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Opioids that have NMDA antagonist effects

cdin said:
www.ncbi.nlm.nih.gov

Opioid Receptor Antagonism Attenuates Antidepressant Effects of Ketamine

In addition to N-methyl D-aspartate receptor antagonism, ketamine produces opioid system activation. The objective of the study was to determine if opioid receptor antagonism prior to administration of intravenous ketamine attenuates its acute antidepressant ...
www.ncbi.nlm.nih.gov www.ncbi.nlm.nih.gov
it's not an opioid antagonist. but naloxone does negate the anti-depressant effects, so if anything, ket downstream activates mu in some way that is part of the anti-depressant effect. i have used them together a lot. it's fine assuming your tolerance/everything is in line.
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Yea it says mu antagonist on wiki.
 
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The Holy Quadruplty said:
Promethazine that I take, but am out right now, has anticholinergic, and NMDA effects forsure. It gives strong deliriant, and dissociative effects, but doesn't work on AMPA receptors tho.
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My understanding is that any NMDA antagonist has indirect AMPA promoting effects because there are NMDA autoreceptors being blocked as well, what causes an increase in glutamate output and thus more AMPA activity.

But I had high hopes for AMPAkines like unifiram and when I had the chance to try that, it disappointed me. Not that super-cognition I imagined. But maybe I've under-dosed it, don't remember how much I took, just that it was pretty expensive.

Interesting that promethazine is an NMDA antagonist. Maybe that's why the opioid folks love it?
 
The Holy Quadruplty said:
It looks like there is Magnesium Stearate in the Subutex pills I take. I wonder if it's enough to have effects. I also wish I knew how strong of a NMDA antagonist Buprenorphine is, and if I actually get any NMDA antagonist effects from Subutex, or not?
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Nah stearate is in most pills, a way of letting it break down into your body better or something like that (actually it appears it delays breakdown in something I'm reading?). There's multiple reasons why it might be there. If this was someone's only source of magnesium in their diet they'd become severely deficient to say the least, it's such a tiny amount. It's not nutritionally enough to matter, always go for Glycinate or L-Theronate though the former is better for anxiety and muscle tension since Glycine is great stuff. The latter will also relax muscles as this is something magnesium just does, but it isn't sedating like Glycinate and some people find it has nootropic effects. These are the 2 best as far as I'm concerned although I've found citrate can have great muscle relaxation too and helps with constipation.

Personally it never gave me the runs like it seems to for many, so I just tend to recommend the other two. The first form I ever tried was Citrate in this brand of gummies "Calm." Citrate is just the only other form that isn't an extreme laxative like Oxide is, and Oxide is the most commonly found form in just about any store, often not said right on the front of the label leading many people to discomfort. A friend of mine was shitting and puking at the same time on this stuff and to top it all off, it has horrible bioavailability. It's like 5% whereas Glycinate for instance is probably around 70%, 80%. Citrate is also well absorbed, the gummies I found relaxed my muscles even more actually and I can't figure out why, citrate capsules at the same amount won't do this for me. Maybe it's more bioavailable when eaten since not even the dissolvable powder form of Calm worked like the gummies did. Buying these to potentially potentiate kratom is how I found out I'd had a deficiency, as I was experiencing periods of psychosis for awhile and suddenly without any idea, within 45 minutes of eating a few of them it was like I could see clearly again. Everyone could notice I seemed more alert, and there I was just expecting to potentiate my next dose of kratom.
 
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Btw I heard that NMDA antagonist lower the effect of THC, or block the cannabinoid receptors. I'm not sure if that's true, or not, but I hope not I love weed! I don't do any NMDA antagonist regularly unless Buprenorphine is, but sometimes I do some DXM for the NMDA antagonist effects, and only tried Ketamine once a long time ago. I only did one little bump I think, and the only thing I can remember is that it felt weird to walk. Lol I didn't know anything about NMDA receptors back then, or much about Ketamine at that time either. I would love to do some right now, but I never hear of Ketamine. I can only get Meth that I know of even tho I've done it a few times I don't prefer to do Meth, and probably won't again. I actually threw some out the car window last time I bought it, but wish I would have saved it incase I ever needed it for something that takes a lot of energy, and that I don't feel like doing. I kinda want to get some Adderall I think I can get them, and sometimes I can get Valium, Klonopin, real Xanax although I take Xanax everyday I was prescribed it (I have a bunch left over still), Gabapentin, and Somas. I wish I knew what Lyrics was the time my friend's mom gave me some, and then we fucked that night. Lol I was trying to say that's all I can get tho, because I was also trying to say everything I take now I get from the pharmacy (besides the over the counter stuff) legally instead of buying stuff off the streets like I used to. There's no way I'd be alive if it wasn't for Buprenorphine, and being able to be prescribed to it in the form of Subutex only!
 
I don't think that's so, I use cannabis every night and magnesium almost every night and haven't noticed this. Some people prone to anxiety from THC have reported taking magnesium an hour or so before smoking alleviates it though. This is likely just due to the regular anti-anxiety effects magnesium (particularly glycinate) have. I haven't heard of and can't find anything about it reducing absorption of THC.
 
BourbonMac said:
I don't think that's so, I use cannabis every night and magnesium almost every night and haven't noticed this. Some people prone to anxiety from THC have reported taking magnesium an hour or so before smoking alleviates it though. This is likely just due to the regular anti-anxiety effects magnesium (particularly glycinate) have. I haven't heard of and can't find anything about it reducing absorption of THC.
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Yea I read it somewhere, but can't remember where at the moment. If I find it I'll share it!
 
BourbonMac said:
Nah stearate is in most pills, a way of letting it break down into your body better or something like that (actually it appears it delays breakdown in something I'm reading?). There's multiple reasons why it might be there. If this was someone's only source of magnesium in their diet they'd become severely deficient to say the least, it's such a tiny amount. It's not nutritionally enough to matter, always go for Glycinate or L-Theronate though the former is better for anxiety and muscle tension since Glycine is great stuff. The latter will also relax muscles as this is something magnesium just does, but it isn't sedating like Glycinate and some people find it has nootropic effects. These are the 2 best as far as I'm concerned although I've found citrate can have great muscle relaxation too and helps with constipation.

Personally it never gave me the runs like it seems to for many, so I just tend to recommend the other two. The first form I ever tried was Citrate in this brand of gummies "Calm." Citrate is just the only other form that isn't an extreme laxative like Oxide is, and Oxide is the most commonly found form in just about any store, often not said right on the front of the label leading many people to discomfort. A friend of mine was shitting and puking at the same time on this stuff and to top it all off, it has horrible bioavailability. It's like 5% whereas Glycinate for instance is probably around 70%, 80%. Citrate is also well absorbed, the gummies I found relaxed my muscles even more actually and I can't figure out why, citrate capsules at the same amount won't do this for me. Maybe it's more bioavailable when eaten since not even the dissolvable powder form of Calm worked like the gummies did. Buying these to potentially potentiate kratom is how I found out I'd had a deficiency, as I was experiencing periods of psychosis for awhile and suddenly without any idea, within 45 minutes of eating a few of them it was like I could see clearly again. Everyone could notice I seemed more alert, and there I was just expecting to potentiate my next dose of kratom.
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It doesn't just say stearate as an active ingredient in the Subutex pills (the ones that say 54 411on them). It says Magnesium stearate as an active ingredient.
 
The Holy Quadruplty said:
Yea it says mu antagonist on wiki.
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right, but look at how high that binding value is -- that is a very weak action, if anything it's working to potentiate in the same kind of way that ultra low dose naltrexone does -- tiny bits of antagonism prune receptors back and make the opioids work better and make it easier to come off. there was a formulation called oxytrex that should have made it to market -- the fucking sacklers kiboshed it when they realized it had a WAY lower retention rate than the straight oxycodone. you can look it up, empire of pain is a good book about this.
 
Yes, methadone has fair NMDA antagonist activity, that's why it's such a fucking good painkiller. Unfortunately, in most people's (ignorant) eyes, it has the junkie stigma attached to it...
 
The Holy Quadruplty said:
Promethazine that I take, but am out right now, has anticholinergic, and NMDA effects forsure. It gives strong deliriant, and dissociative effects, but doesn't work on AMPA receptors tho.
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Promethazine is one of the first antipsychotics, marketed by Rhone-Pholec, in the late 40s. It was superceded by other drugs, but still has useful sedative qualities. I had an argument with a psychiatrist, when I got sectioned after my wife's death. She kept insisting it was an antihistamine. A quick scribble to show it's phenothiazine skeleton, followed by references to shut her up worked (also made staff well wary of me, apparently!)
 
fastandbulbous said:
Promethazine is one of the first antipsychotics, marketed by Rhone-Pholec, in the late 40s. It was superceded by other drugs, but still has useful sedative qualities. I had an argument with a psychiatrist, when I got sectioned after my wife's death. She kept insisting it was an antihistamine. A quick scribble to show it's phenothiazine skeleton, followed by references to shut her up worked (also made staff well wary of me, apparently!)
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It's an antihistamine, antipsychotic, anticholinergic, and more!
 
cdin said:
right, but look at how high that binding value is -- that is a very weak action, if anything it's working to potentiate in the same kind of way that ultra low dose naltrexone does -- tiny bits of antagonism prune receptors back and make the opioids work better and make it easier to come off. there was a formulation called oxytrex that should have made it to market -- the fucking sacklers kiboshed it when they realized it had a WAY lower retention rate than the straight oxycodone. you can look it up, empire of pain is a good book about this.
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Do you know of any other books about "drugs"?
 
The Holy Quadruplty said:
It doesn't just say stearate as an active ingredient in the Subutex pills (the ones that say 54 411on them). It says Magnesium stearate as an active ingredient.
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Yeah I'm implying magnesium stearate, since I go on to talk about it not being a nutritional form of magnesium. It's in active ingredient in the vast majority of pills out there.
 
The Holy Quadruplty said:
It looks like there is Magnesium Stearate in the Subutex pills I take. I wonder if it's enough to have effects. I also wish I knew how strong of a NMDA antagonist Buprenorphine is, and if I actually get any NMDA antagonist effects from Subutex, or not?
Click to expand...
Magnesium stearate is likely near non-bioavailable.

Magnesium sits in the channel of NMDA type receptors glutamate, preventing them from allowing calcium into the cell until AMPA type glutamate receptors on the same cell are activated, which raises the voltage potential of the cell and knocks the magnesium out of the channel. It doesn't block NMDA channels like classic NMDA antagonists, which bind inside of the channel and block opening regardless of voltage.

Buprenorphine is not an NMDA antagonist. It is however a kappa opioid antagonist, which causes it to feel different than other partial agonists at the mu opioid receptor.

Gabapentenoids bind to calcium channels containing alpha2 delta subunits, and inhibit their activity. There are many other calcium channels in the brain.
 
fastandbulbous said:
Promethazine is one of the first antipsychotics, marketed by Rhone-Pholec, in the late 40s. It was superceded by other drugs, but still has useful sedative qualities. I had an argument with a psychiatrist, when I got sectioned after my wife's death. She kept insisting it was an antihistamine. A quick scribble to show it's phenothiazine skeleton, followed by references to shut her up worked (also made staff well wary of me, apparently!)
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"In 2009, the US Supreme Court ruled on a product liability case involving promethazine. Diana Levine, a woman with a migraine, was administered Wyeth's Phenergan via IV push. The drug was injected improperly, resulting in gangrene and subsequent amputation of her right forearm below the elbow. A state jury awarded her $6 million in punitive damages. " Wikipedia

Apparently injecting promethazine is not a good idea. Just decided to share this for the sake of harm reduction.
 
fastandbulbous said:
Yeah, it's shite (Jack of all trades, master of non)
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Idk about that, because I've had some of the best feelings of my life on Promethazine mixed with an opioid, and benzodiazepines. I've done pretty much every drug there is too, and in many different strengths/combinations.
 
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