Piracetam | |
Piracetamum | |
Chemical compound | |
IUPAC | 2-oxo-1-pyrrolidinacetamide |
Gross formula | C6H10N2O2 |
CAS | 7491-74-9 |
PubChem | 4843 |
DrugBank | 09210 |
Classification | |
Pharmacol. group | Nootropics (neurometabolic stimulants)[1] |
ATX | N06BX03 |
Pharmacokinetics | |
Bioavailable | 100% |
Metabolism | practically not metabolized |
Half-life | 4-5 hours |
Excretion | kidneys |
Dosage forms | |
granules for the preparation of syrup (for children), capsules, solution for intravenous and intramuscular administration, solution for oral administration, syrup, film-coated tablets[2] | |
Methods of administration | |
orally, intramuscularly, intravenously | |
Other names | |
Lucetam, Memotropil, Nootropil, Piratropil, Piracetam, Cerebril, Oykamid, Pyrabene, Piramem, Pyranol, Stamin, etc. | |
Media files on Wikimedia Commons |
Piracetam
is a nootropic drug, historically the first (synthesized in 1964[3]) and the main representative of this group of drugs; it remains one of the most important in it[4]. Chemically, it is a derivative of pyrrolidone and is the founder of the family of so-called “racetams” [5].
In most countries of the world, including the United States and Western European countries, piracetam and other nootropics are not registered as medicines, since their effectiveness in the treatment of dementia and neurodegenerative diseases has not been proven in controlled studies [6]. Despite this, in Russia and some other countries, piracetam is widely used in clinical practice for the treatment of many neurological, psychiatric and other diseases. In the resolution of the meeting of the Presidium of the Formulary Committee of the Russian Academy of Medical Sciences on March 16, 2007, piracetam was recognized as “an outdated drug with unproven effectiveness” [7]. As of 2019, it is included in the list of vital and essential medicines in the Russian Federation.
In Russia, the drug is used in neurological, psychiatric and drug treatment practice. As a result of the action of the drug, the concentration of ATP in brain tissue increases, the biosynthesis of ribonucleic acid and phospholipids is enhanced, and glycolytic processes are stimulated. Piracetam is believed to be effective in recovery from stroke, but there is no reliable scientific evidence for this or successful clinical trials.
According to research conducted in the USSR, piracetam improves brain function during oxygen deprivation and improves the formation of neural connections during the learning process[8].
Main characteristics
Piracetam is the main representative of the group of nootropic drugs. Currently, a number of its direct analogues and homologues (oxiracetam, etiracetam, etc.) similar to it in action have been synthesized, but piracetam continues to be the main drug of this group.
Piracetam is well absorbed when taken orally. When introduced into the body, it penetrates into various organs and tissues, including brain tissue. Practically not metabolized. Excreted by the kidneys.
The mechanism of action of the drug is not completely clear. Its purported effects are still poorly described, and clinical trials were conducted many years ago, using techniques that are not now considered standard[6].
Presumably, piracetam has a positive effect on metabolic processes and blood circulation in the brain. Stimulates redox processes, enhances glucose utilization, improves regional blood flow in ischemic areas of the brain. The drug increases the energy potential of the body by accelerating ATP turnover, increasing the activity of adenylate cyclase and inhibiting nucleotide phosphatase. Improvement in energy processes under the influence of piracetam leads to increased resistance of brain tissue to hypoxia and toxic influences. There is evidence of an increase in the synthesis of nuclear RNA in the brain under the influence of piracetam.
Oxiracetam and Aniracetam: pros and cons
Oxiracetam and Aniracetam are similar in their effects on the human body; there are no significant differences. The only significant difference between the drugs is the strength of their effect. Aniracetam is approximately twice as potent as Oxiracetam. Regarding opinions for and against: both remedies are good, they can be taken to improve brain activity and memory. Of course, if in doubt, it is better to consult a specialist.
Some patients experience a feeling of strong inhibition, lack of emotions, and apathy as a result of use. Therefore, they advise resorting to such means only once and only in case of anxiety.
Indications for use
It is used to improve metabolic processes occurring in the cerebral cortex in various diseases of the central nervous system, especially those associated with vascular disorders and pathology of metabolic processes in the brain. The medicinal properties of piracetam are determined by its ability to enhance the integrative activity of the brain and intellectual activity, promote memory consolidation, improve learning processes, restore and stabilize brain functions, including in elderly and senile people[4]
In neurological practice, it is prescribed for cerebral atherosclerosis, vascular parkinsonism and other diseases with symptoms of chronic cerebrovascular insufficiency, manifested in memory impairment, attention, speech, dizziness, etc., as well as for changes in cerebral circulation, in comatose and subcomatose states after brain injuries and intoxications, as well as during the period of rehabilitation therapy after such conditions [9][10][11]. Piracetam is also used for diseases of the nervous system, accompanied by a decrease in intellectual-mental functions and disturbances in the emotional-volitional sphere.
In psychiatric practice, piracetam is used in patients with neurotic and asthenoadynamic depressive states of various origins with a predominance in the clinical picture of signs of adynamia, asthenic and senesto-hypochondriacal disorders, phenomena of ideational inhibition, as well as in flaccid apathetic defective states in patients with schizophrenia, with psychoorganic syndromes of various etiologies, senile and atrophic processes, in complex therapy of various mental diseases. Piracetam can also be used as an adjuvant in the treatment of patients with depressive conditions, resistant to antidepressants, as well as with poor tolerance to antipsychotics and other psychotropic drugs in order to eliminate or prevent the somatovegetative, neurological and mental complications caused by them.
There is evidence of the positive effect of piracetam in patients with coronary heart disease in the elderly and senile [12]. An increase in the effect of antianginal drugs, a decrease in the need for nitroglycerin, and regression of signs of heart failure were noted[13].
The drug is also used in pediatric practice for various cerebroasthenic, encephalopathic disorders, memory disorders, intellectual disability, etc.
There is evidence of the advisability of using piracetam to reduce the phenomena of hypoxia and cerebral ischemia in acute viral neuroinfections[14].
Piracetam is also used to relieve withdrawal, pre- and delirious states in alcoholism and drug addiction, as well as in cases of acute poisoning with alcohol, morphine, barbiturates, etc.
The use of piracetam in a complex of means for relieving acute effects of alcohol withdrawal reduces the severity of cerebral vascular disorders, reduces headaches, dizziness, a feeling of apathy, and drowsiness[15]. In chronic alcoholism, piracetam is prescribed to reduce the phenomena of asthenia, intellectual-mnestic and other mental disorders.
General information about the drug
Oskiracetam is a drug that acts directly on the nervous system.
Belongs to the group of psychoanaleptic nootropic drugs. Its use can enhance the development of logic and helps people whose professions involve constantly counting numbers or solving complex mathematical problems. With regular use, it helps to establish long-term memory functions and restores nerve cells.
This substance belongs to Racetams and was one of the first synthesized by scientists. However, despite this it remains not fully studied. It cannot be isolated from food and does not occur naturally. Often used among students and schoolchildren, this allows them to better concentrate their attention.
Clinical experience
According to experimental data, piracetam enhances the effect of antidepressants and, when used in combination, can increase their effectiveness [16].
Due to its antihypoxic effect, the use of piracetam is recommended in the complex treatment of patients with ischemic stroke and myocardial infarction[17].
However, the randomized multicenter placebo-controlled trial PASS (Piracetam in Acute Stroke Study) showed the lack of effectiveness of piracetam in the treatment of acute ischemic stroke. The observed results of using piracetam are similar to those of placebo. In this study, patients received piracetam at a dose of 12 grams per day, therapy began within the first 12 hours from the onset of stroke. Upon additional analysis, however, it was found that the positive effect of piracetam still manifests itself in a subgroup of patients with earlier (up to 7 hours) initiation of therapy for moderate and severe (Orgogozo score less than 55 out of 100 points) stroke [18]. Another study, PASS II, was conducted with the inclusion of 800 patients and the administration of piracetam in the first 7 hours after the onset of stroke [19]. The results of the study were never published by the sponsor[20].
Analogs
Among the analogues, the following nootropic drugs can be distinguished:
- Piracetam is the leader of all Racetams, improves memory, thinking, learning and memorization. Stimulates both brain centers;
- Pramiracetam is the most powerful drug. Its effect lasts for 8 hours after the first dose;
- Aniracetam - the effect of its action occurs in a short time. Reduces anxiety, stabilizes the emotional background, activates the functions of creativity and eloquence.
Before starting treatment, you should definitely consult your doctor.
Contraindications
Hypersensitivity to piracetam and pyrrolidone derivatives; hemorrhagic stroke, severe renal failure (creatinine clearance less than 20 ml/min), agitated depression, Huntington's disease, pregnancy, breastfeeding, children under 1 year of age [1].
Restrictions on use
Impaired hemostasis, severe bleeding, during major surgical operations; hyperthyroidism; epilepsy.
People with severe cerebral atherosclerosis should not take the drug, since an increase in metabolism in the nervous tissue under the influence of the drug can lead to increased symptoms of dementia and irreversible deterioration of cognitive functions. This condition occurs due to the inability of the brain vessels to provide a sufficient flow of metabolites.
Persons prone to neurotic reactions should take into account that the drug, with long-term use, causes an increase in the level of anxiety, which can lead to sleep disturbances (mainly insomnia) and an indirect decrease in intellectual functions due to deterioration in concentration.
Use during pregnancy and breastfeeding: contraindicated during pregnancy; breastfeeding should be stopped during treatment.
If not well tolerated
If one or more side effects appear during the use of Aniracetam, first of all it is necessary to add choline to the course of treatment. In addition, the dosage is reduced. This is usually enough to get rid of unpleasant symptoms. If such measures do not improve your well-being, it is recommended to stop using the drug.
If the nootropic is taken for a very long time, addiction may develop. That is why it is better to adhere to course treatment with long breaks. In medicine, there are isolated cases of withdrawal syndrome occurring when stopping the use of the drug.
Side effects
Main source: [1]
- From the nervous system and sensory organs: hyperkinesia (>1%), increased irritability (>1%), drowsiness (<1%), depression (<1%), asthenia (<1%), agitation, aggressive behavior, disorder sleep, dizziness, headache, increased libido, tremor.
- Exacerbation of coronary insufficiency;
- nausea, vomiting, diarrhea, abdominal pain;
- weight gain (>1%);
- skin hypersensitivity reactions.
Notes
- ↑ 1 2 3
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Encyclopedia of Medicines
. Register of Medicines of Russia (2002). Access date: October 27, 2011. - Search in the drug database, search options: INN - Piracetam
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Circulation of medicines
. Federal State Institution “Scientific Center for Expertise of Medical Products” of Roszdravnadzor of the Russian Federation (March 27, 2008). — A standard clinical and pharmacological article is a by-law and is not protected by copyright in accordance with part four of the Civil Code of the Russian Federation No. 230-FZ of December 18, 2006. Access date: May 3, 2008. Archived September 3, 2011. - Dr. Corneliu E. Giurgea – The Father of Nootropics
- ↑ 12
Mashkovsky, 2005, pp. 111-113. - S. Shorvon. Pyrrolidone derivatives // The Lancet, 2001, V. 358, P. 1885-1892.
- ↑ 1 2 3 Flicker L., Grimley Evans J.
Piracetam for dementia or cognitive impairment. Cochrane Database of Systematic Reviews 2001, Issue 2. Art. No.: CD001011. doi:10.1002/14651858.CD001011 - RESOLUTION of the Meeting of the Presidium of the Formal Committee of the Russian Academy of Medical Sciences on March 16, 2007, RAMS
- Karkishchenko, Nikolai Nikolaevich. Psychounitropism of drugs - M.: Medicine, 1993. ISBN 5-225-02213-8
- Veselyekiy I. Sh., Voronyuk M. I.
The effect of piracetam on central hemodynamics in patients with atherosclerosis with discircular encephalopathy. // Wedge. Med. - 1986. - No. 6. - P. 41-44 - Sharava E.V., Potapov A.A., Kulikov M.A.
The effect of piracetam on the functional activity of the brain in patients with traumatic brain injury. // Journal. neuropathol. and a psychiatrist. - 1988 - No. 5. - P. 42-48 - Eninya G.I.
Timofeeva T. N. Piracetam and indicators of cerebral hemodynamics, lipid metabolism and rheological properties of blood in initial forms of cerebrovascular accident. // Journal. neuropathol. and a psychiatrist. - 1990. - No. 11 - P. 20-23. - Pimenov L. T., Kalinina S. A., Churshin A. D.
Clinical and hemodynamic effectiveness of piracetam (nootropil) in patients with coronary heart disease in the elderly and senile at the outpatient stage of rehabilitation. // Cardiol. - 1992. - No. 5. - P. 35-38 - Pimenov L. T., Churshin A. D., Ezhov A. V.
On the ability of piracetam and tocopherol acetate to potentiate the clinical effectiveness of antianginal drugs in patients with coronary heart disease. // Wedge. honey. - 1997. - No. 1. - P. 32-35. - Niss A.I., Umansky K.G. et al.
On the effectiveness of treatment of acute viral neuroinfections with piracetam. // Journal. neuropathol. and a psychiatrist. - 1985. - No. 2. - P. 189-195. - Entin G. M.
Treatment of alcoholism. - M.: Medicine, 1990. - Mashkovsky M. D., Andreeva N. I., Parshin V. A.
The effect of piracetam on the effect of antidepressants. // Journal. neuropathol. and a psychiatrist. - 1989. - No. 2. - P. 129-131. - Leshchinsky L. A., Pimenov L. T., Fedorov V. S.
Therapeutic use of piracetam in patients with myocardial infarction. // Cardiol. - 1987. - No. 2 - P. 46-49. - Peter Paul De Deyn, Jacques De Reuck, Walter Deberdt, Robert Vlietinck, Jean-Marc Orgogozo.
Treatment of Acute Ischemic Stroke With Piracetam (English) // Stroke (English) Russian.. - Lippincott Williams & Wilkins (English) Russian., 1997. - Vol. 28, no. 12. - P. 2347—2352. — ISSN 0039-2499. - doi:10.1161/01.STR.28.12.2347. - Major Ongoing Stroke Trials. (English) // Stroke (English) Russian.. - Lippincott Williams & Wilkins (English) Russian., 2000. - Vol. 31, no. 6. - P. 1474-1480. — ISSN 0039-2499. - doi:10.1161/01.STR.31.6.1474.
- Graeme J. Hankey, Stefano Ricci, Maria Grazia Celani, Teresa Anna Cantisani, Enrico Righetti.
Piracetam for Acute Ischemic Stroke (English) // Stroke (English) Russian.. - Lippincott Williams & Wilkins (English) Russian., 2006. - Vol. 37, no. 8. - P. 2191-2192. — ISSN 0039-2499. - doi:10.1161/01.STR.0000231643.42650.a9. - Malykh AG, Sadaie MR
Piracetam and piracetam-like drugs: from basic science to novel clinical applications to CNS disorders (English) // Drugs (English) Russian. - Adis International, February 2010. - No. 70(3). — P. 287—312. - A.H. Gouliaev, A. Senning.
Piracetam and other structurally related nootropics // Brain Research. Brain Research Reviews. - May 1994. - No. 19(2). — P. 180—222.