187 replies to this topic

[edward]

I'd like to know everyone's experiences with sleep enhancing substances. Sleep is so critical for health, in particular slow wave sleep is very important for hormone regulation, repair of tissues, memory consolidation (REM also important here), and arguably longevity etcetera, etcetera... The focus of this thread is Sleep Enhancers not Sleep Aids. Many things will get you to sleep but fewer things actually preserve or enhance natural sleep architecture.

Yes there is information about sleep enhancers scattered throughout this site and yes I could resurrect some old thread but there is no real "one stop shop" catch all thread that includes herbs, drugs, hormones and everything else that enhances sleep.

Personally, a good night sleep makes a dramatic difference in the way I function. It has always been a challenge for me to get a good night's sleep and thus daytime sleepiness has been a burden.

Things I have actually tried and my thoughts and selected info on them: ************************

Melantonin: Alright for enhancing sleep though by itself dosen't do the job (I have and will continue to take melantonin on a nightly basis because I am convinced of its health and longevity promoting properties)

Lunesta (Ezopiclone, USA), Imovane (Zopiclone, outside USA): Works very well, 5 hour half life which is perfect for sleep (I found no tolerance even after long term use) and in sleep studies it preserves natural sleep architecture. However it seemed to mess with my memory. http://www.biopsychi.../zopiclone.html

Valerian: Great for about two weeks then it stops working unless you escalate the dose.

GABA: Some benefit but not enough of it crosses the blood brain barrier to be effective IMO.

GHB (Xyrem by prescription): Ehh, ok for a little while, supposedly compresses total sleep time, enhances slow wave sleep but not a long term solution unless you have narcolepsy and nothing else works.

Trazodone (Desyrel): Antidepressant that is very good and effective for sleep (sleep architecture is reasonably preserved with some decrease in REM) but tends to leave one tired all morning and makes is very hard to wake up. Maybe with a shorter half life it would be good but not as is.

Diphenhydramine (Benedryl) and other Antihistimines: Well what can I say, they will make you sleep but definitely will not preserve or enhance sleep architecture. These are definitely sleep aids not sleep enhancers. Probably not a good idea in the long term, for health, longevity etc.

5htp/ Tryptophan: Not bad for getting to sleep but for those of us taking other serontonin enhancing drugs probably not a good idea. Also of note is the fact that serotonin is actually a daytime hormone and its only when it converts to melantonin that the sleep enhancing effects are apparent so in my opinion why not just take more melantonin rather than these.

Things I am interested in and considering: ************************

Gabapentin (Neurontin): Signifigantly enhances slow wave sleep, reduces stage 1 sleep dramatically (this is a good thing, Stage 1 is the barely falling asleep stage), and only shortens REM a little bit (maybe a good thing). There have been some posts on this site about this drug being very effective for sleep. Gabapentin was originally marked as an anti-seizure medication but like almost all of the anti-seizure meds it has been used as a mood stabilizer for bipolar depression. It was so flexible a substance that it became over marketed for off label use sadly tainting its reputation. But of all the anti-seizure meds it appears to have the best profile for a sleep enhancer. 6 hour half life which is pretty good for sleep. http://download.jour...45702002174.pdf

Ambien CR: Yes its a mainstream popular drug but it seems very positive. Enhances slow wave sleep, reduces stage 1 sleep dramatically and again also only shortens REM a little bit. Apparently has no side effects on memory unlike Zopiclone/Ezopiclone. The CR version extends the blood levels to closely mimic a sleep enhancer with a half life of 5 to 6 hours again ideal for a sleep enhancer. http://www.biopsychi...olpidemcomp.htm

Rozerem (Ramelteon): Very interesting, supposedly enhances the sensitivity of Melantonin receptors, perhaps if taken along with melantonin it might be excellent. I hate their commercials but that aside it looks very promising, I'd be curious to see the results from someone who has tried other sleep enhancers.

Things I am NOT interested in trying: ************************

Phenibut: From what I have read its a dead end unless you use it only a couple of times a week. Tolerance develops very fast and can lead to a very negative situation.

The Sleep Machine: This was mentioned in either food, diet and exercise or Nootropics. Basically its a machine that using magnetic fields sends one directly to slow wave sleep and supposedly one can sleep only 4 hours a night instead of 8. To me it sounds like the results are similar to GHB/Xyrem i.e. only worth considering if you have narcolepsy or if for some reason you need to function on reduced sleep for a period of time.

************************
Note: I take Ashwagandha and Bacopa at night as they tend to make me sleepy and Ash seems to help with recovery from exercise but I don't consider either effective sleep enhancers.

Edited by edward, 22 May 2007 - 01:49 PM.

[rfarris]

Phenibut: From what I have read its a dead end unless you use it only a couple of times a week. Tolerance develops very fast and can lead to a very negative situation.

I've been using phenibut from time-to-time. I really appreciate the hard sleep I get from it. Without it it takes me an hour, or so, to go to sleep and I wake up every hour-or-two during the night.

My current situation is way better than it was before I had a stroke (bleeder) due to sleep apnea. So I suppose we should add the C-PAP as a sleep enhancer. Prior to it I rarely got an hour of sleep a night.

[rfarris]

I was interested in Gabapentin. Mostly because I'm interested in an SGRI, like Gabitril (strangely difficult to find), but it isn't -- based on this quote I found:

Gabapentin is structurally related to the neurotransmitter GABA (gamma-aminobutyric acid) but it does not modify GABAA or GABAB radioligand binding, it is not converted metabolically into GABA or a GABA agonist, and it is not an inhibitor of GABA uptake or degradation.

Another issue -- when I read the monograph posted by Edward, I noted that zonisamide was included in the sleeping test. I've been taking 600mg/day of zonisamide for almost a year and I'm in the process of tapering off and I'm having sleep problems, so I wonder if the zonisamide was helping my sleep. A complication is that I've also been taking Lexapro (an SSRI) that I've completely tapered off at the same time.

At any rate, none of the results included zonisamide, although it was included in the testing. My conclusion is that it had no effect.

[stillalive]

A very intresting topic indeed. I have used 5 HTP with good resultats and GABA but with lesser succes for sleep.

I'm intreseted if anyone else has any experinces of 5HTP. Two of my friend has tested it and one had didn't noticed anything but the other noticed big diffrences.

5Htp increases deep sleep and REM sleep. In a book about 5HTP I read that the REM sleep is needed for recovering from deep sleep. So REM sleep isn't nesscary a bad thing.
To feel that i have slept sufficent I need about 8 ½h but with 5HTp I do fine with 7,5-7,75h. I often wake up a bit earlier than 7,75h, but I fall asleep again. But it makes me a lot more awake in the morning. But i really felt that my sleep quality was really bad before I started using 5HTP. Have only used 100mg, but I it's enough at least for me.

5HTP work by increasing the storage of melatonine and it's more effective than just melatonine. only people with low levels of Melatonin benefits from melatonin supplementing but 5HTP help all people by taking another way to archive it's resultats.
But it increases ACTH levels which isn't really a good thing for sleep, sometimes I wake up more often and have more nightmares when I increase dosage. I think it's because of ACTh.

Gapapentin seems lika a good supplement for sleep, but it very expensive if you can't get it prescribed ofcourse.

[shifter]

Is it okay to take 5-htp and Melatonin together? Thats what I have been doing for a few days. I think I sleep just as good as taking melatonin on its own.

[edward]

I don't see a problem with melatonin and 5htp together. For me that combo just doesn't truly enhance sleep. With me some sort of gabaergic substance is needed.

[mike250]

3-4g of taurine knock me out cold. I think I might be deficient or lack in one or more neurotransmitters.

[shifter]

I wouldn't take melatonin throughout the day but an you do the same with 5-htp? I took some this morning before work (after a nice sleep) and didn't notice any drowsiness or tired eyes that melatonin sometimes gives me...

[basho]

I try the following combination sometimes and it seems to work as long as it is restricted to a couple of times per week:

LEF Melatonin Natural Sleep (includes C, Niacin, B6, B12, Calcium, Magnesium, Chromium, Melatonin immidiate release 2.5 mg, Melatonin timed release 2.5 mg, and Inositol)
LEF Glycine 3000mg
L-Theanine 100mg (not always)
Bacopa 225 - 450 mg (not always)
LEF Ashwagandha (Stimulant Free) 125mg

I have almost *no* logical reasoning behind that combination, except that I saw some postings in another thread indicating some variations of the above helped with sleep. However it never works if I have been drinking alcohol earlier in the night, but now I rarely drink so its not an issue.

I have found that the bigger obstacle to good sleep is anxiousness, stress and worry. If there's anything on my mind causing any of those feelings, nothing will help me sleep.

[Gerald W. Gaston]

Here I take:

Swanson Dual Release 3mg Melatonin (1.5mg immediate, 1.5mg over next 6-8 hrs)
Swanson Sleep Essentials (has Valerian, 3mg Melatonin, GABA, and more)
Swanson Bacopa 250mg

Swanson Ultra L-Trypophan 500mg (seldom)

Swanson Ashwagandha Extract 450mg - I usually take this later in the evening. Not right before bed.

As with Basho, stress will keep me awake even with this stuff. No matter what time I finally fall asleep or what I take, I'm awake at 6:45am. :-( Unless I pulled an all-nighter at work and have been up for 24+ hours... then I get that heavy feeling and never move. My wife can't even wake me up then.

[medievil]

Rozerem (Ramelteon): Very interesting, supposedly enhances the sensitivity of Melantonin receptors, perhaps if taken along with melantonin it might be excellent. I hate their commercials but that aside it looks very promising, I'd be curious to see the results from someone who has tried other sleep enhancers.


are there any papers showing that?

[edward]

Rozerem (Ramelteon): Very interesting, supposedly enhances the sensitivity of Melantonin receptors, perhaps if taken along with melantonin it might be excellent. I hate their commercials but that aside it looks very promising, I'd be curious to see the results from someone who has tried other sleep enhancers.


are there any papers showing that?

That is what I heard when it first came out. On further research I have found that it actually acts as a Melantonin Receptor Agonist (MT1 and MT2) http://jcp.sagepub.c.../47/4/485?rss=1

This makes it less interesting than I had at first thought.

[medievil]

Rozerem (Ramelteon): Very interesting, supposedly enhances the sensitivity of Melantonin receptors, perhaps if taken along with melantonin it might be excellent. I hate their commercials but that aside it looks very promising, I'd be curious to see the results from someone who has tried other sleep enhancers.


are there any papers showing that?

That is what I heard when it first came out. On further research I have found that it actually acts as a Melantonin Receptor Agonist (MT1 and MT2) http://jcp.sagepub.c.../47/4/485?rss=1

This makes it less interesting than I had at first thought.

I know it actis as an agonist thats why i asked
but it still might have advantages to melatonin...

Also, is there any substance that totally supresses REM sleep, i'm sure alot of you dont agree but i tend to think thats a good thing:)

[edward]

GHB aka Sodium Oxybate aka Xyrem (prescription) is the closest thing that I know of. Basically it sends you directly into about 3 or 4 hours of uninterrupted slow wave sleep with minimal REM. http://www.immunesup...cle.cfm/id/4850

As I mentioned I tried this awhile back as a substitute for and to augment real sleep and it works well for a few days but then there are some major sleep deprivation side effects. My conclusion on my little self experiement was that REM is important, for what I haven't a clue since there are so many theories, but at least for me, without REM I don't feel quite right.

[medievil]

GHB aka Sodium Oxybate aka Xyrem (prescription) is the closest thing that I know of. Basically it sends you directly into about 3 or 4 hours of uninterrupted slow wave sleep with minimal REM. http://www.immunesup...cle.cfm/id/4850

As I mentioned I tried this awhile back as a substitute for and to augment real sleep and it works well for a few days but then there are some major sleep deprivation side effects. My conclusion on my little self experiement was that REM is important, for what I haven't a clue since there are so many theories, but at least for me, without REM I don't feel quite right.

weird, i know phenelzine (a maoi) fully supresses rem sleep
the day it kicks in is associated with full rem inhibition
the antidepressant effects of sleep deprivation are also associated with "avoiding rem"

reports on GHB are very minimal tough, so i'l have to try myself before i can make a conclusion

[bacopacabana]

I suffered from insomnia for about 15 years. This past year I did neurofeedback and substantially cured it. Went from using ambien every single night for 10+ years to about two nights a month. The nice thing about neurofeedback is that it's a permanent cure, although it's expensive and somewhat time consuming. You teach the brain a better way to operate, as opposed to trying to force it into doing something with drugs or supps.

Ambien is the only thing that really worked for me. Lunesta didn't cut it, melatonin and the other supplements are a joke to me, although I take melatonin for other reasons. Tried some Neurontin a friend gave me for a couple of weeks - nothing (besides the major side effects). Have not tried Ambien CR, it sounds like an ideal solution, but friends of mine have tried it and gone back to the regular.

[meatwad]

Warning for those taking GHB concurrently with deprenyl (or deprenyl within a short period of time.) GHB has a rebound affect on dopamine levels, and with deprenyl you can find yourselves in quite a dopamine abundant state.

I felt psychotic several days after using GHB, the sleep was incredible but the mania that ensued was so stressful that I nearly killed myself.

Deprenyl + GHB is a BAD idea.

Ambien is obviously a gift from God himself though.

[meatwad]

I heard 5-htp insufflated (ie snorted) worked very well, in very small amounts. like, 30-75 mg (match pinhead sized)

dunno abuot melatonin though

[edward]

Now thats an idea, lol I thought my days of snorting stuff were over long ago lol. Don't think ill go there.

[tintinet]

Moi non plus:

"The olfactory nerves provide a direct connection to the central nervous system and may serve as a route of entry for a variety of exogenous substances, including viruses, solvents and some metals (Evans and Hastings 1992). This mechanism may contribute to some of the olfactory-related dementias (Monteagudo, Cassidy and Folb 1989; Bonnefoi, Monticello and Morgan 1991) through, for example, transmittal of aluminium centrally. Intranasally, but not intraperitoneally or intracheally, applied cadmium can be detected in the ipsilateral olfactory bulb (Evans and Hastings 1992). There is further evidence that substances may be preferentially taken up by olfactory tissue irrespective of the site of initial exposure (e.g., systemic versus inhalation). Mercury, for example, has been found in high concentrations in the olfactory brain region in subjects with dental amalgams (Siblerud 1990). On electroencephalography, the olfactory bulb demonstrates sensitivity to many atmospheric pollutants, such as acetone, benzene, ammonia, formaldehyde and ozone (Bokina et al. 1976). Because of central nervous system effects of some hydrocarbon solvents, exposed individuals might not readily recognize and distance themselves from the danger, thereby prolonging exposure. Recently, Callender and colleagues (1993) obtained a 94% frequency of abnormal SPECT scans, which assess regional cerebral blood flow, in subjects with neurotoxin exposures and a high frequency of olfactory identification disorders. The location of abnormalities on SPECT scanning was consistent with distribution of toxin through olfactory pathways."

Encylopedia of Occupational Health and Safety

[edward]

Update:

Currently taking Ambien CR 12.5 mg along with 3mg regular release melantonin and 3mg timed release melantonin (along with ashwagandha and bacopa)

Interestingly I am not getting the expected response from the Ambien CR. I expected it to be much like Lunesta / Immovane (ezopiclone / zopiclone) i.e. seven to nine hours of sleep, wake up feeling refreshed but not have the memory issues the Lun/Imm seemed to have.

Basically I sleep wonderfully for about 4-5 hours then wake up energized and refreshed but wondering as to why I didn't continue to sleep, I seem to function fine with no memory problems but I am a little hesitant about living on only 4-5 hours of sleep. Basically I am getting the same result from Ambien CR that I got from regular Ambien, which is very weird as it should last longer. Any thoughts?

[zoolander]

Basho,

LEF Melatonin Natural Sleep (includes C, Niacin, B6, B12, Calcium, Magnesium, Chromium, Melatonin immidiate release 2.5 mg, Melatonin timed release 2.5 mg, and Inositol)
LEF Glycine 3000mg
L-Theanine 100mg (not always)
Bacopa 225 - 450 mg (not always)
LEF Ashwagandha (Stimulant Free) 125mg

That is a sound regime and can be explained easily with logic. I take the same minus the glycine and bacopa. I have 5-HTP added to the above regime.

I'm very fortunate in that I have never had problems with sleep. I can count the amount of times on one hand where I've had a night of disturbed sleep. Keep in mind that I do shift work that include the dreaded graveyard. Additionally I can also count on one hand the amount of times that I've had a headache (not migrane) in my life i.e (less than 5 times). I know I know.....I'm rubbing it in.

[meatwad]

I think I will be adding in melatonin for the oxidant help. I have ambien (WHICH IS A GODSEND!) - I had a very problematic sleep cycle and it was causing me psychotic problems. Now it has been months and i sleep fine, all anxiety issues have been cleared up.

melatonin may increase the helpfulness of a real sleep cycle so I will start tonight.

[lucid]

Basically I sleep wonderfully for about 4-5 hours then wake up energized and refreshed but wondering as to why I didn't continue to sleep,

Well when I took larger doses of melatonin I didn't sleep as long, even with some of it being time released. I imagine that the body releases some counter hormone to drive melatonin levels down. Hence too much to start with will make you wake up sooner. (but put you in a deep sleep faster)

[zoolander]

Now thats an idea, lol I thought my days of snorting stuff were over long ago lol.

I wouldn't go there.

[FunkOdyssey]

Well when I took larger doses of melatonin I didn't sleep as long, even with some of it being time released. I imagine that the body releases some counter hormone to drive melatonin levels down. Hence too much to start with will make you wake up sooner. (but put you in a deep sleep faster)

Something similar happens to my fiancee and I. A large-ish dose (2mg) of immediate release melatonin prevented us from sleeping whatsoever for a few hours immediately after ingestion. In another experiment, 500mcg of a time-release formulation allowed us to sleep initially at 10:30pm, but then we both awoke around 2am and could not fall back asleep until 4-5am. I find it very strange that we would both have this unusual, paradoxical reaction to a substance that seems to be universally helpful for others. Any ideas for the mechanism here? Maybe the exogenous melatonin is desensitizing the receptors?

The brand used was Source Naturals.

[lucid]

I have tried lots of different brands and dosages. And for me 2mg Source Natrurals (1mg instant release, 1mg time released) is best. I weigh 240lbs though, so for you smaller folk, I would try a smaller dosage.

[tedsez]

Those of you who take regular Ambien (not CR) should know that there's now a generic version available.

At the Costco pharmacy, you can get 10 pills for less than $5.

[diamondhead]

I heard 5-htp insufflated (ie snorted) worked very well, in very small amounts. like, 30-75 mg (match pinhead sized)

dunno abuot melatonin though

very odd