Best time of day to take LDN?

[Zebra]

Hi, Comrades,

My prescribing physician is not available between appointments, so I'm reaching out to the group for information, advice, experiences, etc.

I am going to be giving low-dose Naltrexone a try and I have a few questions:

1. If LDN is notorious for causing insomnia, then why do physicians and pharmacies recommend taking it before bed?

2. Does anyone take LDN with breakfast or lunch instead of at bedtime?

3. What's been your worse side-effect and did it eventually subside?

Thank you x 3!

 

[Springbok1988]

I’ve always heard it’s because LDN boosts endorphins which are naturally highest in the morning so the nighttime dosing helps align with the circadian rhythm. If that’s the case, I don’t understand why it’s not taken in the morning, given its short half life.

It has also been hypothesized that it helps calm parts of the immune system that are most active at night. I didn’t find much evidence to support this but I did see a couple of research papers that mention it.

My worst side effect was insomnia and it never got better in my case. Because of that, I took it with lunch. It helped with pain for a while but it stopped working for me. I never experienced improvements in brain fog or fatigue.

 

[Wishful]

I had no side effects from LDN. I found that a dose lasted ~36hrs for me (pain blocking), so to minimize drug use, I alternated mornings and evenings every 2nd day. That worked well, and I didn't notice any differences between the two dosings.

FWIW, my minimal effective dose was 2.25 mg sublingually. 2.0 mg was ineffective, so you can see how sharp the cutoff is. Dosing above 2.25 mg gave no extra benefit, and became ineffective above 6 mg. Taking it sublingually is ~1/3 more effective.

 

[bad1080]

if it is activating for you then in the morning, if it is sedating then in the evening.
i had to switch mine from pm to am recently because it stopped making me sleepy.

 

[Zebra]

@Springbok1988
@Wishful
@bad1080

So grateful for your responses. Thank you!

 

[pamojja]

I’ve always heard it’s because LDN boosts endorphins which are naturally highest in the morning so the nighttime dosing helps align with the circadian rhythm.

It boosts endogenous endorphins' production, by blocking endorphins first. So the rationale for taking it before sleep is for sleeping through a lower mood. If that doesn't apply, no reason not to take at any other time.

 

[jasperZA]

I always thought LDN should be taken at night because it takes ~8 hours to act (conversion to active metabolite has a half life of 4h). So that ir acts throughout the day (half life of active metabolite 13h) instead of in the afternoon to night.

 

[pamojja]

It boosts endogenous endorphins' production, by blocking endorphins first. So the rationale for taking it before sleep is for sleeping through a lower mood.

Should have been more precise: It blocks endorphins receptors for a few hours.

LDN in form of 1 dose nasal spray, is here finally promoted to addicts and social institutions. It blocks endorphins - and opioid - receptors in the form of a nasal spray on the spot. And thereby is a miracle to bring heroin overdoses back. But that has the side effect of sobering the user so much, that one has to take precaution preventing the person getting the next shot straight away. Which could be more deathly.

Guess the endorphin receptor blocking property here last only a short time, because it gets overwhelmed by lots of heroin.

I always thought LDN should be taken at night because it takes ~8 hours to act (conversion to active metabolite has a half life of 4h).

Could it be what you consider the active metabolite, be the upregulated endogenous endorphins? Which is what has the immunity modulating properties.

 

[jasperZA]

I was talking about 6 beta-Naltrexol. But now I‘m not so sure if it is tje relevant mechanism. I might be mistaken.

 

[DonPepe]

Not sure. Didn’t have a positive experience on LDN and it didn’t move the needle.

 

[pamojja]

Could it be what you consider the active metabolite, be the upregulated endogenous endorphins?

I was talking about 6 beta-Naltrexol

https://en.wikipedia.org/wiki/6β-Naltrexol - you were right that it is a metabolite of naltrexone,

With naltrexone therapy, 6β-naltrexol is present at approximately 10- to 30-fold higher concentrations than naltrexone at steady state due to extensive first-pass metabolism of naltrexone into 6β-naltrexol.[4]

Which one would think would apply to usual 50 mg Naltrexone doses. Used to prevent alcohol and drug abuse. But not certainly with low dose naltrexone - I don't think with 4 mg a similar steady state could be reached. And which mainly aims at up regulating endogenous endorphins only (probably ineffective with a high steady state).

 

[SnappingTurtle]

I take 2.5mg in the morning, since it gives me crazy dreams.

 

[Wishful]

So that ir acts throughout the day (half life of active metabolite 13h)

Well, that theory seems a bit off to me, since for me, LDN lasted ~36 hrs, and the pain didn't gradually return over that time. So, there's likely more to the overall mechanism than just molecular half-life. The changes it does to cells might last longer.

 

[kangaSue]

I had the insomnia issue with LDN. Only way I could get around that was to take LDN in the morning, but no later than 7:00 am or I'd still have insomnia that night.

 

[DonPepe]

I had the insomnia issue with LDN. Only way I could get around that was to take LDN in the morning, but no later than 7:00 am or I'd still have insomnia that night.

ditto

I also had crazy nightmares once I finally got asleep. I may try again but take it in mornings.

 

[Zebra]

Ugh. I am also experiencing the sleep disturbance. Started out as mild, but increased in intensity.

I will try taking it in the mornings instead of before bed, and see how that goes.

I really hope I can tolerate LDN and eventually (very slowly) increase the dose.

About a week after starting LDN, I began to experience physical agitation and restlessness which I am hoping are precursors to energy?

 

[bad1080]

began to experience physical agitation and restlessness

i had something similar, i felt very agitated but also cranky when i got to 1mg with my dose. i backed down to 0.75mg and the agitation went away. i also started implementing off-days and that seems to help with tolerance build up. i guess my body is either slower with metabolizing the drug or it takes longer than 24h to go back to baseline. naltrexone has a half-life of ~4h but there is a secondary metabolite with a much longer half life (~14h iirc).

if you switch to morning dosing it is best to skip your evening dose before taking it the next morning.

 

[kushami]

I took my dose very late today (8pm instead of morning) and it seems to be keeping me awake. Should have just skipped a day.

I am having bad dreams with it. Not nightmares, but somewhat unpleasant or sad storylines. However, I often have bad dreams when I get too hot while sleeping, and it also seems to be making me hot (and thirsty). Hoping that wears off as we are heading into summer here.

 

[*GG*]

I was recently prescribed this again, major health care system in the USA. Neurology department, I was told to take it in the morning because it can cause sleep issues. Same advice I was given 15 years ago by my unconventional Dr.

they prescribe the 50mg tablet and I dissolve it. surprised by that, last time I saw the specialist, they mention getting it in pill form and costing me $20 to 30 per month. My copay is nothing for the 50mg tablets, and I am on about month 2 of a 6 month trial.

GG

 

[Wishful]

50 mg is not Low dosage; that's regular dosage AFAIK. Completely different effect from low dosage.