Noopept: research, FAQs and dosage recommendations

Impairment of higher cortical functions is one of the most frequent and maladaptive complications among cerebrovascular diseases. Cognitive impairment, especially pronounced, can lead to significant restrictions in work, socialisation, and self-care. In such cases the quality of life of not only the patients themselves, but also their relatives may be significantly affected. Patients with cognitive impairment often fail to comply with the doctor’s recommendations regarding the treatment of the underlying vascular disease leading to brain damage. For those who have suffered a stroke, the effectiveness of rehabilitation measures can thus be reduced. That is why cognitive impairment in cerebrovascular diseases is always associated with a less favorable prognosis.

The range of conditions in which there are impairments to the basic cognitive functions (attention, memory, ability to analyze information and make decisions, spatial orientation) is very wide and include:

  • strokes,
  • chronic cerebrovascular insufficiency, 
  • brain injury, 
  • various chronic neurodegenerative brain lesions, 
  • neuroinfections, 
  • posthypoxic encephalopathies, 
  • chronic alcoholism, 
  • natural aging of the body,
  • mental retardation in children. 

The prevalence of cognitive pathology, as well as the variety of its individual manifestations in different people evoke the need to expand the arsenal of substances that normalize impaired cognitive functions. 

Insufficiency of mnestic functions arising after neurotrauma, strokes, senile disorders of the vascular and neurodegenerative nature develops against the background of pronounced structural changes in the brain tissue. For the treatment of these conditions, it is advisable to use drugs that combine nootropic and neuroprotective actions. 

Noopept (N-phenyl-acetyl-L-prolylglycine ethyl ester) is a Russian over-the-counter nootropic drug with a long history of use. It was developed in the early 1990s and a bit later it started gaining popularity in the Western countries. Its effect is physiological to the human body, as it is based on the formation of an active compound cyclopropyl glycine, which is naturally occurring in the brain. This substance is also called the “memory peptide”. The drug has pronounced nootropic and neuroprotective properties and contributes to:

  • Reduction of headaches, dizziness, palpitations;
  • Normalization of sleep;
  • Decreasing of irritability and improving the emotional background;
  • Improving health and reducing fatigue;
  • Improving memory.
Noopept pills

According to the manufacturer it might be useful for young people who want to restore high concentration of attention and good memory and for people over 50 y.o. who need to maintain mental performance in the family, at work, and in society. The clinical applications of the compound also include traumatic brain injury and stroke, asthenic disorders, and autonomic disorders. [14]

The Department and Clinic of Nervous Diseases of the Military Medical Academy (St. Petersburg, Russia) assessed the effectiveness and safety of Noopept in patients with mild post-traumatic cognitive impairments. A comprehensive analysis of the results of neuropsychological methods and scales used in the study showed that the use of the drug led to a significant improvement in a number of cognitive indicators within 30 days after the start of treatment. During the 2nd month of the drug administration, the improvement became less obvious, although it was characterized by a persisting tendency towards normalization. In general it is reasonable to believe that this phenomenon is due to the presence of the so-called “saturation”, which, however, is not a reason to reduce the treatment time. The drug was recommended for use in patients with mild concussion or contusion accompanied by cognitive impairment in the residual period. [10]

Pharmacological action of Noopept

The main effects of Noopept are: [14]

  • Nootropic (improves cognitive functions, promotes their recovery in case of damage, facilitates learning processes by stimulating intellectual activity);
  • Anxiolytic (reduces anxiety and irritability);
  • Vegetotropic (including sleep normalization);
  • Anti Asthenic;
  • A complex effect on the rheological properties of blood.

The nootropic effect of the compound is selective, i.e. there is no psychostimulatory, sedative action, it does not disturb the coordination of movements, and there is no muscle relaxant action. 

There is no cumulative effect, the development of tolerance and appearance of new components of the drug’s action. When the compound is discontinued, slight activation phenomena may be noted, with no signs of the development of “rebound” anxiety, characteristic of some nootropics. [6]

The mechanism of action of Noopept has been studied since the time of its synthesis. It was found that the drug enhances the expression of NGF and BDNF in the hippocampus [7], exhibits choline-positive properties at the behavioral and neuronal levels [12], reduces oxidative stress and enhances the activity of antioxidant systems [4], and inhibits stress-induced kinases pSAPK/JNK and pERK1 [9].

According to official information from the manufacturer, Noopept acts on specific binding sites in the cerebral cortex and forms cycloprolylglycine, which is similar in structure to an endogenous cyclic dipeptide with antiamnestic activity [13]. 

The neuroprotective effect is provided by weakening the neurotoxic effect of glutamates, counteracting the accumulation of intracellular calcium, reducing the formation of free radicals and the anti-inflammatory activity of the drug. This increases the resistance of the brain tissue to damaging influences (neurotrauma, hypoxia, electroconvulsive, toxic) and weakens the degree of damage to brain neurons. [14]

Noopept research and its History of creation

Noopept (N-phenylacetyl-Lprolylglycine ethyl ester) was developed in 1992 in the Zakusov Scientific Research Institute of Pharmacology named after Vasiliy Zakusov an honored pharmacologist of the Soviet Union. It is the result of more than 20 years of work by researchers. The non-peptide prototype of Noopept was the nootropic drug Piracetam. The pharmacological activity of the new compound was generally similar to the activity of Piracetam, but it was manifested in 1000 times lower doses [5]. The most pronounced antiamnestic effect was determined in doses of 0.5–0.8 mg/kg. The duration of action was 4-6 hours after a single intake. When it was increased to 1.2 mg/kg, the effect disappeared (“dome-shaped” dependence). For the reference nootropic Piracetam, the maximum effect was revealed at a dose of 500 mg/kg, with an increase in the dose to 800–1000 mg/kg the effect also disappeared. [6] In addition, Noopept is said to have more pronounced anxiolitic and neuroprotective properties in comparison to Piracetam.

Since its creation, the preparation has been tested and passed a lot of different clinical trials. Below you will find a short description of just a few of them.

A randomized clinical trial of comparative efficacy of Noopept and Piracetam in the treatment of asthenic disorders and disorders of organic genesis [6]

Clinical comparison of Noopept and Piracetam in patients with organic emotional labile disorder showed that the effectiveness of both drugs in terms of assessing the severity of psychopathological and somatic neurological symptoms, and cognitive functions was almost the same. However, Noopept was characterized by a lower risk of developing adverse events (by 12 – 62%). Besides Noopept revealed a number of advantages:

  • Significantly lower (almost 100 times) effective doses compared to Piracetam;
  • Influence on all phases of memory (introduction, consolidation, storage and retrieval of information), while Piracetam mainly affected the early phases of information processing;
  • Significantly broader (500 times) therapeutic margin;
  • Active on models of ischemic and hemorrhagic stroke (Piracetam – on models of ischemic stroke);
  • Reduction of glutamate excitotoxicity;
  • Significant reduction of the accumulation of intracellular calcium;
  • Pronounced anti-apoptotic effect;
  • Antioxidant and immunostimulating effects.

Multicenter study of the efficacy and safety of Noopept in the treatment of discirculatory encephalopathy (DE) with moderate cognitive impairment [8]

The study involved 360 patients aged 50–80 y.o. with DE of I and II stages of atherosclerotic and hypertensive genesis with moderate cognitive impairment. The study was carried out with the participation of specialists from 12 medical institutions in Russia. All patients took Noopept in a daily dose of 20 mg (10 mg 2 times a day) for 2 months. 

  • According to the results of the study, the positive effect of Noopept therapy on the cognitive functions of the examined patients was shown: attention, memory, neurodynamic functions, which confirms a significant improvement in the overall score according to MMSE against the background of Noopept treatment.
  • There was also a significant improvement in the CDT index, which reflected an improvement in constructive praxis.
  • Also, against the background of the use of Noopept, an improvement in neurodynamic functions and speech production was revealed, which was confirmed by a significant improvement in the categorical associations test and a positive trend obtained when comparing the results of the literal associations test.
  • Noopept was well tolerated.

Study of the efficacy and tolerability of Noopept in the treatment of moderate cognitive impairments (MCI) in patients after ischemic stroke [11]

The open prospective study included 60 patients aged 50 to 80 y.o. who had had an ischemic stroke during the last year before enrollment in the study. Patients of the main group were prescribed Noopept at a dose of 10 mg 2 times a day after meals for 2 months. The comparison group did not receive Noopept treatment. Patients of both groups, according to indications, continued treatment with antihypertensive, antiplatelet, and hypocholesterolemic agents.

  • After 2 months of therapy, there was a more pronounced improvement in the MMSE scale indicators in the main group of patients receiving additional Noopept therapy, compared with the control group.
  • Evaluation of the indicators of literal and categorical associations revealed a significant improvement in the performance of the categorical association test in patients receiving Noopept.
  • According to the scale of the general clinical impression on the change in GCIC, the overall assessment of the effectiveness of the therapy in the Noopept treatment group corresponded to a moderate improvement, while in the control group there was no dynamics on this scale.
  • During the study, no significant adverse reactions were detected when taking Noopept. There were no cases of discontinuation.

Use of Noopept in patients with moderate cognitive impairment of post-traumatic genesis [10]

The study enrolled 30 patients aged 19 to 66 with a history of documented TBI at least 6 months ago (concussion or contusion of the brain of mild degree), with moderate cognitive impairment, the development of which was directly related to the previous trauma and did not reach the degree of dementia. All patients received Noopept according to the scheme: 10 mg 2 times a day for 60 days.

  • Against the background of the ongoing therapy, significant changes from the baseline level were shown on the MMSE scale 30 days after the start of treatment (a significant improvement in concentration, decrease in attention fatigue, etc.).
  • The majority of patients noted a partial regression of subjective signs of the disease – many of them noted decreased headache, lower severity of dizziness, normalization of sleep, i.e. there was a trend to minimize symptoms that form the pseudoneurotic syndrome.

During Noopept administration, only 1 patient had an undesirable phenomenon – headache, which was regarded as insignificant and not related to taking the drug and it did not require cancellation.

About the Manufacturer of Noopept

OTCPharm JSC is a Russian pharmaceutical company which was formed as a result of the branching of the OTC business during the reorganization of Pharmstandard at the end of 2013.

The portfolio of OTCPharm is represented by such well-known and popular brands as: Arbidol, Afobazole, Noopept and others. 

All OTCPharm products are manufactured in strict accordance with the quality management system at Russia’s largest production facilities. The quality management system operating at the enterprises has been developed and implemented in accordance with the requirements of the national standards of the Russian Federation: 

OTCPharm production of Noopept
Production facilities of OTCPharm

Only raw materials that have passed the incoming inspection and received the appropriate permission are used in production. During the production process, monitoring of the main parameters is carried out, including environmental ones (microbiological control of air, equipment, clothing and hands of personnel, etc.), and product quality control.

The finished product is not subject to sale until the Authorized Body confirms in writing that each of its series has been produced and controlled in accordance with the requirements of the registration dossier.

Internal audits (self-inspections) at Pharmstandard enterprises are carried out in order to assess the effectiveness of the quality management system, increase its effectiveness, and determine further development paths. Audits are carried out in accordance with annually developed schedules, at a set time and with a certain frequency. All Pharmstandard enterprises undergo regular external audits, both by the state regulatory authorities of the Russian Federation and by independent European and Russian auditors.

Noopept pills production

What is the recommended dosage of Noopept?

Noopept dosage recommended by the producer is 10 mg orally, twice a day. With this dosage, the development of a full-fledged nootropic effect is known to occur at the 2nd or 3rd week of therapy. You can read the translation of the official instruction here.

There are some anecdotal reviews saying that Noopept is more effective in forms other than pills, for example spray or sublingual. But these unconventional forms are not spread in Russia, the country of origin of Noopept. We were unable to find any valid research supporting the effectiveness and safety of new forms of the preparation. Some enthusiasts argue that Noopept is a peptide and when taken orally, its main part dissolves (like ordinary proteins) and does not pass the blood-brain barrier, therefore it may not reach the brain. Some people state that in order for it to act faster, it must be taken intranasally or sublingually. Some compare it to Semax in this sense. But that is not quite correct, because Noopept is not a Semax.

Prior to the product launch in the form of pills in 1992, Noopept had undergone a number of clinical trials. Many forms of Noopept have been tested during Soviet research. Obviously, scientists came up with the most reliable mode and it is exactly how it is used in Russia nowadays which is in 10 mg pills.

Foreign vendors suggest various dosages, and the most common one is 30 mg pills. However the bioavailability of 10 mg is sufficient enough when administered orally, which is again supported by years of Noopept research in Russia and USSR. Read more in the “Research” tab on the product page!

In Russia, Noopept is sold in its original form only: pills with 10 mg of the active substance in each of them. 

FAQs

Can you get used to Noopept if you take it for a long time?

During the research, it was found that Noopept does not cause drug dependence (you cannot get used to it) and withdrawal syndrome (you can stop taking it at any time).

Can Noopept be used after a mixed stroke, and if there were epileptic seizures?

Noopept is indicated for the treatment of cerebrovascular insufficiency, including patients after stroke. There is no data on the adverse effect of Noopept on the course of epilepsy, and there is clinical experience about its good tolerance and effectiveness in these patients.

Is it possible to use the drug during pregnancy or lactation?

In the course of the experiment, it was found that Noopept has no teratogenic, mutagenic and immunotoxic properties. However, Noopept has not been studied in women during pregnancy and lactation, so it is not indicated for use in these cases.

Can Noopept be used in children to improve learning ability?

Noopept is registered for use in persons over 18 years old. Given the low level of toxicity, it is planned to conduct a number of studies that could allow registering Noopept in children.

Can Noopept be used for vegetative-vascular dystonia?

Noopept has a vegetative-normalizing effect, it helps to reduce headaches, orthostatic disorders, tachycardia and can be used for memory impairment in patients with vegetative-vascular dystonia.

Can Noopept be taken simultaneously with alcoholic beverages, if necessary?

The use of alcohol does not affect the metabolism and effects of Noopept in the body. At the same time, the neuroprotective properties of Noopept increase the resistance of the brain tissue to the damaging effects of toxic substances, including alcohol.

How often can a course of Noopept treatment be repeated?

The duration of taking Noopept depends on the nature of the disease, usually a course of 1.5-3 months is recommended, which can be repeated after a month’s break.

Can Noopept cause headaches?

Noopept has a vegetative normalizing effect, which leads to a decrease in headaches caused by autonomic dysfunction.

Can Noopept increase blood pressure?

When Noopept is taken in patients with arterial hypertension, mainly III degree, and with inadequate intake of antihypertensive drugs, an increase in blood pressure may be observed.

The chemical name of the active ingredient contains glycine. What is the difference between Noopept and glycine, why is it better?

Noopept has a peptide structure – it consists of amino acids and along with glycine the amino acid proline is included in Noopept, together they form the compound cycloprolylglycine in the human body, which has a pronounced effect on memory functions. Also, Noopept, unlike glycine, has a vegetative-normalizing effect (helps to reduce headaches, orthostatic disorders, tachycardia) and is taken orally, while glycine is digested in the intestines and is not absorbed.

Can Noopept be taken together with other psychotropic drugs?

Noopept has no drug interactions and is compatible with other centrally acting drugs.

Bibliography 

  1. Solntseva EI, Bukanova JV et al (1997). The effects of piracetam and its novel peptide analogue GVS-111 on neuronal voltage-gated calcium and potassium channels. https://pubmed.ncbi.nlm.nih.gov/9195198/
  2. Ostrovskaya RU, Romanova GA et al (1997). The novel substituted acylproline-containing dipeptide, GVS-111, promotes the restoration of learning and memory impaired by bilateral frontal lobectomy in rats. https://pubmed.ncbi.nlm.nih.gov/9833021/
  3. Ostrovskaya RU, Romanova GA, Barskov IV et al (1999). Memory restoring and neuroprotective effects of the proline-containing dipeptide, GVS-111, in a photochemical stroke model. https://pubmed.ncbi.nlm.nih.gov/10780261/
  4. Pelsman A, Hoyo-Vadillo C, Ostrovskaya RU et al (2003). GVS-111 prevents oxidative damage and apoptosis in normal and Down’s syndrome human cortical neurons. https://pubmed.ncbi.nlm.nih.gov/12711349/
  5. Kraineva VA, Galaeva IP et al (2006). Comparative activity of noopept and piracetam in the model of intracerebral post-traumatic hematoma. https://cyberleninka.ru/article/n/sravnitelnaya-aktivnost-noopepta-i-piratsetama-na-modeli-intratserebralnoy-posttravmaticheskoy-gematomy/viewer
  6. Avedisova AS, Yastrebov DV (2007). Comparative efficacy of Noopept and Piracetam in the treatment of asthenic disorders and disorders of organic genesis https://www.rmj.ru/articles/nevrologiya/Sravnitelynaya_effektivnosty_Noopepta_i_piracetama_pri_terapii_astenicheskih_rasstroystv_i_narusheniy_organicheskogo_geneza/
  7. Ostrovskaya RU, Gudasheva TA, Zaplina AP, et al (2008). Noopept stimulates the expression of NGF and BDNF in rat hippocampus. https://pubmed.ncbi.nlm.nih.gov/19240853/
  8. Yakhno NN, Damulin IV, Antonenko LM (2009). Noopept in the treatment of discirculatory encephalopathy with moderate cognitive impairment. http://kremlin-neurology.ru/library/Yahno_Noo_v_lechenii_DE_umer_kogn_r-va.pdf
  9. Ostrovskaya RU, Iu V Vakhitova IuV, M Kh Salimgareeva MKh et al (2010). On the mechanism of noopept action: decrease in activity of stress-induced kinases and increase in expression of neutrophines. https://pubmed.ncbi.nlm.nih.gov/21395007/
  10. Odinak MM et al (2011). Use of Noopept in patients with moderate cognitive impairment of post-traumatic genesis https://noopept.ru/themes/m/docs/4.pdf
  11. Amelin AV, Ilyukhina AYu, Shmonin AA (2011). Noopept in the treatment of mild cognitive impairment in patients with stroke. https://pubmed.ncbi.nlm.nih.gov/22500312/
  12. Vakhitova IuV et al (2015). Molecular mechanism of action of Noopept – a substituted by Pro-Gly dipeptide. https://noopept.ru/themes/m/docs/molekuljarnyj-mehanizm-dejstvija-preparata-noopept.pdf
  13. Mironova ES, Khavinson VKh et al (2020). Neuroprotective effects of peptides. https://khavinson.info/assets/files/skan/mironova-ag.pdf
  14. The official web-site of Noopept [https://noopept-ru.translate.goog/?_x_tr_sl=auto&_x_tr_tl=en&_x_tr_hl=ru&_x_tr_pto=nui_pto=nui]

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