal. The presence of food can be enough to double the amount of Gabapentin that is absorbed. It's a pretty unusual substance in many ways.
 
This afternoon i staggered 600mg, 900mg, 600mg, 900mg, and 1500mg of Gabapentin, orally. I can not even imagine the horrible taste of doing this drug intransally. Better off swallowing it, eating a light meal and continue to stagger up.
 
Not sure what end goals are but a lot of info so far and some very interesting stuff too.

Reboxetine being an anti depressant I have no input as I have never tried or used them.

The 2 benzo are like 90% or close in oral bioavailability. So not going down that route.

Gabapentin staggered for me depending on the dose staggered will also change the time I wait between staggering and within 3-4 hrs of staggering I'm well gabbed up dep3nding on dose and where I wanna be.

But this combo looks like you just want to knock yourself into coma, j/k but sleep is all I can see you gonna get out this.

Interesting info on the intranasal part and also can vouch for fatty meals before taking it. Does help.
 
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