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Phenibut (beta-phenyl-GABA):


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#1 stellar

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Posted 01 December 2004 - 06:45 AM


1: CNS Drug Rev. 2001 Winter;7(4):471-81. Related Articles, Links

Phenibut (beta-phenyl-GABA): a tranquilizer and nootropic drug.

Lapin I.

Department of Clinical and Experimental Psychopharmacology, Bekhterev's Psychoneurological Institute, Bekhterev Street, 3, St. Petersburg, 193019, Russia. spbinstb@infopro.spb.su

Phenibut (beta-phenyl-gamma-aminobutyric acid HCl) is a neuropsychotropic drug that was discovered and introduced into clinical practice in Russia in the 1960s. It has anxiolytic and nootropic (cognition enhancing) effects. It acts as a GABA-mimetic, primarily at GABA(B) and, to some extent, at GABA(A) receptors. It also stimulates dopamine receptors and antagonizes beta-phenethylamine (PEA), a putative endogenous anxiogenic. The psychopharmacological activity of phenibut is similar to that of baclofen, a p-Cl-derivative of phenibut. This article reviews the structure-activity relationship of phenibut and its derivatives. Emphasis is placed on the importance of the position of the phenyl ring, the role of the carboxyl group, and the activity of optical isomers. Comparison of phenibut with piracetam and diazepam reveals similarities and differences in their pharmacological and clinical effects. Phenibut is widely used in Russia to relieve tension, anxiety, and fear, to improve sleep in psychosomatic or neurotic patients; as well as a pre- or post-operative medication. It is also used in the therapy of disorders characterized by asthenia and depression, as well as in post-traumatic stress, stuttering and vestibular disorders.

Publication Types:

* Review
* Review, Tutorial


PMID: 11830761 [PubMed - indexed for MEDLINE]


1: Pharmacol Toxicol. 1990 Jan;66(1):41-4. Related Articles, Links

Stress-protection action of beta-phenyl(GABA): involvement of central and peripheral type benzodiazepine binding sites.

Rago L, Kiivet RA, Adojaan A, Harro J, Allikmets L.

Department of Pharmacology, Tartu University, Estonia, USSR.

Forced swimming stress caused a significant increase in the density of central type benzodiazepine binding sites in rat cerebral cortex and hippocampus. The number of peripheral type benzodiazepine binding sites was also enhanced on blood platelets. The affinity of neither central nor peripheral type benzodiazepine binding sites was changed considerably after swimming stress. Pretreatment of rats with beta-(phenyl)GABA (100 mg/kg), a GABAB agonist, almost completely eliminated the described changes of the both types of benzodiazepine binding sites caused by swimming stress. In an elevated plus-maze model of anxiety beta-(phenyl)GABA itself was inactive but like diazepam effectively counteracted the behavioural effects of DMCM, a beta-carboline derivative with anxiogenic properties. The possible involvement of benzodiazepine receptors in the mechanism of action of beta-(phenyl)GABA is discussed.

PMID: 2155416 [PubMed - indexed for MEDLINE]

#2 nootropi

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Posted 01 December 2004 - 02:12 PM

Thanks for sharing the data, stellar.

Phenibut is perfect for treating acute anxiety. However, it also can make one too relaxed; so much so that, for example, one might say something they may regret later. Phenibut also reduces sensitivity to social cueing.

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#3 stellar

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Posted 01 December 2004 - 06:49 PM

I'm ordering some, can't wait to try it. Going to try it with high dose L-theanine, 500mg or more.

I really like Kava-Kava, but it's not something you can take constantly. I'll be able to cycle these different substances, Phenibut, L-Theanine and Kava Kava.

I might try magnesium at some point......

#4 stellar

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Posted 01 December 2004 - 07:26 PM

PS on rec.drugs.smart there is quite a bit of debate going on about the longevity in regards to legality of this stuff. Some say that it will be "banned", however, I'm not quite certain of that because GABA and other GABA agonists have been around for quite some time.

I've even seen discussions of people mentioning a method of vaporizing phenibut.

#5 geigertube

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Posted 02 December 2004 - 11:22 PM

Thanks for sharing the data, stellar.

Phenibut is perfect for treating acute anxiety.  However, it also can make one too relaxed; so much so that, for example, one might say something they may regret later.  Phenibut also reduces sensitivity to social cueing.



So it's kind of like the Internet in a pill, eh? :)

Steven

#6 scottl

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Posted 02 December 2004 - 11:31 PM

:)

#7 olderbutwiser

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Posted 03 December 2004 - 01:28 AM

PS on rec.drugs.smart there is quite a bit of debate going on about the longevity in regards to legality of this stuff. Some say that it will be "banned", however, I'm not quite certain of that because GABA and other GABA agonists have been around for quite some time.

GHB was banned. and vilified.
If Phenibut remains on the market, it will be because it is less effective and with less abuse potential. If people are smoking Phenibut, the end is near.

OBW

#8 nootropi

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Posted 04 December 2004 - 05:53 PM

Thanks for sharing the data, stellar.

Phenibut is perfect for treating acute anxiety.  However, it also can make one too relaxed; so much so that, for example, one might say something they may regret later.  Phenibut also reduces sensitivity to social cueing.



So it's kind of like the Internet in a pill, eh? :)

Steven


No, the Internet does not treat acute anxiety, neither does it make one feel too relaxed; and if, in fact, you do say something you regret in an Internet forum, you can always "edit" the post to your liking; however, this certainly does not add to your credibility. Unfortunately, in real life, there is not "edit" feature. So no.

:)

#9 lynx

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Posted 06 December 2004 - 02:10 AM

Thankfully, spiking someones drink with Phenibut would be pretty hard to do, it tastes too nasty and takes too much.

#10 zg00

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Posted 07 December 2004 - 06:13 AM

While Phenibut looks like an interesting anxiolytic and (socializing) 'mood brightener', it appears at higher doses to be used as more of an intoxicant, often as a GHB replacement (1,2,3).

Even at lower doses it seems to be more frequently compared to benzodiazepines then anything I've read about the nootropic profile.

There are also a few (and contradictory) reports about tolerance, which I'd tend to believe.

I haven't used it yet, but I will in the next week or so (mainly for anxiety, which seems to be getting the upper hand). From the sound of it Phenibut is not what I'd call a nootropic and with attention already being called to it from the party crowd, you might want to stock up on it (or stick with a more traditional benzo). Fortunately its sold quite cheaply at everyones favorite bulk nutritional supplement shop.

I'm new here. (:

#11 krieg

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Posted 07 December 2004 - 12:35 PM

I tried 0,3g for a couple of days. Didn't notice anything. Then stopped and tried 0.5g after that. Nothing either. I've got a presentation this friday and will try 1g and see if it finally relaxes me. (I'm taking small doses because I don't want to use it recreationally).

#12 dopamine

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Posted 07 December 2004 - 04:08 PM

Phenibut's effects are consciously noticeable only after a 1-2 g dose, in my opinion.

It works great for insomnia - especially in combination with Kava and Valerian. Although, for some reason it makes me feel really dizzy the next morning if I take more than 3 g the night before.

#13 hyoomen

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Posted 07 December 2004 - 04:59 PM

For what it is worth, given the history of GHB, I'd recommend a bit of caution when using related substances as sleep aids several nights in a row. Despite claims by the medical community, GHB can become extremely habit-forming and the withdrawal has been described by friends as worse than any other withdrawal there is.

A lot of us also found (when GHB was legal) that using it as a sleep aid gave us a thorough sleep period of about 4 hrs at which point we'd have to wake up and try again.

With Phenibut, Kava, and Valerian, it is no wonder you are waking up feeling dizzy, though! It's simply a wonder you are waking up! hahaha.

#14 lynx

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Posted 08 December 2004 - 08:28 PM

A lot of us also found (when GHB was legal) that using it as a sleep aid gave us a thorough sleep period of about 4 hrs at which point we'd have to wake up and try again.


There is no Dopamine rebound with Phenibut, like there is with GHB, however, at high doses I believe its respiratory depressing effects provide a net loss in sleep efficacy.

#15 zg00

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Posted 11 December 2004 - 07:55 AM

I'm on my second full day with Phenibut. Along with the *mild* but strangely...comprehensive anxiolytic effect I've noticed: persistent grogginess, fuzzy headedness, transient headaches (ibuprophin worked great and they are declining). When I go to sleep at night I actually feel like I am falling into sleep. I've never had trouble sleeping, but the speed at which I fall asleep on Phenibut is a little startling (my wife is noticing I also snore more, and further into the night then I usually do..all the way through the night).

My mood is better, but I wouldn't call it brighter. While I feel less anxious with the grogginess I definitely feel...well dumber. And that in itself can be kind of nice, its much harder to get worried about things.

I'll try changing up my dosage to see if the effects get better. Right now I'm taking about 1300 mg morning and maybe another 650 in the afternoon.

For me, the abuse potential for this is zero. Increasing my dose inappropriately would probably provide nothing more then a headache and increased drowsiness. Mixed with beer...same results. I have no doubt I'll sleep well tonight, but I'd probably do better treating transient anxiety with traditional benzodiazepines.

Btw, taste isn't so terrible. Its like mixing aspirin with a little salt and baking soda. I've tasted worse (*shudders*).

Edited by zg00, 11 December 2004 - 07:02 PM.


#16 jpars82

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Posted 14 December 2004 - 12:49 AM

I don't see much of any abuse potential with Phenibut. From my experience, I didn't notice much of any effect even taking 1-2 grams.

#17 nootropi

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Posted 14 December 2004 - 01:53 AM

I find phenibut to be excellent for social anxiety situations. 2 grams is effective.

#18 zg00

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Posted 19 December 2004 - 07:23 PM

I take it you didn't find the headaches problematic.

#19 gwiens

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Posted 26 December 2004 - 01:29 AM

Phenibut's effects are consciously noticeable only after a 1-2 g dose, in my opinion.

It works great for insomnia - especially in combination with Kava and Valerian. Although, for some reason it makes me feel really dizzy the next morning if I take more than 3 g the night before.


I tried it (phenibut) last night (2+ g) for the first time and woke up this morning after sleeping nearly 12 hours feeling extremely dizzy and some involuntary body motion (tardive dyskinesia?). I don't remember feeling this way using any drug previously. I hope it subsides tomorrow...

#20 zg00

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Posted 26 December 2004 - 07:36 AM

2+ grams seems to me like a rather high attack dose. I'd have recommended starting with maybe 650 mg. For me, I got headaches that took a few days to start to recede (at least to be manageable, they became more of a light but transitory symptom). After about a week I was up to using 1.2 grams in the morning and another 650 mg in the afternoon. For anxiety this was pretty effective, but I also had some apnea, dry mouth and eyes (I did drink lots of water which helped, but I ended up waking up to pee a lot) and those regular transient headaches (I also had some drowsiness, but only chronically at lower doses). Those symptoms were enough to bring me to a physician, who I explained my complaint (recently increased anxiety levels) and the problems with the supplement I was using. He of course recommended a more traditional approach (namely, Xanax).

I still am left scratching my head how Phenibut has become so intrenched in the smart drugs community, but I suppose anxiety itself could be considered detractor of optimal mental performance. However, in my experience Phenibut also induced some noticable 'brain fog'. I'd reverse words, or more often experience the dreaded on the tip of your tounge syndrom. But at higher doses of Phenibut, honestly, I didn't really care.

Anyone else have similar experience or did it simply not agree with me?

#21 lynx

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Posted 26 December 2004 - 08:19 PM

I too have noticed apnea, and I think that this represents one of the serious problems with phenibut. Because it crosses the blood brain barrier so easily and is totally non-specific for receptors, it depresses brain stem activity just as easily as cortical activity.

Phenibut will disappear eventually because of the horrible withdrawal and brain fog. Right now it is big because it is a legal "high", which will probably end when someone drinks too much and dies from it.

#22 lancelot

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Posted 26 December 2004 - 09:18 PM

Phenibut does nothing for me recreationally. It actually feels "dirty" if you know what i mean. It can never come close to be a GHB replacement as many use this approach to sell phenibut. Good ole' GHB where are tho?

#23 jpars82

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Posted 29 December 2004 - 12:48 PM

Phenibut does nothing for me recreationally. It actually feels "dirty" if you know what i mean. It can never come close to be a GHB replacement as many use this approach to sell phenibut. Good  ole' GHB where are tho?


I have social anxiety disorder and unfortunately never got the chance to try GHB... I almost thought about making it. And yeah, Phenibut is nowhere near being a replacement for GHB or Benzos. I actually prefer the Picamilon over Phenibut even though it's not all that strong.

#24 geigertube

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Posted 29 December 2004 - 03:10 PM

I actually prefer the Picamilon over Phenibut even though it's not all that strong.



Yeah, me too. At least at far as using it to get work done goes. I like decompressing with phenibut, though.

Steven

#25 stellar

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Posted 29 December 2004 - 06:50 PM

Well that sucks, I was going to order Picamilon but the reports I read weren't positive. Now I wish I would have....

#26 geigertube

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Posted 29 December 2004 - 08:23 PM

Well that sucks, I was going to order Picamilon but the reports I read weren't positive. Now I wish I would have....


The main side effect I saw reported was that some people can hit a "wall", where it makes them over-anxious after awhile if they don't watch the dosage. I'm assuming that cycling it, and watching dosage should avoid that.

I'm taking it every other day, currently. 50mg x 2/day. We'll see how that goes.

Steven

#27 stellar

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Posted 29 December 2004 - 11:17 PM

Geiger,
Have you taken doses above 50mg? I've seen old posts where some took as high as 150mg.

#28 zg00

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Posted 30 December 2004 - 04:19 AM

Phenibut does nothing for me recreationally. It actually feels "dirty" if you know what i mean. It can never come close to be a GHB replacement as many use this approach to sell phenibut. Good  ole' GHB where are tho?


GHB also interested me, but I missed the days when it was legal and never bothered trying one of the exothermic reaction kits. However, I think GHB like a lot of other 'legal highs' was under studied and over marketed. Here's one of my favorite erowid reports on a chronic GHB user:

http://www.erowid.or...xp.php?ID=10946

I did GHB for about four months two years ago and although I just missed killing myself with it, I did a pretty good job of screwing up my life.

Note: I'm not blaming the drug for what I did. My choices were my own. And some people appear to have no problem taking G on a sporadic basis. Many do, however -- many message boards show examples. A lot of the info I read about GHB back in '99 was pretty misleading, and in retrospect, obviously written by people using.

I've always been a pretty depressed type, with a few sporadic and short mildly manic periods; possibly bipolar with emphasis on depression.

In my teens/early 20s I became a pretty big pothead -- which doesn't help depression -- but I stopped cold, with zero problems, once I moved to the States. About three years ago, I wanted to get some pot again, but the places where I had once seen it sold on the street had been long shut down by the cops. So I asked around and was referred to a 'house dealer' by a friend, who brought me along. I buy some pot, and he gets an 'ecstasy'. Although I had heard of this, I didn't know much about it. I read up on it and decided to try it -- for personal/spiritual development more than any kind of high while clubbing (I don't do the nightlife thing).

So far, so good -- excellent even. Had some wonderful experiences and insights on E as did my girlfriend. Also experimented with LSD, again after much research, and more from a personal development interest than a desire for trippy visuals (which I got a minimum of). Again, a great learning experience. Then I started to fuck it up (well, taking either of those drugs with unresolved psychiatric issues wasn't too bright to begin with, but I wasn't that aware of them). I came into a chunk of cash and decided to lay in a large supply (50 pills) of E. After a rapid tolerance buildup, doing 3 E at a time would give me little more than a too much caffeine buzz. And I was doing more and more LSD trying to recapture the 'high', with less and less effect.

At this point, I had for a while been struggling with the realisation that my original intentions with this stuff had been replaced by thrill seeking. I stopped using (except for pot) -- not very difficult, as they weren't doing much for me any more. My girlfriend had also burned out a bit on E, though she never used it in the amounts I did.

Well, I guess all that E really screwed over my already probably screwed serotonin and other brain chemistry. Major depression, suicidal thoughts. Despite knowing my motives weren't so pure, I still wanted to get back to the strange spaces and feelings E and LSD had brought me initially. So I tried Ketamine around this time and had some weird, interesting experiences but with an overall very disconnected, gritty, depressing feel -- think Dark City or Pi. Overdid that for a few weeks and worsened the depression. Stopped doing it.

More and more, I withdrew from my girlfriend and other people, dreaded going to work each day. This depression went on for six months with no end in sight, and I decided that, turning thirty that year, I was going to be just as in debt, out of shape, etc. as I was when I turned twenty; and that if things didn't change I'd kill myself over New Years. Not a heat of the moment thing, just what seemed a cold and clear decision to end it if nothing changed.

At which point my girlfriend called one day, excited and giddy. She had read about this stuff that gave an E-like high, without tolerance buildup or serotonin dips, and had ordered a kit. She was totally excited by the results, which she was more than glad to share. I started looking for info on GHB on the web and it all seemed good -- the few exceptions were all at government 'info' sites, which due to my experience with marijuana, I tended to take with a pretty large grain of salt.

I took my first dose later that day, and OH MY GOD was it what I needed, or thought I did. For what seemed like the first time in my life, I actually *wanted* to live. I felt good about my options, I felt good about everything. Giddy, high, but not impaired. I decided that very first day that I *never* wanted to be without it again. I truly felt it had saved me, since I had been serious about committing suicide come year's end if nothing changed.

So I ordered a big supply. Used on a daily basis, and ramped up to 24/7 dosing pretty rapidly -- taking a dose every two hours or so. There were a number of positive effects initially, in terms of overcoming anxiety and depression, abreacting out some long standing personal issues, and on creativity and productivity. But over time, I became totally manic -- I was having more ideas than I could keep track of (and everybody who would stand still was going to hear all about them at 200 words per minute); quit work because I was going to be a genius mastermind artist who, while getting rich off brilliant inventions, would save the world in his spare time; became very irritable and intolerant with anybody who couldn't keep up with me. My girlfriend never had these issues with G. She did, however, have issues with how I was acting -- but much more seriously, with her mother's breast cancer having returned with a vengeance. What did I care, I was happy.

I pretty much withdrew from or pissed off her and the few good friends I had. Wrote scathing, rambling emails to my parents about what I perceived as their wrongs, then got defensive and angry when they asked what was going on with me, why I was acting and sounding so different.

I started acting in pretty disturbing ways. I was writing lots of poetry which I thought clever and performing it at local poetry slams -- not that bad; but I insisted on reciting it to passing strangers, people who live in my apartment building, etc. Got pissed off at everybody in a huge traffic jam in the city leaning on their horns -- not unreasonable in itself, since horns don't help that situation; but decided to yell 'STOP FUCKING HONKING YOU IDIOTS' at them and almost got the crap beat out of me by a driver who didn't take that advice too kindly. Felt much more confident approaching women, not a bad thing; but ended having unprotected sex with a few whom I, in retrospect, should have had serious concerns about.

That was pretty mild, though, compared to waking up on the pavement to find EMS workers and police staring at me. I told them I had drunk too much and passed out, was charming about it, and they brought me home. Didn't seem like a big deal.

BTW, I never dosed to get to sleep, only to get high. I would sleep when I could no longer stay up/get high, maybe a few hours a day.

Next time, I was stumbling home from the poetry reading, woke up with EMS workers and police around, bleeding from my face. No charm this time, I angrily insisted they let me walk the few blocks home. No dice -- handcuffed to the stretcher in the ambulance; they were convinced I was on crystal meth. I kept saying I wasn't, but I wasn't very pleasant and I refused to say what I had been using. I left the hospital as soon as I could walk and sign the disclaimer forms.

Well, at this point I realized things weren't too good. I thought of this as a pretty mild 'not too good'. But I started looking for more info on GHB and read some posts on usenet about dopamine rebound and other withdrawal symptoms. I decided to lay off it for a while, after finishing my current stash. So I did. Had a few pretty bad days, but that seemed to be it. This is after approximately two months of use, with the last few weeks on the every two hour diet. Overall mood was fine after withdrawal, I felt reasonably good with periods of manic happiness.

I ordered more GBL after a month off. Didn't have the money for proper NaOH, so when the GBL came two weeks later I opted for Red Devil Lye.

The period that followed is still pretty much a blur to me.

I do remember one incident: being woken up in my building's elevator by the cops. Again, I insisted they let me go back to my apartment; they insisted I don't. I particularly recall asking aggressively and haughtily whether they were arresting me, and saying that if they weren't, they ought to let me go. Here's a little tip: don't call the cop who is handcuffing you 'bitch'. Same deal as before -- emergency room, and as soon as I could get the disclaimer forms, I signed myself out and headed back home for my fix.

After that, I remember my apartment in fits and spurts, in a nightmarish state. Kept dosing up but had no effects, would feel tremendously agitated, then suddenly fall asleep. Wake up suddenly in a confused panic. Do more G. Going to the side of my apartment where my bed is, but it's confusing, my bed's not there, there's a table -- oh, wrong end of the apartment. Spin, knock stuff over, fall, repeat. Somewhere in there my lights were cut for non payment. Somewhere in there I drank something like half a liter of GBL, straight. Somewhere in there I decided to do laundry in the bathtub -- dumped all my clothes and some detergent in, and started the tap.

That's how they found me: the downstairs neighbors complaining about a leak. EMS thought I was dead when they saw me. I had been comatose for three days and was lying in a few inches of water. Kept me in the ICU for a week and a half or so, very touch and go with heartrate and blood pressure, massive dehydration, massive kidney problems, major muscle breakdown in my legs, all sorts of fun. I slipped in and out of consciousness; they had me on massive doses of Ativan and I was having extremely scary, hallucinatory nightmares. They transferred me to the psych ward, where I ended up for four weeks. I was in a wheelchair because of muscle loss, and the first few weeks are a drugged haze. The doctor there later told me I held forth at length about GHB and displayed aggressive and narcissistic tendencies early in my stay, so I guess the G or its effects was still in my system at the time.

They got me off Ativan and on Klonopin, and weaned me off Klonopin during the last week. I could walk again, if a bit wobbly. Welcome to the shape of your new, freshly fucked up life. My girlfriend visited a few times and was, and has been, very supportive. Welcome to the new life you were too busy selfishly screwing up while your girlfriend -- your amazing girlfriend's -- mom died. No health insurance either, so hello astronomical hospital bill.

Yep, I started feeling quite a bit of anxiety about going out into the world again -- being in a psych ward on heavy meds is a pretty low pressure lifestyle. Talked about it a bit with the docs, they thought I'd do fine.

Well, I haven't done GHB for two years now. Unfortunately, what I'm doing instead is drinking heavily. Never had much taste for alcohol before, but I appear to have been cross trained by the G addiction. Life is fucked, and I've been thinking about doing G again, even though I'm pretty sure that this time, it'll kill me.

Results so far:

~130K hospital bill.

Outstanding IRS debt and other debts, don't know the total, don't want to.

Teeth in horrible shape, some literally rotting away, due to heavy drinking and smoking and neglecting my health generally, possibly also due to heavy G use.

Loss of trust of family and friends.

Shame, guilt and fear over all the wrongs I've done and all the people who saw me do it.


Smart drugs, and mood elevating chemicals in general walk a tightrope that seems too often over looked in the initial excitement.

Personally (as I'm sure I've mentioned) because of the apnea and transient headaches, my medical cabinet now contains a more traditional benzodiazepine for those occasions I might find centering myself to be a problem. My doctor was quite comfortable with this (much more so then knowing that I'd self-medicate with a chemical that he'd never even heard of!).

Don't get me totally wrong, I think Phenibut is a useful chemical. But I would recommend very moderate use. I would not consider it a safe addition to any regular stack, or I might end up reading your own reports on the not so well understood long term effects of chronic Phenibut abuse (the medically tested doses I've seen appears to be 250 mg, well below the popular 'effective' doseages). Of course, as always YMMV.

#29 zg00

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Posted 30 December 2004 - 04:51 AM

I should add to my above post, regarding the tightrope: more with the latter.

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#30 geigertube

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Posted 30 December 2004 - 01:26 PM

Geiger,
Have you taken doses above 50mg? I've seen old posts where some took as high as 150mg.


Truth be told, im estimating the 50mg figure. I dont have a scale that goes down that low, and I havent messed with any alternative methods of measuring dosages. I just stick the end of my finger in the bottle and lick what sticks to the end of it. That dose gives me a calm, but stimulating dose. If I get a heavy coverage, it can be too stimulating. But, I tend to be sensitive to stimulants.

Eventually, im going to get around to actually measuring the dose. :)

Steven




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