Centrophenoxine: Benefits, Dosage, Side Effects, Drug Interactions, And Other Important Information

The nootropic substance centrophenoxine, also known as meclofenoxate or Lucidril, has recently attracted much attention due to its potential to improve cognitive function, alertness, and focus.  Because it is a cognitive enhancer, centrophenoxine is particularly intriguing to people looking to boost their cognitive function and overall brain health. This article includes in-depth information about centrophenoxine’s chemical makeup, health advantages, recommended dosage, adverse effects, probable drug interactions, and safe use.

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Centrophenoxine: Benefits, Dosage, Side Effects, Drug Interactions, And Other Important Information is an original (NootropicsPlanet) article.

Nature of Centrophenoxine

Dimethylaminoethanol (DMAE) and parachlorphenoxyacetic acid are the main components of the synthetic chemical centrophenoxine (pCPA). DMAE is a naturally occurring substance in the human brain in trace amounts. It shares structural similarities with choline, an essential vitamin for various physiological activities. The family of chlorophenoxyacetic acids, known for their ability to regulate plant growth, includes the synthetic substance known as pCPA.

DMAE and pCPA combine to form a lipophilic molecule that can easily penetrate the blood-brain barrier to exert their nootropic effects more effectively. Centrophenoxine’s main mechanism of action is to boost cholinergic activity, which is essential for memory, learning, and other cognitive processes.

Health Benefits of Centrophenoxine

Many possible health advantages of centrophenoxine have been identified through research, particularly in cognitive improvement and neuroprotection.

1. Cognitive Improvement: Centrophenoxine has been shown to enhance memory, learning, attention, and information processing, among other cognitive functions. Those who have Alzheimer’s disease, other neurological illnesses, or age-related cognitive decline may find these effects to be especially helpful.
2. Neuroprotection: Centrophenoxine may shield neurons from harm brought on by inflammation and oxidative stress. It has been demonstrated to inhibit lipofuscin, an aging-related pigment that may impede cellular function and lipid peroxidation, two major causes of cellular damage and neurodegeneration.
3. Age-related cognitive decline: Centrophenoxine’s ability to reduce age-related cognitive decline has been researched. According to some research, long-term treatment with Centrophenoxine may enhance memory, learning, and attention in senior citizens, possibly postponing or correcting some aging-related cognitive decline.

Chemistry of Centrophenoxine

Dimethylaminoethanol (DMAE) and parachlorphenoxyacetic acid are the main components of the synthetic chemical centrophenoxine (pCPA). The molecular formula C12H17ClNO3 describes the chemical makeup of centrophenoxine.

A choline analog found in nature, dimethylaminoethanol (DMAE) is distinguished by having two methyl groups linked to an aminoethanol group. DMAE is converted to choline in the liver and then absorbed by the brain, serving as an essential choline precursor.

A chlorine atom is present at the para position of the phenyl ring in parachlorphenoxyacetic acid (pCPA), a synthetic halogenated phenoxyacetic acid derivative. The chlorine atom makes the molecule more lipophilic, making it easier for it to penetrate the blood-brain barrier and work its nootropic magic in the brain.

Centrophenoxine is created when DMAE and pCPA combine to form an ester bond.  The esterification process increases centrophenoxine’s lipophilicity, making it more easily able to penetrate the blood-brain barrier and effectively transfer its choline precursor to the brain. Once it reaches the brain, centrophenoxine is hydrolyzed into its component parts, with DMAE being changed into choline and pCPA being broken down and eliminated.

Physiological Mechanism of Action

Centrophenoxine’s physiological mode of action, which involves the modulation of cholinergic activity and its antioxidant and neuroprotective qualities, can be ascribed to the drug’s cognitive-improving effects. The main mechanisms of action are summarized as follows:

1. Cholinergic activity modulation: Centrophenoxine’s main mechanism of action is an increase in cholinergic activity in the brain. Memory development, learning, and attention are only a few of the cognitive activities that depend on cholinergic neurotransmission.
2. Acetylcholine synthesis: As centrophenoxine penetrates the blood-brain barrier, it is degraded into DMAE, which can then be turned into choline, increasing acetylcholine synthesis. The creation of the neurotransmitter acetylcholine uses choline as a precursor. Centrophenoxine can stimulate acetylcholine synthesis by increasing choline availability, which raises acetylcholine levels in the brain. Increased acetylcholine levels can help with memory, learning, and other cognitive processes.
3. Acetylcholinesterase inhibition: Centrophenoxine may also function as a marginally effective acetylcholinesterase inhibitor, thereby preserving acetylcholine levels in the brain and preventing their degradation. By extending acetylcholine’s activity, this inhibition helps to boost the improvement of cognitive function even more.
4. Neuroprotective and antioxidant qualities: Centrophenoxine has antioxidant and neuroprotective qualities in addition to its effects on cholinergic activity, which add to its overall nootropic benefits. Centrophenoxine has been demonstrated to protect neuronal cells against damage brought on by oxidative stress, among other qualities. This neuroprotection is accomplished by scavenging reactive oxygen species, which can lead to oxidative damage to cellular components and decreasing lipid peroxidation, a primary source of cellular damage and dementia.
5. Lipofuscin clearance: Centrophenoxine encourages the removal of lipofuscin, a pigment that builds up in aging cells and is linked to a loss in cognitive function with advancing age. By lowering lipofuscin buildup, centrophenoxine may support cellular function maintenance and avert age-related cognitive decline.

Optimal Dosage of Centrophenoxine

The ideal dosage must be determined to maximize centrophenoxine’s nootropic effects while lowering the risk of adverse effects. Centrophenoxine dosage recommendations change depending on a person’s age, sex, and response. Most investigations on the usage of centrophenoxine supplements have employed daily dosages of 250 to 1,000 mg, split into two or three doses.

To each patient’s tolerance and response, it is best to start with a smaller dosage (250 mg per day) and then gradually raise it as necessary. Some people may need greater dosages to attain the intended cognitive-enhancing effects, whereas others might be more sensitive to the substance and only need lower amounts.

Side Effects of Centrophenoxine

Little side effects have been documented with centrophenoxine, which is often well tolerated. However, particularly at higher dosages, some people may develop moderate gastrointestinal problems, such as nausea, vomiting, diarrhea, and stomach pain. Lowering the dosage or taking the supplement with food will often lessen these unwanted effects.

Extreme centrophenoxine use has occasionally been linked to sleeplessness, restlessness, and overstimulation, especially when combined with other stimulants or taken at high levels. It is crucial to keep an eye out for any possible adverse effects and to change the dosage or stop using the medication as needed.

Potential Substance Interactions with Centrophenoxine

As with any dietary supplement, it is critical to be aware of any potential interactions between centrophenoxine and other medications. Among the probable interactions are:

1. Acetylcholine is a neurotransmitter blocked by anticholinergic medicines, which may lessen Centrophenoxine’s ability to improve cognition. Antihistamines, tricyclic antidepressants, and antipsychotic drugs are a few examples.
2. Acetylcholinesterase inhibitors: These drugs prevent the breakdown of acetylcholine, and they are used to treat Alzheimer’s disease and other neurological diseases. However, using acetylcholinesterase inhibitors and centrophenoxine together may result in high acetylcholine levels and raise the possibility of negative effects.
3. Drugs that boost acetylcholine activity, such as cholinergic, may combine with centrophenoxine to produce additive or synergistic effects. Nicotine, donepezil, and rivastigmine are other examples.

Best Responsible Uses of Centrophenoxine

When using centrophenoxine as a nootropic supplement, take into account the following advice to achieve the best and safest results:

1. Speak with a healthcare physician before beginning any new supplement. This consultation is essential if you have any pre-existing medical conditions, are taking any drugs, are pregnant, or are nursing.
2. Begin with a modest dosage and gradually raise it as necessary, considering each person’s tolerance and response.
3. Watch for adverse effects: If any emerge, change the dosage or stop using the product as appropriate.
4. Integrate with a healthy lifestyle: To get the most out of Centrophenoxine, combine it with a healthy lifestyle that includes a balanced diet, frequent exercise, and enough sleep.

Centrophenoxine:

Conclusion

Centrophenoxine, a nootropic compound, presents several potential health benefits, particularly in cognitive enhancement and neuroprotection. It offers a multifaceted approach to supporting cognitive health, protecting against neurodegeneration, and potentially enhancing mental well-being. While centrophenoxine shows significant promise, it is essential to approach its use cautiously. To avoid potential side effects and interactions, consulting with a healthcare professional before starting supplementation is advisable, particularly for individuals with pre-existing health conditions or those taking other medications. Centrophenoxine’s diverse benefits make it a valuable addition to the regimen of those looking to maintain or improve their brain function and overall neurological health.

References:

1. Effects of centrophenoxine on body composition and some biochemical parameters of demented elderly people as revealed in a double-blind clinical trial. Link: https://www.sciencedirect.com/science/article/abs/pii/0167494390900252
2. The unapproved drug centrophenoxine (meclofenoxate) in cognitive enhancement dietary supplements. Link: https://pubmed.ncbi.nlm.nih.gov/35959800/
3. Effects of centrophenoxine on lipofuscin in the retinal pigment epithelium of old mice. Link: https://pubmed.ncbi.nlm.nih.gov/6410295/
4. Potentiation of antitumor drug action by centrophenoxine: specificity. Link: https://pubmed.ncbi.nlm.nih.gov/323465/

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.