The substance was first developed in Russia and records show that it was documented in the 1983 but was originally produced in the early 1990s. It was developed as a supplement to boost physical strength and as a nootropic agent. Its production began under the brand name Carphedon in Russia, and it was mainly administered to Russian military personnel and astronauts to boost their work capacity. With time, international athletes used Phenylpiracetam as a doping control to boost endurance and skills. Russian authorities approved the use of Phenylpiracetam as a prescription drug in 2003, for enhancement of physical and cognitive skills in individuals with memory and somatic conditions.
Phenylpiracetam is not as popular as the other racetams and was predominantly used as a prescription drug only in Russia until 2006 when Olga Pyleva, an Olympic athlete was disqualified after testing positive in a drug test. In the recent past, its popularity has been skyrocketing among nootropic users. It is used as an enhancer for cognitive and physical skills pertaining memory and somatic conditions. There are many scientific and clinical studies that have been carried out to evaluate phenylpiracetam. Russian manufacturers suggest that Phenotropil is effective in treating depression, fatigue, epilepsy, and conditions that result from low levels of oxygen in the brain.
A clinical trial was conducted in which 99 patients who had developed encephalopathy due to brain traumas, acute lesions of cerebral blood circulation, and cerebral gliomas. Phenylpiracetam was given in doses of 200mg daily for four weeks. With the use of ACT survey, it was established that when the brain was in a stable state of changes, Phenylpiracetam caused the highest manifested influence on movement disturbances. These influences included higher brain functions, counting, attention, and memory, enhanced motor coordination, and a decrease in the degree of pareses in both limb and face muscles. The study subjects showed an increase in mobility and daily activity, lower anxiety and depression, and lower discomfort. An analysis of EGG indicated more intensive alpha-rhythms and beta-rhythms, a fall in slow waves and paroxysmal activity, and a general tendency towards its normalization.
In a study aimed at testing the stimulating and cognitive improving effects of Phenylpiracetam in rats, passive avoidance and forced swim tests were employed for evaluations. The study results showed that the R enantiomer of Phenylpiracetam boosted the retention latency by about 195% whereas the R and the S enantiomers were observed to lower immobility time (implying an antidepressant effect) when the rats were undergoing the forced swim test. The high dose R enantiomer was noted to be superior to S-enantiomer in reducing mobility.
Phenylpiracetam was observed to have antiepileptic effects in rodents. The metrazol-induced seizure in rats was observed to reduce by 50% after Phenylpiracetam therapy was administered at a dose of 300mg/kg. Metrazol is a drug that acts as a respiratory and circulatory stimulant.
A clinical trial involving 61 patients who were suffering from different forms of epilepsy contrasted Phenylpiracetam combined with AEDs vs. AEDs (anti-epilepsy drugs) alone. When administered together with an additional standard AED (carbamazepine, topiramate, lamotrigine, valproyl amide, barbiturate, or structured polytherapy) in human subjects, it was observed to significantly lower the frequency and number of seizures in individuals receiving AED only. In patients with desynchronous EGG profile, the number dropped from 8 to 3, and the number of patients with seizure remissions rose reasonably. Accordingly, the epileptic patients showed little improvements in cognitive functions when evaluated using the MMSE test. Another study that featured 400 patients who had ischemic stroke indicated that Phenylpiracetam was able to enhance the recovery rate compared to a placebo.
A study focusing on the efficacy of Phenylpiracetam in the treatment of patients with cognitive impairments or depression as a result of brain injuries and encephalopathy established that it had beneficial effects. Phenylpiracetam was noted enhance the quality of life in individuals suffering from encephalopathy as a result of brain tumors (in 33 patients), acute lesions (in 30 patients), and gliomas surgery (in 36 patients. In all the groups under study, the average MMSE scores denoted improvements. MMSE is a standard 30-point questionnaire employed in evaluating cognition. An improvement was observed in anxiety while depression showed a substantial decline. As a result, discomfort levels were lower, and the ability to carry out everyday activities was enhanced. When compared to Piracetam, Phenylpiracetam had better results in the treatment of chronic vascular encephalopathy since it enhanced the cognitive performance in all eight tests whereas Piracetam had positive results in only two test scores.
Phenylpiracetam was also observed to improve scores in depression and asthenia, although in MS patients the changes were relatively lower. A comparative study was conducted that contrasted phenylpiracetam and piracetam in treating chronic fatigue syndrome (CFS) and asthenia. Among the study subjects, 68 patients were treated with Phenylpiracetam, 65 patients with Piracetam, and 47 patients were administered with the placebo. The study used ten-word memory test and attention switching tests. Scores for Phenylpiracetam showed a significant improvement compared to scores for Piracetam, and the placebo. In general, Phenylpiracetam was observed to have a positive response in 83% of asthenic patients and 87% of CFS patients compared to Piracetam's 48% and 55% respectively. In another case, Phenylpiracetam was noted to significantly boost the problem-solving skills in adolescents suffering from asthenia who showed positive effects to the attention and memory tests after the first, second and third efforts from 11%,15%,73%(initial) to 23%,40%,37% (post treatment) respectively. Phenylpiracetam gave higher results when evaluated against 400mg/ day of Piracetam in combination with physiotherapy and multivitamins.
A recent clinical trial focused on the use of Phenylpiracetam in the prevention or delay of ganglia cell death (leads to blindness). Phenotropil was administered to patients who suffered from unstable open-angle glaucoma following the normalization of the eye pressures with laser trabeculoplasty and ocular hypo-tensive therapy. After the therapy, the average incidence of blind spots/ islands of impairment of visual acuity dropped, and glaucoma levels stabilized in 80% of the individuals within a six-month follow-up period. However, this study did not employ a placebo control that makes it hard to verify the effectiveness of Phenylpiracetam since other factors/ variables may have influenced the results.
A comparative study between phenotropil and piracetam was carried out to examine the neuroprotective effects of both in Wistar rats that had low and high sensitivity due to cerebral ischemia. The study also evaluated the effects of these substances on microcirculation within the brain cortex. Phenylpiracetam had a slightly higher efficacy in lowering degree of neuralgic deficiency manifestations, retained the research, locomotor, and memory functions in rodents with gravitational cerebral ischemia helped in the restoration of local cerebral flow when carotid arteries were occluded, and boosted the survival of the animals used in the study.
Another rodent based study tested the effects of Phenylpiracetam on psychoemotional and immune state of Wistar rats that had LPS-induced immune stress. The substance was administered via injections of 25mg/kg for five days. The LPS was administered intraperitoneally at 100μg/kg for three days, and the results indicated phagocytic activities in peripheral blood neutrophils, antibody titer in the reaction of passive hemagglutination, and delayed hypersensitivity type index. Exploratory, locomotor, and orientation activities fell, and anxiety rose in rodents with immune stress. Phenylpiracetam indicated psycho- immunomodulatory effects (increase in exploratory behavior and locomotion, improved immunoreactivity, and prevention of anxiety) under this conditions.