Opioids Gabapentin and its effect on opioids

[RxVeritas]

Gabapentin is an interesting drug in my opinion. It's not metabolized via the cytochrome P450, so my initial assumption was that the slight potentiating effect that I get from taking it with kratom, suboxone, tramadol or oxycodone (although unfortunately I haven't had the resources to test that as much) would be more or less the same with other opiates, as there is no CYP3A4 component.

For context, I'm prescribed gabapentin 800mg x 3 daily, and I almost always cut the pills into quarters (or occasionally even smaller pieces) and I won't give you my whole gabapentin dosing regimen spiel, but long story short I take the prescribed amount most days, and take the majority of it earlier in the day. If I intend to use it as an opiate potentiaor I usually make sure to take a couple doses in the preceeding hour and a half or so, as well as other things, but I don't think they're relavent in this case.

Both studies and experience reports seem to indicate that, for some reason yet unbeknownst to me (although it's possible I didn't dig hard enough), gabapentin seems to have a pronounced effect on the bioavailability of hydrocodone. When gabapentin is taken one (or two? I don't recall exactly) hours before, it decreases the bioavailability of hydrocodone by something like 15%. It's also interesting that when taking gabapentin an hour after hydrocodone, apparently the bioavailabilty of the gabapentin *actually increases as well*.

A couple days ago I got a small script for Vicodin 5mg.

Now, taking into consideration that for the first half of the day I am continously dosing gabapentin (every 15-30 miniutes, depending on the specific dose and the day) it would make sense to me that taking hydrocodone at any point (exluding first thing in the morning) should lead to a decrease in bioavailibity, because of the gabapentin. To me this effect definitely seemed to be more substantial than just a placebo, as I definitely didn't feel like I was getting as much out of the hydrocodone as I have in the past, before I was taking gabapentin the way I currently do (which is OPTIMAL, and I've brought it up before so I won't do it here lol, if you're really curious just PM me lol).


I got a small script for oxycodone 5mg today, and as far as I can tell it mixes great with gabapentin the way I take it, and there is definitely potentiation, and that makes sense to me, so yay!

Does anybody know the mechanism behind hydrocodone exhibiting such a strange, highly time-dependent relationship in regards to gabapentin and the bioavailibity of both?

I'm also curious if there are other opiates that are diminished in effect after taking gabapentin, as hydrocodone seems like an anomoly in this respect, and it's really eatin' away at the back of my mind the past couple days.

Can anybody help my understand any of things?





Mods: please move this if you feel it necesary.

 

[brokedownpalace10]

I don't have an answer as to why, but I've read the same and I've experienced the same.
Always take your Gabapentin a couple/few hours after your Hydrocodone. Never before. It's a nice thing after. Right about when the hydro begins to fade, the gaba feels pretty good.

 

[RxVeritas]

I don't have an answer as to why, but I've read the same and I've experienced the same.
Always take your Gabapentin a couple/few hours after your Hydrocodone. Never before. It's a nice thing after. Right about when the hydro begins to fade, the gaba feels pretty good.

Thank you for that feedback, I appreciate it.

I've more or less scrounged bluelight for any info on this effet, and maybe I'm not searching optimally, but there doesn't seem to be much info available aside from a few studies.

A good friend of mine who's prescribed both drugs has also verified that this is the case with her.

I'm just really curious what the mechanism is behind this, and if the effect gabapentin has on hydrocodone bioavailability and vice versa is a unique mechanism that is specific to these two drugs, because every other opioid I've taken is definitely potentiated by gabapentin.

 

[brokedownpalace10]

I'm just really curious what the mechanism is behind this, and if the effect gabapentin has on hydrocodone bioavailability and vice versa is a unique mechanism that is specific to these two drugs, because every other opioid I've taken is definitely potentiated by gabapentin.

So, with the other opioids, they are potentiated even if you take the Gabapentin first?

 

[RxVeritas]

Every one that I've tried, yes, absolutely.

 

[brokedownpalace10]

Every one that I've tried, yes, absolutely.

Even Oxycodone?
Interesting, BTW.

 

[RxVeritas]

Even Oxycodone?
Interesting, BTW.

Absolutely. It's subtle for me, although I'm sure that it would probably be a lot less subtle to somebody that's not taking 2400mg of gabapentin daily.

I feel almost nothing from 800mg gabapentin tablets unless I break them into halves (quarters or more are ideal though) and stagger doses annoyingly (depending on who you are; for me, taking something every 15-20 minutes isn't an issue) often. At this point, although it's a dose I've been on for a few years at this point and it's not my first run with it. Until I got Xanax ER a few months ago, gabapentin was my primary anti-anxiety drug... which kind of sucks, because it's like 15% as good as an actual benzodiazapene, but it is a unique drug with some unique quirks and features.

It is *very* effective for relieving Restless Leg Syndrome, although that becomes somewhat of a double bladed sword when you are taking it every day.

But yeah... I cannot think of an opioid other than hydrocodone that doesn't seem to go well with gabapentin, from my experience.

Today, I took hydrocodone before taking any gabapentin and these results seem pretty repeatable to me.

Anybody out there who's way more knowledgable on this stuff and can possibly chime in?

 

[Dextro .45]

Gabapentin potentiation for Opioids…..yaaa, kinda, depending on several factors

Pregabalin (Lyrica) 300-500mg with its 90% oral bioavailability and 1.5h onset/peak serum levels in fasting conditions (empty stomach). All the Gabapentin you can take can’t even hold a candle to a FAT Pregabalin dose in a properly formulated oral Brompton Cocktail lol

The “Gold Standard” of pleasurable euphoric anxiolytic relaxation & content full bliss lol

Methadone 80mg
Ritalin 50mg IR
Valium 30mg
Pregabalin 300-400mg
Cannabis Indica 10mg

45min onset creeps in …..making by standard drink, Tanqueray Jin 3.oz in Ginger Ale, 4 icers

1 hour I’m close to peak serum levels, before heading out to patio with mixed drink to smoke a fresh Belmont cigarette I’ll blast a long thin line of oily shimmering fish scale tropane alkaloid mixed with Ketamine HCL 50/50 mix

Smoking that cigarette while enjoying that ice cold Tanqueray Jin cocktail while a laxed Bob Marley track’s playing (Mystic River) YouTube it and listen ……WOW lol

Not to forget mentioning, that Saturday morning at 10am I took 1.5g Phenibut and a 100ug standard dose tab of LSD-25 under my tongue for a full 30min until paper starts to fall apart, under the tongue is rich with blood vessels allowing the LSD to absorb directly into my bloodstream. 3 hour onset, just like Phenibut.

Such a BEAUTIFUL Sunny Saturday, outside on the patio feeling the warm rays of the Sun

GF back home at 6pm from Library work….fire up the bbq, steak, lobster tail, colossal jumbo tiger shrimp (3 in a pack for $10), juicy honey garlic sausage, red peppers, onions in butter, beer, white wine….caramalizes in the bbq and taste like sweet candy….coconut basmati rice, fresh baked Calibrese buns, crisp fresh lettuce, tomatoes, cucumbers, etc.

I cook it all to perfection. Cooking to me is like foreplay before sex. Absolutely essentail, makes your brain wet with desire and anticipation. Cooking is such an art form and Fun as F@ck. My northern Italian background and my dad in the kitchen when I was 5 years old, prep work, bbq burgers, etc. Both my parents are professional master chefs lol

When my GF and I were finished this exquisite decadent meal fit for the gods, I sat back in my chair basking in the Sun, the LSD still very apparent along with the oral Brompton Cocktail…..I calmly lit a smoke and cracked an ice hold Heineken bottle while she got up to clean everything up to a spotless condition lol.

I cook….she cleans

 

[BourbonMac]

Even Oxycodone?
Interesting, BTW.

Oxy may reduce the absorption of Gabapentin some if I remember correctly, I could've sworn I read it in a study awhile back but I can't find it anymore. Maybe it's the other way around, someone can correct me if I'm wrong.

I don't know why I can't find the study, it was something like Gabapentin absorption was reduced by 20% if taken with oxycodone, or maybe it was oxycodone absorption reduced instead. I don't recall waiting to take the gabapentin until later before though.

I think potentiate might be the wrong word either way. It's a unique synergy but it's not potentiating per say like cimetidine or white grapefruit would by increasing blood plasma, or eating something fatty after it kicks in which seems to kick it into higher gear for a lot of people, I was definitely one of them.

 

[DeathIndustrial88]

Oxy may reduce the absorption of Gabapentin some if I remember correctly, I could've sworn I read it in a study awhile back but I can't find it anymore. Maybe it's the other way around, someone can correct me if I'm wrong.

I don't know why I can't find the study, it was something like Gabapentin absorption was reduced by 20% if taken with oxycodone, or maybe it was oxycodone absorption reduced instead. I don't recall waiting to take the gabapentin until later before though.

I think potentiate might be the wrong word either way. It's a unique synergy but it's not potentiating per say like cimetidine or white grapefruit would by increasing blood plasma, or eating something fatty after it kicks in which seems to kick it into higher gear for a lot of people, I was definitely one of them.

Gabapentin reduces the absorbtion of hydrocodone.
So whatever you read might have said the same for oxycodone.

I've actually found that taking gabapentin after hydrocodone almost throws me into withdrawal from the hydros.

 

[JackARoe]

Methadone 80mg
Ritalin 50mg IR
Valium 30mg
Pregabalin 300-400mg
Cannabis Indica 10mg

45min onset creeps in …..making by standard drink, Tanqueray Jin 3.oz in Ginger Ale, 4 icers

It is Happy Hour somewhere! I am taking notes Dextro, I think you did have a cocktail recipe that had gabapentin in it. Hopefully no one in your family is in need of the true Bromptom Cocktail so I hope all is well. I notice you leave out the thorazine and spice it up with some better stuff.

Whenever I take gabapetin it is usually an hour after kratom. Not that I notice anything different but I have that in my head that gabapentin lessens morphine absorption, so in a superstitious way I make sure it does not interfere with any kratom absorption. Saying that I also have taken kratom after gabepentin but the only thing I notice is I don't need the kratom anymore once the gabapentin takes effect.

Never tried it with other real opiates like morphine or oxy. But I can see that both opiates and gabapentin (or pregabalin) would fight each other on what makes a person feel better. They feel good in their own way. But I think the thread is about absorption and what hinders and what does not.

 

[RxVeritas]

Gabapentin potentiation for Opioids…..yaaa, kinda, depending on several factors

Pregabalin (Lyrica) 300-500mg with its 90% oral bioavailability and 1.5h onset/peak serum levels in fasting conditions (empty stomach). All the Gabapentin you can take can’t even hold a candle to a FAT Pregabalin dose in a properly formulated oral Brompton Cocktail lol

The “Gold Standard” of pleasurable euphoric anxiolytic relaxation & content full bliss lol

Methadone 80mg
Ritalin 50mg IR
Valium 30mg
Pregabalin 300-400mg
Cannabis Indica 10mg

45min onset creeps in …..making by standard drink, Tanqueray Jin 3.oz in Ginger Ale, 4 icers

1 hour I’m close to peak serum levels, before heading out to patio with mixed drink to smoke a fresh Belmont cigarette I’ll blast a long thin line of oily shimmering fish scale tropane alkaloid mixed with Ketamine HCL 50/50 mix

Smoking that cigarette while enjoying that ice cold Tanqueray Jin cocktail while a laxed Bob Marley track’s playing (Mystic River) YouTube it and listen ……WOW lol

Not to forget mentioning, that Saturday morning at 10am I took 1.5g Phenibut and a 100ug standard dose tab of LSD-25 under my tongue for a full 30min until paper starts to fall apart, under the tongue is rich with blood vessels allowing the LSD to absorb directly into my bloodstream. 3 hour onset, just like Phenibut.

Such a BEAUTIFUL Sunny Saturday, outside on the patio feeling the warm rays of the Sun

GF back home at 6pm from Library work….fire up the bbq, steak, lobster tail, colossal jumbo tiger shrimp (3 in a pack for $10), juicy honey garlic sausage, red peppers, onions in butter, beer, white wine….caramalizes in the bbq and taste like sweet candy….coconut basmati rice, fresh baked Calibrese buns, crisp fresh lettuce, tomatoes, cucumbers, etc.

I cook it all to perfection. Cooking to me is like foreplay before sex. Absolutely essentail, makes your brain wet with desire and anticipation. Cooking is such an art form and Fun as F@ck. My northern Italian background and my dad in the kitchen when I was 5 years old, prep work, bbq burgers, etc. Both my parents are professional master chefs lol

When my GF and I were finished this exquisite decadent meal fit for the gods, I sat back in my chair basking in the Sun, the LSD still very apparent along with the oral Brompton Cocktail…..I calmly lit a smoke and cracked an ice hold Heineken bottle while she got up to clean everything up to a spotless condition lol.

I cook….she cleans

Completely agree with you on pregabalin. It is a very similar potentiation, or syngergy which I think may be a better word to use in this case, as somebody said earlier.

It also doesn't seem to affect the absorption or bioavailibility of hydrocodone, as far as I can tell both personally and on the internet. Don't get me wrong, I very much prefer pregabalin over gabapentin, in every aspect. I would absolutely prefer to dose once or twice a day with a drug thats many times stronger, as opposed to many, many, many times (for optimal absorption) thoughout the day. I've just never found somebody who'll prescribe me high dose benzodiazapenes and pregabalin together, although 2400mg/day gabapentin with benzos they don't seem to give a second thought.


I've never had a Brompton cocktail, at least formally, but I cannot count the number of times that I would casually mix oxycodone or heroin with amphetamine, cocaine, or methylphenidate (although I think I prefer dextroamphetamine, specifically) while taking (often more than) prescribed high doses of clonazepam and gabapentin (and occasionally illicitly acquired pregabalin) and smoking a lot of weed,

"What’s in a name? That which we call a Brompton Cocktail​

By any other name would hit as hard."​

-Shakespeare

 

[Dextro .45]

Lmao

Although 90% of all my CII controlled substances are legally prescribed due to a medical condition which chronic pain is the lifelong c@nt ….having reliable & regular access of pharmaceutical grade CII substances have it a bit more tolerable. Although is has caused me some concern

Basically, on a daily basis I orally consume a hybrid customized Brompton Cocktail…for about 10 years +

Methadone 80mg
Ritalin 50mg
Diazepam 20-30mg
Pregabalin 300mg
Indica Cannabis 10mg

All tablets pulverize is a pharmaceutical grade glass motor & pastal, add warm after to dissolve, little orange juice to mask bitter taste and drink. 30-45min to feel that warm blanket of comfort. Both Opioid & Dopaminergic stimulant euphoria combined in an oral speedball, the Valium & Lyrica to relax with their potent anxiolytic & prominent muscle relaxant properties. India cannabis & Ethanol are also original components of the Brompton Cocktail (Jin specifically)

Diacetylmorphine (Heroin) & pharmaceutical Cocaine Hydrochloride would be great, but I guess the substitutes available are VERY similar in their MOA, onset, duration of action, potency, etc

Diazepam & Diclazepam (2-Chloro-Diazepine) both synthesized by the same chemist, which is pretty cool. I have very large quantities of both. Diclazepam is very interesting in that it’s essentially a prodrug to 3 licensed pharmaceutical benzodiazepine medications currently on the market. The most significant by far being Delorazepam (licensed in Italy)

Diclazepam 1mg > Delorazepam >>Lorazepam (Ativan) - 200 hours half-life
Diazepam 10mg (a few active metabolites also licensed by themselves as anxiolytic)


Regardless after my oral Brompton Cocktail I’ll blast a line a decent Cocaine & Ketamine (50/50) mixed

LSD-25 / 100ug blotter tabs …..the most beautiful molecule ever synthesized. Every beautiful sunny Saturday I’ll place a tab under my tongue around Noon. 3 hour onset…..5-8 h of heavenly effects followed by an afterglow. Best antidepressant and spiritual & mental medicine to appreciate all of life’s beauty. Family…..friends…..Mother Nature….animals….the cosmos as a whole and our gift of life and the short time we have here on this earth (which really is heaven on earth)

It’s Saturday 9pm and I’m listening to beautiful vibe music still feeling the LSD that hit at 3pm, took affect around 6pm…….after erotic lovemaking with my GF I ingested my Brompton Cocktail so the Valium 30mg & Lyrica 300mg is slowing things down and bit

Having cigarettes out on the balcony looking at the stars, mixed drink Jin & ginger ale and a little Cocaine lol

What can I say lol

Great long weekend everyone

 

[Dextro .45]

Gabapentinoids (gabapentin/pregabalin/maybe Baclofen) inhibit the release of excitatory neurotransmitters in the CNS. Dopamine, Norepinephrine, Substance P, Acetylcholine, Glutamate

Starting using oral Methylphenidate (Ritalin) would give me SIGNIFICANT Euphoria and a dopaminergic pleasurable experience. I then started taking Gabapentin and would notice the Ritalin would be be so pleasurable (and not due to tolerance)….just like this medical journal stated….this Gabapentin would inhibit the release of dopamine and all those stimulating feel good neurotransmitters

Just an interesting observation…..I backed off Gabapentin.

Phenibut is a totally different GABA analog….which releases dopamine too

Cocaine & Ritalin (Methylphenidate) are nearly identical in their MOA
Amphetamines (Dexedrine, Adderall, Vyvanse, Desoxyn) are a whole different story

I like an oral Speedball first …..then anxiolytic benzos, GABA analog, etc