Naltrexone

naltima

I was gifted naltrexone. This is a special ligand I’ve wanted to try for a very long time. It binds to all three opioid receptors as an antagonist. I started at doses of 0.5mg and went to 1mg. Mostly this post focuses on the potential effects and applications of low dose naltrexone, which seems to be a somewhat popular trend in certain circles of the web.

THE IMMEDIATE-EFFECTS

The effect can first be felt in 15 minutes or so. It starts as a sobering heightened state. Feels somewhat like a common terpene found in marijuana that I’m unsure of. A distinct NMDAr agonist effect is apparent. Cold and clear vision. Colorful or yellow even. This could relate to the effects of opioid withdrawal, where glutamate increases are observed. The least distractible, and more highly perceptual, state of mind. Noticeable GABAergic freedom and disinhibition effect. I feel no fear, possibly due to kappa antagonism. Pain is increased, but yet I have no averse reaction. Pleasurable sensations increased too, but no euphoria. Likely due to the μ and δ antagonism, this reveals the disconnect between the physical sensation and the psychological response. We must usually inherently associate the two, and naltrexone appears to reduce the euphoric-exciting, as well as the inspiring-dysphoric element. I could see anti-psychotic, anti-manic (iffy), and anti-anxiety potential with the first dose. This very much changed later on though, where manic effects, or at the very least, anxious and stressful symptoms emerged. More on that later on. Anti-dopaminergic effects were noticeable. Likely, this effect is produced via opioid heteromers, which is seen in D1-μ interaction.

I vaporized marijuana while under the influence of naltrexone. This seemed to result in a diminished pleasure response from marijuana, but also a much more clear effect. I had more self-control, it felt less physically intoxicating, likely because naltrexone would promote NMDAr activity, which marijuana would downregulate generally. Sometimes marijuana results in this mindless absorption state, noted by obsessively consuming media, or observing something, or running through a bunch of thoughts without your usual level of self-awareness. This usually makes it much harder to stop immersing into whatever task you are doing, a sort of hyper-focus. Naltrexone eliminates this effect. I suspect this effect relates back to the D1-μ heteromer.

I was at a vegan meeting held at Au Lac in Los Angeles. Initially I was nervous, and so I took naltrexone (1mg) in hopes that it would combat this issue. The resulting effect made it easier to confront strangers, where I networked with about 5 new friends (nearly strangers) and suggested projects I likely cannot afford to take on. Vision appeared full and peripheral. It feels like the beginning of a traumatic experience, but without the actual fear. Just the perceptual heightening, peripheral visual awareness, and auditory expansion as if I were going to freak out. Luckily, I still felt very neutral, which was a very bizarre effect.

It causes laxative effects. It reduces anxiety. After three days of using, I developed a depressive state reminiscent of opioid withdrawal. It is very mild though, most likely because opioid withdrawal usually includes high amounts of dynorphin, which cause you to freak out a bit more. This is likely a different story if you are used to high μ and δ receptor activity, which naltrexone is said to precipitate stronger opioid withdrawal effects upon dosing, if you are dependent on this opioid activity.

It caused borderline manic and insomniac effects. I could not sleep much that night, even with marijuana. It very much felt like crashing from stimulants, most notably Methylphenidate, which I’ve taken for most of my life (not anymore though).

THE AFTER-EFFECTS

I noticed waking up increasingly sleepy a few days after stopping my naltrexone use. It altered my mood, increasing calmness, possibly apathy, and possibly mania in some situations. My endurance for pain was certainly increased. One of my jobs requires me to stand for up to 6 hours, which usually, and predictably, leads to the same run-down feeling by the end of my shift. During my 6 hour shift, I did not experience the run-down feeling, and I was able to tune-out the impatient sensations I usually have.

It altered the effects of Marijuana, restoring opioid effects, noted by the sensitive histamine reactions. After vaporizing my usual dose of marijuana, while walking around in a park, I experienced itchy legs, usually associated with exercising. I have not experienced this effect since before I took Tianeptine and Kratom on a daily basis. It seems I may have downregulated opioid transmission by using Tianeptine and Kratom. I have not used these for more than a year now, and I feel generally normal otherwise. I have noticed niacin does not flush nearly as much as of late either. After using naltrexone, my histamine response seems to be restored. I experience significant itchiness in many non-exercise related circumstances as well. I did not fully realize I was living without the presence of itches, before this.

It restored the excitement effect of marijuana as well as some of the mildly psychedelic effects, though this was not fully restored, and marijuana did not act as if it were the first time taking the substance. It also seems to reduce anxiety from marijuana both while on naltrexone, and after it wears off, by most likely different mechanisms. Likely, it is the blockade of kappa receptors that prevents some of the anxiety during intoxication, and then the upregulation of μ and δ that prevent anxiety after intoxication.

Many days later, it has restored a very opioid-like effect to marijuana, and very much reduced the psychedelic or perhaps dissociative elements of marijuana. Warm-fuzzy feet, itchy histamine release, and disorienting feelings. This was very welcoming at first, but after just two days of this, I prefer my previous effects, mostly because the trippy effects actually facilitated growth and the generation of novel ideas.

I have felt a greater sense of well-being since stopping naltrexone, but my motivation-level has not much changed. Overall, I am very glad to have been gifted such a substance.

POSSIBLE MEDICAL USES

I would suggest researching a few hypotheses. First, it appears that this drug treats addictions, even internet addiction. The reason appears to be that kappa receptor antagonism downregulates kappa receptors, while also treating the problem immediately, by blocking kappa receptors. Another important factor is that blocking μ and δ receptors helps prevent addicts from getting pleasure from their drugs, while also prompting upregulation of these receptors and their corresponding neurotransmitters, which addicts have likely downregulated by the time they have become addicts. These mechanisms would also be useful to conditions involving chronic pain. On the other hand, this study appears to say that naltrexone does not have efficacy in treating addiction to alcohol.

It seems to share some kind of clarity effect that is usually associated to psychedelic glutamatergic effects. Research on the effect of psychedelics on dynorphin levels would be highly valuable. My hypothesis is that psychedelics likely downregulate dynorphins, and treat addiction via a similar pathology. This is something worth further research into.

One study suggests that opioid activity may increase cognition, something I was sometimes noticing with Tianeptine use, probably due to glutamatergic downstream mechanisms common with most opioids. There may be long-term benefits after naltrexone cessation that promote cognition, slightly, in the long-term or until you eat enough stimulating junk food to trigger opioid responses that cause downregulation again. The fact that kappa activity is associated with NMDAr activity reduction, likely due to heteromers between kappa and NMDA receptors, also hints at a possible mechanistic explanation for cognitive alterations caused by μ and δ activity, which is shown to reduce kappa activity.

I could see how naltrexone could treat dissociative symptoms, it definitely had this effect in the first few uses, but in later experiences this was replaced with a kind of suicidal depressive feeling. In one study, nearly 10% of the participants died, with many attempting suicide before, and at least one successfully committing suicide within the 1 year trial period. I would not be surprised if the researchers had incentive to cover up the suicidal effects and blame overdose instead, when realistically the 4 participants who tried suicide before ‘accidentally’ overdosing, could easily have just been successful by overdosing. This is even more warrant for concern. I definitely felt suicidal on it. With spinning thoughts that seem to have little basis on practical life. I would just randomly get angry at things and feel an urge to impulsively kill myself simply for feeling negative. I definitely won’t do this, so don’t worry about me. I have no intention to leave this world.

Approximately,

Someone Who Is Me

 

 

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2 thoughts on “Naltrexone

  1. How do you know about feelings of NMDAr agonism, dopamine antagonism etc. ? Also I have never heard marijuana making these kind of effects. I’m interested in hearing.

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    1. I’ve taken NMDAr agonists and also things that indirectly increase NMDAr activity by glutamate release.

      I’ve also taken dopamine antagonists before.

      Which effect of marijuana? I am likely bipolar so my response is intense perhaps.

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