187 replies to this topic

[niner]

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

Do you mean micrograms? mg is the usual abbreviation for milligram. Microgram is usually abbreviated with a Greek mu, which looks kind of like a "u". In ASCII, people sometimes use "ug" for microgram. 30-75 mg would be a pretty good sized little pile, way bigger than a pinhead. Sorry to be such a pedant, but in medications, a factor of a thousand can cause a lot of trouble.

[edward]

Snorting anything other than prescription (sterile, pure, and especially prepared for nasal administration) sinus, allergy and asthma type medications is frankly, stupid and probably not conducive to the extension of life.

[krillin]

I used to dab capsaicin cream on the inside of my nostrils to combat muscle tension. It worked even better than eating cayenne powder. Both had quite a time delay: something like 45 minutes until the wave of relaxation came over the body. Didn't feel like the endorphins I get (only when allergen load is low) from DLPA/chocolate or low dose naltrexone. Capsaicin on skin didn't work: you have to burn mucosal tissue for it to work. It doesn't work anymore, as my body is dead set on having me suffer.

Possible mechanism:

Cephalalgia. 1993 Apr;13(2):114-6.
A double-blind placebo-controlled trial of intranasal capsaicin for cluster headache.
Marks DR, Rapoport A, Padla D, Weeks R, Rosum R, Sheftell F, Arrowsmith F.
Clinical Immunology Unit, Massachusetts General Hospital, Boston 92114.

It has been suggested that treatment of cluster headache (CH) patients with topical capsaicin may desensitize sensory neurons by depleting the nerve terminals of substance P. We attempted to determine whether capsaicin is effective in aborting CH attacks. Patients in acute cluster were randomized to receive either capsaicin or placebo in the ipsilateral nostril for 7 days. Patients recorded the severity of each headache for 15 days. Headaches on days 8-15 of the study were significantly less severe in the capsaicin group vs the placebo group. There was also a significant decrease in headache severity in the capsaicin group on days 8-15 compared to days 1-7, but not in the placebo group. Episodic CH patients appeared to benefit more than chronic CH patients. These results indicate that intranasal capsaicin may provide a new therapeutic option for the treatment of this disease.

PMID: 8495452

[health_nutty]

ouch! I can't imagine that being worth it, you must be in some serious pain.

[Gerald W. Gaston]

Still not having much success with getting more than 4-5hrs sleep lately. No matter what I take (haven't tried Ambien or such yet).

Past 3 nights I have added X-Dream (3-OH-GABA and N-Arachidonyl-dopamine HCl). Got it from NutraPlanet - See: http://www.ibe-techn...ucts.php?pid=19

This doesn't seem to phase me in the least.

I dropped Swanson Sleep Essentials (which has Valerian, 3mg Melatonin, and GABA) about 2 weeks ago.

Nothing seems to do it these days. In the right mood, environment, etc., yes they do have a calming effect, but I just can't seem to shutdown.

Anyway, just curious if anyone else had tried X-Dream.

[quarter]

I just wanted to bump this to see if there were any more thoughts on melatonin plus 5-HTP?

I already take melatonin. Heard some good reports about 5-HTP and was wondering if it was worth adding as I am currently under a lot of stress at work and could do with something to take the edge off at night?

Also would 5-HTP be a better option than L-Tryptophan? What is the comparison between the two in terms of efficacy and saftety?

Sorry if this has been asked before, I did search but I couldn't discern conclusive answers (maybe there arn't any but I thought I'd ask anyway).

[krillin]

I just wanted to bump this to see if there were any more thoughts on melatonin plus 5-HTP?

I already take melatonin. Heard some good reports about 5-HTP and was wondering if it was worth adding as I am currently under a lot of stress at work and could do with something to take the edge off at night?

Also would  5-HTP be a better option than L-Tryptophan? What is the comparison between the two in terms of efficacy and saftety?

Sorry if this has been asked before, I did search but I couldn't discern conclusive answers (maybe there arn't any but I thought I'd ask anyway).

Meatwad nearly died from a 5-HTP induced gastric lesion. 5-HTP is taken up by stomach cells and converted to serotonin. Serotonin causes acetylcholine release which causes stomach acid secretion.

The silver lining to Meatwad's pain is that it's given me an idea as to how to get rid of my mold allergy muscle tension. Leaving the mold belt got rid of my joint inflammation and psychological cortisol symptoms (despair attacks, anxiety, insomnia), but the water retention and tonic muscle tension remain. I used to blame those on cortisol too, but every anti-cortisol trick in the book failed. Going outside almost instantly gets rid of the tension: much too quick for it to be a cortisol effect. My new theory is that mast cells release some mediator that activates the trigeminal nerve, which releases substance P which causes brain mast cells to release serotonin which increases anti-diuretic hormone and acetylcholine and bang, my muscles assume the dead bug position. This must be why nasally applied capsaicin used to cause a wave of relaxation: it depletes substance P and prevents the trigeminal nerve from signaling.

I'm taking a slew of phytochemicals that inhibit mast cell degranulation (Citrus bioflavonoids were the first, added to my stack in 1996, and have kept histamine symptoms at bay to this day. Unless I take low-dose naltrexone. Endorphins massively increase degranulation.), but mast cells can release their other mediators (serotonin, cytokines, etc) without degranulation, in a process sometimes called "differential secretion". I tried 1 g quercetin in the past to stop this to no avail. It might have been poorly absorbed, so I'm going to try Algonot Plus, which has quercetin in olive kernel oil to improve absorption.

Additionally, I'll try feverfew, which is a serotonin antagonist and inhibits serotonin secretion (PMID: 17163262, 11603284).

[edward]

Update:

Current Sleep Stack (Monday- Friday as the weekends are much less regimented):

Taken at around 9pm due to long half lives:
450 mg Ashwagandha (4.5%)
450 mg Bacopa (20%)

Taken at Bedtime 11pm or so:
3 mg Melatonin Immediate Release
3 mg Melatonin Timed Release
15 mg Ambien (generic, the CR is just too expensive and I have found the benefits negligible)

[Mind]

Frankbuzzin. You could always try physical exhaustion (maybe along with some light sleep supps). It works pretty good for me. Something strenuous, but not real hard on the joints, like swimming, light weights for a long period of time, and a nice 10 mile walk/jog....all in the same day, then go down to the Salvation army soup kitchen and unload a truckload of potatoes. Then crash for a nice 10 hour night sleep.

[hulahoop]

5htp has been most successful in helping me sleep and i combine with valerian when needed. i find keeping consistent sleep times is very helpful, as well as exercise.

i also take synthroid and i believe that interferes with sleep.

interested in gaba as a stress reliever - stress (obviously) adds to sleep disturbance.

tried melatonin, but only worked for 1-2 nights. similar problem with valerian.

[hulahoop]

I just wanted to bump this to see if there were any more thoughts on melatonin plus 5-HTP?

I already take melatonin. Heard some good reports about 5-HTP and was wondering if it was worth adding as I am currently under a lot of stress at work and could do with something to take the edge off at night?

Also would  5-HTP be a better option than L-Tryptophan? What is the comparison between the two in terms of efficacy and saftety?

Sorry if this has been asked before, I did search but I couldn't discern conclusive answers (maybe there arn't any but I thought I'd ask anyway).

Meatwad nearly died from a 5-HTP induced gastric lesion. 5-HTP is taken up by stomach cells and converted to serotonin. Serotonin causes acetylcholine release which causes stomach acid secretion.

The silver lining to Meatwad's pain is that it's given me an idea as to how to get rid of my mold allergy muscle tension. Leaving the mold belt got rid of my joint inflammation and psychological cortisol symptoms (despair attacks, anxiety, insomnia), but the water retention and tonic muscle tension remain. I used to blame those on cortisol too, but every anti-cortisol trick in the book failed. Going outside almost instantly gets rid of the tension: much too quick for it to be a cortisol effect. My new theory is that mast cells release some mediator that activates the trigeminal nerve, which releases substance P which causes brain mast cells to release serotonin which increases anti-diuretic hormone and acetylcholine and bang, my muscles assume the dead bug position. This must be why nasally applied capsaicin used to cause a wave of relaxation: it depletes substance P and prevents the trigeminal nerve from signaling.

I'm taking a slew of phytochemicals that inhibit mast cell degranulation (Citrus bioflavonoids were the first, added to my stack in 1996, and have kept histamine symptoms at bay to this day. Unless I take low-dose naltrexone. Endorphins massively increase degranulation.), but mast cells can release their other mediators (serotonin, cytokines, etc) without degranulation, in a process sometimes called "differential secretion". I tried 1 g quercetin in the past to stop this to no avail. It might have been poorly absorbed, so I'm going to try Algonot Plus, which has quercetin in olive kernel oil to improve absorption.

Additionally, I'll try feverfew, which is a serotonin antagonist and inhibits serotonin secretion (PMID: 17163262, 11603284).

[hulahoop]

i have no scientific reason, but take acidophilus in the night with 5htp and calcium. (sometimes i add valerian which can make me feel like my heart rate is slower and scares me.) anyway, acidophilus is great for stomach acid.

[malbecman]

When I was having difficulty sleeping, I found meditation very useful (and still do). I tend to have an overactive mind which likes to try to think and plan about the future a lot. Meditation, specifically the Vipassana kind, usually enables me to decouple my mind and its thoughts and allow me a good nights sleep. I also exercise regularly which I also find very useful.

I am of the mindset that sleep and the need for rest is natural. Most people should not need daily chemical help to get them to sleep. There is likely something else going on that needs your attention......

[krillin]

I guess I'll update my post that hulahoop just quoted without comment: feverfew does nothing for me, so serotonin probably isn't in the chain of nastiness. Substance P and CGRP can elevate acetylcholine on their own.

[chipdouglas]

Serotonin causes acetylcholine release which causes stomach acid secretion.

Would you be so kind as to provide scientific reference to the above quote ? I'm not saying this sarcastically, but this is information I've been wondering about for a long time.

Thanks

[krillin]

Would you be so kind as to provide scientific reference to the above quote ? I'm not saying this sarcastically, but this is information I've been wondering about for a long time.

Thanks

Here's evidence of 5-HTP in the stomach being converted to serotonin in the stomach cells, which causes acetylcholine release. The second abstract explains how acetylcholine causes stomach acid secretion.

Eur J Pharmacol. 1986 Aug 15;127(3):179-85
Increased gastric cholinergic activity evoked by 5-hydroxy-L-tryptophan in the rat.
Sanger GJ, McClelland CM.

In gastrointestinal tissues such as rat stomach, exogenous 5-hydroxytryptamine (5HT) has little or no ability to affect nerve activity. However, endogenous 5HT might act differently, and this was investigated by stimulating 5HT synthesis using 5-hydroxy-L-tryptophan (5HTP). In longitudinal strips of rat forestomach, 5HTP (50 and 500 microM) increased cholinergically mediated contractions evoked by electrical field stimulation, probably by facilitating acetylcholine release; contractions evoked by exogenous acetylcholine were unaffected by 5HTP. The ability of 5HTP to increase electrically evoked contractions was long-lasting, required the presence of pyridoxal (a monoamine decarboxylase cofactor) and was reduced by the decarboxylase inhibitor carbidopa, but not by 6-hydroxydopamine. In the presence of paroxetine and nialamide, the 5HTP-induced increase in cholinergically mediated contractions was short-lasting. In anaesthetised rats 5HTP caused stimulation of gastric motility, which was blocked or reduced by atropine. These findings suggest that in the rat 5HTP stimulates gastric cholinergic activity, by increasing the concentration of 5HT at sites which normally synthesise 5HT.

PMID: 3019729

Curr Opin Gastroenterol. 2001 Nov;17(6):481-8.
Gastric secretion.
Schubert ML.
Department of Medicine, Division of Gastroenterology, Medical College of Virginia and McGuire VAMC, Richmond, Virginia 23249, USA. mitchell.schubert@med.va.gov

The influence of central and peripheral stimuli on gastric acid secretion is mediated via activation of histaminergic, gastrinergic, and cholinergic pathways coupled to intracellular second-messenger systems that determine the trafficking and activity of H+ K+-ATPase, the proton pump of the parietal cell. Histamine, released from enterochromaffin-like cells stimulates the parietal cell directly via H-2 receptors coupled to generation of cAMP. Gastrin, acting via cholecystokinin-2 receptors on enterochromaffin-like cells coupled to an increase in intracellular calcium, stimulates the parietal cell indirectly by activating histidine decarboxylase, releasing histamine, and inducing enterochromaffin-like cell hypertrophy and hyperplasia. Acetylcholine, released from gastric postganglionic intramural neurons, stimulates the parietal cell directly via M-3 receptors coupled to intracellular calcium release and calcium entry. The second-messenger systems activated in the parietal cell converge on H+ K+-ATPase that catalyzes the exchange of luminal K+ for cytoplasmic H+ and is responsible for gastric luminal acidification. The main inhibitor of acid secretion is somatostatin which, acting via sst2 receptors, exerts a tonic inhibitory influence on parietal, enterochromaffin-like, and gastrin cells. Acute infection with Helicobacter pylori results in hypochlorhydria, whereas chronic infection may be associated with either hypo- or hyperchlorhydria. Although prostaglandins are thought to play a physiologic role in the regulation of acid secretion and maintenance of gastric mucosal integrity, the precise roles of cyclooxygenase-1 and cyclooxygenase-2 in these processes still eludes us.

PMID: 17031207

There's also the possibility that the 5-HTP gastric lesions are initiated by reduced blood flow (due to vasoconstriction?), and that increased stomach acid merely aggravates things.

Pharmacol Res. 1999 Apr;39(4):261-7.
Role of endogenous serotonin and histamine in the pathogenesis of gastric mucosal lesions in unanaesthetised rats with a single treatment of compound 48/80, a mast cell degranulator.
Ohta Y, Kobayashi T, Ishiguro I.
Department of Biochemistry, School of Medicine, Fujita Health University, Toyoake, Aichi, 470-1192, Japan.

In unanaethetised rats with a single injection of compound 48/80, a mast cell degranulator (0.75 mg kg-1, i.p.), gastric lesions occurred with increased serum serotonin and histamine levels and reduced gastric mucosal blood flow at 0.5 h after the injection and developed at 3 h. Pretreatment with either cyproheptadine (a serotonin and histamine antagonist) or methysergide (a serotonin antagonist) prevented the formation of gastric mucosal lesions with attenuation of reduced gastric mucosal blood flow at 0.5 h after compound 48/80 injection, while pretreatment with either amitriptyline (a selective inhibitor of histamine release from mast cells), tripelennamine (a histamine H1-receptor antagonist), famotidine (a histamine H2-receptor antagonist) or cimetidine (a histamine H2-receptor antagonist) had no effect. Pretreatment with either cyproheptadine, methysergide, amitriptyline or tripelennamine prevented the development of gastric mucosal lesions at 3 h after compound 48/80 injection, while pretreatment with either famotidine or cimetidine had no effect. These results indicate that in unanaesthetised rats with a single compound 48/80 treatment, acutely released endogenous serotonin causes gastric mucosal lesions, while released endogenous histamine mainly contributes to the lesion development and that gastric acid plays little role in the pathogenesis of the compound 48/80-induced acute gastric lesions. Copyright 1999 The Italian Pharmacological Society.

PMID: 10208755

[chipdouglas]

Thanks Krillin

[rfarris]

I really like phenibut, but I can only use it three or four times a week, or it quits working. So I need to take a pharmaceutical sleep aid once or twice a week.

My doctor suggested Lunesta and gave me some 2mg samples. The 2mg dose didn't help much -- it took me more than an hour to get to sleep and I still awakened every hour or two. I tried 4mg, and I got to sleep but it wasn't nearly as deep a sleep as phenibut.

My question is: Is Ambien stronger? Should I ask for some Ambien samples? Or is Lunesta as good as it gets?

Thank you.

[pycnogenol]

Hi, rfarris

Where do you get your Phenibut? I'm looking to try it out. I've taken Ambien and it worked
very quickly. I was able to get 9 solid hours of quality sleep with no morning grogginess,
headache or hangover. I have not tried Lunesta.

I regularly take Melatonin 1 to 2 hours before bedtime which helps somewhat but it's nowhere
near as effective as Ambien. Not even close.

A low-dose of Pamelor (Nortriptyline) taken 1 hour before bedtime will make me tired
but it can sometimes make me hung-over the next day.

Edited by pycnogenol, 29 September 2007 - 03:14 PM.

[edward]

I mentioned Lunesta (Ezopiclone, USA), Imovane (Zopiclone, outside USA) in the first post I made to start this thread. I found it to be the best sleep aid with regards to consistent results and no tolerance, perfect half life (5hrs) leading to 8-9 hours of perfect sleep. Studies show that it preserves natural sleep architecture as well.

The only problem I had was some memory issues with Lunesta which is why I take Ambien now instead. I might try it again and see if I have the same effect as Ambien is good but not as good as Lunesta.

[rfarris]

I get phenibut from Relentless Improvement.

[krillin]

J Pineal Res. 2006 Aug;41(1):73-8.
Comment in: J Pineal Res. 2007 Mar;42(2):210-1.
Blue blocker glasses impede the capacity of bright light to suppress melatonin production.
Sasseville A, Paquet N, Sévigny J, Hébert M.
Centre de recherche Université Laval Robert-Giffard/Département d'ophtalmologie, Québec City, QC, Canada.

Blocking morning light exposure with dark goggles can contribute to the adjustment to night work but these glasses are incompatible with driving. Recently, it was discovered that the biological clock is most sensitive to short wavelengths (blue light). Therefore, we tested the hypothesis that cutting the blue portion of the light spectrum with orange lens glasses (blue blockers) would prevent the light-induced melatonin suppression, a test broadly used as an indirect assessment of the circadian clock sensitivity. Fourteen normal subjects were exposed at night to a 60 min bright light pulse (1300 lx behind filters) between 01:00 and 02:00 hr while wearing orange lens glasses (experimental condition) or grey lens glasses (control condition). The amount of salivary melatonin change observed during the light pulse was compared with a melatonin baseline obtained the night before. Although both glasses transmitted the same illuminance (1300 lx) but at an irradiance 25% higher for the orange lens (408 microW/cm2) compared with the grey lens (327 microW/cm2), a non-significant increase of 6% (95% CI, -20% to 9%) was observed with the orange lens whereas a significant (P < 0.05) reduction of 46% (95% CI, 35-57%) was observed with the grey lens. Blue blockers represent an elegant means to prevent the light-induced melatonin suppression. Further studies are needed to show that these glasses, which are suitable for driving, could facilitate adaptation to night work.

PMID: 16842544

[wiserd]

My girlfriend has fibromyalgia, which is essentially an end stage of PTSD. It's nearly impossible for people with FM to get uninterupted deep sleep, and a lot of the symptoms of FM result from the body's inability to produce growth hormone, which is produced during deep sleep. She swears by L-theanine, though she seems to be building an increasing tolerance to it. She tried GABA and while it helped with sleep it made her nightmares unbearably worse, so she quit it and went back to the theanine.

REM sleep seems to be required for memory, incidentally, and a lot of memory enhancement herbs (like Gotu Kola) seem to increase dreaming.

Acetylcholine antagonists like scopolamine or atropine tend to remove the benefits of REM.
http://www.ncbi.nlm....Pubmed_RVDocSum

[edward]

Update Sleep Related Night Time Supps

450 mg Ashwagandha (4.5%)
450 mg Bacopa (20%)

3 mg Melatonin Immediate Release
3 mg Melatonin Timed Release
10 mg Ambien generic
300 mg Taurine

Edited by edward, 28 January 2008 - 03:34 AM.

[rfarris]

I get phenibut from Relentless Improvement.

Bulk is much cheaper. Pregabalin is fun stuff.

How much cheaper?

[Matt]

There is another natural method of increasing GABA levels, that is Yoga according to this study. They found a 30% increase after the session. Even when exhausted now I can only sleep for around 3-4 hours at a time, compared to about 10 hours prior to taking Cipro (antibiotic). It totally screwed up my brain... so I might try a few things in this thread, didn't see it around before. When I was exhausted by activities during the day, or if I spent more than 36 hours awake prior to cipro I could actually sleep for 12-18 hours straight. Hoping my sleep comes back to normal one day because its really hard when you're working.

I don't have any trouble falling to sleep anymore, not like the first month after I took it, I just can't stay asleep and I don't know why! I'm not anxious, depressed or anything like that. Even when I did have extreme anxiety a couple years back I slept very well lol.

Yoga May Elevate Brain GABA Levels, Suggesting Possible Treatment For Depression
http://www.scienceda...70521145516.htm

"The researchers found a twenty-seven percent increase in GABA levels in the yoga practitioner group"

Edited by Matt, 29 January 2008 - 05:47 PM.

[Ghostrider]

I have found that 600 EPA / 400 DHA of the Costco brand Omega3 fish oil seems to help me sleep deeper. I realized this when I became tired after taking it at work.

[Spiral Architect]

How do you use Phenibut? I've had some for a while but haven't tried it yet.

I take Melatonin (0.75mg) 3-4 times a week and small doses of GABA (0.5-2g) occasionally when my brain is too active and needs help slowing down before sleep. I have great sleep unless interrupted by too much light or noise.
I got Phenibut so it can knock me out occasionally when I have to go to sleep 3+ hours before the last night's sleeping hour. If I sleep well and have to go back to sleep again after 12-13 hours it takes a while to fall asleep and sleep is lighter.

I want to use it very sporadically and in small doses. What's the best way to approach this? I want to be conservative with it.

[edward]

How do you use Phenibut? I've had some for a while but haven't tried it yet.

I take Melatonin (0.75mg) 3-4 times a week and small doses of GABA (0.5-2g) occasionally when my brain is too active and needs help slowing down before sleep. I have great sleep unless interrupted by too much light or noise.
I got Phenibut so it can knock me out occasionally when I have to go to sleep 3+ hours before the last night's sleeping hour. If I sleep well and have to go back to sleep again after 12-13 hours it takes a while to fall asleep and sleep is lighter.

I want to use it very sporadically and in small doses. What's the best way to approach this? I want to be conservative with it.

I personally have never taken Phenibut, it is on my list of supps not to touch with a ten foot pole. I have read a lot about it. My conclusion is that it should only be used at maximum 3 times a week, preferably only once or twice a week. Apparently tolerance develops very quickly, and I have seen people escalate the dose dramatically and then end up in a situation where they are anxious all the time and can't sleep without a massive dose. To me it seems like advanced benzodiazepine addiction. But since I have never tried it I can't personally verify that tolerance develops quickly, I am only relaying what I have read on countless sites.