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Questions about Nootropics - Nefiracetam


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#1 blaise

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Posted 02 June 2005 - 03:08 PM


I am going to try the folowing nootropics and was wondering which ones needed to be taken with food (fat soluble) and at which dosage. Also, do any need to be refrigerated.

Oxiracetam 500mg 2x a day ?
Nefiracetam 300mg 2x a day ?
Pyritionol 500mg 2x a day ?
Centrophenoxine 250mg 2x a day ?

Edited by blaise, 02 June 2005 - 05:08 PM.


#2 lemon

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Posted 02 June 2005 - 03:42 PM

Blaise,

Where are you getting your nefiracetam?

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#3 blaise

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Posted 02 June 2005 - 05:03 PM

I purchased it from Custom Nutrition Warehouse (CNW). They have recently added a bunch of bulk powder nootropics, that can not be found in bulk form anywhere else that I know of.

I can't praise them enough as far as shipping and customer service goes. I once placed an order through CNW and BN on the same night and I tracked both orders. They both were shipped the next day. The CNW order which was shipped USPS Priority mail arrived 2 days before the BN order which was shipped via UPS. Every order that I place with CNW arrives within 2-3 days. CNW is located in MO and I am located in NY.

Custom Nutrition Warehouse

Here is the description of Nefiracetam that is posted at their site:

Nefiracetam appears to have a more far-reaching effect over the mechanisms of cognition and memory than either aniracetam or pramiracetam. It induces greater intensity of theta spindles in hippocampus, which are a sign of greater LTP. Also, it increases intracellular cAMP levels and Ca2+ ion levels. When Ca2+ ions flood a neuron, it causes the release of assistor proteins like C-kinase. cAMP is essentially a signal protein that binds with C-kinase proteins and others, which thus encourages the release of CREB proteins, the be-all, end-all of the master memory molecules that results in a permanent memory formation.

Nefiracetam is a cross between Galantamine, a Nicotinic receptor agonist and a low powered GABA agonist like Phenibut.It would be quite different in effect from a pure Acetylcholine product like Piracetam.

It should be like smoking a cig or chewing a piece of nicotine gum and taking 0.5 to 1.0 grams of phenibut. That sound weird, but it should have the dual properties of stimulation and sedation and be quite interesting as a nootropic. It also has a calcium channel sedation effect, the combo of GABA and this would make it similar to Dilantin, an antieplipetic drug that is used as a nootropic.



#4 wannafulfill

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Posted 02 June 2005 - 06:07 PM

Please let us know how the nefiracetam works,
thanks

#5 Guest_da_sense_*

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Posted 02 June 2005 - 09:12 PM

I really can't remember well, but I have a feeling i've read something about nefiracetam being somewhat toxic racetam...anyone?

#6 brooklynjuice

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Posted 02 June 2005 - 10:05 PM

yea i have read some berry berry bad stuff about it but cant remember source

#7 wannafulfill

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Posted 02 June 2005 - 11:13 PM

This is enough to make me stay away from prolonged use:

1: Reprod Toxicol. 2004 May;18(3):423-30. Related Articles, Links


Testicular toxicity induced in dogs by nefiracetam, a neutrotransmission enhancer.

Shimomura K, Shimada M, Hagiwara M, Harada S, Kato M, Furuhama K.

Drug Safety Research Laboratory, Daiichi Pharmaceutical Co, Ltd, 1-16-13 Kitakasai, Edogawa-ku, Tokyo 134-8630, Japan. shimop7x@daiichipharm.co.jp

To investigate mechanisms of the testicular toxicity of nefiracetam and to find sensitive parameters to predict the toxicity, male beagle dogs were orally administered 180 or 300 mg/kg per day of the drug once and for 1 and 4 weeks. Time-course changes in serum and/or testicular hormone levels and semen parameters, and testicular morphology were examined. The testicular testosterone level was decreased 4 h after single administration of nefiracetam at 300 mg/kg per day, but the progesterone level showed no change at that time. The serum testosterone level was decreased after single, 1-week or 2-week treatment. In contrast, the serum estradiol level was increased from 1- to 4-week treatment. No changes in serum LH, FSH and inhibin B levels were observed throughout the experimental period. Decreased sperm motility and increased number of malformed sperms were first observed in semen after 4-week treatment. Histopathological examination of the testis revealed moderate and severe seminiferous atrophy with multinucleated giant cell formation at 180 and 300 mg/kg per day, respectively, after 4-week treatment, but not 1-week treatment. These results show that nefiracetam decreases testicular testosterone level in dogs following single oral administration of a high dose, and induces severe morphologic changes after 4-week treatment. This reduction is shown to be a sensitive parameter to detect the toxicity, and is suggested to be induced by the impaired conversion of progesterone to testosterone in Leydig cells.

PMID: 15082078 [PubMed - indexed for MEDLINE]

1: Toxicol Lett. 2003 Aug 28;143(3):307-15. Related Articles, Links


Investigation of testicular toxicity of nefiracetam, a neurotransmission enhancer, in rats.

Shimada M, Shikanai Y, Shimomura K, Harada S, Watanabe G, Taya K, Kato M, Furuhama K.

Drug Safety Research Laboratory, Daiichi Pharmaceutical Co. Ltd., Tokyo, Japan.

Testicular toxicity of nefiracetam (N-(2,6-dimethylphenyl)-2-(2-oxo-1-pyrrolidinyl) acetamide), a neurotransmission enhancer, was investigated in male Slc:SD rats. Nefiracetam was orally administered daily at 1500 mg/kg for 4 weeks, and the animals were killed sequentially during the course of administration to determine testicular histopathological changes and sperm head counts (SHC), and hormonal changes. Retention of step 19 spermatids, sporadic degeneration of pachytene spermatocytes and step 7 spermatids in the stage VII seminiferous tubules, and a decrease in SHC were seen as earliest changes after 1 week of administration. These changes gradually advanced up to atrophy of seminiferous tubules with multinucleated-giant-cell formation after 4-week administration. Serum and testicular testosterone levels were decreased, but recovered to the control levels within a day following a single administration, and the decreases were repeated after 1-week administration. These results suggest that nefiracetam-induced earliest changes could be caused by the decreased level of testicular testosterone.

PMID: 12849691 [PubMed - indexed for MEDLINE]

#8 blaise

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Posted 02 June 2005 - 11:25 PM

da sense, Thanks for letting me know about that. I would like to find more information about its toxicity. Anyone have any info?

So far with about 300mg of Nefiracetam I sorta feel a slight head rush type feeling, and a somewhat stimulating effect - but in a calm way. Feels a little like ephedrine without the jitters.

So far I really like the effects of Nefiracetam. I hope it is not toxic.

#9 Guest_da_sense_*

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Posted 02 June 2005 - 11:41 PM

Ummm i don't want to mess with my reproductive organs :) altough dose used in above studies is quite large, even taking so much of vitC per body kg would have negative effects :)

#10 wannafulfill

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Posted 03 June 2005 - 12:55 AM

maybe the doses are high, but the testicular testosterone level was decreased 4 h after a SINGLE administration

#11 blaise

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Posted 03 June 2005 - 03:03 AM

Wow those studies scare me. The last thing I want to do is decrease my testosterone levels! What do you think LifeMirage?

#12 blaise

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Posted 03 June 2005 - 04:43 AM

I did some research and found out this topic was discussed in detail on Feb. 10, 2005. The post by vortexentity was called "Nefiracetam Experiment log, Working with Nefiracetam" .

It seems to work well for some people as far as nootropics go (even better then other racetams) but some people have problems with cardiac arrhythmia while taking this. Also, the doses are no where near high enough to cause testicular toxicity. Read the previous thread:

Nefiracetam Experiment log, Working with Nefiracetam

I am still interested to hear LifeMirage's take on Nefiracetam.

#13 LifeMirage

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Posted 03 June 2005 - 05:39 AM

I currently do not recommend Nefiracetam, unlike many nootropics there is not much available human data concerning its effects and safety.

Example Piracetam has been in use for over 30 years, 100 countries, and over a million people have used it.

With Nefiracetam I can't find any human studies or approved use in any country.

It should be consider a research chemical unless a fair amount of human studies are performed.

While there are few studies [Reprod Toxicol. 2004 May;18(3):423-30.Testicular toxicity induced in dogs by nefiracetam, a neutrotransmission enhancer, Toxicol Pathol. 1996 Sep-Oct;24(5):549-57. Examination of lesions in the urinary bladder and kidney of dogs induced by nefiracetam, a new nootropic agent, J Toxicol Sci. 1995 Aug;20(3):309-17.Male reproductive toxicity study of nefiracetam in rats] showing toxicity when using 180, 300 mg, and 1500 mg/kg.

However studies using lower doses show little signs of damage. [Arzneimittelforschung. 1994 Feb;44(2A):254-9.Oncogenicity studies of the cognition-enhancing agent nefiracetam in mice and rats, Arzneimittelforschung. 1994 Feb;44(2A):251-3.Mutagenicity study of the new cognition-enhancing agent nefiracetam]

An excellent study although in dogs: Arzneimittelforschung. 1994 Feb;44(2A):228-38. Fifty-two-week oral toxicity study of the new cognition-enhancing agent nefiracetam in dogs.]

"There were no treatment-related findings at the low dosage level (10 mg/kg/d) and, therefore, this level was considered as the non-toxic effect level of nefiracetam."

Also in: Arzneimittelforschung. 1994 Feb;44(2A):217-9. Thirteen-week oral toxicity study of the new cognition-enhancing agent nefiracetam in dogs.

"The non-toxic dose was 20 mg/kg under these experimental conditions."

A study comparing the effects of Aniracetam to Nefiracetam found in ineffective [Pharmacol Biochem Behav. 2000 Aug;66(4):827-33.Recovery of diminished mealtime-associated anticipatory behavior by aniracetam in aged rats.]

Perhaps if the human studies conducted outside the US become available and/or more research is done it still may prove it be of benefit.

#14 lemon

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Posted 03 June 2005 - 03:34 PM

Drug companies are out to make money. No-one can make money off piracetam as it's been around for 30 years and it's simple to make. This is why all the other 'racetams are in existance.

Aside from a fat soluable 'racetam such as Ani, no big reason to take an analogue with a jacked up price. Choose your metabolic preference or take both. You're just wasting money IMHO

All of Piracetam's testing happened over a decade ago... on a sliding scale it's also likely p'tam shares the same affects with it's analogues.

#15 pinballwizard

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Posted 26 June 2005 - 07:17 PM

Blaise,

what is the update on Nefiracetam? Is it any good?

#16 pinballwizard

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Posted 26 June 2005 - 07:18 PM

also, what dosage are you taking? what is the dosage with the other cetams too? What dosage do you recommend?

#17 caveoli

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Posted 26 June 2005 - 09:36 PM

Nefiracetam has also been found to cause renal papillary necrosis in dogs.
(PM me for the full study).

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#18 ScienceGuy

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Posted 21 February 2012 - 09:06 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... see THIS thread for details: NEFIRACETAM - Another reason to avoid prolonged usage :)




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