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What is Piracetam


  
Piracetam is a cerebral function regulating drug which is claimed to be able to enhance cognition as well as slow down brain aging and may play a critical role in maintaining optimal mental performance.  It is a member of the class of drugs known as nootropics (“smart drugs” or “cognitive enhancers’), which substances purportedly enhance mental performance.

Piracetam is one of the racetams, and is similar in molecular structure to the amino acid pyroglutamate.  Piracetam and pyroglutamate have the same base chemical structure, the 2-oxo-pyrrolidine, but they differ by a side chain. Pyroglutamate is 2-oxo-pyrrolidine carboxylic acid, and piracetam is 2-oxo-pyrrolidine acetamide.  It is a cyclic derivative of GABA.  Piracetam was created about 30 years ago by UCB Laboratories.  Other trade names may include, Avigilen, Cerebroforte, Cerebrospan, Cetam, Dinagen, Encefalux, Encetrop, Euvifor, Gabacet, Genogris, Memo-Puren, Nootron, Nootrop, Nootropil, Nootropyl, Normabrain, Norzetam, Pirroxil, Psycotron, Stimucortex, and UCB-6215.

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Brief History

Piracetam was synthesized in 1964 by scientists at the Belgian pharmaceutical company UCB led by Dr. Corneliu E. Giurgea, as the first nootropic or cognitive enhancement drug of its type. The term nootropic was coined by Giurgea, and was launched clinically by UCB in the early 1970s.

Piracetam has been sold in Europe for over 40 years, and widely studied on a variety of animals including: goldfish, mice, rats, guinea pigs, rabbits, cats, dogs, marmosets, monkeys and humans. Studies illustrated that, given intravenously to rats at 8gm/kg body weight, there was no resultant toxicity. "Piracetam apparently is virtually non-toxic.

Piracetam is not regulated in the United States (it is neither a controlled substance nor a prescription drug, but instead sold as a dietary supplement.

 

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Popularity

Smart Drugs have continually gained popularity, because of its ability to enhance cognitive functions of the brain.  It is said to enhance memory, attention span, intelligence, etc.  That is the reason it is known as the aforementioned “smart drug”.  Piracetam is believed to increase blood flow between the two hemispheres of the brain and it has also been reported to protect brain tissue from various physical and chemical abrasions such as alcohol damage.

Piracetam has become popular a nootropic drug among students, looking for that extra edge, which may help them to perform better on an overall basis.  They often buy it in bulk as a powder and then consume it with their favorite juice to mask the bitter taste.

Maintaining cognitive ability is very important not only to students, but to all individuals, because as we begin to age, we begin to develop a decline in memory performance—memory learning, and concentration, which can seriously affect our quality of life and even our productivity.  This is not only true of the elderly.  Some younger people have been impacted by some form of cognitive deficit, whether due to an illness or accident.

Benefits

One study described the benefits of piracetam in this way:  “In animal models and in healthy volunteers, piracetam improves the efficiency of the higher telencephalic functions of the brain involved in cognitive processes such as learning and memory. 

The pharmacology of piracetam is unusual because it protects against various physical and chemical insults applied to the brain.  It facilitates learning and memory in healthy animals and in animals whose brain function has been compromised and it enhances interchemispheric transfer of information via callosal transmission.  At the same time, even in relatively high dosages it is devoid of any sedative, analeptic or autonomic activities.”

Research

Several meta-review of literature on piracetam indicate that it increases performance on a variety of cognitive tasks among dyslexic children, and it has shown positive results in the treatment of post –stroke aphasia, epilepsy, cognitive decline following heart and brain surgery, and age-related dementia.

Also, preclinical research suggests that piracetam (a nootropic drug) may improve cognitive functions, but previous studies have failed to demonstrate a clear benefit for the treatment of Alzheimer’s disease (AD).  A one year double-blind, placebo-controlled, parallel-group study with a high dose of piracetam (8 g/d per oz) in 33 ambulant patients with early probable AD was conducted. With Thirty subjects completing the one year study, no improvements occurred in either group.  However, the results support the hypothesis that long-term administration of high doses of piracetam might slow the progression of cognitive deterioration in patients with AD.  The most significant differences concerned the recall of picture series and recent incident and remote memory. The drug was well tolerated.

Another Study was done on elderly drivers, whereas 101 elderly motorists with reduced reaction capacity were examined under real traffic conditions with regard to their driving ability.  They were given a daily dose of 4.8 grams of piracetam or placebo over a six-week period in a randomized double-blind study.   The percentage of correctly solved sign-observance items, which reflects orientation and perception in real traffic conditions, increased in the placebo-treated test-group from 79.86% in the pretest to 80.07% in the retest, whereas the test subjects of the piracetam-treated group improved their performance from 77.08% to 84.16%.  After being treated with piracetam for six weeks, the drivers showed a significantly better performance rate than the placebo-group.  Of particular interest is the finding that the test-subjects who had scored less than 80% in the pretest improved dramatically, without exception in the retest after treatment with piracetam.

Another study was conducted with sixty children with dyslexia (41 boys, 19 girls; ages 9 to 13).  These children were enrolled in a ten week summer tutoring program that emphasized word-building skills.  They were randomly and blindly assigned to receive either placebo or piracetam, a purportedly memory-enhancing drug that has been reported to facilitate reading skill acquisition.  The children were sub-typed as “dysphonetic” or “phonetic” on the basis of scores from tests of phonological sensitivity and phoneme-grapheme correspondence skills.  Of the 53 children who completed the program, 37 were classified as dysphonetic and 16 as phonetic.  The phonetic group improved significantly more in word-recognition ability than the dysphonetic group.  Overall, the children on medication did not improve more than the non-medicated ones in any aspect of reading.  The phonetic sub-group on piracetam gained more in word recognition than any subgroup, but did not improve significantly more than the phonetic subgroup on placebo. 

There was also a study done on Parkinson’s disease, whereas twenty patients inflicted with this disease and marked intellectual impairment or dementia participated in a double-blind placebo controlled trial of the nootropic, piracetam.  A standardized neurological examination, a neuropsychological test battery, and a functional scale, The Sickness Impact Profile, were completed for all patients.  They were then assigned by blind randomization to drug or placebo conditions receiving 3.2 g of piracetam or an identical amount of placebo for 12 weeks.  The dose was increased to 4.8 grams for an additional 12 seeks.  Neurological, psychological and functional measures were rated as improved, unchanged, or worsened in comparison to baseline performance.  Twenty-five percent of the patients did not complete the trial for reasons unrelated to the medication.  Although there was a significant improvement on one subtest of the functional scale, no significant effects were demonstrated in cognitive or neurological measures.

How does it work?

How it works continues to be somewhat of a mystery.  Although its mechanism of action remains unknown to date, its use has precipitated increased blood flow and oxygen levels to areas of the brain. It is thought to facilitate movement of information between the brain's two hemispheres, via the corpus callosum, while improving the function of the neurotransmitter acetylcholine via muscarinic cholinergic (Ach) receptors which are implicated in memory processes.  Furthermore, piracetam may have an effect on NMDA glutamate receptors which are involved with learning and memory processes. 

Also, piracetam is thought to increase cell membrane permeability.  Finally, Piracetam may exert its global effect on brain neurotransmission via modulation of ion channels (i.e. CA2+, K+), which has been found to increase oxygen consumption in the brain.

How piracetam exerts its effects on memory disorders is still under investigation, although among other proposed mechanism of action it is thought to facilitate central nervous system efficiency of cholinergic neurotransmission.    Results from trials involving elderly patients with senile cognitive disorders have been equivocal, as have the results obtained when piracetam has been combined with acetylcholine precursors.

Approval and Usage

Piracetam is primarily used in Europe.  Piracetam is legal to import into the United Kingdom for personal use with or without prescription as with other prescription-only drugs.  As of June, 2006, piracetam is not regulated in the United States (it is neither a controlled substance nor a prescription drug but instead sold as a dietary supplement). As mentioned above, one group in particular, students, have embarked on this drug  as a cognitive enhancement drug , and often buy it in bulk as a powder.  Despite positive anecdotal reports, no study has yet confirmed any cognitive benefit of the drug in normal, unimpaired humans.  It is used by parents as a treatment for childhood autism, though no study has yet produced results which would support such a use.

Piracetam is useful as a long term treatment for clotting, coagulation, and vasospastic disorders such as Raynaud’s phenomenon and deep vein thrombosis.   Piracetam is an extremely safe anti-thrombotic agent which operates through the novel mechanism of inhibiting platelet aggregation and enhancing blood cell deformability.  Because traditional anti-thrombotic drugs operate through the separate mechanism of inhibiting clotting factors, co-administration of piracetam as been shown to highly complement the efficacy and safety of traditional Warfarin/Heparin anti-coagulation therapy.  The most effective treatment range for this use is a daily dose of 4.8 to 9.6 grams divided into three daily doses at 8 hours apart. 

Piracetam is currently being investigated as a complement or alternative to Warfarin as a safe and effective long term treatment for recurring deep vein thrombosis.

 

Dosage

Piracetam is usually supplied in 800 mg tablets or capsules.  The recommended dosage varies based on the indication, usually ranging from 1.6-9.6 grams daily (2-12 pills daily).  Some individuals report faster results when taking 1-2 pills every hour for 4-6 hours or taking 4-8 pills at once for the first few days.

For blood coagulation, clotting, and vasospastic disorders such as Raynaud’s phenomenon or deep vein thrombosis, the most effective treatment range is a daily dose of 4l8 to 96 grams divided into three daily doses at 8 hours apart.

Studies have indicated that individuals have taken up to 45 grams daily without major side effects, while others report that they could feel strong effects at 800 mg on the first day.  On subsequent days at the same dosage the effects were not as noticeable.  Therefore, it is unclear whether maximum benefits are obtained from daily use over time or if occasional use has benefits.  This is something that should be discussed with your doctor.

However, due to the effect of piracetam on platelet aggregation, caution is recommended in patients with underlying disorders of haemostasis, major surgery or severe haemorrhage.
Abrupt discontinuation of treatment should be avoided as this may induce myoclonic or generalized seizures in some myoclonic patients.

As piracetam is almost exclusively excreted by the kidneys caution should be exercised in treating patients with known renal impairment.  In renal impaired and elderly patients, an increase in terminal half-life is directly related to renal function as measured by creatinine clearance.  Dosage adjustment is therefore required in those with mild to moderate renal impairment and elderly patients with diminished renal function.

Contraindications

Piracetam should not be taken by individuals with severe renal impairment, hepatic impairment and those under 16 years of age.

Piracetam has been found to have very few side effects, and those it has are typically “few, mild, and transient.”  Studies have found Piracetam to be very well- tolerated in humans through a wide range of doses.

However, due to the effect of piracetam on platelet aggregation, caution is recommended in patients with underlying disorders of haemostasis, major surgery or severe haemorrhage

Headache may occur from use of piracetam.

Women who are breast feeding or pregnant should not use this drug.  Piracetam may cause stomach upset.  The effects of piracetam are largely subjective.  Some of the effects may be undesirable.

Abrupt discontinuation of treatment should be avoided as this may induce myoclonic or generalized seizures in some myoclonic patients.

Piracetam is said to increase the effects of alcohol and amphetamines.  No other drug interactions have been noted.  It is recommended that alcohol be avoided as one of the reported effects of piracetam is increased flow of blood to the brain which would increase damage and intoxication.

Hopefully, this information will help you make an informed decision before experiencing with the drug piracetam.



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