NOOPEPT REVIEW

by L F

Noopept (Also known as GVS-111) is a relatively new Russian nootropic substance, developed in 1992 by Zakusov Institute of Pharmacology. Noopept is a dipeptide drug, which is a combination of non-peptide Piracetam and a fragment of Vasopressin peptide. Pharmacological study of the drug showed its advantages over peptide and non-peptide analogs.   
The developments were done within the idea that some regulatory neuropeptides may have a significant impact on memory and learning process. Unlike Vasopressin, which shows nootropic activity only when delivered to the brain structures, Noopept is active even upon oral administration. It affects memory and learning process, and effective in the treatment of a wide variety of cognitive disorders.  
Pharmacokinetic studies of this Nootropic showed good bioavailability to the brain.   
 

NOOPEPT EFFECTS

Studies show that a 20-30mg daily dose of Noopept provides mild stimulating and anxiolytic effect, and also improves attention, memory and cognitive functions. By its anxiolytic action, it can reduce anxiety, irritability, insomnia and affective lability (mood swings). Noopept has a broad spectrum of nootropic action. It improves not only initial memory acquisition and consolidation but also the process of memory recalling, unlike Piracetam.   
Neuroprotective effects of the drug manifested in increasing the resistance of brain tissue to damaging conditions like hypoxia (oxygen deficiency), intoxication, stressful events or traumatic injuries. Studies have shown that Noopept prevents neurodegeneration (the death of neurons) caused by the influence of toxic concentrations of glutamate and active forms of oxygen.    
Noopept also can be considered as BDNF (Brain-derived neurotrophic factor) and NGF (nerve growth factor) supplement. Studies done in rats show that prolonged usage of Noopept does increase BDNF and NGF levels in the hippocampus. Those neurotrophic factors promote growth and survival of neurons and modulate the long-term memory.   
Summing this up, you can expect the following effects of taking Noopept: 
 
  • Improvement of memory, attention, and cognitive functions.
  • Anti-anxiety effect.
  • Increased brain resistance to stressful conditions.
  • Mild stimulating effect.
  
 

MECHANISM OF ACTION

Noopept has a complex mechanism of action. The principle of memory-enhancing effect based not on simple cerebral blood flow improvement. Noopept has a direct impact on the synaptic structure, especially at the Hippocampus. The nootropic effect of the drug associated with one of its active metabolites, cyclo-Glycyl-L-Proline. Cycloprolylglycine is an endogenous peptide with anti-amnesic and selective anxiolytic effect. Recent studies show that Cycloprolylglycine can increase BDNF levels and acts as a positive allosteric AMPA modulator, thus having a significant impact on memory and learning.  
In Russian clinical practice, Noopept used as the treatment of various neurodegenerative diseases. The reason for this its wide spectrum of Neuroprotective action.   
  Here are ways how Noopept protects your brain:
  • Activation of endogenous antioxidant systems.
  • Blockage of voltage-dependent calcium and potassium channels.
  • Anti-inflammatory activity.
  • Reduction of glutamate release.
  • Increasing the level of antibodies to beta-amyloid and decreasing its toxicity. Beta-amyloid is a peptide that is involved in the development of Alzheimer’s disease. It is toxic to the nerve cells.

NOOPEPT DOSAGE AND HOW TO TAKE IT

The therapeutic dosage of Noopept is 1000 times lower compared to Piracetam.   
Suggested daily dosage is 20mg daily in two divided doses. The first dose in the morning, the second in the afternoon. You can increase the dosage for up to 40mg daily. It is not recommended to take Noopept later than 6 PM.   
The length of Noopept cycle is 1.5-3 months. You can start taking it again after the one-month rest period. The effect becomes more pronounced during long-term usage.   
The drug has high oral bioavailability, especially compared to Piracetam. However, you can take Noopept sublingually for a faster and more intense effect.   
Another way to take Noopept is a nasal drops or spray. This method is for experienced users. You can dissolve a small amount of Noopept powder in saline, and use it as nasal drops. Start with a 0.1mg dosage. Saline is a 0.9% sodium chloride solution. You can buy a bottle for just two dollars. This method is not only effective but also very economical because of the lower effective dosage.  
 

SIDE EFFECTS AND CONTRADICTIONS

Noopept side effects are similar to Racetams. The most frequent side effect is a headache, which usually is a result of poor Choline intake. This side effect can be overcome with Choline supplementation. You can either take choline supplement like Alpha-GPC, CDP-choline, and Choline Bitartrate or eat a choline-rich diet. Eggs, liver, fish, and nuts are high in choline.   
Less frequent and noticeable side effect is an increased blood pressure. If you suffer from hypertension, you should use Noopept cautiously.  
Next possible side effect is irritability. If you experienced this side effect and it’s overcome the benefits, you can reduce the dosage or stop taking this supplement.  
The least possible side effects are anxiety and dizziness. Some people who take Noopept before bed experience insomnia. This is why it should be taken not later than 6 PM.  
The official contradictions are pretty standard. They include pregnancy, lactation, age below 18, Hypersensitivity to the drug, liver and kidneys dysfunction.  
So, the possible side effects (from more to less frequent) is:  
  • Headaches.
  • Increased blood pressure.
  • Irritability.
  • Anxiety.
  • Dizziness.
  • Insomnia.
  • Allergic reaction.
  
Most people, however, don’t experience any side effects. But you should know about possible difficulties when taking this Nootropic. The responsible usage is the key to the satisfying results.  
The Ability of Noopept to be metabolized to endogenous substances (substances that produce naturally in the body) is the main reason of its low toxicity and high therapeutic index.   
The therapeutic index is the ratio between the lethal dosage and effective dosage. A safer drug has a higher therapeutic index. TI for Piracetam is 60, while TI for Noopept is 10.000. Such low toxicity determines the possibility of long-term usage with less risk of side effects.  
 

NOOPEPT REVIEW CONCLUSION

Noopept is a very effective Nootropic for memory. It can increase your concentration and improve your cognitive functions as well. Besides that, some people may experience the stimulating and anxiolytic effect.   
This Nootropic has higher bioavailability compared to Piracetam, and significantly less effective dosage. Low toxicity and abuse potential allow long-term usage of Noopept.   
Some people experience side-effects. For someone, the benefits of Noopept overweight it, for some people not. So the best way to test how your body responds to this substance is to start with the small dosages. Just like with any Nootropic or any other supplement.   
The benefits of Noopept  
  • Strong Nootropic effect. Significantly improves memory processing and recall, concentration and cognitive functions.
  • A wide range of Neuroprotective action.
  • Small therapeutic dosage, particularly in the intranasal administration.
  • Low toxicity (20 times higher therapeutic index than Piracetam).
  • May used long-term.
   
The downside  
  • It may be difficult to dose such little amount of powder precisely. Having a pocket scales or taking capsulated version makes everything easier.
  • Extremely bitter taste. It’s even more noticeable during sublingual usage of Noopept. And again, capsules are a solution.
  • Side effects. They are rare but possible.
 

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  References  
  1. Ostrovskaia R.U. et al The original novel nootropic and neuroprotective agent noopept (2002)
  2. Gudasheva TA, et al The major metabolite of dipeptide piracetam analogue GVS-111 in rat brain and its similarity to endogenous neuropeptide cyclo-L-prolylglycine . Eur J Drug Metab Pharmacokinet. (1997)
  3. Ostrovskaya RU, et al Noopept stimulates the expression of NGF and BDNF in rat hippocampus . Bull Exp Biol Med. (2008)
  4. Bochkarev VK, Teleshova ES, Siuniakov SA, Davydova DV, Neznamov GG. Clinical and electroencephalographic characteristic of noopept in patients with mild cognitive impairment of posttraumatic and vascular origin. Zh Nevrol Psikhiatr Im S S Korsakova. 2008
  5. Neznamov GG, Teleshova ES. Comparative studies of Noopept and piracetam in the treatment of patients with mild cognitive disorders in organic brain diseases of vascular and traumatic origin. Neurosci Behav Physiol. 2009
  6. Amelin AV, Iliukhina AIu, Shmonin AA. Noopept in the treatment of mild cognitive impairment in patients with stroke. Zh Nevrol Psikhiatr Im S S Korsakova. 2011
  7. Bobkova NV, Gruden' MA, Samokhin AN, Medvinskaia NI, Morozova-Roch L, Uudasheva TA, Ostrovskaia RU, Seredinin SB. Noopept improves the spatial memory and stimulates prefibrillar beta-amyloid(25-35) antibody production in mice. Eksp Klin Farmakol. 2005
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