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Phenibut and its danger

phenibut dangerous overdose

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#1 Tom_

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Posted 06 November 2013 - 12:41 AM

A lot of people have had a spin with Phenibut on here. A fair few have had to deal with sometimes very dramatic and severe withdrawal - in equivelence to that of Benzo withdrawal, although it would appear while the withdrawal can be more severe it tends not to have chronic sequelae.

Before I continue I want to make it clear I'm not against the use of it but would like people to be aware of its inherent dangers. I won't focus on its additive qualities - a thread on M&M deals with that much better than I ever could hope to. But this drug has the potential to be lethal.

It acts as a GABA-b agonist and at higher dosages it is also a significant GABA-A agonist and has some BDZ receptor affinity. It antagonizes PEA and increases dopamine activity (attenuated by halopradol). Its effects are anxiolytic, hypnotic and euphoric in nature. At higher doses it lowers temperature and in clear overdosage seems to eventually cause an acute disorder indisernable from Serotoninergicly induced akinthesia - with the same risks to kidneys.

I've twice used the substance as part of a poly-overdose to kill myself (clearly didn't work) but it seems to have been at least as dangerous as the 360mg of Tranylcypromine I took along side it (among other things).

It also doesn't seem to cause nausea or emesis.

With ultra high dosages symptoms are as follows (at least in me):
Acute onset and severe agitated delirium - it took 8 security guards to hold me down on one occation
Coma onset seems to be around the same time as delirium with reduced response to pain being the first sign - obviously of most importance is maintaining airway as this would be an immediate cause of death

Providing the airway is protected it seems death would likley be from a combination of execessive movement and hypothermia causing severe rhabdomyolysis and eventually acute renal injury leading to arrhythmia and cardiac death. If airway protection isn't maintained its possible the drug could kill you within a few hours although I suspect a massive dose would be required. As the worsening coma sets in by 8-24th hour failure to protect the airway would be a more realisitic problem. The agitation and the hypothermia are what's more likely to kill you - within a day I imagine.

So what's the treatment for Phenibut toxidrome?
Seems to be best to just throw bucket loads of halopardol (will antagonize some of the effects and reduce agitation) at it until the agitation disapates and if absoutely nesseary use a paralytic (of course induce a coma and protect the air way) in conjunction if the halparadol isn't working. Monitioring and if urine output falls below 0.5mg/hr for six hours and/or there is a rise in Serum creatine (GRF) increases or is suspected to increase 50% then fluids should be administered ASAP. If its a severe cause or true acute renal failure then jump the guns and use renal replacement therapy as well.

I can't see much use in using Flumazenil in conjunction with Haloparadol although it could be attempted (BDZ is a very small part of its MOA, although it would potentiate its GABA-A agonism so may be of use) - more as a last resort in persistant coma or some such. None of the GABA-B antagonists are even remotely ready for clinical use so they can't be used. Paradoxyically low dose stimulant therapy could be used but while this might improve hypothermia and hypotension it could worsen agitation (it could also improve it). If it was tried very low doses would have to be used at first to assertain safety. Other theoretical ideas could be gluatemate agonists or mimentics but I can't think of any potent enough and again should be regulated to last line in persistant coma.

I would imagine an LD50 in humans would be about 1-2g/kg (Rats and Rabbits have an LD50 of 900 and 700 mg/kg). In a 70 kg healthy man I theorize as little as 70 grams could be leathal. Significantly less than the average meal.

Do bare in mind everything I wrote might be a load of shit. Both experiences where poly drug overdoses but no other drugs seemed likely to cause that paticular set of symptoms and while the research is sparse the above is consistent with it.

So there ya have it...my take on Phenibut toxicity and its management.
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#2 NZT-49

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Posted 06 November 2013 - 01:46 AM

Now why would you go and try to kill yourself with a poly-overdose with phenibut?

Anyways when I try Phenibut in the future I will follow these rules as gathered from online research.
1. Keep dosing limited to 2 times/week max.
2. Do not dose 2 consecutive days.
3. Keep within recommended dosing guidelines.
4. Do not mix with alcohol.
5. Do not re-dose within 4 hours of the same day.
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#3 focus83

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Posted 06 November 2013 - 01:25 PM

Tom, did I understand it correctly that you tried to commit suicide again very recently by using Phenibut + Tranylcypromine + other drugs? Good god, I thought you had improved so much since you've been on Tranylcypromine? What happened? Did its effects dissipate?

With regards to Phenibut I would say that the Tranylcypromine as well as the other drugs you took potentiated the effects of the Phenibut overdose enormously (whatever amount of grams is actually considered an overdose). Taken in isolation I believe one has to swallow absolutely massive amounts of Phenibut in order to get into a life threatening situation. I remember people regularly taking 30+ grams daily without serious issues except for pronounced withdrawals.
In general I'd say that a poly drug overdose doesn't lend itself to judge the dangers of an overdose of each single drug.

#4 Breezey

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Posted 06 November 2013 - 03:34 PM

Tom I am not going to ask you not commit suicide, but I will ask you to come to this 3rd world country and run a tea shop in the rural area for a couple of months before trying again. Maybe run a school, and teach the local kids a thing or two.
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#5 Tom_

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Posted 06 November 2013 - 03:59 PM

NZT I think those are very good guidelines. Although I don't think rule 2 is nessary and dosing shouldn't be more than 3-4 times a week (although there are a lot of people that make the arguement for up to 5 days a week). I also think there should be a week break after every second week, more to stave off tolerance than anything else. But as I said before it the guidelines you mentioned are the safest most conservertive.

focus, not sure how you managed to peice it together but yes I did, on the first I think. Tranylcypromine, Phenibut, Clonazepam and Modafinil. My current working hypothesis is tachyphylaxis. Either way its a full relapse.

Breezey - there is something wrong with my brain and the way it communicates with the rest of my body, I truely don't believe going to africa or the far east is going to give me a drastically different perspective on life. Depression has a roughly equal prevalence across the world although it does sometimes have a very different presentation - even in the same culture (male vs female depression, child vs adult depression, adolecent vs child or adult etc)...The only finacial protective factor seems to be how well off you are compared to the rest of the country.

#6 focus83

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Posted 06 November 2013 - 04:50 PM

focus, not sure how you managed to peice it together but yes I did, on the first I think. Tranylcypromine, Phenibut, Clonazepam and Modafinil. My current working hypothesis is tachyphylaxis. Either way its a full relapse.

Tom, how very sad to hear that :( I thought you were finally on a good way with a MAOI. Increasing the dosage didn't help? At which dosage have you been at the end?

If you have access to Nardil that might be another option although at the end of the day it's also a MAOI similar to Tranylcypromine and tachyphylaxis is thus to be expected, too. However, its GABA raising properties might do you well in case anxiety is also part of your condition.
Damn, I never heard Tranylcypromine stop working that quickly before. Maybe you grew tolerant to its NA and DA releasing properties. That wouldn't be so surprising as stimulants in general are known to rapidly produce tolerance and Tranylcypromine is a substituted ampethamine.
Then again, it's not unheard of that MAOI users occasionally have a couple of bad days for no apparent reason before the effects kick back in. How long have you had the relapse before you took the overdose?

What are you currently on now? What are your docs suggesting for the future in terms of pharmacological treatment?

Are you actually participating in the second NSI-189 group buy? Maybe that would be something for you in case you can afford it.

#7 Tom_

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Posted 06 November 2013 - 05:15 PM

Now the MAOI kicked it its out of research land so I'm not sure. I have an appointment on Friday. The actual onset of dsyphoria was very fast over just a few hours but it seems that there may have been signs (very significant ones - worsening sleep, up to two weeks beforehand of flagging response.

I was actually 'only' on 40mg and while I could go higher ( the research on tacki in ADs while small all point towards only short term benefits before eventual poop out). Alongside Modafinil 400mg and chronic benzo use.

I never tried a TCA as it didn't seem indicated for my symptoms but maybe its time to change that and try one. Maybe a combination of Moclobremide and Amitriptyline, Nortriptyline or Lofepramine.

Other options include Lithium or T3 agumentation and they in combo with TCAs are the gold standard. The quality of my depressive symptoms seem to have changed as well with sudden severe worsening of hypersomnia (could just be the AKI) and a subjectively diffferent dsyphoria. The poor response to Benzos and impusivity could point towards a more bi-polar spectrum disorder (there are certainly features of borderline PD) and so one could make the argument for a mood stabilizer. I've tried Quetiapine, Aripiprazole & Lamotragine but a trial of Amisulpride, Valporate or Lithium could prove useful.

A combintion could end up looking like Moclobremide, Amitrptyline and Lithium. Or even at total treatment resistance an obcene combination of Moclobremide, Ami, Lithium, T3, Amisulpride, Amphetamine & Rulizol. I've alwasys wanted to find someone on a combination similar to that, it seems so facinating....completely rediculous, with a tolerence profile from hell and risks barely outweighing the benefit...but still faciniating.

I'm being refered to the regional teriatry sleep center and I'm seeing my psychiatrist on friday whom I suspect will recommend re-starting Tranylcypromine and titrating to 60-90mg. I will ask for a referal to the teriarty affective disorders clinic however and be entirely frank about my suspion that re-starting Tranylcypromine will be of little use in the long run.

Glutemaergic drugs are options.

#8 focus83

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Posted 06 November 2013 - 05:46 PM

If your doc wants to reintroduce the Tranylcypromine I would definitely do it. Don't give up on it until you've been at 90mg for several weeks.
I forgot to mention Amisulpride in my earlier post. Good that you did as it has shown to be a potent antidepressant and anxiolytic even in monotherapy. I'm not sure though whether this was with low dosages or higher ones, but I believe it was with low dosages. It also hits the GHB receptor which could fill in the activating/stimulating part that you seem to need in every drug regime.

I'm curious how you are going to respond to TCAs. Most likely you will have to manage some serious sedation. But what is truly worrying about TCAs is their very high toxicity and morbidity in overdose. With your history of multiple suicide attempts I would be deeply concerned to see them in your hands. Would your doc be willing to give them a shot?

#9 Tom_

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Posted 06 November 2013 - 09:04 PM

MAOI's and in particular Tranylcypromine are at least as dangerous, there are case reports of up to 200mg being used for treatment refactory MDD and there are also treatment reports of monooverdose fatalities with Tranylcypromine at 200mg - it looks like I'm a slow metabolizer because I clearly should be dead. On the other hand at the moment I have one days worth in my hand so I don't forsee that being a big problem.

So maybe raising the dose to between 60-90mg but the sudden onset tacki...well that could be more dangerous than remaining off ADs. I have to say the Moclobremide and Amitryptyline combo is currently more persuasive to me.

Wait a week for the MAO to be replaced then start:
week 1 150mg Moc and 100mg Ami
week 2 300mg Moc and 100mg Ami
week 3 300mg Moc and 150mg Ami
week 4 600mg Moc and 150mg Ami

wait 6 weeks and then add in Amisulpride, Amphetamine/Methylphenidate/Bupropion or other ideas if significant improvement isn't seen. I may decide to continue you the Modafinil from week 1, that is assuming arse face agrees...which is a stretch.

Edited by Tom_, 06 November 2013 - 09:05 PM.

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#10 Introspecta

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Posted 06 November 2013 - 11:04 PM

I honestly feel like using phenibut at 1 dose 1 to 2 times a week is pointless. The true effects don't shine unless spreading your doses out ex. 400mgs 4 times a day for 2-3 days then washing out for 4 days due to the gaba b agonizing, PEA antagonizing then agonizing effect,lol. So usually the first day for me I feel somewhat tired but by the second day the dopamine effects start building up giving more of a speedy relaxed feeling. But if you are getting good effects from 1 dose per day then I wouldn't change a thing. Also dosing 3 days and getting semi euphoric effects can make it hard to stop dosing which is where you need discipline and a good remembrance of the ugly phenibut withdrawal.

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