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Why does valproate cancel out pregabalin?

plumbus-nine

plumbus-nine

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Ok, for about a week I've been taking valproate magnesium now, titrated up to 800mg/d, only effect so far was nausea when upping the dose, but otherwise absolutely nothing. Because of frustration with that I bought pregabalin and used the box of 28x 150mg = 4.2g within three days, yesterday was about 2g, today one gram, next to no effects when usually after a period of abstinence pregab works, not how it did the first times but nice enough for to take it here and there. But now really nothing besides a little calmness as expected from a mood stabilizer but for the excessive dosages taken effects should be more.

So what's the interaction behind valproate + pregabalin? Anybody a hunch?
 
you talking valproic acid? There's an very interesting thread about how gabapentinoids in general make all other Euphoria producing drugs less likely to do so
 
darvocet21 said:
you talking valproic acid? There's an very interesting thread about how gabapentinoids in general make all other Euphoria producing drugs less likely to do so
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Yeah, it's valproic acid + Mg, more common seems to be sodium valproate but it's the same active compound.

Do you have a link to this thread?
But weird, I experience the opposite, that valproic acid cancels the euphoria and stimulation from pregabalin ... usually do drugs work for me even when on pregab but I don't use it regularly anymore because I get complete tolerance, no more effects besides some cognitive limitation with 600mg/d. Taken at once they give slight effects, with 900+mg more effects and now 2g in short time w/o anything.

My theory is that pregabalin stimulates something which valproic acid blocks, I once had seizures from too much pregabalin (it was also around 2g! possibly 2.3) so it makes some sense. First suspect might be glutamate, I read that gabapentinoids in high dosage block glutamate transporter 1 thus the stimulation ... now it can't be at this transporter but that valproate blocks channels which are necessary for pregab euphoria.
 
plumbus-nine said:
Yeah, it's valproic acid + Mg, more common seems to be sodium valproate but it's the same active compound.

Do you have a link to this thread?
But weird, I experience the opposite, that valproic acid cancels the euphoria and stimulation from pregabalin ... usually do drugs work for me even when on pregab but I don't use it regularly anymore because I get complete tolerance, no more effects besides some cognitive limitation with 600mg/d. Taken at once they give slight effects, with 900+mg more effects and now 2g in short time w/o anything.

My theory is that pregabalin stimulates something which valproic acid blocks, I once had seizures from too much pregabalin (it was also around 2g! possibly 2.3) so it makes some sense. First suspect might be glutamate, I read that gabapentinoids in high dosage block glutamate transporter 1 thus the stimulation ...
Click to expand...

Shouldn't gabapentin attenuate the effects of other drugs?

"Gabapentin increases non-synaptic GABA responses from neuronal tissues in vitro. In vitro, gabapentin reduces the release of several mono-amine neurotransmitters." Shouldn't this mean that gabapentin should reduce euphoria from stimulants/opioids? https://pubmed.ncbi.nlm.nih.gov/9686247/...
bluelight.org bluelight.org
 
I haven't read all the posts but the reason I like @Fiori di Bella 's nickname Gabba goo is that I've never enjoyed Neurontin except for like sleep but it doesn't even it's not like half as strong as Seroquel
 
darvocet21 said:
I haven't read all the posts but the reason I like @Fiori di Bella 's nickname Gabba goo is that I've never enjoyed Neurontin except for like sleep but it doesn't even it's not like half as strong as Seroquel
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Never did gabapentin, I might try it in future to compare because I read that it's a bit different and not just a less potent variant with a ceiling effect but overall it appears inferior... Pregab doesn't make me tired, just the first 300mg's were like being drunken. Seroquel definitely is stronger for sleep.. I like zopiclone but it's prescription so limited supply.
 
plumbus-nine said:
Never did gabapentin, I might try it in future to compare because I read that it's a bit different and not just a less potent variant with a ceiling effect but overall it appears inferior... Pregab doesn't make me tired, just the first 300mg's were like being drunken. Seroquel definitely is stronger for sleep.. I like zopiclone but it's prescription so limited supply.
Click to expand...
What with Zopi cornering the market?
 
darvocet21 said:
What with Zopi cornering the market?
Click to expand...
Well here in MX most meds are freely available but everything benzo-like, ketamine and antibiotics are prescription while opioids and stimulants are controlled (scheduled), requiring a special numbered prescription. Now problem is people rarely use the controlled things, they don't stock what people don't request often and nobody is willing to order for you, so it's a doctor and pharmacy odyssey to find what you want. At least pregabalin and memantine are abundant. For testosterone I had no luck so far. Even dextromethorphan in pills is rare, only syrup with 300mg/bottle.

With limited supply I meant that docs know it's only for temporary use and won't do repeated scripts unless you find somebody who is open for money...

Checked DNMs but little domestic offers, mainly DMT which I could extract myself when I feel ready for it. Found somebody selling ket vials w/o prescription but for a high price specially given the usual low prices of most things here.

Reading the linked thread, thanx!
 
plumbus-nine said:
Well here in MX most meds are freely available but everything benzo-like, ketamine and antibiotics are prescription while opioids and stimulants are controlled (scheduled), requiring a special numbered prescription. Now problem is people rarely use the controlled things, they don't stock what people don't request often and nobody is willing to order for you, so it's a doctor and pharmacy odyssey to find what you want. At least pregabalin and memantine are abundant. For testosterone I had no luck so far. Even dextromethorphan in pills is rare, only syrup with 300mg/bottle.

With limited supply I meant that docs know it's only for temporary use and won't do repeated scripts unless you find somebody who is open for money...

Checked DNMs but little domestic offers, mainly DMT which I could extract myself when I feel ready for it. Found somebody selling ket vials w/o prescription but for a high price specially given the usual low prices of most things here.

Reading the linked thread, thanx!
Click to expand...
You're welcome oh and by the way I once went to Mexico and all I could get was nalbuphine
 
darvocet21 said:
You're welcome oh and by the way I once went to Mexico and all I could get was nalbuphine
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Interesting, in which part of the country did you go? I heard that pharmacies near the border sell more stuff because of travelers asking for them, possibly even without prescription for a bit more, or you visit the free doc next door.. while here in City people mostly only ask for the usual suspects like paracetamol etc.. Didn't find an online pharmacy yet, just a webpage from a border pharmacy specialized for steroids...

Importing seems to be tricky, you need to be lucky, know somebody to pay, or import yourself in person ... otherwise they stop it and want clearing papers which you can't get as an individual.

But nalbuphine is interesting. What year was it? The legislation changed afaik recently, enforcing prescription for opioids and stimulants.
 
plumbus-nine said:
Interesting, in which part of the country did you go? I heard that pharmacies near the border sell more stuff because of travelers asking for them, possibly even without prescription for a bit more, or you visit the free doc next door.. while here in City people mostly only ask for the usual suspects like paracetamol etc.. Didn't find an online pharmacy yet, just a webpage from a border pharmacy specialized for steroids...

Importing seems to be tricky, you need to be lucky, know somebody to pay, or import yourself in person ... otherwise they stop it and want clearing papers which you can't get as an individual.

But nalbuphine is interesting. What year was it? The legislation changed afaik recently, enforcing prescription for opioids and stimulants.
Click to expand...
Nogales
 
Magnesium makes it harder for your body to absorb gabapentin, which is already not greatly absorbed anyway. We're talking at least 50% reduction in bioavailability from a standalone 300mg dose (at once of course, assuming stagger). Always wait at least 2-3 hours before or after gabapentin to use anything with magnesium in it.
 
BourbonMac said:
Magnesium makes it harder for your body to absorb gabapentin, which is already not greatly absorbed anyway. We're talking at least 50% reduction in bioavailability from a standalone 300mg dose (at once of course, assuming stagger). Always wait at least 2-3 hours before or after gabapentin to use anything with magnesium in it.
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Well I snorted the pregabalin, even when this route won't bring benefits over oral, bad habits die hard. But it should avoid this reduction in BA?
 
BourbonMac said:
Snorting preg is already significantly less bioavailable, but yes, it would still result in reduction even if you snorted it.
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Interesting. Do you have an explanation for this phenomenon? Usually nasal BA is at least same if not higher than oral.
 
From some mod on the gabagoodness sub: "
Both gabapentin and pregabalin are only absorbed through your intestines. Everyone who says they snort them and get stronger effects are falling under the placebo spell. They do still get high but it's all from the drip lol.

They need to be absorbed and transported by LAT1 which is done through the intestines. However there's other ways pregabalin is transported which I'm currently researching. LAT1 seems to be the main one from what I've read."
 
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