Naltrexone

Therapeutic Efforts Pharmaceutical
#1

Link: en.wikipedia.org/wiki/Naltrexone

Naltrexone is an opioid receptor antagonist used primarily in the management of alcohol dependence and opioid dependence. It is marketed in generic form as its hydrochloride salt, naltrexone hydrochloride, and marketed under the trade names Revia and Depade. In some countries including the United States, an extended-release formulation is marketed under the trade name Vivitrol. Also in the US, Methylnaltrexone Bromide, a closely related drug, is marketed as Relistor, for the treatment of Opioid Induced Constipation. It should not be confused with naloxone (which is used in emergency cases of overdose rather than for longer-term dependence control) nor nalorphine. Both naltrexone and naloxone are full antagonists and will treat an opioid overdose, but naltrexone is longer-acting than naloxone (although neither is an irreversible antagonist like naloxazone), making naloxone a better emergency antidote.

Pharmacology
Naltrexone and its active metabolite 6-β-naltrexol are competitive antagonists at μ- and κ-opioid receptors, and to a lesser extent at δ-opioid receptors.[1] The plasma halflife of naltrexone is about 4 hours, for 6-β-naltrexol 13 h. The blockade of opioid receptors is the basis behind its action in the management of opioid dependence—it reversibly blocks or attenuates the effects of opioids.

Its use in alcohol (ethanol) dependence has been studied and has been shown to be effective[2]. Its mechanism of action in this indication is not fully understood, but as an opioid-receptor antagonist it’s likely to be due[citation needed] to the modulation of the dopaminergic mesolimbic pathway which ethanol is believed to activate.

Naltrexone is metabolised mainly to 6β-naltrexol by the liver enzyme dihydrodiol dehydrogenase. [b]Other metabolites include 2-hydroxy-3-methoxy-6β-naltrexol and 2-hydroxy-3-methoxy-naltrexone. These are then further metabolised by conjugation with glucuronide.[/b]

Sexual dysfunction

Naltrexone can induce early morning erections in patients who suffer from psychogenic erectile dysfunction. The exact pathway of this effect is unknown. Priapism has been reported in two individuals receiving Vivitrol.

Naltrexone has been shown to be effective in the reversal of sexual satiety and exhaustion in male rats.[20]

This drug is also being used for fertility treatment.

Low Dose Naltrexone
#2

LINK: andrologyjournal.org/cgi/con … t/14/6/407

Opiate antagonists can indirectly stimulate the secretion of luteinizing hormone (LH) and testosterone, as well as sexual functions in animals and humans. We therefore treated 20 otherwise healthy men with idiopathic erectile dysfunction aged 46.3 +/- 2.7 years (mean +/- SE, range 23.9-63.3) in a double-blind study with an opiate antagonist, naltrexone, or placebo. The erectile dysfunction of these men had persisted for 3.6 +/- 0.5 years despite libido maintenance; standard procedures had excluded any organic causes. Trial duration was 12 weeks overall. After a 4-week forerun, the patients received at first 25 mg naltrexone/day orally or placebo for 4 weeks followed by 4 weeks of a 50-mg dose of naltrexone/day or placebo. Each day the patients filled out a questionnaire detailing libido, degree of erection, frequency of sexual intercourse, and spontaneous morning erections. Serum concentrations of gonadotropins and testosterone were determined radioimmunologically in the initial stage and at the end of each phase. Both patient collectives had similar initial factors. The group treated with naltrexone showed a significant rise in spontaneous early morning erections during the treatment: from 2.8 +/- 0.3 to 4.2 +/- 0.3 a week (P < 0.001). The placebo group showed no significant change in spontaneous erections (2.4 +/- 0.3 and 2.6 +/- 0.3, respectively). The subjective parameters, however, such as libido, degree of erection, and frequency of sexual intercourse showed no significant difference within each group. There was no difference in LH, follicle-stimulating hormone, or testosterone concentrations in both groups. Thus, treatment with naltrexone significantly raises the rate of spontaneous early morning erections when compared to controls.(ABSTRACT TRUNCATED AT 250 WORDS)

#3

LINK: ncbi.nlm.nih.gov/pubmed/2543996

Abstract

In the present study we evaluated whether naltrexone administration could stimulate sexual function in 30 male patients, ages 25 to 50 years, with idiopathic impotence of at least one year’s duration and not of organic etiology. The patients received naltrexone (50 mg/day) or placebo, on a random basis for two weeks. Sexual performance, expressed as the number of full coitus/week, was assessed before (time 0) and during (on days 7 and 15) each treatment. The naltrexone therapy significantly increased the number of successful coitus compared to placebo after 7 and 15 days of treatment: improvement of sexual performance was evident in 11 out of the 15 treated patients. All the patients experienced a significant increase in morning and spontaneous full penile erections/week. No significant side effects were reported. Endocrine studies revealed no significant modification of plasma LH, FSH or testosterone by naltrexone, suggesting that the positive effect of the drug on sexual behavior was exerted at a central level. A two-month follow-up, at which time patients were off treatment, erectile capacity had returned to baseline in 10 patients, while five reported complete recovery of their sexual ability. We hypothesize that an alteration in central opioid tone is present in idiopathic impotence and is involved in the impairment of sexual behavior.

#4

I tried this for over 6 months, no improvements.

#5

.

#6

In total, how many have tried Naltrexone?

Do you have to use a specially formulated pill for low dose? or can i just buy 50 mg pills and split them?

#7

I’ve been taking it for years. It’s a great drug, you will feel more alive, but it’s not enough. By not enough I mean you will experience 10% less brain fog, 10% better cognitive abilities, 10% better sleep, 10% better libido, etc.

The best thing for me is that it absolutely SLAYED my anxiety/stress. I used to go into a panic at work over every little thing and had trouble making eye contact when speaking to people. All of that is pretty much gone.

I never took low dose naltrexone for PFS, I took it to cure my colitis. It did that, and it did it in about a week.

I think if there was some way to magically boost the power of the naltrexone we would have our cure.

1 Like
#8

So you have to keep taking it to sustain benefits?

#9

yes, you keep taking it, but unlike everything else I have taken, the benefits never seem to wear off. It never loses its effectiveness. Another great thing about it is, in the 4.5 mg dose, it’s very inexpensive. I have it custom compounded at a nearby drug store and 30 dollars buys me a 2 month supply.

LDN is a remarkable drug, check out some of the embedded videos in this link lowdosenaltrexone.org/

#10

Wow, it certainly seems like an amazing drug.

#11

I respond very well to LDN

I am one of the lucky ones. The doc who gave it to me says a lot of his patients take it and have no reaction at all…

#12

Very interesting website. I think I’m going to ask my Endo about trying the 4.5mg low dose at my next visit. I know it its no “cure” but I would put this in the category of “it can’t hurt to try”. Who knows, maybe it’ll put at least1 or 2 of the pieces of the PFS puzzle into place.

#13

What I find interesting is the results it has in patients with auto-immune illness.

#14

You can actually try this stuff low dose for next to nothing.

ÂŁ14 for 10x 50 mg tablets here:

unitedpharmacies.co.uk/product.php?productid=694&cat=&page=1

Then follow the simple instructions provided on this website to dissolve it in water:

webspawner.com/users/howtoobtainldn/index.html

#15

forums.phoenixrising.me/showthread.php?379-Low-dose-Naltrexone

"I knew one person who did very well on low dose naltrexone (LDN). It’s another of those odd central nervous system drugs that is being tried out in all sorts of disorders. Originally used to help detox patients going off of opioids and to combat alcohol dependence very low doses of it are being examined in fibromyalgia, AIDS, Parkinson’s, MS and other auto-immune diseases, autism, etc.

I particularly like it’s ability to induce erections. The ME/CFS patient I knew who tried it occasionally couldn’t get to sleep because of his erections - an automatic winner in my book.

In this recent study on FM patients LDN was described as being an effective, tolerable and inexpensive :smiley: treatment for them. It’s effects occur because

Naltrexone, in addition to antagonizing opioid receptors on neurons, also inhibits microglia activity in the central nervous system. At low doses (4.5 mg), naltrexone may inhibit the activity of microglia and reverse central and peripheral inflammation.
They found that
Low-dose naltrexone reduced fibromyalgia symptoms in the entire cohort, with a greater than 30% reduction of symptoms over placebo. In addition, laboratory visits showed that mechanical and heat pain thresholds were improved by the drug.
If you have a high sedimentation rate you might be in luck.
Individuals with higher sedimentation rates (indicating general inflammatory processes) had the greatest reduction of symptoms in response to low-dose naltrexone."

#16

Med Hypotheses. 2009 Mar;72(3):333-7. Epub 2008 Nov 28.
Low-dose naltrexone for disease prevention and quality of life.
Brown N, Panksepp J.
SourceDepartment of Humanities and Social Sciences, Embry-Riddle Aeronautical University, Daytona Beach, FL 32114, United States. NPHbrown@aol.com

Abstract
The use of low-dose naltrexone (LDN) for the treatment and prophylaxis of various bodily disorders is discussed. Accumulating evidence suggests that LDN can promote health supporting immune-modulation which may reduce various oncogenic and inflammatory autoimmune processes. Since LDN can upregulate endogenous opioid activity, it may also have a role in promoting stress resilience, exercise, social bonding, and emotional well-being, as well as amelioration of psychiatric problems such a autism and depression. It is proposed that LDN can be used effectively as a buffer for a large variety of bodily and mental ailments through its ability to beneficially modulate both the immune system and the brain neurochemistries that regulate positive affect.

ncbi.nlm.nih.gov/pubmed/19041189

#17

Shippen has used this on some patients to raise testosterone levels by the way

#18

andrologyjournal.org/cgi/content/abstract/14/6/407
ncbi.nlm.nih.gov/pubmed/2543996
ncbi.nlm.nih.gov/pubmed/8536780
ncbi.nlm.nih.gov/pubmed/11395188

#19

I will be starting on Naltrexone very shortly. I intend to stay on the drug indefinitely if there are no side effects so i will only give updates when there is something worthwhile to say.

I am going to start off with the low dose, as you are supposed to with chronic illness, but i will also try higher dosages that were used in the studies i posted above.

As usual, i am not building any expectations because the cause of my problems (PFS) is completely unknown but the studies and reports out there are very promising. Hopefully this can relieve my symptoms somewhat.

#20

Been on Naltrexone for two days now. I intend to stay on for a very long time. A huge thanks to Joetz for helping me out.