Agmatine for opioid taper and dependency

[Ligaturd]

I searched and found a few threads on this from years ago and was wondering if anyone had tried it and if it had worked for them. Animal studies found it potentiated morphine and lowered dependance as well as tolerance levels, or at least hindered tolerance development. It having analgesic effects on it's own. Mice were implanted with 75mg morphine pellets and after 3 days were injected with either saline or agmatine, an hour later they were all injected with naloxone to induce withdrawal. The mice who were administered Agmatine were fine and didn't enter into a precipitated withdrawal state while the other mice did.

The implications of this are fascinating although in threads that I had read through, a few were worried about it's ability to cross the BBB. Not being able to find any success stories also makes me wonder if this will be a fruitless endeavour as well. Anyways, if anyone has happened to try it I would be curious to hear the results as I will be utilizing it while on my Suboxone taper.

 

[dopamimetic]

Bodybuilders are using this all over, so either you have to do megadoses, or it's really about not crossing the BBB in human. It's a putative endogenous neurotransmitter btw. No way this could counter naloxone imo.

But for you, I'd suggest to look up about memantine. It can and does work greatly to get people off opioids, is proven to keep tolerance down and withdrawal away, there are even some papers (although no one appears to be interested in real world studies) about... really strange that nobody uses it. It is very safe, easily available too...

 

[Weltmeister]

Agmatine has a LogP of -1.0 to -1.2 (http://www.drugbank.ca/drugs/DB08838) so i dont think it can cross the BBB too well.

 

[aced126]

Agmatine has a LogP of -1.0 to -1.2 (http://www.drugbank.ca/drugs/DB08838) so i dont think it can cross the BBB too well.

Good point. However this doesn't explain the results reported in the original post. Diffusion is not the only way compounds can cross into the brain. Amino acids including 5-HTP are actively transported across by amino acid transporters. This won't take place here. However, agmatine functions as a neurotransmitter and binds to a variety of receptors. Having said that, it is synthesised in the brain itself which suggests that the brain doesn't actively uptake it from outside the brain.

That still doesn't explain the experiment conclusions in the original post however.

 

[Weltmeister]

So it does cross the blood brain barrier. At least in monkeys. Maybe theres a transporter for it ?

The question of whether agmatine crosses the blood-brain barrier has not been directly addressed, even though peripheral injection of this compound has produced behavioral responses in drug withdrawal, antidepressant, and anti-anxiety paradigms. Two models were used in this investigation. In the first, mice were injected intraperitoneally (i.p.) with agmatine (10, 50, or 300 mg/kg body weight) or arginine (600 mg/kg). After 1 or 3 hours, the animals were killed under gas anesthesia by perfusing their brains with ice-cold saline, and whole-brain agmatine was measured by HPLC. In parallel studies, a rhesus monkey was injected under gas anesthesia either intravenously (i.v.) with agmatine (30 mg/kg) or arginine (150 mg/kg), or intracerebroventricularly (i.c.v.) with agmatine (0.3 mg/kg i.c.v.). At varying times thereafter, cisterna magna cerebrospinal fluid (CSF) and blood plasma were collected and analyzed for agmatine levels. A rise in mouse brain agmatine was apparent after doses of 50 and 300 mg/kg i.p. Monkey CSF agmatine peaked in parallel with plasma agmatine 15 minutes following intravenous (i.v.) agmatine injection and at one sixth the level of the plasma peak. Monkey CSF agmatine peaked 43 minutes after i.v. arginine injection. The ventricular injection of agmatine resulted in a threefold sustained rise in blood plasma agmatine for at least 24 hours after injection. Therefore, agmatine and its precursor, arginine, cross the blood-brain barrier. CSF agmatine may be newly synthesized from peripherally injected arginine.

Source : http://onlinelibrary.wiley.com/doi/...nticated=false&deniedAccessCustomisedMessage=

 

[Ligaturd]

Well. I guess I will try it as I only see people talking about how it shouldn't be able to cross the BBB but no real human trials. I am not sure if I am comfortable trying to inject Agmatine powder, especially at those doses when I am not sure how pure it will be.

I don't have anything to lose by doing so. I will also try memantine but only if the Agmatine isn't doing much of anything. It wont exactly be very scientific but an anecdotal experience report could help illuminate whether there is anything to it or not.

Here is a link to the original study.
http://www.chinaphar.com/1671-4083/24/631.pdf

 

[DL-ark]

Bodybuilders are using this all over, so either you have to do megadoses, or it's really about not crossing the BBB in human. It's a putative endogenous neurotransmitter btw. No way this could counter naloxone imo.

But for you, I'd suggest to look up about memantine. It can and does work greatly to get people off opioids, is proven to keep tolerance down and withdrawal away, there are even some papers (although no one appears to be interested in real world studies) about... really strange that nobody uses it. It is very safe, easily available too...

I tried memantine once.. It wasn't like the best dissociative ever or even close. Made me very dizzy as I came up on it VERY quickly about an hour after taking it orally. It wasn't really that euphoric, although I did notice as the initial shock wore off the stimulant effect it has, but it wasn't anything special. I can't really imagine using it to get off opiates because for me it feels like the feeling you get after waking up from an afternoon nap except for about 4 hours with some dissociation and slightly redeeming euphoric qualities. DXM is honestly better than memantine in my experience. But that's just me.

 

[Ligaturd]

Memantine is definitely not a drug of abuse. It's used for it's purported nootropic effects and also to lower tolerance.

 

[dopamimetic]

Yeah, but recreational properties aren't everything ... when you want an instant euphoric high, you have to go for other drugs. Memantine is a real medicine in the way that it is usually well tolerated, relatively non-toxic and sustainable. There is some initial brain fog, don't know how much one can avoid that with -slow- tapering (5mg every two weeks or so!), dopaminergics can help too but this gets in the recreational area again. Will fade quickly anyways and to my knowledge there is currently nothing that could top memantine to help with opioid tolerance and withdrawal (without being an opioid itself, of course). Also memantine does not just mask withdrawal symptoms but has the potential to help with PAWS ...

Another approach is to directly use high dosages, this has been done in studies too. As it's not that well tested, I wouldn't recommend that, and one has to watch out for opioid potentiation / tolerance reduction (!!), but you could go straight with 30-40mg. Up to 60mg's have been used without complications. My personal experience is that it behaves differently when used this way, with potentially having a shorter adjustment period and better / faster effects. Also keep the long half life in mind - up to 100h!

 

[User145667]

Bodybuilders are using this all over, so either you have to do megadoses, or it's really about not crossing the BBB in human. It's a putative endogenous neurotransmitter btw. No way this could counter naloxone imo.

But for you, I'd suggest to look up about memantine. It can and does work greatly to get people off opioids, is proven to keep tolerance down and withdrawal away, there are even some papers (although no one appears to be interested in real world studies) about... really strange that nobody uses it. It is very safe, easily available too...

Why do people say this like memantine is a drug you can just go buy from the store? You need Alzheimer's to get it prescribed and no one on the street knows what the hell it is

 

[Dextro .45]

You can just go out and buy Memantine online…..several Canadian vendors carry it and will ship the the U.S.

Agmatine is a Nootropic used for opioid potentiation and a useful tool for tapering. I have a bottle of 100 capsules, it significantly potentiated my daily Methadone and was nodding hard….could be dangerous actually and could cause an o.d. during sleep

But reducing your opioid usage, using Agmatine would definitely be useful in keeping you comfortable