Pramiracetam

Pramiracetam is derived from Racetam, is used to improve cognitive functions, and according to preliminary results helps in the formation of long-term memory. Although the mechanisms of its action is almost completely unknown, apparently Pramiracetam enhances acetylcholine synthesis.

Basic information about Pramiracetam

Pramiracetam (racetam molecule) is synthesized from piracetam and because their modifications has great potential in the fight against amnesia in rats. Compared to other racetam, pramiracetam not as well studied, but behaves relatively well with the people of the reception. In an animal study, such as healthy young and old rats, pramiracetam process was effective in long-term memory formation. These improvements were observed while taking the drug for 1-2 hours prior to testing, and improvements have been observed short-term memory. Tests on humans suggest a similar effect, but due to lack of data on the positive effects of the drug on cognitive abilities in healthy young people, this information does not have adequate statistical significance. Mechanisms of action Pramiracetam still not fully understood, but the drug is able to influence the EEG readings during studies in rats (both young and old) as well as to increase the capture of choline with high affinity. Pramiracetam similar to piracetam and other racetam, since the mechanisms of its action are based on the functioning of the adrenal glands and some external effects, but this is the only explanation pramiracetam mechanisms of action. Other Names: CI-879, diisopropyl-yl- (2-oxopyrrolidin-1-yl) acetamide, CI879.

Not to be confused with piracetam (also Racetam)!
Variety: 

• racetam
• nootropics

Pramiracetam: instructions for use
According to information obtained during the study of the drug in humans, Pramiracetam dosage should be 400 mg three times daily or 600 mg twice daily or 1200mg a day. Should I take pramiracetam with food, it is not clear, nor is it clear whether the optimal dosage of 1200mg, but it brings visible results.

Sources and structure
sources
Pramiracetam (full chemical name - diisopropyl-yl- (2-oxopyrrolidin-1-yl) acetamide and the code name - C-1 879)) is a synthetic molecule racetam and has similarity to the parent molecule, Piracetam is used as a nootropic agent. It was synthesized in 1984 by piracetam modification. Pramiracetam is a structural derivative of piracetam, which was synthesized as an anti-amnesia.

Structure
Pramiracetam is obtained by substitution of the piracetam group amidic group dipropan-2-ylamino-ethyl.
Pharmacology
Serum

Maximum plasma concentration (Cmax) was 2.71 +/- 0,54mkg / ml after administration of 400mg Pramiracetam, 1.34mkg +/- 5.40 / ml (800mg), 6.13 +/- 0.71mkg / ml (1,200mg) and 8.98 +/- 0.71mkg / ml (1,600mg) 3) after receiving 600mg figure was 5,80-6,80mkg / ml. The half-life in dogs is 2,3-3,9 hours, and in humans at a dosage of 400 to 1600mg Pramiracetam this figure is higher - from 4.5 to 6.5 hours, and at 600 mg and of longer - from 2 to 8 hours . Pramiracetam good digested in the human body and has a half-life of a considerable period of time, which depends on the dosage.
Neurology

After oral pramiracetam rats, the drug was detected in the brain, however, was negligible absorption of blood-brain barrier.

Neurology
Mechanics of Action
Effect of the drug (0,15-1,5mm) in the hippocampus had indicators -2.9 / -3.8% of the standard value, which is not significant. Moreover, at 10 microns and the IC50 was observed relationship with dopaminergic, adrenergic, serotonergic, GABAergic, muscarinic and adenosine receptors. In vitro, pramiracetam itself caused no significant effects in the hippocampal cells. Just as when receiving piracetam memory improving effects of reception may be terminated at Pramiracetam adrenektomia, 6) which indicates the importance of the adrenal mechanisms drug exposure. The results of further research revealed that aminoglutethimide (prevents the formation of pregnenolone from cholesterol) and epoximexeron (receptor antagonist of aldosterone) also reduced the effectiveness of the drug. Elevated levels of corticosteroid is generally also blocked the effect of the drug groups racetam. In Pramiracetam effects associated with improved cognitive processes involved metabolism of steroids, in fact aldosterone receptor. It is also noted that pramiracetam able to restore changes in the EEG functions in aged rats as well as young and in the range of 5 to 20 mg and the efficiency exceeding 200-400mg / kg of Piracetam. At the use of piracetam in healthy rats were marked changes in the function of brain waves, and changes in the magnitude of slow waves in the cerebral cortex and hippocampal theta waves contributed to the improvement of cognitive functions by passing water maze of rats. 8) In fact, pramiracetam affect the EEG and young adult rats. The mechanisms underlying these changes, are still unknown.

cholinergic neurotransmission
Intraperitoneal injection of Pramiracetam to the rats (44-88mg / kg) was able to increase high affinity choline levels increase in hippocampal sections of rats for 30 minutes. A similar effect is absent when using piracetam and aniracetam, as well as lower doses (8 mg / kg) or more (176mg / kg) were not effective. Pramiracetam (as do piracetam) normalized changes in the transfer of choline, which were caused by scopolamine. In in vitro tests, the direct application of pramiracetam on hippocampal sections of animals that were not previously used in the experiments did not lead to an increase in high affinity choline increase.

Memory and cognitive functions
The earliest studies of the impact Pramiracetam amnesia revealed that the potential ramiracetam pay amnesia with low efficiency (96% treatment) is shown at 5 mg / kg dose (effective within 12,5-80mg / kg, intraperitoneal injection). This study showed that the potential is greater than that of piracetam, which is the basis of Pramiracetam. In addition it was found that the amnesia caused by anticholinergic toxin hemiholinium-3 suppressed pre Pramicetam reception. With regard to the amnesia Studies in animals, data is not enough, however, we can say that pramiracetam behaves better than piracetam. Pramiracetam differentially affects the research activity, which increases with the dose of 15mg / kg and 60mg suppressed at / kg dose (a dose of 30mg / kg has no effect). In studies kynurenic acid effects pramiracetam was used as a comparative component, and 30 mg / kg of the drug improved the memory (better recognition of objects). Improvements in learning objects were observed at 30 mg / kg Pramiracetam (this dose was more effective than 15 mg / kg and 60 mg / kg) and is comparable to the effects of 400 mg / kg Piracetam. Avoiding collisions with objects in mice were also observed with the dosage Pramiracetam in 100mg / kg adopted for 1-2 hours prior to testing, which is comparable with the effect of oxiracetam (same dose), but superior to piracetam and aniracetam. Improvements were also observed with the passage of the water maze, a single dose was 10mg / kg, and more lower doses were less effective. Intraperitoneal administration of a dose pramiracetam 7,5-15mg / kg in rats for 7 weeks in a radial maze test improved the long-term memory, but has no effect on the short-term memory. And although the 15 mg / kg dose was more effective than the 7.5 mg / kg, there was little difference. It was confirmed influence of the drug on long-term memory, short-term memory but not exposed. Cognitive efficacy in animal studies appears when administered prior to testing. Older people with memory loss for the period of 12 weeks of taking the drug improved memory when recognizing objects, and the result was better than the simple memory training (90 minutes lessons with a teacher during the week). In young healthy people with cerebral injury after taking Pramiracetam (400 mg three times a day) have been observed to improve thought processes and memory that lasted for 18 months. In healthy volunteers, after which the 10-day course Pramiracetam (600 mg twice per day) was given scopolamine was marked decrease of amnesia caused by scopolamine. You can also like Piracetam.

Alzheimer's disease
In the course of a single experiment in the fight against this disease using pramiratsetama (dosage was chosen based on how the patient responded to the drug, from 1200 mg to 4000 mg daily) the drug's effectiveness has not been confirmed.

Interactions with other substances
Lithium
Since pramiracetam can increase the activity of nitric oxide synthase in rat cerebral cortex that occurs when administered intraperitoneally 300 mg / kg (up to 20% above the baseline value) but not 100 mg / kg, of lithium and 100 mg / kg pramiracetam increases the activity of nitric oxide synthase to 40 % of base.