36 replies to this topic

[yowza]

Wow. Last night I found out about Naltrexone for the first time and here it was right in front of me on these boards all the while. Huge coincidence.

I just glanced over this thread quickly so maybe I missed something, but have you tried increasing the dosage just to get a closer bead on the effects aLurker?

[aLurker]

Thanks for the advice adamh, I appreciate you're trying to help me out and I hope LDN works out for you.

I kept the dose at 3 mg until three days ago. I've taken 2 mg two days and yesterday I skipped my dose entirely. You are probably right I should be more consistent and persistent here if I want to give LDN a fair chance.

The naltrexone definitely seems to be the real deal and the effects are quite consistent with what people have reported about LDN so far regarding taste and acutely noticeable effects.

The melatonin seems to be treating me fine. I tried 0.15 mg at 21:45 and no LDN yesterday. I went to bed just after midnight, slept to 6 a.m. when I awoke feeling rested, took a cup of white tea in the morning and I've been feeling pretty good all day. I think my hands felt a lot warmer today so the previous coldness might be a side effect from the LDN although I suspect it is because my body isn't used to it yet. That was also the reason I skipped a day, to check if there was any difference.

I also noticed yesterday that my tongue is basically entirely without plaque. That is kind of miraculous since I usually can scrape of heaps of plaque from it. I haven't even used a tongue scraper at all, the plaque has just disappeared. There are a lot possible explanations to this though, I can think of four: vitamin K, LDN, new toothpaste (Pepsodent Xylitol) and occasional supplementation of Xylitol-powder in what I drink. It is probably not the toothpaste but all the explanations seem perfectly reasonable to me and this is the downside of trying several things without waiting for the effects. Like I said, I'm impatient, but yeah I should give this some more time.

Today I took 0.2 mg melatonin at 22:00 and 2 mg LDN at midnight. Bedtime at about 00:30, feeling kind of sleepy and that's a good thing.

[yowza]

Naloxone, suboxone (sublingual form of 2 ingredients 1 of which is naloxone), and naltrexone all seem like they could be used to increase "affect" in those suffering effects of derealization/depersonalization or even brain fog. These effects can start at any time, I'm guessing, probably due to a variety of things (trauma, epilepsy, marijuana usage, ect.).
I just started checking these boards again and a conversation on a totally different subject (http://www.imminst.o...ceptor-agonist/ ) lead me to finding this drug.

[aLurker]

I'm still on 2 mg/day of Naltrexone, not much to report. My hands haven't been colder than usual the last few days so I guess what I said before was merely a fluke or temporary, either way they seem fine now.

Regarding the melatonin I'm still struggling to get the timing and the dose right. Sometime before 10 p.m. seems pretty reasonable so far. 0.2 mg seems enough to get me to sleep sometime before 1 a.m. although I've had trouble sleeping for 7 hours straight. Either I wake up too early and can't get back to sleep or I oversleep. I'll get back when I find a dosage here that works somewhat more consistently for me, I tried 0.3 mg yesterday but I took it too late so I'll try again tonight. I also suspect the LDN is still interfering with my sleep somewhat although I hope those effects are fading.

[yowza]

I also suspect the LDN is still interfering with my sleep somewhat although I hope those effects are fading.

I may have missed something but have you noticed a difference with this issue depending on the dosage level you take? From reading through some of your reports, it seems you haven't felt a prominent effect from low dose Naltroxene?


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Here's some interesting info. I could find on chemicals with similar modes of action to naltroxene:
Naloxone:
In a class of medications called opioid antagonists; it is one of the most potent opioid antagonist out there used for heroin overdose.

According to several studies there are several offlabel usages for this as well (although due to the potency of this chemical, I'd say for nootropic purposes it would probably have to be at a very low dosage sort of like how naltroxene is used). However, it doesn't appear too many have tried taking this for these offlabel purposes as naloxone only is commercially available in injectable form.

However, compared to naltroxene, this chemical does seem to be more effective for symptoms of depersonalization; this is briefly mentioned at the end of the following article http://www.articlesb...ss-1040613.html. The article doesn't get into much detail about why naltroxene is less effective than naloxone but it may be simply due to the higher potency of naloxone as an opioid antagonist I'm guessing.

　

Here's some info. I could find on other similar chemicals with similar modes of action out there:
The following medications seem to be used most commonly to treat opioid dependence (pain killers or heroin); both of the following are taken in sublingual form usually once per day for this treatment purpose:

Suboxone (buprenorphone+naloxone combo)-naloxone (the opoid antagonist part)+a semi-synthetic opioid Buprenorphone (partial opioid agonist/antagonist)

Subutex (buprenorphone): This is a sem-synthetic opoid in a class of medications called opioid partial agonist-antagonists; for more info. simply wikipedia it at:
http://en.wikipedia....i/Buprenorphine




The most common usage of Suboxone and Subutex seem to go along the following guidelines as seen at http://www.ncbi.nlm....000285</strong> :

"Buprenorphine alone and the combination of buprenorphine and naloxone prevent withdrawal symptoms when someone stops taking opioid drugs by producing similar effects to these drugs."

"You will start your treatment with buprenorphine, which you will take in the doctor's office. Your doctor will start you on a low dose of buprenorphine and will increase your dose for several days before switching you to buprenorphine and naloxone (suboxone). Your doctor may increase or decrease your buprenorphine and naloxone dose until the medication works properly."

While this may be the most common usage for suboxone, I'm thinking that (like naloxone and naltroxene) this may also be used to treat depersonalization symptoms.

　

While googling "suboxone" I came across this message board discussing it's effects for depersonalization symptoms (I'm looking at this since based on this offlabel usage it's not too far out to see this as an affect enhancing nootropic depending on one's underlying physiology I'm thinking):
http://www.dpselfhel...21355-suboxone/:

"I've been on suboxone for about a week and have been feeling a lot better. I am also taking hydrocortisone because I have low cortisol levels. I missed my dose of suboxone one day and could definitely tell that a large part of what has been making me feel so much better is the suboxone. Suboxone is a partial opioid. They give it to people who are withdrawling from opiates. I've read about naloxone and naltrexone and how some people have found relief from opioid antagonists. Just curious to see if anyone else has tried suboxone or knows how it compares to naloxone/naltrexone."

Interesting that this poster mentions that he takes hydrocortisone as his circadian rhythm may be off. One of the ways to tell if this is the case is through adrenal stress testing (check out the various clinical issues that can arise out of this at the following site http://www.diagnoste...asi_doctor.html).
As seen at the DiagnosTech website, there are many issues that can arise out of this, however besides this stuff, triggering feelings of depersonalization can also happen according to the same article I posted above (http://www.articlesb...40613.html</em> ; what's posted below is just one of the numerous interesting peices of info. I found here):

"Recent research has brought to light the potential involvement of cortisol in the generation of DD. Cortisol, the "stress hormone," is produced in the adrenal glands. It's best known for ramping-up our physical response to phenomena such as life stressors, trauma, excessive exercise, anxiety, and depression by passing word to the neurotransmitter and hormone norepinephrine (noradrenaline) to flip the switch on our sympathetic nervous system, our fight/flight headquarters. And, boom, off to the races we go. Obviously, situational secretion of cortisol is natural and necessary; however, when it's secreted in the presence of chronic stress all sorts of icky physical consequences may occur, as well as generalized anxiety and panic. And DD. The bottom-line is the researchers used a measurement instrument known as the "Dissociative Experiences Scale." And the subjects that tested high on the DD subscale had a much higher cortisol response to stimuli. So if the connection between stress, anxiety, and DD weren't already obvious to you, the research bangs the point home."

Going away from this topic about cortisol back to the poster's main question (how suboxone compares to naloxone/naltroxene), here's a quote that someone responded with:

"...some research implicates the endogenous opiate system as playing a major role in dp (depersonalization). This is because Naloxone, the most potent opiate antagonist out there has produced the greatest DP alleviation in limited trials. However, it is IV administered only, and it is a non-selective opiate antagonist. Naltrexone does similar things but not as powerfully.

The opioid receptor thought to be most likely responsible for DP is the kappa-opioid receptor. Stimulating this receptor can induce feelings of dysphoria and DP. Naloxone and naltrexone antagonize this receptor, but they also antagonize the feel-good opiate receptors (a factor we don't really want).

Currently, no selective kappa-opioid antagonists are approved for human use. However, buprenorphine (in suboxone as well as subutex) is an opiate that agonizes the mu-opioid receptor (feel-good receptor) while antagonizing the kappa-receptor. As such, it theoretically could help alleviate DP. A Harvard study showed that it had promise for "treatment-resistant depression" which I suspect often means misdiagnosed DP.

But it is very taboo to use it for anything other than getting people off of opiate addiction or for chronic pain management. One would be very lucky to get a sympathetic doctor to prescribe it. Even then, docs need special certification to prescribe it."

I'll try researching into this stuff more and maybe starting a seperate thread at some point but for now it would be interesting to hear if anyone's followed these sort of chemicals as nootropics in the past?

Edited by yowza, 13 September 2010 - 02:44 AM.

[vaarmen]

Hi LC community!

I have been doing some research on LDN and came across to the major active metabolite of Naltrexone 6-beta-Naltrexol. It is known that 6-beta-Naltrexol has a half-life of about 13 hours, and that Naltrexone undergoes much first pass metabolism which make the plasma levels of 6-beta be much higher than Naltrexone. 6-beta is reported to have lower affinity for mu opioids, but not too low and combined with the large AUC it can even have more effects on the receptor than Naltrexone itself (controversial). The problem with the 6-beta is the longer half-life, as it means opioid receptors will be blocked the next day as well after a bedtime dose.

What is your take on the above information?
Do you know how significant is 6-beta-Naltrexol in LDN effects?

How long do you feel dysphoria after taking an LDN dose. Does small amount continue up to 24 hours or more?
What if the effectiveness of LDN is because of constantly blocking Opioid receptors rather than causing rebound and desensitization?
Has anyone tried LDN with Naloxone rather than Naltrexone? It has shorter half life and no active metabolites as far as I know, so could potentially cause more rebound and less blockade the next day after a dose.

Any insight will be appreciated!

Thanks in advance!

[John250]

Any other reports of low dose naltrexone? What have you noticed,etc..?