• Log in with Facebook Log in with Twitter Log In with Google      Sign In    
  • Create Account
  LongeCity
              Advocacy & Research for Unlimited Lifespans

Photo
* * * * * 1 votes

NEFIRACETAM - Another reason to avoid prolonged usage

nefiracetam racetams racetam memory piracetam cognitive cognition aniracetam oxiracetam pramiracetam

  • Please log in to reply
17 replies to this topic

#1 ScienceGuy

  • Life Member
  • 851 posts
  • 1,129
  • Location:UK

Posted 21 February 2012 - 09:01 AM


Aside from the possible TESTICULAR TOXICITY concerns, there is in fact another reason to avoid prolonged usage of NEFIRACETAM for the medium to long-term, namely the fact that NEFIRACETAM is a GABA RECEPTOR AGONIST, which is that unique amongst the existing RACETAMS, and hence prolonged usage will to an extent induce down-regulation of the GABA RECEPTORS. Consequently usage should be restricted to short-term use only or CYCLING ON/OFF :)

See the following:

Brain Res Brain Res Rev. 1994 May;19(2):180-222.

Piracetam and other structurally related nootropics.

Gouliaev AH, Senning A.

Source
Department of Chemistry, Aarhus University, Denmark.
Abstract

Nearly three decades have now passed since the discovery of the piracetam-like nootropics, compounds which exhibit cognition-enhancing properties, but for which no commonly accepted mechanism of action has been established. This review covers clinical, pharmacokinetic, biochemical and behavioural results presented in the literature from 1965 through 1992 (407 references) of piracetam, oxiracetam, pramiracetam, etiracetam, nefiracetam, aniracetam and rolziracetam and their structural analogues. The piracetam-like nootropics are capable of achieving reversal of amnesia induced by, e.g., scopolamine, electroconvulsive shock and hypoxia. Protection against barbiturate intoxication is observed and some benefit in clinical studies with patients suffering from mild to moderate degrees of dementia has been demonstrated. No affinity for the alpha 1-, alpha 2-, beta-, muscarinic, 5-hydroxytryptamine-, dopamine, adenosine-A1-, mu-opiate, gamma-aminobutyric acid (GABA) (except for nefiracetam (GABAA)), benzodiazepine and glutamate receptors has been found. The racetams possess a very low toxicity and lack serious side effects. Increased turnover of different neurotransmitters has been observed as well as other biochemical findings, e.g., inhibition of enzymes such as prolylendopeptidase. So far, no generally accepted mechanism of action has, however, emerged. We believe that the effect of the racetams is due to a potentiation of already present neurotransmission and that much evidence points in the direction of a modulated ion flux by, e.g., potentiated calcium influx through non-L-type voltage-dependent calcium channels, potentiated sodium influx through alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor gated channels or voltage-dependent channels or decreases in potassium efflux. Effects on carrier mediated ion transport are also possible.

PMID: 8061686
  • Informative x 2
  • dislike x 2
  • Ill informed x 1
  • like x 1

#2 karma02

  • Guest
  • 35 posts
  • 4
  • Location:Canada

Posted 13 April 2012 - 03:40 PM

Pirtacetam will kill my testicles? But I love them... AND I love piracetam. What to choose - what to choose ?

Edited by karma02, 13 April 2012 - 03:51 PM.


sponsored ad

  • Advert
Click HERE to rent this advertising spot for BRAIN HEALTH to support LongeCity (this will replace the google ad above).

#3 Baten

  • Guest
  • 785 posts
  • 57
  • Location:Belgium

Posted 13 April 2012 - 04:33 PM

Piracetam will kill my testicles? But I love them... AND I love piracetam. What to choose - what to choose ?


Err.. nefiracetam is said to be harmful for your testicles, but only at large doses; at low doses it should be harmless although prolonged usage is discouraged.
Piracetam is absolutely harmless.

Edited by Baten, 13 April 2012 - 04:33 PM.


#4 golden1

  • Guest
  • 681 posts
  • 141
  • Location:US

Posted 13 April 2012 - 05:10 PM

Pirtacetam will kill my testicles? But I love them... AND I love piracetam. What to choose - what to choose ?


it's not helping with the reading comprehension :P

no insult intended just a joke.

#5 medievil

  • Guest Guest
  • 3,750 posts
  • 20
  • Location:Belguim

Posted 14 April 2012 - 08:26 PM

With that logic youd want to deplete gaba in the brain as it activates GABAA; really this is just some wild assumption that because it activates GABAA it can cause addiction like GABAA PAMS (benzo's).

Lets go to scie

nce!





Arzneimittelforschung.

1994 Feb;44(2A):243-7.


Drug dependence study of the new cognition-enhancing agent nefiracetam in rats.


Fujikawa K, Akiyama Y, Takayama S.



Source

Drug Safety Research Center, Developmental Research Laboratories, Daiichi Pharmaceutical Co., Ltd., Tokyo, Japan.



Abstract

The new cognition-enhancing agent nefiracetam (N-(2,6-dimethylphenyl)-2-(2-oxo-1-pyrrolidinyl) acetamide, DM-9384, CAS 77191-36-7) was assessed for dependence liability in rats using the DAF (drug admixed food) method and an intravenous self-administration system. In the physical dependence test, nefiracetam and codeine phosphate were administered to rats mixed with food for 43 days in a gradually increasing dosage schedule, followed by feeding a drug-free normal diet to detect signs of withdrawal. After the withdrawal, rats in the nefiracetam treated groups showed no withdrawal symptoms (e.g. body weight loss) and exhibited greater body weight gains than control. On the other hand, rats in the codeine phosphate treated group showed overt withdrawal symptoms (e. g. soft stool, diarrhea, vocalization) and a significant body weight loss, suggesting development of physical dependence on the drug. It was concluded that nefiracetam did not possess physical dependence liability in rats. In the reinforcement liability test, through an indwelling cannula implanted into the right jugular vein rats were allowed to self-administer nefiracetam, morphine hydrochloride or pentobarbital for 14 days. Saline was administered to negative control animals for the same period. The daily frequency of self-administration increased progressively with time in rats of the morphine hydrochloride and pentobarbital groups. In the nefiracetam groups, it remained comparable to or was even lower than that in the saline control group. When compared with the saline control, the group mean frequency of self-administration showed a tendency to be small for nefiracetam, whereas the morphine hydrochloride and pentobarbital showed greater frequencies.(ABSTRACT TRUNCATED AT 250 WORDS)




Edited by medievil, 14 April 2012 - 08:26 PM.

  • like x 1

#6 Junk Master

  • Guest
  • 1,032 posts
  • 87
  • Location:United States

Posted 15 April 2012 - 03:36 AM

I just want to know how much better it is than a multi-racetam stack plus choline source, and if the risk/damage is reversible.

I mean, it can't be worse than coke, or meth can it? Yet, I'd venture to guess that most posters here have lab ratted both.

Who cares about seminal volume if it's reversible?

Is this stuff better than say, 4.5 G of piracetam plus 500 mg of Ani, and 500 mg Centro?

Will it give me 3 hours of super creative, productive focus?

#7 Baten

  • Guest
  • 785 posts
  • 57
  • Location:Belgium

Posted 15 April 2012 - 07:37 AM

Will it give me 3 hours of super creative, productive focus?


No. But I found it to be very synergistic with pramiracetam, for sustained clear thoughts, very nice for studying.

#8 karma02

  • Guest
  • 35 posts
  • 4
  • Location:Canada

Posted 16 April 2012 - 02:18 AM

Just read the title. Thought there was a need for humor.

Piracetam and other structurally related nootropics.



#9 Introspecta

  • Guest
  • 622 posts
  • 55
  • Location:Massachusetts U.S

Posted 16 April 2012 - 02:17 PM

Nefiracetam made me number than a Halodol patient

#10 Wanderer2

  • Guest
  • 23 posts
  • 15
  • Location:Michigan

Posted 22 April 2013 - 09:34 PM

I read in a more recent Wikipedia article that the testicle problem was found to happen only in animals. Not humans, or primates.

Edited by Wanderer2, 22 April 2013 - 09:35 PM.

  • like x 1
  • Needs references x 1

#11 tydi

  • Guest
  • 25 posts
  • 26
  • Location:Canada

Posted 26 May 2013 - 03:31 PM

Nefiracetam at nights seemed to be somewhat efficient due to the GABA Agonist factors, but i also like how it attenuates the tolerance and dependence of the opioid receptor. The combination just of GABA/Opioid receptor modulation/attenuation still holds value for this Racetam IF drug-safety could be reached. .

is there any other Racetam that has similar effects to this that would meet the safety profile of more rigorously tested Racetams?

Reference:
http://onlinelibrary...enticated=false

#12 Synaesthesiac

  • Guest
  • 115 posts
  • 8
  • Location:Los Angeles
  • NO

Posted 27 September 2013 - 11:35 PM

Nefiracetam is only testicularly toxic in DOGS and other animals that metabolize it differently. The poster a few posts above is correct. Everyone can stop freaking out now.

#13 xsiv1

  • Guest
  • 463 posts
  • 40
  • Location:Canada

Posted 28 September 2013 - 02:02 AM

What do others think of Nefiracetam? It's available but I've rarely heard of many people liking it's effects.

#14 Introspecta

  • Guest
  • 622 posts
  • 55
  • Location:Massachusetts U.S

Posted 28 September 2013 - 03:11 PM

It made me feel quite numb. It did seem to really make me focus and relieve anxiety but just felt off like something was wrong and I couldn't have any pleasure. I through away 70 dollars worth. This was years ago. I'd keep the doses as low as possible which may have less side effects. Not everyone gets this numbing feeling either some actually enjoy the effects.

#15 xsiv1

  • Guest
  • 463 posts
  • 40
  • Location:Canada

Posted 28 September 2013 - 03:54 PM

Sounds more up my alley given it's gaba activity (to be used now and again). I don't think I'll be using my 5-10grams of Sunifiram. I can't even remember how much I bought at this point lol. It's been months. I'm just too concerned over it's glutamatergic activity and the fact that I take regular stimulants like caffeine, nicotine and ephedrine pre-workout.

#16 Reformed-Redan

  • Guest
  • 2,200 posts
  • -9
  • Location:Thousand Oaks, CA

Posted 28 September 2013 - 04:47 PM

Sounds more up my alley given it's gaba activity (to be used now and again). I don't think I'll be using my 5-10grams of Sunifiram. I can't even remember how much I bought at this point lol. It's been months. I'm just too concerned over it's glutamatergic activity and the fact that I take regular stimulants like caffeine, nicotine and ephedrine pre-workout.

I wouldent worry about that. I took a COMT inhibitor with MAOB inhibitor and that Detonate preworkout stimulant with 23 mg of methanphetamine analogue and ate some of those MSG ramen noodles and still lived to tell the story. Although my heart was in pain for a while after the whole experience. lol

#17 InquilineKea

  • Guest
  • 763 posts
  • 88
  • Location:Redmond,WA (aka Simfish)

Posted 04 November 2015 - 11:19 PM

What about nefiracetam's activation of PKC-alpha?



sponsored ad

  • Advert
Click HERE to rent this advertising spot for BRAIN HEALTH to support LongeCity (this will replace the google ad above).

#18 jroseland

  • Guest
  • 953 posts
  • 120
  • Location:Europe

Posted 10 January 2017 - 09:17 AM

ScienceGuy you mention that Nefiracetam is a GABA RECEPTOR AGONIST, if I'm understand correctly that means that over time it desensitizes or uses up all the Gaba receptors. Which kind of has an effect similar to alcohol wherein your tolerance goes up over time and you become increasingly dependent on a Gaba source to feel normal.







Also tagged with one or more of these keywords: nefiracetam, racetams, racetam, memory, piracetam, cognitive, cognition, aniracetam, oxiracetam, pramiracetam

0 user(s) are reading this topic

0 members, 0 guests, 0 anonymous users