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HBr

Valerian for sleep improvement

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Doesn't do anything noticeable. Studies generally don't show efficacy for valerian doing anything either. Kava if used properly is probably the only thing close to herbal that might improve sleep. Downside is that it can interact with medications and it tastes like dirt. 

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I tried this a few years ago.  I don't remember the exact details of the dose or brand, but it was something I picked up at Boots (essentially, our CVS) to try as I was looking for some relief and thought this was worth a try at the time.  I think it might have been Kalms, but don't quote me on that.  (http://www.kalmsrange.com/)  

I didn't find that it did anything noticeable, and after about 2-3 weeks of giving it a go, I eventually ditched it.  Of course, your mileage may vary and there's always interactions to think about, but personally, it didn't do anything for me.

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Thanks for the input, Jasonm and Athene. Kava didn't work for me. I recall IH saying valerian was good and there's plenty of positive reviews out there. The effectiveness may depend on the formulation - apparently the extraction process leaves little "isovaltrate, which has been shown to be an inverse agonist for adenosine A1 receptor sites."*

* Wikipedia

EDIT: The Wikipedia link may be wrong about the "inverse agonist for adenosine A1 receptor sites" part, so please read the next article by nutraingredients.com.

This method of action interests me as I've read that one way sleep can be fragmented is for adenosine to be 'burned-off' too quickly and this isovaltrate has been shown to increase it, as I understand.

http://www.nutraingredients.com/Research/Scientists-unravel-mechanism-behind-valerian-s-calming-effect

Perhaps the ground-up root itself would be better?

I'm seeing a benefit from orexin-a, but it is frustrating to still have severe sleep fragmentation and Lyrica and Trazadone and Baclofen, and many others, all failed me.

The PONS area of the brain stem is not often discussed in conjunction with sleep regulation, but it has a lot to do with REM regulation and is vulnerable to damage from toxins such as alcohol. In that vein, I'm also going to look into re-myelination* herbs/supplements. Suggestions on this are welcome as well.

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2737567/

https://en.wikipedia.org/wiki/Pons

250px-Gray768.png

If you suffer from tinnitus, apparently the PONS area has connections to the cochlear nerve as well.

* Healthy food sources: :)

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http://www.livestrong.com/article/500681-foods-that-improve-myelination/

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An inverse agonist is similar in function to an antagonist actually. The naming is confusing. It actually can be more potent. Antagonizing adenosine receptors would generally be bad. That's caffeine's mechanism of action. One problem with a lot of herbal stuff is they are generally dirty drugs in that they might produce sedating effects with one receptor and activating with another. Add on to the fact that several studies have shown often times there's little to none of the herb in supplements and they are usually a waste. 

Kava definitely can be a sedating herb. It can get you intoxicated if used properly in enough quantity. Unfortunately most people don't know enough about kava to get any benefit, not that I'm recommending it. If you want to increase adenosine activity, there's really only two ways to do it I've found with evidentiary support. Don't use caffeine and exercise. 

Sleep fragmentation is the most difficult kind of insomnia to treat. Trust me I feel your pain! If you take adderall, it's going to worsen it. I've never found much that works for long. I think an intelligent combination approach is probably best but strictly taboo in the medical community. Low dose doxepin and lunesta might work for awhile. 

 

 

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I probably shouldn't have linked to Wikipedia - the relevant info is in the following article re: adenosine.

http://www.nutraingredients.com/Research/Scientists-unravel-mechanism-behind-valerian-s-calming-effect

One may need access to friends in 'medical places' to get the 'good stuff'!? In the fairly distant past, hospitals did find a way to give me what I rated as my best lifetime sleep - I want more, lots more!

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HBr

Just a word of caution if you dont mind. Be very careful with "natural" supplements please, just because they are ticketed as natural does not mean they are harmless. I would also caution against buying any supplement from herbal suppliers. First you have no idea what the actual combination is in the tablet you buy, every manufacturer will use different combinations. Also in order for any of these suppliers to make a profit they must mass produce these supplements and they have to have a long shelf life in the store which means that there has to be some type of preservative added to be able to accomplish this. (some well known preservatives are silica, alcohol, propylene glycol, shellac, aspartame and sulfites, does'nt really sound very natural does it.

With all this being said I am a great fan of natural medicine conducted appropriately, perhaps consult with an herbalist may prove of some benefit for you. If this is the route you choose please do not expect an overnight result, not gonna happen, most truly natural therapies take months

Best of luck

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14 hours ago, Natdoc said:

some well known preservatives are silica, alcohol, propylene glycol, shellac, aspartame and sulfites, does'nt really sound very natural does it.

So is the organic herb itself a better idea? And used in moderation, of course - we don't want to be getting high on the wild wood weed, now do we? :)

Apparently, in the case of valerian anyway, the extraction process can destroy some wanted active ingredients, never mind the antifreeze and wood preservative additives.

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Okay after doing some more digging, the research conducted so far shows the dry valerian and alcohol root extracts do not work for improving sleep. The water extract, however may increase slow wave sleep. I always tried the dried form, which seems to act as wikipedia states, an adenosine receptor inverse agonist. The water extract form seems to act as a partial agonist of one receptor subtype. It doesn't seem to improve subjective sleep quality or increase duration of sleep.

It's not clear what dose would be optimal or what the half life of the active constituent is. It's also unclear if alcohols destroy the active constituent or if the constituent is simply better extracted by water. In a nut shell, you'd want to find a water extracted from the roots of the plant form.

One last thing I'll say is damn near every supplement has good reviews from people. The placebo effect is a powerful thing. 

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1 hour ago, Jasonm said:

the active constituent

There's more than one. The extraction medium is important and shelf-life and contaminants are an issue for almost everything we ingest. 

I'm willing to experiment provided I deem the supplier to be reasonably trustworthy. A university sleep doctor in my city, says all meds for sleep issues cause more problems than they solve (he still Rxs Xyrem for N though), otherwise, he's a fan of CBTi.

Personally, I've seen far fewer negative side effects from supplements/herbals than Rx meds and some indication of better positive effects too.

The articles I read suggest the alcohol extraction method produces more active ingredients, including the adenosine effect I referred to.

Until recently it was assumed that valerian intervened in the GABA regulatory circuit. GABA is a chemotransmitter and one of various chemicals in the brain that bring on a feeling of tiredness.But the new research suggests that valerian works on a different 'tiredness molecule' called adenosine, targeting specific adenosine receptors of type A1 and triggering drowsiness.  Caffeine can also attach itself to the same receptors but it merely blocks the A1 receptors without causing a reaction. The result is that the coffee drinker becomes more wide awake.  Christa Müller, professor of Pharmaceutical Chemistry at Bonn, said: "We repeated the experiments and were able to confirm that aqueous alcoholic full extracts from the valerian root can attach themselves to the A1 receptor, at least in the brains of rats."  "What is more, we were able to show for the first time that the extract activates the receptors rather like adenosine does. Experiments with genetically produced human receptors had a similar result," she addd.

And also:

B. Schumacher, S. Scholle, J. Hölzl, N. Khudeir, S. Hess, and C. E. Müller, “Lignans isolated from Valerian: identification and characterization of a new olivil derivative with partial agonistic activity at A1 adenosine receptors,” Journal of Natural Products, vol. 65, no. 10, pp. 1479–1485, 2002. View at Publisher · View at Google Scholar · View at Scopus

Here's the nih abstract:

Lignans isolated from valerian: identification and characterization of a new olivil derivative with partial agonistic activity at A(1) adenosine receptors.

I will try to find a supplier and I'll be the lab rat! :)

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Valerian seemed to have too powerful an effect as far as causing more EDS the next day, and I couldn't particularly tell my sleep was more restful, though it didtend to knock me out pretty good. I'd say its a decent insomnia cure, but only if you can get away with taking a small dose, other wise you'll wake up a zombie.

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2 hours ago, DeathRabbit said:

Valerian seemed to have too powerful an effect as far as causing more EDS the next day, and I couldn't particularly tell my sleep was more restful, though it didtend to knock me out pretty good. I'd say its a decent insomnia cure, but only if you can get away with taking a small dose, other wise you'll wake up a zombie.

I have a problem with all the gaba drugs - they tend to help me sleep a bit better the first half of the night, initially at least, and then seem to keep me awake for the second half. So, like you say, you get diminishing returns the next day.

I was hoping that if I could get the right formulation and get that adenosine thing to kick in, I might overcome the unwanted gaba effect. We tend to grasp at straws in our desperation. I've spent 2 years trying to convince my doctors to let me try Xyrem, but I'm aware of the poor odds of it actually working for me. Then what? Orexin-a seems like it's working, but you can't ignore the sleep part or nothing will work for long.

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You're right hbr. That's what I get for using the word alcohol instead of ethanol. Ethanol extracts don't seem to work. They used methanol, a different "alcohol" for the extraction in the study you mentioned. Question becomes how in the world do you find out the extraction method. 

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3 hours ago, Jasonm said:

You're right hbr. That's what I get for using the word alcohol instead of ethanol. Ethanol extracts don't seem to work. They used methanol, a different "alcohol" for the extraction in the study you mentioned. Question becomes how in the world do you find out the extraction method. 

Could you please point out the reference to "methanol"? Thanks!

Suppliers may provide info on request. For example: Herb Pharm.

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It's the first sentence of the abstract you linked to above. 

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On the topic of adenosine, medicinal mushrooms such as Reishi or Lion's Mane directly contain adenosine:

http://www.dl.begellhouse.com/journals/708ae68d64b17c52,23ce65314f371f4f,1aa242b64fe041c7.html

https://www.mdidea.com/products/new/new03608.html (Ctrl+F Adenosine. The whole CNS effects section sounds promising)

On the whole, more sustainable than Gaba agonists and they have neurogenic effects themselves while modulating the immune system (lowers inflammation, raises immunity). Not sure what taking it would do after taking coffee in the morning but it's worth a shot.

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I totally read that as magical mushrooms. Adenosine unfortunately has a half life of 10 seconds so consuming it probably won't do much. 

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27 minutes ago, Jasonm said:

Thanks. The hindawi article was done in Puerto Rico and apparently used ethanol, however, the Bonn study referring to adenosine used methanol*. I was conflating the two different studies.

* I'm not sure that is a critical matter though - it may be just aqueous vs. ethanol/methanol, i.e. alcohol?

Note that the nutraingredients article says:

Christa Müller, professor of Pharmaceutical Chemistry at Bonn, said: "We repeated the experiments and were able to confirm that aqueous alcoholic full extracts from the valerian root can attach themselves to the A1 receptor"

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36 minutes ago, Jasonm said:

Adenosine unfortunately has a half life of 10 seconds so consuming it probably won't do much. 

Yes, the Bonn study mentions that problem.

37 minutes ago, Jasonm said:

magical mushrooms

I have an old buddy of mine who swears by these. Peace, brother. :)

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1 hour ago, HBr said:

Thanks. The hindawi article was done in Puerto Rico and apparently used ethanol, however, the Bonn study referring to adenosine used methanol*. I was conflating the two different studies.

* I'm not sure that is a critical matter though - it may be just aqueous vs. ethanol/methanol, i.e. alcohol?

Note that the nutraingredients article says:

Christa Müller, professor of Pharmaceutical Chemistry at Bonn, said: "We repeated the experiments and were able to confirm that aqueous alcoholic full extracts from the valerian root can attach themselves to the A1 receptor"

If you read the research paper, the Bonn study used methanol, which is the alcohol they are referring to, not ethanol. Ethanol extracts in at least one study didn't have the adenosine agonist quality. 

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The Hindawi article states:

2.2. Valerian Extracts:

Quote

Organically grown and certified Valerian dry powdered roots (Lot. 1111H-OUP), harvested in 2004, were obtained from Pacific Botanicals (LLC Grants Pass, Oregon). Commercial Valerian. Nature’s Resources Extract (Lot. LD11282N) and Nature’s Resource Herb (Lot. MG11258) were purchased from a local pharmacy. Valerian was extracted in ultra pure water or ethyl alcohol (EtOH) 70% (1 : 10 w/v) at ~23°C, stirred for 1 hour, and filtered through a 12.5 cm Whatman Qualitative no. 1 filter. Aliquots were centrifuged at 6,700 g to remove particulates and stored at 4°C.

EtOH = ethanol?

And in their abstract  and 'Results':

Quote

the hydroalcoholic extract markedly potentiated (200%) [3H]FW binding to AMPA receptors.

Aren't both studies seeing much the same results, even though only the Bonn study goes on to elucidate that effect as adenosine release?

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