Phenibut

Discussion in 'Alternative Treatments and Research' started by Danny Boy, Dec 29, 2015.

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    1. Danny Boy
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      Phenibut (or, alternatively, fenibut, phenybut) (brand name Noofen, Citrocard), contracted from β-phenyl-γ-aminobutyric acid (β-phenyl-GABA), is a central depressant and derivative of the naturally occurring inhibitory neurotransmitter γ-aminobutyric acid (GABA). The addition of aphenyl ring allows phenibut to cross the blood–brain barrier.[1] Phenibut was developed in the Soviet Union in the 1960s, and has since been used there as a pharmaceutical drug to treat a wide range of ailments, including posttraumatic stress disorder, anxiety, depression, asthenia, insomnia,alcoholism, stuttering, and vestibular disorders, among other conditions.[1][4][5] In the rest of the world, phenibut is not approved for clinical use, and is instead sold as a nutritional supplement.[6] It has been reported by some researchers to possess nootropic actions for its ability to improve neurological functions,[4][medical citation needed] but others have not observed these effects.[7] It is generally accepted that phenibut has anxiolyticeffects in both animal models and in humans.[1]

      Phenibut is a close structural analogue of GABA, as well as of baclofen (β-(4-chlorophenyl)-GABA), pregabalin (β-isobutyl-GABA), and GABOB (β-hydroxy-GABA).[8] Originally thought to act as a selective GABAB receptor agonist, phenibut has since been found to act preferentially as a blocker of α2δ subunit-containing voltage-gated calcium channels, similarly to gabapentin and pregabalin.[9] As such, phenibut is a gabapentinoid.[10][


      Anyone tried this?
       
    2. Danny Boy
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      "Phenibut: The Soviet smart drug

      1963, St.Petersburg, Russia –
      A Soviet Union lab scientist by the name of Perekalin synthesizes 3-phenyl-4-aminobutyric acid, an experimental drug intended to calm psychiatric children.

      1964 – Professor Khaunma labels the drug Phenigamma and reports the first findings of its tranquilizing effects in the Byulleten Eksperimental’noi Biologii i Meditsiny.

      1975 – Phenigamma has spread from clinical practice to public use under the name of Phenibut. The Soviet Ministry mandates its use for astronauts in space flights due to the drug’s revolutionary psychologically calming yet cognitively stimulating effects.

      2001 – Over 300 scientific publications have studied Phenibut’s nootropic and pharmacological properties.

      2014 – Phenibut is used all over the globe as a smart drug, mood enhancer, sleep aid and recovery booster.


      Phenibut is a derivative of GABA (gamma-aminobutyric acid). GABA is the primary neurotransmitter in your body that regulates the neuronal excitability of the central nervous system. Basically, GABA makes sure that your brain does not become hyperactive.

      Why not just supplement with GABA directly then? Phenibut crosses the blood-brain barrier more effectively than GABA itself in supplement form. GABA is naturally produced in the brain itself, therefore it normally does not need to cross the blood-brain barrier to be effective [1].

      In humans, Phenibut supplementation has 2 main effects [2, 3, 4].

      1. It is a nootropic (smart drug). Phenibut primarily increases motivation, attention and concentration with a weaker effect on memory and little effect on overall intelligence.
      2. It is a strong anxiolytic (anxiety killer). Phenibut is used to treat panic attacks, stuttering, Parkinson’s disease, neuroses, vestibular (balance) disorders, spasticity, epilepsy, hyperactivity, insomnia and post-traumatic stress disorder. Pick-up artists use Phenibut to shake the nerves of cold-approaching beautiful women.
      Both are the result of Phenibut’s effect on the activity of your nervous system.

      In addition, Phenibut has mood enhancing effects. It has thymoleptic (anti-depressant) properties and can reduce irritability and fatigue. It is clinically used to treat asthenic-depressive syndrome. [2]

      These psychoactive effects are similar in mechanism to alcohol but without the depressant effects. In the upper/downer classification of drugs, alcohol is a downer, but Phenibut is neither. Phenibut gives you focus and calmth without the jitters of caffeine or the cloudiness of alcohol.

      Phenibut’s effects can easily last the rest of the day, even though Phenibut’s plasma half-life is only 5.3 hours [2]. This is because Phenibut’s action on the GABA receptors can linger long after your kidneys have excreted all the Phenibut [16, 17]."
       
    3. Markku
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      Markku Director Staff Benefactor Hall of Fame Team Trobalt Team Tech Team Awareness Team Research

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      I have. Phenibut did nothing for me. Well maybe relaxed a little, but that's it.

      It's worthwhile to remember that Phenibut builds up tolerance quite quickly. If you google for "phenibut tolerance" or "phenibut withdrawal", you'll find plenty of hits.
       
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    4. Danny Boy
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      That's a big shame. So is it worse than GABA drugs?
       
    5. Markku
      Inspired

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      • Helpful Helpful x 1
    6. Danny Boy
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      Hm, best not to play around with this drug it seems. Thanks for the information Markku.
       
      • Agree Agree x 1
    7. Dutchy
      Not worthy

      Dutchy Member Benefactor

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      It's like anything can cause tinnitus while on it,that withdrawal story is pretty severe though.
      One of the reasons i like to stick to low dosage and unregular usage,those short period symptoms
      are very rare though and as i explained numerous times to psychologists and psychiatrists.
      " Your treatment seems plausible and effective BUT not everyone reacts the same way to meds ".
      I prefer not to be an exception to the rule,they hold on to the rule without exception.

      " We're puzzled " i like to look at the big picture first.
       
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    8. Danny Boy
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      Just got some today and it does work! Well, works for me anyway! I combined it with trobalt and it worked like a treat! I'll try this combo for a few weeks see if it lowers it even further.
       
    9. Danny Boy
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      [Comparative evaluation of the neuroprotective activity of phenibut and piracetam under experimental cerebral ischemia conditions in rats].
      [Article in Russian]
      Tiurenkov IN, Bagmetov MN, Epishina VV, Borodkina LE, Voronkov AV.
      Abstract
      The neuroprotective properties of phenibut and piracetam were studied in rats with cerebral ischemia caused by bilateral irreversible simultaneous occlusion of carotid arteries and gravitational overload in craniocaudal vector. In addition, the effects of both drugs on microcirculation in brain cortex under ischemic injury conditions were studied. Phenibut and (to a lower extent) piracetam reduced a neuralgic deficiency, amnesia, and the degree of cerebral circulation drop, and improved the spontaneous movement and research activity deteriorated by brain ischemia.



      The neuroprotective effects of R-phenibut after focal cerebral ischemia.
      Vavers E1, Zvejniece L2, Svalbe B2, Volska K3, Makarova E2, Liepinsh E2, Rizhanova K4, Liepins V4, Dambrova M3.
      Author information

      Abstract
      R-phenibut is a γ-aminobutyric acid (GABA)-B receptor and α2-δ subunit of the voltage-dependent calcium channel (VDCC) ligand. The aim of the present study was to test the effects of R-phenibut on the motor, sensory and tactile functions and histological outcomes in rats following transient middle cerebral artery occlusion (MCAO). In this study, MCAO was induced by filament insertion (f-MCAO) or endothelin-1 (ET1) microinjection (ET1-MCAO) in male Wistar or CD rats, respectively. R-phenibut was administrated at doses of 10 and 50mg/kg for 14 days in the f-MCAO or 7 days in the ET1-MCAO. The vibrissae-evoked forelimb-placing and limb-placing tests were used to assess sensorimotor, tactile and proprioceptive function. Quantitative reverse transcriptase-PCR was used to detect brain-derived neurotrophic factor (BDNF) and vascular endothelial growth factor (VEGF) gene expression in the damaged brain hemisphere. Both f-MCAO and ET1-MCAO resulted in statistically significant impairment of sensorimotor function and brain infarction. R-phenibut at a dose of 10mg/kg significantly improved histological outcome at day 7 in the ET1-MCAO. R-phenibut treatment at a dose of 50mg/kg significantly alleviated reduction of brain volume in damaged hemisphere in both f-MCAO and ET1-MCAO. In R-phenibut treated animals a trend of recovery of tactile and proprioceptive stimulation in the vibrissae-evoked forelimb-placing test was observed. After R-phenibut treatment at a dose of 50mg/kg statistically significant increase of BDNF and VEGF gene expression was found in damaged brain hemisphere. Taken together, obtained results provide evidence for the neuroprotective activity of R-phenibut in experimental models of stroke. These effects might be related to the modulatory effects of the drug on the GABA-B receptor and α2-δ subunit of VDCC.
       
    10. PatrickG

      PatrickG Member Benefactor

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      @Danny Boy could you please specify the dosages you used?
       
    11. Bertman
      No Mood

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      @Danny Boy are you sure its not the trobalt that lowered your T and not the phenibut?
       
    12. Danny Boy
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      Sadly not. Trobalt doesn't work as well anymore. Phenibut works on GABA and dopamine, which are already two useful tools which work for tinnitus.
       
    13. Danny Boy
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      500mgx3 is what they recommend. But I take 500-1000 personally.
       
    14. linearb
      Psychedelic

      linearb Member Hall of Fame

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      this stuff basically functions as a weak, less predictable benzo. It's a positive allosteric modulator of GABAb, and has some GABAa action as well as I recall.

      The withdrawals from phenibut are horrific; fairly similar to withdrawing from one of the fast-acting benzos (Xanax).

      There's literally no reason to take this stuff. It's a less effective, more dangerous benzo. If you want to take benzos, take one of the long-acting ones, instead.

      Over the years I have read numerous and reliable reports of people developing chronic tinnitus as a direct result of phenibut use.
       
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    15. Aussie Lea
      Dramaqueen

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      @Danny Boy what are you thinking taking this? stop before you hurt yourself!
       
    16. Danny Boy
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      Danny Boy Member Benefactor Hall of Fame

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      It's not classed as a benzo-It's classed as a gabapentinoid


      "Gabapentinoids are 3-substituted derivatives of the neurotransmitter γ-aminobutyric acid (GABA) which block α2δ subunit-containing voltage-dependent calcium channels (VDCCs).[1][2]Clinically-used gabapentinoids include gabapentin (Neurontin) and pregabalin (Lyrica),[1][2] as well as a gabapentin prodrug, gabapentin enacarbil (Horizant).[3] Another analogue mirogabalin is in clinical trials but has not yet been approved.[4] Other compounds from this family used in research but not developed for medical use include atagabalin, 4-methylpregabalin and PD-217,014. Gabapentinoids are used clinically in the treatment of conditions including epilepsy, neuropathic pain, fibromyalgia, anxiety, and restless legs syndrome, among others.[1][3][5]

      Recently, phenibut (β-phenyl-GABA), a close analogue of pregabalin (β-isobutyl-GABA), has been found to similarly bind to and block α2δ-containing VDCCs, notably with an affinity exceeding that of its other actions, effectively making it a gabapentinoid.[6] Baclofen (β-(4-chlorophenyl)-GABA) has also been found to do this, but relatively weakly.[6]"


      Nothing to do with a benzo, also, I take low doses not high doses.
       
    17. linearb
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      linearb Member Hall of Fame

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      I didn't say it was a benzo, I said that it was functionally equivalent, causes dependence in the same way that benzos do, and has essentially the same withdrawal effects including tinnitus.

      1-2 grams a day isn't a staggering dose, but you're definitely playing with fire, whether or not you want to believe that.

      http://www.tandfonline.com/doi/abs/10.3109/14659891.2012.668261?journalCode=ijsu20#.VoqiSZMrJE4
      https://www.google.com/webhp?sourceid=chrome-instant&ion=1&espv=2&ie=UTF-8#q=phenibut tinnitus
      http://www.longecity.org/forum/topic/58327-phenibut-withdrawal-after-only-a-handful-of-uses/

      etc, etc, etc. This stuff is dangerous. It comes up over and over on benzo boards; people have absolutely developed tinnitus and had seizures as a result of phenibut use and withdrawal.

      If you want some anecdotes of people developing chronic tinnitus after using what you're calling "low doses", I can certainly point you towards some.

      Be careful with this stuff, Danny. I'm not trying to be a jerk, I just don't want you to get hurt.
       
    18. Danny Boy
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      Danny Boy Member Benefactor Hall of Fame

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      I understand your concern. I'm only gonna take it for two weeks. Thanks for caring.
       
    19. undecided
      Fine

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      I fully agree with @linearb
      Phenibut works for me as well but it'is probably worse than benzos when it comes to tolerance building (not addiction). Way less potent though.
      If you take it for 4-5 days continuously, take a break for a couple of days at least.

      My usual dosage is 750mg-1g once a day. But I've only used it 5-6 times in the past 6 months.
       
    20. pebbles

      pebbles Member

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      I thought keppra had helped you how bad is your tinnitus know
       
    21. Danny Boy
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      Danny Boy Member Benefactor Hall of Fame

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      Keppra doesn't work for tinnitus? My tinnitus is fine.
       
    22. linearb
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      linearb Member Hall of Fame

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      then why are you taking phenibut?
       
    23. Danny Boy
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      Danny Boy Member Benefactor Hall of Fame

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      Because, someone combined Neurontin with trobalt and was practically cured. So thought I'd experiment.
       
    24. Aussie Lea
      Dramaqueen

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      @Danny Boy: why can't you tell us clearly how your tinnitus and hyperacusis are when you are not taking any drugs or supplements?
       
    25. Danny Boy
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      Danny Boy Member Benefactor Hall of Fame

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      I don't have hyperacusis anymore and tinnitus is a 2-3
       
    26. linearb
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      linearb Member Hall of Fame

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      gotcha. Well, do be careful mixing all these gabaergics. And also note, phenibut is not equivalent to Neurontin. Yes, they are both technically gabapentinoids, but the mechanisms are not the same (despite some overlap).
       
    27. Danny Boy
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      Danny Boy Member Benefactor Hall of Fame

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      I understand. Maybe I'll attempt to get neurontin from the Doctor. Say it's for social anxiety.
       
    28. linearb
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      linearb Member Hall of Fame

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      at least in the US, it's trivially easy to get a prescription for it; again, be careful, there are a number of reports of people having long-term worsening as a result of fairly short-term neurontin use; I'm sure you have read the same threads here as I have.

      I have a giant bottle of neurontin at home; not really planning on doing anything with it. In fact, I took Neurontin for several months prior to my worsening in 2011, and I have long wondered if it might have been a factor.
       
    29. Danny Boy
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      Danny Boy Member Benefactor Hall of Fame

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      Well, seems like I'd be better off just stopping them all. At least I've managed to get from a 10 to a 2-3 at it's worse.
       
    30. linearb
      Psychedelic

      linearb Member Hall of Fame

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      out of curiousity, what does "2-3" mean to you? Are you only able to hear it in very quiet environments, or are you able to hear it lightly any time you listen for it?
       

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