A synthetic nootropic substance from the racetam family, phenotropil is also known as phenylpiracetam or carphedon. The ability of this group of medications to support and enhance brain health and cognitive performance is well-known. The ability of phenotropil to improve alertness, focus, and cognition in healthy individuals has recently attracted more scientific attention. The purpose of this article is to provide a thorough, scientifically supported analysis of phenotropil’s chemistry, physiological properties, health advantages, ideal dosage, side effects, potential drug interactions, and responsible use as a nootropic supplement.
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Nature of Phenotropil
A phenyl derivative of piracetam‘, the original synthetic nootropic created in the 1960s, is phenotropil. Piracetam is a crucial ingredient of its phenyl group, which gives phenotropil has a lipophilic characteristic that makes it simple to cross the blood-brain barrier and affect the central nervous system. When compared to other racetam nootropics like piracetam, phenotropil has a higher potency due to its improved bioavailability and central nervous system penetration.
Chemistry of Phenotropil
Phenotropil is a derivative of the racetam class of nootropics, specifically piracetam, and is known chemically as (R,S)-2-(2-oxo-4-phenylpyrrolidin-1-yl)acetamide. A pyrrolidinone ring, a 2-oxo group, an acetamide moiety, and a phenyl ring make up its structure. Phenotropil has the chemical formula C12H14N2O2. The parent molecule piracetam’s bioavailability and lipophilicity are improved by the phenyl ring’s addition, leading to greater efficacy and better blood-brain barrier penetration.
Two enantiomers—the R-enantiomer and the S-enantiomer—are produced when chiral centers are present in the pyrrolidinone ring. The racemic combination of phenotropil contains both enantiomers. More research is required to clarify any variations in pharmacokinetic and pharmacodynamic characteristics between the enantiomers.
Physiological Properties of Phenotropil
Phenotropil’s precise physiological properties are not fully understood. Yet, research indicates that a number of variables may be responsible for its cognitive-improving effects, including:
1. Neurotransmitter Modulation: Phenotropil is known to raise the amounts of necessary neurotransmitters in the brain, including dopamine, norepinephrine, and serotonin. These neurotransmitters are essential for controlling mood, drive, focus, and alertness.
2. Improvement of the Cholinergic System: The cholinergic system, which is involved in memory formation and consolidation, is another benefit of phenotropil. It can enhance learning and memory functions by increasing the production of acetylcholine, a crucial neurotransmitter in the cholinergic system.
3. Control of the Glutamatergic System: Phenotropil has the ability to modify this system, which is vital for the transmission of neurons and cognitive function. It might contribute to the cognitive-enhancing effects by balancing the excitatory and inhibitory neurotransmission in the brain.
4. Neuroprotection: Phenotropil demonstrates neuroprotective properties that aid in preventing neuronal damage and advancing brain health. It has been demonstrated to guard against oxidative stress and excitotoxicity brought on by glutamate, both of which can result in the death of neuronal cells.
Health Benefits of Phenotropil
Many cognitive and physical advantages of phenotropil have been reported, including:
1. Improved Cognitive Function: Phenotropil can help with memory, learning, attention, and problem-solving, among other cognitive functions. Research has shown that the supplement can help both young and elderly individuals with memory consolidation and retrieval.
2. Improved Alertness and Focus: Phenotropil is a popular choice for individuals looking to increase their productivity and mental performance due to its stimulant characteristics, which can aid in enhancing alertness and focus.
3. Neuroprotection: As was already noted, phenotropil has neuroprotective properties that can help protect the brain from harm caused by a variety of sources, such as oxidative stress and excitotoxicity.
4. Anxiolytic Effects: Phenotropil can have anxiolytic effects, which can lower feelings of tension and anxiety, according to some research. Its ability to regulate neurotransmitter levels and maintain a balance between excitatory and inhibitory neurotransmission can be the cause of this.
5. Better Physical Performance: Phenotropil has been found to improve physical performance in research on animals and has been linked to a rise in human endurance, stamina, and cold resistance. Its impact on the central nervous system and ability to boost the production of specific neurotransmitters involved in controlling physical performance may be responsible for these effects.
Optimal Dosage of Phenotropil
The ideal phenotropil dosage can change depending on the individual and the desired results. A normal starting dose is one or two divided doses of 100 to 200 mg daily. Some individuals might find it advantageous to up the dosage to 300 or 400 mg daily, but it is important to speak with a healthcare provider before making any changes to the dosage.
Phenotropil should be taken on an empty stomach in order to achieve maximum absorption and effectiveness, as food may reduce its bioavailability. Phenotropil should also be taken earlier in the day because, due to its stimulant properties, taking it later in the day can cause sleep difficulties.
Side Effects of Phenotropil
When taken at recommended dosages, phenotropil is typically well tolerated. However, some individuals can experience negative effects, such as:
1. Headache: Some individuals may develop headaches, which are frequently relieved by taking a choline source supplement, like alpha-GPC or citicoline.
2. Insomnia: Phenotropil, which has stimulant properties, can disrupt sleep if taken too late in the day.
3. Anxiety and Irritability: Phenotropil can occasionally make individuals more agitated and anxious. These negative effects can be lessened by lowering the dosage or stopping use.
4. Digestive Symptoms: Some individuals who take phenotropil can have gastrointestinal discomfort like nausea or diarrhea.
Potential Substance Interactions with Phenotropil
Despite limited reports of substantial interactions between phenotropil and the majority of drugs, the following compounds should be avoided when using phenotropil:
1. Cholinergic Medications: When combined with other cholinergic medications like donepezil, rivastigmine, or galantamine, phenotropil’s impact on the cholinergic system can have additive or synergistic effects. As a result, there may be a higher chance of side effects from excessive acetylcholine release.
2. Stimulants: Owing to the stimulant nature of phenotropil, mixing it with other stimulants, such as amphetamines or caffeine, can result in overstimulation and raise the risk of side effects, which include elevated heart rate, blood pressure, and anxiety.
Best Responsible Use of Phenotropil
The following guidelines should be taken into account by individuals of phenotropil as a nootropic supplement to ensure responsible use:
1. Speak with a Healthcare Expert: Consult a medical expert before beginning phenotropil supplements to go over your unique needs, possible hazards, and the best dosage.
2. Begin with a Low Dose: To reduce the possibility of side effects, start phenotropil at a lower dose and gradually raise it as tolerated.
3. Keep an Eye Out for Negative Reactions and Drug Interactions: When using phenotropil, you might have negative reactions and drug interactions. See a healthcare provider for advice on changing the dosage or stopping phenotropil supplementation if side symptoms arise or if there are worries about potential drug interactions.
4. Keep a Healthy Lifestyle: Phenotropil supplementation need to be seen as an addition to healthy living rather than as a substitute for it. Have a healthy diet, exercise frequently, get enough sleep, and use stress-reduction techniques to enhance cognitive performance.
5. Consider Cycling: To preserve phenotropil supplementation’s effectiveness and reduce potential hazards, you may want to consider cycling its use. For instance, take phenotropil for 4-6 weeks, then pause for two weeks, then take it again. This strategy can help sustain phenotropil’s positive effects while lowering the risk of tolerance or negative side effects.
6. Monitor Your Progress: Maintain a notebook to record how phenotropil affects your memory and general wellbeing. By doing so, you can assess the supplement’s efficacy and make any necessary changes to the dosage or usage patterns.
Phenotropil: Conclusion
Phenylpiracetam, also known as phenotropil, belongs to the racetam family of nootropics. Derived from piracetam, it features an added phenyl group to its structure. Research suggests that phenylpiracetam is more neuroprotective than piracetam and possesses psychostimulatory properties. It can enhance physical performance and attenuate cognitive decline. Typical dosages range from 100 to 250 mg per dose, taken up to three times daily. New users should start at the lower end of the dosage range and adjust as needed. However, it’s essential to note that Phenylpiracetam is not a dietary supplement and hasn’t been extensively studied for long-term human consumption.
References:
- Investigation into stereoselective pharmacological activity of phenotropil. Basic & Clinical Pharmacology & Toxicology. URL: https://onlinelibrary.wiley.com/doi/abs/10.1111/j.1742-7843.2011.00742.x
- Phenotropil as a Nootropic Drug with an Activating Effect on the Integrative Activity of the Brain. URL: https://www.researchgate.net/publication/268706932_Phenotropil_as_a_Nootropic_Drug_with_an_Activating_Effect_on_the_Integrative_Activity_of_the_Brain
- Phenylpiracetam: A scientific review of a potent cognitive-enhancing drug. URL: https://selfhacked.com/blog/phenylpiracetam/
- Phenylpiracetam (Phenotropil) – The Ultimate Guide. URL: https://nootropicszone.com/phenylpiracetam-phenotropil-the-ultimate-guide/
Important Note: The information contained in this article is for general informational purposes only, and should not be construed as health or medical advice, nor is it intended to diagnose, prevent, treat, or cure any disease or health condition. Before embarking on any diet, fitness regimen, or program of nutritional supplementation, it is advisable to consult your healthcare professional in order to determine its safety and probable efficacy in terms of your individual state of health.
Regarding Nutritional Supplements Or Other Non-Prescription Health Products: If any nutritional supplements or other non-prescription health products are mentioned in the foregoing article, any claims or statements made about them have not been evaluated by the U.S. Food and Drug Administration, and such nutritional supplements or other health products are not intended to diagnose, treat, cure, or prevent any disease.
